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Sample records for active constituents responsible

  1. Constituents of response rates

    PubMed Central

    Pear, Joseph J.; Rector, Brian L.

    1979-01-01

    Response rate and the proportion of time pigeons allocated to a key-pecking activity were measured on several basic types of reinforcement schedules. Reinforcement frequency was varied within each type of basic schedule, and the effects on two constituents of response rate were noted. Propensity, the proportion of time the birds spent on a platform in front of the key, showed very consistent effects as reinforcement frequency varied: in general, it decreased when reinforcement frequency markedly decreased and it increased when reinforcement frequency increased. Speed, key pecks per unit of time spent on the platform, showed inconsistent effects when reinforcement frequency varied. Consequently, response rate showed less consistent effects than did propensity. Cumulative response records demonstrated the existence of several different types of transitions or boundary states between the key-pecking activity and other activities. The types of transitions that occurred between activities depended on both the type of reinforcement schedule and the frequency of reinforcement. The propensity data support the position that general laws of behavior can be based on temporal measures of behavior. The speed data suggest that, if a complete assessment of the dynamic properties of behavior is to be achieved, measures of behavior must incorporate the structural variations in the operant unit. PMID:16812155

  2. Recombinant cannabinoid type 2 receptor in liposome model activates g protein in response to anionic lipid constituents.

    PubMed

    Kimura, Tomohiro; Yeliseev, Alexei A; Vukoti, Krishna; Rhodes, Steven D; Cheng, Kejun; Rice, Kenner C; Gawrisch, Klaus

    2012-02-03

    Human cannabinoid type 2 (CB(2)) receptor expressed in Escherichia coli was purified and successfully reconstituted in the functional form into lipid bilayers composed of POPC, 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine, 1-palmitoyl-2-oleoyl-sn-glycero-3-phospho-L-serine (POPS), and cholesteryl hemisuccinate (CHS). Reconstitution was performed by detergent removal from the protein/lipid/detergent mixed micelles either on an adsorbent column, or by rapid dilution to below the critical micelle concentration of detergent followed by removal of detergent monomers on a concentrator. Proteoliposomes prepared at a protein/phospholipid/CHS molar ratio of 1/620-650/210-220 are free of detergent as shown by (1)H NMR, have a homogeneous protein/lipid ratio shown by isopycnic gradient ultracentrifugation, and are small in size with a mean diameter of 150-200 nm as measured by dynamic light scattering. Functional integrity of the reconstituted receptor was confirmed by quantitative binding of (2)H-labeled agonist CP-55,940-d(6) measured by (2)H magic angle spinning NMR, as well as by activation of G protein. The efficiency of G protein activation by agonist-bound CB(2) receptor was affected by negative electric surface potentials of proteoliposomes controlled by the content of anionic CHS or POPS. The activation was highest at an anionic lipid content of about 50 mol %. There was no correlation between the efficiency of G protein activation and an increase of hydrocarbon chain order induced by CHS or cholesterol. The results suggest the importance of anionic lipids in regulating signal transduction by CB(2) receptor and other class A GPCR. The successful reconstitution of milligram quantities of pure, functional CB(2) receptor enables a wide variety of structural studies.

  3. Evidence for contributions of interactions of constituents to the anti-inflammatory activity of Hypericum perforatum.

    PubMed

    Hammer, Kimberly D P; Birt, Diane F

    2014-01-01

    Hypericum perforatum (Hp) extracts contain many different classes of constituents including flavonoids and biflavonoids, phloroglucinols, naphthodianthrones, caffeic acid derivatives, and unknown and/or unidentified compounds. Many constituents may be responsible for the anti-inflammatory activity of Hp including quercetin and derivatives, hyperforin, pseudohypericin, and amentoflavone. In line with antidepressant data, it appears that the interactions of constituents may be important for the anti-inflammatory activity of Hp. Interactions of constituents, tested in bioavailability models, may explain why synergistic mechanisms have been found to be important for antidepressant and antiproliferative bioactivities. This review highlights the relationship among individual constituents and the anti-inflammatory activity of Hp extracts and proposes that interactions of constituents may be important for the anti-inflammatory activity of botanical extracts, although the exact mechanisms of the interactions are still unclear.

  4. Effects of Saffron (Crocus sativus L.) Stigma Extract and its Active Constituent Crocin on Neuropathic Pain Responses in a Rat Model of Chronic Constriction Injury.

    PubMed

    Safakhah, Hossein Ali; Taghavi, Tahereh; Rashidy-Pour, Ali; Vafaei, Abbas Ali; Sokhanvar, Mina; Mohebbi, Narges; Rezaei-Tavirani, Mostafa

    2016-01-01

    This study was designed to investigate the therapeutic effects of saffron (Crocus sativus L.) and its main constituent crocin on neuropathic pain behavioral responses induced by chronic constriction injury (CCI) in rats. Adult male Wistar rats (200 to 250 g) were randomly assigned into 5 groups: Sham + saline, CCI + saline, CCI+ saffron (30 mg/kg), CCI + crocin (15 mg/kg) and CCI + crocin (30 mg/kg). CCI was induced by applying 4 loose ligatures around the sciatic nerve. Two weeks after nerve lesion, injections of saline, saffron or crocin were started and continued until 26(th) day post-surgery. Pain behavioral responses including mechanical allodynia (von Frey filament testing) and thermal hyperalgesia were measured in 14, 17, 20, 23, 26, and 40(th) days after CCI. CCI significantly increased pain behavioral responses. Saffron and crocin (30 mg/kg) decreased thermal hyperalgesia and mechanical allodynia on day 26, and this effect continued until the day 40. Crocin at lower dose (15 mg/kg) was ineffective. These findings indicate that treatment of saffron and crocin after CCI may have a therapeutic effect against neuropathic pain, suggesting that these substances may offer new strategies for the treatment of this highly debilitating condition.

  5. Effects of Saffron (Crocus sativus L.) Stigma Extract and its Active Constituent Crocin on Neuropathic Pain Responses in a Rat Model of Chronic Constriction Injury

    PubMed Central

    Safakhah, Hossein Ali; Taghavi, Tahereh; Rashidy-Pour, Ali; Vafaei, Abbas Ali; Sokhanvar, Mina; Mohebbi, Narges; Rezaei-Tavirani, Mostafa

    2016-01-01

    This study was designed to investigate the therapeutic effects of saffron (Crocus sativus L.) and its main constituent crocin on neuropathic pain behavioral responses induced by chronic constriction injury (CCI) in rats. Adult male Wistar rats (200 to 250 g) were randomly assigned into 5 groups: Sham + saline, CCI + saline, CCI+ saffron (30 mg/kg), CCI + crocin (15 mg/kg) and CCI + crocin (30 mg/kg). CCI was induced by applying 4 loose ligatures around the sciatic nerve. Two weeks after nerve lesion, injections of saline, saffron or crocin were started and continued until 26th day post-surgery. Pain behavioral responses including mechanical allodynia (von Frey filament testing) and thermal hyperalgesia were measured in 14, 17, 20, 23, 26, and 40th days after CCI. CCI significantly increased pain behavioral responses. Saffron and crocin (30 mg/kg) decreased thermal hyperalgesia and mechanical allodynia on day 26, and this effect continued until the day 40. Crocin at lower dose (15 mg/kg) was ineffective. These findings indicate that treatment of saffron and crocin after CCI may have a therapeutic effect against neuropathic pain, suggesting that these substances may offer new strategies for the treatment of this highly debilitating condition. PMID:27610166

  6. Electrorheology of suspensions containing interfacially active constituents.

    PubMed

    McIntyre, Carl; Yang, Hengxi; Green, Peter F

    2013-09-25

    We recently showed that a suspension of micrometer-sized polystyrene (PS) particles in a PDMS liquid, mixed with small (1 wt %) amounts of a nanocage, sulfonated polyhedral oligomeric silsesquioxane (s-POSS), exhibited significant electrorheological (ER) behavior. This behavior was associated with the formation of a thin adsorbed layer of s-POSS onto the surfaces of PS and the subsequent formation of polarization-induced aggregates, or structures, responsible for the ER effect in an applied electric, E, field. Current theory suggests that the ER effect would largely be determined by the dielectric and conductive properties of the conductive layer of core/shell particles in ER suspensions. We show here that sulfonated-PS (s-PS)/PDMS suspensions exhibit further increases in the yield stress of over 200%, with the addition of s-POSS. The yield stress of this system, moreover, scales as τy [proportionality] E(2). The dielectric relaxation studies reveal the existence of a new relaxation peak in the s-POSS/s-PS/PDMS system that is absent in the s-POSS/PS/PDMS suspension. The relative sizes of these peaks are sensitive to the concentration of s-POSS and are associated with changes in the ER behavior. The properties of this class of ER fluids are not appropriately rationalized in terms of current theories.

  7. Tetrapleura tetraptera: molluscicidal activity and chemical constituents.

    PubMed

    Aladesanmi, Adetunji J

    2006-08-28

    Tetrapleura tetraptera (Schumach. And Thonn) Taub, Mimosaceae, commonly known as Aridan (fruit), A single stemmed, robust, perennial tree of about 30 m. It has a grey/brown, smooth/rough bark with glabrous yound branchlets. The flower is yellow/pink and racemes white the fruit has dark brown, four winged pods 12-25 x 3.5-6.5 cm. It is generally found in the lowland forest of tropical Africa. The fruit consists of a fleshy pulp with small, brownish-black seeds. The fruit possesses a fragrant, characteristically pungent aromatic odour, which is attributed to its insect repellent property. It is used as spices and aroma (exotic tropical scents) and fish poisoning. It is one of the molluscicidal medicinal plants of Nigeria, also useful in the management of convulsions, leprosy, inflammation and/or rheumatoid pains. The documented biological and-or pharmacological activities are found to be molluscicidal, cardio-vascular, neuromuscular, hypotensive, anti-convulsant, trypanocidal, hirudinicidal, schistosomiasis control, anti-ulcerative, ectoxicity, anti-inflammatory, hypoglycaemic, anti-microbial, emulsifying property, birth control, food value and the control of intestinal parasites. Activity-guided fractionation of the methanol extract of the fruits of T. tetraptera led to the isolation of a saponin glycoside with an oleanolic acid aglycone, a monodesmosidic diglycoside of the rare sapogenin 27-hydroxyolean-12 (13)-en-28-oic acid; echinocystic acid-3-0-sodium sulfate from the stembark, umbelliferone and ferulic acid from the leaves and branches respectively. Also isolated from the fruits were aridanin and three of its olean-12-en-28-oic acid derivatives. All the compounds isolated either from the fruits or other parts were found to exhibit strong molluscicidal properties against the schistosomiasis-transmitting snails Biomphalaria glabrata.

  8. Constituents of chyme responsible for postprandial intestinal hyperemia.

    PubMed

    Chou, C C; Kvietys, P; Post, J; Sit, S P

    1978-12-01

    While local venous outflow was measured in anesthetized dogs, various constituents of intestinal chyme were placed in the jejunal lumen to identify those responsible for postprandial intestinal hyperemia. Digested food and its supernatant increased local blood flow, whereas its precipitate, undigested food, and pancreatic enzymes did not. In the jejunum bile alone had no effect, but it markedly enhanced the hyperemic effect of digested food. Bile in the ileal lumen, however, increased local blood flow. At physiological postprandial concentrations in the jejunum, glucose, and micellar solutions of oleic acid and monoolein increased flow, but taurocholate and 16 common dietary amino acids did not. The hyperemic effect of lipids required the presence of taurocholate. Of the 16 amino acids, only Glu and Asp increased flow at 10 times the physiological concentrations (28 and 20 mM, respectively). The study indicates that the constituents of chyme responsible for postprandial intestinal hyperemia are the hydrolytic products of food, especially those of carbohydrates and fats and that bile plays an important role in the hyperemia.

  9. SUMO Ligase Protein Inhibitor of Activated STAT1 (PIAS1) Is a Constituent Promyelocytic Leukemia Nuclear Body Protein That Contributes to the Intrinsic Antiviral Immune Response to Herpes Simplex Virus 1

    PubMed Central

    Brown, James R.; Conn, Kristen L.; Wasson, Peter; Charman, Matthew; Tong, Lily; Grant, Kyle; McFarlane, Steven

    2016-01-01

    ABSTRACT Aspects of intrinsic antiviral immunity are mediated by promyelocytic leukemia nuclear body (PML-NB) constituent proteins. During herpesvirus infection, these antiviral proteins are independently recruited to nuclear domains that contain infecting viral genomes to cooperatively promote viral genome silencing. Central to the execution of this particular antiviral response is the small ubiquitin-like modifier (SUMO) signaling pathway. However, the participating SUMOylation enzymes are not fully characterized. We identify the SUMO ligase protein inhibitor of activated STAT1 (PIAS1) as a constituent PML-NB protein. We show that PIAS1 localizes at PML-NBs in a SUMO interaction motif (SIM)-dependent manner that requires SUMOylated or SUMOylation-competent PML. Following infection with herpes simplex virus 1 (HSV-1), PIAS1 is recruited to nuclear sites associated with viral genome entry in a SIM-dependent manner, consistent with the SIM-dependent recruitment mechanisms of other well-characterized PML-NB proteins. In contrast to that of Daxx and Sp100, however, the recruitment of PIAS1 is enhanced by PML. PIAS1 promotes the stable accumulation of SUMO1 at nuclear sites associated with HSV-1 genome entry, whereas the accumulation of other evaluated PML-NB proteins occurs independently of PIAS1. We show that PIAS1 cooperatively contributes to HSV-1 restriction through mechanisms that are additive to those of PML and cooperative with those of PIAS4. The antiviral mechanisms of PIAS1 are counteracted by ICP0, the HSV-1 SUMO-targeted ubiquitin ligase, which disrupts the recruitment of PIAS1 to nuclear domains that contain infecting HSV-1 genomes through mechanisms that do not directly result in PIAS1 degradation. IMPORTANCE Adaptive, innate, and intrinsic immunity cooperatively and efficiently restrict the propagation of viral pathogens. Intrinsic immunity mediated by constitutively expressed cellular proteins represents the first line of intracellular defense against

  10. Possible relationships between solar activity and atmospheric constituents

    NASA Technical Reports Server (NTRS)

    Roosen, R. G.; Angione, R. J.

    1975-01-01

    The large body of data on solar variations and atmospheric constituents collected between 1902 and 1953 by the Astrophysical Observatory of the Smithsonian Institution (APO) was examined. Short-term variations in amounts of atmospheric aerosols and water vapor due to seasonal changes, volcanic activity, air pollution, and frontal activity are discussed. Preliminary evidence indicates that increased solar activity is at times associated with a decrease in attenuation due to airborne particulates.

  11. Nigella sativa and its active constituent thymoquinone in oral health

    PubMed Central

    AlAttas, Safia A.; Zahran, Fat’heya M.; Turkistany, Shereen A.

    2016-01-01

    In this review, we summarized published reports that investigated the role of Nigella sativa (NS) and its active constituent, thymoquinone (TQ) in oral health and disease management. The literature studies were preliminary and scanty, but the results revealed that black seed plants have a potential therapeutic effect for oral and dental diseases. Such results are encouraging for the incorporation of these plants in dental therapeutics and hygiene products. However, further detailed preclinical and clinical studies at the cellular and molecular levels are required to investigate the mechanisms of action of NS and its constituents, particularly TQ. PMID:26905343

  12. Yucca schidigera bark: phenolic constituents and antioxidant activity.

    PubMed

    Piacente, Sonia; Montoro, Paola; Oleszek, Wieslaw; Pizza, Cosimo

    2004-05-01

    Two new phenolic constituents with unusual spirostructures, named yuccaols D (1) and E (2), were isolated from the MeOH extract of Yucca schidigera bark. Their structures were established by spectroscopic (ESIMS and NMR) analysis. The new yuccaols D and E, along with resveratrol (3), trans-3,3',5,5'-tetrahydroxy-4'-methoxystilbene (4), yuccaols A-C (5-7), yuccaone A (8), larixinol (9), the MeOH extract of Yucca schidigera bark, and the phenolic portion of this extract, were assayed for antioxidant activity by measuring the free radical scavenging effects using two different assays, namely, the Trolox Equivalent Antioxidant Capacity (TEAC) assay and the coupled oxidation of beta-carotene and linoleic acid (autoxidation assay). The significant activities exhibited by the phenolic fraction and its constituents in both tests show the potential use of Y. schidigera as a source of antioxidant principles.

  13. Interaction of digoxin with activated dimethicone and other antacid constituents.

    PubMed

    McElnay, J C; Harron, D W; D'Arcy, P F; Eagle, M R

    1979-01-15

    A study was made of the effect of activated dimethicone on the absorption of digoxin in relation to other commonly used antacid constituents using an in vitro experimental model. Dimethicone was found not to affect the absorption of digoxin in relation to aluminium hydroxide, bismuth carbonate, light magnesium carbonate and magnesium trisilicate whose effects on the absorption of digoxin were in agreement with values reported in the literature.

  14. Thymus mastichina: chemical constituents and their anti-cancer activity.

    PubMed

    Gordo, Joana; Máximo, Patrícia; Cabrita, Eurico; Lourenço, Ana; Oliva, Abel; Almeida, Joana; Filipe, Mariana; Cruz, Pedro; Barcia, Rita; Santos, Miguel; Cruz, Helder

    2012-11-01

    The cytotoxicity-guided study of the dichloromethane and ethanol extracts of Thymus mastichina L. using the HCT colon cancer cell line allowed the identification of nine compounds, sakuranetin (1), sterubin (2), oleanolic acid (3), ursolic acid (4), lutein (5), beta-sitosterol (6), rosmarinic acid (7), 6-hydroxyluteolin-7-O-beta-glucopyranoside (8), and 6-hydroxyapigenin-7-O-beta-glucopyranoside (9). All compounds were tested for their cytotoxicity against the HCT colon cancer cell line. Compound 4 showed cytotoxicity with GI50 value of 6.8 microg/mL. A fraction composed of a mixture (1:1) of triterpenoid acids 3 and 4 displayed improved cytotoxicity with a GI50 of 2.8 microg/mL suggesting a synergistic behavior. This is the first report on the chemical constituents of Thymus mastichina L. based on structural assignments by spectroscopic analysis. The presence of these constituents identified by colon cancer cytotoxicity-guided activity indicates that extracts of T. mastichina L. may have a protective effect against colon cancers.

  15. Constituents of Quinchamalium majus with potential antitubercular activity.

    PubMed

    Gua, Jian-Qiao; Wang, Yuehong; Franzblau, Scott G; Montenegro, Gloria; Timmermann, Barbara N

    2004-01-01

    Antitubercular bioassay-guided fractionation of the dichloromethane extracts of the above-ground biomass and roots of Quinchamalium majus led to the identification of six known constituents, betulinic acid (1), daucosterol (2), 5,7-dihydroxyflavone (3), oleanolic acid (4), (-)-2S-pinocembrin (5), and ursolic acid (6), for the first time in this species. Their chemical structures were determined on the basis of spectroscopic evidence and chemical transformation methods. All of these compounds along with additional 11 analogues were evaluated for their antitubercular potential against Mycobacterium tuberculosis in a microplate alamar blue assay, and the primary structure-activity relationships (SARs) for 4 and 6 were discussed. In addition, all the isolates were tested for cytotoxicity against African green monkey Vero cells in order to evaluate for their selectivity potential.

  16. Modulatory Mechanism of Nociceptive Neuronal Activity by Dietary Constituent Resveratrol

    PubMed Central

    Takeda, Mamoru; Takehana, Shiori; Sekiguchi, Kenta; Kubota, Yoshiko; Shimazu, Yoshihito

    2016-01-01

    Changes to somatic sensory pathways caused by peripheral tissue, inflammation or injury can result in behavioral hypersensitivity and pathological pain, such as hyperalgesia. Resveratrol, a plant polyphenol found in red wine and various food products, is known to have several beneficial biological actions. Recent reports indicate that resveratrol can modulate neuronal excitability, including nociceptive sensory transmission. As such, it is possible that this dietary constituent could be a complementary alternative medicine (CAM) candidate, specifically a therapeutic agent. The focus of this review is on the mechanisms underlying the modulatory effects of resveratrol on nociceptive neuronal activity associated with pain relief. In addition, we discuss the contribution of resveratrol to the relief of nociceptive and/or pathological pain and its potential role as a functional food and a CAM. PMID:27727178

  17. Antineuroinflammatory and Antiproliferative Activities of Constituents from Tilia amurensis.

    PubMed

    Kim, Ki Hyun; Moon, Eunjung; Cha, Joon Min; Lee, Seulah; Yu, Jae Sik; Kim, Chung Sub; Kim, Sun Yeou; Choi, Sang Un; Lee, Kang Ro

    2015-01-01

    As part of our ongoing search for bioactive constituents of natural Korean medicinal resources, we found in a preliminary study that the methanol (MeOH) extract from the trunks of Tilia amurensis RUPR. showed an inhibitory effect on nitric oxide (NO) production in an activated murine microglial cell line. A bioassay-guided fractionation and chemical investigation of the MeOH extract resulted in the isolation and identification of a new isoflavonoid glycoside, orobol 4'-O-β-D-apiofuranosyl-(1→6)-β-D-glucopyranoside (1) and 16 known compounds (2-17). The structure of the new compound was determined by spectroscopic methods, i.e., one-dimensional (1D) and two-dimensional (2D)-NMR techniques and high resolution (HR)-MS, and chemical methods. The antineuroinflammatory activities of the isolated compounds were determined by measuring NO levels in the medium using murine microglial BV-2 cells. Among them, 12 compounds, including compound 1 (most active with an IC50 value of 23.42 µM), inhibited NO production in lipopolysaccharide-stimulated BV-2 cells. Moreover, compounds 1-4 showed moderate antiproliferative activities against the SK-MEL-2 cell line, with IC50 values ranging from 12.31 to 19.67 µM.

  18. Chemical constituents and biological activities of two Iranian Cystoseira species.

    PubMed

    Yegdaneh, Afsaneh; Ghannadi, Alireza; Dayani, Ladan

    2016-07-01

    The marine environment represents approximately half of the global biodiversity and could provide unlimited biological resources for the production of therapeutic drugs. Marine seaweeds comprise few thousands of species representing a considerable part of the littoral biomass. Extracts of the Cystoseira indica and Cystoseira merica were subjected to phytochemical and cytotoxicity evaluation. The amount of total phenol was determined with Folin-Ciocalteu reagent. Cytotoxicity was characterized by IC50 of human cancer cell lines including MCF-7 (human breast adenocarcinoma), HeLa (cervical carcinoma), and HT-29 (human colon adenocarcinoma) using Sulforhodamin assay. Antioxidant activities were evaluated using 2,2-diphenylpicrylhydrazyl (DPPH) method. The analysis revealed that tannins, saponins, sterols and triterpenes were the most abundant constituents in these Cystoseira species while cyanogenic and cardiac glycosides were the least ones. C. indica had the higher content of total phenolics and also showed higher antioxidant activity. Cytotoxic results showed that both species inhibited cell growth effectively, especially against MCF-7 cell line. The present findings suggest potential pharmacological applications of selected seaweeds but require further investigation and identification of their bioactive principles.

  19. Chemical constituents and biological activities of two Iranian Cystoseira species

    PubMed Central

    Yegdaneh, Afsaneh; Ghannadi, Alireza; Dayani, Ladan

    2016-01-01

    The marine environment represents approximately half of the global biodiversity and could provide unlimited biological resources for the production of therapeutic drugs. Marine seaweeds comprise few thousands of species representing a considerable part of the littoral biomass. Extracts of the Cystoseira indica and Cystoseira merica were subjected to phytochemical and cytotoxicity evaluation. The amount of total phenol was determined with Folin-Ciocalteu reagent. Cytotoxicity was characterized by IC50 of human cancer cell lines including MCF-7 (human breast adenocarcinoma), HeLa (cervical carcinoma), and HT-29 (human colon adenocarcinoma) using Sulforhodamin assay. Antioxidant activities were evaluated using 2,2-diphenylpicrylhydrazyl (DPPH) method. The analysis revealed that tannins, saponins, sterols and triterpenes were the most abundant constituents in these Cystoseira species while cyanogenic and cardiac glycosides were the least ones. C. indica had the higher content of total phenolics and also showed higher antioxidant activity. Cytotoxic results showed that both species inhibited cell growth effectively, especially against MCF-7 cell line. The present findings suggest potential pharmacological applications of selected seaweeds but require further investigation and identification of their bioactive principles. PMID:27651811

  20. Acaricidal activity of active constituent isolated in Chamaecyparis obtusa leaves against Dermatophagoides spp.

    PubMed

    Jang, Young-Su; Lee, Chi-Hoon; Kim, Moo-Key; Kim, Jeong-Hak; Lee, Sang-Hyun; Lee, Hoi-Seon

    2005-03-23

    Acaricidal activities of materials derived from Chamaecyparis obtusa leaves against Dermatophagoides farinae and Dermatophagoides pteronyssinus were examined using the dry film method and compared with that of commercial benzyl benzoate and N,N-diethyl-m-toluamide (DEET). The active constituent of the C. obtusa leaves was identified as beta-thujaplicin (C10H12(O2)) by spectroscopic analyses. Responses varied with dose. On the basis of a 24 h LC50 value, acaricidal activity against D. farinaewas more pronounced with beta-thujaplicin (72.2 mg/m2) than benzyl benzoate (89.9 mg/m2) and DEET (377 mg/m2). Acaricidal activity against D. pteronyssinus was more pronounced in beta-thujaplicin (62.1 mg/m2) than benzyl benzoate (72.4 mg/m2) and DEET (193 mg/m2). These results indicate that acaricidal activity of C. obtusa leaves likely results from by beta-thujaplicin. Beta-thujaplicin merits further study as potential house dust mite control agents or lead compounds.

  1. Antifungal activity of Glycyrrhiza glabra extracts and its active constituent glabridin.

    PubMed

    Fatima, Atiya; Gupta, Vivek K; Luqman, Suaib; Negi, Arvind S; Kumar, J K; Shanker, Karuna; Saikia, Dharmendra; Srivastava, Suchita; Darokar, M P; Khanuja, Suman P S

    2009-08-01

    Glabridin, an active constituent of Glycyrrhiza glabra roots, was found to be active against both yeast and filamentous fungi. Glabridin also showed resistance modifying activity against drug resistant mutants of Candida albicans at a minimum inhibitory concentration of 31.25-250 microg/mL. Although the compound was reported earlier to be active against Candida albicans, but this is the first report of its activity against drug resistant mutants.

  2. Stratospheric constituent response to vertically propagating equatorial waves

    NASA Astrophysics Data System (ADS)

    Salby, Murry L.

    1988-02-01

    Planetary-scale equatorial waves play an important role in the dynamics of the tropical atmosphere. They are believed to be excited in unsteady convective heating in the tropical troposphere. From convective centers in the intertropical convergence zone (ITCZ), equatorial waves propagate vertically into the upper atmosphere where they are eventually absorbed, e.g., through radiative dissipation. A spectrum of vertically propagating Kelvin waves was revealed to be trapped about the equator, radiating vertically out of the tropical troposphere. Two other Kelvin waves were found with phase velocities 2 and 4 times as fast. The ultrafast Kelvin waves move at nearly 120 m/s and are seen to propagate to the highest altitude observed by Nimbus-7 LIMS. Each class has the form of a Kelvin wave, a Gaussian centered on the equator and propagating vertically, and all satisfy the dispersion relationship for equatorial Kelvin waves. These vertically propagating Kelvin waves account for a substantial fraction of the temperature variability in the tropical stratosphere. In combination, they lead to temperature fluctuations in excess of 5K in the upper stratosphere and mesosphere. Because several chemical constituents are photochemically controlled in this region, vertically propagating Kelvin waves are expected to lead to variations in the abundances of such species.

  3. Identification of the effective constituents for anti-inflammatory activity of Ju-Zhi-Jiang-Tang, an ancient traditional Chinese medicine formula.

    PubMed

    Wang, Shufang; Chen, Pinghong; Jiang, Wei; Wu, Leihong; Chen, Lulin; Fan, Xiaohui; Wang, Yi; Cheng, Yiyu

    2014-06-27

    The anti-inflammatory constituents of Ju-Zhi-Jiang-Tang (JZJT), a formula used for thousands of years in China, were identified by LC-MS and pharmacological activity evaluation. In this study, the whole extract of formula was separated into multiple components to facilitate the analytical process. To characterize their contributions to pharmacological activity of formula, activity indexes of constituents were proposed and calculated for the first time, which integrated the chemical and pharmacological information of multiple components. Among the 151 constituents detected in JZJT by LC-Q-TOF-MS and LC-IT-MS, a total number of 108 constituents were identified unambiguously or tentatively, including eighteen potential novel compounds. And, the structures of some constituents were confirmed by NMR. According to their activity indexes, polymethoxy flavones were indicated as the major active constituents responsible for the anti-inflammatory activity of JZJT. To verify the feasibility of activity indexes in predicting the active constituents, nine compounds with positive and negative index values were selected to validate their anti-inflammatory activity in vitro. The results showed that two polymethoxy flavones with higher positive index values, i.e., nobiletin and tangeretin can significantly exert anti-inflammatory effects, while other compounds with negative values did not show any activity. In conclusion, our results indicated the proposed approach might be an efficient and rapid way to identify active constituents of TCM formulae.

  4. Anticonflict effects of rose oil and identification of its active constituents.

    PubMed

    Umezu, Toyoshi; Ito, Hiroyasu; Nagano, Kimiyo; Yamakoshi, Miho; Oouchi, Hiroko; Sakaniwa, Misao; Morita, Masatoshi

    2002-11-22

    The present study investigates the pharmacologically active constituents of rose oil, which possesses anti-conflict effects. Analysis using GC/MS revealed that rose oil contains 9 substances that were identified as myrcene, benzyl alcohol, 2-phenethyl alcohol, citronellol, geraniol, citronellyl acetate, eugenol, geranyl acetate and methyl eugenol. We examined the effects of each of these substances using the Geller and Vogel conflict tests in ICR mice. Myrcene, benzyl alcohol and citronellyl acetate did not produce any effects in either tests. Geranyl acetate and methyl eugenol produced no effect in the Geller conflict test. Geraniol and eugenol decreased the response rate during the safe period of the Geller conflict test, but did not affect the response rate during the alarm period. In contrast, 2-phenethyl alcohol and citronellol, like rose oil, produced an increasing effect on the response rate during the alarm period in the Geller conflict test. In addition, both chemicals increased the number of electric shocks mice received in the Vogel conflict test in a manner similar to that of rose oil. Given that 2-phenethyl alcohol and citronellol produced the same anti-conflict effects in both tests as rose oil, we concluded that they are the pharmacologically active constituents of anti-anxiety-like effect of rose oil.

  5. Pheromonal activity of single castoreum constituents in beaver,Castor canadensis.

    PubMed

    Müller-Schwarze, D; Houlihan, P W

    1991-04-01

    Behavioral activity of single components of beaver castoreum was demonstrated for the first time. In four experiments samples were presented to free-ranging beaver in their family territories. First, responses to whole castoreum and anal gland secretion (AGS) from males and females were tested. Second, 24 compounds, known to be constituents of beaver castoreum, were individually screened for activity. Four of these consistently released immediate responses during the observation periods. These are the phenols 4-ethylphenol and 1,2-dihydroxybenzene and the ketones acetophenone and 3-hydroxyacetophenone. In the most complete responses, the beaver sniffed from the water, were attracted to the odor, swam toward its source, went on land, and then approached, sniffed, pawed, and scent-marked the artificial scent mound. 4-Ethoxyphenol, a compound not yet found in castoreum, also released these responses. Five additional compounds resulted in a few delayed visits to the samples during the night following the observations, as evidenced by destroyed scent mounds. These are 4-methyl-1,2-dihydroxybenzene, 4-methoxyacetophenone, 5-methoxysalicylic acid, salicylaldehyde, and 3-hydroxybenzoic acid. Third, mixtures of 24 and six compounds were tested. Responses to these mixtures could be as strong as those to whole castoreum. Fourth, the four regularly active compounds were tested in two additional beaver populations and proved to be active there, too. The response was strongest in the densest beaver population.

  6. Triterpene Constituents of Euphorbia Erythradenia Bioss. and their Anti-HIV Activity

    PubMed Central

    Ayatollahi, Abdul Majid; Zarei, Seyed Mohammad; Memarnejadian, Arash; Ghanadian, Mustafa; Heydarian Moghadam, Mohammad; Kobarfard, Farzad

    2016-01-01

    Phytochemical investigation of the aerial parts of Euphorbia erythradenia Bioss. (Euphorbiaceae), one of Iranian endemic Euphorbias, with particular attention to triterpene constituents, using methanol solvent extraction was carried out. Five known triterpenes, including four cycloartanes and oleanolic acid, were isolated for the first time and identified using NMR and Mass techniques. Anti HIV activity of the isolated triterpenes and ingenoid diterpenes was evaluated using single cycle replicable HIV-1 (SCR HIV-1) virions. Molecular features of the most active compound (IC50 = 0.008 μM, CC50 = 3.264 μM, TI = 380.64), which showed higher therapeutic index than nevirapine, was assessed using molecular docking. Docking studies demonstrated three hydrogen bonds between HIV-1 virion protease active site and this compound with a distance less than 3 A° which can be responsible for the observed anti HIV-1 activity. PMID:28228800

  7. Inhibition of Human Neutrophil Responses by Essential Oil of Artemisia kotuchovii and Its Constituents

    PubMed Central

    Schepetkin, Igor A.; Kushnarenko, Svetlana V.; Özek, Gulmira; Kirpotina, Liliya N.; Utegenova, Gulzhakhan A.; Kotukhov, Yuriy A.; Danilova, Alevtina N.; Özek, Temel; Başer, K. Hüsnü Can; Quinn, Mark T.

    2015-01-01

    Essential oils were obtained by hydrodistillation of the flowers+leaves and stems of Artemisia kotuchovii Kupr. (AKEOf+l and AKEOstm, respectively) and analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC/MS). The primary components of the oils were estragole, (E)- and (Z)-β-ocimenes, methyl eugenol, limonene, spathulenol, β-pinene, myrcene, and (E)-methyl cinnamate. Seventy four constituents were present at concentrations from 0.1 to 1.0%, and 34 compounds were identified in trace (<0.1%) amounts in one or both plant components. Screening of the essential oils for biological activity showed that AKEOstm, but not AKEOf+l, inhibited N-formyl-Met-Leu-Phe (fMLF)-stimulated Ca2+ flux and chemotaxis and phorbol-12-myristate-13-acetate (PMA)-induced reactive oxygen species (ROS) production in human neutrophils. Selected pure constituents, representing >96% of the AKEOstm composition, were also tested in human neutrophils and HL-60 cells transfected with N-formyl peptide receptor 1 (FPR1). We found that one component, 6-methyl-3,5-heptadien-2-one (MHDO), inhibited fMLF- and interleukin 8 (IL-8)-stimulated Ca2+ flux, fMLF-induced chemotaxis, and PMA-induced ROS production in human neutrophils. MHDO also inhibited fMLF-induced Ca2+ flux in FPR1-HL60 cells. These results suggest that MHDO may be effective in modulating some innate immune responses, possibly by an inhibition of neutrophil migration and ROS production. PMID:25959257

  8. Inhibition of Human Neutrophil Responses by the Essential Oil of Artemisia kotuchovii and Its Constituents.

    PubMed

    Schepetkin, Igor A; Kushnarenko, Svetlana V; Özek, Gulmira; Kirpotina, Liliya N; Utegenova, Gulzhakhan A; Kotukhov, Yuriy A; Danilova, Alevtina N; Özek, Temel; Başer, K Hüsnü Can; Quinn, Mark T

    2015-05-27

    Essential oils were obtained by hydrodistillation of the flowers+leaves and stems of Artemisia kotuchovii Kupr. (AKEO(f+l) and AKEO(stm), respectively) and analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). The primary components of the oils were estragole, (E)- and (Z)-β-ocimenes, methyleugenol, limonene, spathulenol, β-pinene, myrcene, and (E)-methyl cinnamate. Seventy-four constituents were present at concentrations from 0.1 to 1.0%, and 34 compounds were identified in trace (<0.1%) amounts in one or both plant components. Screening of the essential oils for biological activity showed that AKEO(stm), but not AKEOf+l, inhibited N-formyl-Met-Leu-Phe (fMLF)-stimulated Ca(2+) flux and chemotaxis and phorbol-12-myristate-13-acetate (PMA)-induced reactive oxygen species (ROS) production in human neutrophils. Selected pure constituents, representing >96% of the AKEO(stm) composition, were also tested in human neutrophils and HL-60 cells transfected with N-formyl peptide receptor 1 (FPR1). One component, 6-methyl-3,5-heptadien-2-one (MHDO), inhibited fMLF- and interleukin 8 (IL-8)-stimulated Ca(2+) flux, fMLF-induced chemotaxis, and PMA-induced ROS production in human neutrophils. MHDO also inhibited fMLF-induced Ca(2+) flux in FPR1-HL60 cells. These results suggest that MHDO may be effective in modulating some innate immune responses, possibly by inhibition of neutrophil migration and ROS production.

  9. Screening of Thai medicinal plant extracts and their active constituents for in vitro antimalarial activity.

    PubMed

    Ichino, C; Soonthornchareonnon, N; Chuakul, W; Kiyohara, H; Ishiyama, A; Sekiguchi, H; Namatame, M; Otoguro, K; Omura, S; Yamada, H

    2006-04-01

    To discover antimalarial substances from plants cultivated in Thailand 80%-EtOH extracts from selected plants were screened for in vitro antimalarial activity against the drug resistant K1 strain of Plasmodium falciparum. In total, 86 Thai medicinal plant samples representing 48 species from 35 genera in 16 families were screened and two species (Polyalthia viridis and Goniothalamus marcanii) were found to show notable antimalarial activity (IC50: 10.0 and 6.3 microg/mL). Marcanine A and 16-hydroxycleroda-3,13(14)Z-dien-15,16-olide were identified as the respective major active constituents in P. viridis and G. marcanii, respectively.

  10. [Antimicrobial activity and constituents in rumput roman extract as a natural food preservative].

    PubMed

    Sugimoto, Naoki; Tada, Atsuko; Yamazaki, Takashi; Tanamoto, Kenichi

    2007-08-01

    Rumput roman extract is used as a natural food preservative. Its antimicrobial activity and constituents were investigated as part of an ongoing study to evaluate its quality and safety as a food additive. The constituents were analyzed by GC/MS, and 5 major constituents were isolated and identified as capillin, capillene, caryophyllene oxide, alpha-curcumene and methyleugenol using NMR analysis. The antimicrobial activities against E. coli, S. cerevisiae and A. niger were measured by means of the halo test. Based on the results, we confirmed that capillin was the major active constituent. The concentrations of capillin and capillene were determined to 17.9 mg/mL and 36.1 mg/mL, respectively, from standard curves of authentic compounds on HPLC.

  11. Chemical constituents of Tilia taquetii leaves and their inhibition of MMP-1 expression and elastase activities.

    PubMed

    Kim, Su Yeong; Kim, Jung Eun; Bu, Hee Jung; Hyun, Chang-Gu; Lee, Nam Ho

    2014-12-01

    The ethanol extract of Tilia taquetii Schneider leaves was investigated for its anti-wrinkle properties and for the relevant chemical constituents. Phytochemical studies led to the identification of five known compounds, viz. phytol (1), isoquercitrin (2), oleanderolide (3), arjunolic acid (4) and maslinic acid (5) from the extract. Of these, compounds 4 and 5 inhibited the expression of matrix metalloproteinase-1 (MMP-1), an enzyme responsible for the breakdown of collagen fiber. Moreover, compound 5 showed inhibition activity on elastase, a protease enzyme capable of degrading elastin. These results suggest that the extract of T. taquetii containing the triterpenes 4 and 5 could be applied as anti-wrinkle ingredients in cosmetic preparations.

  12. Phytochemical constituents and antibacterial activity of some green leafy vegetables

    PubMed Central

    Bhat, Ramesa Shafi; Al-Daihan, Sooad

    2014-01-01

    Objective To investigate the antibacterial activity and photochemicals of five green leafy vegetables against a panel of five bacteria strains. Methods Disc diffusion method was used to determine the antibacterial activity, while kanamycin was used as a reference antibiotic. The phytochemical screening of the extracts was performed using standard methods. Results All methanol extracts were found active against all the test bacterial strains. Overall maximum extracts shows antibacterial activity which range from 6 to 15 mm. Proteins and carbohydrates was found in all the green leaves, whereas alkaloid, steroids, saponins, flavonoids, tannins were found in most of the test samples. Conclusions The obtain result suggests that green leafy vegetables have moderate antibacterial activity and contain various pharmacologically active compounds and thus provide the scientific basis for the traditional uses of the studied vegetables in the treatment of bacterial infections. PMID:25182436

  13. Anti-ulcer activity of essential oil constituents.

    PubMed

    Oliveira, Francisco de Assis; Andrade, Luciana Nalone; de Sousa, Elida Batista Vieira; de Sousa, Damião Pergentino

    2014-05-05

    Essential oils have attracted considerable worldwide attention over the last few decades. These natural products have wide-ranging pharmacological activities and biotechnological applications. Faced with the need to find new anti-ulcer agents and the great effort on the development of drugs for the treatment of ulcers, in this review, the anti-ulcer activities of 21 bioactive compounds found in essential oils are discussed.

  14. Chemical Constituents Antioxidant and Anticholinesterasic Activity of Tabernaemontana catharinensis

    PubMed Central

    Moura, Sidnei; Echeverrigaray, Sergio

    2013-01-01

    The present work aimed to analyze the alkaloid content of the ethanolic extract of Tabernaemontana catharinensis (Apocynaceae family) and its fractions as well as to evaluate their antioxidant and anticholinesterasic activities. The analyses of the ethanolic extract of T. catharinensis by mass spectrometry allowed identifying the presence of the alkaloids 16-epi-affinine, coronaridine-hydroxyindolenine, voachalotine, voacristine-hydroxyindolenine, and 12-methoxy-n-methyl-voachalotine, as well as an alkaloid with m/z 385.21 whose spectrum suggests a derivative of voacristine or voacangine. The extract and its alkaloid rich fractions showed antioxidant activity, especially those that contain the alkaloid m/z 385.21 or 16-epi-affinine with DPPH scavenging activity (IC50) between 37.18 and 74.69 μg/mL. Moreover, the extract and its fractions exhibited anticholinesterasic activity, particularly the fractions characterized by the presence of 12-methoxy-n-methyl-voachalotine, with IC50 = 2.1 to 2.5 μg/mL. Fractions with 16-epi-affinine combined good antioxidant (IC50 = 65.59 to 74.69 μg/mL) and anticholinesterasic (IC50 = 7.7 to 8.3 μg/mL) activities, representing an option for further studies aimed at treating neurodegenerative diseases. PMID:23983637

  15. Extract of lotus leaf ( Nelumbo nucifera ) and its active constituent catechin with insulin secretagogue activity.

    PubMed

    Huang, Chun Fa; Chen, Ya Wen; Yang, Ching Yao; Lin, Hui Yi; Way, Tzong Der; Chiang, Wenchang; Liu, Shing Hwa

    2011-02-23

    The effect of lotus leaf ( Nelumbo nucifera Gaertn.) on diabetes is unclear. We hypothesized that lotus leaf can regulate insulin secretion and blood glucose levels. The in vitro and in vivo effects of lotus leaf methanolic extract (NNE) on insulin secretion and hyperglycemia were investigated. NNE increased insulin secretion from β cells (HIT-T15) and human islets. NNE enhanced the intracellular calcium levels in β cells. NNE could also enhance phosphorylation of extracellular signal-regulated protein kinases (ERK)1/2 and protein kinase C (PKC), which could be reversed by a PKC inhibitor. The in vivo studies showed that NNE possesses the ability to regulate blood glucose levels in fasted normal mice and high-fat-diet-induced diabetic mice. Furthermore, the in vitro and in vivo effects of the active constituents of NNE, quercetin, and catechin, on glucose-induced insulin secretion and blood glucose regulation were evaluated. Quercetin did not affect insulin secretion, but catechin significantly and dose-dependently enhanced insulin secretion. Orally administered catechin significantly reversed the glucose intolerance in high-fat-diet-induced diabetic mice. These findings suggest that NNE and its active constituent catechin are useful in the control of hyperglycemia in non-insulin-dependent diabetes mellitus through their action as insulin secretagogues.

  16. Constituents of Dalbergia sissoo Roxb. leaves with osteogenic activity.

    PubMed

    Dixit, Preety; Chillara, Raju; Khedgikar, Vikram; Gautam, Jyoti; Kushwaha, Priyanka; Kumar, Avinash; Singh, Divya; Trivedi, Ritu; Maurya, Rakesh

    2012-01-15

    One new isoflavone glucoside, caviunin 7-O-[β-d-apiofuranosyl-(1→6)-β-d-glucopyranoside] (10) and a new itaconic derivative, (E)-4-methoxy-2-(3,4-dihydroxybenzylidene)-4-oxobutanoic acid (15) along with series of isoflavones and flavonols with their glucosides (1-9 and 11-14) and a lignan glucoside (16) were isolated from the ethanolic extract of Dalbergia sissoo leaves. The structures of these compounds were established on the basis of IR, UV, (1)H and (13)C NMR, DEPT, COSY, HSQC, HMBC and MS data. All compounds (1-16) were assessed for osteogenic activity in primary calvarial osteoblast cultures. Compounds 1-4 and 10 increased alkaline phosphatase activity and mineralization thus resulting in significant osteogenic activity.

  17. Anti-trypanosomal activity of nigerian plants and their constituents.

    PubMed

    Nwodo, Ngozi Justina; Ibezim, Akachukwu; Ntie-Kang, Fidele; Adikwu, Michael Umale; Mbah, Chika John

    2015-04-28

    African trypanosomiasis is a vector-borne parasitic disease causing serious risks to the lives of about 60 million people and 48 million cattle globally. Nigerian medicinal plants are known to contain a large variety of chemical structures and some of the plant extracts have been screened for antitrypanosomal activity, in the search for potential new drugs against the illness. We surveyed the literatures on plants and plant-derived products with antitrypanosomal activity from Nigerian flora published from 1990 to 2014. About 90 plants were identified, with 54 compounds as potential active agents and presented by plant families in alphabetical order. This review indicates that the Nigerian flora may be suitable as a starting point in searching for new and more efficient trypanocidal molecules.

  18. Antiprotozoal activity of the constituents of Teloxys graveolens.

    PubMed

    Calzada, Fernando; Velázquez, Claudia; Cedillo-Rivera, Roberto; Esquivel, Baldomero

    2003-08-01

    Antiprotozoal activity-guided fractionation of a methanol extract of the aerial parts of Teloxys graveolens led to the isolation of one coumarinic acid derivative, melilotoside, and five flavonoids, pinocembrine, pinostrobin, chrysin, narcissin and rutin. Among them, melilotoside exhibited the most potent activity toward Entamoeba histolytica and Giardia lamblia (IC(50) 12.5 and 16.8 micro g/mL, respectively). Narcissin showed selectivity against E. histolytlica (IC(50) 17.2 micro g/mL). The results support data for the traditional use of T. graveolens in some gastrointestinal diseases.

  19. Chemical constituents from the rhizomes of Smilax glabra and their antimicrobial activity.

    PubMed

    Xu, Shuo; Shang, Ming-Ying; Liu, Guang-Xue; Xu, Feng; Wang, Xuan; Shou, Cheng-Chao; Cai, Shao-Qing

    2013-05-08

    Six new phenolic compounds, named smiglabrone A (1), smiglabrone B (2), smilachromanone (3), smiglastilbene (4), smiglactone (5), smiglabrol (6), together with fifty-seven known ones 7-63 were isolated from the rhizomes of Smilax glabra. Their structures were elucidated on the basis of extensive spectroscopic analyses, as well as by comparison with literature data. Twenty-seven of these compounds were obtained from and identified in the genus Smilax for the first time. The absolute configuration of (2S)-1,2-O-di-trans-p-coumaroylglycerol (43) was determined for the first time using the exciton-coupled circular dichroism (ECCD) method. Thirty isolated compounds were evaluated for their antimicrobial activity against three Gram-negative bacteria, three Gram-positive bacteria and one fungus, and the corresponding structure-activity relationships were also discussed. Eighteen compounds were found to be antimicrobial against the microorganisms tested and the minimum inhibitory concentrations (MIC) were in the range of 0.0794-3.09 mM. Among them, compound 1 showed antimicrobial activity against Canidia albicans with MIC value of 0.146 mM, which was stronger than cinchonain Ia with an MIC of 0.332 mM. Compounds 3 and 4 exhibited inhibitory activity against Staphylococcus aureus with MIC values of 0.303 and 0.205 mM, respectively. The results indicated that these antimicrobial constituents of this crude drug might be responsible for its clinical antimicrobial effect.

  20. Responses by pacific halibut to air exposure: Lack of correspondence among plasma constituents and mortality

    USGS Publications Warehouse

    Davis, M.W.; Schreck, C.B.

    2005-01-01

    Age-1 and age-2 Pacific halibut Hippoglossus stenolepis were exposed to a range of times in air (0-60 min) and air temperatures (10??C or 16??C) that simulated conditions on deck after capture to test for correspondence among responses in plasma constituents and mortality. Pacific halibut mortality generally did not correspond with cortisol, glucose, sodium, and potassium since the maximum observed plasma concentrations were reached after exposure to 30 min in air, while significant mortality occurred only after exposure to 40 min in air for age-1 fish and 60 min in air for age-2 fish. Predicting mortality in discarded Pacific halibut using these plasma constituents does not appear to be feasible. Lactate concentrations corresponded with mortality in age-1 fish exposed to 16??C and may be useful predictors of discard mortality under a limited set of fishing conditions.

  1. Anti-Aromatase Activity of the Constituents from Damiana (Turnera diffusa)

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Ethnopharmacological relevance: Damiana (Turnera diffusa Willd. Ex Schult) has traditionally been used as an herbal aphrodisiac. Aim of the study: The study was aimed to investigate the anti-aromatse activity and the estrogenic activity of the constituents isolated from T. diffusa. Material and me...

  2. Flavonoid constituents and free radical scavenging activity of Alchemilla mollis.

    PubMed

    Trendafilova, Antoaneta; Todorova, Milka; Nikolova, Milena; Gavrilova, Anna; Vitkova, Antonina

    2011-12-01

    Antioxidant capacity of the methanolic extract of Alchemilla mollis was measured by its ability to scavenge the DPPH radical. The EtOAc fraction obtained after partition of the total extract was found to be the most active radical scavenger (IC50 9.8 +/- 1.8 microg/mL) and was subjected to fractionation by Sephadex LH-20 CC. Further purification by RP-18 CC led to the isolation of eight flavonoid glycosides: cis- and trans-tiliroside (1 and 2), rhodiolgin (3), hyperoside (4), isoquercitrin (5), miquelianin (6), sinocrassoside D2 (7), and gossypetin-3-O-beta-D-galactopyranosyl-7-O-alpha-L-rhamnopyranoside (8). It was found that 8 is a new compound and its antioxidant activity is also reported. Identification of the isolated compounds was carried out by spectroscopic and spectrometric analysis (1D and 2D NMR, UV and MS).

  3. Anti-HBV active constituents from Piper longum.

    PubMed

    Jiang, Zhi-Yong; Liu, Wen-Feng; Zhang, Xue-Mei; Luo, Jie; Ma, Yun-Bao; Chen, Ji-Jun

    2013-04-01

    In the screening search for Hepatitis B virus inhibitory agents from medicinal plants, the ethanol extract of Piper longum Linn. was found to possess superior anti-HBV activity in vitro. Bioassay-guided fractionation coupled with repeated purification resulted in the isolation of four new compounds, involving two new glycosides longumosides A (1) and B (2) and two new amide alkaloids erythro-1-[1-oxo-9(3,4-methylenedioxyphenyl)-8,9-dihydroxy-2E-nonenyl]-piperidine (3), threo-1-[1-oxo-9(3,4-methylenedioxyphenyl)-8,9-dihydroxy-2E-nonenyl]-piperidine (4), as well as two compounds 3β,4α-dihydroxy-2-piperidinone (5), 5,6-dihydro-2(1H)-pyridinone (6) from natural source for the first time. The structures of the four new compounds were determined by extensive analyses of the MS, IR, 1D and 2D NMR data. Besides, the compounds 2-6, together with the known compounds 7-11 obtained previously, were assayed for their anti-HBV activity by using Hep G 2.2.15 cell line in vitro. Results suggested the compound piperine (7) possessed remarkable inhibitory HBV activity, against the secretion of hepatitis B virus surface antigen (HBsAg) and hepatitis B virus e antigen (HBeAg) with the Selectivity Index (SI) values of 15.7 and 16.8, respectively.

  4. Anti-arthritic active fraction of Capparis spinosa L. fruits and its chemical constituents.

    PubMed

    Feng, Xiaolu; Lu, Jincai; Xin, Hailiang; Zhang, Lei; Wang, Yuliang; Tang, Kexuan

    2011-03-01

    The aim of this study was to ascertain the anti-arthritic active fraction of Capparis spinosa L. (Capparidaceae) fruits and its chemical constituents. The adjuvant arthritic rat model was developed to evaluate the anti-arthritic effects of different fractions of ethanol extraction from C. spinosa L. The fraction eluted by ethanol-water (50:50, v/v) had the most significant anti-arthritic activity. The chemical constituents of this fraction were therefore studied; seven known compounds were isolated and identified as: P-hydroxy benzoic acid; 5-(hydroxymethyl) furfural; bis(5-formylfurfuryl) ether; daucosterol; α-D-fructofuranosides methyl; uracil; and stachydrine.

  5. [Advances on investigation of chemical constituents, pharmacological activities and clinical applications of Capparis spinosa].

    PubMed

    Yang, Tao; Liu, Yu-Qing; Wang, Chang-Hong; Wang, Zheng-Tao

    2008-11-01

    In this paper, the chemical constituents, pharmacological activities and clinical applications of Capparis spinosa had been reviewed. The constituents of C. spinosa include the saccharides and glycosides, flavonoids, alkaloids, terpenoids and volatile oils, fatty acids and steroides and so on. C. spinosa had many extensive pharmacological effects such as anti-inflammatory, odynolysis, antifungus, hepatoprotective effect, hypoglycemic activity, antioxidation, anti-hyperlipemia, anticoagulated blood, smooth muscle stimulation, anti-stress reaction, improve memory. It was used to treat arthrolithiasis, rheumarthritis and dermatosis in clinic in domestic, and it would have a broad application prospects.

  6. Biologically active constituents from the fruiting body of Taiwanofungus camphoratus.

    PubMed

    Shi, Li-Shian; Chao, Chih-Hua; Shen, De-Yang; Chan, Hsiu-Hui; Chen, Chou-Hsiung; Liao, Yu-Ren; Wu, Shwu-Jen; Leu, Yann-Lii; Shen, Yuh-Chiang; Kuo, Yao-Haur; Lee, E-Jian; Qian, Keduo; Wu, Tian-Shung; Lee, Kuo-Hsiung

    2011-01-01

    Five new benzenoids, benzocamphorins A-E (1-5), and 10 recently isolated triterpenoids, camphoratins A-J (16-25), together with 23 known compounds including seven benzenoids (6-12), three lignans (13-15), and 13 triterpenoids (26-38) were isolated from the fruiting body of Taiwanofungus camphoratus. Their structures were established by spectroscopic analysis. Selected compounds were examined for cytotoxic and anti-inflammatory activities. Compounds 9 and 21 showed moderate cytotoxicity against MCF-7 and Hep2 cell lines with ED(50) values of 3.4 and 3.0μg/mL, respectively. Compounds 21, 25, 26, 29-31, 33, and 36 demonstrated potent anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced nitric oxide (NO) production with IC(50) values of 2.5, 1.6, 3.6, 0.6, 4.1, 4.2, 2.5, and 1.5μM, respectively, which were better than those of the nonspecific nitric oxide synthase (NOS) inhibitor N-nitro-l-arginine methyl ester (l-NAME) (IC(50): 25.8μM). These results may substantiate the use of T. camphoratus in traditional Chinese medicine (TCM) for the treatment of inflammation and cancer-related diseases. The newly discovered compounds deserve further development as anti-inflammatory candidates.

  7. Biologically Active Constituents from the Fruiting Body of Taiwanofungus camphoratus

    PubMed Central

    Shi, Li-Shian; Chao, Chih-Hua; Shen, De-Yang; Chan, Hsiu-Hui; Chen, Chou-Hsiung; Liao, Yu-Ren; Wu, Shwu-Jen; Leu, Yann-Lii; Shen, Yuh-Chiang; Kuo, Yao-Haur; Lee, E-Jian; Qian, Keduo; Wu, Tian-Shung; Lee, Kuo-Hsiung

    2010-01-01

    Five new benzenoids, benzocamphorins A–E (1–5), and ten recently isolated triterpenoids, camphoratins A–J (16–25), together with 23 known compounds including seven benzenoids (6–12), three lignans (13–15), and 13 triterpenoids (26–38) were isolated from the fruiting body of Taiwanofungus camphoratus. Their structures were established by spectroscopic analysis. Selected compounds were examined for cytotoxic and anti-inflammatory activities. Compounds 9 and 21 showed moderate cytotoxicity against MCF-7 and Hep2 cell lines with ED50 values of 3.4 and 3.0 µg/mL, respectively. Compounds 21, 25, 26, 29–31, 33, and 36 demonstrated potent anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced nitric oxide (NO) production with IC50 values of 2.5, 1.6, 3.6, 0.6, 4.1, 4.2, 2.5, and 1.5 µM, respectively, which were better than those of the nonspecific nitric oxide synthase (NOS) inhibitor N-nitro-L-arginine methyl ester (L-NAME) (IC50: 25.8 µM). These results may substantiate the use of T. camphoratus in traditional Chinese medicine (TCM) for the treatment of inflammation and cancer-related diseases. The newly discovered compounds deserve further development as anti-inflammatory candidates. PMID:21115251

  8. [Chemical constituents of Jasminum giraldii and their antioxidant activity].

    PubMed

    Zhang, Xiu-Peng; Qin, Hui; Yang, Fang; Chai, Jiang; Wang, Xin; Song, Xiao-Mei; Mei, Qi-Bing; Feng, Feng; Yue, Zheng-Gang

    2014-06-01

    Ten compounds were isolated from the barks of Jasminum giraldii by means of various of chromatographic techniques such as silica gel, Sephadex LH-20 and Rp-HPLC. Their structures were identified by spectroscopic data analysis as (+)-medioresinol (1), (+) -syringaresinol (2), syringaresinol-4'-O-beta-D-glucopyranoside (3), oleanic acid (4), 3-methoxy-4-hydroxy-trans-cinnamaldehyde (5), trans-sinapaldehyde (6), syringaldehyde (7), 1-(4-methoxy -phenyl) -ethanol (8), trans-cinnamic acid (9), and 4-(1-methoxyethyl) -phenol (10). Among them, compounds 1-3, 5-8 and 10 were isolated from the J. genus for the first time and compounds 4 and 9 were obtained from J. giraldii for the first time. In the DPPH free radical scavenging assay, compound 1 exhibited significant activity (IC50 55.1 micromol x L(-1)), compared with vitamin C(IC50 59.9 micromol x L(-1)); and compound 2 showed moderate activity (IC50 79.0 micromol x L(-1)), compared with 2, 6-di-tert-butyl4-methylphenol (IC50 236 micromol x L(-1)).

  9. Chemical constituents and antioxidant activity of Mallotus roxburghianus leaves.

    PubMed

    Rana, Virendra S; Rawat, Mohan S M; Pant, Geeta; Nagatsu, Akito

    2005-06-01

    Mallotus roxburghianus is used in the traditional medicine in North-Eastern India, but previously no work has been done on the identification of bioactive compounds. Two new compounds, 3-(1-C-beta-D-glucopyranosyl)-2,6-dihydroxy-5-methoxybenzoic acid (6) and 2,4,8,9,10-pentahydroxy-3,7-dimethoxyanthracene-6-O-beta-D-rhamnopyranoside (7) together with beta-sitosterol (1), stigmasterol (2), betulinic acid (3), 4-hydroxybenzoic acid (4), beta-sitosterol-beta-D-glucoside (5), and bergenin (8) were isolated and identified from the leaves of M. roxburghianus. The chloroform soluble portion of the alcoholic extract of leaf, and compounds 3, 6, 7, and 8 exhibited encouraging antioxidant activities.

  10. Estrogenic activity of chemical constituents from Tephrosia candida.

    PubMed

    Hegazy, Mohamed-Elamir F; El-Hamd H Mohamed, Abou; El-Halawany, Ali M; Djemgou, Pierre C; Shahat, Abdelaaty A; Paré, Paul W

    2011-05-27

    In a continued investigation of medicinal plants from the genus Tephrosia, phytochemical analysis of a methylene chloride-methanol (1:1) extract of the air-dried aerial parts of Tephrosia candida afforded two new 8-prenylated flavonoids, namely, tephrocandidins A (1) and B (2), a new prenylated chalcone, candidachalcone (3), a new sesquiterpene (4), and a previously reported pea flavonoid phytoalexin, pisatin (5). The structures of 1-4 were established by spectroscopic methods, including HREIMS, and 1H, 13C, DEPT, HMQC, and HMBC NMR experiments. The most potent estrogenic activity of these isolated natural products in an estrogen receptor (ERα) competitive-binding assay was for 3, which exhibited an IC50 value of 80 μM, compared with 18 nM for the natural steroid 17β-estradiol. Results were interpreted via virtual docking of isolated compounds to an ERα crystal structure.

  11. Antimicrobial activity of Arctium lappa constituents against microorganisms commonly found in endodontic infections.

    PubMed

    Pereira, Juliana Vianna; Bergamo, Débora Cristina Baldoqui; Pereira, José Odair; França, Suzelei de Castro; Pietro, Rosemeire Cristina Linhares Rodrigues; Silva-Sousa, Yara T Corrêa

    2005-01-01

    This study evaluated in vitro the antimicrobial activity of rough extracts from leaves of Arctium lappa and their phases. The following microorganisms, commonly found in the oral cavity, specifically in endodontic infections, were used: Enterococcus faecalis, Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus subtilis and Candida albicans. The agar-diffusion method allowed detection of the hexanic phase as an inhibitor of microbial growth. Bioautographic assays identified antimicrobial substances in the extract. The results showed the existence, in the rough hexanic phase and in its fractions, of constituents that have retention factors (Rf) in three distinct zones, thereby suggesting the presence of active constituents with chemical structures of different polarities that exhibited specificity against the target microorganisms. It may be concluded that the Arctium lappa constituents exhibited a great microbial inhibition potential against the tested endodontic pathogens.

  12. Activation of octopaminergic receptors by essential oil constituents isolated from aromatic plants: possible mode of action against insect pests.

    PubMed

    Kostyukovsky, Moshe; Rafaeli, Ada; Gileadi, Carina; Demchenko, Nataly; Shaaya, Eli

    2002-11-01

    As a result of screening a large number of essential oils from Israeli aromatic plants and their biologically active constituents, we isolated two oils with high activity against several stored-product insects. In this study the effect of these compounds on the acetylcholinesterase and the octopamine systems in insects was studied in order to elucidate their mode of action. Inhibition of acetylcholinesterase activity in vitro was evident only at high concentrations (10(-3) M) and could not account effectively for the low-dose mortality for some stored-product insects observed in vivo. However, the essential oil constituents were found to cause a significant increase in the levels of the intracellular messenger, cyclic AMP of abdominal epidermal tissue in the model insect, Helicoverpa armigera Hübn. The effect was significant even at low, physiological concentrations (10(-8) M) when tested directly on abdominal epidermal tissue preparations in vitro. This intracellular response was found to resemble closely the significant increases in the levels of the cyclic AMP of abdominal epidermal tissue due to treatment with the neurotransmitter/neuromodulator, octopamine. Subsequent treatment with the octopaminergic antagonist, phentolamine, effectively inhibited the cyclic AMP levels induced by essential oil treatment, indicating possible competitive activation of octopaminergic receptors by essential oil constituents.

  13. Insecticidal Constituents and Activity of Alkaloids from Cynanchum mongolicum.

    PubMed

    Ge, Yang; Liu, Pingping; Yang, Rui; Zhang, Liu; Chen, Hongxing; Camara, Ibrahima; Liu, Yiqing; Shi, Wangpeng

    2015-09-21

    Based on MS and NMR data and bioassay-guided tracing, three insecticidal alkaloids I, II and III from Cynanchum mongolicum were identified to be antofine N-oxide, antofine and tylophorine. Alkaloid I was more toxic than alkaloids II and III, but they were less active against Spodoptera litura than total alkaloids. The contact toxicity from these alkaloids against the aphid Lipaphis erysimi was significant, as the 24 h-LC50 values of alkaloids I, II, III and total alkaloids were 292.48, 367.21, 487.791 and 163.52 mg/L, respectively. The development disruption of S. litura larvae was tested, the pupation and emergence rates of S. litura decreased and the acute mortality of S. litura increased significantly by day 3 after being injected in their body cavity with 10-40 mg/L of total alkaloid. The ecdysone titer of treated S. litura larvae and prepupae declined with increasing alkaloid concentration. The alkaloids of Cynanchum mongolicum are potential insect growth inhibitors.

  14. Antioxidant potential of spices and their active constituents.

    PubMed

    Srinivasan, K

    2014-01-01

    Excessive free radical generation overbalancing the rate of their removal leads to oxidative stress. Oxidative stress has been implicated in the etiology of cardiovascular disease, inflammatory diseases, cancer, and other chronic diseases. Antioxidants are compounds that hinder the oxidative processes and thereby delay or suppress oxidative stress. There is a growing interest in natural antioxidants found in plants. Herbs and spices are most important targets to search for natural antioxidants from the point of view of safety. A wide variety of phenolic compounds present in spices that are extensively used as food adjuncts possess potent antioxidant, anti-inflammatory, antimutagenic, and cancer preventive activities. This paper reviews a host of spice compounds as exogenous antioxidants that are experimentally evidenced to control cellular oxidative stress, both in vitro and in vivo, and their beneficial role in preventing or ameliorating oxidative-stress-mediated diseases, from atherosclerosis to diabetes to cataract to cancer. The antioxidative effects of turmeric/curcumin, clove/eugenol, red pepper/capsaicin, black pepper/piperine, ginger/gingerol, garlic, onion, and fenugreek, which have been extensively studied and evidenced as potential antioxidants, are specifically reviewed in this treatise.

  15. Characterization of antiproliferative activity constituents from Artocarpus heterophyllus.

    PubMed

    Zheng, Zong-Ping; Xu, Yang; Qin, Chuan; Zhang, Shuang; Gu, Xiaohong; Lin, Yingying; Xie, Guobin; Wang, Mingfu; Chen, Jie

    2014-06-18

    Artocarpus heterophyllus is an evergreen fruit tree cultivated in many tropical regions. Previous studies have shown that some of its compositions exhibited potential tyrosinase inhibition activities. This study indentified 8 new phenolic compounds, artoheterophyllins E-J (1-6), 4-geranyl-2',3,4',5-tetrahydroxy-cis-stilbene (7), and 5-methoxymorican M (8) and 2 new natural compounds (9 and 10), 2,3-dihydro-5,7-dihydroxy-2-(2-hydroxy-4-methoxyphenyl)-4H-benzopyran-4-one and 6-[(1S,2S)-1,2-dihydroxy-3-methylbutyl]-2-(2,4-dihydroxyphenyl)-5-hydroxy-7-methoxy-3-(3-methyl-2-buten-1-yl)-4H-1-benzopyran-4-one, together with 23 known compounds (11-33), from the ethanol extract of the wood of A. heterophyllus. The structures of the eight new compounds (1-8) and two new natural compounds were established by extensive 1D- and 2D-NMR experiments. The anticancer effects of the isolated compounds were examined in MCF-7, H460, and SMMC-7721 human cancer cell lines by MTT assay. Compounds 5, 11, 12, and 30 significantly reduced the cell viabilities of these cell lines. Especially, compounds 11 and 30 resulted in more potent cytotoxicity than the positive control, 5-fluorouracil (5-Fu), in SMMC-7721 cell line, with IC50 values of 15.85 and 12.06 μM, whereas compound 30 exhibited more potent cytotoxicity than 5-Fu in NCI-H460 cell line, with an IC50 value of 5.19 μM. In addition, this study suggests that compounds 11 and 30 from the wood of A. heterophyllus have anticancer potential via MAPK pathways.

  16. Repellent activity of essential oils and some of their individual constituents against Tribolium castaneum herbst.

    PubMed

    Caballero-Gallardo, Karina; Olivero-Verbel, Jesús; Stashenko, Elena E

    2011-03-09

    A tool for integrated pest management is the use of essential oils (EOs) and plant extracts. In this study, EOs from Tagetes lucida , Lepechinia betonicifolia , Lippia alba , Cananga odorata , and Rosmarinus officinalis , species grown in Colombia, were analyzed by gas chromatography-mass spectrometry. These oils as well as several of their constituents were tested for repellent activity against Tribolium castaneum , using the area preference method. The main components (>10%) found in EOs were methylchavicol, limonene/α-pinene, carvone/limonene, benzyl acetate/linalool/benzyl benzoate, and α-pinene, for T. lucida, L. betonicifolia, L. alba, C. odorata, and R. officinalis, respectively. All EOs were repellent, followed a dose-response relationship, and had bioactivity similar to or better than that of commercial compound IR3535. EOs from C. odorata and L. alba were the most active. Compounds from EOs, such benzyl benzoate, β-myrcene, and carvone, showed good repellent properties. In short, EOs from plants cultivated in Colombia are sources of repellents against T. castaneum.

  17. Antiplatelet effects of Rhus verniciflua stokes heartwood and its active constituents--fisetin, butein, and sulfuretin--in rats.

    PubMed

    Lee, Jun-Hyeong; Kim, Mikyung; Chang, Kyung-Hwa; Hong, Cheol Yi; Na, Chun-Soo; Dong, Mi-Sook; Lee, Dongho; Lee, Moo-Yeol

    2015-01-01

    Rhus verniciflua stokes (RVS) is known to promote blood circulation by preventing blood stasis, although the active ingredients and the underlying mechanism are unclear. Platelets are the primary cells that regulate circulation and contribute to the development of diverse cardiovascular diseases by aggregation and thrombosis. The study assessed the antiplatelet activity of RVS and sought to identify the active constituents. Pretreatment of washed platelets with RVS heartwood extract blunted the aggregatory response of platelets to collagen. In the subfractions, fisetin, butein, and sulfuretin were identified as effective inhibitors of platelet aggregation by collagen, thrombin, and adenosine-5'-diphosphate. Antiplatelet activities of all three compounds were concentration dependent, and fisetin had longer in vitro duration of action compared with butein or sulfuretin. Extracellular signal-regulated kinase (ERK) mitogen-activated protein kinase activation by collagen was prevented by fisetin, whereas butein and sulfuretin failed to inhibit ERK and p38 activation was not affected by any of the compounds. Rats orally administered 100 mg/(kg·day(-1)) fisetin for 7 days were resistant to arterial thrombosis, although total extract of RVS heartwood exhibited little effect at a dose of 1000 mg/(kg·day(-1)). RVS heartwood may have cardiovascular protective activity by inhibiting platelet aggregation. The active constituents are fisetin, butein, and sulfuretin, and fisetin is orally effective against thrombosis.

  18. Smooth muscle relaxant activity of Crocus sativus (saffron) and its constituents: possible mechanisms.

    PubMed

    Mokhtari-Zaer, Amin; Khazdair, Mohammad Reza; Boskabady, Mohammad Hossein

    2015-01-01

    Saffron, Crocus sativus L. (C. sativus) is rich in carotenoids and used in traditional medicine for treatment of various conditions such as coughs, stomach disorders, amenorrhea, asthma and cardiovascular disorders. These therapeutic effects of the plant are suggested to be due to its relaxant effect on smooth muscles. The effect of C. sativus and its constituents on different smooth muscles and the underlying mechanisms have been studied. Several studies have shown the relaxant effects of C. sativus and its constituents including safranal, crocin, crocetin and kaempferol on blood vessels. In addition, it was reported that saffron stigma lowers systolic blood pressure. The present review highlights the relaxant effects of C. sativus and its constituents on various smooth muscles. The possible mechanisms of this relaxing effect including activation of ß2-adrenoceptors, inhibition of histamine H1 and muscarinic receptors and calcium channels and modulation of nitric oxide (NO) are also reviewed.

  19. Antinociceptive activity and chemical composition of constituents from Caragana microphylla seeds.

    PubMed

    Huo, Y; Guo, C; Zhang, Q-Y; Chen, W-S; Zheng, H-C; Rahman, K; Qin, L-P

    2007-02-01

    This investigation was undertaken to ascertain the antinociceptive activity of Caragana microphylla Lam. seeds and isolate and characterize the constituents. Antinociceptive activity was screened using acetic acid-induced abdominal constriction in ICR mice. The 75% ethanol extract and some fractions showed analgesic activity, but the antinociceptive activity of chloroform fraction was the strongest and was more productive than other fractions. Seven compounds were isolated from it and identified as: (1) machaeric acid, (2) beta-sitosterol, (3) stigmasterol, (4) pratol, (5) dehydrocavidine, (6) formononetin and (7) sucrose. Caragana microphylla Lam. seeds showed analgesic activity, with the chloroform fraction showing the strongest analgesic activity among the fractions.

  20. Hypoglycemic activity of leaf organic extracts from Smallanthus sonchifolius: Constituents of the most active fractions.

    PubMed

    Genta, Susana B; Cabrera, Wilfredo M; Mercado, María I; Grau, Alfredo; Catalán, César A; Sánchez, Sara S

    2010-04-29

    The aim of the present study was to determine the in vivo hypoglycemic activity of five organic extracts and enhydrin obtained from yacon leaves. The main constituents of the most active fraction were identified. Five organic extracts and pure crystalline enhydrin were administered to normoglycemic, transiently hyperglycemic and streptozotocin (STZ)-diabetic rats. The fasting and post-prandial blood glucose, and serum insulin levels were estimated and an oral glucose tolerance test (OGTT) was performed for the evaluation of hypoglycemic activity and dose optimization of each extract. We found that the methanol, butanol and chloroform extracts showed effective hypoglycemic activity at minimum doses of 50, 10 and 20mg/kg body weight, respectively, and were selected for further experiments. Oral administration of a single-dose of each extract produced a slight lowering effect in the fasting blood glucose level of normal healthy rats, whereas each extract tempered significantly the hyperglycemic peak after food ingestion. Daily administration of each extract for 8 weeks produced an effective glycemic control in diabetic animals with an increase in the plasma insulin level. Phytochemical analysis of the most active fraction, the butanol extract, showed that caffeic, chlorogenic and three dicaffeoilquinic acids were significant components. Additionally, enhydrin, the major sesquiterpene lactone of yacon leaves, was also effective to reduce post-prandial glucose and useful in the treatment of diabetic animals (minimum dose: 0.8mg/kg body weight). The results presented here strongly support the notion that the phenolic compounds above as well as enhydrin are important hypoglycemic principles of yacon leaves that could ameliorate the diabetic state.

  1. Cancer Chemoprevention Effects of Ginger and its Active Constituents: Potential for New Drug Discovery.

    PubMed

    Wang, Chong-Zhi; Qi, Lian-Wen; Yuan, Chun-Su

    2015-01-01

    Ginger is a commonly used spice and herbal medicine worldwide. Besides its extensive use as a condiment, ginger has been used in traditional Chinese medicine for the management of various medical conditions. In recent years, ginger has received wide attention due to its observed antiemetic and anticancer activities. This paper reviews the potential role of ginger and its active constituents in cancer chemoprevention. The phytochemistry, bioactivity, and molecular targets of ginger constituents, especially 6-shogaol, are discussed. The content of 6-shogaol is very low in fresh ginger, but significantly higher after steaming. With reported anti-cancer activities, 6-shogaol can be served as a lead compound for new drug discovery. The lead compound derivative synthesis, bioactivity evaluation, and computational docking provide a promising opportunity to identify novel anticancer compounds originating from ginger.

  2. Genetic stability, active constituent, and pharmacoactivity of Salvia miltiorrhiza hairy roots and wild plant.

    PubMed

    Yuan, Yuan; Liu, Yunjun; Lu, Dongmei; Huang, Luqi; Liang, Rixin; Yang, Zhaochun; Chen, Shunqin

    2009-01-01

    Salvia miltiorrhiza is an annual plant growing in China, Mongolia, Korea and some other Asian countries. The extract from S. miltiorrhiza roots has been used for supporting healthy cardiovascular and circulatory systems during the last decade. The active constituents of S. miltiorrhiza from different areas vary significantly, and the wild resources are overexploited. To adapt the demand for active constituents of S. miltiorrhiza against cardiovascular-related diseases, alternative materials need to be developed. The aim of the present work was to investigate the possibility of S. miltiorrhiza hairy roots as the alternative materials. The results showed that S. miltiorrhiza hairy roots are genetically stable. The contents of salvianolic acid B and tanshinone IIA, two main active constituents in hairy roots, determined by the assessment of combining flow cytometry and phytochemical analysis, are comparable to or significantly lower than in wild plant roots. The extract from S. miltiorrhiza hairy roots also had similar protection activity for hypoxia and reoxygenation injury in rat cardiac myocytes like that from wild plant roots. S. miltiorrhiza hairy roots may be alternative materials to obtain the drug or healthy food for cardiovascular-related diseases.

  3. Antischistosomal Activity of Two Active Constituents Isolated from the Leaves of Egyptian Medicinal Plants

    PubMed Central

    Ali, Sanaa A; El-Regal, Nagy S; Saeed, Samar M

    2015-01-01

    In this paper, we investigate the role of two active constituents isolated from the leaves of Egyptian medicinal plants. D-mannitol a naturally occurring sugar isolated from the leaves Ixora undulata Roxb., and the pectin a linear chain homogalacturonan (HG) polysaccharide isolated from the leaves of Linum grandiflorum Desf. (scarlet flax). Both are evaluated for their therapeutic effect against schistosomiasis with biochemical and histochemical evaluations and compared with praziquantel, a reference drug. Biochemical studies of hepatic glucose, the glycogen content, and total serum protein were carried out, and histochemical evaluations through serum protein fractions separated by polyacrylamide gel electrophoresis with different molecular weights (260–10 kDa) were made in all groups, in addition to liver and body weight. D-mannitol and pectin show a remarkable effect in enhancing liver and kidney functions through enhancing most protein fractions in the serum of mice infected with Schistosoma mansoni. Also, the glucose and glycogen content in injured liver tissues improved, in addition liver and body weight in the infected groups. Thus they may be of therapeutic potential in the treatment hepatoxicity and nephrotoxicity. PMID:26124666

  4. Analysis and antimicrobial activity of volatile constituents from Quercus leucotrichophora (Fagaceae) bark.

    PubMed

    Sati, Sushil Chandra; Sati, Nitin; Sati, O P; Biswas, D; Chauhan, B S

    2012-01-01

    The chemical composition of the volatile extract (yield ≈ 0.13%, v/w) from the bark of Quercus leucotrichophora (Fagaceae) was analysed for the first time by GC-MS. Twenty-three constituents, amounting to 93.0% of the total detected contents of the volatile extract, were identified. The volatile extract contained approximately 86.36% monoterpenoids, 6.53% sesquiterpenoids and 0.11% aliphatic aldehydes. 1,8-Cineol (40.359%) followed by γ-terpinene (16.369%) were the major monoterpene constituents of the volatile extract. The residue of volatile extract (0.00025-250 µg  mL(-1)) exhibited a potent antimicrobial activity against Streptococcus pyogenes ATCC 19615. This study concludes that residues of the volatile extract of Q. leucotrichophora could serve as an important bioresource for the extraction and isolation of monoterpenoids exhibiting antimicrobial activity, and thus has good potential for use in the pharmaceutical industry.

  5. Inhibition of the myotoxic and hemorrhagic activities of crotalid venoms by Eclipta prostrata (Asteraceae) extracts and constituents.

    PubMed

    Melo, P A; do Nascimento, M C; Mors, W B; Suarez-Kurtz, G

    1994-05-01

    The antimyotoxic and antihemorrhagic effects of Eclipta prostrata (EP) and three of its constituents (wedelolactone, WE; stigmaterol, ST; and sitosterol, SI) were investigated. The myotoxicity of crotalid venoms (Bothrops jararaca, Bothrops jararacussu and Lachesis muta), purified myotoxins (bothropstoxin, BthTX; bothropasin; and crotoxin), and polylysine was quantified in vitro by the release rate of creatine kinase (CK) from rat or mouse extensor digitorum muscles, and in vivo by the plasma CK activity in mice. The in vitro myotoxicity of the crotalid venoms and myotoxins was neutralized by simultaneous exposure of the muscles to an aqueous extract of EP or to WE. ST and SI were less effective than WE, but interacted synergistically with it. Both the EP extract and WE failed to neutralize the in vitro myotoxic effects of polylysine. The in vivo myotoxicity of venoms and myotoxins was neutralized by their preincubation with the EP extract or WE. Intravenous administration of the plant extract or WE attenuated the increase in plasma CK activity induced by subsequent intramuscular injections of the crotalid venoms or the myotoxins. EP and WE inhibited the hemorrhagic effect of B. jararaca venom, as well as the phospholipase A2 activity of crotoxin and the proteolytic activity of B. jararaca venom. The data provide direct evidence for antimyotoxic and antihemorrhagic effects of EP and WE against the crotalid venoms responsible for most cases of envenomation by snakebites in Brazil. These effects are interpreted as consequences of antiproteolytic and antiphospholipase A2 activities of EP and its constituents.

  6. Effects of Thymol and Carvacrol, Constituents of Thymus vulgaris L. Essential Oil, on the Inflammatory Response

    PubMed Central

    Fachini-Queiroz, Fernanda Carolina; Kummer, Raquel; Estevão-Silva, Camila Fernanda; Carvalho, Maria Dalva de Barros; Cunha, Joice Maria; Grespan, Renata; Bersani-Amado, Ciomar Aparecida; Cuman, Roberto Kenji Nakamura

    2012-01-01

    Thyme (Thymus vulgaris L., Lamiaceae) is an aromatic and medicinal plant that has been used in folk medicine, phytopharmaceutical preparations, food preservatives, and as an aromatic ingredient. The effect of Thymus vulgaris essential oil (TEO) and its isolated constituents thymol and cavacrol (CVL) were studied in the following experimental models: ear edema, carrageenan-induced pleurisy, and chemotaxis in vitro. In the pleurisy model, TEO, CVL, and thymol significantly inhibited inflammatory edema. However, only TEO and CVL inhibited leukocyte migration. In the in vitro chemotaxis experiment, CVL inhibited leukocyte migration, whereas thymol exerted a potent chemoattractant effect. In the ear edema model, CVL (10 mg/ear), applied topically, reduced edema formation, exerting a topical anti-inflammatory effect. Thymol did not reduce edema formation but rather presented an irritative response, probably dependent on histamine and prostanoid release. Our data suggest that the antiinflammatory effects of TEO and CVL are attributable to the inhibition of inflammatory edema and leukocyte migration. PMID:22919415

  7. The effect of activated dimethicone, other antacid constituents, and kaolin on the absorption of propranolol.

    PubMed

    McElnay, J C; D'Arcy, P F; Leonard, J K

    1982-05-15

    A study was made of the effect of 6 commonly used gastrointestinal preparations on the absorption of propranolol using an in vitro experimental model. The constituents examined were activated dimethicone, aluminium hydroxide gel, bismuth carbonate, kaolin, magnesium carbonate, and magnesium trisilicate. A slight decreased propranolol absorption was given by kaolin (-13.0%), the other components showed smaller effects ranging from -6.8% to +6.6%. None of the results were statistically significantly different from control absorption values.

  8. Testosterone 5alpha-reductase inhibitory active constituents of Piper nigrum leaf.

    PubMed

    Hirata, Noriko; Tokunaga, Masashi; Naruto, Shunsuke; Iinuma, Munekazu; Matsuda, Hideaki

    2007-12-01

    Previously we reported that Piper nigrum leaf extract showed a potent stimulation effect on melanogenesis and that (-)-cubebin (1) and (-)-3,4-dimethoxy-3,4-desmethylenedioxycubebin (2) were isolated as active constituents. As a part of our continuous studies on Piper species for the development of cosmetic hair-care agents, testosterone 5alpha-reductase inhibitory activity of aqueous ethanolic extracts obtained from several different parts of six Piper species, namely Piper nigrum, P. methysticum, P. betle, P. kadsura, P. longum, and P. cubeba, were examined. Among them, the extracts of P. nigrum leaf, P. nigrum fruit and P. cubeba fruit showed potent inhibitory activity. Activity-guided fractionation of P. nigrum leaf extract led to the isolation of 1 and 2. Fruits of P. cubeba contain 1 as a major lignan, thus inhibitory activity of the fruit may be attributable to 1. As a result of further assay on other known constituents of the cited Piper species, it was found that piperine, a major alkaloid amide of P. nigrum fruit, showed potent inhibitory activity, thus a part of the inhibitory activity of P. nigrum fruit may depend on piperine. The 5alpha-reductase inhibitory activities of 1 and piperine were found for the first time. In addition, the P. nigrum leaf extract showed in vivo anti-androgenic activity using the hair regrowth assay in testosterone sensitive male C57Black/6CrSlc strain mice.

  9. Chemical Constituents and Insecticidal Activities of Ajania fruticulosa Essential Oil.

    PubMed

    Liang, Jun-Yu; Guo, Shan-Shan; You, Chun-Xue; Zhang, Wen-Juan; Wang, Cheng-Fang; Geng, Zhu-Feng; Deng, Zhi-Wei; Du, Shu-Shan; Zhang, Ji

    2016-08-01

    The insecticidal activity and chemical constituents of the essential oil from Ajania fruticulosa were investigated. Twelve constituents representing 91.0% of the essential oil were identified, and the main constituents were 1,8-cineole (41.40%), (+)-camphor (32.10%), and myrtenol (8.15%). The essential oil exhibited contact toxicity against Tribolium castaneum and Liposcelis bostrychophila adults with LD50 values of 105.67 μg/adult and 89.85 μg/cm(2) , respectively. The essential oil also showed fumigant toxicity against two species of insect with LC50 values of 11.52 and 0.65 mg/l, respectively. 1,8-Cineole exhibited excellent fumigant toxicity (LC50  = 5.47 mg/l) against T. castaneum. (+)-Camphor showed obvious fumigant toxicity (LC50  = 0.43 mg/l) against L. bostrychophila. Myrtenol showed contact toxicity (LD50  = 29.40 μg/cm(2) ) and fumigant toxicity (LC50  = 0.50 mg/l) against L. bostrychophila. 1,8-Cineole and (+)-camphor showed strong insecticidal activity to some important insects, and they are main constituents of A. fruticulosa essential oil. The two compounds may be related to insecticidal activity of A. fruticulosa essential oil against T. castaneum and L. bostrychophila.

  10. Antioxidant, Antibacterial, and Cytotoxic Activities of the Ethanolic Origanum vulgare Extract and Its Major Constituents

    PubMed Central

    Coccimiglio, John; Alipour, Misagh; Jiang, Zi-Hua; Gottardo, Christine

    2016-01-01

    Oregano is a perennial shrub that grows in the mountains of the Mediterranean and Euro/Irano-Siberian regions. This study was conducted to identify the major constituents of the ethanolic Origanum vulgare extract and examine the cytotoxic, antioxidant, and antibacterial properties of the extract but more importantly the contribution of its specific major constituent(s) or their combination to the overall extract biological activity. Gas chromatography/mass spectroscopy analysis showed that the extract contained monoterpene hydrocarbons and phenolic compounds, the major ones being carvacrol and thymol and to a lesser extent p-cymene, 1-octacosanol, creosol, and phytol. A549 epithelial cells challenged with the extract showed a concentration-dependent increase in cytotoxicity. A combination of thymol and carvacrol at equimolar concentrations to those present in the extract was less cytotoxic. The A549 cells pretreated with nonlethal extract concentrations protected against hydrogen-peroxide-induced cytotoxicity, an antioxidant effect more effective than the combination of equimolar concentrations of thymol/carvacrol. Inclusion of p-cymene and/or 1-octacosanol did not alter the synergistic antioxidant effects of the carvacrol/thymol mixture. The extract also exhibited antimicrobial properties against Gram-positive and Gram-negative bacterial strains including clinical isolates. In conclusion, the oregano extract has cytotoxic, antioxidant, and antibacterial activities mostly attributed to carvacrol and thymol. PMID:27051475

  11. Antioxidant, Antibacterial, and Cytotoxic Activities of the Ethanolic Origanum vulgare Extract and Its Major Constituents.

    PubMed

    Coccimiglio, John; Alipour, Misagh; Jiang, Zi-Hua; Gottardo, Christine; Suntres, Zacharias

    2016-01-01

    Oregano is a perennial shrub that grows in the mountains of the Mediterranean and Euro/Irano-Siberian regions. This study was conducted to identify the major constituents of the ethanolic Origanum vulgare extract and examine the cytotoxic, antioxidant, and antibacterial properties of the extract but more importantly the contribution of its specific major constituent(s) or their combination to the overall extract biological activity. Gas chromatography/mass spectroscopy analysis showed that the extract contained monoterpene hydrocarbons and phenolic compounds, the major ones being carvacrol and thymol and to a lesser extent p-cymene, 1-octacosanol, creosol, and phytol. A549 epithelial cells challenged with the extract showed a concentration-dependent increase in cytotoxicity. A combination of thymol and carvacrol at equimolar concentrations to those present in the extract was less cytotoxic. The A549 cells pretreated with nonlethal extract concentrations protected against hydrogen-peroxide-induced cytotoxicity, an antioxidant effect more effective than the combination of equimolar concentrations of thymol/carvacrol. Inclusion of p-cymene and/or 1-octacosanol did not alter the synergistic antioxidant effects of the carvacrol/thymol mixture. The extract also exhibited antimicrobial properties against Gram-positive and Gram-negative bacterial strains including clinical isolates. In conclusion, the oregano extract has cytotoxic, antioxidant, and antibacterial activities mostly attributed to carvacrol and thymol.

  12. Chemical constituents and antioxidant activity of the essential oil from leaves of Annona vepretorum Mart. (Annonaceae)

    PubMed Central

    Araújo, Camila de Souza; de Oliveira, Ana Paula; Lima, Rafaely Nascimento; Alves, Péricles Barreto; Diniz, Tâmara Coimbra; da Silva Almeida, Jackson Roberto Guedes

    2015-01-01

    Background: Annona vepretorum (AV) is a native tree from Caatinga biome (semiarid region of Brazil) popularly known as “araticum” and “pinha da Caatinga.” Objective: This study was carried out to evaluate the chemical constituents and antioxidant activity (AA) of the essential oil from the leaves from AV (EO-Av) collected in Petrolina, Pernambuco, Brazil. Materials and Methods: Fresh leaves of AV were cut into pieces, and subjected to distillation for 2 h in a clevenger-type apparatus. Gas chromatograph (GC) analyses were performed using a mass spectrometry/flame ionization detector. The identification of the constituents was assigned on the basis of comparison of their relative retention indices. The antioxidant ability of the EO was investigated through two in vitro models such as radical scavenging activity using 2,2-diphenyl-1-picrylhydrazyl method and β-carotene-linoleate-model system. The positive controls (ascorbic acid, butylated hydroxyanisole and butylated hydroxytoluene) were those using the standard solutions. Assays were carried out in triplicate. Results: The oil showed a total of 21 components, and 17 were identified, representing 93.9% of the crude EO. Spathulenol (43.7%), limonene (20.5%), caryophyllene oxide (8.1%) and α-pinene (5.5%) were found to be the major individual constituents. Spathulenol and caryophyllene oxide could be considered chemotaxonomic markers of these genera. The EO demonstrated weak AA. PMID:26246740

  13. Phenolic constituents and antioxidant activity of Wendita calysina leaves (Burrito), a folk Paraguayan tea.

    PubMed

    Piccinelli, Anna Lisa; De Simone, Francesco; Passi, Siro; Rastrelli, Luca

    2004-09-22

    Burrito tea originates from the leaves of Wendita calysina, an indigenous Paraguayan plant, which is commonly consumed in South America and in Western countries. Phytochemical investigation of this species has led to the isolation of 14 constituents, among them 2 new flavanonols, dihydroquercetagetin (1) and 3,5,6,7,4'-pentahydroxyflavanonol (2), in addition to several known methoxyflavones, methoxyflavonols, phenylethanoid glycosides, and benzoic acid derivatives (4-14). All structures were elucidated by ESI-MS and NMR spectroscopic methods. Quantitative determination of phenolic constituents from burrito water infusions has been performed by HPLC-UV-DAD. The total antioxidant activity of the tea was measured by the ABTS(*)(+) radical cation decolorization and chemiluminescence (CL) assays and compared with the values of other commonly used herbal teas (green and black teas, mate, and rooibos).

  14. Tetra-acetylajugasterone a new constituent of Vitex cienkowskii with vasorelaxant activity.

    PubMed

    Dongmo, Alain Bertrand; Nkeng-Efouet, Pepin Alango; Devkota, Krishna Prasad; Wegener, Jörg W; Sewald, Norbert; Wagner, Hildebert; Vierling, Wolfgang

    2014-05-15

    Tetra-acetylajugasterone C (TAAC) was found to be one of the naturally occurring compounds of the Cameroonian medicinal plant Vitex cienkowskii which is responsible for a vasorelaxant activity of an extract of this plant. The evaluation of the underlying mechanisms for the relaxing effect of TAAC was determined using aortic rings of rats and mice. TAAC produced a concentration-dependent relaxation in rat artery rings pre-contracted with 1μM noradrenaline (IC50: 8.40μM) or 60mM KCl (IC50: 36.30μM). The nitric oxide synthase inhibitor l-NAME (100μM) and the soluble guanylate cyclase inhibitor ODQ (10μM) significantly attenuated the vasodilatory effect of TAAC. TAAC also exerted a relaxing effect in aorta of wild-type mice (cGKI(+/+); IC50=13.04μM) but a weaker effect in aorta of mice lacking cGMP-dependent protein kinase I (cGKI(-/-); IC50=36.12μM). The involvement of calcium channels was studied in rings pre-incubated in calcium-free buffer and primed with 1μM noradrenaline prior to addition of calcium to elicit contraction. TAAC (100μM) completely inhibited the resulting calcium-induced vasoconstriction. The same concentration of TAAC showed a stronger effect on the tonic than on the phasic component of noradrenaline-induced contraction. This study shows that TAAC, a newly detected constituent of Vitex cienkowskii contributes to the relaxing effect of an extract of the plant. The effect is partially mediated by the involvement of the NO/cGMP pathway of the smooth muscle but additionally inhibition of calcium influx into the cell may play a role.

  15. [Biological activity tests of chemical constituents from two Brazilian Labiatae plants].

    PubMed

    Isobe, Takahiko; Doe, Matsumi; Morimoto, Yoshiki; Nagata, Kumiko; Masuoka, Noriyoshi; Ohsaki, Ayumi

    2007-02-01

    We studied the bioactivities of constituents from two tropical medicinal plants, Cunila spicata and Hyptis fasciculata. These plants found in Brazil belong to the Labiatae family. Four known compounds obtained from these herbs were identified as 3alpha, 24-dihydoxylurs-12-en-28-oic acid, betulinic acid, aurantiamide acetate, and aurantiamide benzoate by spectroscopic means. 3alpha, 24-Dihydoxylurs-12-en-28-oic acid has potent inhibitory activity against Streptococcus salivarius, Streptococcus pneumoniae, Streptococcus pyogenes, and Porphyromomas gingivalis. Aurantiamide benzoate exhibited moderate inhibitory activity against xanthine oxidase. It was clarified that herbs Cunila spicata and Hyptis fasciculata are effective against bronchitis and gout.

  16. Antimicrobial Activity and Phytochemical Constituents of Leaf Extracts of Cassia auriculata.

    PubMed

    Murugan, T; Wins, J Albino; Murugan, M

    2013-01-01

    Plants produce a wide variety of phytochemical constituents, which are secondary metabolites and are used either directly or indirectly in the pharmaceutical industry. 'For centuries, man has effectively used various components of plants or their extracts for the treatment of many diseases, including bacterial infections. In the present study methanol, chloroform and aqueous extracts of Cassia auriculata leaf were subjected for antimicrobial activity by well-diffusion method against six bacterial strains namely Bacillus cereus, Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and Proteus mirabilis. The results revealed that the methanol and chloroform extracts exhibited strong inhibitory activity against all the tested organisms (zone of inhibition of 12-20 mm), except Pseudomonas aeruginosa (zone of inhibition 10 mm or nil). The aqueous extracts showed moderate activity by 'Zone of inhibition ≤12 or nil). The extracts were screened for their phytochemical constituents by standard protocols' and were shown to contain carbohydrates, proteins, alkaloids, flavonoids, steroids, saponins and tannins. The antibacterial activity of these extracts is possibly linked to the presence of flavonoids, steroid, saponins and/or tannins. Further studies are needed to determine the precise active principles from Cassia auriculata.

  17. Antimicrobial Activity and Phytochemical Constituents of Leaf Extracts of Cassia auriculata

    PubMed Central

    Murugan, T.; Wins, J. Albino; Murugan, M.

    2013-01-01

    Plants produce a wide variety of phytochemical constituents, which are secondary metabolites and are used either directly or indirectly in the pharmaceutical industry. ‘For centuries, man has effectively used various components of plants or their extracts for the treatment of many diseases, including bacterial infections. In the present study methanol, chloroform and aqueous extracts of Cassia auriculata leaf were subjected for antimicrobial activity by well-diffusion method against six bacterial strains namely Bacillus cereus, Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and Proteus mirabilis. The results revealed that the methanol and chloroform extracts exhibited strong inhibitory activity against all the tested organisms (zone of inhibition of 12-20 mm), except Pseudomonas aeruginosa (zone of inhibition 10 mm or nil). The aqueous extracts showed moderate activity by ‘Zone of inhibition ≤12 or nil). The extracts were screened for their phytochemical constituents by standard protocols’ and were shown to contain carbohydrates, proteins, alkaloids, flavonoids, steroids, saponins and tannins. The antibacterial activity of these extracts is possibly linked to the presence of flavonoids, steroid, saponins and/or tannins. Further studies are needed to determine the precise active principles from Cassia auriculata. PMID:23901174

  18. Evaluation of Antiplasmodial activity of extracts and constituents from Ampelozizyphus amazonicus

    PubMed Central

    do Carmo, Dominique F. M.; Amaral, Ana Claudia F.; Machado, Marta; Lopes, Dinora; Echevarria, Aurea; Rosário, Virgílio E.; Silva, Jefferson Rocha de A.

    2015-01-01

    Background: Ampelozizyphus amazonicus Ducke, a plant that is widely used by the population of the Amazonian region to prevent and treat malaria, was investigated in this work, which describes, for the first time, the antiplasmodial activity of its extracts and associates this activity with its isolated constituents. Methods: Different extracts with solvents of increasing polarity (hexane, chloroform, ethanol, and water) were obtained of the root bark. This procedure resulted in extracts that were characterized for their constituents. The cytotoxicity and activity of the extracts against Plasmodium berghei (schizontocidal activity, liver stage) and Plasmodium falciparum (3D7 and Dd2 strains, erythrocyte stage) were assessed in vitro. Results: Of the four extracts assayed against P. berghei, the chloroform extract showed the greatest activity, with an inhibitory concentration 50% (IC50) value of 30.1 µg/mL, followed by the aqueous extract (IC50 = 39.9 µg/mL). The chloroform extract exhibited the highest antiplasmodial activity in the erythrocyte stage of P. falciparum, with an IC50 value lower than 15 µg/mL. Fractionation of this more active extract led to the isolation and elucidation of pentacyclic triterpenes, lupeol, betulin and betulinic acid, which showed antiplasmodial activities with IC50 values ranging from 5.6 to 80.30 µM. The most active of these, betulinic acid, was further quantified in the extracts by high-performance liquid chromatography-photodiode array detector analyzes. The higher amount was found in the chloroform extract, which was the most active one against P. falciparum. Conclusion: The results obtained in this work may partly explain the popular intake of A. amazonicusas an antimalarial remedy in the Amazon region. PMID:26664012

  19. Anti-inflammation activities of essential oil and its constituents from indigenous cinnamon (Cinnamomum osmophloeum) twigs.

    PubMed

    Tung, Yu-Tang; Chua, Meng-Thong; Wang, Sheng-Yang; Chang, Shang-Tzen

    2008-06-01

    In this study, chemical compositions of hydrodistilled essential oil and anti-inflammatory activities from the twigs of Cinnamomum osmophloeum Kaneh. were investigated for the first time. The chemical constituents of the twig essential oil were further analyzed by GC-MS and they were found to be L-bornyl acetate (15.89%), caryophyllene oxide (12.98%), gamma-eudesmol (8.03%), beta-caryophyllene (6.60%), T-cadinol (5.49%), delta-cadinene (4.79%), trans-beta-elemenone (4.25%), cadalene (4.19%), and trans-cinnamaldehyde (4.07%). The effects of essential oil on nitric oxide (NO) and prostaglandin E2 (PGE2) production in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages were also examined. Results of nitric oxide tests indicated that twig essential oil and its major constituents such as trans-cinnamaldehyde, caryophyllene oxide, L-borneol, L-bornyl acetate, eugenol, beta-caryophyllene, E-nerolidol, and cinnamyl acetate have excellent activities. These findings demonstrated that essential oil of C. osmophloeum twigs have excellent anti-inflammatory activities and thus have great potential to be used as a source for natural health products.

  20. Chemical constituents and activities of the essential oil from Myristica fragrans against cigarette beetle Lasioderma serricorne.

    PubMed

    Du, Shu-Shan; Yang, Kai; Wang, Cheng-Fang; You, Chun-Xue; Geng, Zhu-Feng; Guo, Shan-Shan; Deng, Zhi-Wei; Liu, Zhi-Long

    2014-09-01

    Essential oil extracted from nutmeg seeds (Myristica fragrans Houtt.) by hydrodistillation was subjected to GC/MS and GC analysis. A total of 27 constituents were identified, of which eugenol (19.9%), methylisoeugenol (16.8%), methyleugenol (16.7%), sabinene (11.8%), and terpinen-4-ol (8.5%) were the major components. The essential oil was tested against Lasioderma serricorne for insecticidal and repellent activity, the LD50 value at the end of 24 h exposure period was 19.3 μg/adult. Six active compounds were isolated by bioassay-guided fractionation. They were identified as eugenol (1), methyleugenol (2), methylisoeugenol (3), elemicin (4), myristicin (5), and safrole (6). Among these isolates, 4 showed the strongest contact toxicity against L. serricorne adults with an LD50 value of 9.8 μg/adult. Repellency of crude oil and active compounds were also determined. Compounds 1, 2, 4, and 5 were strongly repellent against the cigarette beetle and exhibited the same level of repellency compared with the positive control, DEET. The results indicate that the essential oil of M. fragrans and its active constituents have potential for development as natural insecticides and repellents to control L. serricorne.

  1. Chemical constituents of Phragmanthera austroarabica A. G. Mill and J. A. Nyberg with potent antioxidant activity

    PubMed Central

    Badr, Jihan M.

    2015-01-01

    Background: Phragmanthera austroarabica A.G. Mill. and J. A. Nyberg is a semi parasitic plant belonging to family Loranthaceae. It was collected from Saudi Arabia. It is widely used in folk medicine among the kingdom in treatment of various diseases including diabetes mellitus. Objective: The total alcoholic extract of P. austroarabica collected from Saudi Arabia was investigated for the chemical structure and prominent biological activity of the main constituents. Materials and Methods: Isolation of the active constituents was performed using different chromatographic techniques including column chromatography packed with silica or sephadex and preparative thin layer chromatography. The structures of the isolated compounds were established based on different spectroscopic data as mass spectrum, one-dimensional and two-dimensional nuclear magnetic resonance (correlation spectroscopy, heteronuclear single quantum coherence, and heteronuclear multiple-bond correlation). Results: Phytochemical investigation of the plant resulted in isolation of 12 compounds. The isolated compounds were identified as chrysophanic acid, emodin, chrysophanic acid-8-O-glucoside, emodin-8-O-glucoside, pectolinarigenin, quercetin, dillenetin-3-O-glucoside, catechin, catechin-4’-O-gallate, methyl gallate, lupeol and ursolic acid. All the isolated phenolic compounds revealed significant free radical scavenging activities when tested using 2,2-diphenyl-1-picrylhydrazyl reagent. Conclusion: The antioxidant activities of the isolated compounds can justify the use of P. austroarabica in traditional medicine for treatment of diabetes and verify its possible application as an antihyperglycemic drug. PMID:26692747

  2. Antioxidant, larvicidal and antiacetylcholinesterase activities of cashew nut shell liquid constituents.

    PubMed

    Oliveira, Micheline Soares Costa; Morais, Selene Maia de; Magalhães, Davi Varela; Batista, Williams Pereira; Vieira, Icaro Gusmão Pinto; Craveiro, Afrânio Aragão; de Manezes, Jane Eire Silva Alencar; Carvalho, Ana Fontenelle Urano; de Lima, Glauber Pacelli Gomes

    2011-03-01

    Anacardic acid, cardanol and cardol, the main constituents of natural cashew nut shell liquid (CNSL), were obtained by solvent extraction and assayed for antioxidant, larvicidal and antiacetylcholinesterase activity. Their relative percent composition was obtained by HPLC analysis. Antioxidant activity was assessed using the DPPH and ABTS(+) tests, which showed cardanol as the most active, followed by cardol and anacardic acid. The three CNSL components demonstrated good larvicidal activity against Aedes aegypti (LC(50)=12.40 for anacardic acid, 10.22 for cardol and 14.45 for cardanol) and exhibited inhibition zones for acetylcholinesterase enzymes in the TLC test similar to carbachol, which was used as standard. Based on the results, these multipotent compounds represent promising agents in the control of Ae. aegypti, the main dengue vector in Brazil.

  3. Antidepressant-like activity of adhyperforin, a novel constituent of Hypericum perforatum L.

    PubMed

    Tian, Jingwei; Zhang, Fangxi; Cheng, Jucan; Guo, Shuren; Liu, Pinglan; Wang, Hongbo

    2014-07-09

    Adhyperforin is a novel constituent of Hypericum perforatum L., but its antidepressant-like activity remains unclear. To explore that, several well-validated animal models of depression as well as neurotransmitter reuptake and transporter binding assays were conducted. The results showed adhyperforin could reduce the immobility time of mice in the forced swimming test and tail suspension assay, antagonize the behaviors induced by reserpine, and have no effect on locomotor activity. Furthermore, following establishment of a chronic unpredictable mild stress model, adhyperforin increased the number of crossings and rearings in rats in the open field test and increased the sucrose consumption. Finally, adhyperforin inhibited uptake of serotonin, norepinephrine, and dopamine, and displayed robust binding affinities for the serotonin and norepinephrine transporters. Overall, the current study provides the first evidence that adhyperforin is a novel, active ingredient of Hypericum perforatum L. with robust antidepressant-like activity.

  4. Neurite outgrowth-promoting active constituents of the Japanese cypress (Chamaecyparis obtusa).

    PubMed

    Kuroyanagi, Masanori; Ikeda, Ryuya; Gao, Hui Yuan; Muto, Norio; Otaki, Keisuke; Sano, Toshikazu; Kawahara, Nobuo; Nakane, Takahisa

    2008-01-01

    In the screening of biologically active constituents from woody plants, the methanol extract of leaves of Chamaecyparis obtusa showed potent neurite outgrowth-promoting activity in neuronal PC12 cells. The ethyl acetate-soluble fraction of the methanol extract showed potent activity and was separated by means of various chromatographic methods to give the two new compounds 1 and 2, as well as 11 known lignan and sesquiterpene derivatives. The structures of the new compounds were determined to be 9-O-acetyldihydrosesamin (1) and 9-O-(11-hydroxyeudesman-4-yl)dihydrosesamin (2), respectively, in NMR studies including 2D-NMR experiments. Of the 13 compounds, the known compound hinokinin (5) and the new compound 2 showed potent neurite outgrowth-promoting activity in PC 12 cells.

  5. Quantification of phenolic constituents and antioxidant activity of Pterodon emarginatus vogel seeds.

    PubMed

    Dutra, Rafael C; Leite, Magda N; Barbosa, Nádia R

    2008-04-01

    In the present study the phenolic (Folin-Dennis) and flavonoid (colorimetric assay) constituents and the antioxidant activity of Pterodon emarginatus seeds were investigated in several samples prepared with different extraction procedures: essential oil (EO) using a Clevenger-type apparatus; hexanic (HF), ethyl acetate (EAF), buthanolic (BF) and methanolic (MF) fractions using Soxhlet extraction, and extracts (1 g/extract) obtained from different methods: reflux 80 degrees C/30 min, ultrasound/30 min, static maceration/48 h and heating plate 100 degrees C/45 min. These extracts were prepared using water or ethanol/water at 30:70 v/v, 50:50 v/v or 70:30 v/v. Antioxidant activity [2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH)] was tested only in the fractions obtained from Soxhlet extraction. The extract obtained from reflux using ethanol/water (70:30, v/v) showed the highest phenolic constituents level. The EAF, BF and MF showed DPPH scavenging activities with IC(50)=163.22, 18.89 and 10.15 microg/ml, respectively.

  6. Fractionation and identification of minor and aroma-active constituents in Kangra orthodox black tea.

    PubMed

    Joshi, Robin; Gulati, Ashu

    2015-01-15

    The aroma constituents of Kangra orthodox black tea were isolated by simultaneous distillation extraction (SDE), supercritical fluid extraction and beverage method. The aroma-active compounds were identified using gas chromatography-olfactometry-mass spectrometry. Geraniol, linalool, (Z/E)-linalool oxides, (E)-2-hexenal, phytol, β-ionone, hotrienol, methylpyrazine and methyl salicylate were major volatile constituents in all the extracts. Minor volatile compounds in all the extracts were 2-ethyl-5-methylpyrazine, ethylpyrazine, 2-6,10,14-trimethyl-2-pentadecanone, acetylfuran, hexanoic acid, dihydroactinidiolide and (E/Z)-2,6-nonadienal. The concentrated SDE extract was fractionated into acidic, basic, water-soluble and neutral fractions. The neutral fraction was further chromatographed on a packed silica gel column eluted with pentane and diethyl ether to separate minor compounds. The aroma-active compounds identified using gas chromatography-olfactometry-mass spectrometry were 2-amylfuran, (E/Z)-2,6-nonadienal, 1-pentanol, epoxylinalool, (Z)-jasmone, 2-acetylpyrrole, farnesyl acetone, geranyl acetone, cadinol, cubenol and dihydroactinidiolide. AEDA studies showed 2-hexenal, 3-hexenol, ethylpyrazine, (Z/E)-linalool oxides, linalool, (E/Z)-2,6-nonadienal, geraniol, phenylethanol, β-ionone, hotrienol and dihydroactinidiolide to be odour active components.

  7. Quantification of Phenolic Constituents and Antioxidant Activity of Pterodon emarginatus Vogel Seeds

    PubMed Central

    Dutra, Rafael C.; Leite, Magda N.; Barbosa, Nádia R.

    2008-01-01

    In the present study the phenolic (Folin-Dennis) and flavonoid (colorimetric assay) constituents and the antioxidant activity of Pterodon emarginatus seeds were investigated in several samples prepared with different extraction procedures: essential oil (EO) using a Clevenger-type apparatus; hexanic (HF), ethyl acetate (EAF), buthanolic (BF) and methanolic (MF) fractions using Soxhlet extraction, and extracts (1 g/extract) obtained from different methods: reflux 80°C/30 min, ultrasound/30 min, static maceration/48 h and heating plate 100°C/45 min. These extracts were prepared using water or ethanol/water at 30:70 v/v, 50:50 v/v or 70:30 v/v. Antioxidant activity [2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH)] was tested only in the fractions obtained from Soxhlet extraction. The extract obtained from reflux using ethanol/water (70:30, v/v) showed the highest phenolic constituents level. The EAF, BF and MF showed DPPH scavenging activities with IC50=163.22, 18.89 and 10.15 μg/ml, respectively. PMID:19325773

  8. Computer-Guided Approach to Access the Anti-influenza Activity of Licorice Constituents

    PubMed Central

    2013-01-01

    Neuraminidase (NA), a key enzyme in viral replication, is the first-line drug target to combat influenza. On the basis of a shape-focused virtual screening, the roots of Glycyrrhiza glabra (licorice) were identified as plant species with an accumulation of constituents that show 3D similarities to known influenza NA inhibitors (NAIs). Phytochemical investigation revealed 12 constituents identified as (E)-1-[2,4-dihydroxy-3-(3-methyl-2-butenyl)phenyl]-3-(8-hydroxy-2,2-dimethyl-2H-1-benzopyran-6-yl)-2-propen-1-one (1), 3,4-dihydro-8,8-dimethyl-2H,8H-benzo[1,2-b:3,4-b′]dipyran-3-ol (2), biochanin B (3), glabrol (4), glabrone (5), hispaglabridin B (6), licoflavone B (7), licorice glycoside B (8), licorice glycoside E (9), liquiritigenin (10), liquiritin (11), and prunin (12). Eleven of these constituents showed significant influenza virus NA inhibition in a chemiluminescence (CL)-based assay. Additional tests, including (i) a cell-based cytopathic effect inhibition assay (general antiviral activity), (ii) the evaluation of cytotoxicity, (iii) the inhibition of the NA of Clostridium perfringens (CL- and fluorescence (FL)-based assay), and (iv) the determination of self-fluorescence and quenching, provided further perspective on their anti-influenza virus potential, revealing possible assay interference problems and false-positive results. Compounds 1, 3, 5, and 6 showed antiviral activity, most likely caused by the inhibition of NA. Of these, compounds 1, 3, and 6 were highly ranked in shape-focused virtual screening. PMID:24313801

  9. Filterable redox cycling activity: a comparison between diesel exhaust particles and secondary organic aerosol constituents.

    PubMed

    McWhinney, Robert D; Badali, Kaitlin; Liggio, John; Li, Shao-Meng; Abbatt, Jonathan P D

    2013-04-02

    The redox activity of diesel exhaust particles (DEP) collected from a light-duty diesel passenger car engine was examined using the dithiothreitol (DTT) assay. DEP was highly redox-active, causing DTT to decay at a rate of 23-61 pmol min(-1) μg(-1) of particle used in the assay, which was an order of magnitude higher than ambient coarse and fine particulate matter (PM) collected from downtown Toronto. Only 2-11% of the redox activity was in the water-soluble portion, while the remainder occurred at the black carbon surface. This is in contrast to redox-active secondary organic aerosol constituents, in which upward of 90% of the activity occurs in the water-soluble fraction. The redox activity of DEP is not extractable by moderately polar (methanol) and nonpolar (dichloromethane) organic solvents, and is hypothesized to arise from redox-active moieties contiguous with the black carbon portion of the particles. These measurements illustrate that "Filterable Redox Cycling Activity" may therefore be useful to distinguish black carbon-based oxidative capacity from water-soluble organic-based activity. The difference in chemical environment leading to redox activity highlights the need to further examine the relationship between activity in the DTT assay and toxicology measurements across particles of different origins and composition.

  10. Effects of the active constituents of Crocus sativus L., crocins, in an animal model of anxiety.

    PubMed

    Pitsikas, N; Boultadakis, A; Georgiadou, G; Tarantilis, P A; Sakellaridis, N

    2008-12-01

    Crocus sativus L. is a plant cultivated in various parts of the world. Crocins are among the active components of Crocus sativus L. The present study was designed to investigate in the rat whether or not crocins possess anxiolytic properties. For this aim, the light/dark test was selected. Either crocins, at a dose which did not influence animals' motor activity (50mg/kg), or diazepam (1.5 mg/kg), significantly increased the latency to enter the dark compartment and prolonged the time spent in the lit chamber in the rats. Conversely, lower doses of crocins (15-30 mg/kg) did not substantially modify animals' behaviour. The present results indicate that treatment with these active constituents of Crocus sativus L. induce anxiolytic-like effects in the rat.

  11. Phenolic constituents from the aerial parts of Glycyrrhiza inflata and their antibacterial activities.

    PubMed

    Zhou, Biao; Wan, Chuan-Xing

    2015-01-01

    Chemical investigation on 90% ethanol extracts of the aerial parts of Glycyrrhiza inflata afforded two new phenolic constituents, 2-(3-methyl-2-butenyl)-3,5,4'-trihydroxy-bibenzyl (1) and (2S)-6-[(E)-3-hydroxymethyl-2-butenyl]-3',4',5,7-tetrahydroxy-dihydroflavanone (2) along with seven known dihydroflavanones (3-9). Compounds 1-9 were tested for their minimum inhibitory concentration (MIC) values of inhibiting Staphylococcus aureus and Staphylococcus epidermidis. Compound 1 showed moderate antibacterial activities against both S. aureus (MIC of 50.00 μg/ml) and S. epidermidis (MIC of 12.50 μg/ml). The analysis of structure-activity relationships revealed that the antibacterial activity of dihydroflavanones (2-9) was significantly affected by the position of prenyl group.

  12. Chemical constituents, antioxidant and antimocrobial activity of essential oil of Pogostemon paniculatus (Willd.).

    PubMed

    Manoj, Godbole; Manohar, Shiragambi Hanumantagouda; Murthy, Hosakatte Niranjana

    2012-01-01

    The essential oil extracted from the leaves of Pogostemon paniculatus (Willd.) Benth. (Lamiaceae), was analysed by gas chromatography-mass spectrometry (GC-MS). Nineteen compounds constituting 85.36% of the total oil were identified in the oil. Patchouli alcohol (30.65%), α-guaiene (10.67%), β-guaiene (9.09%), caryophyllene (8.64%), eicosene (5.27%) were the major constituents present. The essential oil was analysed for antimicrobial activity by disc diffusion assay and minimum inhibition concentration against six bacteria and three fungi. Results showed inhibitory activity against some of the tested microorganisms. The essential oil was also tested for the DPPH free-radical scavenging activity and had an inhibitory concentration (IC(50)) value of 18.5 µg mL(-1).

  13. [Advances in research of chemical constituents and pharmacological activities of common used spices].

    PubMed

    Sun, Chao-nan; Zhu, Yuan; Xu, Xi-ming; Yu, Jiang-nan

    2014-11-01

    Spices have enjoyed a long history and a worldwide application. Of particular interest is the pharmaceutical value of spices in addition to its basic seasoning function in cooking. Concretely, equipped with complex chemical compositions, spices are of significant importance in pharmacologic actions, like antioxidant, antibacterial, antitumor, as well as therapeutical effects in gastrointestinal disorders and cardiovascular disease. Although increasing evidences in support of its distinct role in the medical field has recently reported, little information is available for substantive, thorough and sophisticated researches on its chemical constituents and pharmacological activities, especially mechanism of these actions. Therefore, in popular wave of studies directed at a single spice, this review presents systematic studies on the chemical constituents and pharmacological activities associated with common used spices, together with current typical individual studies on functional mechanism, in order to pave the way for the exploitation and development of new medicines derived from the chemical compounds of spice (such as, piperine, curcumin, geniposide, cinnamaldehyde, cinnamic acid, linalool, estragole, perillaldehyde, syringic acid, crocin).

  14. Chemical Constituents from the Fruits of Forsythia suspensa and Their Antimicrobial Activity

    PubMed Central

    Chen, Guo-Feng; Yang, Mei-Lin; Lin, Ya-Hua; Peng, Chi-Chung

    2014-01-01

    Lignans and phenylethanoid glycosides purified from Forsythia suspensa were reported to display various bioactivities in the previous literature, including the antimicrobial activity. Therefore, the present research is aimed to purify and identify the chemical constituents of the methanol extracts of fruits of F. suspensa. The methanol extracts of fruits of F. suspensa were fractionated and further purified with the assistance of column chromatography to afford totally thirty-four compounds. Among these isolates, 3β-acetoxy-20α-hydroxyursan-28-oic acid (1) was reported from the natural sources for the first time. Some of the purified principles were subjected to the antimicrobial activity examinations against Escherichia coli to explore new natural lead compounds. PMID:24745011

  15. Calamintha nepeta (L.) Savi and its Main Essential Oil Constituent Pulegone: Biological Activities and Chemistry.

    PubMed

    Božović, Mijat; Ragno, Rino

    2017-02-14

    Medicinal plants play an important role in the treatment of a wide range of diseases, even if their chemical constituents are not always completely recognized. Observations on their use and efficacy significantly contribute to the disclosure of their therapeutic properties. Calamintha nepeta (L.) Savi is an aromatic herb with a mint-oregano flavor, used in the Mediterranean areas as a traditional medicine. It has an extensive range of biological activities, including antimicrobial, antioxidant and anti-inflammatory, as well as anti-ulcer and insecticidal properties. This study aims to review the scientific findings and research reported to date on Calamintha nepeta (L.) Savi that prove many of the remarkable various biological actions, effects and some uses of this species as a source of bioactive natural compounds. On the other hand, pulegone, the major chemical constituent of Calamintha nepeta (L.) Savi essential oil, has been reported to exhibit numerous bioactivities in cells and animals. Thus, this integrated overview also surveys and interprets the present knowledge of chemistry and analysis of this oxygenated monoterpene, as well as its beneficial bioactivities. Areas for future research are suggested.

  16. Comparison of Essential Oil Content, Constituents, and Antioxidant Activity of Nepeta Glomerulosa during Three Developmental Stages

    NASA Astrophysics Data System (ADS)

    Moradi, H.; Azizi, M.; Rowshan, V.

    2014-12-01

    The genus Nepeta with the common Persian name "Pune-Sa" is one of the most important genera of Lamiaceae family. More than 250 species in the world and 67 annual or perennial species in Iran have been reported. Some of these species are valuable in medicine and are used for medicinal purposes. The aim of this study was to identify essential oil content, its chemical composition, and antioxidant activity in the N. glomerulosa during vegetative, flowering and seed set stages. The samples of N. glomerulosa in the three above-mentioned stages were collected from Abade region of Fars Province. The essential oil was obtained though hydrodistillation and was analyzed by GC and GC/MS. Essential oil of the plant in vegetative, flowering and seed set stages were measured to be 55, 53 and 53 components, respectively, with geranyl acetate (16.644%, 18.182% and 24.441%), geraniol (10.797%, 11.372% and 12.389%), caryophyllene oxide (8.302%, 10.515% and 6.661%), humulene epoxide ΙΙ (7.974%, 7.112% and 2.587%), α-pinene (4.743%, 4.126% and 6.724%), limonene (4.086%, 3.848% and 4.711%) and 1,8-cineol (3.397%, 4.609% and 3.759%) being the major components of the essential oil. The results confirmed that phonological stages have a significant effect on essential oils constituents. Geranyl acetate and geraniol increased by development of plant from vegetative to seed set stage and geranyl acetate was the main essential oils constituent of the plants throughout the three phonological stages. Antioxidant activity in flowering and seed set stages was significantly higher than vegetative stage, but compared with Gallic acid, which is a very strong antioxidant substance, had insignificant antioxidant activity.

  17. Anti-inflammatory and free radial scavenging activities of the constituents isolated from Machilus zuihoensis.

    PubMed

    Mao, Yi-Wen; Tseng, Hsiang-Wen; Liang, Wen-Li; Chen, Ih-Sheng; Chen, Shui-Tein; Lee, Mei-Hsien

    2011-11-10

    A new biflavonol glycoside, quercetin-3-O-β-D-glucopyranoside-(3'→O-3''')-quercetin-3-O-β-D-galactopyranoside (9), together with eight known compounds was isolated for the first time from the leaves of Machilus zuihoensis Hayata (Lauraceae). The structure of compound 9 was elucidated by various types of spectroscopic data analysis. Analysis of the biological activity assay found that compound 9 showed significant superoxide anion scavenging activity (IC₅₀ is 30.4 μM) and markedly suppressed LPS-induced high mobility group box 1 (HMGB-1) protein secretion in RAW264.7 cells. In addition, the HMGB-1 protein secretion was also inhibited by quercitrin (3), ethyl caffeate (6), and ethyl 3-O-caffeoylquinate (7) treatment. In the LPS-stimulated inducible nitric oxide synthase (iNOS) activation analysis, two known compounds, quercetin (1) and ethyl caffeate (6), were found to markedly suppress nitric oxide (NO) production (IC₅₀ value, 27.6 and 42.9 μM, respectively) in RAW264.7 cells. Additionally, it was determined that ethyl caffeate (6) down-regulated mRNA expressions of iNOS, IL-1β, and IL-10 in the LPS-treatment of RAW264.7 cells via a suppressed NF-kB pathway. These results suggested for the first time that the new compound 9 and other constituents isolated from M. zuihoensis have potential anti-inflammatory and superoxide anion scavenging effects. These constituents may be useful for treating various inflammatory diseases.

  18. Hydrophobic constituents and their potential anticancer activities from Devil’s Club Oplopanax horridus

    PubMed Central

    Sun, Shi; Du, Guang-Jian; Qi, Lian-Wen; Williams, Stainley; Wang, Chong-Zhi; Yuan, Chun-Su

    2011-01-01

    Ethnopharmacological relevance Devil’s Club Oplopanax horridus (Sm.) Miq. is a widely used folk medicine in the Pacific Northwest such as Alaska and British Columbia for treating a variety of ailments including arthritis, cold, fever, infections, diabetes and cancer. Aim of the study To investigate hydrophobic constituents and their potential anticancer activity from Devil’s Club O. horridus. Materials and methods The root bark of O. horridus (Sm.) Miq was isolated by chromatographic techniques. Structures of isolated compounds were identified by spectroscopic methods and comparison with published data. The anti-proliferation of isolated hydrophobic constituents in human breast cancer MCF-7 cells, human colon cancer SW-480 and HCT-116 cells were tested. The potential mechanism of anti-proliferation was also investigated using cell cycle and apoptosis assays. Results and discussion Six compounds were isolated and structurally identified as 9,17-octadecadiene-12,14-diyne-1,11,16-triol, 1-acetate (1), oplopandiol acetate (2), falcarindiol (3), oplopandiol (4), trans-nerolidol (5) and t-cadinol (6). These compounds showed potential anticancer activities on human breast cancer and colon cancer cells, of which compound 3 possesses the strongest activity. Further cell cycle and apoptosis test by flow cytometry showed the polyacetylenes 1–4 induced HCT-116 cell arresting in G2/M phase and inhibited proliferation by the induction of apoptosis at both earlier and later stage. Conclusion These results provide promising baseline information for the potential use of O. horridus as well as some of the isolated compounds in the treatment of cancer. PMID:20723598

  19. Engineers and Active Responsibility.

    PubMed

    Pesch, Udo

    2015-08-01

    Knowing that technologies are inherently value-laden and systemically interwoven with society, the question is how individual engineers can take up the challenge of accepting the responsibility for their work? This paper will argue that engineers have no institutional structure at the level of society that allows them to recognize, reflect upon, and actively integrate the value-laden character of their designs. Instead, engineers have to tap on the different institutional realms of market, science, and state, making their work a 'hybrid' activity combining elements from the different institutional realms. To deal with this institutional hybridity, engineers develop routines and heuristics in their professional network, which do not allow societal values to be expressed in a satisfactory manner. To allow forms of 'active' responsibility, there have to be so-called 'accountability forums' that guide moral reflections of individual actors. The paper will subsequently look at the methodologies of value-sensitive design (VSD) and constructive technology assessment (CTA) and explore whether and how these methodologies allow engineers to integrate societal values into the design technological artifacts and systems. As VSD and CTA are methodologies that look at the process of technological design, whereas the focus of this paper is on the designer, they can only be used indirectly, namely as frameworks which help to identify the contours of a framework for active responsibility of engineers.

  20. In vitro effects of standardized extract of Bacopa monniera and its five individual active constituents on human P-glycoprotein activity.

    PubMed

    Singh, Rajbir; Rachumallu, Ramakrishna; Bhateria, Manisha; Panduri, Jagadeesh; Bhatta, Rabi Sankar

    2015-01-01

    1. For centuries Bacopa monniera (BM) has been used as an herbal drug for the treatment of various mental ailments. A chemically standardized alcoholic extract of BM is clinically available over the counter herbal remedy for memory enhancement in children and adults. Consumption of herbal preparations has been reported to alter the function of membrane transporters, especially P-glycoprotein (P-gp), ATP-dependent drug efflux transporter responsible for the development of herb-drug interactions. 2. In the present study, we evaluated the in vitro effect of BM extract and its five individual active constituents (namely, bacopaside I, bacopaside II and bacopasaponin C, bacoside A and bacoside A3) on P-gp function using luminescent P-gp ATPase assay and Rh123 transport assay across human MDR1 gene transfected LLC-GA5-COL150 cell line. 3. It was observed that BM extract and its five individual constituents inhibited both basal activity as well as verapamil-stimulated ATPase activity, suggesting their affinity towards P-gp. Further, BM and its five active constituents inhibited the rhodamine 123 (Rh123) transport across LLC-GA5-COL150 cell monolayer with bacopaside II being the most potent inhibitor of P-gp, which decreased P-gp efflux ratio of Rh123 by fourfold in comparison to control. 4. Our finding may prove beneficial in predicting the potential herb-drug interactions of BM on concomitant medication with P-gp substrate drugs in clinical settings.

  1. Evaluation of antioxidant activity of vetiver (Vetiveria zizanioides L.) oil and identification of its antioxidant constituents.

    PubMed

    Kim, Hyun-Jin; Chen, Feng; Wang, Xi; Chung, Hau Yin; Jin, Zhengyu

    2005-10-05

    Antioxidant capacities of vetiver (Vetiveria zizanioides) oil were evaluated by two different in vitro assays: the DPPH* free radical scavenging assay and the Fe2+-metal chelating assay. Results showed that the vetiver oil (VO) possessed a strong free radical scavenging activity when compared to standard antioxidants such as butylated hydroxytoluene (BHT) and alpha-tocopherol. However, its metal chelating capacity was relatively weak. VO (10 microL/mL) dissolved in methanol exhibited approximately 93% free radical scavenging activity in the DPPH* assay and approximately 34% Fe2+ chelating activity in the metal chelating assay. By contrast, 10 mM BHT and 0.1 mM alpha-tocopherol exhibited 93 and 89% free radical scavenging activities in the DPPH* assay, respectively, and 1 mM EDTA exhibited approximately 97% activity in the metal chelating assay. Among the complex constituents in the crude VO, beta-vetivenene, beta-vetivone, and alpha-vetivone, which had shown strong antioxidant activities, were isolated and identified using various chromatographic techniques including silica gel open column chromatography, silica HPLC, and GC-MS. These results show that VO and some of its inherent components can be potential alternative natural antioxidants.

  2. Chemical Constituents and Antimicrobial Activity of Indian Green Leafy Vegetable Cardiospermum halicacabum.

    PubMed

    Jeyadevi, R; Sivasudha, T; Ilavarasi, A; Thajuddin, N

    2013-06-01

    The present study was carried out to analyze chemical constituents and antibacterial activity of ethanolic leaf extract of Cardiospermum halicacabum (ECH). The FT-IR spectrum confirmed the presence of alcohols, phenols, alkanes, alkynes, aliphatic ester and flavonoids in ECH. The GC-MS analysis revealed that ECH contained about twenty four compounds. The major chemical compounds identified were cyclohexane-1, 4, 5-triol-3-one-1-carboxylic acid, benzene acetic acid, caryophyllene, phytol and neophytadiene. The ECH was screened for its antibacterial activity against different bacterial strains and anti fungal activity against Candida albicans by agar well diffusion and minimum inhibitory concentration (MIC) assay. ECH exhibited antibacterial and antifungal activity. All the tested bacterial strains showed MIC values ranging from 80 to 125 μg of extract/ml and C. albicans showed 190 μg of extract/ml as a MIC. The maximum activity ECH was observed against human pathogen Staphylococcus aureus followed by Escherichia coli and the fish pathogen Aeromonas hydrophila. ECH exhibited moderate activity against some of the tested multidrug resistant strains.

  3. Nitrogen-Containing Constituents of Black Cohosh: Chemistry, Structure Elucidation, and Biological Activities

    PubMed Central

    Lankin, David C.; Cisowska, Tamara; Chen, Shao-Nong; Pauli, Guido F.; van Breemen, Richard B.

    2016-01-01

    The roots/rhizomes of black cohosh (Actaea racemosa L. syn. Cimicifuga racemosa [L]. Nutt., Ranunculaceae) have been used traditionally by Native Americans to treat colds, rheumatism, and a variety of conditions related to women’s health. In recent years black cohosh preparations have become popular dietary supplements among women seeking alternative treatments for menopausal complaints. The popularity of the plant has led to extensive phytochemical and biological investigations, including several clinical trials. Most of the phytochemical and biological research has focused on two abundant classes of compounds: the triterpene glycosides and phenolic acids. A third group of phytoconstituents that has received far less attention consists of the alkaloids and related compounds that contain nitrogen. This chapter summarizes the current state of knowledge of the chemistry and biological activities associated with this group of constituents and provides some perspective on their significance for future research on this interesting plant. PMID:27795590

  4. Chemical Constituents of the Culture Broth of Phellinus linteus and Their Antioxidant Activity.

    PubMed

    Lee, Myeong-Seok; Hwang, Byung Soon; Lee, In-Kyoung; Seo, Geon-Sik; Yun, Bong-Sik

    2015-03-01

    The medicinal fungus Phellinus linteus, in the family Hymenochaetaceae, has been used as a traditional medicine for the treatment of various diseases. In this study, the chemical constituents of the culture broth of P. linteus were investigated. P. linteus was cultured in potato dextrose broth medium, and the culture broth was extracted with ethyl acetate. The ethyl acetate-soluble portion was concentrated and subjected to ODS column chromatography, followed by Sephadex LH-20 column chromatography. Six compounds (1~6) were purified by preparative reversed-phase high-performance liquid chromatography. Spectroscopic methods identified their structures as caffeic acid (1), inotilone (2), 4-(3,4-dihydroxyphenyl)-3-buten-2-one (3), phellilane H (4), (2E,4E)-(+)-4'-hydroxy-γ-ionylideneacetic acid (5), and (2E,4E)-γ-ionylideneacetic acid (6). Compounds 1, 2, and 3 exhibited potent dose-dependent antioxidant activity.

  5. Influence of harvest season on antioxidant activity and constituents of rabbiteye blueberry ( Vaccinium ashei ) leaves.

    PubMed

    Zhu, Liancai; Liu, Xi; Tan, Jun; Wang, Bochu

    2013-11-27

    To select rabbiteye blueberry leaves from an appropriate harvest season to develop functional foods, this paper studied the bioactive secondary metabolites and the antioxidant capacity of rabbiteye blueberry leaves from May, September, and November. The results showed the leaves from May had the highest content of total flavonoids (114.21 mg/g) and the leaves from November had the highest content of total polyphenols and proanthocyanidins (425.24 and 243.29 mg/g, respectively). It was further found that blueberry leaves from different seasons have similar bioactive constituents, but their contents are obviously different by HPLC. The rabbiteye blueberry leaves from November had the highest antioxidant capacity, which was well correlated with their highest proanthocyanidin content. The results clarify that the blueberry leaves from different seasons have different contents of bioactive secondary metabolites and different antioxidant activities, which implied that leaves from November should be selected first for utilization in functional foods.

  6. Chemical Constituents of the Culture Broth of Phellinus linteus and Their Antioxidant Activity

    PubMed Central

    Lee, Myeong-Seok; Hwang, Byung Soon; Lee, In-Kyoung; Seo, Geon-Sik

    2015-01-01

    The medicinal fungus Phellinus linteus, in the family Hymenochaetaceae, has been used as a traditional medicine for the treatment of various diseases. In this study, the chemical constituents of the culture broth of P. linteus were investigated. P. linteus was cultured in potato dextrose broth medium, and the culture broth was extracted with ethyl acetate. The ethyl acetate-soluble portion was concentrated and subjected to ODS column chromatography, followed by Sephadex LH-20 column chromatography. Six compounds (1~6) were purified by preparative reversed-phase high-performance liquid chromatography. Spectroscopic methods identified their structures as caffeic acid (1), inotilone (2), 4-(3,4-dihydroxyphenyl)-3-buten-2-one (3), phellilane H (4), (2E,4E)-(+)-4'-hydroxy-γ-ionylideneacetic acid (5), and (2E,4E)-γ-ionylideneacetic acid (6). Compounds 1, 2, and 3 exhibited potent dose-dependent antioxidant activity. PMID:25892914

  7. Influence of sulfur fumigation on the chemical constituents and antioxidant activity of buds of Lonicera japonica.

    PubMed

    Guo, Ai-Li; Chen, Liang-Mian; Wang, Yan-Min; Liu, Xiao-Qian; Zhang, Qi-Wei; Gao, Hui-Min; Wang, Zhi-Min; Xiao, Wei; Wang, Zhen-Zhong

    2014-10-15

    Lonicera japonica flos is widely used as a pharmaceutical resource and a commonly-employed ingredient in healthy food, soft beverages and cosmetics in China. Sometimes, sulfur fumigation is used during post-harvest handling. In this study, a comprehensive comparison of the chemical profile between sun-dried and sulfur-fumigated samples was conducted by HPLC fingerprints and simultaneous quantification of nine constituents, including secologanic acid, along with another eight usually-analyzed markers. Secologanic acid was destroyed, and its sulfonates were generated, whereas caffeoylquinic acids were protected from being oxidized. The residual sulfur dioxide in sulfur-fumigated samples was significantly higher than that in sun-dried samples, which might increase the potential incidence of toxicity to humans. Meanwhile, compared with sun-dried samples, sulfur-fumigated samples have significantly stronger antioxidant activity, which could be attributed to the joint effect of protected phenolic acids and flavonoids, as well as newly-generated iridoid sulfonates.

  8. Phenolic constituents in the fruits of Cinnamomum zeylanicum and their antioxidant activity.

    PubMed

    Jayaprakasha, G K; Ohnishi-Kameyama, Mayumi; Ono, Hiroshi; Yoshida, Mitsuru; Jaganmohan Rao, L

    2006-03-08

    Defatted cinnamon fruit powder was successively extracted with benzene ethyl acetate, acetone, MeOH, and water. The concentrated water extract contained the maximum amount of phenolics and showed the highest antioxidant activities. Hence, it was fractionated by Diaion HP-20SS, Diaion HP-20, and Sephadex LH-20 column chromatographies. It gave five purified compounds, the purities of which were analyzed by HPLC. Compounds 1-5 were identified as 3,4-dihydroxybenzoic acid (protocatechuic acid), epicatechin-(2beta-->O-7,4beta-->8)-epicatechin-(4beta-->8)-epicatechin (cinnamtannin B-1), 4-[2,3-dihydro-3-(hydroxymethyl)-5-(3-hydroxypropyl)-7-(methoxy)benzofuranyl]-2-methoxyphenyl beta-d-glucopyranoside (urolignoside), quercetin-3-O-(6-O-alpha-l-rhamnopyranosyl)-beta-d-glucopyranoside (rutin), and quercetin-3-O-alpha-l-rhamnopyranoside by using extensive spectral studies. The antioxidant activities of purified compounds were screened for their antioxidative potential using beta-carotene-linoleate and 1,1-diphenyl-2-picrylhydrazyl model systems. All of the compounds showed antioxidant and radical scavenging activities. This is the first report of the isolation and identification of nonvolatile constituents and as well as antioxidant activities from cinnamon fruits.

  9. Anti-inflammatory and analgesic activities of Edgeworthia chrysantha and its effective chemical constituents.

    PubMed

    Hu, Xiao-Jia; Jin, Hui-Zi; Xu, Wen-Zheng; Chen, Ming; Liu, Xiao-Hua; Zhang, Wei; Su, Juan; Zhang, Chuan; Zhang, Wei-Dong

    2008-09-01

    The barks and roots of Edgeworthia chrysantha LINDL., which have been used as the folk medicine "Zhu shima" in southern China due to their detumescence and acesodyne effects, were investigated for their anti-inflammatory and analgesic activities using a xylene-induced ear edema assay in mice and Freund's complete adjuvant-induced paw edema as inflammation models, and the acetic acid-induced writhing test as an analgesic model. Fractions effective in terms of anti-inflammatory and analgesic activities were obtained from E. chrysantha. The chloroform-soluble fraction (CHF) showed significant anti-inflammatory (p<0.01-0.001) and analgesic (p<0.01) effects. On further purification by silica gel, three major coumarins, edgeworin (EdN), edgeworosides A and C (EdeA and EdeC), were isolated from the chloroform fraction and both anti-inflammatory and analgesic activities were evaluated. EdN and EdeA had anti-inflammatory (p<0.05-0.01) and analgesic (p<0.001) effects, while EdeC only showed an analgesic effect. The results of this study thus demonstrated that the coumarins EdN, EdeA and EdeC in this plant may be active constituents that contribute to the anti-inflammatory and analgesic effects.

  10. Isolation and identification of chemical constituents from the bacterium Bacillus sp. and their nematicidal activities.

    PubMed

    Zeng, Liming; Jin, Hui; Lu, Dengxue; Yang, Xiaoyan; Pan, Le; Cui, Haiyan; He, Xiaofeng; Qiu, Hongdeng; Qin, Bo

    2015-10-01

    A strain SMrs28 was isolated from the rhizosphere soil of a toxic plant Stellera chamaejasme and identified as Bacillus sp. on the basis of morphological and partial 16S rRNA gene sequence analysis. The crude extract of SMrs28 fermentation broth showed strong nematocidal activities in preliminary test. To define the active nematocidal metabolites of SMrs28, a novel compound (1), 4-oxabicyclo[3.2.2]nona-1(7), 5,8-triene, along with five known compounds (2-6), were isolated from the strain by various column chromatographic techniques and characterized on the basis of spectroscopic analysis. Results of the in vitro nematicidal tests showed that the metabolites presented different levels of activity at certain exposure conditions. Compounds (1-3) displayed LC50 values of 904.12, 451.26, 232.98 µg/ml and 1594.0, 366.62, 206.38 µg/ml against Bursaphelenchus xylophilus and Ditylenchus destructor at 72 h, respectively. This is the first report of the nematicidal activity of the compounds as constituents of Bacillus sp.. Our findings help to find potential chemical structures to develop nematicides from microbial source for the management of nematode-infected plant diseases.

  11. Season-controlled changes in biochemical constituents and oxidase enzyme activities in tomato (Lycopersicon esculentum Mill.).

    PubMed

    Sen, Supatra; Mukherji, S

    2009-07-01

    Season-controlled changes in biochemical constituents viz. carotenoids (carotene and xanthophyll) and pectic substances along with IAA-oxidase and polyphenol oxidase (PPO) enzyme activities were estimated/assayed in leaves of Lycopersicon esculentum Mill. (tomato) in two developmental stages--pre-flowering (35 days after sowing) and post-flowering (75 days after sowing) in three different seasons--summer rainy and winter Carotenoid content along with pectic substances were highest in winter and declined significantly in summer followed by rainy i.e. winter > summer > rainy. Carotenoid content was significantly higher in the pre-flowering as compared to post-flowering in all three seasons while pectic substances increased in the post-flowering as compared to pre-flowering throughout the annual cycle. IAA oxidase and PPO enzyme activities were enhanced in rainy and decreased sharply in summer and winter i.e. rainy > summer > winter. Both the enzymes exhibited higher activity in the post-flowering stage as compared to pre-flowering in all three seasons. These results indicate winter to be the most favourable season for tomato plants while rainy season environmental conditions prove to be unfavourable (stressful) with diminished content of carotenoid and pectic substances and low activities of IAA oxidase and PPO, ultimately leading to poor growth and productivity.

  12. Contact and fumigant activities of constituents of Foeniculum vulgare fruit against three coleopteran stored-product insects.

    PubMed

    Kim, D H; Ahn, Y J

    2001-03-01

    The insecticidal activities of materials derived from the fruit of fennel, Foeniculum vulgare, against adults of Sitophilus oryzae, Callosobruchus chinensis and Lasioderma serricorne were examined using direct contact application and fumigation methods. The biologically active constituents of the Foeniculum fruits were characterized as the phenylpropenes (E)-anethole and estragole, and the monoterpene (+)-fenchone, by spectroscopic analysis. Responses varied with insect species, compound, dose and exposure time. In a filter paper diffusion test, estragole at 0.168 mg cm-2 caused 91% mortality to S oryzae adults within 1 day after treatment (DAT), whereas (+)-fenchone and (E)-anethole gave over 90% mortality at 2 and 4 DAT, respectively. Against C chinensis adults, all test compounds revealed potent insecticidal activities at 0.021 mg cm-2 at 2 DAT. Against L serricorne adults at 0.105 mg cm-2, (E)-anethole gave 100% mortality at 1 DAT, whereas 90 and 60% mortality at 4 DAT was achieved with estragole and (+)-fenchone, respectively. In a fumigation test, the compounds were much more effective against adults of S oryzae, C chinensis and L serricorne in closed cups than in open ones, indicating that the insecticidal activity of test compounds was largely attributable to fumigant action. As naturally occurring insect-control agents, the F vulgare fruit-derived materials described could be useful for managing field populations of S oryzae, C chinensis and L serricorne.

  13. Metabolic activation of herbal and dietary constituents and its clinical and toxicological implications: an update.

    PubMed

    Zhou, Shu-Feng; Xue, Charlie Changli; Yu, Xue-Qing; Wang, Guangji

    2007-08-01

    pyrrolizidine alkaloids (e.g. echimidine and jacobine), namely pyrrole-type metabolites, are generated by hepatic CYP2B6 and CYP3A4. Potential mechanisms underlying the hepatotoxicity of kava have been related to intracellular glutathione depletion and/or quinone formation. Some herbal constituents (e.g. capsaicin from chili peppers, glabridin from licorice root, oleuropein in olive oil, dially sulfone in garlic, and resveratrol found in red wine) behave as mechanism-based inhibitors of various CYPs. This may provide an explanation for some reported herb-drug interactions. In addition, the inhibition of CYPs by herbal constituents may decrease the formation of toxic metabolites and thus inhibit carcinogenesis, as CYPs play an important role in procarcinogen activation. Due to the wide use and easy availability of herbal medicines, further research should be conducted to ensure the safety and quality of herbal medicine.

  14. Antiviral Activity and Possible Mechanism of Action of Constituents Identified in Paeonia lactiflora Root toward Human Rhinoviruses

    PubMed Central

    Ngan, Luong Thi My; Jang, Myeong Jin; Kwon, Min Jung; Ahn, Young Joon

    2015-01-01

    Human rhinoviruses (HRVs) are responsible for more than half of all cases of the common cold and cost billions of USD annually in medical visits and missed school and work. An assessment was made of the antiviral activities and mechanisms of action of paeonol (PA) and 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose (PGG) from Paeonia lactiflora root toward HRV-2 and HRV-4 in MRC5 cells using a tetrazolium method and real-time quantitative reverse transcription polymerase chain reaction and enzyme-linked immunosorbent assay. Results were compared with those of a reference control ribavirin. Based on 50% inhibitory concentration values, PGG was 13.4 and 18.0 times more active toward HRV-2 (17.89 μM) and HRV-4 (17.33 μM) in MRC5 cells, respectively, than ribavirin. The constituents had relatively high selective index values (3.3–>8.5). The 100 μg/mL PA and 20 μg/mL PGG did not interact with the HRV-4 particles. These constituents inhibited HRV-4 infection only when they were added during the virus inoculation (0 h), the adsorption period of HRVs, but not after 1 h or later. Moreover, the RNA replication levels of HRVs were remarkably reduced in the MRC5 cultures treated with these constituents. These findings suggest that PGG and PA may block or reduce the entry of the viruses into the cells to protect the cells from the virus destruction and abate virus replication, which may play an important role in interfering with expressions of rhinovirus receptors (intercellular adhesion molecule-1 and low-density lipoprotein receptor), inflammatory cytokines (interleukin (IL)-6, IL-8, tumor necrosis factor, interferon beta, and IL-1β), and Toll-like receptor, which resulted in diminishing symptoms induced by HRV. Global efforts to reduce the level of synthetic drugs justify further studies on P. lactiflora root-derived materials as potential anti-HRV products or lead molecules for the prevention or treatment of HRV. PMID:25860871

  15. Effects of Curcuma xanthorrhiza Extracts and Their Constituents on Phase II Drug-metabolizing Enzymes Activity

    PubMed Central

    Salleh, Nurul Afifah Mohd; Ismail, Sabariah; Ab Halim, Mohd Rohaimi

    2016-01-01

    Background: Curcuma xanthorrhiza is a native Indonesian plant and traditionally utilized for a range of illness including liver damage, hypertension, diabetes, and cancer. Objective: The study determined the effects of C. xanthorrhiza extracts (ethanol and aqueous) and their constituents (curcumene and xanthorrhizol) on UDP-glucuronosyltransferase (UGT) and glutathione transferase (GST) activities. Materials and Methods: The inhibition studies were evaluated both in rat liver microsomes and in human recombinant UGT1A1 and UGT2B7 enzymes. p-nitrophenol and beetle luciferin were used as the probe substrates for UGT assay while 1-chloro-2,4-dinitrobenzene as the probe for GST assay. The concentrations of extracts studied ranged from 0.1 to 1000 μg/mL while for constituents ranged from 0.01 to 500 μM. Results: In rat liver microsomes, UGT activity was inhibited by the ethanol extract (IC50 =279.74 ± 16.33 μg/mL). Both UGT1A1 and UGT2B7 were inhibited by the ethanol and aqueous extracts with IC50 values ranging between 9.59–22.76 μg/mL and 110.71–526.65 μg/Ml, respectively. Rat liver GST and human GST Pi-1 were inhibited by ethanol and aqueous extracts, respectively (IC50 =255.00 ± 13.06 μg/mL and 580.80 ± 18.56 μg/mL). Xanthorrhizol was the better inhibitor of UGT1A1 (IC50 11.30 ± 0.27 μM) as compared to UGT2B7 while curcumene did not show any inhibition. For GST, both constituents did not show any inhibition. Conclusion: These findings suggest that C. xanthorrhiza have the potential to cause herb-drug interaction with drugs that are primarily metabolized by UGT and GST enzymes. SUMMARY Findings from this study would suggest which of Curcuma xanthorrhiza extracts and constituents that would have potential interactions with drugs which are highly metabolized by UGT and GST enzymes. Further clinical studies can then be designed if needed to evaluate the in vivo pharmacokinetic relevance of these interactions Abbreviations Used: BSA: Bovine serum albumin

  16. Comparative analysis of the constituents in Saposhnikoviae Radix and Glehniae Radix cum Rhizoma by monitoring inhibitory activity of nitric oxide production.

    PubMed

    Kamino, Takuya; Shimokura, Toshihiro; Morita, Yusuke; Tezuka, Yasuhiro; Nishizawa, Mikio; Tanaka, Ken

    2016-04-01

    During the development of natural herbal medicines in Japan, Glehniae Radix cum Rhizoma (Hamabofu in Japanese) has been used as a substitute for Saposhnikoviae Radix (Bofu). Bofu and Hamabofu are blended differently in several Kampo formulae. For example, Bofu is included in Jumihaidokuto by a manufacturer, whereas Hamabofu is included instead of Bofu in the same formula by other manufacturers. Although both Bofu and Hamabofu are used for their expected anti-inflammatory effects, differences in their medicinal properties are not well characterized. In addition, there have been very few reports comparing the pharmacological activities of the constituents in Bofu and Hamabofu. In the present study, we investigated the anti-inflammatory effects of the extracts of Bofu and Hamabofu by monitoring levels of the inflammatory mediator nitric oxide (NO) produced in rat hepatocytes. Moreover, the chemical constituents responsible for the activity were investigated. Our results showed that ethyl acetate fractions of Bofu and Hamabofu extracts contain different compounds, although both fractions suppressed NO production in rat hepatocytes. The linear dihydropyranochromones from the Bofu extract (i.e., 3'-O-angeloylhamaudol, ledebouriellol and hamaudol) suppressed NO production, whereas the coumarins from the Hamabofu extract (i.e., umbelliferone and scopoletin) also suppressed NO production. These results suggest that linear dihydropyranochromones and coumarins are responsible for the anti-inflammatory effects of Bofu and Hamabofu. It is plausible that Bofu and Hamabofu are blended differently in several Kampo formulae due to many constituents with as yet unidentified pharmacological activity.

  17. Comparative Studies of Antioxidant Activities and Nutritional Constituents of Persimmon Juice (Diospyros kaki L. cv. Gapjubaekmok)

    PubMed Central

    Lee, Jin Hwan; Lee, Yong Bok; Seo, Woo Duck; Kang, Su Tae; Lim, Jong Woo; Cho, Kye Man

    2012-01-01

    The objectives of this research were to evaluate antioxidant activities and nutritional components, including phenolic acid, catechin, organic acid, sugar, and amino acid, of persimmon juice from persimmons grown in different regions around Korea. Persimmon (Diospyros kaki) exhibits potent antioxidant effects in DPPH, ABTS, reducing power, and FRAP methods of analysis. The levels of nutritional constituents showed significant differences among all the samples. In particular, tartaric acid, glucose, gallic acid, epicatechin gallate and aspartic acid were observed to be the predominant component for each of their general chemical groups, with total average contents of 1876.51 mg/kg, 62.69 g/kg, 12.73 mg/kg, 208.99 mg/kg, and 31.84 mg/100 g, respectively. Interestingly, persimmons from the Hadong region presented the highest sugar (130.60 g/kg), phenolic acid (42.27 mg/kg), and catechin (527.97 mg/kg) contents in comparison with other regional samples. Moreover, this location exhibited the greatest antioxidant activity with highest total phenolic (298.01 mg GAE/kg) and flavonoid (32.11 mg/kg RE) contents. Our results suggest that strong antioxidant activities of persimmons correlate with high phenolic acid and catechin contents, particularly gallic acid and epicatechin gallate. Additionally, these two compounds may be key factors when considering the useful ingredients of persimmon. PMID:24471076

  18. Constituents of the leaves of Peucedanum japonicum Thunb. and their biological activity.

    PubMed

    Hisamoto, Masashi; Kikuzaki, Hiroe; Nakatani, Nobuji

    2004-02-11

    In the course of our study on the isolation and structure determination of constituents in tropical plants, we focused on Peucedanum japonicum Thunb., belonging to the family Umbelliferae. In this study, a new C(13) norisoprenoid glucoside, (3S)-O-beta-d-glucopyranosyl-6-[3-oxo-(2S)-butenylidenyl]-1,1,5-trimethylcyclohexan-(5R)-ol (1), and two new phenylpropanoid glucosides, 3-(2-O-beta-d-glucopyranosyl-4-hydroxyphenyl)propanoic acid (3) and methyl 3-(2-O-beta-d-glucopyranosyl-4-hydroxyphenyl)propanoate (4), were isolated from the n-butanol soluble fraction of this plant's leaves, together with five known compounds. The structures of these compounds were determined on the basis of spectroscopic evidence. In addition, all isolated compounds were examined for scavenging activity against 1,1-diphenyl-2-picrylhydrazyl radical and inhibitory activity against mushroom tyrosinase. These results suggested that 2-(4-hydroxy-3-methoxyphenyl)propane-1,3-diol (7) and 3-O-beta-d-glucopyranosyl-2-(4-hydroxy-3-methoxyphenyl)propanol (8) showed an appreciable activity in both assay systems.

  19. Comparative Studies of Antioxidant Activities and Nutritional Constituents of Persimmon Juice (Diospyros kaki L. cv. Gapjubaekmok).

    PubMed

    Lee, Jin Hwan; Lee, Yong Bok; Seo, Woo Duck; Kang, Su Tae; Lim, Jong Woo; Cho, Kye Man

    2012-06-01

    The objectives of this research were to evaluate antioxidant activities and nutritional components, including phenolic acid, catechin, organic acid, sugar, and amino acid, of persimmon juice from persimmons grown in different regions around Korea. Persimmon (Diospyros kaki) exhibits potent antioxidant effects in DPPH, ABTS, reducing power, and FRAP methods of analysis. The levels of nutritional constituents showed significant differences among all the samples. In particular, tartaric acid, glucose, gallic acid, epicatechin gallate and aspartic acid were observed to be the predominant component for each of their general chemical groups, with total average contents of 1876.51 mg/kg, 62.69 g/kg, 12.73 mg/kg, 208.99 mg/kg, and 31.84 mg/100 g, respectively. Interestingly, persimmons from the Hadong region presented the highest sugar (130.60 g/kg), phenolic acid (42.27 mg/kg), and catechin (527.97 mg/kg) contents in comparison with other regional samples. Moreover, this location exhibited the greatest antioxidant activity with highest total phenolic (298.01 mg GAE/kg) and flavonoid (32.11 mg/kg RE) contents. Our results suggest that strong antioxidant activities of persimmons correlate with high phenolic acid and catechin contents, particularly gallic acid and epicatechin gallate. Additionally, these two compounds may be key factors when considering the useful ingredients of persimmon.

  20. Chemical constituents and anti-inflammatory activities of Maqian (Zanthoxylum myriacanthum var. pubescens) bark extracts.

    PubMed

    Zhang, Huan-Li; Gan, Xiao-Qing; Fan, Qing-Fei; Yang, Jing-Jing; Zhang, Ping; Hu, Hua-Bin; Song, Qi-Shi

    2017-04-06

    In this study, 44 compounds in the petroleum ether extract of Maqian (Zanthoxylum myriacanthum var. pubescens) bark, a traditional Dai herbal medicine, were identified by GC-MS. Major components included 3(2H)-benzofuranone, asarinin and (dimethoxymethyl)-3-methoxy-benzene. A total of 18 compounds were isolated from the ethyl acetate extracts of Maqian bark by column chromatography and identified by chemical and spectral analyses. Rhoifoline B, zanthoxyline dimethoxy derivative, N-nortidine, nitidine, decarine are the major alkaloids. Both the petroleum ether and ethyl acetate extracts showed significant inhibition on NO production, which imply anti-inflammatory activity, in lipopolysaccharide-induced RAW 264.7 cells without cell toxicity. Decarine is the major anti-inflammatory constituent with NO IC50 values of 48.43 μM on RAW264.7 cells. The petroleum ether extract, the ethyl acetate extract and decarine showed anti-inflammatory activities through inhibiting TNF-α and IL-1β production in lipopolysaccharide-stimulated THP-1 cells without cell toxicity too. Decarine showed anti-inflammatory activity on human colon cells by reducing IL-6 and IL-8 production in TNF-α+IL-1β-induced Caco-2 cells. These results support the use of Maqian bark as a remedy for enteritis and colitis recorded by Dai medicine in China, and elucidate the major pharmacological compounds in Maqian bark.

  1. Chemical constituents and anti-inflammatory activities of Maqian (Zanthoxylum myriacanthum var. pubescens) bark extracts

    PubMed Central

    Zhang, Huan-li; Gan, Xiao-qing; Fan, Qing-fei; Yang, Jing-jing; Zhang, Ping; Hu, Hua-bin; Song, Qi-shi

    2017-01-01

    In this study, 44 compounds in the petroleum ether extract of Maqian (Zanthoxylum myriacanthum var. pubescens) bark, a traditional Dai herbal medicine, were identified by GC-MS. Major components included 3(2H)-benzofuranone, asarinin and (dimethoxymethyl)-3-methoxy-benzene. A total of 18 compounds were isolated from the ethyl acetate extracts of Maqian bark by column chromatography and identified by chemical and spectral analyses. Rhoifoline B, zanthoxyline dimethoxy derivative, N-nortidine, nitidine, decarine are the major alkaloids. Both the petroleum ether and ethyl acetate extracts showed significant inhibition on NO production, which imply anti-inflammatory activity, in lipopolysaccharide-induced RAW 264.7 cells without cell toxicity. Decarine is the major anti-inflammatory constituent with NO IC50 values of 48.43 μM on RAW264.7 cells. The petroleum ether extract, the ethyl acetate extract and decarine showed anti-inflammatory activities through inhibiting TNF-α and IL-1β production in lipopolysaccharide-stimulated THP-1 cells without cell toxicity too. Decarine showed anti-inflammatory activity on human colon cells by reducing IL-6 and IL-8 production in TNF-α+IL-1β-induced Caco-2 cells. These results support the use of Maqian bark as a remedy for enteritis and colitis recorded by Dai medicine in China, and elucidate the major pharmacological compounds in Maqian bark. PMID:28383530

  2. Evaluation of Antibacterial Activity, Phytochemical Constituents, and Cytotoxicity Effects of Thai Household Ancient Remedies

    PubMed Central

    Sinvaraphan, Naruephan; Chaipak, Ploypailin; Luxsananuwong, Atita; Voravuthikunchai, Supayang Piyawan

    2014-01-01

    Abstract Aim: Household ancient remedies reported here are described in the National List of Essential Medicines and have traditionally been used in Thailand to treat infection-related ailments. However, the safety and effectiveness of these remedies have been poorly evaluated. The aim of this study was to evaluate the antibacterial properties of these remedies against seven gram-positive and gram-negative multidrug-resistant bacteria species. Phytochemical constituents and cytotoxicity of these remedies were also determined. Methods: Seven remedies, consisting of Um-Ma-Luk-Ka-Wa-Tee, Chan-Ta-Lee-La, Kheaw-Hom, Learng-Pid-Sa-Mud, Pra-Sa-Chan-Dang, Dhart-Ban-Chob, and Tree-Hom, were prepared by a licensed traditional medical doctor using a mixture of medicinal plants. Antibacterial activity of ethanol extracts of the remedies was determined by using a broth microdilution method. Qualitative phytochemical screening analysis was carried out to identify the presence of major components. Cytotoxicity activities of the extracts against Vero cells were assessed by green fluorescent protein–based assay. Results: With the exception of Dhart-Ban-Chob extract, significant minimum inhibitory concentrations (MICs) of <16 to 32 μg/mL were observed for the remedy extracts depending on the bacterial strains. The Um-Ma-Luk-Ka-Wa-Tee extract was noncytotoxic against Vero cells and possessed the highest activity, with MICs of <16 to 31 μg/mL against all methicillin-resistant Staphylococcus aureus isolates. Conclusions: Remarkable antibacterial activities against multidrug-resistant pathogens, as well as low toxicity on Vero cells, of Um-Ma-Luk-Ka-Wa-Tee support the use of this remedy in traditional medicine. Further investigation on other biological activities related to traditional applications, appropriate biomarkers, and treatment mechanisms of the household remedy are required. PMID:25415453

  3. Volatile constituents and antioxidant activity of flowers, stems and leaves of Nasturtium officinale R. Br.

    PubMed

    Amiri, Hamzeh

    2012-01-01

    GC-MS analyses of the essential oils of leaves, stems and flower of Nasturtium officinale resulted in the identification of 9, 8 and 15 compounds, representing 97%, 100% and 94.7% of the oils, respectively. The main compounds of the oil of leaves were myristicin (57.6%), α-terpinolene (8.9%) and limonene (6.7%). Caryophyllene oxide (37.2%), p-cymene-8-ol (17.6%), α-terpinolene (15.2%) and limonene (11.8%) were the main components in stems, whereas limonene (43.6%), α-terpinolene (19.7%), p-cymene-8-ol (7.6%) and caryophyllene oxide (6.7%) were the major constituents in the oil of flowers. All the samples were subjected to a screening for their possible antioxidant activities using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and β-carotene-linoleic acid assays. In the above tests, methanol extracts of leaves showed higher antioxidant activity than the oils and methanol extracts of stems and flowers.

  4. In vitro and in vivo activity of major constituents from Pluchea carolinensis against Leishmania amazonensis.

    PubMed

    Montrieux, Elly; Perera, Wilmer H; García, Marley; Maes, Louis; Cos, Paul; Monzote, Lianet

    2014-08-01

    The search for new therapeutic agents from natural sources has been a constant for the treatment of diseases such as leishmaniasis. Herein, in vitro and in vivo pharmacological activities of pure major phenolic constituents (caffeic acid, chlorogenic acid, ferulic acid, quercetin, and rosmarinic acid) from Pluchea carolinensis against Leishmania amazonensis are presented. Pure compounds showed inhibitory activity against promastigotes (IC50 = 0.2-0.9 μg/mL) and intracellular amastigotes (IC50 = 1.3-2.9 μg/mL). Four of them were selected after testing against macrophages of BALB/c mice: caffeic acid, ferulic acid, quercetin, and rosmarinic acid, with selective indices of 11, 17, 10, and 20, respectively. Ferulic acid, rosmarinic acid, and caffeic acid controlled lesion size development and parasite burden in footpads from BALB/c experimentally infected mice, after five injections of compounds by intralesional route at 30 mg/kg every 4 days. Pure compounds from P. carolinensis demonstrated antileishmanial properties.

  5. Structural Basis of Human PXR Activation by the Hops Constituent Colupulone

    PubMed Central

    Teotico, Denise G.; Bischof, Jason J.; Peng, Li; Kliewer, Steven A.; Redinbo, Matthew R.

    2008-01-01

    Hops extracts are used to alleviate menopausal symptoms and as an alternative to hormone replacement therapy, but can produce potentially harmful drug-drug interactions. The nuclear xenobiotic receptor PXR is promiscuously activated by a range of structurally distinct chemicals. It has a key role in the transcriptional regulation of genes that encode xenobiotic metabolism enzymes. In this study, hops extracts are shown to induce the expression of numerous drug metabolism and excretion proteins. The β-bitter acid colupulone is demonstrated to be a bioactive component and direct activator of human PXR. The 2.8 Å resolution crystal structure of the ligand binding domain of human PXR in complex with colupulone was elucidated, and colupulone was observed to bind in a single orientation stabilized by both Van der Waals and hydrogen bonding contacts. The crystal structure also indicates that related α- and β-bitter acids have the capacity to serve as PXR agonists, as well. Taken together, these results reveal the structural basis for drug-drug interactions mediated by colupulone and related constituents of hops extracts. PMID:18768384

  6. Antioxidant activity and characterization of volatile constituents of Taheebo (Tabebuia impetiginosa Martius ex DC).

    PubMed

    Park, Byeoung-Soo; Lee, Kwang-Geun; Shibamoto, Takayuki; Lee, Sung-Eun; Takeoka, Gary R

    2003-01-01

    Volatiles were isolated from the dried inner bark of Tabebuia impetiginosa using steam distillation under reduced pressure followed by continuous liquid-liquid extraction. The extract was analyzed by gas chromatography and gas chromatography-mass spectrometry. The major volatile constituents of T. impetiginosa were 4-methoxybenzaldehyde (52.84 microg/g), 4-methoxyphenol (38.91 microg/g), 5-allyl-1,2,3-trimethoxybenzene (elemicin; 34.15 microg/g), 1-methoxy-4-(1E)-1-propenylbenzene (trans-anethole; 33.75 microg/g), and 4-methoxybenzyl alcohol (30.29 microg/g). The antioxidant activity of the volatiles was evaluated using two different assays. The extract exhibited a potent inhibitory effect on the formation of conjugated diene hydroperoxides (from methyl linoleate) at a concentration of 1000 microg/mL. The extract also inhibited the oxidation of hexanal for 40 days at a level of 5 microg/mL. The antioxidative activity of T. impetiginosa volatiles was comparable with that of the well-known antioxidants, alpha-tocopherol, and butylated hydroxytoluene.

  7. Chemical Constituents and Activity of Murraya microphylla Essential Oil against Lasioderma serricorne.

    PubMed

    You, Chun-Xue; Guo, Shan-Shan; Zhang, Wen-Juan; Yang, Kai; Wang, Cheng-Fang; Geng, Zhu-Feng; Du, Shu-Shan; Deng, Zhi-Wei; Wang, Yong-Yan

    2015-09-01

    The chemical composition, contact and repellent activities of the essential oil from Murraya microphylla branches and leaves against Lasioderma serricorne adults were determined and six compounds from the essential oil were isolated as well. The essential oil of M microphylla obtained by hydrodistillation was analyzed by gas chromatography-mass spectrometric (GC-MS) analysis; 22 compounds were identified. The main constituents of the essential oil included β-caryophyllene (18.0%), α-pinene (13.8%), spathulenol (9.5%), α-humulene (6.0%), γ-elemene (5.1%) and zingiberene (4.6%), followed by α-cadinol (3.9%) and caryophyllene oxide (3.8%). Six of these compounds were isolated and fully identified as α-pinene, β-caryophyllene, α-humulene, caryophyllene oxide, spathulenol and α-cadinol. L. serricorne adults had different sensitivities to the crude essential oil and isolated compounds. α-Humulene exhibited the strongest contact activity against L. serricorne, showing an LD50 value of 13.1 µg adult(-1). However, spathulenol, the crude essential oil and α-cadinol showed stronger contact activity against L. serricorne than caryophyllene oxide and β-caryophyllene. The essential oil, α-humulene and spathulenol showed comparable repellency against L. serricorne adults at 2 h after exposure, relative to the positive control, DEET. The results demonstrate that the essential oil and isolated compounds exhibited important contact and repellent activities against L. serricorne. Thus, they could become potential natural insecticides or repellents for control of insects in stored products.

  8. Effects of constituents from the bark of Magnolia obovata on nitric oxide production in lipopolysaccharide-activated macrophages.

    PubMed

    Matsuda, H; Kageura, T; Oda, M; Morikawa, T; Sakamoto, Y; Yoshikawa, M

    2001-06-01

    The methanolic extract from a Japanese herbal medicine, the bark of Magnolia obovata, was found to inhibit nitric oxide (NO) production in lipopolysaccharide (LPS)-activated macrophages. By bioassay-guided separation, three neolignans (magnolol, honokiol, obovatol) and three sesquiterpenes (alpha-eudesmol, beta-eudesmol, gamma-eudesmol) were obtained as active constituents. A trineolignan (magnolianin), a phenylpropanoid glycoside (syringin), lignan glycosides (liriodendrin, (+)-syringaresinol 4'-O-beta-D-glucopyranoside) and a sesquiterpene (caryophyllene oxide) did not show any activity. On the other hand, sesquiterpene-neolignans (eudesmagnolol, clovanemagnolol, caryolanemagnolol, eudeshonokiol A, eudesobovatol A) showed the strong cytotoxic effects. Active constituents (magnolol, honokiol, obovatol) showed weak inhibition for inducible NO synthase (iNOS) enzyme activity, but potent inhibition of iNOS induction and activation of nuclear factor-kappaB.

  9. Synergy and Antagonism of Active Constituents of ADAPT-232 on Transcriptional Level of Metabolic Regulation of Isolated Neuroglial Cells.

    PubMed

    Panossian, Alexander; Hamm, Rebecca; Kadioglu, Onat; Wikman, Georg; Efferth, Thomas

    2013-01-01

    Gene expression profiling was performed on the human neuroglial cell line T98G after treatment with adaptogen ADAPT-232 and its constituents - extracts of Eleutherococcus senticosus root, Schisandra chinensis berry, and Rhodiola rosea root as well as several constituents individually, namely, eleutheroside E, schizandrin B, salidroside, triandrin, and tyrosol. A common feature for all tested adaptogens was their effect on G-protein-coupled receptor signaling pathways, i.e., cAMP, phospholipase C (PLC), and phosphatidylinositol signal transduction pathways. Adaptogens may reduce the cAMP level in brain cells by down-regulation of adenylate cyclase gene ADC2Y and up-regulation of phosphodiesterase gene PDE4D that is essential for energy homeostasis as well as for switching from catabolic to anabolic states and vice versa. Down-regulation of cAMP by adaptogens may decrease cAMP-dependent protein kinase A activity in various cells resulting in inhibition stress-induced catabolic transformations and saving of ATP for many ATP-dependant metabolic transformations. All tested adaptogens up-regulated the PLCB1 gene, which encodes phosphoinositide-specific PLC and phosphatidylinositol 3-kinases (PI3Ks), key players for the regulation of NF-κB-mediated defense responses. Other common targets of adaptogens included genes encoding ERα estrogen receptor (2.9-22.6 fold down-regulation), cholesterol ester transfer protein (5.1-10.6 fold down-regulation), heat shock protein Hsp70 (3.0-45.0 fold up-regulation), serpin peptidase inhibitor (neuroserpin), and 5-HT3 receptor of serotonin (2.2-6.6 fold down-regulation). These findings can be reconciled with the observed beneficial effects of adaptogens in behavioral, mental, and aging-associated disorders. Combining two or more active substances in one mixture significantly changes deregulated genes profiles: synergetic interactions result in activation of genes that none of the individual substances affected, while antagonistic

  10. Synergy and Antagonism of Active Constituents of ADAPT-232 on Transcriptional Level of Metabolic Regulation of Isolated Neuroglial Cells

    PubMed Central

    Panossian, Alexander; Hamm, Rebecca; Kadioglu, Onat; Wikman, Georg; Efferth, Thomas

    2013-01-01

    Gene expression profiling was performed on the human neuroglial cell line T98G after treatment with adaptogen ADAPT-232 and its constituents – extracts of Eleutherococcus senticosus root, Schisandra chinensis berry, and Rhodiola rosea root as well as several constituents individually, namely, eleutheroside E, schizandrin B, salidroside, triandrin, and tyrosol. A common feature for all tested adaptogens was their effect on G-protein-coupled receptor signaling pathways, i.e., cAMP, phospholipase C (PLC), and phosphatidylinositol signal transduction pathways. Adaptogens may reduce the cAMP level in brain cells by down-regulation of adenylate cyclase gene ADC2Y and up-regulation of phosphodiesterase gene PDE4D that is essential for energy homeostasis as well as for switching from catabolic to anabolic states and vice versa. Down-regulation of cAMP by adaptogens may decrease cAMP-dependent protein kinase A activity in various cells resulting in inhibition stress-induced catabolic transformations and saving of ATP for many ATP-dependant metabolic transformations. All tested adaptogens up-regulated the PLCB1 gene, which encodes phosphoinositide-specific PLC and phosphatidylinositol 3-kinases (PI3Ks), key players for the regulation of NF-κB-mediated defense responses. Other common targets of adaptogens included genes encoding ERα estrogen receptor (2.9–22.6 fold down-regulation), cholesterol ester transfer protein (5.1–10.6 fold down-regulation), heat shock protein Hsp70 (3.0–45.0 fold up-regulation), serpin peptidase inhibitor (neuroserpin), and 5-HT3 receptor of serotonin (2.2–6.6 fold down-regulation). These findings can be reconciled with the observed beneficial effects of adaptogens in behavioral, mental, and aging-associated disorders. Combining two or more active substances in one mixture significantly changes deregulated genes profiles: synergetic interactions result in activation of genes that none of the individual substances affected, while

  11. Combined experimental and DFT-TDDFT study of photo-active constituents of Canarium odontophyllum for DSSC application

    NASA Astrophysics Data System (ADS)

    Ekanayake, Piyasiri; Kooh, Muhammad Raziq Rahimi; Kumara, N. T. R. N.; Lim, Andery; Petra, Mohammad Iskandar; Voo, Nyuk Yoong; Lim, Chee Ming

    2013-10-01

    The active constituents of Canarium odontophyllum (COP) were investigated experimentally and theoretically for dye sensitized solar cell (DSSC) application. Three main flavonoid pigments (cyanidin, pelargonidin and maritimein) were detected in COP showing photo-energy conversion efficiencies of 1.43%, 0.87% and 0.60%, respectively. The molecular geometries, electronic structures, optical absorption spectra and proton affinity of these molecules were investigated with DFT/TDDFT. All three molecules displayed π→π* transition dominant in HOMO→LUMO transition. The anchoring groups onto TiO2 surface were deduced from combined experimental and calculated data. All the constituents of COP are potential sensitizers for DSSC.

  12. Attenuation of quorum sensing-regulated behaviour by Tinospora cordifolia extract & identification of its active constituents

    PubMed Central

    Gala, Viraj C.; John, Nithya R.; Bhagwat, Ashok M.; Datar, Ajit G.; Kharkar, Prashant S.; Desai, Krutika B.

    2016-01-01

    Background & objectives: The pathogenicity of the nosocomial pathogens, Pseudomonas aeruginosa and Acinetobacter baumannii is regulated by their quorum sensing (QS) systems. The objective of the present study was to examine the effect of the cold ethyl acetate extract of Tinospora cordifolia stem on virulence and biofilm development in the wild type and clinical strains of P. aeruginosa and A. baumannii. The study was further aimed to identify the probable active constituents in the plant extract. Methods: P. aeruginosa virulence factors viz., LasA protease, LasB elastase and pyocyanin production were analyzed spectrophotometrically. Biofilm formation was studied using crystal violet staining-microtitre plate assay. The plant extract was fractionated using silica gel column chromatography and the most active fraction was derivatized using silylation and analyzed by gas chromatography-mass spectrometry (GC-MS). In silico testing of the molecules identified in GC-MS was performed, for binding to the P. aeruginosa LasI and LasR proteins, to predict the QS inhibitory molecules. Results: The plant extract inhibited three major virulence factors in P. aeruginosa; it exhibited enhanced biofilm formation in P. aeruginosa while decreased biofilm development in A. baumannii. The most active fraction obtained from column chromatography, exhibited suppression of virulence as well as biofilm in both the organisms. Docking scores were calculated for all the molecules identified in GC-MS, and high docking scores were obtained for 2,3,4-triacetyloxybutyl acetate, methyl 16-methyl heptadecanoate, 2-(5-ethenyl-5-methyloxolan-2-yl)propan-2-ol, methyl hexadecanoate and 2-methoxy-4-vinyl phenol. Interpretation & conclusions: The compounds showing high docking scores could probably be the QS inhibitors. These molecules can be screened further for the development of new anti-infective drugs. PMID:27834332

  13. Alkenylresorcinols and cytotoxic activity of the constituents isolated from Labisia pumila.

    PubMed

    Al-Mekhlafi, Nabil Ali; Shaari, Khozirah; Abas, Faridah; Kneer, Ralf; Jeyaraj, Ethel Jeyaseela; Stanslas, Johnson; Yamamoto, Naoshi; Honda, Toshio; Lajis, Nordin H

    2012-08-01

    Phytochemical investigation on the leaves of Labisia pumila (Myrsinaceae), an important medicinal herb in Malaysia, has led to the isolation of 1-O-methyl-6-acetoxy-5-(pentadec-10Z-enyl)resorcinol (1), labisiaquinone A (2) and labisiaquinone B (3). Along with these, 16 known compounds including 1-O-methyl-6-acetoxy-5-pentadecylresorcinol (4), 5-(pentadec-10Z-enyl)resorcinol (5), 5-(pentadecyl)resorcinol (6), (-)-loliolide (7), stigmasterol (8), 4-hydroxyphenylethylamine (9), 3,4,5-trihydroxybenzoic acid (10), 3,4-dihydroxybenzoic acid (11), (+)-catechin (12), (-)-epicatechin (13), kaempferol-3-O-α-rhamnopyranosyl-7-O-β-glycopyranoside (14), kaempferol-4'-O-β-glycopyranoside (15), quercetin-3-O-α-rhamnopyranoside (16), kaempferol-3-O-α-rhamnopyranoside (17), (9Z,12Z)-octadeca-9,12-dienoic acid (18) and stigmasterol-3-O-β-glycopyranoside (19) were also isolated. The structures of these compounds were established on the basis of 1D and 2D NMR spectroscopy techniques (¹H, ¹³C, COSY, HSQC, NOESY and HMBC experiments), mass spectrometry and chemical derivatization. Among the constituents tested 1 and 4 exhibited strongest cytotoxic activity against the PC3, HCT116 and MCF-7 cell lines (IC₅₀ values ≤ 10 μM), and they showed selectivity towards the first two-cell lines relative to the last one.

  14. Mentha suaveolens Ehrh. (Lamiaceae) Essential Oil and Its Main Constituent Piperitenone Oxide: Biological Activities and Chemistry.

    PubMed

    Božović, Mijat; Pirolli, Adele; Ragno, Rino

    2015-05-13

    Since herbal medicines play an important role in the treatment of a wide range of diseases, there is a growing need for their quality control and standardization. Mentha suaveolens Ehrh. (MS) is an aromatic herb with fruit and a spearmint flavor, used in the Mediterranean areas as a traditional medicine. It has an extensive range of biological activities, including cytotoxic, antimicrobial, antioxidant, anti-inflammatory, hypotensive and insecticidal properties, among others. This study aims to review the scientific findings and research reported to date on MS that prove many of the remarkable various biological actions, effects and some uses of this species as a source of bioactive natural compounds. On the other hand, piperitenone oxide (PO), the major chemical constituent of the carvone pathway MS essential oil, has been reported to exhibit numerous bioactivities in cells and animals. Thus, this integrated overview also surveys and interprets the present knowledge of chemistry and analysis of this oxygenated monoterpene, as well as its beneficial bioactivities. Areas for future research are suggested.

  15. Chemical constituents of the bark of Dipteryx alata vogel, an active species against Bothrops jararacussu venom.

    PubMed

    Puebla, Pilar; Oshima-Franco, Yoko; Franco, Luiz M; Santos, Marcio G Dos; Silva, Renata V da; Rubem-Mauro, Leandro; Feliciano, Arturo San

    2010-11-12

    The effect of four sub-extracts prepared from the lyophilized hydroalcoholic bark of Dipteryx alata (Leguminosae-Papilionoideae) dissolved in a methanol-water (80:20) mixture through a liquid-liquid partition procedure has been investigated against the neuromuscular blockade of the venom of the snake Bothrops jararacussu. The active CH₂Cl₂ sub-extract has been extensively analyzed for its chemical constituents, resulting in the isolation of four lupane-type triterpenoids: lupeol, lupenone, 28-hydroxylup-20(29)-en-3-one, betulin, nine isoflavonoids: 8-O-methylretusin, 7-hydroxy-5,6,4'-trimethoxyisoflavone, afrormosin, 7-hydroxy-8,3',4'-trimethoxyisoflavone, 7,3'-dihydroxy-8,4'-dimethoxyisoflavone, odoratin, 7,8,3'-trihydroxy-4'-methoxyisoflavone, 7,8,3'-trihydroxy-6,4'-dimethoxyisoflavone, dipteryxin, one chalcone: isoliquiritigenin, one aurone: sulfuretin and three phenolic compounds: vanillic acid, vanillin, and protocatechuic acid. Their chemical structures were elucidated on the basis of spectroscopic analysis, including HRMS, 1D- and 2D-NMR techniques.

  16. New constituents with iNOS inhibitory activity from mycelium of Antrodia camphorata.

    PubMed

    Yang, Sien-Sing; Wang, Guei-Jane; Wang, Shiang-Yi; Lin, Yu-Ying; Kuo, Yueh-Hsiung; Lee, Tzong-Huei

    2009-04-01

    In continuing our investigation on the bioactive constituents of mycelium of Antrodia camphorata, antroquinonol B (1), 4-acetyl-antroquinonol B (2), 2,3-(methylenedioxy)-6-methylbenzene-1,4-diol (3) and 2,4-dimethoxy-6-methylbenzene-1,3-diol (4) along with antrodin D (5) were isolated by the guidance of an inducible nitric oxide synthase (iNOS) inhibitory assay and identified on the basis of their spectroscopic analysis. The effect of these compounds on the inhibition of NO production in lipopolysaccharide (LPS)-activated murine macrophages was further evaluated. Compounds 4 and 5 significantly inhibited NO production without any cytotoxicity, the IC(50) values being 32.2 +/- 0.1 and 26.3 +/- 1.6 microg/mL, respectively. Compounds 1 and 2 possessed greater effects on NO inhibition, with IC(50) values of 16.2 +/- 0.8 and 14.7 +/- 2.8 microg/mL, respectively, but displayed cytotoxicity at considerably higher concentrations. Compound 3 showed the lowest percent cell viability of 45.5 +/- 1.8 % as observed in treated cells at a concentration of 16.8 microg/mL.

  17. Polar Constituents and Biological Activity of the Berry-Like Fruits from Hypericum androsaemum L.

    PubMed Central

    Caprioli, Giovanni; Alunno, Alessia; Beghelli, Daniela; Bianco, Armandodoriano; Bramucci, Massimo; Frezza, Claudio; Iannarelli, Romilde; Papa, Fabrizio; Quassinti, Luana; Sagratini, Gianni; Tirillini, Bruno; Venditti, Alessandro; Vittori, Sauro; Maggi, Filippo

    2016-01-01

    Hypericum androsaemum, also known as Tutsan, is a small evergreen shrub common in the Mediterranean basin where it is traditionally used as diuretic and hepatoprotective herbal drug. This plant possesses the peculiarity to produce fleshy and berry-like fruits that ripen from red to shiny black. In the present work, the chemical constituents of methanolic extracts and infusions of red and black fruits were analyzed by HPLC, and correlated with their antioxidant properties which were evaluated by the DPPH, β-Carotene/linoleic acid, and hypochlorous acid tests. In addition, the red pigment of the fruit was isolated by column chromatography and structurally elucidated by NMR. Results showed that H. androsaemum fruits contain high amounts of shikimic and chlorogenic acids, while their color was given by a tetraoxygenated-type xanthone, reported for the first time in Hypericum species. The red berries infusion gave the highest content of total phenolic compounds, DPPH, and hypochlorous acid scavenging activity, and β-carotene bleaching. Cytotoxicity of the berries extracts on three human tumor cell lines (malignant melanoma, breast adenocarcinoma, and colon carcinoma) was evaluated by MTT assay, and relevant inhibition on colon carcinoma cells (IC50 value of 8.4 μg/mL) was found. Finally, the effects of red berries extract on the immune system were evaluated by peripheral blood mononuclear cell (PBMC) proliferation assay that revealed a strong stimulation on lymphocytes at low doses (0.4–6 μg/mL). PMID:26973675

  18. Bryophyllum pinnatum and Related Species Used in Anthroposophic Medicine: Constituents, Pharmacological Activities, and Clinical Efficacy.

    PubMed

    Fürer, Karin; Simões-Wüst, Ana Paula; von Mandach, Ursula; Hamburger, Matthias; Potterat, Olivier

    2016-07-01

    Bryophyllum pinnatum (syn. Kalanchoe pinnata) is a succulent perennial plant native to Madagascar that was introduced in anthroposophic medicine in the early 20th century. In recent years, we conducted a large collaborative project to provide reliable data on the chemical composition, pharmacological properties, and clinical efficacy of Bryophyllum. Here, we comprehensively review the phytochemistry, as well as the pharmacological and clinical data. As to the pharmacology, special emphasis is given to properties related to the use in anthroposophic medicine as a treatment for "hyperactivity diseases", such as preterm labor, restlessness, and sleep disorders. Studies suggesting that B. pinnatum may become a new treatment option for overactive bladder syndrome are also reviewed. Tolerability is addressed, and toxicological data are discussed in conjunction with the presence of potentially toxic bufadienolides in Bryophyllum species. The few data available on two related species with medicinal uses, Bryophyllum daigremontianum and Bryophyllum delagoense, have also been included. Taken together, current data support the use of B. pinnatum for the mentioned indications, but further studies are needed to fully understand the modes of action, and to identify the pharmacologically active constituents.

  19. Antioxidant activities of Lampaya medicinalis extracts and their main chemical constituents

    PubMed Central

    2014-01-01

    Background Lampaya medicinalis Phil. (Verbenaceae) is a plant used by Aymara and Quechua ethnic groups from Northern Chile as folk medicine in the treatment and cure of various diseases. The aim of this study was to investigate the in vitro antioxidant activity, total phenols content, total flavonoids content, total antioxidant activity, reducing power, brine shrimp cytotoxicity and identify the principal chemical constituents. Methods The crude hydroethanolic extract (HEE) and its partitioned fraction: hexane (HF), dichloromethane (DF), ethyl acetate (EAF), n-butanol (BF) and soluble residual aqueous fraction (RWF) were evaluated for their antioxidant activity using different assays namely, DPPH, ABTS, FRAP, β-carotene bleaching assay. The content of total phenolics and total flavonoids were measured by Folin-Ciocalteau and by the AlCl3 colorimetric method, respectively. Reducing power was determined by phosphomolybdate and hexacyanoferrate (III) methods. Biotoxicity assays were performed on shrimps of Artemia salina. The EAF was fractionated using chromatographic methods. Results Considerable amount of phenolic and flavonoid contents were recorded in the hydroethanolic extract (HEE) and its derived fractions. Although HEE and all its derived fractions exhibited good antioxidant activities, the most distinguished radical scavenging potential was observed for ethyl acetate fraction (EAF). EAF showed the higher radical scavenging activity by DPPH (95%) and by ABTS (98%), antioxidant activity by FRAP (158.18 ± 5.79 mg equivalent Trolox/g fraction), β-carotene bleaching assay (86.8%), the highest total phenols content (101.26 ± 1.07 mg GAE/g fraction), the highest total flavonoids content (66.26 ± 3.31 μg quercetin/g fraction). The EAF extract showed an reducing power of 78% and 65% using the phosphomolybdate and hexacyanoferrate (III) assays, respectively. Four flavonoids, two p-hydroxyacetophenone derivatives and one iridoid were isolated from Lampaya

  20. Mosquito larvicidal activity of active constituent derived from Chamaecyparis obtusa leaves against 3 mosquito species.

    PubMed

    Jang, Young-Su; Jeon, Ju-Hyun; Lee, Hoi-Seon

    2005-12-01

    Mosqutio larvicidal activity of Chamaecyparis obtusa leaf-derived materials against the 4th-stage larvae of Aedes aegypti (L.), Ochlerotatus togoi (Theobald), and Culex pipiens pallens (Coquillett) was examined in the laboratory. A crude methanol extract of C. obtusa leaves was found to be active (percent mortality rough) against the 3 species larvae; the hexane fraction of the methanol extract showed a strong larvicidal activity (100% mortality) at 100 ppm. The bioactive component in the C. obtusa leaf extract was characterized as beta-thujaplicin by spectroscopic analyses. The LC50 value of beta-thujaplicin was 2.91, 2.60, and 1.33 ppm against Ae. aegypti, Oc. togoi, and Cx. pipiens pallens larvae. This naturally occurring C. obtusa leaves-derived compound merits further study as a potential mosquito larval control agent or lead compound.

  1. [Progress in researches on active constituents and molluscicidal activity of Sapium sebiferum].

    PubMed

    Luo, Kun-shui; He, Yi-chang; Xu, Lin-chu; Huang, Cheng-lin; Sun, Qi-xiang

    2013-10-01

    Sapium sebiferum contains a variety of organic acids, flavonoids and phenolic substances, which were linked with the functions of poisoning Oncomelania. Sapium sebiferum is a good plant material of inhibiting Oncomelania. This paper reviews the variety, resources and active ingredients of Sapium sebiferum, and the researches of Sapium sebiferum inhibiting Oncomelania, and forecasts the development of Sapium sebiferum as an inhibiting Oncomelania forest in order to provide the evidence for its penetrating research and development.

  2. Chemical constituents of Swertia longifolia Boiss. with α-amylase inhibitory activity

    PubMed Central

    Saeidnia, Soodabeh; Ara, Leila; Hajimehdipoor, Homa; Read, Roger W.; Arshadi, Sattar; Nikan, Marjan

    2016-01-01

    α-Amylase inhibitors play a critical role in the control of diabetes and many of medicinal plants have been found to act as α-amylase inhibitors. Swertia genus, belonging to the family Gentianaceae, comprises different species most of which have been used in traditional medicine of several cultures as antidiabetic, anti-pyretic, analgesic, liver and gastrointestinal tonic. Swertia longifolia Boiss. is the only species of Swertia growing in Iran. In the present investigation, phytochemical study of S. longifolia was performed and α-amylase inhibitory effects of the plant fractions and purified compounds were determined. Aerial parts of the plant were extracted with hexane, chloroform, methanol and water, respectively. The components of the hexane and chloroform fractions were isolated by different chromatographic methods and their structures were determined by 1H NMR and 13C NMR data. α-Amylase inhibitory activity was determined by a colorimetric assay using 3,5-dinitro salysilic acid. During phytochemical examination, α-amyrin, β-amyrin and β-sitosterol were purified from the hexane fraction, while ursolic acid, daucosterol and swertiamarin were isolated from chloroform fraction. The results of the biochemical assay revealed α-amylase inhibitory activity of hexane, chloroform, methanol and water fractions, of which the chloroform and methanol fractions were more potent (IC50 16.8 and 18.1 mg/ml, respectively). Among examined compounds, daucosterol was found to be the most potent α-amylase inhibitor (57.5% in concentration 10 mg/ml). With regard to α-amylase inhibitory effects of the plant extracts, purified constituents, and antidiabetic application of the species of Swertia genus in traditional medicine of different countries, S. longifolia seems more appropriate species for further mechanistic antidiabetic evaluations. PMID:27051429

  3. Antimicrobial activity of Calotropis procera Ait. (Asclepiadaceae) and isolation of four flavonoid glycosides as the active constituents.

    PubMed

    Nenaah, Gomah

    2013-07-01

    Antimicrobial activity of solvent extracts and flavonoids of Calotropis procera growing wild in Saudi Arabia was evaluated using the agar well-diffusion method. A bioassay-guided fractionation of the crude flavonoid fraction (Cf3) of MeOH extract which showed the highest antimicrobial activity led to the isolation of four flavonoid glycosides as the bioactive constituents. Structure of compounds have been elucidated using physical and spectroscopic methods including (UV, IR, (1)H, (13)C-NMR, DEPT, 2D (1)H-(1)H COSY, HSQC, HMBC and NOESY). Compounds were found to be the 3-O-rutinosides of quercetin, kaempferol and isorhamnetin, besides the flavonoid 5-hydroxy-3,7-dimethoxyflavone-4'-O-β-glucopyranoside. Most of the isolated extracts showed antimicrobial activity against the test microorganisms, where the crude flavonoid fraction was the most active, diameter of inhibition zones ranged between 15.5 and 28.5 mm against the tested bacterial strains, while reached 30 mm against the fungal Candida albicans. The minimal inhibitory concentrations varied from 0.04 to 0.32 mg/ml against all of the tested microorganisms in case of the crude flavonoid fraction. Quercetin-3-O-rutinoside showed superior activity over the remainder flavonoids. The Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis) were more susceptible than the Gram-negative (Pseudomonas aeruginosa and Salmonella enteritidis) and the yeast species were more susceptible than the filamentous fungi. The study recommend the use of such natural products as antimicrobial biorationals.

  4. Change in chemical constituents and free radical-scavenging activity during Pear (Pyrus pyrifolia) cultivar fruit development.

    PubMed

    Cho, Jeong-Yong; Lee, Sang-Hyun; Kim, Eun Hee; Yun, Hae Rim; Jeong, Hang Yeon; Lee, Yu Geon; Kim, Wol-Soo; Moon, Jae-Hak

    2015-01-01

    Changes in chemical constituent contents and DPPH radical-scavenging activity in fruits of pear (Pyrus pyrifolia) cultivars during the development were investigated. The fruits of seven cultivars (cv. Niitaka, Chuhwangbae, Wonhwang, Hwangkeumbae, Hwasan, Manpungbae, and Imamuraaki) were collected at 15-day intervals after day 20 of florescence. Vitamins (ascorbic acid and α-tocopherol), arbutin, chlorogenic acid, malaxinic acid, total caffeic acid, total flavonoids, and total phenolics were the highest in immature pear fruit on day 20 after florescence among samples at different growth stages. All of these compounds decreased gradually in the fruit during the development. Immature pear fruit on day 35 or 50 after florescence exhibited higher free radical-scavenging activity than that at other times, although activities were slightly different among cultivars. The chemical constituent contents and free radical-scavenging activity were largely different among immature fruits of the pear cultivars, but small differences were observed when they matured.

  5. Jumping the gun: Smoking constituent BaP causes premature primordial follicle activation and impairs oocyte fusibility through oxidative stress

    SciTech Connect

    Sobinoff, A.P.; Pye, V.; Nixon, B.; Roman, S.D.; McLaughlin, E.A.

    2012-04-01

    Benzo(a)pyrene (BaP) is an ovotoxic constituent of cigarette smoke associated with pre-mature ovarian failure and decreased rates of conception in IVF patients. Although the overall effect of BaP on female fertility has been documented, the exact molecular mechanisms behind its ovotoxicity remain elusive. In this study we examined the effects of BaP exposure on the ovarian transcriptome, and observed the effects of in vivo exposure on oocyte dysfunction. Microarray analysis of BaP cultured neonatal ovaries revealed a complex mechanism of ovotoxicity involving a small cohort of genes associated with follicular growth, cell cycle progression, and cell death. Histomorphological and immunohistochemical analysis supported these results, with BaP exposure causing increased primordial follicle activation and developing follicle atresia in vitro and in vivo. Functional analysis of oocytes obtained from adult Swiss mice treated neonatally revealed significantly increased levels of mitochondrial ROS/lipid peroxidation, and severely reduced sperm-egg binding and fusion in both low (1.5 mg/kg/daily) and high (3 mg/kg/daily) dose treatments. Our results reveal a complex mechanism of BaP induced ovotoxicity involving developing follicle atresia and accelerated primordial follicle activation, and suggest short term neonatal BaP exposure causes mitochondrial leakage resulting in reduced oolemma fluidity and impaired fertilisation in adulthood. This study highlights BaP as a key compound which may be partially responsible for the documented effects of cigarette smoke on follicular development and sub-fertility. -- Highlights: ► BaP exposure up-regulates canonical pathways linked with follicular growth/atresia. ► BaP causes primordial follicle activation and developing follicle atresia. ► BaP causes oocyte mitochondrial ROS and lipid peroxidation, impairing fertilisation. ► Short term neonatal BaP exposure compromises adult oocyte quality.

  6. Autoignition response of n-butanol and its blend with primary reference fuel constituents of gasoline.

    DOE PAGES

    Kumar, Kamal; Zhang, Yu; Sung, Chi -Jen; ...

    2015-04-13

    We study the influence of blending n-butanol on the ignition delay times of n-heptane and iso-octane, the primary reference fuels for gasoline. The ignition delay times are measured using a rapid compression machine, with an emphasis on the low-to-intermediate temperature conditions. The experiments are conducted at equivalence ratios of 0.4 and 1.0, for a compressed pressure of 20 bar, with the temperatures at the end of compression ranging from 613 K to 979 K. The effect of n-butanol addition on the development of the two-stage ignition characteristics for the two primary reference fuels is also examined. The experimental results aremore » compared to predictions obtained using a detailed chemical kinetic mechanism, which has been obtained by a systematic merger of previously reported base models for the combustion of the individual fuel constituents. In conclusion, a sensitivity analysis on the base, and the merged models, is also performed to understand the dependence of autoignition delay times on the model parameters.« less

  7. Intestinal bacteria activate estrogenic effect of main constituents puerarin and daidzin of Pueraria thunbergiana.

    PubMed

    Park, Eun-Kyung; Shin, Jieun; Bae, Eun-Ah; Lee, Young-Chul; Kim, Dong-Hyun

    2006-12-01

    To understand the relationship between the metabolites and estrogenic activity of the main isoflavones puerarin and daidzin of the rhizome of Pueraria thunbergiana (PT, family Leguminosae), PT and its isoflavones were transformed by human intestinal bacteria and their estrogenic effects were investigated. All human fecal specimens hydrolyzed puerarin and daidzin to daidzein, but their hydrolyzing activities varied depending on the individuals. All intestinal bacteria isolated from human also hydrolyzed daidzin to daidzein, but a few bacteria transformed puerarin to daidzein. When the estrogenic effect of PT, puerarin and daidzin was compared with those of their metabolites, the metabolites more potently increased proliferation of MCF-7 cells than PT, puerarin and daidzin. The metabolite daidzein also potently increased estrogen-response c-fos mRNA and PR protein expressions. These findings suggest that intestinal bacteria, which can hydrolyze puerarin and/or daidzin, may activate a potent estrogenic activity of PT.

  8. A review of current smoke constituent measurement activities and aspects of yield variability.

    PubMed

    Purkis, Stephen W; Meger, Michael; Wuttke, Roland

    2012-02-01

    An increasing number of initiatives to regulate cigarette smoke constituents beyond 'tar', nicotine and carbon monoxide are being launched. The objective of existing and proposed regulation is presumably either to gain a better understanding of product performance, to be able to discriminate between products, or to impose limits for selected constituents. However, without standardized analytical methods and measurement tolerances a meaningful comparison of data or verification against regulated limits is challenging if not impossible. Hence, an understanding of the validity and limitations of generated data is important for industry and regulators alike to avoid unjustified 'out-of-compliance' situations, and consequent competitive and reputational concerns for manufacturers. This paper reviews smoke constituent regulation and provides examples of technical challenges and good practice. It discusses approaches used to standardize measurements; the role of the International Organization for Standardization; factors influencing result variability and limitations and possible misinterpretations of generated data. If smoke constituents regulation is to be introduced, a standardized, science-based approach must be the pre-requisite for the generation and comparison of data. Potential analytical and technical issues must be resolved in discussion, both before and after the implementation of regulation, to the benefit of the public, regulators and manufacturers.

  9. Characterization of volatile constituents of Origanum onites and their antifungal and antibacterical activity

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Essential oils obtained by hydrodistillation (HD) and microwave-assisted hydrodistillaton (MWHD) of Origanum onites aerial parts were analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC/MS). Thirty-one constituents representing 98.6% of the water distilled oil and fifty-...

  10. Idiosyncratic responses of evergreen broad-leaved forest constituents in China to the late Quaternary climate changes

    PubMed Central

    Fan, Dengmei; Hu, Wan; Li, Bo; Morris, Ashley B.; Zheng, Min; Soltis, Douglas E.; Soltis, Pamela S.; Zhang, Zhiyong

    2016-01-01

    Subtropical evergreen broad-leaved forest (EBLF) is one of the most important vegetation types in China. Inferences from palaeo-biome reconstruction (PBR) and phylogeography regarding range shift history of EBLF during the late Quaternary are controversial and should be reconciled. We compared phylogeographic patterns of three EBLF constituents in China, Castanopsis tibetana, Machilus thunbergii and Schima superba. Contrary to a chorus of previous phylogeographic studies and the results of species distribution modelling (SDM) of this study (in situ survival during the LGM), the three species displayed three different phylogeographic patterns that conform to either an in situ survival model or an expansion-contraction model. These results are partially congruent with the inference of PBR that EBLF was absent to the north of 24° N at the LGM. This study suggests that the constituents of EBLF could have responded idiosyncratically to climate changes during the Late Quaternary. The community assemblages of EBLF could have been changing over time, resulting in no palaeo-analogs to modern-day EBLF, which may be the main reason responsible for the failure of PBR to detect the occurrence of EBLF north of 24° N at the LGM. PMID:27534981

  11. Type II pneumocytes modulate surfactant production in response to cigarette smoke constituents: restoration by vitamins A and E.

    PubMed

    Xue, Yuan; Williams, Tracy L; Li, Ting; Umbehr, Joshua; Fang, Liang; Wang, Weiqun; Baybutt, Richard C

    2005-12-01

    This study was to evaluate the effects of cigarette smoke constituents upon type II pneumocyte surfactant production in vitro, and how vitamins A and E may alter the response. Freshly isolated type II pneumocytes from Sprague-Dawley rats were incubated 20 h in medium with fetal bovine serum that was or was not treated with cigarette smoke. The number of adherent cells was inversely related to the dose of smoke or benzo(a)pyrene. Despite the decreased number of treated cells, the total amount of surfactant per culture well was unchanged, whereas surfactant production per cell was significantly increased (P<0.05). Vitamin A concentration was significantly (P<0.05) lower in the smoke-treated serum compared with untreated serum. When vitamin A or E was added to the cigarette smoke-treated serum, cell adherence and surfactant production returned to control values. In conclusion, cigarette smoke constituents or benzo(a)pyrene alone decreased the number of adherent type II pneumocytes, but did not alter surfactant amounts because of an increased production of surfactant per cell. Type II pneumocytes seem to adjust surfactant production dependent upon the number of type II pneumocytes to produce it and vitamin A or E enhance cell attachment in the presence of the smoke toxins.

  12. Trypanocidal constituents in plants 5. Evaluation of some Mexican plants for their trypanocidal activity and active constituents in the seeds of Persea americana.

    PubMed

    Abe, Fumiko; Nagafuji, Shinya; Okawa, Masafumi; Kinjo, Junei; Akahane, Hiroshige; Ogura, Tetsuya; Martinez-Alfaro, Miguel Angel; Reyes-Chilpa, Ricardo

    2005-07-01

    Crude extracts of Mexican medicinal plants were screened for trypanocidal activity against Trypanosoma cruzi, which is the etiological agent for Chagas' disease, one of the most serious protozoan diseases in Latin America. There were 71 kinds of methanolic and other organic extracts from 65 plants, which were newly examined by a preliminary screening test to observe immobilization of epimastigotes and trypomastigotes of T. cruzi in vitro. The MeOH extract of seeds of Persea americana (avocado) showed moderate activity against epimastigotes. In order to identify the principal compounds for the activity, the MeOH extract was subjected to bioassay-guided fractionation. From the active fractions, six 1,2,4-trihydroxyheptadecane derivatives and two 1,2,4-trihydroxynonadecane derivatives including a new one were isolated. These compounds showed moderate activity against epimastigotes and trypomastigotes.

  13. Therapeutics Role of Azadirachta indica (Neem) and Their Active Constituents in Diseases Prevention and Treatment.

    PubMed

    Alzohairy, Mohammad A

    2016-01-01

    Neem (Azadirachta indica) is a member of the Meliaceae family and its role as health-promoting effect is attributed because it is rich source of antioxidant. It has been widely used in Chinese, Ayurvedic, and Unani medicines worldwide especially in Indian Subcontinent in the treatment and prevention of various diseases. Earlier finding confirmed that neem and its constituents play role in the scavenging of free radical generation and prevention of disease pathogenesis. The studies based on animal model established that neem and its chief constituents play pivotal role in anticancer management through the modulation of various molecular pathways including p53, pTEN, NF-κB, PI3K/Akt, Bcl-2, and VEGF. It is considered as safe medicinal plants and modulates the numerous biological processes without any adverse effect. In this review, I summarize the role of Azadirachta indica in the prevention and treatment of diseases via the regulation of various biological and physiological pathways.

  14. Therapeutics Role of Azadirachta indica (Neem) and Their Active Constituents in Diseases Prevention and Treatment

    PubMed Central

    Alzohairy, Mohammad A.

    2016-01-01

    Neem (Azadirachta indica) is a member of the Meliaceae family and its role as health-promoting effect is attributed because it is rich source of antioxidant. It has been widely used in Chinese, Ayurvedic, and Unani medicines worldwide especially in Indian Subcontinent in the treatment and prevention of various diseases. Earlier finding confirmed that neem and its constituents play role in the scavenging of free radical generation and prevention of disease pathogenesis. The studies based on animal model established that neem and its chief constituents play pivotal role in anticancer management through the modulation of various molecular pathways including p53, pTEN, NF-κB, PI3K/Akt, Bcl-2, and VEGF. It is considered as safe medicinal plants and modulates the numerous biological processes without any adverse effect. In this review, I summarize the role of Azadirachta indica in the prevention and treatment of diseases via the regulation of various biological and physiological pathways. PMID:27034694

  15. Potential of garlic and its active constituent, S-allyl cysteine, as antihypertensive and cardioprotective in presence of captopril.

    PubMed

    Asdaq, S M; Inamdar, M N

    2010-11-01

    . SACS in low dose was less effective than low dose of FGH; similarly, high dose of FGH was more efficacious than high dose of SACS. Corroborating with this, combined therapy of garlic (250 mg/kg) with CAP demonstrated higher synergistic action than combination of SACS (0.222 mg/kg) with CAP suggesting the role of additional bioactive constituents apart from SACS, responsible for therapeutic efficacy of garlic. Moreover, combination of SACS and CAP exerted super-additive (synergistic) interaction with respect to fall in blood pressure and ACE inhibition. This study may represent an advertence on concomitant use of garlic or its bioactive constituent, SACS, with captopril.

  16. Matrix metalloproteinase-1 inhibitory activities of Morinda citrifolia seed extract and its constituents in UVA-irradiated human dermal fibroblasts.

    PubMed

    Masuda, Megumi; Murata, Kazuya; Naruto, Shunsuke; Uwaya, Akemi; Isami, Fumiyuki; Matsuda, Hideaki

    2012-01-01

    The objective of this study was to examine whether a 50% ethanolic extract (MCS-ext) of the seeds of Morinda citrifolia (noni) and its constituents have matrix metalloproteinase-1 (MMP-1) inhibitory activity in UVA-irradiated normal human dermal fibroblasts (NHDFs). The MCS-ext (10 μg/mL) inhibited MMP-1 secretion from UVA-irradiated NHDFs, without cytotoxic effects, at 48 h after UV exposure. The ethyl acetate-soluble fraction of MCS-ext was the most potent inhibitor of MMP-1 secretion. Among the constituents of the fraction, a lignan, 3,3'-bisdemethylpinoresinol (1), inhibited the MMP-1 secretion at a concentration of 0.3 μM without cytotoxic effects. Furthermore, 1 (0.3 μM) reduced the level of intracellular MMP-1 expression. Other constituents, namely americanin A (2), quercetin (3) and ursolic acid (4), were inactive. To elucidate inhibition mechanisms of MMP-1 expression and secretion, the effect of 1 on mitogen-activated protein kinases (MAPKs) phosphorylation was examined. Western blot analysis revealed that 1 (0.3 μM) reduced the phosphorylations of p38 and c-Jun-N-terminal kinase (JNK). These results suggested that 1 suppresses intracellular MMP-1 expression, and consequent secretion from UVA-irradiated NHDFs, by down-regulation of MAPKs phosphorylation.

  17. Lipid constituents of the edible mushroom, Pleurotus giganteus demonstrate anti-Candida activity.

    PubMed

    Phan, Chia-Wei; Lee, Guan-Serm; Macreadie, Ian G; Malek, Sri Nurestri Abd; Pamela, David; Sabaratnam, Vikineswary

    2013-12-01

    Different solvent extracts of Pleurotus giganteus fruiting bodies were tested for antifungal activities against Candida species responsible for human infections. The lipids extracted from the ethyl acetate fraction significantly inhibited the growth of all the Candida species tested. Analysis by GC/MS revealed lipid components such as fatty acids, fatty acid methyl esters, ergosterol, and ergosterol derivatives. The sample with high amounts of fatty acid methyl esters was the most effective antifungal agent. The samples were not cytotoxic to a mammalian cell line, mouse embryonic fibroblasts BALB/c 3T3 clone A31. To our knowledge, this is the first report of antifungal activity of the lipid components of Pleurotus giganteus against Candida species.

  18. Effect of Crocus sativus extracts and its active constituent safranal on the harmaline-induced tremor in mice

    PubMed Central

    Amin, Bahareh; Malekzadeh, Mahshad; Heidari, Mahmoud Reza; Hosseinzadeh, Hossein

    2015-01-01

    Objective(s): Due to unsatisfactory response or intolerable side effects of current drugs, treatment of essential tremor remains inadequate. Thus, we aimed to investigate the protective and therapeutic effects of aqueous and ethanolic extracts of Crocus sativus (saffron), and its active consistent, safranal, on the harmaline-induced tremor in mice. Materials and Methods: To induce tremor, harmaline (30 mg/kg) was injected intraperitoneally. Test groups were also given the aqueous and ethanolic extracts of saffron (40, 80, and 160 mg/kg) as well as safranal (0.1, 0.3, and 0.5 ml/kg), intraperitoneally, 10 min before harmaline administration (prophylactic study) or 10 min after the onset of tremors (curative study). The latency of onset, duration, and intensity of tremor were recorded. Results: The extracts (80 and160 mg/kg) dose dependently attenuated duration of harmaline-induced tremors as did reference drug, propranolol (2 and 5 mg/kg). Only the highest dose of extracts (160 mg/kg) attenuated intensity of harmaline-induced tremors throughout the study. Safranal at the doses of (0.1 and 0.3 ml/kg) but not 0.5 ml/kg attenuated duration and intensity of tremor. Onset of tremor increased with the extracts (80 and 160 mg/kg) in prophylactic study, as the effect observed with propranolol at the dose of 5 mg/kg. Safranal did not affect the latency of tremor. Conclusion: Both aqueous and ethanolic extracts of saffron and with a less effect, low doses of safranal, have relatively protective and suppressive effects on the harmaline-induced tremor and different constituents of extracts seem to participate in the protective effects against harmaline induced tremor. PMID:26124930

  19. Phytochemical Constituents and Antioxidant and Antimicrobial Activity of Selected Plants Used Traditionally as a Source of Food.

    PubMed

    Tabit, Frederick Tawi; Komolafe, Naomi Tope; Tshikalange, Thilivhali Emmanuel; Nyila, Monde Alfred

    2016-03-01

    Many indigenous plants have also been used as a source of food and medicine in many African rural communities in the past. The study investigated the antimicrobial activity, phytochemical constituent, and antioxidant activity of selected traditional plants used traditionally as a source of food and medicine. The methanol and water extracts of different plant parts were analyzed for phytochemicals using standard phytochemical screening reagents while the broth microdilution assays were used to analyze antimicrobial activities. Alkaloids, phenols, flavonoids, saponins, tannins, and terpenes were found in one or more of the plant extracts, and all the plant extracts demonstrated scavenging activities. The back extracts of Sclerocarya birrea and the leaf extracts of Garcinia livingstonei exhibit the best antioxidant activities, while the water and methanol back extracts of S. birrea and G. livingstonei were the most active against all the tested foodborne bacteria.

  20. Estrogenic activity of constituents of underarm deodorants determined by E-Screen assay.

    PubMed

    Lange, Claudia; Kuch, Bertram; Metzger, Jörg W

    2014-08-01

    The purpose of this study was to ascertain whether different kinds of underarm deodorants commercially available in Germany might contain substances with estrogenic potential which after use enter the aquatic environment via wastewater. Twenty five deodorants produced by ten different manufacturers in the form of sprays, roll-ons and sticks were investigated using an in vitro-test system (E-Screen assay) for the determination of estrogenic activity based on the human breast cancer cell line MCF-7. Seven out of ten spray deodorant samples showed a quantifiable estrogenic activity. In the case of the sticks and roll-ons it was only one out of six and one out of nine, respectively. The 17β-estradiol equivalent concentrations (EEQs) of the samples ranged from 0.1 ng g(-1) to 9 ng g(-1) deodorant. Spray deodorant samples showed the highest activities in the E-Screen assay compared to the stick and roll-on deodorants. In order to identify substances possibly contributing to the observed biological activity the samples were additionally analyzed by GC/MS. The obtained results of this non-target screening led to the selection of 62 single substances present in the deodorants which for their part were analyzed by E-Screen assay. Eight of these single substances, all of them fragrances, showed estrogenic effects with estradiol equivalence factors (EEFs) similar to parabens, a group of 4-hydroxybenzoic acid esters commonly used as preservatives in personal care products, which are known to have a slight estrogenic effect. Thus, these fragrances are obviously responsible to a substantial degree for the observed estrogenic activity of the deodorants.

  1. Modeling of the effect of freezer conditions on the principal constituent parameters of ice cream by using response surface methodology.

    PubMed

    Inoue, K; Ochi, H; Taketsuka, M; Saito, H; Sakurai, K; Ichihashi, N; Iwatsuki, K; Kokubo, S

    2008-05-01

    A systematic analysis was carried out by using response surface methodology to create a quantitative model of the synergistic effects of conditions in a continuous freezer [mix flow rate (L/h), overrun (%), cylinder pressure (kPa), drawing temperature ( degrees C), and dasher speed (rpm)] on the principal constituent parameters of ice cream [rate of fat destabilization (%), mean air cell diameter (mum), and mean ice crystal diameter (mum)]. A central composite face-centered design was used for this study. Thirty-one combinations of the 5 above-mentioned freezer conditions were designed (including replicates at the center point), and ice cream samples were manufactured and examined in a continuous freezer under the selected conditions. The responses were the 3 variables given above. A quadratic model was constructed, with the freezer conditions as the independent variables and the ice cream characteristics as the dependent variables. The coefficients of determination (R(2)) were greater than 0.9 for all 3 responses, but Q(2), the index used here for the capability of the model for predicting future observed values of the responses, was negative for both the mean ice crystal diameter and the mean air cell diameter. Therefore, pruned models were constructed by removing terms that had contributed little to the prediction in the original model and by refitting the regression model. It was demonstrated that these pruned models provided good fits to the data in terms of R(2), Q(2), and ANOVA. The effects of freezer conditions were expressed quantitatively in terms of the 3 responses. The drawing temperature ( degrees C) was found to have a greater effect on ice cream characteristics than any of the other factors.

  2. Antimutagenic constituents of adlay (Coix lachryma-jobi L. var. ma-yuen Stapf) with potential cancer chemopreventive activity.

    PubMed

    Chen, Huang-Hui; Chiang, Wenchang; Chang, Jang-Yang; Chien, Ya-Lin; Lee, Ching-Kuo; Liu, Ko-Jiunn; Cheng, Yen-Ting; Chen, Ting-Fang; Kuo, Yueh-Hsiung; Kuo, Ching-Chuan

    2011-06-22

    Adlay has long been used in traditional Chinese medicine and as a nourishing food. The acetone extract of adlay hull had previously been demonstrated to possess potent antimutagenic activity. The aims of this study were to identify the antimutagenic constituents from adlay hull by using Ames antimutagenic activity-guide isolation procedures and to investigate their chemopreventive efficacies in cultured cells. The results demonstrated that six compounds showing great antimutagenic activity were identified by spectroscopic methods and by comparison with authentic samples to be p-hydroxybenzaldehyde, vanillin, syringaldehyde, trans-coniferylaldehyde, sinapaldehyde, and coixol. Two of them, trans-coniferylaldehyde and sinapaldehyde, exhibit relatively potent scavenging of DPPH radicals, inhibit TPA stimulated superoxide anion generation in neutrophil-like leukocytes, and induce Nrf2/ARE-driven luciferase activity in HSC-3 cells. Moreover, trans-coniferylaldehyde possesses cytoprotective efficacy against tert-butyl hydroperoxide-induced DNA double-strand breaks in cultured cells, and the chemopreventive potency induced by trans-coniferylaldehyde may be through the activation of kinase signals, including p38, ERK1/2, JNK, MEK1/2, and MSK1/2. In summary, we first identified six antimutagenic constituents from adlay hull. Among them, trans-coniferylaldehyde would be a highly promising agent for cancer chemoprevention and merits further investigation.

  3. Anacardic Acid Constituents from Cashew Nut Shell Liquid: NMR Characterization and the Effect of Unsaturation on Its Biological Activities

    PubMed Central

    Morais, Selene M.; Silva, Katherine A.; Araujo, Halisson; Vieira, Icaro G.P.; Alves, Daniela R.; Fontenelle, Raquel O.S.; Silva, Artur M.S.

    2017-01-01

    Anacardic acids are the main constituents of natural cashew nut shell liquid (CNSL), obtained via the extraction of cashew shells with hexane at room temperature. This raw material presents high technological potential due to its various biological properties. The main components of CNSL are the anacardic acids, salicylic acid derivatives presenting a side chain of fifteen carbon atoms with different degrees of unsaturation (monoene–15:1, diene–15:2, and triene–15:3). Each constituent was isolated by column chromatography using silica gel impregnated with silver nitrate. The structures of the compounds were characterized by nuclear magnetic resonance through complete and unequivocal proton and carbon assignments. The effect of the side chain unsaturation was also evaluated in relation to antioxidant, antifungal and anticholinesterase activities, and toxicity against Artemia salina. The triene anacardic acid provided better results in antioxidant activity assessed by the inhibition of the free radical 1,1-diphenyl-2-picrylhydrazyl (DPPH), higher cytotoxicity against A. salina, and acetylcholinesterase (AChE) inhibition. Thus, increasing the unsaturation of the side chain of anacardic acid increases its action against free radicals, AChE enzyme, and A. salina nauplii. In relation to antifungal activity, an inverse result was obtained, and the linearity of the molecule plays an important role, with monoene being the most active. In conclusion, the changes in structure of anacardic acids, which cause differences in polarity, contribute to the increase or decrease in the biological activity assessed. PMID:28300791

  4. Anacardic Acid Constituents from Cashew Nut Shell Liquid: NMR Characterization and the Effect of Unsaturation on Its Biological Activities.

    PubMed

    Morais, Selene M; Silva, Katherine A; Araujo, Halisson; Vieira, Icaro G P; Alves, Daniela R; Fontenelle, Raquel O S; Silva, Artur M S

    2017-03-16

    Anacardic acids are the main constituents of natural cashew nut shell liquid (CNSL), obtained via the extraction of cashew shells with hexane at room temperature. This raw material presents high technological potential due to its various biological properties. The main components of CNSL are the anacardic acids, salicylic acid derivatives presenting a side chain of fifteen carbon atoms with different degrees of unsaturation (monoene-15:1, diene-15:2, and triene-15:3). Each constituent was isolated by column chromatography using silica gel impregnated with silver nitrate. The structures of the compounds were characterized by nuclear magnetic resonance through complete and unequivocal proton and carbon assignments. The effect of the side chain unsaturation was also evaluated in relation to antioxidant, antifungal and anticholinesterase activities, and toxicity against Artemia salina. The triene anacardic acid provided better results in antioxidant activity assessed by the inhibition of the free radical 1,1-diphenyl-2-picrylhydrazyl (DPPH), higher cytotoxicity against A. salina, and acetylcholinesterase (AChE) inhibition. Thus, increasing the unsaturation of the side chain of anacardic acid increases its action against free radicals, AChE enzyme, and A. salina nauplii. In relation to antifungal activity, an inverse result was obtained, and the linearity of the molecule plays an important role, with monoene being the most active. In conclusion, the changes in structure of anacardic acids, which cause differences in polarity, contribute to the increase or decrease in the biological activity assessed.

  5. Biofunctional constituent isolated from Citrullus colocynthis fruits and structure-activity relationships of its analogues show acaricidal and insecticidal efficacy.

    PubMed

    Jeon, Ju-Hyun; Lee, Hoi-Seon

    2014-08-27

    The acaricidal and insecticidal potential of the active constituent isolated from Citrullus colocynthis fruits and its structurally related analogues was evaluated by performing leaf disk, contact toxicity, and fumigant toxicity bioassays against Tetranychus urticae, Sitophilus oryzae, and Sitophilus zeamais adults. The active constituent of C. colocynthis fruits was isolated by chromatographic techniques and was identified as 4-methylquinoline on the basis of spectroscopic analyses. To investigate the structure-activity relationships, 4-methylquinoline and its structural analogues were tested against mites and two insect pests. On the basis of the LC50 values, 7,8-benzoquinoline was the most effective against T. urticae. Quinoline, 8-hydroxyquinoline, 2-methylquinoline, 4-methylquinoline, 6-methylquinoline, 8-methylquinoline, and 7,8-benzoquinoline showed high insecticidal activities against S. oryzae and S. zeamais regardless of the application method. These results indicate that introduction of a functional group into the quinoline skeleton and changing the position of the group have an important influence on the acaricidal and insecticidal activities. Furthermore, 4-methylquinoline isolated from C. colocynthis fruits, along with its structural analogues, could be effective natural pesticides for managing spider mites and stored grain weevils.

  6. Depolymerized carrageenan ameliorates growth, physiological attributes, essential oil yield and active constituents of Foeniculum vulgare Mill.

    PubMed

    Hashmi, Nadeem; Khan, M Masroor A; Moinuddin; Idrees, Mohd; Khan, Zeba H; Ali, Akbar; Varshney, Lalit

    2012-09-01

    Irradiated carrageenan (IC) elicits an array of plant defense responses and biological activities in plants. An experiment was carried out in the naturally illuminated conditions of net house in order to assess the effects of foliar spray of IC on agricultural performance of fennel (Foeniculum vulgare Mill.), which is a high-value essential oil bearing medicinal crop used in pharmaceutical, food and cosmetic industries. There were applied four IC concentrations (40, 60, 80 and 100 mg L(-1)) as foliar sprays. Application of IC significantly improved the growth attributes, physiological and biochemical parameters, essential oil yield and the contents of main components of essential oil of fennel. IC applied at 80 mg L(-1) enhanced these parameters maximally. Unirradiated carrageenan and deionized water had no effect on the attributes studied. Moreover, GLC analysis revealed a significant increase in the components of essential oil, viz. fenchone (4.48-7.82%) and anethole (78.38-86.08%) compared to the control.

  7. Effect of substituting increasing levels of organic Zn for inorganic Zn on performance, hematological and serum biochemical constituents, antioxidant status and immune response in rat

    PubMed Central

    Nagalakshmi, D.; Sridhar, K.; Swain, P. S.; Reddy, A. G.

    2016-01-01

    The effect of replacing dietary Zn supplemented from inorganic (ZnCO3) source with organic Zn (Zn methionine; Zn-met) was investigated in 72 rats (98.42 ± 1.483 g) by randomly allotting to 4 diets (6 replicates/diet, 3 rats/replicate). Basal diet was prepared with purified ingredients without Zn. The control diet (AIN-76A) contained 12 ppm of Zn from ZnCO3 (100-I). In the other diets ZnCO3 was replaced with Zn-met at the rates of 50 (50I:50O), 75 (25I:75O) or 100% (100-O). Weekly body weight and daily feed intake were recorded for 14 weeks. Blood was collected by retro-orbital puncture on the 70th and 80th day to determine haematological and various serum biochemical constituents, and antioxidant enzyme activities in haemolysate, respectively. Rats were antigenically challenged with sheep RBC on day 73 to assess humoral immune response (HIR), and on day 95 for cell mediated immune response (CMIR) and rats were sacrificed at the end of rearing period to collect liver, muscle, pancreas and kidneys for Zn estimation and oxidative stress markers in liver. The data were analysed using completely randomized design. Weight gain and feed intake, hematological and serum biochemical constituents, Zn content in organs (except liver) were not influenced by replacing ZnCO3 with Zn-met. Zinc concentrations in the serum and liver were higher (P<0.05) with 50% replacement of ZnCO3 with Zn-met compared to 0 or 100% replacement. Lower (P<0.05) lipid peroxidation and higher (P<0.05) glutathione peroxidase and glutathione reductase activities were observed with 50 and 75% replacement of ZnCO3 with Zn-met compared to 0 or 100% replacement. Protein carbonyls and reduced glutathione in liver were not affected, while TBARS decreased (P<0.05) with substituting Zn-met (50-100%) for ZnCO3. The HIR and CMIR increased with increasing Zn-met supplementation and the highest response was observed with 75-100% replacement of ZnCO3 with Zn-met. It is concluded that replacement of 50 or 75% of Zn

  8. Effect of substituting increasing levels of organic Zn for inorganic Zn on performance, hematological and serum biochemical constituents, antioxidant status and immune response in rat.

    PubMed

    Nagalakshmi, D; Sridhar, K; Swain, P S; Reddy, A G

    2016-01-01

    The effect of replacing dietary Zn supplemented from inorganic (ZnCO3) source with organic Zn (Zn methionine; Zn-met) was investigated in 72 rats (98.42 ± 1.483 g) by randomly allotting to 4 diets (6 replicates/diet, 3 rats/replicate). Basal diet was prepared with purified ingredients without Zn. The control diet (AIN-76A) contained 12 ppm of Zn from ZnCO3 (100-I). In the other diets ZnCO3 was replaced with Zn-met at the rates of 50 (50I:50O), 75 (25I:75O) or 100% (100-O). Weekly body weight and daily feed intake were recorded for 14 weeks. Blood was collected by retro-orbital puncture on the 70th and 80th day to determine haematological and various serum biochemical constituents, and antioxidant enzyme activities in haemolysate, respectively. Rats were antigenically challenged with sheep RBC on day 73 to assess humoral immune response (HIR), and on day 95 for cell mediated immune response (CMIR) and rats were sacrificed at the end of rearing period to collect liver, muscle, pancreas and kidneys for Zn estimation and oxidative stress markers in liver. The data were analysed using completely randomized design. Weight gain and feed intake, hematological and serum biochemical constituents, Zn content in organs (except liver) were not influenced by replacing ZnCO3 with Zn-met. Zinc concentrations in the serum and liver were higher (P<0.05) with 50% replacement of ZnCO3 with Zn-met compared to 0 or 100% replacement. Lower (P<0.05) lipid peroxidation and higher (P<0.05) glutathione peroxidase and glutathione reductase activities were observed with 50 and 75% replacement of ZnCO3 with Zn-met compared to 0 or 100% replacement. Protein carbonyls and reduced glutathione in liver were not affected, while TBARS decreased (P<0.05) with substituting Zn-met (50-100%) for ZnCO3. The HIR and CMIR increased with increasing Zn-met supplementation and the highest response was observed with 75-100% replacement of ZnCO3 with Zn-met. It is concluded that replacement of 50 or 75% of Zn

  9. Cardiopulmonary responses of intratracheally instilled tire particles and constituent metal components

    USGS Publications Warehouse

    Gottipolu, R.R.; Landa, E.R.; Schladweiler, M.C.; McGee, J.K.; Ledbetter, A.D.; Richards, J.H.; Wallenborn, G.J.; Kodavanti, U.P.

    2008-01-01

    Tire and brake wear particles contain transition metals, and contribute to near-road PM. We hypothesized that acute cardiopulmonary injury from respirable tire particles (TP) will depend on the amount of soluble metals. Respirable fractions of two types of TP (TP1 and TP2) were analyzed for water and acid-leachable metals using ICP-AES. Both TP types contained a variety of transition metals, including zinc (Zn), copper (Cu), aluminum, and iron. Zn and Cu were detected at high levels in water-soluble fractions (TP2 > TP1). Male Wistar Kyoto rats (12-14 wk) were intratracheally instilled, in the first study, with saline, TP1 or TP2 (5 mg/kg), and in the second study, with soluble Zn, Cu (0.5 ??mol/kg), or both. Pulmonary toxicity and cardiac mitochondrial enzymes were analyzed 1 d, 1 wk, or 4 wk later for TP and 4 or 24 h later for metals. Increases in lavage fluid markers of inflammation and injury were observed at d 1 (TP2 > TP1), but these changes reversed by wk 1. No effects on cardiac enzymes were noted with either TP. Exposure of rats to soluble Zn and Cu caused marked pulmonary inflammation and injury but temporal differences were apparent (Cu effects peaked at 4 h and Zn at 24 h). Instillation of Zn, Cu, and Zn+ Cu decreased the activity of cardiac aconitase, isocitrate dehydrogenase, succinate dehydrogenase, cytochrome-c-oxidase and superoxide dismutase suggesting mitochondrial oxidative stress. The observed acute pulmonary toxicity of TP could be due to the presence of water soluble Zn and Cu. At high concentrations these metals may induce cardiac oxidative stress. Copyright ?? Informa Healthcare USA, Inc.

  10. Studies on the constituents of seeds of Pachyrrhizus erosus and their anti herpes simplex virus (HSV) activities.

    PubMed

    Phrutivorapongkul, Ampai; Lipipun, Vimolmas; Ruangrungsi, Nijsiri; Watanabe, Toshiko; Ishikawa, Tsutomu

    2002-04-01

    Studies on the chemical constituents of the seeds of Pachyrrhizus erosus (Leguminosae) resulted in the isolation of nine known components: five rotenoids [dolineone (3), pachyrrhizone (5), 12a-hydroxydolineone (7), 12a-hydroxypachyrrhizone (9), and 12a-hydroxyrotenone (2)], two isoflavonoids [neotenone (4) and dehydroneotenone (8)], one phenylfuranocoumarin [pachyrrhizine (6)], and a monosaccharide (dulcitol). The full 1H- and 13C-NMR assignments for the isolated products except a sugar, including revision of previous assignments in the literature, are reported. Moderate anti herpes simplex virus (HSV) activity was observed in 12a-hydroxydolineone (7) and 12a-hydroxypachyrrhizone (9) among the isolated products.

  11. The Role of Nigella sativa and Its Active Constituents in Learning and Memory

    PubMed Central

    Sahak, Mohamad Khairul Azali; Kabir, Nurul; Abbas, Ghulam; Draman, Suhaimi; Hashim, Noor Hashida; Hasan Adli, Durriyyah Sharifah

    2016-01-01

    The loss of the ability for learning and memory is a prominent feature of dementia, which affects millions of individuals all over the world, due to either neurodegenerative diseases or brain injury. Although a lot of information is known about the pathology involved, treatment remains elusive at best. The Black Seed of Nigella sativa has been historically and religiously used for thousands of years for preventing and treating many different kinds of diseases. This review article looks at Nigella sativa and its potential role in facilitating learning and memory. The possible use of this seed's extract or compounds isolated from it, such as thymoquinone, for treating damaged brain neural tissue is discussed. The evidence presented in this paper appears to be supporting the hypothesis that this plant and/or its bioactive constituents can enhance learning and memory in health and disease in animals and humans. PMID:27022403

  12. Polar Constituents, Essential Oil and Antioxidant Activity of Marsh Woundwort (Stachys palustris L.).

    PubMed

    Venditti, Alessandro; Frezza, Claudio; Bianco, Armandodoriano; Serafini, Mauro; Cianfaglione, Kevin; Nagy, David U; Iannarelli, Romilde; Caprioli, Giovanni; Maggi, Filippo

    2016-12-10

    Stachys palustris, well-known as marsh woundwort, is a perennial herb growing in wet environments of Europe. Its tubers, leaves and seeds are eaten raw or cooked. Alike other Stachys species, the plant is also used as a traditional remedy. Despite S. palustris has been consumed for centuries, little is known about its chemical constituents. In this work the main secondary metabolites of S. palustris from Hungary and France have been analysed. From the plant ethanolic extracts, ethanoid glucosides, isoscutellarein derivatives, caffeoyl-quinic acids and iridoids have been isolated and structurally characterized by NMR. The essential oils were analysed by GC/MS and showed (E)-phytol, fatty acids and carbonylic compounds as the most abundant compounds. The radical scavenging capacity of plant ethanolic extracts, as evaluated by the DPPH assay, was noteworthy, with IC50 values of 92.08 - 105.42 μg/ml.

  13. Effects of the active constituents of Crocus Sativus L., crocins, in an animal model of obsessive-compulsive disorder.

    PubMed

    Georgiadou, G; Tarantilis, P A; Pitsikas, N

    2012-10-18

    Crocins are among the active components of the plant Crocus Sativus L. C. Sativus L. and its constituents were effective in different models of psychiatric disorders including anxiety and depression. Obsessive-compulsive disorder (OCD) is a common psychiatric disorder defined by the presence of obsessive thoughts and repetitive compulsive actions. The non selective serotonin (5-HT) receptor agonist mCPP is known to induce OCD-like behavior (excessive self-grooming) in rodents and exacerbate symptoms in patients with OCD. The present study investigated whether or not crocins were able to counteract excessive self-grooming induced by mCPP (0.6 mg/kg, i.p.) in rats. Crocins (30 and 50mg/kg, i.p.) attenuated mCPP-induced excessive self-grooming. The present results also indicate that these effects of crocins on an animal model of OCD cannot be attributed to changes in locomotor activity. Our findings suggest that the active constituents of C. Sativus L. crocins might play a role in compulsive behavior and support a functional interaction between crocins and the serotonergic system.

  14. Rapid discovery and identification of anti-inflammatory constituents from traditional Chinese medicine formula by activity index, LC-MS, and NMR

    PubMed Central

    Wang, Shufang; Wang, Haiqiang; Liu, Yining; Wang, Yi; Fan, Xiaohui; Cheng, Yiyu

    2016-01-01

    The traditional activity-guided approach has the shortcoming of low accuracy and efficiency in discovering active compounds from TCM. In this work, an approach was developed by integrating activity index (AI), liquid chromatography – mass spectrometry (LC-MS), and nuclear magnetic resonance (NMR) to rapidly predict and identify the potential active constituents from TCM. This approach was used to discover and identify the anti-inflammatory constituents from a TCM formula, Gui-Zhi-Jia-Shao-Yao-Tang (GZJSYT). The AI results indicated that, among the 903 constituents detected in GZJSYT by LC-MS, 61 constituents with higher AI values were very likely to have anti-inflammatory activities. And eight potential active constituents of them were isolated and validated to have significant inhibitory effects against NO production on LPS-induced RAW 264.7 cell model. Among them, glycyrrhisoflavone (836), glisoflavanone (893) and isoangustone A (902) were reported to have anti-inflammatory effects for the first time. The proposed approach could be generally applicable for rapid and high efficient discovery of anti-inflammatory constituents from other TCM formulae or natural products. PMID:27499135

  15. DIFFERENTIAL GENE EXPRESSION PROFILES IN RAT TRACHAEL EPITHELIAL (RTE) CELLS IN RESPONSE TO COMBUSTION-SOURCE PARTICULATE MATTER (PM) AND VANADIUM (V) A PRIMARY METAL CONSTITUENT

    EPA Science Inventory

    Differential gene expression profiles in rat tracheal epithelial (RTE) cells in response to combustion-source particulate matter (PM) and vanadium (V) a primary metal constituent
    Srikanth S. Nadadur, Janice A. Dye and Daniel L. Costa, US EPA, ORD, NHEERL (ETD, Pulmonary Toxico...

  16. In Silico and In Vitro Analysis of Bacoside A Aglycones and Its Derivatives as the Constituents Responsible for the Cognitive Effects of Bacopa monnieri

    PubMed Central

    Ramasamy, Seetha; Chin, Sek Peng; Sukumaran, Sri Devi; Buckle, Michael James Christopher; Kiew, Lik Voon; Chung, Lip Yong

    2015-01-01

    Bacopa monnieri has been used in Ayurvedic medicine to improve memory and cognition. The active constituent responsible for its pharmacological effects is bacoside A, a mixture of dammarane-type triterpenoid saponins containing sugar chains linked to a steroid aglycone skeleton. Triterpenoid saponins have been reported to be transformed in vivo to metabolites that give better biological activity and pharmacokinetic characteristics. Thus, the activities of the parent compounds (bacosides), aglycones (jujubogenin and pseudojujubogenin) and their derivatives (ebelin lactone and bacogenin A1) were compared using a combination of in silico and in vitro screening methods. The compounds were docked into 5-HT1A, 5-HT2A, D1, D2, M1 receptors and acetylcholinesterase (AChE) using AutoDock and their central nervous system (CNS) drug-like properties were determined using Discovery Studio molecular properties and ADMET descriptors. The compounds were screened in vitro using radioligand receptor binding and AChE inhibition assays. In silico studies showed that the parent bacosides were not able to dock into the chosen CNS targets and had poor molecular properties as a CNS drug. In contrast, the aglycones and their derivatives showed better binding affinity and good CNS drug-like properties, were well absorbed through the intestines and had good blood brain barrier (BBB) penetration. Among the compounds tested in vitro, ebelin lactone showed binding affinity towards M1 (Ki = 0.45 μM) and 5-HT2A (4.21 μM) receptors. Bacoside A and bacopaside X (9.06 μM) showed binding affinity towards the D1 receptor. None of the compounds showed any inhibitory activity against AChE. Since the stimulation of M1 and 5-HT2A receptors has been implicated in memory and cognition and ebelin lactone was shown to have the strongest binding energy, highest BBB penetration and binding affinity towards M1 and 5-HT2A receptors, we suggest that B. monnieri constituents may be transformed in vivo to the

  17. In Silico and In Vitro Analysis of Bacoside A Aglycones and Its Derivatives as the Constituents Responsible for the Cognitive Effects of Bacopa monnieri.

    PubMed

    Ramasamy, Seetha; Chin, Sek Peng; Sukumaran, Sri Devi; Buckle, Michael James Christopher; Kiew, Lik Voon; Chung, Lip Yong

    2015-01-01

    Bacopa monnieri has been used in Ayurvedic medicine to improve memory and cognition. The active constituent responsible for its pharmacological effects is bacoside A, a mixture of dammarane-type triterpenoid saponins containing sugar chains linked to a steroid aglycone skeleton. Triterpenoid saponins have been reported to be transformed in vivo to metabolites that give better biological activity and pharmacokinetic characteristics. Thus, the activities of the parent compounds (bacosides), aglycones (jujubogenin and pseudojujubogenin) and their derivatives (ebelin lactone and bacogenin A1) were compared using a combination of in silico and in vitro screening methods. The compounds were docked into 5-HT1A, 5-HT2A, D1, D2, M1 receptors and acetylcholinesterase (AChE) using AutoDock and their central nervous system (CNS) drug-like properties were determined using Discovery Studio molecular properties and ADMET descriptors. The compounds were screened in vitro using radioligand receptor binding and AChE inhibition assays. In silico studies showed that the parent bacosides were not able to dock into the chosen CNS targets and had poor molecular properties as a CNS drug. In contrast, the aglycones and their derivatives showed better binding affinity and good CNS drug-like properties, were well absorbed through the intestines and had good blood brain barrier (BBB) penetration. Among the compounds tested in vitro, ebelin lactone showed binding affinity towards M1 (Ki = 0.45 μM) and 5-HT2A (4.21 μM) receptors. Bacoside A and bacopaside X (9.06 μM) showed binding affinity towards the D1 receptor. None of the compounds showed any inhibitory activity against AChE. Since the stimulation of M1 and 5-HT2A receptors has been implicated in memory and cognition and ebelin lactone was shown to have the strongest binding energy, highest BBB penetration and binding affinity towards M1 and 5-HT2A receptors, we suggest that B. monnieri constituents may be transformed in vivo to the

  18. Chemical composition of hexane extract of Citrus aurantifolia and anti-Mycobacterium tuberculosis activity of some of its constituents.

    PubMed

    Sandoval-Montemayor, Nallely E; García, Abraham; Elizondo-Treviño, Elizabeth; Garza-González, Elvira; Alvarez, Laura; del Rayo Camacho-Corona, María

    2012-09-19

    The main aim of this study was to isolate and characterize the active compounds from the hexane extract of the fruit peels of Citrus aurantiifolia, which showed activity against one sensitive and three monoresistant (isoniazid, streptomycin or ethambutol) strains of Mycobacterium tuberculosis H37Rv. The active extract was fractionated by column chromatography, yielding the following major compounds: 5-geranyloxypsoralen (1); 5-geranyloxy-7-methoxycoumarin (2); 5,7-dimethoxycoumarin (3); 5-methoxypsoralen (4); and 5,8-dimethoxypsoralen (5). The structures of these compounds were elucidated by 1D and 2D NMR spectroscopy. In addition, GC-MS analysis of the hexane extract allowed the identification of 44 volatile compounds, being 5,7-dimethoxycoumarin (15.79%), 3-methyl-1,2-cyclopentanedione (8.27%), 1-methoxy-ciclohexene (8.0%), corylone (6.93%), palmitic acid (6.89%), 5,8-dimethoxypsoralen (6.08%), a-terpineol (5.97%), and umbelliferone (4.36%), the major constituents. Four isolated coumarins and 16 commercial compounds identified by GC-MS were tested against M. tuberculosis H37Rv and three multidrug-resistant M. tuberculosis strains using the Microplate Alamar Blue Assay. The constituents that showed activity against all strains were 5 (MICs = 25-50 mg/mL), 1 (MICs = 50-100 mg/mL), palmitic acid (MICs = 25-50 mg/mL), linoleic acid (MICs = 50-100 mg/mL), oleic acid (MICs = 100 mg/mL), 4-hexen-3-one (MICs = 50-100 mg/mL), and citral (MICs = 50-100 mg/mL). Compound 5 and palmitic acid were the most active ones. The antimycobacterial activity of the hexane extract of C. aurantifolia could be attributed to these compounds.

  19. Neural activation during response competition

    NASA Technical Reports Server (NTRS)

    Hazeltine, E.; Poldrack, R.; Gabrieli, J. D.

    2000-01-01

    The flanker task, introduced by Eriksen and Eriksen [Eriksen, B. A., & Eriksen, C. W. (1974). Effects of noise letters upon the identification of a target letter in a nonsearch task. Perception & Psychophysics, 16, 143--149], provides a means to selectively manipulate the presence or absence of response competition while keeping other task demands constant. We measured brain activity using functional magnetic resonance imaging (fMRI) during performance of the flanker task. In accordance with previous behavioral studies, trials in which the flanking stimuli indicated a different response than the central stimulus were performed significantly more slowly than trials in which all the stimuli indicated the same response. This reaction time effect was accompanied by increases in activity in four regions: the right ventrolateral prefrontal cortex, the supplementary motor area, the left superior parietal lobe, and the left anterior parietal cortex. The increases were not due to changes in stimulus complexity or the need to overcome previously learned associations between stimuli and responses. Correspondences between this study and other experiments manipulating response interference suggest that the frontal foci may be related to response inhibition processes whereas the posterior foci may be related to the activation of representations of the inappropriate responses.

  20. A Hybrid-Body Containing Constituents of Both P-Bodies and Stress Granules Forms in Response to Hypoosmotic Stress in Saccharomyces cerevisiae

    PubMed Central

    Shah, Khyati H.; Varia, Sapna N.; Cook, Laura A.; Herman, Paul K.

    2016-01-01

    The cytoplasm of the eukaryotic cell is a highly compartmentalized space that contains a variety of ribonucleoprotein (RNP) granules in addition to its complement of membrane-bound organelles. These RNP granules contain specific sets of proteins and mRNAs and form in response to particular environmental and developmental stimuli. Two of the better-characterized of these RNP structures are the stress granule and Processing-body (P-body) that have been conserved from yeast to humans. In this report, we examined the cues regulating stress granule assembly and the relationship between stress granule and P-body foci. These two RNP structures are generally thought to be independent entities in eukaryotic cells. However, we found here that stress granule and P-body proteins were localized to a common or merged granule specifically in response to a hypoosmotic stress. Interestingly, these hybrid-bodies were found to be transient structures that were resolved with time into separate P-body and stress granule foci. In all, these data suggest that the identity of an RNP granule is not absolute and that it can vary depending upon the nature of the induction conditions. Since the activities of a granule are likely influenced by its protein constituency, these observations are consistent with the possibility of RNP granules having distinct functions in different cellular contexts. PMID:27359124

  1. Geomagnetic response to solar activity.

    NASA Technical Reports Server (NTRS)

    Mead, G. D.

    1972-01-01

    The relationship between solar activity and geomagnetic variations is discussed in the light of spacecraft data obtained during the last decade. The effects of centers of solar activity responsible for producing geomagnetic activity on earth are believed to be transmitted through the solar wind, and there is usually a delay of two or three days before the onset of magnetic activity. Attempts to make a one-to-one correspondence between specific solar events and specific magnetic storms, however, are usually unsuccessful, because of the complex and indirect processes linking the two phenomena. Normally, only statistical tendencies can be shown.

  2. Acaricidal activities of some essential oils and their monoterpenoidal constituents against house dust mite, Dermatophagoides pteronyssinus (Acari: Pyroglyphidae)

    PubMed Central

    Saad, El-Zemity; Hussien, Rezk; Saher, Farok; Ahmed, Zaitoon

    2006-01-01

    The acaricidal activities of fourteen essential oils and fourteen of their major monoterpenoids were tested against house dust mites Dermatophagoides pteronyssinus. Five concentrations were used over two different time intervals 24 and 48 h under laboratory conditions. In general, it was noticed that the acaricidal effect based on LC 50 of either essential oils or monoterpenoids against the mite was time dependant. The LC 50 values were decreased by increasing of exposure time. Clove, matrecary, chenopodium, rosemary, eucalyptus and caraway oils were shown to have high activity. As for the monoterpenoids, cinnamaldehyde and chlorothymol were found to be the most effective followed by citronellol. This study suggests the use of the essential oils and their major constituents as ecofriendly biodegradable agents for the control of house dust mite, D. pteronyssinus. PMID:17111463

  3. Activity-guided isolation of constituents of Tephrosia purpurea with the potential to induce the phase II enzyme, quinone reductase.

    PubMed

    Chang, L C; Gerhäuser, C; Song, L; Farnsworth, N R; Pezzuto, J M; Kinghorn, A D

    1997-09-01

    An isoflavone, 7,4'-dihydroxy-3',5'-dimethoxyisoflavone (1), and a chalcone, (+)-tephropurpurin (2), both novel compounds, as well as six constituents of known structure, (+)-purpurin (3), pongamol (4), lanceolatin B (5), (-)-maackiain (6), (-)-3-hydroxy-4-methoxy-8,9-methylene-dioxypterocarpan (7), and (-)-medicarpin (8), were obtained as active compounds from Tephrosia purpurea, using a bioassay based on the induction of quinone reductase (QR) activity with cultured Hepa 1c1c7 mouse hepatoma cells. Additionally, three inactive compounds of known structure, 3'-methoxydaidzein, desmoxyphyllin B, and 3,9-dihydroxy-8-methoxycoumestan, were isolated and identified. The structure elucidation of compounds 1 and 2 was carried out by spectral data interpretation.

  4. Volatile constituents and antioxidant activity of peel, flowers and leaf oils of Citrus aurantium L. growing in Greece.

    PubMed

    Sarrou, Eirini; Chatzopoulou, Paschalina; Dimassi-Theriou, Kortessa; Therios, Ioannis

    2013-09-02

    The volatile constituents of the essential oils of the peel, flower (neroli) and leaves (petitgrain) of bitter orange (Citrus aurantium L.) growing in Greece were studied by GC-MS. The analytical procedures enabled the quantitative determination of 31 components. More specifically, the components of the essential oils identified were: twelve in the peel, twenty-six in the flowers, and twenty and sixteen in old and young leaves, respectively. The major constituents of the different parts of Citrus aurantium L. essential oils were: β-pinene (0.62%-19.08%), limonene (0.53%-94.67%), trans-β-ocimene (3.11%-6.06%), linalool (0.76%-58.21%), and α-terpineol (0.13%-12.89%). The DPPH test demonstrated that the essential oils in the old leaves had the maximum antioxidant activity, followed by the flowers, young leaves and the peel in that order. This study updates the data in the literature on the essential oils of bitter orange, and provides information on the composition of the oils for a further evaluation of this product.

  5. Volatile oil constituents and antibacterial activity of different parts of Falcaria vulgaris Bernh. growing wild in two localities from Iran.

    PubMed

    Shafaghat, A

    2011-02-01

    The chemical composition of essential oils obtained by hydrodistillation from the flower, leaf and stem of Falcaria vulgaris Bernh., which is endemic to Iran, were analysed by GC and GC/MS (samples were from two different localities: A from Ardabil and B from Khalkhal). α-Pinene was the major constituent in all the three oils (flower, leaf and stem) from sample A (43.8%, 33.0% and 50.9%, respectively). The oil of F. vulgaris flower was characterised by a higher amount of β-caryophyllene (25.2%) and 1,8-cineole (12.8%) among the eight components comprising 96.2% of the total oil detected. α-Terpinyl acetate (23.2%) and limonene (14.4%) predominated in the leaf oil. In the oils of sample B, α-pinene (16.1% in the flower oil, 31.5% in the leaf oil and 34.5% in the stem oil) was the major compound. Limonene (14.2%) and germacrene D (32.1%) were also the main constituents found in the leaf oil from sample B. α-Terpinyl acetate (21.9% in the leaf oil) and limonene (29.8% in stem oil) were the other major compounds obtained from this sample. Antibacterial activity was determined by the measurement of growth inhibitory zones.

  6. [Chemical constituents of Myristica fragrans Houttuyn seed and their physiological activities].

    PubMed

    Maeda, Aki; Tanimoto, Shinichi; Abe, Tomo; Kazama, Shunsuke; Tanizawa, Hisayuki; Nomura, Masato

    2008-01-01

    The antioxidative activity of phenylpropanoid compound extracts from nutmeg (Myristica fragragrans Houttuyn) seed was determined. The antioxidant activity was evaluated using the 1,1-diphenyl-2-picrylhydrazyl radical-scavenging method, superoxide disumutase assay, ferric thiocyanate assay, and radical-scavenging effect assay with electron-spin resonance. High antioxidant activity was found in monoterpenoid extracts including terpinene-4-ol (3), alpha-terpineol (4), and 4-allyl-2,6-dimethoxyphenol (12). Compound, 12 expressed particularly high antioxidant activity.

  7. Concentrations of the active constituents of the Tibetan folk medicine Qinjiao (Gentiana sect. Cruciata) within and between taxonomic species across the Qinghai-Tibetan Plateau.

    PubMed

    Zhou, Dangwei; Hou, Qinzheng; Si, Qinwen; Liu, Jianquan; Yang, Huiling

    2010-08-01

    The Tibetan folk medicine Qinjiao is traditionally used to treat various conditions, and its main active constituents comprise four iridoid glycosides, i.e., loganic acid, swertiamarin, gentiopicroside, and sweroside. The traditional crude medicine Qinjiao is derived from the dried roots of three species belonging to Gentiana sect. Cruciata (Gentianaceae) growing in the Qinghai-Tibetan Plateau (QTP). In this study, we determined by HPLC the contents of the four main active constituents in the dried roots collected from 83 localities at different altitudes across the QTP. The material was classified under the seven taxonomic species G. straminea, G. dahurica, G. crassicaulis, G. waltonii, G. officinalis, G. ihassica, and G. macrophylla. Our results suggested that the four constituents were present in the roots of all seven species for all localities, but their concentrations varied greatly within and between species. The level of gentiopicroside revealed to be the most dominant for all examined localities (2.1-12.4 mg/g), and G. macrophylla Pall. contained the highest concentration of all the four constituents at the species level. Except for loganic acid in G. officinalis, there was no significant correlation between the contents of these constituents and the altitude of the sampling localities. These results suggest that all species of all origins can be used as reliable resource for the crude medicine Qinjiao. However, a few species contain higher concentrations of the main active constituents, irrespective of their origin.

  8. Anti-inflammatory activity of constituents isolated from Terminalia chebula ***waiting for publication date

    Technology Transfer Automated Retrieval System (TEKTRAN)

    This study was aimed at the evaluation of the anti-inflammatory activity of twelve compounds isolated from the methanolic extract of fruits of Terminalia chebula. The activity was determined in terms of their ability to inhibit inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in L...

  9. The main constituents of Tulipa systola Stapf. roots and flowers; their antioxidant activities.

    PubMed

    Ibrahim, Mohammed Farhad; Hussain, Faiq Hama Saeed; Zanoni, Giuseppe; Vidari, Giovanni

    2016-12-28

    People living on the mountains of the Kurdistan Region, Iraq make a large use of herbs in the local traditional medicine. Among them, Tulipa systola, which grows under and between rocks, is very popular as an anti-inflammatory remedy and pain-relief. The phytochemical study of an ethanolic extract obtained from flowers and roots of Tulip (T systola Stapf.) afforded three compounds, identified as (+)-1-O-E-feruloyl-3-O-E-p-coumaroylglycerol (1), (+)-6-tuliposide A (2), and (-)-kaempferol-3-O-rutinoside (3). The significant radical scavenging and antioxidant activity of the isolated compounds were evaluated on three tests, by determining the DPPH free radical scavenging activity, the total antioxidant activity and the hydrogen peroxide scavenging activity. Tuliposide A shows potent allergenic activity.

  10. Molluscicidal activity of Aglaia duperreana and the constituents of its twigs and leaves.

    PubMed

    Zhang, Heng; Xu, Han-Hong; Song, Zhi-Jun; Chen, Lin-Yan; Wen, Hao-Ju

    2012-09-01

    The methanol (MeOH) extract of the twigs and leaves of Aglaia duperreana was investigated for its molluscicidal activity against Pomacea canaliculata. The extract was found to exhibit significant molluscicidal activity. The ethyl acetate soluble fraction of the extract showed the most potent molluscicidal activity among different solvent fractions. The bioactivity-guided chemical investigation of the ethyl acetate soluble fraction led to a new triterpenoid along with 15 known compounds. Their structures were elucidated by spectroscopic methods, including one- and two-dimensional nuclear magnetic resonance techniques as well as mass spectroscopic analysis. The molluscicidal activities of compounds 2-16 against P. canaliculata were also investigated. Naringenin trimethyl ether showed significant molluscicidal activity with a median lethal concentration (LC(50)) of 3.9 μg/mL, which was indicated higher potency than the positive control, tea saponin (LC(50)=4.5 μg/mL).

  11. Biological activity and toxicity of the Chinese herb Magnolia officinalis Rehder & E. Wilson (Houpo) and its constituents

    PubMed Central

    Poivre, Mélanie; Duez, Pierre

    2017-01-01

    Traditional Chinese herbal drugs have been used for thousands of years in Chinese pharmacopoeia. The bark of Magnolia officinalis Rehder & E. Wilson, known under the pinyin name “Houpo”, has been traditionally used in Chinese and Japanese medicines for the treatment of anxiety, asthma, depression, gastrointestinal disorders, headache, and more. Moreover, Magnolia bark extract is a major constituent of currently marketed dietary supplements and cosmetic products. Much pharmacological activity has been reported for this herb and its major compounds, notably antioxidant, anti-inflammatory, antibiotic and antispasmodic effects. However, the mechanisms underlying this have not been elucidated and only a very few clinical trials have been published. In vitro and in vivo toxicity studies have also been published and indicate some intriguing features. The present review aims to summarize the literature on M. officinalis bark composition, utilisation, pharmacology, and safety. PMID:28271656

  12. Antibacterial and Anti-Inflammatory Activities of Physalis Alkekengi var. franchetii and Its Main Constituents

    PubMed Central

    Shu, Zunpeng; Xing, Na; Wang, Qiuhong; Li, Xinli; Xu, Bingqing; Li, Zhenyu; Kuang, Haixue

    2016-01-01

    This study was designed to determine whether the 50% EtOH fraction from AB-8 macroporous resin fractionation of a 70% EtOH extract of P. Alkekengi (50-EFP) has antibacterial and/or anti-inflammatory activity both in vivo and in vitro and to investigate the mechanism of 50-EFP anti-inflammatory activity. Additionally, this study sought to define the chemical composition of 50-EFP. Results indicated that 50-EFP showed significant antibacterial activity in vitro and efficacy in vivo. Moreover, 50-EFP significantly reduced nitric oxide (NO), prostaglandin E2 (PGE2), tumor necrosis factor alpha (TNF-α), interleukin 1 (IL-1), and interleukin 6 (IL-6) production in lipopolysaccharide- (LPS-) stimulated THP-1 cells. Nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) (examined at the protein level) in THP-1 cells were suppressed by 50-EFP, which inhibited nuclear translocation of p65. Consistent with this anti-inflammatory activity in vitro, 50-EFP reduced inflammation in both animal models. Finally, seventeen compounds (8 physalins and 9 flavones) were isolated as major components of 50-EFP. Our data demonstrate that 50-EFP has antibacterial and anti-inflammatory activities both in vitro and in vivo. The anti-inflammatory effect appears to occur, at least in part, through the inhibition of nuclear translocation of p65. Moreover, physalins and flavones are probably the active components in 50-EFP that exert antibacterial and anti-inflammatory activities. PMID:27057196

  13. Chemical constituents and insecticidal activities of the essential oil from Amomum tsaoko against two stored-product insects.

    PubMed

    Wang, Ying; You, Chun-Xue; Wang, Cheng-Fang; Yang, Kai; Chen, Ran; Zhang, Wen-Juan; Du, Shu-Shan; Geng, Zhu-Feng; Deng, Zhi-Wei

    2014-01-01

    The aim of this research was to determine the chemical constituents and toxicities of the essential oil derived from Amomum tsaoko Crevost et Lemarie fruits against Tribolium castaneum (Herbst) and Lasioderma serricorne (Fabricius). Essential oil of A. tsaoko was obtained from hydrodistillation and was investigated by gas chromatography-mass spectrometry (GC-MS). GC-MS analysis of the essential oil resulted in the identification of 43 components, of which eucalyptol (23.87%), limonene (22.77%), 2-isopropyltoluene (6.66%) and undecane (5.74%) were the major components. With a further isolation, two active constituents were obtained from the essential oil and identified as eucalyptol and limonene. The essential oil and the two isolated compounds exhibited potential insecticidal activities against two storedproduct insects. Limonene showed pronounced contact toxicity against both insect species (LD50 = 14.97 μg/adult for T. castaneum; 13.66 μg/adult for L. serricorne) and was more toxic than eucalyptol (LD50 = 18.83 μg/adult for T. castaneum; 15.58 μg/adult for L. serricorne). The essential oil acting against the two species of insects showed LD50 values of 16.52 and 6.14 μg/adult, respectively. Eucalyptol also possessed strong fumigant toxicity against both insect species (LC50 = 5.47 mg/L air for T. castaneum; 5.18 mg/L air for L. serricorne) and was more toxic than limonene (LC50 = 6.21 mg/L air for T. castaneum; 14.07 mg/L air for L. serricorne), while the crude essential oil acting against the two species of insects showed LC50 values of 5.85 and 8.70 mg/L air, respectively. These results suggested that the essential oil of A. tsaoko and the two compounds may be used in grain storage to combat insect pests.

  14. Cannabinoid inhibition of adenylate cyclase: relative activity of constituents and metabolites of marihuana.

    PubMed

    Howlett, A C

    1987-05-01

    delta 9Tetrahydrocannabinol (THC) has been shown to inhibit the activity of adenylate cyclase in the N18TG2 clone of murine neuroblastoma cells. The concentration of delta 9THC exhibiting half-maximal inhibition was 500 nM. delta 8Tetrahydrocannabinol was less active, and cannabinol was only partially active. Cannabidiol, cannabigerol, cannabichromene, olivetol and compounds having a reduced length of the C3 alkyl side chain were inactive. The metabolites of delta 8THC and delta 9THC hydroxylated at the C11 position were more potent than the parent drugs. However, hydroxylation at the C8 position of the terpenoid ring resulted in loss of activity. Compounds hydroxylated along the C3 alkyl side chain were equally efficacious but less potent than delta 9THC. These findings are compared to the pharmacology of cannabinoids reported for psychological effects in humans and behavioral effects in a variety of animal models.

  15. Analgesic, anti-inflammatory, and CNS depressant activities of new constituents of Nepeta clarkei.

    PubMed

    Hussain, Javid; Ur Rehman, Najeeb; Hussain, Hidayat; Al-Harrasi, Ahmed; Ali, Liaqat; Rizvi, Tania Shamim; Ahmad, Mansoor; Mehjabeen

    2012-04-01

    Two new pentacyclic triterpenes named kirmanoic acid (1) and kurramanoic acid (2) have been isolated from the chloroform-soluble portion of the whole plant of Nepeta clarkei Hook. The structures of the two new compounds were assigned on the basis of their ¹H and ¹³C NMR spectra including two-dimensional NMR techniques such as COSY, HMQC, and HMBC experiments. Kirmanoic acid (1) was investigated for analgesic, anti-inflammatory, and CNS depressant activities. Interestingly kirmanoic acid (1) showed strong analgesic activity than standard drug in acetic induced writhing and formalin tests. Similarly kirmanoic acid (1) also showed strong anti-inflammatory activity than its standard drug. The gross behavioral study of kirmanoic acid (1) revealed that it exhibited mild CNS stimulant and muscle relaxant in the mice. Compound 1 showed a slight increase in Locomotor activity and possesses the antidepressant effect.

  16. Chemical constituents from the rhizome of Polygonum paleaceum and their antifungal activity.

    PubMed

    Yang, Yi-Xi; An, Mao-Mao; Jin, Yong-Sheng; Chen, Hai-Sheng

    2017-01-01

    A new compounds neopaleaceolactoside (1), along with nine known compounds phyllocoumarin (2), quercetin (3), quercitrin (4), quercetin-3-methyl ether (5), vincetoxicoside B (6), isoquercitrin (7), kaempferol (8), (-)-epicatechin (9), and chlorogenic acid (10), was isolated from Polygonum paleaceum Wall. Their chemical structures were established based on one-dimensional and two-dimensional nuclear magnetic resonance techniques, mass spectrometry and by comparison with spectroscopic data reported. Some selected compounds were screened for their antifungal activity. Quercetin (3), vincetoxicoside B (6), kaempferol (8), and (-)-epicatechin (9) showed synergistic antifungal activities with the FICI values <0.5. A preliminary structure-activity relationship could be observed that free 3-OH in the structure of flavonoids was important for synergistic antifungal activity.

  17. Inhibition of UDP-Glucuronosyltransferases (UGTs) Activity by constituents of Schisandra chinensis.

    PubMed

    Song, Jin-Hui; Cui, Li; An, Li-Bin; Li, Wen-Tao; Fang, Zhong-Ze; Zhang, Yan-Yan; Dong, Pei-Pei; Wu, Xue; Wang, Li-Xuan; Gonzalez, Frank J; Sun, Xiao-Yu; Zhao, De-Wei

    2015-10-01

    Structure-activity relationship for the inhibition of Schisandra chinensis's ingredients toward (Uridine-Diphosphate) UDP-glucuronosyltransferases (UGTs) activity was performed in the present study. In vitro incubation system was employed to screen the inhibition capability of S. chinensis's ingredients, and in silico molecular docking method was carried out to explain possible mechanisms. At 100 μM of compounds, the activity of UGTs was inhibited by less than 90% by schisandrol A, schisandrol B, schisandrin, schisandrin C, schisantherin A, gomisin D, and gomisin G. Schisandrin A exerted strong inhibition toward UGT1A1 and UGT1A3, with the residual activity to be 7.9% and 0% of control activity. Schisanhenol exhibited strong inhibition toward UGT2B7, with the residual activity to be 7.9% of control activity. Gomisin J of 100 μM inhibited 91.8% and 93.1% of activity of UGT1A1 and UGT1A9, respectively. Molecular docking prediction indicated different hydrogen bonds interaction resulted in the different inhibition potential induced by subtle structure alteration among schisandrin A, schisandrin, and schisandrin C toward UGT1A1 and UGT1A3: schisandrin A > schisandrin > schisandrin C. The detailed inhibition kinetic evaluation showed the strong inhibition of gomisin J toward UGT1A9 with the inhibition kinetic parameter (Ki ) to be 0.7 μM. Based on the concentrations of gomisin J in the plasma of the rats given with S. chinensis, high herb-drug interaction existed between S. chinensis and drugs mainly undergoing UGT1A9-mediated metabolism. In conclusion, in silico-in vitro method was used to give the inhibition information and possible inhibition mechanism for S. chinensis's components toward UGTs, which guide the clinical application of S. chinensis.

  18. Trigonelline, a naturally occurring constituent of green coffee beans behind the mutagenic activity of roasted coffee?

    PubMed

    Wu, X; Skog, K; Jägerstad, M

    1997-07-14

    Trigonelline and amino acids are natural components in green coffee beans. Model systems mimicking coffee roasting were used to produce heated samples of trigonelline, amino acids and glucose. Trigonelline and amino acids were heated separately or in combinations for 20 min at 250 degrees C. The results of bacteria mutation assays (Salmonella typhimurium strains TA 98, YG 1024 and YG 1029) showed that trigonelline, alone or in combination with most of the single amino acids and mixtures of amino acids, yielded potent mutagenic activity. Of the singly heated compounds, the highest mutagenic activity was found for trigonelline. The mutagenic activity detected with metabolic activation of the heated trigonelline samples indicated that the mutagenic compounds might be amines; however, higher mutagenic activity was found for trigonelline and its combinations without metabolic activation, which suggests that other types of mutagens (direct-acting) were predominant. High-performance liquid chromatographic analysis of some of the heated samples did not reveal the presence of any known mutagenic heterocyclic amine.

  19. Stellera chamaejasme and its constituents induce cutaneous wound healing and anti-inflammatory activities

    PubMed Central

    Kim, Myungsuk; Lee, Hee Ju; Randy, Ahmad; Yun, Ji Ho; Oh, Sang-Rok; Nho, Chu Won

    2017-01-01

    Stellera chamaejasme L. (Thymelaeaceae) is a perennial herb that is widely used in traditional Chinese medicine to treat tumours, tuberculosis and psoriasis. S. chamaejasme extract (SCE) possesses anti-inflammatory, analgesic and wound healing activities; however, the effect of S. chamaejasme and its active compounds on cutaneous wound healing has not been investigated. We assessed full-thickness wounds of Sprague-Dawley (SD) rats and topically applied SCE for 2 weeks. In vitro studies were performed using HaCaT keratinocytes, Hs68 dermal fibroblasts and RAW 264.7 macrophages to determine cell viability (MTT assay), cell migration, collagen expression, nitric oxide (NO) production, prostaglandin E2 (PGE2) production, inflammatory cytokine expression and β-catenin activation. In vivo, wound size was reduced and epithelisation was improved in SCE-treated SD rats. In vitro, SCE and its active compounds induced keratinocyte migration by regulating the β-catenin, extracellular signal-regulated kinase and Akt signalling pathways. Furthermore, SCE and its active compounds increased mRNA expression of type I and III collagen in Hs68 fibroblasts. SCE and chamechromone inhibited NO and PGE2 release and mRNA expression of inflammatory mediators in RAW 264.7 macrophages. SCE enhances the motility of HaCaT keratinocytes and improves cutaneous wound healing in SD rats. PMID:28220834

  20. Antioxidant and antimicrobial activities of the edible medicinal halophyte Tamarix gallica L. and related polyphenolic constituents.

    PubMed

    Ksouri, Riadh; Falleh, Hanen; Megdiche, Wided; Trabelsi, Najla; Mhamdi, Baya; Chaieb, Kamel; Bakrouf, Amina; Magné, Christian; Abdelly, Chedly

    2009-08-01

    Tamarix gallica is a halophytic species having hepatotonic and stimulant properties, as it was traditionally used in the treatment of various liver disorders. Leaf and flower infusion have anti-inflammatory and anti-diarrheic properties. In this work, we have investigated antioxidant and antimicrobial activities of leaf and flower extracts and their phenolic composition. Results showed that flowers exhibit a higher antioxidant activity as compared to the leaves, IC(50) values of the flower extracts are being 1.3 (beta-carotene bleaching) to 19 times (lipid peroxidation inhibition) lower than those for leaves. Accordingly, flower extracts exhibited the highest total phenolic content (135.35 mgGAE/gDW) and RP-HPLC analysis showed that syringic acid, isoquercitin as well as catechin were the major phenolics. Furthermore, Tamarix extracts showed appreciable antibacterial properties against human pathogen strains. The mean inhibition zone was from 0 to 6.5mm when the concentration increased from 2 to 100mg/l. The strongest activity was recorded against Micrococcus luteus and the lowest activity was observed against Escherichia coli. Moreover, organ extracts show a weakly to moderate activity against the tested Candida. These findings suggest that Tamarix may be considered as an interesting source of antioxidants for therapeutic or nutraceutical industries and for food manufactures.

  1. Stellera chamaejasme and its constituents induce cutaneous wound healing and anti-inflammatory activities.

    PubMed

    Kim, Myungsuk; Lee, Hee Ju; Randy, Ahmad; Yun, Ji Ho; Oh, Sang-Rok; Nho, Chu Won

    2017-02-21

    Stellera chamaejasme L. (Thymelaeaceae) is a perennial herb that is widely used in traditional Chinese medicine to treat tumours, tuberculosis and psoriasis. S. chamaejasme extract (SCE) possesses anti-inflammatory, analgesic and wound healing activities; however, the effect of S. chamaejasme and its active compounds on cutaneous wound healing has not been investigated. We assessed full-thickness wounds of Sprague-Dawley (SD) rats and topically applied SCE for 2 weeks. In vitro studies were performed using HaCaT keratinocytes, Hs68 dermal fibroblasts and RAW 264.7 macrophages to determine cell viability (MTT assay), cell migration, collagen expression, nitric oxide (NO) production, prostaglandin E2 (PGE2) production, inflammatory cytokine expression and β-catenin activation. In vivo, wound size was reduced and epithelisation was improved in SCE-treated SD rats. In vitro, SCE and its active compounds induced keratinocyte migration by regulating the β-catenin, extracellular signal-regulated kinase and Akt signalling pathways. Furthermore, SCE and its active compounds increased mRNA expression of type I and III collagen in Hs68 fibroblasts. SCE and chamechromone inhibited NO and PGE2 release and mRNA expression of inflammatory mediators in RAW 264.7 macrophages. SCE enhances the motility of HaCaT keratinocytes and improves cutaneous wound healing in SD rats.

  2. Characterization of the Phytochemical Constituents of Taif Rose and Its Antioxidant and Anticancer Activities

    PubMed Central

    Abdel-Hameed, El-Sayed S.; Bazaid, Salih A.; Salman, Mahmood S.

    2013-01-01

    Ward Taifi (Taif rose) is considered one of the most important economic products of Taif, Saudi Arabia. In this study both fresh and dry Taif rose were biologically and phytochemically investigated. The 80% methanol extracts and n-butanol fractions of dry and fresh Taif rose had high radical scavenging activity toward artificial 1,1-diphenyl picrylhydrazyl (DPPH)• radical with SC50 values range 5.86−12.24 µg/ml whereas the aqueous fractions showed weak activity. All samples had in vitro anticancer activity toward HepG2 with IC50 < 20 µg/ml which fall within the criteria of the American Cancer Institute. High positive correlation appeared between the antioxidant activity and total phenolics whereas there is no correlation between total phenolics and anticancer activity. The LC-ESI(− ve)-MS analysis of all extracts indicate the presence of phenolic compounds belonging to hydrolysable tannins and flavonol glycosides. In conclusion, the presence of this is considered to be the first phytochemical report that identifies the major compounds in dry and fresh roses using HPLC-ESI-MS. The methanol extracts and its n-butanol and aqueous fractions for both fresh and dry Taif rose could be used as preventive and therapeutic effective natural agents for diseases in which free radicals involved after more in vitro and in vivo studies. PMID:24282813

  3. Chemical constituents and biological activities of Senecio aegyptius var. discoideus Boiss.

    PubMed

    Hassan, Wafaa; Al-Gendy, Amal; Al-Youssef, Hanan; El-Shazely, Assem

    2012-01-01

    A new eremophilane sesquiterpene, 1-beta-hydroxy-8-oxoeremophila-7,9-dien-12-oic acid (1), in addition to two known flavonol glycosides, rutin (2) and quercetin-3-O-glucoside-7-O-rutinoside (3), was isolated from the ethyl acetate fraction obtained from the aqueous alcoholic extract of the aerial parts of Senecio aegyptius var. discoideus Boiss. (family Asteraceae). The chemical structures of the isolated compounds were established by 1D and 2D NMR analysis (1H, 13C, COSY, HMQC, HMBC), MS and UV data, and through comparison with the literature. The ethyl acetate fraction and the isolated rutin showed significant cytotoxic activity against colorectal carcinoma (HCT 116) and to less extent against brain (U 251) and breast carcinoma (MCF 7). The ethyl acetate fraction showed a significant level of activity against Klebsiella pneumoniae, while the total extract showed the best antifungal activity against Candida albicans and Saccharomyces cerevisiae. DPPH radical scavenging activity of the ethyl acetate fraction was significant (96.7%) when compared to ascorbic acid. It also showed anti-inflammatory activity but no diuretic effect.

  4. Review of pharmacological effects of Myrtus communis L. and its active constituents.

    PubMed

    Alipour, Ghazal; Dashti, Saeedeh; Hosseinzadeh, Hossein

    2014-08-01

    Myrtle (Myrtus communis L., Myrtaceae) is a medicinal herb used worldwide in traditional medicine. A large number of components have been isolated from this herb. Polyphenols, myrtucommulone (MC), semimyrtucommulone (S-MC), 1,8-cineole, α-pinene, myrtenyl acetate, limonene, linalool and α-terpinolene are among the compounds considered to be the main biologically active components. Various parts of this herb such as its berries, leaves and fruits have been used extensively as a folk medicine for several centuries. The herb is used traditionally for the treatment of disorders such as diarrhea, peptic ulcer, hemorrhoid, inflammation, pulmonary and skin diseases, although clinical and experimental studies suggest that it possesses a broader spectrum of pharmacological and therapeutic effects such as antioxidative, anticancer, anti-diabetic, antiviral, antibacterial, antifungal, hepatoprotective and neuroprotective activity. The present review attempts to give an overview on the phytochemical, pharmacological, toxicological and clinical studies of total extracts and the most relevant active ingredients of M. communis.

  5. Phytochemical constituents and in vitro radical scavenging activity of different Aloe species.

    PubMed

    Lucini, Luigi; Pellizzoni, Marco; Pellegrino, Roberto; Molinari, Gian Pietro; Colla, Giuseppe

    2015-03-01

    The phytochemical profile of Aloe barbadensis Mill. and Aloe arborescens Mill. was investigated using colorimetric assays, triple quadrupole and time-of-flight mass spectrometry, focusing on phenolic secondary metabolites in the different leaf portions. Hydroxycinnamic acids, several characteristic anthrones and chromones, the phenolic dimer feralolide and flavonoids such as flavones and isoflavones were identified. The stable radical DPPH test and the ORAC assay were then used to determine the in vitro radical scavenging. The outer green rind was the most active, while the inner parenchyma was much less effective. The 5-methylchromones aloesin, aloeresin A and aloesone were the most active among the pure secondary metabolites tested. The results suggest that several compounds are likely to contribute to the overall radical scavenging activity, and indicate that leaf portion must be taken into account when the plant is used for its antioxidant properties.

  6. Antiviral activities of extracts and selected pure constituents of Ocimum basilicum.

    PubMed

    Chiang, Lien-Chai; Ng, Lean-Teik; Cheng, Pei-Win; Chiang, Win; Lin, Chun-Ching

    2005-10-01

    1. Ocimum basilicum (OB), also known as sweet basil, is a well known medicinal herb in traditional Chinese medicine preparations. In the present study, extracts and purified components of OB were used to identify possible antiviral activities against DNA viruses (herpes viruses (HSV), adenoviruses (ADV) and hepatitis B virus) and RNA viruses (coxsackievirus B1 (CVB1) and enterovirus 71 (EV71)). 2. The results show that crude aqueous and ethanolic extracts of OB and selected purified components, namely apigenin, linalool and ursolic acid, exhibit a broad spectrum of antiviral activity. Of these compounds, ursolic acid showed the strongest activity against HSV-1 (EC50 = 6.6 mg/L; selectivity index (SI) = 15.2), ADV-8 (EC50 = 4.2 mg/L; SI = 23.8), CVB1 (EC50 = 0.4 mg/L; SI = 251.3) and EV71 (EC50 = 0.5 mg/L; SI = 201), whereas apigenin showed the highest activity against HSV-2 (EC50 = 9.7 mg/L; SI = 6.2), ADV-3 (EC50 = 11.1 mg/L; SI = 5.4), hepatitis B surface antigen (EC50 = 7.1 mg/L; SI = 2.3) and hepatitis B e antigen (EC50 = 12.8 mg/L; SI = 1.3) and linalool showed strongest activity against AVD-II (EC50 = 16.9 mg/L; SI = 10.5). 3. No activity was noted for carvone, cineole, beta-caryophyllene, farnesol, fenchone, geraniol, beta-myrcene and alpha-thujone. 4. The action of ursolic acid against CVB1 and EV71 was found to occur during the infection process and the replication phase. 5. With SI values greater than 200, the potential use of ursolic acid for treating infection with CVB1 and EV71 merits further investigation.

  7. Flavonoid constituents, cytotoxic and antioxidant activities of Gleditsia triacanthos L. leaves

    PubMed Central

    Mohammed, R.S.; Abou Zeid, A.H.; El Hawary, S.S.; Sleem, A.A.; Ashour, W.E.

    2014-01-01

    Gleditsia triacanthos L. is a deciduous tree belonging to the family Fabaceae. It possesses important biological activities as anti-mutagenic, anticancer, cytotoxic and treating rheumatoid arthritis. The total ethanol extract (EtOHE) and successive extracts (petroleum ether, chloroform, ethyl acetate, and aqueous ethanol) were prepared from the leaves. Eight flavone glycosides and two flavone aglycones named vicenin-I (1), vitexin (2), isovitexin (3), orientin (4), isoorientin (5), luteolin-7-O-ß-glucopyranoside (6), luteolin-7-O-ß-galactopyranoside (7), apigenin-7-O-ß-glucopyranoside (8), luteolin (9) and apigenin (10) were isolated from the aqueous ethanol extract of G. triacanthos L. leaves. Potent cytotoxic activity of the EtOHE extract was observed against the liver (IC50 = 1.68 μg), breast (IC50 = 0.74 μg), cervix (IC50 = 1.28 μg), larynx (IC50 = 0.67 μg) and colon (IC50 = 2.50 μg) cancer cell lines. Cytotoxic activity of compounds 2, 4, 6 and 8 against, the liver, breast and colon cancer cell lines was also proved. Evaluation of the in-vivo antioxidant activity of the EtOHE and successive extracts revealed that the highest activity was exhibited by 100 mg of EtOHE (97.89% potency) as compared with vitamin E (100% potency). Compound 6 showed 91.8% free radical scavenging activity. PMID:25473363

  8. Antitumor Activity of Kielmeyera Coriacea Leaf Constituents in Experimental Melanoma, Tested in Vitro and in Vivo in Syngeneic Mice

    PubMed Central

    Figueiredo, Carlos Rogério; Matsuo, Alisson Leonardo; Massaoka, Mariana Hiromi; Girola, Natalia; Azevedo, Ricardo Alexandre; Rabaça, Aline Nogueira; Farias, Camyla Fernandes; Pereira, Felipe Valença; Matias, Natalia Silva; Silva, Luciana Pereira; Rodrigues, Elaine Guadelupe; Lago, João Henrique Guilardi; Travassos, Luiz Rodolpho; Silva, Regildo Márcio Gonçalves

    2014-01-01

    Purpose: The antitumor activity of Kielmeyera coriacea (Clusiaceae), a medicinal plant used in the treatment of parasitic, as well as fungal and bacterial infections by the Brazilian Cerrado population, was investigated. Methods: A chloroform extract (CE) of K. coriacea was tested in the murine melanoma cell line (B16F10-Nex2) and a panel of human tumor cell lines. Tumor cell migration was determined by the wound-healing assay and the in vivo antitumor activity of CE was investigated in a melanoma cell metastatic model. 1H NMR and GC/MS were used to determine CE chemical composition. Results: We found that CE exhibited strong cytotoxic activity against murine melanoma cells and a panel of human tumor cell lines in vitro. CE also inhibited growth of B16F10-Nex2 cells at sub lethal concentrations, inducing cell cycle arrest at S phase, and inhibition of tumor cell migration. Most importantly, administration of CE significantly reduced the number of melanoma metastatic nodules in vivo. Chemical analysis of CE indicated the presence of the long chain fatty compounds, 1-eicosanol, 1-docosanol, and 2-nonadecanone as main constituents. Conclusion: These results indicate that K. coriacea is a promising medicinal plant in cancer therapy exhibiting antitumor activity both in vitro and in vivo against different tumor cell lines. PMID:25364658

  9. Traditional uses, chemical constituents, and biological activities of Bixa orellana L.: a review.

    PubMed

    Vilar, Daniela de Araújo; Vilar, Marina Suênia de Araujo; de Lima e Moura, Túlio Flávio Accioly; Raffin, Fernanda Nervo; de Oliveira, Márcia Rosa; Franco, Camilo Flamarion de Oliveira; de Athayde-Filho, Petrônio Filgueiras; Diniz, Margareth de Fátima Formiga Melo; Barbosa-Filho, José Maria

    2014-01-01

    Bixa orellana L., popularly known as "urucum," has been used by indigenous communities in Brazil and other tropical countries for several biological applications, which indicates its potential use as an active ingredient in pharmaceutical products. The aim of this work was to report the main evidence found in the literature, concerning the ethnopharmacology, the biological activity, and the phytochemistry studies related to Bixa orellana L. Therefore, this work comprises a systematic review about the use of Bixa orellana in the American continent and analysis of the data collected. This study shows the well-characterized pharmacological actions that may be considered relevant for the future development of an innovative therapeutic agent.

  10. Polysaccharide Constituents of Three Types of Sea Urchin Shells and Their Anti-Inflammatory Activities.

    PubMed

    Jiao, Heng; Shang, Xiaohui; Dong, Qi; Wang, Shuang; Liu, Xiaoyu; Zheng, Heng; Lu, Xiaoling

    2015-09-16

    As a source of potent anti-inflammatory traditional medicines, the quantitative chromatographic fingerprints of sea urchin shell polysaccharides were well established via pre-column derivatization high performance liquid chromatography (HPLC) analysis. Based on the quantitative results, the content of fucose and glucose could be used as preliminary distinguishing indicators among three sea urchin shell species. Besides, the anti-inflammatory activities of the polysaccharides from sea urchin shells and their gonads were also determined. The gonad polysaccharide of Anthocidaris crassispina showed the most potent anti-inflammatory activity among all samples tested.

  11. Polysaccharide Constituents of Three Types of Sea Urchin Shells and Their Anti-Inflammatory Activities

    PubMed Central

    Jiao, Heng; Shang, Xiaohui; Dong, Qi; Wang, Shuang; Liu, Xiaoyu; Zheng, Heng; Lu, Xiaoling

    2015-01-01

    As a source of potent anti-inflammatory traditional medicines, the quantitative chromatographic fingerprints of sea urchin shell polysaccharides were well established via pre-column derivatization high performance liquid chromatography (HPLC) analysis. Based on the quantitative results, the content of fucose and glucose could be used as preliminary distinguishing indicators among three sea urchin shell species. Besides, the anti-inflammatory activities of the polysaccharides from sea urchin shells and their gonads were also determined. The gonad polysaccharide of Anthocidaris crassispina showed the most potent anti-inflammatory activity among all samples tested. PMID:26389925

  12. Selective release of inorganic constituents in broiler manure biochars under different post-activation treatments

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Previous studies determined that poultry litter is a desirable feedstock for activated biochars with enhanced adsorption towards cations. Animal manures such as poultry litter contain a significant fraction of inorganic material that can significantly affect the final physical, chemical and adsorpt...

  13. Molecular docking studies and in vitro cholinesterase enzyme inhibitory activities of chemical constituents of Garcinia hombroniana.

    PubMed

    Jamila, Nargis; Yeong, Khaw Kooi; Murugaiyah, Vikneswaran; Atlas, Amir; Khan, Imran; Khan, Naeem; Khan, Sadiq Noor; Khairuddean, Melati; Osman, Hasnah

    2015-01-01

    Garcinia species are reported to possess antimicrobial, anti-inflammatory, anticancer, anti-HIV and anti-Alzheimer's activities. This study aimed to investigate the in vitro cholinesterase enzyme inhibitory activities of garcihombronane C (1), garcihombronane F (2), garcihombronane I (3), garcihombronane N (4), friedelin (5), clerosterol (6), spinasterol glucoside (7) and 3β-hydroxy lup-12,20(29)-diene (8) isolated from Garcinia hombroniana, and to perform molecular docking simulation to get insight into the binding interactions of the ligands and enzymes. The cholinesterase inhibitory activities were evaluated using acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. In this study, compound 4 displayed the highest concentration-dependent inhibition of both AChE and BChE. Docking studies exhibited that compound 4 binds through hydrogen bonds to amino acid residues of AChE and BChE. The calculated docking and binding energies also supported the in vitro inhibitory profiles of IC50. In conclusion, garcihombronanes C, F, I and N (1-4) exhibited dual and moderate inhibitory activities against AChE and BChE.

  14. Biological activity and chemical constituents of red and brown algae from the persian gulf.

    PubMed

    Jassbi, Amir Reza; Mohabati, Maryam; Eslami, Saba; Sohrabipour, Jelveh; Miri, Ramin

    2013-01-01

    Different solvent extracts of a red algae, Hypnea flagelliformis, and two brown algae, Cystoseira myrica and Sargassum boveanum, which were collected from the Persian Gulf coast were subjected to different bioassays, including: 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay, antibacterial and antifungal activity by thin layer chromatography (TLC)-bioautography, agar disc diffusion (ADD) and nutrient-broth micro-dilution (NBMD) bioassays. The water extracts were found to have the most antioxidant activity. The antibacterial minimum inhibitory concentrations (MIC) of the active extracts were determined for the susceptible organisms, Staphylococcus aurous and Bacillus subtilis, using NBMD bioassays. The active substances were identified as free fatty acids (FFA), by using gas chromatography-mass spectrometry (GC-MS). After derivatization to their methyl esters, their concentrations were measured by using GC- lame ionization detection (GC-FID). In addition to the fatty acids, fucosterol, cholesterol and 22-dehydroxychlosterol were detected as the major sterols in S. boveanum extract using GC-MS analyses.

  15. Acaricidal activity of constituents derived from peppermint oil against Tyrophagus putrescentiae.

    PubMed

    Park, Jun-Hwan; Yang, Ji-Yeon; Lee, Hoi-Seon

    2014-10-01

    The acaricidal activities of peppermint oil and menthol isomers against mites in stored food were evaluated using fumigant and contact bioassays and were compared with the activity of benzyl benzoate as a synthetic acaricide. Based on the 50% lethal dose (LD50) values against Tyrophagus putrescentiae in the fumigant bioassay, menthol (0.96 μg/cm(2)) was approximately 12.18 times more effective than benzyl benzoate (11.70 μg/cm(2)), followed by (+)-neomenthol (1.33 μg/cm(2)), (-)-menthol (1.60 μg/cm(2)), and (+)-menthol (1.90 μg/cm(2)). In the filter paper bioassay, menthol (0.55 μg/cm(2)) was about 15.18 times more active than benzyl benzoate (8.35 μg/cm(2)), followed by (-)-menthol (0.84 μg/cm(2)), (+)-menthol (0.92 μg/cm(2)), and (+)-neomenthol (1.72 μg/cm(2)). However, (+)-isomenthol did not exhibit any acaricidal activity against T. putrescentiae in the fumigant and filter paper bioassays. These results indicate that peppermint oil and menthol isomers could be effective natural acaricides for managing mites in stored food.

  16. Antimycobacterial activity of constituents from Foeniculum vulgare var. dulce grown in Mexico.

    PubMed

    Esquivel-Ferriño, Patricia C; Favela-Hernández, Juan Manuel J; Garza-González, Elvira; Waksman, Noemí; Ríos, María Yolanda; del Rayo Camacho-Corona, María

    2012-07-13

    Bioassay guided fractionation of an antimycobacterial extract of Foeniculum vulgare var dulce (Apiaceae) led to the isolation and characterization of 5-hydroxyfurano-coumarin. The chemical structure of this compound was elucidated by 1H and 13C (1D and 2D) Nuclear Magnetic Resonance (NMR) spectroscopy. In addition, the active fractions were analyzed by GC-MS and seventy eight compounds were identified; the major compounds were 1,3-benzenediol, 1-methoxycyclohexene, o-cymene, sorbic acid, 2-hydroxy-3-methyl-2-cyclopenten-1-one, estragole, limonene-10-ol and 3-methyl-2-cyclopenten-1-one. Twenty compounds identified in the active fractions were tested against one sensitive and three MDR strains of Mycobacterium tuberculosis using the Alamar Blue microassay. Compounds that showed some degree of antimycobacterial activity against all strains tested were the following: linoleic acid (MIC 100 µg/mL), oleic acid (MIC 100 µg/mL), 1,3-benzenediol (MIC 100-200 µg/mL), undecanal (MIC 50-200 µg/mL), and 2,4-undecadienal (MIC 25-50 µg/mL), the last being the most active compound. To our knowledge, this is the first report of the presence of 5-hydroxy-furanocoumarin in F. vulgare.

  17. Biological Activity and Chemical Constituents of Red and Brown Algae from the Persian Gulf

    PubMed Central

    Jassbi, Amir Reza; Mohabati, Maryam; Eslami, Saba; Sohrabipour, Jelveh; Miri, Ramin

    2013-01-01

    Different solvent extracts of a red algae, Hypnea flagelliformis, and two brown algae, Cystoseira myrica and Sargassum boveanum, which were collected from the Persian Gulf coast were subjected to different bioassays, including: 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging assay, antibacterial and antifungal activity by thin layer chromatography (TLC)-bioautography, agar disc diffusion (ADD) and nutrient-broth micro-dilution (NBMD) bioassays. The water extracts were found to have the most antioxidant activity. The antibacterial minimum inhibitory concentrations (MIC) of the active extracts were determined for the susceptible organisms, Staphylococcus aurous and Bacillus subtilis, using NBMD bioassays. The active substances were identified as free fatty acids (FFA), by using gas chromatography-mass spectrometry (GC-MS). After derivatization to their methyl esters, their concentrations were measured by using GC- lame ionization detection (GC-FID). In addition to the fatty acids, fucosterol, cholesterol and 22-dehydroxychlosterol were detected as the major sterols in S. boveanum extract using GC-MS analyses. PMID:24250640

  18. Phenolic constituents of Carex vulpinoidea seeds and their tyrosinase inhibitory activities.

    PubMed

    Niesen, Daniel B; Ma, Hang; Yuan, Tao; Bach, Alvin C; Henry, Geneive E; Seeram, Navindra P

    2015-03-01

    Two new phenolics, a stilbenoid, vulpinoideol A (1), and a chalcone, vulpinoideol B (2), along with ten known compounds (3-12) were isolated from Carex vulpinoidea Michx. seeds. The structures of compounds 1-12 were elucidated based on spectrometric and spectroscopic analyses including HRESIMS, 1D and 2D NMR data. All compounds were evaluated for their tyrosinase enzyme inhibitory activities.

  19. Ethnobotany, chemical constituents and biological activities of the flowers of Hydnora abyssinica A.Br. (Hydnoraceae).

    PubMed

    Al-Fatimi, M; Ali, N A A; Kilian, N; Franke, K; Arnold, N; Kuhnt, C; Schmidt, J; Lindequist, U

    2016-04-01

    Hydnora abyssinica A.Br. (Hydnoraceae), a holoparasitic herb, is for the first time recorded for Abyan governorate of South Yemen. Flowers of this species were studied for their ethnobotanical, biological and chemical properties for the first time. In South Yemen, they are traditionally used as wild food and to cure stomach diseases, gastric ulcer and cancer. Phytochemical analysis of the extracts showed the presence of terpenes, tannins, phenols, and flavonoids. The volatile components of the air-dried powdered flowers were identified using a static headspace GC/MS analysis as acetic acid, ethyl acetate, sabinene, α-terpinene, (+)-D-limonene and γ-terpinene. These volatile compounds that characterize the odor and taste of the flowers were detected for the first time in a species of the family Hydnoraceae. The flowers were extracted by n-hexane, dichlormethane, ethyl acetate, ethanol, methanol and water. With exception of the water extract all extracts demonstrated activities against Gram-positive bacteria as well as remarkable radical scavenging activities in DPPH assay. Ethyl acetate, methanol and water extracts exhibited good antifungal activities. The cytotoxic activity of the extracts against FL cells, measured in neutral red assay, was only weak (IC50 > 500 μg/mL). The results justify the traditional use of the flowers of Hydnora abyssinica in South Yemen.

  20. Chemical Constituents Identified from Fruit Body of Cordyceps bassiana and Their Anti-Inflammatory Activity.

    PubMed

    Suh, Wonse; Nam, Gyeongsug; Yang, Woo Seok; Sung, Gi-Ho; Shim, Sang Hee; Cho, Jae Youl

    2017-03-01

    Cordyceps bassiana is one of Cordyceps species with anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity, anti-angiogenic, and anti-nociceptive activities. This mushroom has recently demonstrated to have an ability to reduce 2,4-dinitrofluorobenzene-induced atopic dermatitis symptoms in NC/Nga mice. In this study, we further examined phytochemical properties of this mushroom by column chromatography and HPLC analysis. By chromatographic separation and spectroscopic analysis, 8 compounds, such as 1,9-dimethylguanine (1), adenosine (2), uridine (3), nicotinamide (4), 3-methyluracil (5), 1,7-dimethylxanthine (6), nudifloric acid (7), and mannitol (8) were identified from 6 different fractions and 4 more subfractions. Through evaluation of their anti-inflammatory activities using reporter gene assay and mRNA analysis, compound 1 was found to block luciferase activity induced by NF-κB and AP-1, suppress the mRNA levels of cyclooxygenase (COX)-2 and tumor necrosis factor (TNF)-α. Therefore, our data strongly suggests that compound 1 acts as one of major principles in Cordyceps bassiana with anti-inflammatory and anti-atopic dermatitis activities.

  1. Chemical Constituents Identified from Fruit Body of Cordyceps bassiana and Their Anti-Inflammatory Activity

    PubMed Central

    Suh, Wonse; Nam, Gyeongsug; Yang, Woo Seok; Sung, Gi-Ho; Shim, Sang Hee; Cho, Jae Youl

    2017-01-01

    Cordyceps bassiana is one of Cordyceps species with anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity, anti-angiogenic, and anti-nociceptive activities. This mushroom has recently demonstrated to have an ability to reduce 2,4-dinitrofluorobenzene-induced atopic dermatitis symptoms in NC/Nga mice. In this study, we further examined phytochemical properties of this mushroom by column chromatography and HPLC analysis. By chromatographic separation and spectroscopic analysis, 8 compounds, such as 1,9-dimethylguanine (1), adenosine (2), uridine (3), nicotinamide (4), 3-methyluracil (5), 1,7-dimethylxanthine (6), nudifloric acid (7), and mannitol (8) were identified from 6 different fractions and 4 more subfractions. Through evaluation of their anti-inflammatory activities using reporter gene assay and mRNA analysis, compound 1 was found to block luciferase activity induced by NF-κB and AP-1, suppress the mRNA levels of cyclooxygenase (COX)-2 and tumor necrosis factor (TNF)-α. Therefore, our data strongly suggests that compound 1 acts as one of major principles in Cordyceps bassiana with anti-inflammatory and anti-atopic dermatitis activities. PMID:27530115

  2. Biological activities and volatile constituents of Daucus muricatus L. from Algeria

    PubMed Central

    2012-01-01

    Background In order to find new bioactive natural products, the antimicrobial and antioxidant activities of essential oil components extracted from the separated organs of the Algerian medicinal and aromatic plant Daucus muricatus L. were studied. Results The chemical composition of essential oils obtained by hydrodistillation (HD) was investigated using Gas Chromatography–Retention Indices (GC-RI) and GC–Mass Spectrometry (GC-MS). Two types of essential oils were produced by D. muricatus: (i) The oil from roots is mainly composed by nonterpenic oxygenated compounds (59.8 g/100 g), and (ii) the aerial part oils (i.e., the leaves, stems, flowers, and umbels) was mainly composed by terpenic hydrocarbon compounds (62.3–72.2 g/100 g). The chemical composition of the volatile fraction isolated from different organs of Daucus muricatus were studied by HS–SPME/GC–RI and GC–MS after optimization of Solid Phase MicroExtraction parameters. For all organs studied, the main volatiles emitted by the plant were hydrocarbon compounds (60.7–82.2 g/100 g). Only quantitative differences between the volatiles of the separated organs studied were observed. In addition, the activity of the oil of D. muricatus against eight bacterial strains and one yeast was investigated. The oil from roots revealed active against S. aureus, while the essential oil obtained from the aerial parts was active against the yeast C. albicans. Conclusions Daucus muricatus essential oil seems be a promising source of natural products with potential antimicrobial activity. PMID:22647252

  3. Phytochemical constituents and antioxidant activities of the whole leaf extract of Aloe ferox Mill

    PubMed Central

    Wintola, Olubunmi Abosebe; Afolayan, Anthony Jide

    2011-01-01

    Background: Aloe ferox Mill. (Asphodelaceae) is used in South Africa for the treatment of constipation among various ailments. Despite the extensive studies conducted on the antioxidant activities of the leaf gel and pulp extract of the plant, there is no information on the antioxidant properties of the whole leaf extract of the species. Materials and Methods: The antioxidant activities of ethanol, acetone, methanol and aqueous extracts of A. ferox were investigated spectrophotometrically against 1,1- diphenyl-2-picrylhydrazyl (DPPH), 2,2’-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) diammonium salt, hydrogen peroxide (H2O2), nitric oxide (NO), lipid peroxidation and ferric reducing power. Total phenols, flavonoids, flavonols, proanthocyanidins, tannins, alkaloids and saponins were also determined using the standard methods. Results: The percentage compositions of phenols (70.33), flavonols (35.2), proanthocyanidins (171.06) and alkaloids (60.9) were significantly high in the acetone extract, followed by the ethanol extract with values of 70.24, 12.53, 76.7 and 23.76 respectively, while the least composition was found in the aqueous extract. Moreover, both flavonoids and saponins contents were appreciably high in both methanol and ethanol extracts, while others were very low. Tannins levels were, however, not significantly different (P > 0.05) in all the solvent extracts. At 0.5 mg/ml, the free radical scavenging activity of the methanol, acetone and ethanol extracts showed higher inhibition against ABTS, hydrogen peroxide and nitric oxide radicals. Whereas, scavenging activity of the extracts against DPPH* and lipid peroxidation were observed at a concentration of 0.016 and 0.118 mg/ml respectively in comparison to the butylated hydroxyltoluene (BHT), gallic acid and rutin. The ferric reducing potential of the extracts was concentration dependent and significantly different from that of vitamin C and BHT. Conclusion: The present study showed high

  4. Traditional Uses, Chemical Constituents, and Biological Activities of Bixa orellana L.: A Review

    PubMed Central

    Vilar, Daniela de Araújo; Vilar, Marina Suênia de Araujo; Moura, Túlio Flávio Accioly de Lima e; Raffin, Fernanda Nervo; de Oliveira, Márcia Rosa; Franco, Camilo Flamarion de Oliveira; de Athayde-Filho, Petrônio Filgueiras; Diniz, Margareth de Fátima Formiga Melo; Barbosa-Filho, José Maria

    2014-01-01

    Bixa orellana L., popularly known as “urucum,” has been used by indigenous communities in Brazil and other tropical countries for several biological applications, which indicates its potential use as an active ingredient in pharmaceutical products. The aim of this work was to report the main evidence found in the literature, concerning the ethnopharmacology, the biological activity, and the phytochemistry studies related to Bixa orellana L. Therefore, this work comprises a systematic review about the use of Bixa orellana in the American continent and analysis of the data collected. This study shows the well-characterized pharmacological actions that may be considered relevant for the future development of an innovative therapeutic agent. PMID:25050404

  5. Antimicrobial activity of essential oil and major constituents of Salvia chloroleuca.

    PubMed

    Yousefzadi, Morteza; Sonboli, Ali; Ebrahimi, Samad Nejad; Hashemi, Seid Hasan

    2008-01-01

    The aerial parts of Salvia chloroleuca were collected at full flowering stage at Shahrestanak (Tehran province of Iran). The essential oil was isolated by hydrodistillation and analyzed by combination of capillary GC and GC-MS. Thirty-four components were identified, representing 98.5% of the total oil. beta-Pinene (10.6%), alpha-pinene (9.0%), beta-caryophyllene (9.0%), 1,8-cineole (9.0%) and carvacrol (7.9%) were the main components. The in vitro antimicrobial activity of the essential oil of S. chloroleuca was studied against seven Gram-positive and Gram-negative bacteria (Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, S. epidermidis, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae) and three fungi (Candida albicans, Saccharomyces cerevisiae and Aspergillus niger); the disc diffusion method and MIC values indicated that the oil exhibited moderate to high antimicrobial activity.

  6. Chemical Constituents of the New Endophytic Fungus Mycosphaerella sp. nov. and Their Anti-Parasitic Activity

    PubMed Central

    Moreno, Eufemio; Varughese, Titto; Spadafora, Carmenza; Arnold, A. Elizabeth; Coley, Phyllis D.; Kursar, Thomas A.; Gerwick, William H.; Cubilla-Rios, Luis

    2012-01-01

    Chemical investigation of a new endophytic fungus, Mycosphaerella sp. nov. strain F2140 associated with the foliage of the plant Psychotria horizontalis (Rubiaceae) in Panama, resulted in the isolation of cercosporin (1) and a new cercosporin analogue (3) as the major components. The structures of minor compounds in the extract were elucidated by detailed spectroscopic analysis as 2-(2-butyl)-3-hydroxy-6-ethyl-6-methylcyclohex-2-ene-1,5-dione (4), 3-(2-butyl)-6-ethyl-6-methyl-5-hydroxy-2-methoxy-cyclohex-2-eneone (5), and an isomer of 5 (6). To study the influence of the hydroxy groups on the anti-parasitic activity of cercosporin, compound 1 was acetylated to obtain derivative 2. The isolated compounds 1–6 were tested in vitro to determine their anti-parasitic activity against the causal agents of malaria (Plasmodium falciparum), leishmaniasis (Leishmania donovani), and Chagas disease (Trypanosoma cruzi). Also, the cytotoxicity and potential anticancer activity of these compounds were evaluated using mammalian Vero cells and MCF7 cancer cell lines, respectively. Compounds 1 and 2 displayed high potency against L. donovani (IC50 0.46 and 0.64 μM), T. cruzi (IC50 1.08 and 0.78 μM), P. falciparum (IC50 1.03 and 2.99 μM), and MCF7 cancer cell lines (IC50 4.68 and 3.56 μM). Compounds 3–6 were not active in these assays at a concentration of 10 μg/mL. PMID:21815421

  7. Chemical constituents of the new endophytic fungus Mycosphaerella sp. nov. and their anti-parasitic activity.

    PubMed

    Moreno, Eufemio; Varughese, Titto; Spadafora, Carmenza; Arnold, A Elizabeth; Coley, Phyllis D; Kursar, Thomas A; Gerwick, William H; Cubilla-Rios, Luis

    2011-06-01

    Chemical investigation of a new endophytic fungus, Mycosphaerella sp. nov. strain F2140, associated with the foliage of the plant Psychotria horizontalis (Rubiaceae) in Panama, resulted in the isolation of cercosporin (1) and a new cercosporin analog (3) as the major components. The structures of minor compounds in the extract were elucidated by detailed spectroscopic analysis as 2-(2-butyl)-6-ethyl-3-hydroxy-6-methylcyclohex-2-ene-1,5-dione (4), 3-(2-butyl)-6-ethyl-5-hydroxy-2-methoxy-6-methyl-cyclohex-2-enone (5), and an isomer of 5 (6). To study the influence of the hydroxy groups on the anti-parasitic activity of cercosporin, compound 1 was acetylated to obtain derivative 2. The isolated compounds 1- 6 were tested in vitro to determine their anti-parasitic activity against the causal agents of malaria (Plasmodium falciparum), leishmaniasis (Leishmania donovani), and Chagas disease (Trypanosoma cruzi). Cytotoxicity and potential anticancer activity of these compounds were evaluated using mammalian Vero cells and MCF7 cancer cell lines, respectively. Compounds 1 and 2 displayed high potency against L. donovani (IC50 0.46 and 0.64 microM), T. cruzi (IC50 1.08 and 0.78 microM), P. falciparum (IC50 1.03 and 2.99 microM), and MCF7 cancer cell lines (IC50 4.68 and 3.56 microM). Compounds 3-6 were not active in these assays at a concentration of 10 microg/mL.

  8. Borreria and Spermacoce species (Rubiaceae): A review of their ethnomedicinal properties, chemical constituents, and biological activities.

    PubMed

    Conserva, Lucia Maria; Ferreira, Jesu Costa

    2012-01-01

    Borreira and Spermacoce are genera of Rubiaceae widespread in tropical and subtropical America, Africa, Asia, and Europe. Based on its fruits morphology they are considered by many authors to be distinct genera and most others, however, prefer to combine the two taxa under the generic name Spermacoce. Whereas the discussion is still unclear, in this work they were considered as synonyms. Some species of these genera play an important role in traditional medicine in Africa, Asia, Europe, and South America. Some of these uses include the treatment of malaria, diarrheal and other digestive problems, skin diseases, fever, hemorrhage, urinary and respiratory infections, headache, inflammation of eye, and gums. To date, more than 60 compounds have been reported from Borreria and Spermacoce species including alkaloids, iridoids, flavonoids, terpenoids, and other compounds. Studies have confirmed that extracts from Borreria and Spermacoce species as well as their isolated compounds possess diverse biological activities, including anti-inflammatory, antitumor, antimicrobial, larvicidal, antioxidant, gastrointestinal, anti-ulcer, and hepatoprotective, with alkaloids and iridoids as the major active principles. This paper briefly reviews the ethnomedicinal uses, phytochemistry, and biological activities of some isolated compounds and extracts of both genera.

  9. Investigation of contribution of individual constituents to antioxidant activity in herbal drugs using postcolumn HPLC method.

    PubMed

    Raudonis, Raimondas; Jakstas, Valdas; Burdulis, Deividas; Benetis, Raimondas; Janulis, Valdimaras

    2009-01-01

    The most important attention is paid to the search of natural antioxidants and their evaluation in medicinal and food raw materials of plant origin. A number of plants, their extracts, food products, and medicinal preparations appear to be the objects of scientific research. Effectiveness and informative character of research, undoubtedly, depend on relevance, sensitivity, and efficiency of the methods chosen. The aim of this work was to develop and validate the postcolumn high-performance liquid chromatography (HPLC)-DPPH method as well as its application in the evaluation of antioxidant activity of known and unknown compounds scavenging free radicals and existing in medicinal plant raw materials. HPLC-separated compounds were identified at the wavelength of 275 nm, and then the mobile phase with analytes flowed through a mixing tee to the reaction coil, where DPPH reagent solution was supplied. The solution flow rate was 0.4 mL/min. The reaction coil was connected with UV/VIS type detector, which measured absorption of flowing solution at the wavelength of 520 nm. It was determined that vitexin rhamnoside, the dominant compound in the leaves of Crataegus monogyna, was not a significant radical scavenger. The most active antioxidant in the leaves and flowers of Crataegus monogyna was chlorogenic acid. The most active antioxidant in Origanum vulgare raw material was rosmarinic acid. Identified analytes in the extracts of Achillea millefolium that possessed radical-scavenging properties were chlorogenic acid, luteolin-7-O-glucoside, rutin, and luteolin.

  10. Chemical Constituents Analysis and Antidiabetic Activity Validation of Four Fern Species from Taiwan

    PubMed Central

    Chen, Chen-Yu; Chiu, Fu-Yu; Lin, Yenshou; Huang, Wei-Jan; Hsieh, Po-Shiuan; Hsu, Feng-Lin

    2015-01-01

    Pterosins are abundant in ferns, and pterosin A was considered a novel activator of adenosine monophosphate-activated protein kinase, which is crucial for regulating blood glucose homeostasis. However, the distribution of pterosins in different species of ferns from various places in Taiwan is currently unclear. To address this question, the distribution of pterosins, glucose-uptake efficiency, and protective effects of pterosin A on β-cells were examined. Our results showed that three novel compounds, 13-chloro-spelosin 3-O-β-d-glucopyranoside (1), (3R)-Pterosin D 3-O-β-d-(3'-p-coumaroyl)-glucopyranoside (2), and (2R,3R)-Pterosin L 3-O-β-d-(3'-p-coumaroyl)-glucopyranoside (3), were isolated for the first time from four fern species (Ceratopteris thalictroides, Hypolepis punctata, Nephrolepis multiflora, and Pteridium revolutum) along with 27 known compounds. We also examined the distribution of these pterosin compounds in the mentioned fern species (except N. multiflora). Although all pterosin analogs exhibited the same effects in glucose uptake assays, pterosin A prevented cell death and reduced reactive oxygen species (ROS) production. This paper is the first report to provide new insights into the distribution of pterosins in ferns from Taiwan. The potential anti-diabetic activity of these novel phytocompounds warrants further functional studies. PMID:25622260

  11. Borreria and Spermacoce species (Rubiaceae): A review of their ethnomedicinal properties, chemical constituents, and biological activities

    PubMed Central

    Conserva, Lucia Maria; Ferreira, Jesu Costa

    2012-01-01

    Borreira and Spermacoce are genera of Rubiaceae widespread in tropical and subtropical America, Africa, Asia, and Europe. Based on its fruits morphology they are considered by many authors to be distinct genera and most others, however, prefer to combine the two taxa under the generic name Spermacoce. Whereas the discussion is still unclear, in this work they were considered as synonyms. Some species of these genera play an important role in traditional medicine in Africa, Asia, Europe, and South America. Some of these uses include the treatment of malaria, diarrheal and other digestive problems, skin diseases, fever, hemorrhage, urinary and respiratory infections, headache, inflammation of eye, and gums. To date, more than 60 compounds have been reported from Borreria and Spermacoce species including alkaloids, iridoids, flavonoids, terpenoids, and other compounds. Studies have confirmed that extracts from Borreria and Spermacoce species as well as their isolated compounds possess diverse biological activities, including anti-inflammatory, antitumor, antimicrobial, larvicidal, antioxidant, gastrointestinal, anti-ulcer, and hepatoprotective, with alkaloids and iridoids as the major active principles. This paper briefly reviews the ethnomedicinal uses, phytochemistry, and biological activities of some isolated compounds and extracts of both genera. PMID:22654404

  12. Chemical constituents analysis and antidiabetic activity validation of four fern species from Taiwan.

    PubMed

    Chen, Chen-Yu; Chiu, Fu-Yu; Lin, Yenshou; Huang, Wei-Jan; Hsieh, Po-Shiuan; Hsu, Feng-Lin

    2015-01-22

    Pterosins are abundant in ferns, and pterosin A was considered a novel activator of adenosine monophosphate-activated protein kinase, which is crucial for regulating blood glucose homeostasis. However, the distribution of pterosins in different species of ferns from various places in Taiwan is currently unclear. To address this question, the distribution of pterosins, glucose-uptake efficiency, and protective effects of pterosin A on β-cells were examined. Our results showed that three novel compounds, 13-chloro-spelosin 3-O-β-d-glucopyranoside (1), (3R)-Pterosin D 3-O-β-d-(3'-p-coumaroyl)-glucopyranoside (2), and (2R,3R)-Pterosin L 3-O-β-d-(3'-p-coumaroyl)-glucopyranoside (3), were isolated for the first time from four fern species (Ceratopteris thalictroides, Hypolepis punctata, Nephrolepis multiflora, and Pteridium revolutum) along with 27 known compounds. We also examined the distribution of these pterosin compounds in the mentioned fern species (except N. multiflora). Although all pterosin analogs exhibited the same effects in glucose uptake assays, pterosin A prevented cell death and reduced reactive oxygen species (ROS) production. This paper is the first report to provide new insights into the distribution of pterosins in ferns from Taiwan. The potential anti-diabetic activity of these novel phytocompounds warrants further functional studies.

  13. Protein tyrosine phosphatase 1B inhibitory activity of Indonesian herbal medicines and constituents of Cinnamomum burmannii and Zingiber aromaticum.

    PubMed

    Saifudin, Azis; Kadota, Shigetoshi; Tezuka, Yasuhiro

    2013-04-01

    We screened water and methanol extracts of 28 Indonesian medicinal plants for their protein tyrosine phosphatase 1B (PTP1B) inhibitory activities. Nine water extracts, i.e., Alstonia scholaris leaf, Blumea balsamifera, Cinnamomum burmannii, Cymbopogon nardus, Melaleuca leucadendra, Phyllanthus niruri, Piper nigrum, Syzygium aromaticum, and Sy. polyanthum, exhibited ≥70 % inhibition at 25 μg/mL, whereas 11 methanol extracts, i.e., Als. scholaris, Andrographis paniculata, B. balsamifera, Ci. burmannii, Curcuma heyneana, Glycyrrhiza glabra, M. leucadendra, Punica granatum, Rheum palmatum, Sy. polyanthum, and Z. aromaticum, exhibited ≥70 % inhibition at 25 μg/mL. Water extracts of B. balsamifera (IC50, 2.26 μg/mL) and M. leucadendra (IC50, 2.05 μg/mL), and methanol extracts of Ci. burmannii (IC50, 2.47 μg/mL), Pu. granatum (IC50, 2.40 μg/mL), and Sy. polyanthum (IC50, 1.03 μg/mL) exhibited strong inhibitory activity, which was comparable with that of the positive control, RK-682 (IC50, 2.05 μg/mL). The PTP1B inhibitory activity of the constituents of Ci. burmannii and Z. aromaticum was then evaluated. 5'-Hydroxy-5-hydroxymethyl-4″,5″-methylenedioxy-1,2,3,4-dibenzo-1,3,5-cycloheptatriene (2; IC50, 29.7 μM) and trans-cinnamaldehyde (5; IC50, 57.6 μM) were the active constituents of Ci. burmannii, while humulatrien-5-ol-8-one (21; IC50, 27.7 μM), kaempferol-3,4'-di-O-methyl ether (32; IC50, 17.5 μM), and (S)-6-gingerol (33; IC50, 28.1 μM) were those of Z. aromaticum. These results suggest that these medicinal plants may contribute to the treatment and/or prevention of type II diabetes and/or obesity through PTP1B inhibition.

  14. Contents of constituents and antioxidant activity of seed and pulp extracts of Annona coriacea and Annona sylvatica.

    PubMed

    Benites, R S R; Formagio, A S N; Argandoña, E J S; Volobuff, C R F; Trevizan, L N F; Vieira, M C; Silva, M S

    2015-08-01

    The antioxidant potential of fruit pulp and seeds of extracts of the Annona coriacea, and A. sylvatica (Annonaceae) were investigated, as well contents total phenolics, flavonoids, condensed tannins and ascorbic acid. Was used to determine the antioxidant activity the 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH), β-carotene bleaching and ABTS radical cation method. The total phenol, total flavonoid, condensed tannin, and ascorbic acid contents were measured spectrophotometrically. In this study, the pulp and seeds of the fruits were extracted using methanol/water (8:2) for maceration. The seed extracts of A. coriacea demonstrated a moderate antioxidant effect with free radical scavenging activity of 31.53%, by the DPPH test, 51.59% by the β-carotene bleaching test and 159.50 µM trolx/g of extract in the ABTS assay. We found that the hydromethanolic seed extract of A. coriacea had high total phenol (147.08 ± 4.20 mg of GAE/g of extract) and flavonoid (131.18 ± 2.31 mg of QE/g of extract) content. This indicated that the antioxidant activity of the extracts was related to the contents of these constituents.

  15. Study on the effects of sulfur fumigation on chemical constituents and antioxidant activity of Chrysanthemum morifolium cv. Hang-ju.

    PubMed

    Wang, Shan; Hao, Li-Juan; Zhu, Jing-Jing; Zhang, Qi-Wei; Wang, Zhi-Min; Zhang, Xian; Song, Xiao-mei

    2014-04-15

    The traditional after-harvesting drying method of C. morifolium cv. Hang-ju (HJ) is sun drying, but recently sulfur fumigation is increasingly used as a cheap and convenient method. However, the effects of sulfur fumigation on chemical constituents and potential activities of HJ were unknown. A comprehensively comparison of the chemical profiles between non-fumigated HJ (NHJ) and sulfur-fumigated HJ (SHJ) was conducted by HPLC fingerprints analysis and the discrepant peaks were identified or tentatively assigned by HPLC-ESI/MS(n). Dramatic chemical changes were found that the contents of 4 flavonoid aglycones remarkably increased while those of 7 glycosides significantly reduced which suggested that sulfur-fumigation induced flavonoid glycosides transformed into aglycons by hydrolysis reaction. A significant loss of hydroxycinnamoylquinic acids showed the sulfur fumigation was a destructive effect on HJ. Principal component analysis (PCA) was employed to rapidly discriminate NHJ and SHJ samples. By ICP-OES analysis, it was found that the residue of sulfur of SHJ were three times higher than NHJ (p<0.05). The antioxidant activity of NHJ and SHJ were evaluated by DPPH and FRAP assay, and the results showed that NHJ had much stronger antioxidant activities than SCF (p<0.05). Combining the results of chemical analysis, residue of sulfur and pharmacological evaluation, it showed that the sulfur fumigation was a destructive effect on HJ.

  16. Anti-austeric activity of phenolic constituents of seeds of Arctium lappa.

    PubMed

    Tezuka, Yasuhiro; Yamamoto, Keiichi; Awale, Suresh; Lia, Feng; Yomoda, Satoshi; Kadota, Shigetoshi

    2013-04-01

    From seeds of Arctium lappa L. (Asteraceae) we obtained arctigenin (1), arctiin (2), chlorogenic acid (3), 4,5-dicaffeoylquinic acid (4), 3,5-dicaffeoylquinic acid (5), 3,4-dicaffeoylquinic acid (6), matairesinol (11), isolappaol A (12), lappaol F (14), and lappaol B (15), together with 1:1 mixtures of isolappaol C (7) and lappaol C (8), arctignan E (9) and arctignan D (10), and 12 and lappaol A (13), while 3,3',4'-tri-O-demethylarctigenin (16), 3,3'-di-O-demethyl-4'-dehydroxyarctigenin (17), and 3-O-demethylarctigenin (18) were obtained by anaerobic microbiological metabolism of 1. Then, we evaluated the in vitro preferential cytotoxic activity of these pure compounds and 1:1 mixtures, together with enterodiol (19) and enterolactone (20), against human pancreatic cancer PANC-1 cells in nutrient-deprived medium (NDM). Among them, 1 and 18 showed potent activity, with PC50 values of 1.75 and 4.38 microM, respectively, while 11, 15, and 17 showed mild activity with PC50 values of 31.1, 30.9, and 38.7 microM, respectively. By comparing their structures and PC50 values, the following structural moieties could be concluded to be important for the preferential cytotoxicity of 1: 1) the 3-hydroxy-4-methoxyphenyl group at the 2-position on the gamma-butyrolactone ring, 2) the less polar substituent at the 3-position on the gamma-butyrolactone ring, and 3) the gamma-butyrolactone ring.

  17. Acute toxicity, antiedematogenic activity, and chemical constituents of Palicourea rigida Kunth.

    PubMed

    Alves, Vanessa G; da Rosa, Elisa A; de Arruda, Laura L M; Rocha, Bruno A; Bersani Amado, Ciomar A; Santin, Silvana M O; Pomini, Armando M; da Silva, Cleuza C

    2016-03-01

    The phytochemical study of the leaves, roots, and flowers of Palicourea rigida led to the isolation of the triterpenes betulinic acid (1) and lupeol (2), the diterpene phytol (3), and the iridoid glycosides sweroside (4) and secoxyloganin (5). These compounds were identified using NMR 1H and 13C and comparing the spectra with published data. We studied the antiedematogenic activity of crude extracts from the organs, and of different fractions, in mice and found that the n-hexane fraction of the leaf extract significantly inhibited the ear edema resulting from croton oil administration. The crude extract from leaves was not acutely toxic to the mice.

  18. Historic activity of mt. Vesuvius: major elements and volatile constituents of primary melts

    NASA Astrophysics Data System (ADS)

    Cecchetti, A.; Marianelli, P.; Metrich, N.; Sbrana, A.

    2003-04-01

    Mt. Vesuvius experienced a three-century long period of semi-persistent activity, after the 1631 eruption and is presently in a phase of rest. During this period, several eruptions displayed composite style since they started with lava effusions and evolved towards explosive activity (lava fountains, phreatomagmatic explosions and occasionally steady columns). The tephrostratigraphic sequence of post-1631 activity is well reconstructed [1] on the basis of historical chronicles and field investigations, whereas information about the feeding system is still weak. We have selected samples related to energetic lava fountain activity that occurred during the 1794, 1822 and 1872 composite-style eruptions for investigating the deep feeding systems of Mt. Vesuvius, during the 1631--1944 period. We present data on melt inclusions and their host olivines. Major elements, S, Cl and F were obtained using the electron microprobe (SX50, Camparis), CO_2 and H_2O by Fourier Transform InfraRed spectroscopy. Carbon was also analysed by nuclear reaction 12C(d,p)13C. The magma batches emitted during the 1794, 1822 and 1872 eruptions brought to the surface primitive olivines (Fo90.4-88.5) containing spinel (Cr/(Cr+Al) = 0.77--0.75). Their inclusions attest of crystallization at high pressure from K-rich (HK) parental magmas with K_2O varying from 4.3 to 6.0, high K_2O/H_2O (up to 2.4), Cl/H_2O (up to 0.25), Cl/F (up to 3) ratios, and H_2O content systematically high and variable from 2.3 to 4.9 wt.%. The most primitive compositions are recorded in melt inclusions from the oldest samples (1794 and 1822 eruptions). We propose a rather rapid transfer of HK-melts carrying olivine crystals from depth. This process is only detectable by the means of melt inclusions in Fo-rich olivines phenocrysts occurring only in the deposits related to the most powerful episodes of lava fountains while the whole rocks are cumulative with respect to clinopyroxene (± leucite). These new data, in addition to

  19. Chemical Constituents from Andrographis echioides and Their Anti-Inflammatory Activity

    PubMed Central

    Shen, De-Yang; Juang, Shin-Hun; Kuo, Ping-Chung; Huang, Guan-Jhong; Chan, Yu-Yi; Damu, Amooru G.; Wu, Tian-Shung

    2013-01-01

    Phytochemical investigation of the whole plants of Andrographis echioides afforded two new 2′-oxygenated flavonoids (1) and (2), two new phenyl glycosides (3) and (4), along with 37 known structures. The structures of new compounds were elucidated by spectral analysis and chemical transformation studies. Among the isolated compounds, (1–2) and (6–19) were subjected into the examination for their iNOS inhibitory bioactivity. The structure-activity relationships of the flavonoids for their inhibition of NO production were also discussed. PMID:23271366

  20. Activity-guided isolation of cytotoxic bis-bibenzyl constituents from Dumortiera hirsuta.

    PubMed

    Toyota, Masao; Ikeda, Risa; Kenmoku, Hiromichi; Asakawa, Yoshinori

    2013-01-01

    Activity-guided fractionation of the ether extract of Dumortiera hirsute (Japanese liverwort), using cytotoxicity testing with cultured HL 60 and KB cells, resulted in the isolation of a new cytotoxic bis-bibenzyl compound, along with the two known bis-bibenzyls: isomarchantin C and isoriccardin C. The structural determination of the new bis-bibenzyl through extensive NMR spectral data indicated a derivative of marchantin A, which has been isolated from the liverwort Marchantia polymorpha. The cytotoxicity of the bis-bibenzyls was evaluated by the MTT (3-(4,5-di-methylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay using cultured HL 60 and KB cells.

  1. Volatile constituents of Dianthus rupicola Biv. from Sicily: activity against microorganisms affecting cellulosic objects.

    PubMed

    Casiglia, Simona; Bruno, Maurizio; Senatore, Felice

    2014-01-01

    Dianthus rupicola Biv. (cliffs carnation) is a camephytic, suffruticous, perennial plant growing up to 40 cm high. The plant is widespread in Sicily and neighbouring islands (Egadi, Lampedusa, Lipari) and in some areas of southern Italy. GC and GC-MS analyses of the essential oil distilled from the flowers showed the presence of 66 components. Its composition is characterised by the high content of thymol and carvacrol derivatives. A good antibacterial activity against Bacillus cereus and Bacillussubtilis, both infesting cellulosic historical material, was shown, whereas the antioxidant capacity was determined to be quite poor.

  2. Anti-inflammatory Activity of Constituents Isolated from Aerial Part of Angelica acutiloba Kitagawa.

    PubMed

    Uto, Takuhiro; Tung, Nguyen Huu; Taniyama, Risa; Miyanowaki, Tosihide; Morinaga, Osamu; Shoyama, Yukihiro

    2015-12-01

    Recently, the resources of medicinal plants have been exhausting. The root of Angelica acutiloba is one of the most important ingredients in Japanese Kampo medicine for the treatment of gynecological diseases. In our search for alternative medicinal plant resources of the root of A. acutiloba, we found that its aerial part has the anti-inflammatory potency as well as the root. Phytochemical investigation of the aerial part resulted in the isolation of four compounds including a new dimeric phthalide, namely tokiaerialide (2), along with Z-ligustilide (1), falcarindiol (3), and bergaptol (4). Next, we investigated the in vitro anti-inflammatory activity of 1-4 in lipopolysaccharide-stimulated RAW264 macrophages. Among the isolated compounds, 1 exhibited the most potent inhibition against lipopolysaccharide-induced production of prostaglandin E2 , nitric oxide, and pro-inflammatory cytokines (interleukin-6 and tumor necrosis factor-α). Compounds 3 and 4 also inhibited all inflammatory mediators, but their inhibitory abilities were weaker than those of 1. Furthermore, 1, 3, and 4 strongly also induced heme oxygenase-1. These results suggest that 1, 3, and 4 potentially exert anti-inflammatory activity, and the aerial part of A. acutiloba may be considered to be a useful medicinal resource for inflammatory diseases.

  3. Antioxidant Activities and Chemical Constituents of Flavonoids from the Flower of Paeonia ostii.

    PubMed

    Zhang, Huifang; Li, Xiaofang; Wu, Ke; Wang, Mengke; Liu, Pu; Wang, Xinsheng; Deng, Ruixue

    2016-12-23

    Paeonia ostii is a traditional medicinal plant popularly used in China. This study intended to evaluate the antioxidant properties and the chemical components of the flavonoid-rich extracts from the flowers of P. ostii. The results showed that the flavonoid-rich extracts from the flowers of P. ostii had strong scavenging capacities on 2,2'-Azinobis-(3-ethylbenzthiazoline-6-sulphonate) (ABTS), hydroxyls, superoxide anions, and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals in a dose-dependent manner. Five flavonoids, dihydrokaempferol (1), apigenin-7-O-β-d-glucoside (2), apigenin-7-O-β-d-neohesperidoside (3), kaempferol-7-O-β-d-glucopyranoside (4), and kaempferol-3-O-β-d-glucopyranosyl-7-O-β-d-glucopyranoside (5), were isolated from the flavonoid-rich extracts of the flowers of P. ostii. High-performance liquid chromatography (HPLC) analysis revealed that compounds 3 and 4 were abundant in the P. ostii flower and in flavonoid-rich extracts. The main components of the flower of P. ostii are flavonoids. The high antioxidant activity of the flavonoid-rich extracts may be attributed to the high content of flavonoids. The five isolated flavonoids were the primary antioxidant ingredients, and may play important roles in the strong antioxidant activities of this flower. Based on the obtained results, the flower of P. ostii could be a potential source of natural antioxidants in food and pharmaceutical applications.

  4. Odor-active constituents in fresh pineapple (Ananas comosus [L.] Merr.) by quantitative and sensory evaluation.

    PubMed

    Tokitomo, Yukiko; Steinhaus, Martin; Büttner, Andrea; Schieberle, Peter

    2005-07-01

    By application of aroma extract dilution analysis (AEDA) to an aroma distillate prepared from fresh pineapple using solvent-assisted flavor evaporation (SAFE), 29 odor-active compounds were detected in the flavor dilution (FD) factor range of 2 to 4,096. Quantitative measurements performed by stable isotope dilution assays (SIDA) and a calculation of odor activity values (OAVs) of 12 selected odorants revealed the following compounds as key odorants in fresh pineapple flavor: 4-hydroxy-2,5-dimethyl-3(2H)-furanone (HDF; sweet, pineapple-like, caramel-like), ethyl 2-methylpropanoate (fruity), ethyl 2-methylbutanoate (fruity) followed by methyl 2-methylbutanoate (fruity, apple-like) and 1-(E,Z)-3,5-undecatriene (fresh, pineapple-like). A mixture of these 12 odorants in concentrations equal to those in the fresh pineapple resulted in an odor profile similar to that of the fresh juice. Furthermore, the results of omission tests using the model mixture showed that HDF and ethyl 2-methylbutanoate are character impact odorants in fresh pineapple.

  5. Antioxidant activity of prune (Prunus domestica L.) constituents and a new synergist.

    PubMed

    Kayano, Shin-Ichi; Kikuzaki, Hiroe; Fukutsuka, Naoko; Mitani, Takahiko; Nakatani, Nobuji

    2002-06-19

    Ethanol extract of prune was separated into hexane-soluble and H(2)O-soluble fractions, and the H(2)O-soluble fraction was further separated into a methanol (MeOH) eluate and an H(2)O eluate by Diaion HP-20 column chromatography. The MeOH eluate exhibited the strongest antioxidant activity among the separated fractions evaluated by oxygen radical absorbance capacity (ORAC). Further purification of the MeOH eluate led to isolation of a novel compound, 4-amino-4-carboxychroman-2-one, together with four known compounds (p-coumaric acid, vanillic acid beta-glucoside, protocatechuic acid, and caffeic acid), structures of which were identified by NMR and MS analyses. The ORAC values of these isolated compounds showed 0.15-1.43 units (micromol of Trolox equiv)/micromol, and the new compound showed a remarkable synergistic effect on caffeoylquinic acid isomers. The antioxidant activity of the MeOH eluate was highly dependent on the major prune components, caffeoylquinic acid isomers, with a contribution from the new synergist.

  6. Functional constituents and antioxidant activities of eight Chinese native goji genotypes.

    PubMed

    Zhang, Qiuyun; Chen, Weiwei; Zhao, Jianhua; Xi, Wanpeng

    2016-06-01

    We quantified the levels of polyphenols, carotenoids and polysaccharides in fruits of the eight Chinese native goji genotypes, antioxidant activities of these fruit extracts were also evaluated by DPPH, ABTS and FRAP methods. Quercetin-rhamno-di-hexoside (435-1065 μg/g) and quercetin-3-O-rutinoside (159-629 μg/g) were found to be the predominant flavonoids. Chlorogenic acid was the most abundant phenolic acid (113-526 μg/g), while zeaxanthin (17-9306 μg/g) was the major carotenoid. The total antioxidant activities (TAA) of the berry extracts were significantly correlated with the total polysaccharide and phenolic contents, but not with total carotenoid (TC) levels. Overall, fruits of the Ningxia goji (Lycium barbarum L.) genotypes, DM (Damaye), NJ1 (Ningji No.1), BH (Baihua) and NH (Ningxiahuangguo) were not only rich in polyphenols, carotenoids and polysaccharides, but had significantly higher TAA than those of the other genotypes, suggesting that they represent an excellent source of antioxidants for human nutrition.

  7. Flavonoid constituents in the leaves of Myrica rubra sieb. et zucc. with anti-inflammatory activity.

    PubMed

    Kim, Han Hyuk; Kim, Dong Hee; Kim, Manh Heun; Oh, Myoeng Hwan; Kim, So Ra; Park, Kwang Jun; Lee, Min Won

    2013-12-01

    The leaves of Myrica rubra sieb. et zucc. have been used in oriental traditional medicine for the treatment of burns, skin diseases, and as an antidiarrheal in China, Japan, and Korea. Activity guided isolation of the leaves of M. rubra has led to the isolation of five flavonoid: myricetin (1), myricitrin (2), myricetin 3-O-(2″-O-galloyl)-α-L-rhamnopyranoside (3), myricetin 3-O-(2″-O-galloyl)-β-D-galactopyranoside (4), and quercetin 3-O-(2″-O-galloyl)-β-D-galactopyranoside (5). All isolates were evaluated for their antioxidant potency against the superoxide anion (O2 (-)), and compounds 3-5 showed potent scavenging activities with 50 % inhibition concentration (IC50) values compared to the positive control, allopurinol. Compounds 1-5 were evaluated as inhibitors of various macrophage functions involved in the inflammatory process. These five compounds significantly and dose dependently inhibited lipopolysaccharide (LPS)-stimulated nitric oxide (NO), pro-inflammatory cytokines, and the protein levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in LPS-stimulated RAW 264.7 macrophages. Our results suggest that galloyl flavonol glycosides (3-5) isolated from M. rubra might be beneficial for the treatment of inflammation-related diseases.

  8. Volatile constituents from Cinnamomum zeylanicum fruit stalks and their antioxidant activities.

    PubMed

    Jayaprakasha, Guddadarangavvanahally K; Jagan Mohan Rao, Lingamallu; Sakariah, Kunnumpurath K

    2003-07-16

    Cinnamomum zeylanicum Blume is an important spice and aromatic crop having wide applications in flavoring, perfumery, beverages, and medicines. The steam-distilled volatile oil from cinnamon fruit stalks was analyzed with GC and GC-MS. It showed the presence of hydrocarbons (44.7%) and oxygenated compounds (52.6%). Twenty-seven compounds constituting ca. 95.98% of the volatile oil were characterized. (E)-Cinnamyl acetate (36.59%) and (E)-caryophyllene (22.36%) are found to be major compounds. The volatile oil was screened for its potential as an antioxidant by using in vitro models, such as the beta-carotene-linoleate and phosphomolybdenum complex method. The volatile oil showed 55.94% and 66.9% antioxidant activity at 100 and 200 ppm concentration, respectively. Also, the volatile oil showed good antioxidant capacity, using the formation of the phosphomolybdenum complex. A comparison of the chemical composition of the volatile oil was made with that of buds, flowers, and fruits. This is the first report on the chemical composition of volatile oil of the fruit stalks of this species and its antioxidant activity.

  9. Nootkatone, a characteristic constituent of grapefruit, stimulates energy metabolism and prevents diet-induced obesity by activating AMPK.

    PubMed

    Murase, Takatoshi; Misawa, Koichi; Haramizu, Satoshi; Minegishi, Yoshihiko; Hase, Tadashi

    2010-08-01

    AMP-activated protein kinase (AMPK) is a serine/threonine kinase that is implicated in the control of energy metabolism and is considered to be a molecular target for the suppression of obesity and the treatment of metabolic syndrome. Here, we identified and characterized nootkatone, a constituent of grapefruit, as a naturally occurring AMPK activator. Nootkatone induced an increase in AMPKalpha1 and -alpha2 activity along with an increase in the AMP/ATP ratio and an increase the phosphorylation of AMPKalpha and the downstream target acetyl-CoA carboxylase (ACC), in C(2)C(12) cells. Nootkatone-induced activation of AMPK was possibly mediated both by LKB1 and Ca(2+)/calmodulin-dependent protein kinase kinase. Nootkatone also upregulated PPARgamma coactivator-1alpha in C(2)C(12) cells and C57BL/6J mouse muscle. In addition, administration of nootkatone (200 mg/kg body wt) significantly enhanced AMPK activity, accompanied by LKB1, AMPK, and ACC phosphorylation in the liver and muscle of mice. Whole body energy expenditure evaluated by indirect calorimetry was also increased by nootkatone administration. Long-term intake of diets containing 0.1% to 0.3% (wt/wt) nootkatone significantly reduced high-fat and high-sucrose diet-induced body weight gain, abdominal fat accumulation, and the development of hyperglycemia, hyperinsulinemia, and hyperleptinemia in C57BL/6J mice. Furthermore, endurance capacity, evaluated as swimming time to exhaustion in BALB/c mice, was 21% longer in mice fed 0.2% nootkatone than in control mice. These findings indicate that long-term intake of nootkatone is beneficial toward preventing obesity and improving physical performance and that these effects are due, at least in part, to enhanced energy metabolism through AMPK activation in skeletal muscle and liver.

  10. Cytotoxic active constituents of essential oils of Curcuma longa and Curcuma zanthorrhiza.

    PubMed

    Schmidt, Erich; Ryabchenko, Boris; Wanner, Juergen; Jäger, Walter; Jirovetz, Leopold

    2015-01-01

    The polar and apolar fractions of Curcuma longa and C. zanthorriza enriched by ar-turmerone, ar-curcumene and xanthorrizol were screened for cytotoxic activity against the HeLa cell line. Actinomycin D and curcumin were used as reference samples, both known for their cytotoxic properties. Amongst all fractions tested, the xanthorrizol fraction (CC50: 26.1 ± 1.9 μM) showed the strongest cytotoxic properties similar to those of curcumin (CC50: 8.1 ± 1.7 μM). Further studies also revealed that the cytotoxic effects of the extracts and pure compounds are caused by apoptosis induction identified by the cleaved form of PARP protein.

  11. Active and responsive polymer surfaces.

    PubMed

    Zhang, Jilin; Han, Yanchun

    2010-02-01

    A central challenge in polymer science today is creating materials that dynamically alter their structures and properties on demand, or in response to changes in their environment. Surfaces represent an attractive area of focus, since they exert disproportionately large effects on properties such as wettability, adhesiveness, optical appearance, and bioactivity, enabling pronounced changes in properties to be accomplished through subtle changes in interfacial structure or chemistry. In this critical review, we review the recent research progress into active and responsive polymer surfaces. The chief purpose of this article is to summarize the advanced preparation techniques and applications in this field from the past decade. This review should be of interest both to new scientists in this field and the interdisciplinary researchers who are working on "intelligent" polymer surfaces (117 references).

  12. Aortic relaxant activity of Crataegus gracilior Phipps and identification of some of its chemical constituents.

    PubMed

    Hernández-Pérez, Abigail; Bah, Moustapha; Ibarra-Alvarado, César; Rivero-Cruz, José Fausto; Rojas-Molina, Alejandra; Rojas-Molina, Juana Isela; Cabrera-Luna, José Alejandro

    2014-12-15

    This study focused on the assessment of the vasorelaxant activity of the organic and aqueous extracts obtained from leaves and fruits of a Mexican hawthorn (Crataegus gracilior) on isolated rat aorta, and on the purification and identification of some of their secondary metabolites by the use of chromatographic and spectroscopic techniques. The results obtained showed that the methanol extract has a significantly more potent and effective vasorelaxant effect than the other tested extracts, with an EC50 = 8.69 ± 4.34 µg/mL and an Emax = 94.6% ± 11.30%, values that are close to that of acetylcholine, the positive control. From the same extract, two major triterpenes were isolated and identified as ursolic and corosolic acids by comparison of their experimental NMR spectroscopic data with those reported in the literature. Chlorogenic acid, rutin, quercetin, kaempferol and (+)-catechin were also identified using HPLC coupled with PDAD. All these compounds have already been proven to possess on their own antihypertensive effect and other benefits on cardiovascular diseases and they can support, at least in part, the traditional use of this plant species.

  13. Chemical constituents from the roots and stems of Erycibe obtusifolia and their in vitro antiviral activity.

    PubMed

    Fan, Long; Wang, Ying; Liang, Ning; Huang, Xiao-Jun; Li, Man-Mei; Fan, Chun-Lin; Wu, Zhen-Long; Li, Yao-Lan; Ye, Wen-Cai

    2013-11-01

    Three new quinic acid derivatives, 4-O-caffeoyl-3-O-sinapoylquinic acid methyl ester (1), 5-O-caffeoyl-4-O-syringoylquinic acid methyl ester (2), and 4-O-caffeoyl-3-O-syringoylquinic acid methyl ester (3), as well as four new coumarin glycosides, 7-O-(3-O-sinapoyl-β-D-glucopyranosyl)-6-methoxycoumarin (12), 7-O-(6-O-sinapoyl-β-D-glucopyranosyl)-6-methoxycoumarin (13), 7-O-(2-O-sinapoyl-β-D-glucopyranosyl)-6-methoxycoumarin (14), and 7-O-(6-O-syringoyl-β-D-glucopyranosyl)-6-methoxycoumarin (15), together with eight known compounds (4-11) were isolated from the roots and stems of Erycibe obtusifolia. Their structures were elucidated on the basis of spectroscopic analysis and chemical evidence. All the compounds were screened for their in vitro antiviral activity against respiratory syncytial virus with a cytopathic effect reduction assay. Among them, the di-O-caffeoyl quinates 8-11 displayed a potent in vitro anti-respiratory syncytial virus effect.

  14. Chemical Constituents and Evaluation of Antimicrobial and Cytotoxic Activities of Kielmeyera coriacea Mart. & Zucc. Essential Oils

    PubMed Central

    Martins, Carla de M.; do Nascimento, Evandro A.; de Morais, Sérgio A. L.; de Oliveira, Alberto; Chang, Roberto; Cunha, Luís C. S.; Martins, Mário M.; Martins, Carlos Henrique G.; Moraes, Thaís da S.; Rodrigues, Paulla V.; da Silva, Cláudio V.; de Aquino, Francisco J. T.

    2015-01-01

    Many essential oils (EOs) of different plant species possess interesting antimicrobial effects on buccal microorganisms and cytotoxic properties. EOs of Kielmeyera coriacea Mart. & Zucc. were analyzed by gas chromatography coupled to mass spectrometry (GC-MS). The EO from leaves is rich in sesquiterpenes hydrocarbons and oxygenated sesquiterpenes. The three major compounds identified were germacrene-D (24.2%), (E)-caryophyllene (15.5%), and bicyclogermacrene (11.6%). The inner bark EO is composed mainly of sesquiterpenes hydrocarbons and the major components are alpha-copaene (14.9%) and alpha-(E)-bergamotene (13.0%). The outer bark EO is composed mainly of oxygenated sesquiterpenes and long-chain alkanes, and the major components are alpha-eudesmol (4.2%) and nonacosane (5.8%). The wood EO is mainly composed of long-chain alkanes and fatty acids, and the major components are nonacosane (9.7%) and palmitic acid (16.2%). The inner bark EO showed the strongest antimicrobial activity against the anaerobic bacteria Prevotella nigrescens (minimum inhibitory concentration-MIC of 50 µg mL−1). The outer bark and wood EOs showed MICs of 100 µg mL−1 for all aerobic microorganisms tested. The EOs presented low toxicity to Vero cells. These results suggest that K. coriacea, a Brazilian plant, provide initial evidence of a new and alternative source of substances with medicinal interest. PMID:25960759

  15. Antimicrobial activities of Eugenia caryophyllata extract and its major chemical constituent eugenol against Streptococcus pneumoniae.

    PubMed

    Yadav, Mukesh Kumar; Park, Seok-Won; Chae, Sung-Won; Song, Jae-Jun; Kim, Ho Chul

    2013-12-01

    In this study, we investigate the antimicrobial activities of both Eugenia caryophyllata (Ec) extract and its major component eugenol (4-allyl-2-methoxyphenol) against Streptococcus pneumoniae. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were determined by microdilution method. Pneumococcal biofilms were detected by crystal-violet microtiter plate assay, followed by colony-forming unit counts and visualized by scanning electron microscope (SEM). The synergistic effect of eugenol and penicillin was determined by checker-board method. Both the eugenol and the Ec extract inhibited pneumococcal growth in a concentration-dependent manner. The MIC and MBC of eugenol were 0.06% and 0.12%, respectively. Eugenol at a concentration of 0.12% completely killed S. pneumoniae within 60 min of exposure. The kill rate of planktonic cells was most rapid during the first 15 min of contact with eugenol. The addition of eugenol or Ec extract inhibited in vitro biofilm formation. In already established biofilms, the inhibitory effect of eugenol or Ec extract was more significant in terms of cell viability than in terms of disruption of the biofilm matrix. SEM analysis revealed non-viable and disruptive action of eugenol on the cell membrane of bacteria of biofilms. It was found that eugenol and penicillin produced a synergistic effect against S. pneumoniae. In conclusion, eugenol and Ec extract efficiently inhibited S. pneumoniae in planktonic growth and within biofilms.

  16. Constituents of Asparagus officinalis evaluated for inhibitory activity against cyclooxygenase-2.

    PubMed

    Jang, Dae Sik; Cuendet, Muriel; Fong, Harry H S; Pezzuto, John M; Kinghorn, A Douglas

    2004-04-21

    As part of a project directed toward the discovery of new cancer chemopreventive agents from plants, two new natural products, asparagusic acid anti-S-oxide methyl ester (1) and asparagusic acid syn-S-oxide methyl ester (2), a new acetylenic compound, 2-hydroxyasparenyn [3',4'-trans-2-hydroxy-1-methoxy-4-[5-(4-methoxyphenoxy)-3-penten-1-ynyl]-benzene] (3), as well as eleven known compounds, asparenyn (4), asparenyol (5), (+/-)-1-monopalmitin (6), ferulic acid (7), 1,3-O-di-p-coumaroylglycerol (8), 1-O-feruloyl-3-O-p-coumaroylglycerol (9), blumenol C, (+/-)-epipinoresinol, linoleic acid, 1,3-O-diferuloylglycerol, and 1,2-O-diferuloylglycerol, were isolated from an ethyl acetate-soluble fraction of the methanol extract of the aerial parts of Asparagus officinalis (Asparagus), using a bioassay based on the inhibition of cyclooxygenase-2 to monitor chromatographic fractionation. The structures of compounds 1-3 were elucidated by 1D- and 2D-NMR experiments ((1)H NMR, (13)C NMR, DEPT, COSY, HMQC, HMBC and NOESY). All the isolates were evaluated for their inhibitory effects against both cyclooxygenase-1 and -2, with the most active compound being linoleic acid.

  17. Antifungal activity of essential oil and its constituents from Calocedrus macrolepis var. formosana Florin leaf against plant pathogenic fungi.

    PubMed

    Chang, Hui-Ting; Cheng, Ying-Hung; Wu, Chi-Lin; Chang, Shang-Tzen; Chang, Tun-Tschu; Su, Yu-Chang

    2008-09-01

    Resistance to conventional fungicides causes the poor disease control of agriculture. Natural products from plants have great potential as novel fungicide sources for controlling pathogenic fungi. In this study antipathogenic activity of the leaf essential oil and its constituents from Calocedrus macrolepis var. formosana Florin were evaluated in vitro against six plant pathogenic fungi. Chemical analysis of leaf oil by GC/MS allowed identification of alpha-pinene (44.2%), limonene (21.6%), beta-myrcene (8.9%), beta-caryophyllene (8.2%), caryophyllene oxide (2.4%), alpha-cadinol (1.6%), beta-pinene (1.2%), and T-muurolol (1.1%) as main components. Sesquiterpenoid components of the oil were more effective than monoterpenoid components of the oil. In particular, T-muurolol and alpha-cadinol strongly inhibited the growth of Rhizoctonia solani and Fusarium oxysporum, with the IC(50) values < 50 microg ml(-1). These compounds also efficiently inhibited the mycelial growths of Colletotrichum gloeosporioides, P. funerea, Ganoderma australe and F. solani. These results showed that T-muurolol and alpha-cadinol possess antifungal activities against a broad spectrum of tested plant pathogenic fungi and could be used as potential antifungal agents for the control of fungal diseases in plants.

  18. Antifungal activity of Thymus vulgaris L. essential oil and its constituent phytochemicals against Rhizopus oryzae: interaction with ergosterol.

    PubMed

    de Lira Mota, Kelly Samara; de Oliveira Pereira, Fillipe; de Oliveira, Wylly Araújo; Lima, Igara Oliveira; de Oliveira Lima, Edeltrudes

    2012-12-05

    Mucormycoses are emerging infections that have high rates of morbidity and mortality. They show high resistance to antifungal agents, and there is a limited therapeutic arsenal currently available, therefore, there is a great need to give priority to testing therapeutic agents for the treatment of mucormycosis. Along this line, the use of essential oils and phytoconstituents has been emphasized as a new therapeutic approach. The objective of this work was to investigate the antifungal activity of the essential oil (EO) of Thymus vulgaris, and its constituents thymol and p-cymene against Rhizopus oryzae, through microbiological screening, determination of minimal inhibitory concentration (MICs) and minimal fungicidal concentration (MFCs), effects on mycelial growth and germination of sporangiospores and interaction with ergosterol. The MIC of EO and thymol varied 128-512 µg/mL, but the MFC of EO and thymol varied 512-1024 µg/mL and 128-1024 µg/mL, respectively. The results also showed that EO and thymol significantly inhibited mycelial development and germination of sporangiospores. Investigation of the mechanism of antifungal action showed that EO and thymol interact with ergosterol. These data indicate that EO of T. vulgaris and thymol possess strong antifungal activity, which can be related to their interaction with ergosterol, supporting the possible use of these products in the treatment of mucormycosis.

  19. Antibacterial activity and mode of action of the Artemisia capillaris essential oil and its constituents against respiratory tract infection-causing pathogens.

    PubMed

    Yang, Chang; Hu, Dong-Hui; Feng, Yan

    2015-04-01

    Inhalation therapy using essential oils has been used to treat acute and chronic sinusitis and bronchitis. The aim of the present study was to determine the chemical composition of the essential oil of Artemisia capillaris, and evaluate the antibacterial effects of the essential oil and its main components, against common clinically relevant respiratory bacterial pathogens. Gas chromatography and gas chromatography‑mass spectrometry revealed the presence of 25 chemical constituents, the main constituents being: α‑pinene, β‑pinene, limonene, 1,8‑cineole, piperitone, β‑caryophyllene and capillin. The antibacterial activities of the essential oil, and its major constituents, were evaluated against Streptococcus pyogenes, methicillin‑resistant Staphylococcus aureus (MRSA), MRSA (clinical strain), methicillin‑gentamicin resistant Staphylococcus aureus (MGRSA), Streptococcus pneumoniae, Klebsiella pneumoniae, Haemophilus influenzae and Escherichia coli. The essential oil and its constituents exhibited a broad spectrum and variable degree of antibacterial activity against the various strains. The essential oil was observed to be much more potent, as compared with any of its major chemical constituents, exhibiting low minimum inhibitory and bacteriocidal concentration values against all of the bacterial strains. The essential oil was most active against S. pyogenes, MRSA (clinical strain), S. pneumoniae, K. pneumoniae, H. influenzae and E. coli. Piperitone and capillin were the most potent growth inhibitors, among the major chemical constituents. Furthermore, the essential oil of A. capillaris induced significant and dose‑dependent morphological changes in the S. aureus bacterial strain, killing >90% of the bacteria when administered at a higher dose; as determined by scanning electron microscopy. In addition, the essential oil induced a significant leakage of potassium and phosphate ions from the S. aureus bacterial cultures. These results indicate that

  20. Active Response Gravity Offload System

    NASA Technical Reports Server (NTRS)

    Valle, Paul; Dungan, Larry; Cunningham, Thomas; Lieberman, Asher; Poncia, Dina

    2011-01-01

    The Active Response Gravity Offload System (ARGOS) provides the ability to simulate with one system the gravity effect of planets, moons, comets, asteroids, and microgravity, where the gravity is less than Earth fs gravity. The system works by providing a constant force offload through an overhead hoist system and horizontal motion through a rail and trolley system. The facility covers a 20 by 40-ft (approximately equals 6.1 by 12.2m) horizontal area with 15 ft (approximately equals4.6 m) of lifting vertical range.

  1. Acaricidal activities against house dust mites of spearmint oil and its constituents.

    PubMed

    Yang, Ji-Yeon; Kim, Min-Gi; Lee, Sung-Eun; Lee, Hoi-Seon

    2014-02-01

    The aim of this study was to evaluate the acaricidal activities of spearmint oil and carvone derivatives against house dust mites using contact and fumigant toxicity bioassays to replace benzyl benzoate as a synthetic acaricide. Based on the LD50 values, the contact toxicity bioassay revealed that dihydrocarvone (0.95 and 0.88 µg/cm2) was 7.7 and 6.8 times more toxic than benzyl benzoate (7.33 and 6.01 µg/cm2) against Dermatophagoides farinae and Dermatophagoides pteronyssinus, respectively, followed by carvone (3.78 and 3.23 µg/cm2), spearmint oil (5.16 and 4.64 µg/cm2), carveol (6.00 and 5.80 µg/cm2), and dihydrocarveol (8.23 and 7.10 µg/cm2). Results of the fumigant toxicity bioassay showed that dihydrocarvone (2.73 and 2.16 µg/cm2) was approximately 4.0 and 4.8 times more effective than benzyl benzoate (11.00 and 10.27 µg/cm2), followed by carvone (6.63 and 5.78 µg/cm2), carveol (7.58 and 7.24 µg/cm2), spearmint oil (9.55 and 8.10 µg/cm2), and dihydrocarveol (9.79 and 8.14 µg/cm2). Taken together, spearmint oil and carvone derivatives are a likely viable alternative to synthetic acaricides for managing house dust mites.

  2. Chemical constituents of Papulaspora immersa, an endophyte from Smallanthus sonchifolius (Asteraceae), and their cytotoxic activity.

    PubMed

    Gallo, Margareth Borges Coutinho; Cavalcanti, Bruno Coêlho; Barros, Francisco Washington Araújo; Odorico de Moraes, Manoel; Costa-Lotufo, Letícia Veras; Pessoa, Cláudia; Bastos, Jairo Kenupp; Pupo, Mônica Tallarico

    2010-12-01

    Papulaspora immersa H. H. Hotson was isolated from roots and leaves of Smallanthus sonchifolius (Poepp. and Endl.) H. Rob. (Asteraceae), traditionally known as Yacon. The fungus was cultured in rice, and, from the AcOEt fraction, 14 compounds were isolated. Among them, (22E,24R)-8,14-epoxyergosta-4,22-diene-3,6-dione (4), 2,3-epoxy-1,2,3,4-tetrahydronaphthalene-c-1,c-4,8-triol (10), and the chromone papulasporin (13) were new secondary metabolites. The spectral data of the known natural products were compared with the literature data, and their structures were established as the (24R)-stigmast-4-en-3-one (1), 24-methylenecycloartan-3β-ol (2), (22E,24R)-ergosta-4,6,8(14),22-tetraen-3-one (3), (-)-(3R,4R)-4-hydroxymellein (5), (-)-(3R)-5-hydroxymellein (6), 6,8-dihydroxy-3-methylisocoumarin (7), (-)-(4S)-4,8-dihydroxy-α-tetralone (8), naphthalene-1,8-diol (9), 6,7,8-trihydroxy-3-methylisocoumarin (11), 7-hydroxy-2,5-dimethylchromone (12), and tyrosol (14). Compound 4 showed the highest cytotoxic activity against the human tumor cell lines MDA-MB435 (melanoma), HCT-8 (colon), SF295 (glioblastoma), and HL-60 (promyelocytic leukemia), with IC₅₀ values of 3.3, 14.7, 5.0 and 1.6 μM, respectively. Strong synergistic effects were also observed with compound 5 and some of the isolated steroidal compounds.

  3. Evaluation of larvicidal activity of the essential oil of Allium macrostemon Bunge and its selected major constituent compounds against Aedes albopictus (Diptera: Culicidae)

    PubMed Central

    2014-01-01

    Background During the screening programme for new agrochemicals from Chinese medicinal herbs and local wild plants, the essential oil of dried bulbs of Allium macrostemon Bunge (Liliaceae) was found to possess larvicidal activity against mosquitoes. The aim of this research was to determine the larvicidal activity of the essential oil and its major constituent compounds against the larvae of the Culicidae mosquito, Aedes albopictus. Methods Essential oil of A. macrostemon was obtained by hydrodistillation and analyzed by gas chromatography (GC) and gas chromaotography-mass spectrometry (GC-MS). The activity of the essential oil and its two major constituents were evaluated, using World Health Organization (WHO) procedures, against the fourth instar larvae of Ae. albopictus for 24 h and larval mortalities were recorded at various essential oil/compound concentrations ranging from 9.0 - 150 μg/ml. Results The essential oil of A. macrostemon exhibited larvicidal activity against the early fourth instar larvae of Ae. albopictus with an LC50 value of 72.86 μg/ml. The two constituent compounds, dimethyl trisulfide and methyl propyl disulfide possessed strong larvicidal activity against the early fourth instar larvae of Ae. albopictus with LC50 values of 36.36 μg/ml and 86.16 μg/ml, respectively. Conclusion The results indicated that the essential oil of A. macrostemon and its major constituents have good potential as a source for natural larvicides. PMID:24731297

  4. Stereoselective Effects of Abused "Bath Salt" Constituent 3,4-Methylenedioxypyrovalerone in Mice: Drug Discrimination, Locomotor Activity, and Thermoregulation.

    PubMed

    Gannon, Brenda M; Williamson, Adrian; Suzuki, Masaki; Rice, Kenner C; Fantegrossi, William E

    2016-03-01

    3,4-Methylenedioxypyrovalerone (MDPV) is a common constituent of illicit "bath salts" products. MDPV is a chiral molecule, but the contribution of each enantiomer to in vivo effects in mice has not been determined. To address this, mice were trained to discriminate 10 mg/kg cocaine from saline, and substitutions with racemic MDPV, S(+)-MDPV, and R(-)-MDPV were performed. Other mice were implanted with telemetry probes to monitor core temperature and locomotor responses elicited by racemic MDPV, S(+)-MDPV, and R(-)-MDPV under a warm (28°C) or cool (20°C) ambient temperature. Mice reliably discriminated the cocaine training dose from saline, and each form of MDPV fully substituted for cocaine, although marked potency differences were observed such that S(+)-MDPV was most potent, racemic MDPV was less potent than the S(+) enantiomer, and R(-)-MDPV was least potent. At both ambient temperatures, locomotor stimulant effects were observed after doses of S(+)-MDPV and racemic MDPV, but R(-)-MDPV did not elicit locomotor stimulant effects at any tested dose. Interestingly, significant increases in maximum core body temperature were only observed after administration of racemic MDPV in the warm ambient environment; neither MDPV enantiomer altered core temperature at any dose tested, at either ambient temperature. These studies suggest that all three forms of MDPV induce biologic effects, but R(-)-MDPV is less potent than S(+)-MDPV and racemic MDPV. Taken together, these data suggest that the S(+)-MDPV enantiomer is likely responsible for the majority of the biologic effects of the racemate and should be targeted in therapeutic efforts against MDPV overdose and abuse.

  5. Constituents of leaves from Bauhinia curvula Benth. exert gastroprotective activity in rodents: role of quercitrin and kaempferol.

    PubMed

    Beber, Ana Paula; de Souza, Priscila; Boeing, Thaise; Somensi, Lincon Bordignon; Mariano, Luísa Nathália Bolda; Cury, Benhur Judah; Burci, Ligia Moura; da Silva, Cristiane Bezerra; Simionatto, Euclésio; de Andrade, Sérgio Faloni; da Silva, Luísa Mota

    2017-02-07

    The Bauhinia genus is known as "Pata-de-Vaca" and a wide variety of these species are used in Brazilian folk medicine due to their gastroprotective properties. This study aimed to investigate the antiulcer efficacy of the hydroalcoholic extract from B. curvula (HEBC) leaves, as well as its semi-purified fraction (SPFr) and the contribution of their phytochemicals constituents for this effect. For that, ethanol 60%/HCl 0.3 M- and indomethacin-induced gastric ulcer were performed in rodents. Gastric ulcerated tissues were processed for histological, histochemical and biochemical analysis. The oral treatment with HEBC and SPFr decreased the gastric ulcer induced by ethanol/HCl in mice and by indomethacin (only HEBC) in rats. The gastroprotective effect of HEBC was abolished in mice pretreated with Nω-Nitro-L-arginine methyl ester, N-Ethylmaleimide, glibenclamide or indomethacin. Both HEBC and SPFr reduced myeloperoxidase activity in parallel with a decrease of lipoperoxides content at the site of the lesion. On the other hand, HEBC did not alter volume, pH, total acidity or pepsin activity of acid gastric secretion in rats, and neither inhibited the in vitro H(+),K(+)-ATPase activity. Additionally, the compounds identified and isolated from the SPFr, the flavonoids quercitrin (65%) and kaempferol (35%), were able to diminish the extent of ulcerated area induced by both ethanol/HCl and indomethacin. Taking together, these findings show that B. curvula extracts present gastroprotective effect, mainly explained by the presence of flavonoids quercitrin and kaempferol, which may possibly improve the defensive factors of gastric mucosa.

  6. Shallominthe Active Antimicrobial Constituent of Persian Shallot in Treatment of Oral Herpes: A Double-Blind Randomized Clinical Trial

    PubMed Central

    Pipelzadeh, Mohammad Hassan; Amin, Mansour; Shiravi Khozani, Abolfazl; Radmanesh, Mohammad

    2014-01-01

    Background: Previous studies showed that shallomin, the active antimicrobial constituent of Persian shallot, has a wide range of antibacterial and antifungal properties. Objectives: The objective of this randomized clinical trial was to evaluate the effectiveness of topical shallomin alcoholic solution in treatment of cold sore. Patients and Methods: A total of 60 volunteers who met the inclusion criteria were randomly allocated to two equal groups to hourly apply topical of either 0.5% shallomin alcoholic solution or placebo within the first 24 hours of developing cold sores. All the cases were reassessed at six-hour intervals. Results: The cold sores were cleared within six hours among 30% of cases who received shallomin solution and the remaining of the cases in this group were cleared between 6six to 24 hours of application. In the placebo group, clearance of the sores occurred in four cases between 48 to 72 hours and the remaining of cases were cleared after 72 hours. Conclusions: The results of this study demonstrated that shallomin is a useful natural remedy in preventing the progression and treatment of cold sores and can significantly reduce the duration of ulceration. PMID:25237646

  7. The Effect of Zataria multiflora and its Constituent, Carvacrol, on Tracheal Responsiveness and Lung Pathology in Guinea Pig Model of COPD.

    PubMed

    Gholami Mahtaj, L; Boskabady, M H; Mohamadian Roshan, N

    2015-05-01

    The effects of Zataria multiflora (Z. multiflora) and its constituent, carvacrol, in guinea pigs model of chronic obstructive pulmonary disease (COPD) were examined. Animals were divided into control, COPD, COPD + drinking water containing three concentrations of extract of Z. multiflora (0.4, 0.8 and 1.6 mg/ml), COPD + drinking water containing three concentrations of carvacrol (60, 120 and 240 µg/ml) and COPD + dexamethasone (50 µg/ml). COPD was induced by exposing animals to cigarette smoke for 3 months. Emphysema as a pathological change of the lung and tracheal responsiveness were measured (n = 5 for control and COPD groups and n = 6 for another groups). Tracheal responsiveness (p < 0.05) and emphysema were significantly increased (p < 0.001) in COPD compared to the control group. Tracheal responsiveness in COPD groups treated with two higher concentrations of the Z. multiflora and three concentrations of carvacrol, and emphysema in treated with highest concentration of Z. multiflora and carvacrol were significantly improved compared to COPD group. Studied parameters were also significantly improved in the treated group with dexamethasone compared to COPD animals (p < 0.05 to p < 0.01). The results indicated a preventive effect of Z. multiflora extract and its constituent, carvacrol, on tracheal responsiveness and pathological changes of the lung.

  8. In vivo effects of abused 'bath salt' constituent 3,4-methylenedioxypyrovalerone (MDPV) in mice: drug discrimination, thermoregulation, and locomotor activity.

    PubMed

    Fantegrossi, William E; Gannon, Brenda M; Zimmerman, Sarah M; Rice, Kenner C

    2013-03-01

    In recent years, synthetic analogues of naturally occurring cathinone have emerged as psychostimulant-like drugs of abuse in commercial 'bath salt' preparations. 3,4-Methylenedioxypyrovalerone (MDPV) is a common constituent of these illicit products, and its structural similarities to the more well-known drugs of abuse 3,4-methylenedioxymethamphetamine (MDMA), and methamphetamine (METH) suggest that it may have similar in vivo effects to these substances. In these studies, adult male NIH Swiss mice were trained to discriminate 0.3 mg/kg MDPV from saline, and the interoceptive effects of a range of substitution doses of MDPV, MDMA, and METH were then assessed. In separate groups of mice, surgically implanted radiotelemetry probes simultaneously monitored thermoregulatory and locomotor responses to various doses of MDPV and MDMA, as a function of ambient temperature. We found that mice reliably discriminated the MDPV training dose from saline and that cumulative doses of MDPV, MDMA, and METH fully substituted for the MDPV training stimulus. All three drugs had similar ED(50) values in this procedure. Stimulation of motor activity was observed following administration of a wide range of MDPV doses (1-30 mg/kg), and the warm ambient temperature potentiated motor activity and elicited profound stereotypy and self-injurious behavior at 30 mg/kg. In contrast, MDPV-induced hyperthermic effects were observed in only the warm ambient environment. This pattern of effects is in sharp contrast to MDMA, where ambient temperature interacts with thermoregulation, but not locomotor activity. These studies suggest that although the interoceptive effects of MDPV are similar to those of MDMA and METH, direct effects on thermoregulatory processes and locomotor activity are likely mediated by different mechanisms than those of MDMA.

  9. Activation of TGF-β Pathway by Areca Nut Constituents: A Possible Cause of Oral Submucous Fibrosis

    PubMed Central

    Khan, Imran; Kumar, Neeraj; Pant, Ila; Narra, Sivakrishna; Kondaiah, Paturu

    2012-01-01

    Oral submucous fibrosis (OSF) is a chronic inflammatory disease characterized by the accumulation of excess collagen, and areca nut chewing has been proposed as an important etiological factor for disease manifestation. Activation of transforming growth factor-β signaling has been postulated as the main causative event for increased collagen production in OSF. Oral epithelium plays important roles in OSF, and arecoline has been shown to induce TGF-β in epithelial cells. In an attempt to understand the role of areca nut constituents in the manifestation of OSF, we studied the global gene expression profile in epithelial cells (HaCaT) following treatment with areca nut water extract or TGF-β. Interestingly, 64% of the differentially regulated genes by areca nut water extract matches with the TGF-β induced gene expression profile. Out of these, expression of 57% of genes was compromised in the presence of ALK5 (TβRI) inhibitor and 7% were independently induced by areca nut, highlighting the importance of TGF-β in areca nut actions. Areca nut water extract treatment induced p-SMAD2 and TGF-β downstream targets in HaCaT cells but not in human gingival fibroblast cells (hGF), suggesting epithelial cells could be the source of TGF-β in promoting OSF. Water extract of areca nut consists of polyphenols and alkaloids. Both polyphenol and alkaloid fractions of areca nut were able to induce TGF-β signaling and its downstream targets. Also, SMAD-2 was phosphorylated following treatment of HaCaT cells by Catechin, Tannin and alkaloids namely Arecoline, Arecaidine and Guvacine. Moreover, both polyphenols and alkaloids induced TGF-β2 and THBS1 (activator of latent TGF-β) in HaCaT cells suggesting areca nut mediated activation of p-SMAD2 involves up-regulation and activation of TGF-β. These data suggest a major causative role for TGF-β that is induced by areca nut in OSF progression. PMID:23284772

  10. Traditional Chinese Nootropic Medicine Radix Polygalae and Its Active Constituent Onjisaponin B Reduce β-Amyloid Production and Improve Cognitive Impairments

    PubMed Central

    Li, Xiaohang; Cui, Jin; Yu, Yang; Li, Wei; Hou, Yujun; Wang, Xin; Qin, Dapeng; Zhao, Cun; Yao, Xinsheng; Zhao, Jian; Pei, Gang

    2016-01-01

    Decline of cognitive function is the hallmark of Alzheimer’s disease (AD), regardless of the pathological mechanism. Traditional Chinese medicine has been used to combat cognitive impairments and has been shown to improve learning and memory. Radix Polygalae (RAPO) is a typical and widely used herbal medicine. In this study, we aimed to follow the β-amyloid (Aβ) reduction activity to identify active constituent(s) of RAPO. We found that Onjisaponin B of RAPO functioned as RAPO to suppress Aβ production without direct inhibition of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) and γ-secretase activities. Our mechanistic study showed that Onjisaponin B promoted the degradation of amyloid precursor protein (APP). Further, oral administration of Onjisaponin B ameliorated Aβ pathology and behavioral defects in APP/PS1 mice. Taken together, our results indicate that Onjisaponin B is effective against AD, providing a new therapeutic agent for further drug discovery. PMID:26954017

  11. Traditional Chinese Nootropic Medicine Radix Polygalae and Its Active Constituent Onjisaponin B Reduce β-Amyloid Production and Improve Cognitive Impairments.

    PubMed

    Li, Xiaohang; Cui, Jin; Yu, Yang; Li, Wei; Hou, Yujun; Wang, Xin; Qin, Dapeng; Zhao, Cun; Yao, Xinsheng; Zhao, Jian; Pei, Gang

    2016-01-01

    Decline of cognitive function is the hallmark of Alzheimer's disease (AD), regardless of the pathological mechanism. Traditional Chinese medicine has been used to combat cognitive impairments and has been shown to improve learning and memory. Radix Polygalae (RAPO) is a typical and widely used herbal medicine. In this study, we aimed to follow the β-amyloid (Aβ) reduction activity to identify active constituent(s) of RAPO. We found that Onjisaponin B of RAPO functioned as RAPO to suppress Aβ production without direct inhibition of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) and γ-secretase activities. Our mechanistic study showed that Onjisaponin B promoted the degradation of amyloid precursor protein (APP). Further, oral administration of Onjisaponin B ameliorated Aβ pathology and behavioral defects in APP/PS1 mice. Taken together, our results indicate that Onjisaponin B is effective against AD, providing a new therapeutic agent for further drug discovery.

  12. Antidiabetic Effects of Yam (Dioscorea batatas) and Its Active Constituent, Allantoin, in a Rat Model of Streptozotocin-Induced Diabetes.

    PubMed

    Go, Hyeon-Kyu; Rahman, Md Mahbubur; Kim, Gi-Beum; Na, Chong-Sam; Song, Choon-Ho; Kim, Jin-Shang; Kim, Shang-Jin; Kang, Hyung-Sub

    2015-10-15

    The objective of this study was to investigate the therapeutic efficacies of crude yam (Dioscorea batatas) powder (PY), water extract of yam (EY), and allantoin (the active constituent of yam) in streptozotocin (STZ)-induced diabetic rats with respect to glucose, insulin, glucagon-like peptide-1 (GLP-1), C-peptide, glycated hemoglobin (HbAlc), lipid metabolism, and oxidative stress. For this purpose, 50 rats were divided into five groups: normal control (NC), diabetic control (STZ), and STZ plus treatment groups (STZ + PY, STZ + EY, and STZ + allantoin). After treatment for one-month, there was a decrease in blood glucose: 385 ± 7 in STZ, 231 ± 3 in STZ + PY, 214 ± 11 in STZ + EY, and 243 ± 6 mg/dL in STZ + allantoin, respectively. There were significant statistical differences (p < 0.001) compared to STZ (100%): 60% in STZ + PY, 55% in STZ + EY, and 63% in STZ + allantoin. With groups in the same order, there were significant decreases (p < 0.001) in HbAlc (100% as 24.4 ± 0.6 ng/mL, 78%, 75%, and 77%), total cholesterol (100% as 122 ± 3 mg/dL, 70%, 67%, and 69%), and low-density lipoprotein (100% as 29 ± 1 mg/dL, 45%, 48%, and 38%). There were also significant increases (p < 0.001) in insulin (100% as 0.22 ± 0.00 ng/mL, 173%, 209%, and 177%), GLP-1 (100% as 18.4 ± 0.7 pmol/mL, 160%, 166%, and 162%), and C-peptide (100% as 2.56 ± 0.10 ng/mL, 129%, 132%, and 130%). The treatment effectively ameliorated antioxidant stress as shown by a significant decrease (p < 0.001) in malondialdehyde (100% as 7.25 ± 0.11 nmol/mL, 87%, 86%, and 85%) together with increases (p < 0.01) in superoxide dismutase (100% as 167 ± 6 IU/mL, 147%, 159%, and 145%) and reduced glutathione (100% as 167 ± 6 nmol/mL, 123%, 141%, and 140%). The results indicate that yam and allantoin have antidiabetic effects by modulating antioxidant activities, lipid profiles and by promoting the release of GLP-1, thereby improving the function of β-cells maintaining normal insulin and glucose

  13. Bronchial responsiveness in active steelworkers.

    PubMed

    Corhay, J L; Bury, T; Louis, R; Delavignette, J P; Kayembe, J M; Weber, G; Albert, A; Radermecker, M F

    1998-02-01

    Coke-oven workers are exposed to dust and irritant gases. Therefore they are at risk of developing lung diseases including chronic bronchitis. Nonspecific bronchial hyperresponsiveness (BHR) has been advocated as a potential risk factor predisposing to the development of chronic bronchitis. In a previous study, we showed that prevalence of BHR was higher in retired coke-oven workers than in retired blast furnace workers. The present study was carried out to determine the prevalence of BHR in active steelworkers. Thus, 137 coke-oven workers and 150 blast furnace workers underwent clinical examination, a standardized questionnaire for the study of respiratory symptoms, pulmonary function testing and methacholine aerosol challenge. The study demonstrates a higher prevalence and degree of BHR [provocative concentration of methacholine causing a 20% fall in forced expiratory volume in one second (PC20) < or = 8 mg x mL(-1)] in coke-oven workers than in blast furnace workers (31.4 versus 6.7%; p<0.001). Moreover, the frequency of respiratory symptoms and basal bronchial obstruction were greater among coke-oven workers with BHR in nonresponders. The basal maximum expiratory flow from 25-75% of forced vital capacity and the respiratory symptoms were correlated with bronchial responsiveness. The lack of correlation observed between BHR and the intensity of smoking or years spent in coke-oven environment may be explained by the high proportion of smokers, the worker turnover in the steel plant, and the "healthy worker effect". In conclusion, the higher prevalence and degree of bronchial hyperresponsiveness in coke-oven workers suggests that coke-oven pollutants are more intense irritants than those that escape from blast furnaces.

  14. Autoignition response of n-butanol and its blend with primary reference fuel constituents of gasoline.

    SciTech Connect

    Kumar, Kamal; Zhang, Yu; Sung, Chi -Jen; Pitz, William J.

    2015-04-13

    We study the influence of blending n-butanol on the ignition delay times of n-heptane and iso-octane, the primary reference fuels for gasoline. The ignition delay times are measured using a rapid compression machine, with an emphasis on the low-to-intermediate temperature conditions. The experiments are conducted at equivalence ratios of 0.4 and 1.0, for a compressed pressure of 20 bar, with the temperatures at the end of compression ranging from 613 K to 979 K. The effect of n-butanol addition on the development of the two-stage ignition characteristics for the two primary reference fuels is also examined. The experimental results are compared to predictions obtained using a detailed chemical kinetic mechanism, which has been obtained by a systematic merger of previously reported base models for the combustion of the individual fuel constituents. In conclusion, a sensitivity analysis on the base, and the merged models, is also performed to understand the dependence of autoignition delay times on the model parameters.

  15. Enhancing growth, phytochemical constituents and aphid resistance capacity in cabbage with foliar application of eckol--a biologically active phenolic molecule from brown seaweed.

    PubMed

    Rengasamy, Kannan R R; Kulkarni, Manoj G; Pendota, Srinivasa C; Van Staden, Johannes

    2016-03-25

    Although foliar application of seaweed extracts on plant growth and development has and is extensively studied, reliable knowledge and understanding of the mode of action of particular compound(s) responsible for enhancing plant growth is lacking. A brown seaweed Ecklonia maxima is widely used commercially as a biostimulant to improve plant growth and crop protection. Eckol, a phenolic compound isolated from E. maxima has recently shown stimulatory effects in maize, indicating its potential use as a plant biostimulant. Cabbage is a widely cultivated vegetable crop throughout the world, which requires high input of fertilizers and is susceptible to several aphid borne diseases. This study was conducted to evaluate the effect of foliar application of eckol on the growth, phytochemical constituents and myrosinase activity (aphid resistance capacity) of commercially cultivated cabbage. Foliar application of eckol (10(-6) M) significantly enhanced shoot and root length, shoot and root fresh and dry weight, leaf area and leaf number. This treatment also showed a significant increase in photosynthetic pigments (chlorophyll 'a', chlorophyll 'b', total chlorophyll and carotenoid) compared to the untreated plants. The levels of protein, proline and iridoid glycosides were significantly higher in cabbage leaves with eckol treatment. All the control plants were severely infested with cabbage aphid (Brevicoryne brassicae) but no infestation was observed on the eckol-sprayed plants, which can be attributed to an increase in myrosinase activity. This study reveals dual effects (plant growth promoting and insect repelling) of eckol on cabbage plants that need further investigations both under field conditions and in other brassicaceous species.

  16. The effect of thymoquinone, the main constituent of Nigella sativa on tracheal responsiveness and white blood cell count in lung lavage of sensitized guinea pigs.

    PubMed

    Keyhanmanesh, Rana; Boskabady, Mohammad Hossein; Eslamizadeh, Mohammad Javad; Khamneh, Saeed; Ebrahimi, Mohammad Ali

    2010-02-01

    In previous studies, the relaxant, anticholinergic (functional antagonism) and antihistaminic, effects of Nigella sativa have been demonstrated on guinea pig tracheal chains. In the present study, the prophylactic effect of thymoquinone (one of the constituents of Nigella sativa) on tracheal responsiveness and white blood cell (WBC) count in lung lavage of sensitized guinea pigs was examined. Four groups of sensitized guinea pigs to ovalbumin (OA) were given drinking water alone (group S), drinking water containing low or high concentrations of thymoquinone (S + LTQ and S + HTQ groups) or inhaled fluticasone propionate (FP 250 microg) twice a day (positive control group) (n = 7, for all groups). Tracheal responses of control and four groups of sensitized animals to methacholine at an effective concentration causing 50 % of maximum response (EC(50) M) were measured. Tracheal responses to 0.1 % OA, relative to contraction induced by 10 microM methacholine were also examined. Total WBC and its differential count in lung lavage were also measured. The tracheal responsiveness to methacholine, OA and WBC of S guinea pigs was significantly higher than those of controls (p < 0.001 for all cases). Tracheal responsiveness in S + LTQ, S + HTQ, and FP groups to both methacholine (p < 0.05 to p < 0.001) and OA (p < 0.001 for all cases) was significantly decreased compared to that of the S group. Total WBC was also decreased in all experimental groups compared to that of the S group (p < 0.001 for all groups). There was an increase in eosinophils and a decrease in neutrophils, lymphocytes and monocytes in the S animals compared to the controls (p < 0.001 for all cases). Treatment with both concentrations of thymoquinone and FP variably improved differential WBC count changes compared to the S animals (nonsignificant to p < 0.001). The improvement in tracheal responsiveness, total WBC, eosinophils and lymphocytes changes in the S animals treated with both concentrations of TQ

  17. Variation of the Phytochemical Constituents and Antioxidant Activities of Zingiber officinale var. rubrum Theilade Associated with Different Drying Methods and Polyphenol Oxidase Activity.

    PubMed

    Ghasemzadeh, Ali; Jaafar, Hawa Z E; Rahmat, Asmah

    2016-06-17

    The effects of different drying methods (freeze drying, vacuum oven drying, and shade drying) on the phytochemical constituents associated with the antioxidant activities of Z. officinale var. rubrum Theilade were evaluated to determine the optimal drying process for these rhizomes. Total flavonoid content (TFC), total phenolic content (TPC), and polyphenol oxidase (PPO) activity were measured using the spectrophotometric method. Individual phenolic acids and flavonoids, 6- and 8-gingerol and shogaol were identified by ultra-high performance liquid chromatography method. Ferric reducing antioxidant potential (FRAP) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) assays were used for the evaluation of antioxidant activities. The highest reduction in moisture content was observed after freeze drying (82.97%), followed by vacuum oven drying (80.43%) and shade drying (72.65%). The highest TPC, TFC, and 6- and 8-shogaol contents were observed in samples dried by the vacuum oven drying method compared to other drying methods. The highest content of 6- and 8-gingerol was observed after freeze drying, followed by vacuum oven drying and shade drying methods. Fresh samples had the highest PPO activity and lowest content of flavonoid and phenolic acid compounds compared to dried samples. Rhizomes dried by the vacuum oven drying method represent the highest DPPH (52.9%) and FRAP activities (566.5 μM of Fe (II)/g DM), followed by freeze drying (48.3% and 527.1 μM of Fe (II)/g DM, respectively) and shade drying methods (37.64% and 471.8 μM of Fe (II)/g DM, respectively) with IC50 values of 27.2, 29.1, and 34.8 μg/mL, respectively. Negative and significant correlations were observed between PPO and antioxidant activity of rhizomes. Vacuum oven dried rhizomes can be utilized as an ingredient for the development of value-added food products as they contain high contents of phytochemicals with valuable antioxidant potential.

  18. Emergency Response and Management Activities

    EPA Pesticide Factsheets

    This quarterly report, highlighting accomplishments over the past several months, showcases EPA’s unique emergency response capabilities through the use of cutting-edge technologies and innovative cleanup strategies.

  19. Mephedrone interactions with cocaine: prior exposure to the 'bath salt' constituent enhances cocaine-induced locomotor activation in rats.

    PubMed

    Gregg, Ryan A; Tallarida, Christopher S; Reitz, Allen B; Rawls, Scott M

    2013-12-01

    Concurrent use of mephedrone (4-methylmethcathinone; MEPH) and established drugs of abuse is now commonplace, but knowledge about interactions between these drugs is sparse. The present study was designed to test the hypothesis that prior MEPH exposure enhances the locomotor-stimulant effects of cocaine and methamphetamine (METH). For cocaine experiments, rats pretreated with saline, cocaine (15 mg/kg), or MEPH (15 mg/kg) for 5 days were injected with cocaine after 10 days of drug absence. For METH experiments, rats pretreated with saline, METH (2 mg/kg), or MEPH (15 mg/kg) were injected with METH after 10 days of drug absence. Cocaine challenge produced greater locomotor activity after pretreatment with cocaine or MEPH than after pretreatment with saline. METH challenge produced greater locomotor activity after METH pretreatment than after saline pretreatment; however, locomotor activity in rats pretreated with MEPH or saline and then challenged with METH was not significantly different. The locomotor response to MEPH (15 mg/kg) was not significantly affected by pretreatment with cocaine (15 mg/kg) or METH (0.5, 2 mg/kg). The present demonstration that cocaine-induced locomotor activation is enhanced by prior MEPH exposure suggests that MEPH cross-sensitizes to cocaine and increases cocaine efficacy. Interestingly, MEPH cross-sensitization was not bidirectional and did not extend to METH, suggesting that the phenomenon is sensitive to specific psychostimulants.

  20. Antimicrobial Activity of Tulsi (Ocimum tenuiflorum) Essential Oil and Their Major Constituents against Three Species of Bacteria

    PubMed Central

    Yamani, Hanaa A.; Pang, Edwin C.; Mantri, Nitin; Deighton, Margaret A.

    2016-01-01

    In recent years scientists worldwide have realized that the effective life span of any antimicrobial agent is limited, due to increasing development of resistance by microorganisms. Consequently, numerous studies have been conducted to find new alternative sources of antimicrobial agents, especially from plants. The aims of this project were to examine the antimicrobial properties of essential oils distilled from Australian-grown Ocimum tenuiflorum (Tulsi), to quantify the volatile components present in flower spikes, leaves and the essential oil, and to investigate the compounds responsible for any activity. Broth micro-dilution was used to determine the minimum inhibitory concentration (MIC) of Tulsi essential oil against selected microbial pathogens. The oils, at concentrations of 4.5 and 2.25% completely inhibited the growth of Staphylococcus aureus (including MRSA) and Escherichia coli, while the same concentrations only partly inhibited the growth of Pseudomonas aeruginosa. Of 54 compounds identified in Tulsi leaves, flower spikes, or essential oil, three are proposed to be responsible for this activity; camphor, eucalyptol and eugenol. Since S. aureus (including MRSA), P. aeruginosa and E. coli are major pathogens causing skin and soft tissue infections, Tulsi essential oil could be a valuable topical antimicrobial agent for management of skin infections caused by these organisms. PMID:27242708

  1. Antimicrobial Activity of Tulsi (Ocimum tenuiflorum) Essential Oil and Their Major Constituents against Three Species of Bacteria.

    PubMed

    Yamani, Hanaa A; Pang, Edwin C; Mantri, Nitin; Deighton, Margaret A

    2016-01-01

    In recent years scientists worldwide have realized that the effective life span of any antimicrobial agent is limited, due to increasing development of resistance by microorganisms. Consequently, numerous studies have been conducted to find new alternative sources of antimicrobial agents, especially from plants. The aims of this project were to examine the antimicrobial properties of essential oils distilled from Australian-grown Ocimum tenuiflorum (Tulsi), to quantify the volatile components present in flower spikes, leaves and the essential oil, and to investigate the compounds responsible for any activity. Broth micro-dilution was used to determine the minimum inhibitory concentration (MIC) of Tulsi essential oil against selected microbial pathogens. The oils, at concentrations of 4.5 and 2.25% completely inhibited the growth of Staphylococcus aureus (including MRSA) and Escherichia coli, while the same concentrations only partly inhibited the growth of Pseudomonas aeruginosa. Of 54 compounds identified in Tulsi leaves, flower spikes, or essential oil, three are proposed to be responsible for this activity; camphor, eucalyptol and eugenol. Since S. aureus (including MRSA), P. aeruginosa and E. coli are major pathogens causing skin and soft tissue infections, Tulsi essential oil could be a valuable topical antimicrobial agent for management of skin infections caused by these organisms.

  2. Radical scavenging and antimicrobial activities of Croton zehntneri, Pterodon emarginatus and Schinopsis brasiliensis essential oils and their major constituents: estragole, trans-anethole, β-caryophyllene and myrcene.

    PubMed

    Donati, Maddalena; Mondin, Andrea; Chen, Zheng; Miranda, Fabricio Mendes; do Nascimento, Baraquizio Braga; Schirato, Giulia; Pastore, Paolo; Froldi, Guglielmina

    2015-01-01

    The essential oils (EOs) from the Brazilian species Croton zehntneri, Pterodon emarginatus and Schinopsis brasiliensis were examined for their chemical constituents, and antioxidant and antimicrobial activities. The composition of EOs was determined by using gas chromatography coupled with mass spectrometry analysis, while the antioxidant activity was evaluated through the 1,1-diphenyl-2-picrylhydrazyl (DPPH) and oxygen radical absorbance capacity (ORAC) assays. Furthermore, the antimicrobial activity was investigated against Escherichia coli and Pseudomonas aeruginosa (both Gram-negative), Staphylococcus aureus (Gram-positive) and Candida parapsilosis (fungus). The main components of C. zehntneri, P. emarginatus and S. brasiliensis were identified as estragole, trans-anethole, β-caryophyllene and myrcene. Among the EOs, P. emarginatus showed the highest antioxidant activity, with an IC50 of 7.36 mg/mL and a Trolox equivalent antioxidant capacity of 3748 μmol/g determined by DPPH and ORAC assays, respectively. All EOs showed low activities against the bacterial strains tested, whereas the C. zehntneri oil and its main constituent estragole exhibited an appreciable antifungal activity against C. parapsilosis.

  3. Cutin monomers and surface wax constituents elicit H2O2 in conditioned cucumber hypocotyl segments and enhance the activity of other H2O2 elicitors

    PubMed

    Fauth; Schweizer; Buchala; Markstadter; Riederer; Kato; Kauss

    1998-08-01

    Hypocotyls from etiolated cucumber (Cucumis sativus L.) seedlings were gently abraded at their epidermal surface and cut segments were conditioned to develop competence for H2O2 elicitation. Alkaline hydrolysates of cutin from cucumber, tomato, and apple elicited H2O2 in such conditioned segments. The most active constituent of cucumber cutin was identified as dodecan-1-ol, a novel cutin monomer capable of forming hydrophobic terminal chains. Additionally, the cutin hydrolysates enhanced the activity of a fungal H2O2 elicitor, similar to cucumber surface wax, which contained newly identified alkan-1,3-diols. The specificity of elicitor and enhancement activity was further elaborated using some pure model compounds. Certain saturated hydroxy fatty acids were potent H2O2 elicitors as well as enhancers. Some unsaturated epoxy and hydroxy fatty acids were also excellent H2O2 elicitors but inhibited the fungal elicitor activity. Short-chain alkanols exhibited good elicitor and enhancer activity, whereas longer-chain alkan-1-ols were barely active. The enhancement effect was also observed for H2O2 elicitation by ergosterol and chitosan. The physiological significance of these observations might be that once the cuticle is degraded by fungal cutinase, the cutin monomers may act as H2O2 elicitors. Corrosion of cutin may also bring surface wax constituents in contact with protoplasts and enhance elicitation.

  4. Anointing chemicals and ectoparasites: responses by ticks and mosquitoes to Citrus (Rutaceae) peel exudates and monoterpene constituents

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Some birds and mammals rub their feathers or fur with the fruits or leaves of Citrus spp. or other Rutaceae, presumably to deter ectoparasites. We measured avoidance and other responses by the lone star tick (Amblyomma americanum) and the yellow fever mosquito (Aedes aegypti) to lemon peel exudate a...

  5. Fumigant toxicity and acetylcholinesterase inhibitory activity of 4 Asteraceae plant essential oils and their constituents against Japanese termite (Reticulitermes speratus Kolbe).

    PubMed

    Seo, Seon-Mi; Kim, Junheon; Kang, Jaesoon; Koh, Sang-Hyun; Ahn, Young-Joon; Kang, Kyu-Suk; Park, Il-Kwon

    2014-07-01

    This study investigated the fumigant toxicity of 4 Asteraceae plant essential oils and their constituents against the Japanese termite Reticulitermes speratus Kolbe. Fumigant toxicity varied with plant essential oils or constituents, exposure time, and concentration. Among the tested essential oils, those from Chamaemelum nobile exhibited the strongest fumigant toxicity, followed by those from Santolina chamaecyparissus, Ormenis multicaulis, and Eriocephalus punctulatus at 2 days after treatment. In all, 15, 24, 19, and 9 compounds were identified in the essential oils from C. nobile, E. punctulatus, O. multicaulis, and S. chamaecyparissus, respectively, by using gas chromatography, gas chromatography-mass spectrometry, or open-column chromatography. The identified compounds were tested individually for their fumigant toxicity against Japanese termites. Among the test compounds, trans-pinocarveol, caryophyllene oxide, sabinene hydrate, and santolina alcohol showed strong fumigant toxicity against Japanese termites. Acetylcholinesterase (AChE) inhibition activity of the identified compounds from C. nobile, E. punctulatus, O. multicaulis, and S. chamaecyparissus essential oils were tested to determine the mode of their action. The IC50 values of (+)-α-pinene, (-)-limonene, (-)-α-pinene, β-pinene, and β-phellandrene against Japanese termite AChE were 0.03, 0.13, 0.41, 0.42, and 0.67mg/mL, respectively. Further studies are warranted to determine the potential of these essential oils and their constituents as fumigants for termite control.

  6. Therapeutic Implications of Black Seed and Its Constituent Thymoquinone in the Prevention of Cancer through Inactivation and Activation of Molecular Pathways

    PubMed Central

    Rahmani, Arshad H.; Alzohairy, Mohammad A.; Khan, Masood A.; Aly, Salah M.

    2014-01-01

    The cancer is probably the most dreaded disease in both men and women and also major health problem worldwide. Despite its high prevalence, the exact molecular mechanisms of the development and progression are not fully understood. The current chemotherapy/radiotherapy regime used to treat cancer shows adverse side effect and may alter gene functions. Natural products are generally safe, effective, and less expensive substitutes of anticancer chemotherapeutics. Based on previous studies of their potential therapeutic uses, Nigella sativa and its constituents may be proved as good therapeutic options in the prevention of cancer. Black seeds are used as staple food in the Middle Eastern Countries for thousands of years and also in the treatment of diseases. Earlier studies have shown that N. sativa and its constituent thymoquinone (TQ) have important roles in the prevention and treatment of cancer by modulating cell signaling pathways. In this review, we summarize the role of N. sativa and its constituents TQ in the prevention of cancer through the activation or inactivation of molecular cell signaling pathways. PMID:24959190

  7. Comparison of the anti-inflammatory active constituents and hepatotoxic pyrrolizidine alkaloids in two Senecio plants and their preparations by LC-UV and LC-MS.

    PubMed

    Chen, Pinghong; Wang, Yi; Chen, Lulin; Jiang, Wei; Niu, Yan; Shao, Qing; Gao, Lu; Zhao, Quancheng; Yan, Licheng; Wang, Shufang

    2015-11-10

    Two Senecio plants, Senecio cannabifolius Less. and its variety S. cannabifolius Less. var. integrifolius (Kiodz.) Kidam., were both used as the raw material of Feining granule, a traditional Chinese medicine product for treating respiratory diseases. In this study, the chemical profiles of these two plants were investigated and compared by liquid chromatography-mass spectrometry (LC-MS) and nuclear magnetic resonance (NMR). A total number of 83 constituents, including 55 organic acids, 11 flavonoids, 4 alkaloids, 3 terpenes and 10 other types of compounds, were characterized. The results indicated that the levels of most flavonoids were higher in S. cannabifolius than in S. cannabifolius var. integrifolius, however, the levels of hepatotoxic pyrrolizidine alkaloids (PAs) were higher in S. cannabifolius var. integrifolius than in S. cannabifolius. Fifteen constituents were evaluated on lipopolysaccharides (LPS) induced RAW 264.7 cells, and eleven of them showed inhibition effect against nitric oxide (NO) production. Finally, the levels of ten major constituents (including seven anti-inflammatory active ones) and two PAs in Feining granule from two Senecio plants were determined and compared by the LC-UV and LC-MS methods, respectively. It was found that one organic acid (homogentisic acid) and two PAs (seneciphylline and senecionine) had higher contents in the preparation of S. cannabifolius var. integrifolius than in that of S. cannabifolius, however, the situations were inverse for the levels of four organic acids and flavonoids (chlorogenic acid, hyperoside, isoquercitrin, and isochlorogenic acid B). Based on the above results, S. cannabifolius might be a better raw material for Feining granule than S. cannabifolius var. integrifolius, because it contained more anti-inflammatory constituents and less hepatotoxic PAs than the latter. However, more pharmacological evaluations should be carried out to support the selection. The results in this study were helpful

  8. Antifungal activities of the essential oils in Syzygium aromaticum (L.) Merr. Et Perry and Leptospermum petersonii Bailey and their constituents against various dermatophytes.

    PubMed

    Park, Mi-Jin; Gwak, Ki-Seob; Yang, In; Choi, Won-Sil; Jo, Hyun-Jin; Chang, Je-Won; Jeung, Eui-Bae; Choi, In-Gyu

    2007-10-01

    This study was carried out in order to investigate the potential of using plant oils derived from Leptospermum petersonii Bailey and Syzygium aromaticum L. Merr. Et Perry as natural antifungal agents. The antifungal effects of essential oils at concentrations of 0.05, 0.1, 0.15, and 0.2 mg/ml on the dermatophytes Microsporum canis (KCTC 6591), Trichophyton mentagrophytes (KCTC 6077), Trichophyton rubrum (KCCM 60443), Epidermophyton floccosum (KCCM 11667), and Microsporum gypseum were evaluated using the agar diffusion method. The major constituents of the active fraction against the dermatophytes were identified by gas chromatography-mass spectrometry and high-performance liquid chromatography analysis. The antifungal activities of S. aromaticum oil (clove oil) against the dermatophytes tested were highest at a concentration of 0.2 mg/ml, with an effectiveness of more than 60%. Hyphal growth was completely inhibited in T. mentagrophytes, T. rubrum, and M. gypseum by treatment with clove oil at a concentration of 0.2 mg/ml. Eugenol was the most effective antifungal constituent of clove oil against the dermatophytes T. mentagrophytes and M. canis. Morphological changes in the hyphae of T. mentagrophytes, such as damage to the cell wall and cell membrane and the expansion of the endoplasmic reticulum, after treatment with 0.11 mg/ml eugenol were observed by transmission electron microscopy (TEM). At a concentration of 0.2 mg/ml, L. petersonii oil (LPO) was more than 90% effective against all of the dermatophytes tested, with the exception of T. rubrum. Geranial was determined to be the most active antifungal constituent of L. petersonii oil. Taken together, the results of this study demonstrate that clove and tea tree oils exhibited significant antifungal activities against the dermatophytes tested in this study.

  9. Allelopathic activity and chemical constituents of walnut (Juglans regia) leaf litter in walnut-winter vegetable agroforestry system.

    PubMed

    Wang, Qian; Xu, Zheng; Hu, Tingxing; Rehman, Hafeez Ur; Chen, Hong; Li, Zhongbin; Ding, Bo; Hu, Hongling

    2014-01-01

    Walnut agroforestry systems have many ecological and economic benefits when intercropped with cool-season species. However, decomposing leaf litter is one of the main sources of allelochemicals in such systems. In this study, lettuce (Lactuca sativa var. angustata) was grown in the soil incorporated with walnut leaf litter to assess its allelopathic activity. Lettuce growth and physiological processes were inhibited by walnut leaf litter, especially during early growth stage (1-2 euphylla period) or with large amount of litter addition. The plants treated by small amount of leaf litter recovered their growth afterwards, while the inhibition for 180 g leaf litter persisted until harvest. Twenty-eight compounds were identified in the leaf litter, and several of them were reported to be phytotoxic, which may be responsible for the stress induced by walnut leaf litter. Thus, for highest economic value of vegetables such as lettuce, excessive incorporation of leaf litter should be discouraged.

  10. Antihypercholesterolemic and Antioxidative Potential of an Extract of the Plant, Piper betle, and Its Active Constituent, Eugenol, in Triton WR-1339-Induced Hypercholesterolemia in Experimental Rats.

    PubMed

    Venkadeswaran, Karuppasamy; Muralidharan, Arumugam Ramachandran; Annadurai, Thangaraj; Ruban, Vasanthakumar Vasantha; Sundararajan, Mahalingam; Anandhi, Ramalingam; Thomas, Philip A; Geraldine, Pitchairaj

    2014-01-01

    Hypercholesterolemia is a dominant risk factor for atherosclerosis and cardiovascular diseases. In the present study, the putative antihypercholesterolemic and antioxidative properties of an ethanolic extract of Piper betle and of its active constituent, eugenol, were evaluated in experimental hypercholesterolemia induced by a single intraperitoneal injection of Triton WR-1339 (300 mg/kg b.wt) in Wistar rats. Saline-treated hypercholesterolemic rats revealed significantly higher mean blood/serum levels of glucose, total cholesterol, triglycerides, low density and very low density lipoprotein cholesterol, and of serum hepatic marker enzymes; in addition, significantly lower mean serum levels of high density lipoprotein cholesterol and significantly lower mean activities of enzymatic antioxidants and nonenzymatic antioxidants were noted in hepatic tissue samples from saline-treated hypercholesterolemic rats, compared to controls. However, in hypercholesterolemic rats receiving the Piper betle extract (500 mg/kg b.wt) or eugenol (5 mg/kg b.wt) for seven days orally, all these parameters were significantly better than those in saline-treated hypercholesterolemic rats. The hypercholesterolemia-ameliorating effect was better defined in eugenol-treated than in Piper betle extract-treated rats, being as effective as that of the standard lipid-lowering drug, lovastatin (10 mg/kg b.wt). These results suggest that eugenol, an active constituent of the Piper betle extract, possesses antihypercholesterolemic and other activities in experimental hypercholesterolemic Wistar rats.

  11. Insecticidal and acetylcholine esterase inhibition activity of Apiaceae plant essential oils and their constituents against adults of German cockroach (Blattella germanica).

    PubMed

    Yeom, Hwa-Jeong; Kang, Jae Soon; Kim, Gil-Hah; Park, Il-Kwon

    2012-07-25

    We evaluated the insecticidal and acetylcholine esterase (AChE) inhibition activity of 11 Apiaceae plant essential oils and their constituents in adult male and female Blattella germanica. Of the 11 Apiaceae plant essential oils tested, dill (Anethum graveolens), carvi (Carum carvi), and cumin (Cuminum cyminum) demonstrated >90% fumigant toxicity against adult male German cockroaches at a concentration of 5 mg/filter paper. In a contact toxicity test, dill (Anethum graveolens), carvi (Carum carvi), cumin (Cuminum cyminum), and ajowan (Trachyspermum ammi) produced strong insecticidal activity against adult male and female German cockroaches. Among the test compounds, (S)-(+)-carvone, 1,8-cineole, trans-dihydrocarvone, cuminaldehyde, trans-anethole, p-cymene, and γ-terpinene demonstrated strong fumigant toxicity against adult male and female B. germanica. In a contact toxicity test, carveol, cuminaldehyde, (S)-(+)-carvone, trans-anethole, thymol, and p-cymene showed strong contact toxicity against adult male and female B. germanica. IC(50) values of α-pinene, carvacrol, and dihydrocarvone against female AChE were 0.28, 0.17, and 0.78 mg/mL, respectively. The toxicity of the blends of constituents identified in 4 active oils indicated that carvone, cuminaldehyde, and thymol were major contributors to the fumigant activity or contact toxicity of the artificial blend.

  12. Identification and Molecular Characterization of the Homogentisate Pathway Responsible for Pyomelanin Production, the Major Melanin Constituents in Aeromonas media WS

    PubMed Central

    Wang, He; Qiao, Yunqian; Chai, Baozhong; Qiu, Chenxi; Chen, Xiangdong

    2015-01-01

    The pigmentation of many Aeromonas species has been thought to be due to the production of a L-DOPA (L-3,4-dihydroxyphenylalanine) based melanin. However, in this study we found that although L-DOPA synthesis occurs in the high-melanin-yielding Aeromonas media strain WS, it plays a minor, if any, role in pigmentation. Instead, the pigmentation of A. media strain WS is due to the production of pyomelanin through HGA (homogentisate). Gene products of phhA (encodes phenylalanine hydroxylase), tyrB and aspC (both encode aromatic amino acid aminotransferase), and hppD (encodes 4-hydroxyphenylpyruvate dioxygenase) constitute a linear pathway of converting phenylalanine to HGA and disruption of any one of these genes impairs or blocks pigmentation of A. media strain WS. This HGA biosynthesis pathway is widely distributed in Aeromonas, but HGA is only detectable in the cultures of pigmented Aeromonas species. Heterologous expression of HppD from both pigmented and non-pigmented Aeromonas species in E. coli leads to the production of pyomelanin and thus pigmentation, suggesting that most Aeromonas species have the critical enzymes to produce pyomelanin through HGA. Taken together, we have identified a widely conserved biosynthesis pathway of HGA based pyomelanin in Aeromonas that may be responsible for pigmentation of many Aeromonas species. PMID:25793756

  13. Solar activity, the QBO, and tropospheric responses

    NASA Technical Reports Server (NTRS)

    Tinsley, Brian A.; Brown, Geoffrey M.; Scherrer, Philip H.

    1989-01-01

    The suggestion that galactic cosmic rays (GCR) as modulated by the solar wind are the carriers of the component of solar variability that affects weather and climate has been discussed in the literature for 30 years, and there is now a considerable body of evidence that supports it. Variations of GCR occur with the 11 year solar cycle, matching the time scale of recent results for atmospheric variations, as modulated by the quasibiennial oscillation of equatorial stratospheric winds (the QBO). Variations in GCR occur on the time scale of centuries with a well defined peak in the coldest decade of the little ice age. New evidence is presented on the meteorological responses to GCR variations on the time scale of a few days. These responses include changes in the vertical temperature profile in the troposphere and lower stratosphere in the two days following solar flare related high speed plasma streams and associated GCR decreases, and in decreases in Vorticity Area Index (VAI) following Forbush decreases of GCR. The occurrence of correlations of GCR and meteorological responses on all three time scales strengthens the hypothesis of GCR as carriers of solar variability to the lower atmosphere. Both short and long term tropospheric responses are understandable as changes in the intensity of cyclonic storms initiated by mechanisms involving cloud microphysical and cloud electrification processes, due to changes in local ion production from changes in GCR fluxes and other high energy particles in the MeV to low GeV range. The nature of these mechanisms remains undetermined. Possible stratospheric wind (particularly QBO) effects on the transport of HNO3 and other constituents incorporated in cluster ions and possible condensation and freezing nuclei are considered as relevant to the long term variations.

  14. Constituents from the stem barks of Canarium bengalense with cytoprotective activity against hydrogen peroxide-induced hepatotoxicity.

    PubMed

    Le, Hoang Thi; Ha, Do Thi; Minh, Chau Thi Anh; Kim, Tae Hoon; Van Kiem, Phan; Thuan, Nguyen Duy; Na, Minkyun

    2012-01-01

    Phytochemical investigation of the stem barks of Canarium bengalense (Burseraceace) resulted in the isolation of a new flavone glycoside (5) together with six known compounds (1-4, 6, and 7). The chemical structure of the new compound was elucidated as 3'-hydroxy-7,4'-dimethoxyflavone-5-O-α-L-arabinofuranosyl-(1→6)-β-D-glucopyranoside by means of 1D and 2D NMR ((1)H-(1)H COSY, HMQC, and HMBC) and MS analyses. To evaluate the in vitro cytoprotective effect, the isolates (1-7) were tested against hydrogen peroxide (H(2)O(2))-induced damage in primary cultured hepatocytes. The viability of hepatocytes was increased by treatment with each compound, except compound 1. Compounds 3, 4, and 7 exerted cytoprotective effects comparable to curcumin, the positive control. Our results suggest that the cytoprotective constituents of C. bengalense may contribute to its traditional use in the treatment of tumor and liver damage.

  15. Activation of Nrf2 target enzymes conferring protection against oxidative stress in PC12 cells by ginger principal constituent 6-shogaol.

    PubMed

    Peng, Shoujiao; Yao, Juan; Liu, Yaping; Duan, Dongzhu; Zhang, Xiaolong; Fang, Jianguo

    2015-08-01

    Natural compounds containing phenoxyl groups and/or Michael acceptor units appear to possess antioxidant and cytoprotective properties. The ginger principal constituent 6-shogaol (6-S) represents one of such compounds. In this study, we reported that 6-S efficiently scavenges various free radicals in vitro, and displays remarkable cytoprotection against oxidative stress-induced cell damage in the neuron-like rat pheochromocytoma cell line, PC12 cells. Pretreatment of PC12 cells with 6-S significantly upregulates a series of phase II antioxidant molecules, such as glutathione, heme oxygenase 1, NAD(P)H: quinone oxidoreductase 1, thioredoxin reductase 1, and thioredoxin 1. A mechanistic study revealed that 6-S enhanced the translocation of Nrf2 from the cytosol to the nucleus and knockdown of Nrf2 abolished such protection, indicating that this cytoprotection is mediated by the activation of the transcription factor Nrf2. Another ginger constituent 6-gingerol (6-G), having a similar structure of 6-S but lacking the alpha,beta-unsaturated ketone structure (Michael acceptor moiety), failed to shelter PC12 cells from oxidative stress. Our results demonstrate that 6-S is a novel small molecule activator of Nrf2 in PC12 cells, and suggest that 6-S might be a potential candidate for the prevention of oxidative stress-mediated neurodegenerative disorders.

  16. Physiological Response to Physical Activity in Children.

    ERIC Educational Resources Information Center

    Gilliam, Thomas B.

    This is a report on research in the field of physical responses of children to strenuous activity. The paper is divided into three subtopics: (1) peak performance measure in children; (2) training effects on children; and (3) importance of physical activity for children. Measurements used are oxygen consumption, ventilation, heart rate, cardiac…

  17. Public High School Assistant Principals' Reports of Self-Efficacy in Performing Their Professional Job Responsibilities in Accordance with the Educational Leadership Constituency Council's Standards for Advanced Programs in Educational Leadership

    ERIC Educational Resources Information Center

    Bell, Susan A.

    2011-01-01

    The purpose of this study was to explore and describe public high school assistant principals' reports of self-efficacy (Bandura, 1997) in performing their professional job responsibilities in accordance with the Educational Leadership Constituency Council's (ELCC) Standards for Advanced Programs in Educational Leadership (National Policy Board…

  18. Compilation of data to estimate groundwater migration potential for constituents in active liquid discharges at the Hanford Site

    SciTech Connect

    Ames, L.L.; Serne, R.J.

    1991-03-01

    A preliminary characterization of the constituents present in the 33 liquid waste streams at the US Department of Energy's Hanford Site has been completed by Westinghouse Hanford Company. In addition, Westinghouse Hanford has summarized the soil characteristics based on drill logs collected at each site that receives these liquid wastes. Literature searches were conducted and available Hanford-specific data were tabulated and reviewed. General literature on organic chemicals present in the liquid waste streams was also reviewed. Using all of this information, Pacific Northwest Laboratory has developed a best estimate of the transport characteristics (water solubility and soil adsorption properties) for those radionuclides and inorganic and organic chemicals identified in the various waste streams. We assume that the potential for transport is qualified through the four geochemical parameters: solubility, distribution coefficient, persistence (radiogenic or biochemical half-life), and volatility. Summary tables of these parameters are presented for more than 50 inorganic and radioactive species and more than 50 organic compounds identified in the liquid waste streams. Brief descriptions of the chemical characteristics of Hanford sediments, solubility, and adsorption processes, and of how geochemical parameters are used to estimate migration in groundwater-sediment environments are also presented. Groundwater monitoring data are tabulated for wells neighboring the facilities that receive the liquid wastes. 91 refs., 16 figs., 23 tabs.

  19. Cannabidiol, a Major Non-Psychotropic Cannabis Constituent Enhances Fracture Healing and Stimulates Lysyl Hydroxylase Activity in Osteoblasts.

    PubMed

    Kogan, Natalya M; Melamed, Eitan; Wasserman, Elad; Raphael, Bitya; Breuer, Aviva; Stok, Kathryn S; Sondergaard, Rachel; Escudero, Ana V Villarreal; Baraghithy, Saja; Attar-Namdar, Malka; Friedlander-Barenboim, Silvina; Mathavan, Neashan; Isaksson, Hanna; Mechoulam, Raphael; Müller, Ralph; Bajayo, Alon; Gabet, Yankel; Bab, Itai

    2015-10-01

    Cannabinoid ligands regulate bone mass, but skeletal effects of cannabis (marijuana and hashish) have not been reported. Bone fractures are highly prevalent, involving prolonged immobilization and discomfort. Here we report that the major non-psychoactive cannabis constituent, cannabidiol (CBD), enhances the biomechanical properties of healing rat mid-femoral fractures. The maximal load and work-to-failure, but not the stiffness, of femurs from rats given a mixture of CBD and Δ(9) -tetrahydrocannabinol (THC) for 8 weeks were markedly increased by CBD. This effect is not shared by THC (the psychoactive component of cannabis), but THC potentiates the CBD stimulated work-to-failure at 6 weeks postfracture followed by attenuation of the CBD effect at 8 weeks. Using micro-computed tomography (μCT), the fracture callus size was transiently reduced by either CBD or THC 4 weeks after fracture but reached control level after 6 and 8 weeks. The callus material density was unaffected by CBD and/or THC. By contrast, CBD stimulated mRNA expression of Plod1 in primary osteoblast cultures, encoding an enzyme that catalyzes lysine hydroxylation, which is in turn involved in collagen crosslinking and stabilization. Using Fourier transform infrared (FTIR) spectroscopy we confirmed the increase in collagen crosslink ratio by CBD, which is likely to contribute to the improved biomechanical properties of the fracture callus. Taken together, these data show that CBD leads to improvement in fracture healing and demonstrate the critical mechanical role of collagen crosslinking enzymes.

  20. Constituents from Cistus salvifolius (Cistaceae) activate peroxisome proliferator-activated receptor-γ but not -δ and stimulate glucose uptake by adipocytes.

    PubMed

    Kühn, Claudia; Arapogianni, Niki Eliza; Halabalaki, Maria; Hempel, Jana; Hunger, Nicole; Wober, Jannette; Skaltsounis, Alexios Leandros; Vollmer, Günter

    2011-03-01

    A number of medicinal/culinary herbs have been reported to improve glucose metabolism and to yield hypoglycemic effects in patients with diabetes. Since stimulation of insulin sensitivity appears to be a potential mechanism, peroxisome proliferator-activated receptor (PPAR) γ is a likely target molecule for small lipophilic compounds derived from endogenous metabolism and nutrition. Functionally, PPAR γ integrates the control of energy, lipid, and glucose homeostasis. In addition, PPAR δ activity is involved in energy expenditure. Therefore the aim of this study was to investigate whether PPAR γ and PPAR δ as well as the stimulation of glucose uptake is activated by botanical products. CISTUS SALVIFOLIUS (Cistaceae) has been identified as a candidate botanical in a preliminary screening of extracts from medicinal plants of Greek flora. In a bioguided approach, crude extracts, fractions and in the end purified compounds have been evaluated for PPAR γ and PPAR δ specific activities using cell-based transactivation assays. Glucose uptake was measured by nonradioactive 2-[ N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino]-2-deoxyglucose (2-NBDG) uptake. Concerning PPAR γ several extracts induced reporter gene activity, and clear dose-response patterns (0.1-100 µg/mL) could be established in the case of the cyclohexane and dichloromethane extracts. Isolation of individual compounds from the cyclohexane extract revealed that at least 6 out of 7 compounds isolated were active with TRANS-cinnamic acid showing a clear dose-response pattern. In contrast, they were found to be inactive on PPAR δ. The same compounds, however, were also active in stimulating glucose uptake into 3T3-L1 adipocytes. In summary, the bioguided fractionation of CISTUS SALVIFOLIUS yields PPAR γ stimulating metabolites with differing chemical natures. In conclusion, PPAR γ represents a candidate molecule for the mediation of improvement of glucose metabolism by botanical/nutritional products.

  1. Geochemical evidence of groundwater flow paths and the fate and transport of constituents of concern in the alluvial aquifer at Fort Wingate Depot Activity, New Mexico, 2009

    USGS Publications Warehouse

    Robertson, Andrew J.; Henry, David W.; Langman, Jeffery B.

    2013-01-01

    As part of an environmental investigation at Fort Wingate Depot Activity, New Mexico, the U.S. Geological Survey, in cooperation with the U.S. Army Corps of Engineers, interpreted aqueous geochemical concentrations to better understand the groundwater flow paths and the fate and transport of constituents of concern in the alluvial aquifer underlying the study area. The fine-grained nature of the alluvial matrix creates a highly heterogeneous environment, which adds to the difficulty of characterizing the flow of groundwater and the fate of aqueous constituents of concern. The analysis of the groundwater geochemical data collected in October 2009 provides evidence that is used to identify four groundwater flow paths and their extent in the aquifer and indicates the dominant attenuation processes for the constituents of concern. The extent and interaction of groundwater flow paths were delineated by the major ion concentrations and their relations to each other. Four areas of groundwater recharge to the study area were identified based on groundwater elevations, hydrogeologic characteristics, and geochemical and isotopic evidence. One source of recharge enters the study area from the saturated alluvial deposits underlying the South Fork of the Puerco River to the north of the study area. A second source of recharge is shown to originate from a leaky cistern containing production water from the San Andres-Glorieta aquifer. The other two sources of recharge are shown to enter the study area from the south: one from an arroyo valley draining an area to the south and one from hill-front recharge that passes under the reported release of perchlorate and explosive constituents. The spatial extent and interaction of groundwater originating from these various sources along identified flow paths affect the persistence and attenuation of constituents of concern. It was determined that groundwater originating in the area of a former explosives’ wash-out operation and an

  2. Active thermal isolation for temperature responsive sensors

    NASA Technical Reports Server (NTRS)

    Martinson, Scott D. (Inventor); Gray, David L. (Inventor); Carraway, Debra L. (Inventor); Reda, Daniel C. (Inventor)

    1994-01-01

    A temperature responsive sensor is located in the airflow over the specified surface of a body and is maintained at a constant temperature. An active thermal isolator is located between this temperature responsive sensor and the specified surface of the body. The temperature of this isolator is controlled to reduce conductive heat flow from the temperature responsive sensor to the body. This temperature control includes: (1) operating the isolator at the same temperature as the constant temperature of the sensor and (2) establishing a fixed boundary temperature which is either less than or equal to or slightly greater than the sensor constant temperature.

  3. [Constituents relating to anti-oxidative and alpha-glucosidase inhibitory activities in Yacon aerial part extract].

    PubMed

    Terada, Sumio; Ito, Kikuo; Yoshimura, Akira; Noguchi, Naoto; Ishida, Takashi

    2006-08-01

    Hot water extract of the aerial part of Yacon (Smallanthus sonchifolia, Compositae) showed potent free radical-scavenging activity and inhibitory effects on lipid peroxidation in rat brain homogenate. The most potent antioxidative activity focused on the 50% MeOH-eluted fraction on DIAION HP-20 column chromatography. The structure of the major component in the fraction was identified as 2,3,5-tricaffeoylaltraric acid (TCAA) based on spectroscopic evidence. The antioxidative activity of TCAA is superior to that of natural antioxidants such as (+/-)-catechin, alpha-tocopherol, and ellagic acid, and TCAA also showed selective maltase-inhibitory activity (IC(50) 49 microg/ml). As the hypoglycemic activity of Yacon extract was described in a previous report, the present results showing that the aerial part of Yacon has strong antioxidative activity may encourage its potential use as a food supplement to prevent type II diabetes.

  4. Anti-nociceptive, anti-inflammatory and sedative activities of the extracts and chemical constituents of Diospyros lotus L.

    PubMed

    Uddin, Ghias; Rauf, Abdur; Siddiqui, Bina S; Muhammad, Naveed; Khan, Ajmal; Shah, Syed Uzair Ali

    2014-06-15

    Diospyros lotus L. is traditionally used in various diseases including pain and sleep disorders. The pain and inflammation are the common problems, which are treated with various synthetic analgesic drugs, and associated the side effects. The natural products have gained significant importance over synthetic drugs. The importance of phyto-medicine the current study has been designed with the aim to investigate the analgesic and anti-inflammatory effects of Diospyros lotus and bioassay guided isolation from its crude fractions. Seven known compounds; lupeol (1), 7-methyljuglone (2), β-Sitosterol (3), stigmasterol (4) betulinic acid (5), diospyrin (6; DS) and 8-hydroxyisodiospyrin (7; HDS) which were hitherto unreported from D. lotus. The chloroform fraction (CFDL) and isolated compounds DS and HDS were evaluated for anti-nociceptive, sedative and anti-inflammatory effects. The acetic acid induced writing was significantly (p<0.001) protected by CFDL (72.43%), DS (40.87%) and HDS (65.76%) at higher doses which exhibited peripheral and central analgesic effects in acetic acid and hot-plat pain paradigms. Regarding the anti-inflammatory effect the CFDL (77.43%), DS (80.54%) and HDS (75.87%) protected the carrageenan paw edema after 3rd h. The central analgesic effect was significantly antagonized with naloxone (0.5 mg/kg), showing opiodergic mechanism of action. The CFDL, DS and HDS were also proved sedative in open field animal models. In acute toxicity study the chloroform fraction [CFDL (50, 100 and 150 mg/kg)], DS (5 and 10 mg/kg) and HDS (5 and 10 mg/kg) were found safe. Our study concluded that CFDL, DS and HDS have marked anti-nociceptive, anti-inflammatory and sedative effect. The anti-nociceptive and anti-inflammatory effects of the roots of D. lotus are partially attributed due to the presence of analgesic constituents like diospyrin (DS), 8-hydroxyisodiospyrin (HDS) and strongly supports the ethno-pharmacological uses of D. lotus as anti-nociceptive, anti

  5. The serine protease motif of Pic mediates a dose-dependent mucolytic activity after binding to sugar constituents of the mucin substrate.

    PubMed

    Gutiérrez-Jiménez, Javier; Arciniega, Ivonne; Navarro-García, Fernando

    2008-08-01

    The pic gene is harbored on the chromosomes of three important pathogens: enteroaggregative Escherichia coli (EAEC), uropathogenic E. coli (UPEC), and Shigella flexneri. Since Pic is secreted into the intestinal lumen during EAEC infection, we sought to identify intestinal-mucosal substrates for Pic. Pic did not damage epithelial cells, cleave fodrin, or degrade host defense proteins embedded in the mucus layer (sIgA, lactoferrin and lysozyme). However, by using a solid-phase assay to evaluate the mucinolytic activity of EAEC Pic, we documented a specific, dose-dependent mucinolytic activity. A serine protease inhibitor and an enzymatically inactive variant of Pic were used to show that the Pic serine protease motif is required for mucinolytic activity. Pic binds mucin, and this binding was blocked in competition assays using monosaccharide constituents of the oligosaccharide side chains of mucin. Moreover, Pic mucinolytic activity decreased when sialic acid was removed from mucin. Thus, Pic is a mucinase with lectin-like activity that can be related to its reported hemagglutinin activity. Our results suggest that EAEC may secrete Pic into the intestinal lumen as a strategy for penetrating the gel-like mucus layer during EAEC colonization.

  6. An Activation Threshold Model for Response Inhibition

    PubMed Central

    MacDonald, Hayley J.; McMorland, Angus J. C.; Stinear, Cathy M.; Coxon, James P.; Byblow, Winston D.

    2017-01-01

    Reactive response inhibition (RI) is the cancellation of a prepared response when it is no longer appropriate. Selectivity of RI can be examined by cueing the cancellation of one component of a prepared multi-component response. This substantially delays execution of other components. There is debate regarding whether this response delay is due to a selective neural mechanism. Here we propose a computational activation threshold model (ATM) and test it against a classical “horse-race” model using behavioural and neurophysiological data from partial RI experiments. The models comprise both facilitatory and inhibitory processes that compete upstream of motor output regions. Summary statistics (means and standard deviations) of predicted muscular and neurophysiological data were fit in both models to equivalent experimental measures by minimizing a Pearson Chi-square statistic. The ATM best captured behavioural and neurophysiological dynamics of partial RI. The ATM demonstrated that the observed modulation of corticomotor excitability during partial RI can be explained by nonselective inhibition of the prepared response. The inhibition raised the activation threshold to a level that could not be reached by the original response. This was necessarily followed by an additional phase of facilitation representing a secondary activation process in order to reach the new inhibition threshold and initiate the executed component of the response. The ATM offers a mechanistic description of the neural events underlying RI, in which partial movement cancellation results from a nonselective inhibitory event followed by subsequent initiation of a new response. The ATM provides a framework for considering and exploring the neuroanatomical constraints that underlie RI. PMID:28085907

  7. Effect of Zn2+, Fe3+ and Cr3+ addition to hydroxyapatite for its application as an active constituent of sunscreens

    NASA Astrophysics Data System (ADS)

    de Araujo, T. S.; de Souza, S. O.; de Sousa, E. M. B.

    2010-11-01

    Biocompatible phosphate materials are used in different applications like bone and dental implants, drug delivery systems and others, but could also be applied in inorganic sunscreens. Using sunscreens is extremely necessary, because long time exposure to sun can cause skin cancer. In this work chemical precipitation method has been used to produce hydroxyapatite. Cr3+, Zn2+ and Fe3+ doped samples were characterized using powder X-Ray Diffraction (XRD) and Optical Absorption techniques. X-ray diffraction measurements confirmed the materials were in the expected crystalline structures. The crystallite size as measured from the X-ray pattern was 23-27 nm (±1). The absorption spectra in the ultraviolet and visible ranges indicate that appropriately doped and sized hydroxyapatite particles may have potential applications as active constituents of sunscreens.

  8. Study on prevention of two-stage skin carcinogenesis by Hibiscus rosa sinensis extract and the role of its chemical constituent, gentisic acid, in the inhibition of tumour promotion response and oxidative stress in mice.

    PubMed

    Sharma, S; Khan, N; Sultana, S

    2004-02-01

    We designed the present study to investigate the role of gentisic acid in the chemopreventive activity of Hibiscus rosa sinensis extract on 7,12-dimethyl benz(a)anthracene (DMBA)/croton oil-mediated carcinogenesis in mouse skin via 12-O-tetradecanoyl phorbol-13-acetate (TPA)-induced tumour promotion response and oxidative stress. Single topical application of DMBA followed by twice weekly applications of croton oil after one week for 20 weeks resulted in 100% incidence of tumours in animals in 15 weeks. However, application of H. rosa sinensis extract 30 minutes prior to the application of croton oil twice weekly for 20 weeks caused significant reduction in the number of tumours per mouse and the percentage of tumour-bearing mice. Also, the latency period for the appearance of the first tumour was delayed on H. rosa sinensis pretreatment. A single topical application of TPA caused significant depletion in reduced glutathione (GSH) content, activities of its metabolizing and antioxidant enzymes, while malondialdehyde (MDA) formation, H2O2 content, ornithine decarboxylase (ODC) activity and DNA synthesis were significantly increased. Interestingly, pretreatment of H. rosa sinensis extract (3.5 mg and 7 mg/kg body weight) and gentisic acid (2.0 microg and 4.0 microg/0.2 ml acetone per animal) restored the levels of GSH, and its metabolizing and antioxidant enzymes (P<0.05). There was also a statistically significant reduction in MDA formation and H2O2 content (P<0.05) at both doses. Although inhibition of ODC activity by gentisic acid was not dose-dependent, thymidine incorporation in DNA (P<0.05) was dose-dependently recovered by the plant extract and its chemical constituent. We therefore propose that gentisic acid has a role in the modulatory activity of H. rosa sinensis extract.

  9. Biological Activities of Toninia candida and Usnea barbata Together with Their Norstictic Acid and Usnic Acid Constituents

    PubMed Central

    Ranković, Branislav; Kosanić, Marijana; Stanojković, Tatjana; Vasiljević, Perica; Manojlović, Nedeljko

    2012-01-01

    The aim of this study was to investigate the chemical composition of acetone extracts of the lichens Toninia candida and Usnea barbata and in vitro antioxidant, antimicrobial, and anticancer activities of these extracts together with some of their major metabolites. The chemical composition of T. candida and U. barbata extracts was determined using HPLC-UV analysis. The major phenolic compounds in these extracts were norstictic acid (T. candida) and usnic acid (U. barbata). Antioxidant activity was evaluated by free radical scavenging, superoxide anion radical scavenging, reducing power and determination of total phenolic compounds. Results of the study proved that norstictic acid had the largest antioxidant activity. The total content of phenols in the extracts was determined as the pyrocatechol equivalent. The antimicrobial activity was estimated by determination of the minimal inhibitory concentration using the broth microdilution method. The most active was usnic acid with minimum inhibitory concentration values ranging from 0.0008 to 0.5 mg/mL. Anticancer activity was tested against FemX (human melanoma) and LS174 (human colon carcinoma) cell lines using the microculture tetrazolium test. Usnic acid was found to have the strongest anticancer activity towards both cell lines with IC50 values of 12.72 and 15.66 μg/mL. PMID:23203090

  10. Rigor and Responsiveness in Classroom Activity

    ERIC Educational Resources Information Center

    Thomspon, Jessica; Hagenah, Sara; Kang, Hosun; Stroupe, David; Braaten, Melissa; Colley, Carolyn; Windschitl, Mark

    2016-01-01

    Background/Context: There are few examples from classrooms or the literature that provide a clear vision of teaching that simultaneously promotes rigorous disciplinary activity and is responsive to all students. Maintaining rigorous and equitable classroom discourse is a worthy goal, yet there is no clear consensus of how this actually works in a…

  11. Enhancing Engagement through Active Student Response

    ERIC Educational Resources Information Center

    Tincani, Matt; Twyman, Janet S.

    2016-01-01

    Student engagement is critical to academic success. High-Active Student Response (ASR) teaching techniques are an effective way to improve student engagement and are an important component of evidence-based practice. High-ASR teaching strategies accompany important assumptions: (1) ASR is an alterable variable; (2) teachers can increase ASR in…

  12. Teaching Responsibility through Physical Activity. Second Edition.

    ERIC Educational Resources Information Center

    Hellison, Don

    This book guides teachers in using physical activity to foster personal and social responsibility. Focusing on teaching in school settings, the book features comments from real students to motivate teachers to apply the concept; take-aways that summarize each chapter and help teachers consider their own situations; new chapters on the lesson plan…

  13. Comparative investigation of Umbellularia californica and Laurus nobilis leaf essential oils and identification of constituents active against Aedes aegypti.

    PubMed

    Tabanca, Nurhayat; Avonto, Cristina; Wang, Mei; Parcher, Jon F; Ali, Abbas; Demirci, Betul; Raman, Vijayasankar; Khan, Ikhlas A

    2013-12-18

    Umbellularia californica (California bay laurel) and Laurus nobilis (Mediterranean bay laurel) leaves may be mistaken or used as a substitute on the market due to their morphological similarity. In this study, a comparison of anatomical and chemical features and biological activity of both plants is presented. L. nobilis essential oil biting deterrent and larvicidal activity were negligible. On the other hand, U. californica leaf oil showed biting deterrent activity against Aedes aegypti . The identified active repellents was thymol, along with (-)-umbellulone, 1,8-cineole, and (-)-α-terpineol. U. californica essential oil also demonstrated good larvicidal activity against 1-day-old Ae. aegypti larvae with a LD50 value of 52.6 ppm. Thymol (LD50 = 17.6 ppm), p-cymene, (-)-umbellulone, and methyleugenol were the primary larvicidal in this oil. Umbellulone was found as the principal compound (37%) of U. californica essential oil, but was not present in L. nobilis essential oil. Umbellulone mosquito activity is here reported for the first time.

  14. Isolation of Insecticidal Constituent from Ruta graveolens and Structure-Activity Relationship Studies against Stored-Food Pests (Coleoptera).

    PubMed

    Jeon, Ju-Hyun; Lee, Sang-Guei; Lee, Hoi-Seon

    2015-08-01

    Isolates from essential oil extracted from the flowers and leaves of Ruta graveolens and commercial phenolic analogs were evaluated using fumigant and contact toxicity bioassays against adults of the stored-food pests Sitophilus zeamais, Sitophilus oryzae, and Lasioderma serricorne. The insecticidal activity of these compounds was then compared with that of the synthetic insecticide dichlorvos. To investigate the structure-activity relationships, the activity of 2-isopropyl-5-methylphenol and its analogs was examined against these stored-food pests. Based on the 50% lethal dose, the most toxic compound against S. zeamais was 3-isopropylephenol, followed by 2-isopropylphenol, 4-isopropylphenol, 5-isopropyl-2-methylphenol, 2-isopropyl-5-methylphenol, 3-methylphenol, and 2-methylphenol. Similar results were observed with phenolic compounds against S. oryzae. However, when 2-isopropyl-5-methylphenol isolated from R. graveolens oil and its structurally related analogs were used against L. serricorne, little or no insecticidal activity was found regardless of bioassay. These results indicate that introducing and changing the positions of functional groups in the phenol skeleton have an important effect on insecticidal activity of these compounds against stored-food pests.

  15. Effects of thymoquinone, the major constituent of Nigella sativa seeds, on penicillin-induced epileptiform activity in rats

    PubMed Central

    Beyazcicek, Ersin; Ankarali, Seyit; Beyazcicek, Ozge; Ankarali, Handan; Demir, Serif; Ozmerdivenli, Recep

    2016-01-01

    Objective: To investigate the effects of thymoquinone (TQ) in a penicillin-induced epilepsy model in rats. Methods: This experimental study included 56 adult male Wistar rats. Experiments were performed in the Research Laboratory of the Department of Physiology, Medical School, Duzce University, Duzce, Turkey, between October 2013 and December 2014. Animals were divided into the following 7 groups: sham, control, only thymoquinone, vehicle (Dimethylsulfoxide), and doses of 10, 50, and 100 mg/kg of TQ. After rats were anesthetized, the left part of the skull was removed. A pair of silver/silver chloride electrodes was placed on the somatomotor area, and electrocorticographic recording was started. After 5 minutes basal activity was recorded, and TQ was applied intraperitoneally. At the thirtieth minute after TQ, epileptiform activity was induced by intracortical penicillin. The first spike latency, spike frequency, and the amplitude of epileptiform activity were analyzed statistically. Results: The different doses of TQ significantly increased the latency time to onset of first spike wave, and decreased the frequency, and amplitude of epileptiform activity in the first 20 minutes compared with the control group. Conclusion: Thymoquinone shows potential as an antiepileptic drug resulting from its effects of prolonged latency time, and reduced spike wave frequency and amplitude of epileptiform activity. PMID:27094523

  16. Thyme (Thymus vulgaris L.) leaves and its constituents increase the activities of xenobiotic-metabolizing enzymes in mouse liver.

    PubMed

    Sasaki, Keiko; Wada, Keiji; Tanaka, Yoshiko; Yoshimura, Teruki; Matuoka, Koozi; Anno, Takahiko

    2005-01-01

    The effects of thyme (Thymus vulgaris L.) leaves and its phenolic compounds, thymol and carvacrol, on the activities of xenobiotic-metabolizing enzymes, i.e., phase I enzymes such as 7-ethoxycoumarin O-deethylase (ECOD) and phase II enzymes such as glutathione S-transferase (GST) and quinone reductase (QR), were investigated. Mice were fed with a diet containing thyme (0.5% or 2.0%) or treated orally with thymol (50-200 mg/kg) or carvacrol (50-200 mg/kg) once a day for 7 successive days, and then the enzyme activities in the livers were analyzed. Dietary administration of 2% thyme caused slightly but significantly higher ECOD, GST, and QR activities by 1.1-1.4-fold. Thymol (200 mg/kg) treatment resulted in significantly higher ECOD, GST, and QR activities by 1.3-1.9-fold, and carvacrol (200 mg/kg) treatment caused significantly higher ECOD, GST, and QR activities by 1.3-1.7-fold. Thymol-treated animals had significantly higher protein levels of GST alpha and GST micro, and carvacrol-treated animals had significantly higher levels of GST micro. These results imply that thyme contains bifunctional inducers (i.e., substances capable of inducing both phase I and phase II enzymes) and that thymol and carvacrol may account for the effects of thyme.

  17. Seasonal variations of the phenolic constituents in bilberry (Vaccinium myrtillus L.) leaves, stems and fruits, and their antioxidant activity.

    PubMed

    Bujor, Oana-Crina; Le Bourvellec, Carine; Volf, Irina; Popa, Valentin I; Dufour, Claire

    2016-12-15

    The seasonal variations of the content and diversity of phenolic compounds, as well as the antioxidant activity of leaves, stems and fruits of bilberry collected in May, July and September, were evaluated for two consecutive years. UPLC/MS(n) analyses showed the predominance of anthocyanins in fruits, caffeic acid derivatives in leaves whereas flavanol oligomers represented more than half of the phenolic compounds in stems. Thioacidolysis revealed degrees of polymerization between 2 and 4 and (-)-epicatechin as the main flavanol unit. The sum of the phenolic compounds by UPLC was highly correlated with the total polyphenol content and the antioxidant activity in the DPPH test for all the extracts except for May leaves. The latter were relatively rich in p-coumaric acid derivatives. Seasonal effects were more marked for leaves, which exhibited higher antioxidant activities and phenolic contents in July and September when these parameters were at their highest in July for stems.

  18. Heartwood extract of Rhus verniciflua Stokes and its active constituent fisetin attenuate vasoconstriction through calcium-dependent mechanism in rat aorta.

    PubMed

    Park, Jung-Min; Lee, Jun-Hyeong; Na, Chun-Soo; Lee, Dongho; Lee, Jin-Yong; Satoh, Masahiko; Lee, Moo-Yeol

    2016-01-01

    Rhus verniciflua Stokes (RVS) exert cardiovascular protective activity by promoting blood circulation, but its active ingredients and underlying mechanism have yet to be identified. This study investigated the vascular effects of RVS, focusing on vasoconstriction and smooth muscle Ca(2+) signaling. RVS heartwood extract attenuated contraction of aortic rings induced by the vasoconstrictors serotonin and phenylephrine, and inhibited the Ca(2+) signaling evoked by serotonin in vascular smooth muscle cells. Subsequent activity-guided fractionation identified fisetin as an active constituent exerting a Ca(2+) inhibitory effect. Fisetin could inhibit major Ca(2+) mobilization pathways including extracellular Ca(2+) influx mediated by the L-type voltage-gated Ca(2+) channel, Ca(2+) release from the intracellular store and store-operated Ca(2+) entry. In accordance with Ca(2+) inhibitory effect, fisetin attenuated vasoconstriction by serotonin and phenylephrine. These results suggest that the anticontractile effect, which is presumably mediated by inhibition of Ca(2+) signaling, may contribute to the improvement of blood circulation by RVS.

  19. Insecticidal and acetylcholine esterase inhibition activity of Asteraceae plant essential oils and their constituents against adults of the German cockroach (Blattella germanica).

    PubMed

    Yeom, Hwa-Jeong; Jung, Chan-Sik; Kang, Jaesoon; Kim, Junheon; Lee, Jae-Hyeon; Kim, Dong-Soo; Kim, Hyun-Seok; Park, Pil-Sun; Kang, Kyu-Suk; Park, Il-Kwon

    2015-03-04

    The fumigant and contact toxicities of 16 Asteraceae plant essential oils and their constituents against adult male and female Blattella germanica were examined. In a fumigant toxicity test, tarragon oil exhibited 100% and 90% fumigant toxicity against adult male German cockroaches at 5 and 2.5 mg/filter paper, respectively. Fumigant toxicities of Artemisia arborescens and santolina oils against adult male German cockroaches were 100% at 20 mg/filter paper, but were reduced to 60% and 22.5% at 10 mg/filter paper, respectively. In contact toxicity tests, tarragon and santolina oils showed potent insecticidal activity against adult male German cockroaches. Components of active oils were analyzed using gas chromatography, gas chromatography-mass spectrometry, or nuclear magnetic resonance spectrometer. Among the identified compounds from active essential oils, estragole demonstrated potent fumigant and contact toxicity against adult German cockroaches. β-Phellandrene exhibited inhibition of male and female German cockroach acetylcholinesterase activity with IC50 values of 0.30 and 0.28 mg/mL, respectively.

  20. Interleukin-19: A Constituent of the Regulome That Controls Antigen Presenting Cells in the Lungs and Airway Responses to Microbial Products

    PubMed Central

    Hoffman, Carol; Park, Sung-Hyun; Daley, Eleen; Emson, Claire; Louten, Jennifer; Sisco, Maureen; de Waal Malefyt, Rene; Grunig, Gabriele

    2011-01-01

    Background Interleukin (IL)-19 has been reported to enhance chronic inflammatory diseases such as asthma but the in vivo mechanism is incompletely understood. Because IL-19 is produced by and regulates cells of the monocyte lineage, our studies focused on in vivo responses of CD11c positive (CD11c+) alveolar macrophages and lung dendritic cells. Methodology/Principal Findings IL-19-deficient (IL-19-/-) mice were studied at baseline (naïve) and following intranasal challenge with microbial products, or recombinant cytokines. Naïve IL-19-/- mixed background mice had a decreased percentage of CD11c+ cells in the bronchoalveolar-lavage (BAL) due to the deficiency in IL-19 and a trait inherited from the 129-mouse strain. BAL CD11c+ cells from fully backcrossed IL-19-/- BALB/c or C57BL/6 mice expressed significantly less Major Histocompatibility Complex class II (MHCII) in response to intranasal administration of lipopolysaccharide, Aspergillus antigen, or IL-13, a pro-allergic cytokine. Neurogenic-locus-notch-homolog-protein-2 (Notch2) expression by lung monocytes, the precursors of BAL CD11c+ cells, was dysregulated: extracellular Notch2 was significantly decreased, transmembrane/intracellular Notch2 was significantly increased in IL-19-/- mice relative to wild type. Instillation of recombinant IL-19 increased extracellular Notch2 expression and dendritic cells cultured from bone marrow cells in the presence of IL-19 showed upregulated extracellular Notch2. The CD205 positive subset among the CD11c+ cells was 3-5-fold decreased in the airways and lungs of naïve IL-19-/- mice relative to wild type. Airway inflammation and histological changes in the lungs were ameliorated in IL-19-/- mice challenged with Aspergillus antigen that induces T lymphocyte-dependent allergic inflammation but not in IL-19-/- mice challenged with lipopolysaccharide or IL-13. Conclusions/Significance Because MHCII is the molecular platform that displays peptides to T lymphocytes and Notch2

  1. Effect of Scrophularia striata and Ferulago angulata, as alternatives to virginiamycin, on growth performance, intestinal microbial population, immune response, and blood constituents of broiler chickens.

    PubMed

    Rostami, Farhad; Ghasemi, Hossein A; Taherpour, Kamran

    2015-09-01

    An experiment was conducted to investigate the comparative effect of Scrophularia striata, Ferulago angulata, and virginiamycin (VM) on performance, intestinal microbial population, immune response, and blood constituents of broilers. A total of 300 Ross 308 male broiler chickens were randomly assigned to 5 treatments, with 5 replicates/treatment (10 chickens/pen). Birds were fed either a corn-soybean meal basal diet (control) or the basal diet supplemented with 200 mg/kg VM; 4 g/kg S. striata (SS1); 8 g/kg S. striata (SS2); 4 g/kg F. angulata (FA1); or 8 g/kg F. angulata (FA2). After 6 wk, the BW, ADG, and feed-to-gain ratio (F:G) of the VM, SS1, and FA1 groups were better (P<0.01) compared with the control group. At 42 d, cecal lactobacillus counts were higher (P=0.032) in SS2 and FA2 groups compared with the control and VM groups. In addition, broilers fed any of the diets exhibited lower coliform counts (P<0.05) in the ileum and ceca than those fed the control diet. Total and IgG antibody titers against SRBC for secondary responses, relative spleen weight, and lymphocyte counts were higher (P<0.05) in birds fed the SS2 or FA2 diet compared with the control group. Moreover, feeding the SS2 or FA2 diet decreased (P<0.05) the blood heterophil/lymphocyte ratio and plasma triglyceride level, whereas only the SS2 diet increased (P=0.037) the white blood cell counts compared with the control diet. All diets, except for the VM diet, decreased (P=0.009) the plasma cholesterol level compared to the control treatment. The plasma high-density lipoprotein cholesterol level was also increased (P=0.042) in the SS2 and FA2 groups. In conclusion, dietary S. striata or F. angulata at a level of 4 g/kg diet enhanced growth performance, which was comparable to that of VM used as an antibiotic growth promoter. Furthermore, a high dose of both herbs (8 g/kg diet) could beneficially affect the intestinal health and immune status of broilers.

  2. Anti-inflammatory, anti-tumor-promoting, and cytotoxic activities of constituents of marigold (Calendula officinalis) flowers.

    PubMed

    Ukiya, Motohiko; Akihisa, Toshihiro; Yasukawa, Ken; Tokuda, Harukuni; Suzuki, Takashi; Kimura, Yumiko

    2006-12-01

    Ten oleanane-type triterpene glycosides, 1-10, including four new compounds, calendulaglycoside A 6'-O-methyl ester (2), calendulaglycoside A 6'-O-n-butyl ester (3), calendulaglycoside B 6'-O-n-butyl ester (5), and calendulaglycoside C 6'-O-n-butyl ester (8), along with five known flavonol glycosides, 11-15, were isolated from the flowers of marigold (Calendula officinalis). Upon evaluation of compounds 1-9 for inhibitory activity against 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation (1 microg/ear) in mice, all of the compounds, except for 1, exhibited marked anti-inflammatory activity, with ID50 values of 0.05-0.20 mg per ear. In addition, when 1-15 were evaluated against the Epstein-Barr virus early antigen (EBV-EA) activation induced by TPA, compounds 1-10 exhibited moderate inhibitory effects (IC50 values of 471-487 mol ratio/32 pmol TPA). Furthermore, upon evaluation of the cytotoxic activity against human cancer cell lines in vitro in the NCI Developmental Therapeutics Program, two triterpene glycosides, 9 and 10, exhibited their most potent cytotoxic effects against colon cancer, leukemia, and melanoma cells.

  3. Studies on the chemical constituents and antioxidant activities of extracts from the roots of Smilax lanceaefolia Roxb.

    PubMed

    Laitonjam, Warjeet S; Kongbrailatpam, Brajeshwari D

    2010-07-01

    A flavonol glycoside (1) and a steroidal saponin (2), along with beta-sitosterol and beta-sitosterol-D-glucoside, were isolated from the roots of Smilax lanceaefolia Roxb. Mineral contents were determined using the atomic absorption spectrophotometer and the total antioxidant activity was determined using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging method.

  4. HPLC-based activity profiling of anti-hepatocellular carcinoma constituents from the Tibetan medicine, Caragana tibetica.

    PubMed

    Song, Ping; Wang, Qiang; Lv, Jing-Nan; Xu, Chan; Lin, Qin-Xiong; Ma, Xin-Hua; Huang, Mi; Yang, Xin-Zhou

    2015-06-01

    During the screening of a traditional Chinese folk herb library against HepG2 and Hep3B cell lines, the EtOAc extract from the Tibetan medicine, Caragana tibetica (CT-EtOAc) exhibited potential anti-hepatocellular carcinoma (anti-HCC) activity. HPLC-based activity profiling was performed for targeted identification of anti-HCC activity from CT-EtOAc by MS-directed purification method. CT-EtOAc was separated by time-based fractionation for further anti-HCC bioassay by a semipreparative HPLC column (150 mm × 10 mm i.d., 5 μm) with a single injection of 5 mg. Bioassay-guided and ESIMS-directed large scale purification was performed with a single injection of 400 mg of CT-EtOAc by peak-based fractionation. A 1.4-mm heavy wall micro NMR tube with z-gradient was used to measure one and two dimensional NMR spectra for the minor or trace amounts of components of the extract. Two active compounds could be elucidated as naringenin chalcone (CT-1) and 3-hydroxy-8, 9-dimethoxypterocarpan (CT-2) relevant to anti-HCC effects for the EtOAc extract of C. tibetica rapidly and unambiguously by this protocol.

  5. In vitro evaluation of schistosomicidal activity of essential oil of Mentha x villosa and some of its chemical constituents in adult worms of Schistosoma mansoni.

    PubMed

    Matos-Rocha, Thiago José; dos Santos Cavalcanti, Marília Gabriela; Barbosa-Filho, José Maria; Lúcio, Ana Silvia Suassuna Carneiro; Veras, Dyana Leal; Feitosa, Ana Paula Sampaio; de Siqueira Júnior, José Pinto; de Almeida, Reinaldo Nóbrega; Marques, Márcia Ortiz Mayo; Alves, Luiz Carlos; Brayner, Fábio André

    2013-09-01

    This study aimed to determine the composition of the essential oil of Mentha x villosa and to evaluate its biological effects in vitro on adult worms of S. mansoni. Rotundifolone (70.96 %), limonene (8.75 %), trans-caryophyllene (1.46 %), and β-pinene (0.81 %) were shown to be the major constituents of this oil. Adult worms of S. mansoni were incubated with different concentrations of the essential oil (1, 10, 100, 250, 500, and 1000 µg/mL) and of its constituents rotundifolone (0.7, 3.54, 7.09, 70.96, 177.4, 354.8, and 700.96 µg/mL), limonene (43.75 µg/mL), trans-caryophyllene (7.3 µg/mL), and β-pinene (4.03 µg/mL). No schistosomicidal activity was identified at the trans-caryophyllene and β-pinene concentrations studied. However, use of the essential oil (10 µg/mL), rotundifolone (7.09 µg/mL), and limonene (43.75 µg/mL) resulted in decreased worm motility continuing until 96 hours of observation. At higher concentrations (100 and 70.96 µg/mL, respectively), both the essential oil and rotundifolone caused mortality among adult worms of S. mansoni. The positive control praziquantel caused the death of all parasites after 24 h of evaluation. The results from this study suggest that the essential oil of Mentha x villosa presents schistosomicidal efficacy.

  6. Chemical constituents from the aerial parts of Aster koraiensis with protein glycation and aldose reductase inhibitory activities.

    PubMed

    Lee, Jun; Lee, Yun Mi; Lee, Byong Won; Kim, Joo-Hwan; Kim, Jin Sook

    2012-02-24

    Two new eudesmane-type sesquiterpene glucosides, 9β-O-(E-p-hydroxycinnamoyl)-1β,6β-dihydroxy-trans-eudesm-3-en-6-O-β-D-glucopyranoside (1) and 9α-O-(E-p-hydroxycinnamoyl)-1α,6α-11-trihydroxy-trans-eudesm-3-en-6-O-β-D-glucopyranoside (2), were isolated by the activity-guidedfractionation of an EtOAc-soluble fraction from the aerial parts of Aster koraiensis. A new dihydrobenzofuran glucoside, (2R,3S)-6-acetyl-2-[1-O-(β-D-glucopyranosyl)-2-propenyl]-5-hydroxy-3-methoxy-2,3-dihydrobenzofuran (3), was also isolated, in addition to 15 known compounds. The structures of 1-3 were determined by spectroscopic data interpretation. All of the isolates were evaluated for in vitro inhibitory activity against the formation of advanced glycation end-products and rat lens aldose reductase.

  7. Chemical constituents with anti-allergic activity from the root of Edulis Superba, a horticultural cultivar of Paeonia lactiflora.

    PubMed

    Shi, Yan-Hong; Zhu, Shu; Tamura, Takayuki; Kadowaki, Makoto; Wang, Zhengtao; Yoshimatsu, Kayo; Komatsu, Katsuko

    2016-04-01

    The methanolic extract and its subfractions from the dried root of Edulis Superba, a horticultural cultivar of Paeonia lactiflora Pallas, showed potent anti-allergic effect as inhibition of immunoglobulin E (IgE)-mediated degranulation in rat basophil leukemia (RBL)-2H3 cells. Bioassay-guided fractionation led to the isolation of 26 compounds, including a new norneolignan glycoside, paeonibenzofuran (1), together with 25 known ones (2-26). The chemical structure of the new compound was elucidated on the basis of spectroscopic and chemical evidences. Among the isolated compounds, mudanpioside E (5) with paeoniflorin-type skeleton and quercetin (16) showed potent inhibitory activity against a degranulation marker, β-hexosaminidase release with IC50 values of 40.34 and 25.05 μM, respectively. A primary structure-activity relationship of these components was discussed.

  8. In vitro cytotoxic activity of extracts and isolated constituents of Salvia leriifolia Benth. against a panel of human cancer cell lines.

    PubMed

    Tundis, Rosa; Loizzo, Monica R; Menichini, Federica; Bonesi, Marco; Colica, Carmela; Menichini, Francesco

    2011-06-01

    In the course of recent efforts to identify new potential antiproliferative active principles, Salvia leriifolia extracts and isolated constituents were evaluated for their cytotoxic activity against a panel of human cancer cell lines, including renal adenocarcinoma (ACHN), amelanotic melanoma (C32), colorectal adenocarcinoma (Caco-2), lung large cell carcinoma (COR-L23), malignant melanoma (A375), lung carcinoma (A549), and hepatocellular carcinoma (Huh-7D12) cells. The hexane and CH(2) Cl(2) extracts showed the strongest cytotoxic activity against the C32 cell line with IC(50) values of 11.2 and 13.6 μg/ml, respectively, and the AcOEt extract was the most active extract against the COR-L23 cell line (IC(50) of 20.9 μg/ml). Buchariol, a sesquiterpene obtained by biofractionation of the CH(2) Cl(2) extract, exhibited a higher activity than the positive control vinblastine against the C32 and A549 cell lines (IC(50) values of 2.1 and 12.6 μM, resp.). Interesting results were also obtained for naringenin, a flavonoid isolated from the AcOEt extract, which exhibited a strong cytotoxic activity against the C32, LNCaP, and COR-L23 cell lines (IC(50) values of 2.2, 7.7, and 33.4 μM, resp.), compared to vinblastine (IC(50) values of 3.3, 32.2, 50.0 μM, resp.). None of the tested compounds affected the proliferation of skin fibroblasts (142BR), suggesting a selective activity against tumor cells.

  9. GABA-A Receptor Modulation and Anticonvulsant, Anxiolytic, and Antidepressant Activities of Constituents from Artemisia indica Linn

    PubMed Central

    Khan, Imran; Karim, Nasiara; Ahmad, Waqar; Abdelhalim, Abeer; Chebib, Mary

    2016-01-01

    Artemisia indica, also known as “Mugwort,” has been widely used in traditional medicines. However, few studies have investigated the effects of nonvolatile components of Artemisia indica on central nervous system's function. Fractionation of Artemisia indica led to the isolation of carnosol, ursolic acid, and oleanolic acid which were evaluated for their effects on GABA-A receptors in electrophysiological studies in Xenopus oocytes and were subsequently investigated in mouse models of acute toxicity, convulsions (pentylenetetrazole induced seizures), depression (tail suspension and forced swim tests), and anxiety (elevated plus maze and light/dark box paradigms). Carnosol, ursolic acid, and oleanolic acid were found to be positive modulators of α1β2γ2L GABA-A receptors and the modulation was antagonized by flumazenil. Carnosol, ursolic acid, and oleanolic acid were found to be devoid of any signs of acute toxicity (50–200 mg/kg) but elicited anticonvulsant, antidepressant, and anxiolytic activities. Thus carnosol, ursolic acid, and oleanolic acid demonstrated CNS activity in mouse models of anticonvulsant, antidepressant, and anxiolysis. The anxiolytic activity of all three compounds was ameliorated by flumazenil suggesting a mode of action via the benzodiazepine binding site of GABA-A receptors. PMID:27143980

  10. Larvicidal and acetylcholinesterase inhibitory activities of apiaceae plant essential oils and their constituents against aedes albopictus and formulation development.

    PubMed

    Seo, Seon-Mi; Jung, Chan-Sik; Kang, Jaesoon; Lee, Hyo-Rim; Kim, Sung-Woong; Hyun, Jinho; Park, Il-Kwon

    2015-11-18

    This study evaluated the larvicidal activity of 12 Apiaceae plant essential oils and their components against the Asian tiger mosquito, Aedes albopictus, and the inhibition of acetylcholine esterase with their components. Of the 12 plant essential oils tested, ajowan (Trachyspermum ammi), caraway seed (Carum carvi), carrot seed (Daucus carota), celery (Apium graveolens), cumin (Cuminum cyminum), dill (Anethum graveolens), and parsley (Petroselinum sativum) resulted in >90% larval mortality when used at 0.1 mg/mL. Of the compounds identified, α-phellandrene, α-terpinene, p-cymene, (-)-limonene, (+)-limonene, γ-terpinene, cuminaldehyde, neral, (S)-+-carvone, trans-anethole, thymol, carvacrol, myristicin, apiol, and carotol resulted in >80% larval mortality when used at 0.1 mg/mL. Two days after treatment, 24.69, 3.64, and 12.43% of the original amounts of the celery, cumin, and parsley oils, respectively, remained in the water. Less than 50% of the original amounts of α-phellandrene, 1,8-cineole, terpinen-4-ol, cuminaldehyde, and trans-antheole were detected in the water at 2 days after treatment. Carvacrol, α-pinene, and β-pinene inhibited the activity of Ae. albopictus acetylcholinesterase with IC50 values of 0.057, 0.062, and 0.190 mg/mL, respectively. A spherical microemulsion of parsley essential oil-loaded poly(vinyl alcohol) (PVA) was prepared, and the larvicidal activity of this formulation was shown to be similar to that of parsley oil.

  11. Constituents and Pharmacological Activities of Myrcia (Myrtaceae): A Review of an Aromatic and Medicinal Group of Plants

    PubMed Central

    Cascaes, Márcia Moraes; Guilhon, Giselle Maria Skelding Pinheiro; Andrade, Eloisa Helena de Aguiar; Zoghbi, Maria das Graças Bichara; Santos, Lourivaldo da Silva

    2015-01-01

    Myrcia is one of the largest genera of the economically important family Myrtaceae. Some of the species are used in folk medicine, such as a group known as “pedra-hume-caá” or “pedra-ume-caá” or “insulina vegetal” (insulin plant) that it is used for the treatment of diabetes. The species are an important source of essential oils, and most of the chemical studies on Myrcia describe the chemical composition of the essential oils, in which mono- and sesquiterpenes are predominant. The non-volatile compounds isolated from Myrcia are usually flavonoids, tannins, acetophenone derivatives and triterpenes. Anti-inflammatory, antinociceptive, antioxidant, antimicrobial activities have been described to Myrcia essential oils, while hypoglycemic, anti-hemorrhagic and antioxidant activities were attributed to the extracts. Flavonoid glucosides and acetophenone derivatives showed aldose reductase and α-glucosidase inhibition, and could explain the traditional use of Myrcia species to treat diabetes. Antimicrobial and anti-inflammatory are some of the activities observed for other isolated compounds from Myrcia. PMID:26473832

  12. Extracts and constituents of Rubus chingii with 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity.

    PubMed

    Ding, Hsiou-Yu

    2011-01-01

    The 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity of the fruits of Rubus chingii was studied in vitro. Ethanolic extract, ethyl acetate and n-butanol fractions from dried R. chingii fruits revealed strong DPPH free radical scavenging activity with IC(50) values of 17.9, 3.4 and 4.0 μg/mL, respectively. The ethyl acetate and n-butanol fractions were further purified by a combination of silica gel chromatography, Lobar RP-8 chromatography, and high-pressure liquid chromatography (HPLC). Nine compounds were isolated, where methyl (3-hydroxy-2-oxo-2,3-dihydroindol-3-yl)-acetate (2), vanillic acid (5), kaempferol (7), and tiliroside (9) showed stronger DPPH free radical scavenging activity than that of ascorbic acid (131.8 μM) with IC(50) values of 45.2, 34.9, 78.5, and 13.7 μM, respectively. In addition, rubusine (1) is a new compound discovered in the present study and methyl (3-hydroxy-2-oxo-2,3-dihydroindol-3-yl)-acetate (2), methyl dioxindole-3-acetate (3), and 2-oxo-1,2-dihydroquinoline-4-carboxylic acid (4) were isolated from the fruits for the first time.

  13. Estrogen-like activity of licorice root constituents: glabridin and glabrene, in vascular tissues in vitro and in vivo.

    PubMed

    Somjen, Dalia; Knoll, Esther; Vaya, Jacob; Stern, Naftali; Tamir, Snait

    2004-07-01

    Post-menopausal women have higher incidence of heart diseases compared to pre-menopausal women, suggesting a protective role for estrogen. The recently Women's Health Initiative (WHI) randomized controlled trial concluded that the overall heart risk exceeded benefits from use of combined estrogen and progestin as hormone replacement therapy for an average of five years among healthy postmenopausal US women. Therefore, there is an urgent need for new agents with tissue-selective activity with no deleterious effects. In the present study, we tested the effects on vascular tissues in vitro and in vivo of two natural compounds derived from licorice root: glabridin, the major isoflavan, and glabrene, an isoflavene, both demonstrated estrogen-like activities. Similar to estradiol-17beta (E2), glabridin (gla) stimulated DNA synthesis in human endothelial cells (ECV-304; E304) and had a bi-phasic effect on proliferation of human vascular smooth muscle cells (VSMC). Raloxifene inhibited gla as well as E2 activities. In animal studies, both intact females or after ovariectomy, gla similar to E2 stimulated the specific activity of creatine kinase (CK) in aorta (Ao) and in left ventricle of the heart (Lv). Glabrene (glb), on the other hand, had only the stimulatory effect on DNA synthesis in vascular cells, with no inhibition by raloxifene, suggesting a different mechanism of action. To further elucidate the mechanism of action of glb, cells were pre-incubated with glb and then exposed to either E2 or to gla; the DNA stimulation at low doses was unchanged but there was abolishment of the inhibition of VSMC cell proliferation at high doses as well as inhibition of CK stimulation by both E2 and by gla. We conclude that glb behaved differently than E2 or gla, but similarly to raloxifene, being a partial agonist/antagonist of E2. Glabridin, on the other hand, demonstrated only estrogenic activity. Therefore, we suggest the use of glb with or without E2 as a new agent for

  14. Trisomy 21 consistently activates the interferon response.

    PubMed

    Sullivan, Kelly D; Lewis, Hannah C; Hill, Amanda A; Pandey, Ahwan; Jackson, Leisa P; Cabral, Joseph M; Smith, Keith P; Liggett, L Alexander; Gomez, Eliana B; Galbraith, Matthew D; DeGregori, James; Espinosa, Joaquín M

    2016-07-29

    Although it is clear that trisomy 21 causes Down syndrome, the molecular events acting downstream of the trisomy remain ill defined. Using complementary genomics analyses, we identified the interferon pathway as the major signaling cascade consistently activated by trisomy 21 in human cells. Transcriptome analysis revealed that trisomy 21 activates the interferon transcriptional response in fibroblast and lymphoblastoid cell lines, as well as circulating monocytes and T cells. Trisomy 21 cells show increased induction of interferon-stimulated genes and decreased expression of ribosomal proteins and translation factors. An shRNA screen determined that the interferon-activated kinases JAK1 and TYK2 suppress proliferation of trisomy 21 fibroblasts, and this defect is rescued by pharmacological JAK inhibition. Therefore, we propose that interferon activation, likely via increased gene dosage of the four interferon receptors encoded on chromosome 21, contributes to many of the clinical impacts of trisomy 21, and that interferon antagonists could have therapeutic benefits.

  15. Sasa quelpaertensis Nakai extract and its constituent p-coumaric acid inhibit adipogenesis in 3T3-L1 cells through activation of the AMPK pathway.

    PubMed

    Kang, Seung-Woo; Kang, Seong-Il; Shin, Hye-Sun; Yoon, Seon-A; Kim, Jeong-Hwan; Ko, Hee-Chul; Kim, Se-Jae

    2013-09-01

    In this study, we investigated the effects of Sasa quelpaertensis Nakai extract (SQE) and its main constituent, p-coumaric acid, on adipogenesis in 3T3-L1 cells. SQE markedly inhibited adipogenesis by downregulating the expression of CCAAT/enhancer-binding protein α (C/EBPα), peroxisome proliferator-activated receptor γ (PPARγ), sterol regulatory element-binding protein-1c (SREBP-1c), and aP2. It also decreased the expression of fatty acid synthase (FAS) and adiponectin mRNAs in differentiating adipocytes. SQE increased AMP-activated protein kinase (AMPK) and acetyl-CoA carboxylase (ACC) phosphorylation during the early phase of MDI-induced differentiation, suggesting that SQE exerted its anti-adipogenic effect via AMPK activation at an early stage of the differentiation process. p-Coumaric acid suppressed adipogenesis by attenuating the expression of C/EBPα, PPARγ, and SREBP-1c during the late phase of MDI-induced differentiation. In addition, p-coumaric acid increased the phosphorylation of AMPK and ACC, and the expression of carnitine palmitoyl transferase-1 (CPT-1) mRNA, in fully differentiated adipocytes, indicating that it promotes fatty acid β-oxidation via AMPK signaling. Taken together, our data suggest that SQE and p-coumaric acid might have the anti-obesitic effects via AMPK pathway in 3T3-L1 cells.

  16. In vitro anti-acetylcholinesterase activity of an aqueous extract of Unicaria tomentosa and in silico study of its active constituents

    PubMed Central

    Chowdhury, Suman; Shivani; Kumar, Suresh

    2016-01-01

    Depletion of acetylcholine in the central nervous system (CNS) is responsible for memory loss and cognition deficit. Enzyme acetylcholinesterase (AChE) is responsible for destruction of acetylcholine (Ach) in the brain. Many herbal plant extracts have been investigated for their potential use in the treatment of Alzheimer’s disease (AD) by inhibiting AChE and upregulating the levels of Ach. The current study investigated the anti-acetylcholinesterase (AChE) activity of an aqueous extract of Unicaria tomentosa bark which has not been reported so far in the literature. The in vitro study of an aqueous extract of U. tomentosa showed maximum inhibition of 76.2±0.002 % at 0.4mg/ml of final concentration with an IC50 = 0.112 mg/ml. The mechanism of inhibition was elucidated by kinetic study which showed mixed type of inhibition, this might be due to the presence of various phytoconstituents such as oxindole alkaloids present in an aqueous extract. Based on molecular structure of phytoconstituents obtained from U. tomentosa known from the relevant literature, in-silico molecular docking study was performed against AChE protein to validate the results. PMID:28149044

  17. In vitro anti-acetylcholinesterase activity of an aqueous extract of Unicaria tomentosa and in silico study of its active constituents.

    PubMed

    Chowdhury, Suman; Shivani; Kumar, Suresh

    2016-01-01

    Depletion of acetylcholine in the central nervous system (CNS) is responsible for memory loss and cognition deficit. Enzyme acetylcholinesterase (AChE) is responsible for destruction of acetylcholine (Ach) in the brain. Many herbal plant extracts have been investigated for their potential use in the treatment of Alzheimer's disease (AD) by inhibiting AChE and upregulating the levels of Ach. The current study investigated the anti-acetylcholinesterase (AChE) activity of an aqueous extract of Unicaria tomentosa bark which has not been reported so far in the literature. The in vitro study of an aqueous extract of U. tomentosa showed maximum inhibition of 76.2±0.002 % at 0.4mg/ml of final concentration with an IC50 = 0.112 mg/ml. The mechanism of inhibition was elucidated by kinetic study which showed mixed type of inhibition, this might be due to the presence of various phytoconstituents such as oxindole alkaloids present in an aqueous extract. Based on molecular structure of phytoconstituents obtained from U. tomentosa known from the relevant literature, in-silico molecular docking study was performed against AChE protein to validate the results.

  18. Antifungal and cytotoxicity activities of the fresh xylem sap of Hymenaea courbaril L. and its major constituent fisetin

    PubMed Central

    2014-01-01

    Background The great potential of plants as Hymenaea courbaril L (jatoba) has not yet been throughly explored scientifically and therefore it is very important to investigate their pharmacological and toxicological activities to establish their real efficacy and safety. This study investigated the cytotoxicity of xylem sap of Hymenaea courbaril L and its bioactivity against the fungi Cryptococcus neoformans species complex and dermatophytes. Methods The fresh xylem sap of H. courbaril was filtered resulting in an insoluble brown color precipitate and was identified as fisetin. In the filtrate was identified the mixture of fisetinediol, fustin, 3-O-methyl-2,3-trans-fustin and taxifolin, which were evaluated by broth microdilution antifungal susceptibility testing against C. neoformans species complex and dermatophytes. The fresh xylem sap and fisetin were screened for cytotoxicity against the 3T3-A31 cells of Balb/c using neutral red uptake (NRU) assay. Results The fresh xylem sap and the fisetin showed higher in vitro activity than the filtrate. The xylem sap of H. courbaril inhibited the growth of dermatophytes and of C. neoformans with minimal inhibition concentration (MIC) < 256 μg/mL, while the fisetin showed MIC < 128 μg/mL for these fungi. Fisetin showed lower toxicity (IC50 = 158 μg/mL) than the fresh xylem sap (IC50 = 109 μg/mL). Conclusion Naturally occurring fisetin can provide excellent starting points for clinical application and can certainly represent a therapeutic potential against fungal infections, because it showed in vitro antifungal activity and low toxicity on animal cells. PMID:25027026

  19. The hop constituent xanthohumol exhibits hepatoprotective effects and inhibits the activation of hepatic stellate cells at different levels.

    PubMed

    Weiskirchen, Ralf; Mahli, Abdo; Weiskirchen, Sabine; Hellerbrand, Claus

    2015-01-01

    Xanthohumol is the principal prenylated flavonoid of the female inflorescences of the hop plant. In recent years, various beneficial xanthohumol effects including anti-inflammatory, antioxidant, hypoglycemic activities, and anticancer effects have been revealed. This review summarizes present studies indicating that xanthohumol also inhibits several critical pathophysiological steps during the development and course of chronic liver disease, including the activation and pro-fibrogenic genotype of hepatic stellate cells. Also the various mechanism of action and molecular targets of the beneficial xanthohumol effects will be described. Furthermore, the potential use of xanthohumol or a xanthohumol-enriched hop extract as therapeutic agent to combat the progression of chronic liver disease will be discussed. It is notable that in addition to its hepatoprotective effects, xanthohumol also holds promise as a therapeutic agent for treating obesity, dysregulation of glucose metabolism and other components of the metabolic syndrome including hepatic steatosis. Thus, therapeutic xanthohumol application appears as a promising strategy, particularly in obese patients, to inhibit the development as well as the progression of non-alcoholic fatty liver disease.

  20. Acaricidal activity of Lippia gracilis essential oil and its major constituents on the tick Rhipicephalus (Boophilus) microplus.

    PubMed

    Cruz, Elizangela Mércia de Oliveira; Costa, Livio Martins; Pinto, Jessika Andreza Oliveira; Santos, Darlisson de Alexandria; de Araujo, Sandra Alves; Arrigoni-Blank, Maria de Fátima; Bacci, Leandro; Alves, Péricles Barreto; Cavalcanti, Sócrates Cabral de Holanda; Blank, Arie Fitzgerald

    2013-07-01

    The present study aimed to evaluate the activity of Lippia gracilis Schauer essential oil obtained from different L. gracilis genotypes and their major components, carvacrol and thymol against Rhipicephalus (Boophilus) microplus (cattle tick) larvae and engorged females. The larval test was performed parallel to the adult immersion test for engorged females for four L. gracilis genotypes. Similar tests were further performed for their major compounds carvacrol and thymol. Carvacrol (LC50 of 0.22 and 4.46 mg/mL, to larvae and engorged females, respectively) was more efficient than thymol (LC50 of 3.86 and 5.50 mg/mL, to larvae and engorged females, respectively). The lethal concentrations obtained for the isolated essential oil from genotypes LGRA-201 against larvae (1.31 mg/mL) and LGRA-106 against engorged females (4.66 mg/mL) confirmed the acaricidal activity of L. gracilis essential oil and its effectiveness in controlling the southern cattle tick.

  1. The hop constituent xanthohumol exhibits hepatoprotective effects and inhibits the activation of hepatic stellate cells at different levels

    PubMed Central

    Weiskirchen, Ralf; Mahli, Abdo; Weiskirchen, Sabine; Hellerbrand, Claus

    2015-01-01

    Xanthohumol is the principal prenylated flavonoid of the female inflorescences of the hop plant. In recent years, various beneficial xanthohumol effects including anti-inflammatory, antioxidant, hypoglycemic activities, and anticancer effects have been revealed. This review summarizes present studies indicating that xanthohumol also inhibits several critical pathophysiological steps during the development and course of chronic liver disease, including the activation and pro-fibrogenic genotype of hepatic stellate cells. Also the various mechanism of action and molecular targets of the beneficial xanthohumol effects will be described. Furthermore, the potential use of xanthohumol or a xanthohumol-enriched hop extract as therapeutic agent to combat the progression of chronic liver disease will be discussed. It is notable that in addition to its hepatoprotective effects, xanthohumol also holds promise as a therapeutic agent for treating obesity, dysregulation of glucose metabolism and other components of the metabolic syndrome including hepatic steatosis. Thus, therapeutic xanthohumol application appears as a promising strategy, particularly in obese patients, to inhibit the development as well as the progression of non-alcoholic fatty liver disease. PMID:25999863

  2. Constituents from stem barks of Luehea ochrophylla Mart and evaluation of their antiparasitic, antimicrobial, and antioxidant activities.

    PubMed

    Araújo, C R R; Silva, R R; Silva, T M; Takahashi, J A; Sales-Junior, P A; Dessimoni-Pinto, N A V; Souza-Fagundes, E M; Romanha, A J; Murta, S M F; Alcântara, A F C

    2016-12-14

    Luehea species are found in almost all Central and South American countries. The present work describes the phytochemical study, isolation, and structural characterisation of friedelin, β-friedelinol, lupeol, pseudotaraxasterol, β-sitosterol, betulinic acid, taraxasterol, (-)-epicatechin, β-sitosterol-3-O-β-d-glucopyranoside, and (+)-epicatechin-(4β→8)-epicatechin from stem barks of Luehea ochrophylla Mart. The structural identification of the isolated compounds was mainly performed by NMR analyses and comparison with the data from literature. These compounds were isolated for the first time in the genus Luehea, except β-sitosterol glucopyranoside, (-)-epicatechin, and lupeol. Hexane extract (HE) and dichloromethane (DF) and ethyl acetate (AF) fractions exhibited antiparasitic activity against amastigote (intracellular) and trypomastigote culture forms of Trypanosoma cruzi. The ethanol extract (EE), DF, and ethanol fraction (EF) exhibited considerable antifungal activity against Candida albicans. Moreover, extracts and fractions exhibited significant percentage of capture free radicals of 2,2-diphenyl-picrylhydrazyl (DPPH) when compared to the standard of ascorbic acid.

  3. Antioxidant and α-glucosidase inhibitory activities of cucurbit fruit vegetables and identification of active and major constituents from phenolic-rich extracts of Lagenaria siceraria and Sechium edule.

    PubMed

    Sulaiman, Shaida Fariza; Ooi, Kheng Leong; Supriatno

    2013-10-23

    Antioxidant and α-glucosidase activities and total phenolic contents (TPC) in sequential extracts of dried pulps from seven cucurbit fruit vegetables were determined for the first time. The highest TPC and metal chelating activity were obtained from the chloroform extracts of Luffa acutangula (28.04 ± 0.37 mg GAE/g extract) and Benincasa hispida (EC50 = 0.44 ± 0.03 mg/mL), respectively. The ethyl acetate extract of Sechium edule showed the highest 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity (951.73 ± 29.14 mM TE/g extract). The highest reducing and anti-α-glucosidase activities were shown by the methanol and ethyl acetate extracts of Momordica charantia (692.56 ± 43.38 mM AscAE/g extract; 66.64 ± 2.94%, respectively). The highest correlation (r = 0.99) was observed between the TPC and DPPH values of S. edule. Although caffeic acid was quantified as the major constituent in the methanol extract of Lagenaria siceraria , isoquercetin was found to be the main contributor to the activities. Gallic acid was identified as both the main and most active antioxidant constituent in the ethyl acetate extract of S. edule.

  4. Studies on the antimicrobial activity and brine shrimp toxicity of Zeyheria tuberculosa (Vell.) Bur. (Bignoniaceae) extracts and their main constituents

    PubMed Central

    Bastos, Maria Lysete A; Lima, Maria Raquel F; Conserva, Lucia M; Andrade, Vânia S; Rocha, Eliana MM; Lemos, Rosangela PL

    2009-01-01

    Background Due to the indiscriminate use of antimicrobial drugs, the emergence of human pathogenic microorganisms resistant to major classes of antibiotics has been increased and has caused many clinical problems in the treatment of infectious diseases. Thus, the aim of this study was to evaluate for the first time the in vitro antimicrobial activity and brine shrimp lethality of extracts and isolated compounds from Zeyheria tuberculosa (Vell.) Bur., a species used in Brazilian folk medicine for treatment of cancer and skin diseases. Methods Using the disc diffusion method, bioautography assay and brine shrimp toxicity test (Artemia salina Leach), we studied the antimicrobial activity and lethality of extracts and isolated compounds against three microorganisms strains, including Gram-positive (Staphylococcus aureus) and Gram-negative (Pseudomonas aeruginosa) bacteria and yeasts (Candida albicans). Results In this study, the extracts inhibited S. aureus (8.0 ± 0.0 to 14.0 ± 0.0 mm) and C. albicans (15.3 ± 0.68 to 25.6 ± 0.4 mm) growth. In the brine shrimp test, only two of them showed toxic effects (LC50 29.55 to 398.05 μg/mL) and some extracts were non-toxic or showed weak lethality (LC50 705.02 to > 1000 μg/mL). From these extracts, four flavones [5,6,7,8-tetramethoxyflavone (1), 5,6,7-trimethoxyflavone (2), 4'-hydroxy-5,6,7,8-tetramethoxyflavone (3), and 4'-hydroxy-5,6,7-trimethoxyflavone (4)] were isolated through bioassay-guided fractionation and identified based on the 1D and 2D NMR spectral data. By bioautography assays, compounds 1 [S. aureus (16.0 ± 0.0 mm) and C. albicans (20.0 ± 0.0 mm)] and 3 [S. aureus (10.3 ± 0.6 mm) and C. albicans (19.7 ± 0.6 mm)] inhibited both microorganisms while 2 inhibited only S. aureus (11.7 ± 0.6 mm). Compound 4 did not restrain the growth of any tested microorganism. Conclusion Our results showed that extracts and isolated flavones from Z. tuberculosa may be particularly useful against two pathogenic

  5. Effect of constituent phase on mechanical properties of 9Cr-1WVTa reduced activation ferritic-martensitic steels

    NASA Astrophysics Data System (ADS)

    Lee, Chang-Hoon; Moon, Joonoh; Park, Min-Gu; Lee, Tae-Ho; Jang, Min-Ho; Kim, Hyoung Chan; Suh, Dong-Woo

    2014-12-01

    Influence of the formation of ferrite and accompanying carbides in martensite matrix on the tensile and Charpy impact properties was investigated for reduced activation ferritic-martensitic (RAFM) 9Cr-1WVTa steel. As the fractions of ferrite and carbide adjacent to the ferrite grain boundary increase, both tensile and Charpy impact properties deteriorated in as-normalized condition. In particular, the tensile strength and elongation decreased simultaneously, which is believed to be led by the localized deformation in ferrite which is softer than martensite, promoting the formation and growth of voids. In addition, the formation of ferrite was also detrimental to the Charpy impact properties regarding to the absorbed energy because the precipitation of carbides around ferrite were vulnerable to the nucleation and propagation of cleavage cracks. The degradation of tensile properties can be recovered by tempering, but the DBTT temperature still increases with presence of ferrite.

  6. In vivo evaluation of analgesic, anti-inflammatory, and neuropharmacological activities of the chemical constituent from Nepeta clarkei.

    PubMed

    Hussain, Javid; Rehman, Najeeb Ur; Al-Harrasi, Ahmed; Khan, Abdul Latif; Rizvi, Tania Shamim; Mohammad, Faryal Vali; Mehjabeen; Ali, Liaqat

    2015-06-01

    The plant species of genus Nepeta are used to treat various human diseases and for ornamental purposes as well. Nepethalate B (1) was isolated as a result of phytochemical investigations of Nepeta clarkei and was subjected in the present study for investigation of analgesic, anti-inflammatory, and central nervous system (CNS) depressant activities. The percentage inhibition in phase I of the acetic acid induced writhing test of compound 1 (dose of 0.1, 0.2 and 0.4 mg/kg of body weight) was 53.3, 58.0 and 86.7% respectively. These results were found significantly higher (P < 0.01) as compared to the negative control. Moreover, the percentage inhibitions of three phases for 0.1, 0.2 and 0.4 mg/kg were higher than the values obtained for Aspirin (positive control). In formalin test, the percentage pain inhibition between 0 and 5 min (early phase) was 68.0, 25.5, and 75.5% for 0.1, 0.2 and 0.4 mg/kg intra-peritoneal doses of compound 1 respectively. In case of late phase (20-30 min) it was 63.0, 66.7 and 48.1%, respectively. In comparison to aspirin, overall percentage inhibition of compound 1 was significantly higher in early and late phases. Interestingly, at all doses compound 1 showed more potent anti-inflammatory effects in terms of intensity and duration as compared to aspirin. The gross behavioral study of nepethalate B (1) was also carried out and the results revealed that it exhibited CNS depression in the mice and showed a prominent decrease in locomotor activity.

  7. Chemical composition, larvicidal, and biting deterrent activity of essential oils of two subspecies of Tanacetum argenteum (Asterales: Asteraceae) and individual constituents against Aedes aegypti (Diptera: Culicidae).

    PubMed

    Ali, Abbas; Tabanca, Nurhayat; Kurkcuoglu, Mine; Duran, Ahmet; Blythe, Eugene K; Khan, Ikhlas A; Baser, K Husnu Can

    2014-07-01

    Water-distilled essential oils from dried aerial parts of Tanacetum argenteum (Lam.) Willd. subsp. argenteum (Lam.) and T. argenteum (Lam.) Willd. subsp. canum (C. Koch) Grierson were analyzed by gas chromatography and gas chromatography-mass spectrometry. In total, 27 and 32 components were identified representing 97.2 and 98.7% of essential oils of subsp. argenteum and canum, respectively. Main compounds of T. argenteum subsp. argenteum were alpha-pinene (67.9%) and beta-pinene (4.8%), whereas alpha-pinene (53.6%), 1, 8-cineole (14.8%), and camphor (4.7%) were the major constituents of subsp. canum. Essential oil of T. argenteum subsp. canum at 10 microg/cm2 with Biting Deterrent Index (BDI) value of 0.73 showed activity similar to N,N-Diethyl-meta-toluamide (DEET) at 25 mol/cm2, whereas the activity of essential oil of subsp. argenteum was lower (BDI = 0.47) than subsp. canum and DEET. Based on 95% CIs, activity of beta-caryophyllene (BDI value = 0.54) and caryophyllene oxide (BDI = 0.66) were significantly lower than DEET. In larval bioassays, essential oil of T. argenteum subsp. argenteum showed LC50 value of 93.34 ppm, whereas T. argenteum subsp. canum killed only 40% of the larvae at the highest dose of 125 ppm. Among the pure compounds, beta-caryophyllene (LC50 = 26 ppm) was the most potent compound followed by caryophyllene oxide (LC50 = 29 ppm), which was also similar to (-)-beta-pinene (LC50 = 35.9 ppm) against 1-d-old Ae. aegypti larvae at 24-h post treatment. Compounds (-)-alpha-pinene and (+)-beta-pinene showed similar larvicidal activity. Activity of (+)-alpha-pinene with LC50 value of was similar to the essential oil of T. argenteum subsp. argenteum.

  8. Chemical Constituents of Smilax china L. Stems and Their Inhibitory Activities against Glycation, Aldose Reductase, α-Glucosidase, and Lipase.

    PubMed

    Lee, Hee Eun; Kim, Jin Ah; Whang, Wan Kyunn

    2017-03-11

    The search for natural inhibitors with anti-diabetes properties has gained increasing attention. Among four selected Smilacaceae family plants, Smilax china L. stems (SCS) showed significant in vitro anti-glycation and rat lens aldose reductase inhibitory activities. Bioactivity-guided isolation was performed with SCS and four solvent fractions were obtained, which in turn yielded 10 compounds, including one phenolic acid, three chlorogenic acids, four flavonoids, one stilbene, and one phenylpropanoid glycoside; their structures were elucidated using nuclear magnetic resonance and mass spectrometry. All solvent fractions, isolated compounds, and stem extracts from plants sourced from six different provinces of South Korea were next tested for their inhibitory effects against advanced glycation end products, as well as aldose reductase. α-Glucosidase, and lipase assays were also performed on the fractions and compounds. Since compounds 3, 4, 6, and 8 appeared to be the superior inhibitors among the tested compounds, a comparative study was performed via high-performance liquid chromatography with photodiode array detection using a self-developed analysis method to confirm the relationship between the quantity and bioactivity of the compounds in each extract. The findings of this study demonstrate the potent therapeutic efficacy of SCS and its potential use as a cost-effective natural alternative medicine against type 2 diabetes and its complications.

  9. Constituent analysis of the ethanol extracts of Chimonanthus nitens Oliv. leaves and their inhibitory effect on α-glucosidase activity.

    PubMed

    Chen, Hui; Ouyang, Kehui; Jiang, Yan; Yang, Zhanwei; Hu, Wenbing; Xiong, Lei; Wang, Ning; Liu, Xin; Wang, Wenjun

    2017-05-01

    The ethanol extracts of Chimonanthus nitens Oliv. leaves were prepared sequentially by ethanol gradient elution and tested for their α-glucosidase inhibitory. The fraction of 50% ethanol eluate (EE) exhibited the notable inhibition with IC50 of 0.376mg/mL. Also, 50% EE was chemically characterized by liquid chromatography-mass spectrometry (LC-MS) analysis. Eight compounds including rutin (1), hyperin (2), isoquercitrin (3), luteoloside (4), astragalin (6), quercetin (13), naringenin (14), kaempferol (15) were identified by compared with standard substances as well as proper luteolin-5-O-glucoside (5), kaempferol-7-O-rhamnoside (9), 5,7,8-trihydroxy-2-methoxyl-flavone-7-O-glucoside (10), kaempferol-7-O-acetyl-galactoside (11). The experiments of ultra-filtration combined with liquid chromatography-mass spectrometry (UF-LC-MS) guided quercetin and kaempferol as the key factors for 50% EE showing highly inhibitory activity on α-glucosidase. Quercetin and kaempferol inhibited yeast α-glucosidase in a mixed-type manner with IC50 of 66.8 and 109μg/mL, respectively. These results would provide theoretical underpinning for the C. nitens Oliv. leaves ethanol extracts used as nutraceutical health supplement in the management of type 2 diabetes.

  10. Simultaneous quantification of 25 active constituents in the total flavonoids extract from Herba Desmodii Styracifolii by high-performance liquid chromatography with electrospray ionization tandem mass spectrometry.

    PubMed

    Guo, Panpan; Yan, Wenying; Han, Qingjie; Wang, Chunying; Zhang, Zijian

    2015-04-01

    A sensitive and selective high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry method has been developed and validated for the simultaneous determination of 25 active constituents, including 21 flavonoids and four phenolic acids in the total flavonoids extract from Herba Desmodii Styracifolii for the first time. Among the 25 compounds, seven compounds including caffeic acid, acacetin, genistein, genistin, diosmetin, diosmin and hesperidin were identified and quantified for the first time in Herba Desmodii Styracifolii. Chromatographic separation was accomplished on a ZORBAX SB-C18 (250 mm×4.6 mm, 5.0 μm) column using gradient elution of methanol and 0.1‰ acetic acid v/v at a flow rate of 1.0 mL/min. The identification and quantification of the analytes were achieved using negative electrospray ionization mass spectrometry in multiple-reaction monitoring mode. The method was fully validated in terms of limits of detection and quantification, linearity, precision and accuracy. The results indicated that the developed method is simple, rapid, specific and reliable. Furthermore, the developed method was successfully applied to quantify the 25 active components in six batches of total flavonoids extract from Herba Desmodii Styracifolii.

  11. Alkaloid constituents from flower buds and leaves of sacred lotus (Nelumbo nucifera, Nymphaeaceae) with melanogenesis inhibitory activity in B16 melanoma cells.

    PubMed

    Nakamura, Seikou; Nakashima, Souichi; Tanabe, Genzo; Oda, Yoshimi; Yokota, Nami; Fujimoto, Katsuyoshi; Matsumoto, Takahiro; Sakuma, Rika; Ohta, Tomoe; Ogawa, Keiko; Nishida, Shino; Miki, Hisako; Matsuda, Hisashi; Muraoka, Osamu; Yoshikawa, Masayuki

    2013-02-01

    Methanolic extracts from the flower buds and leaves of sacred lotus (Nelumbo nucifera, Nymphaeaceae) were found to show inhibitory effects on melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells. From the methanolic extracts, a new alkaloid, N-methylasimilobine N-oxide, was isolated together with eleven benzylisoquinoline alkaloids. The absolute stereostructure of the new alkaloid was determined from chemical and physicochemical evidence. Among the constituents isolated, nuciferine, N-methylasimilobine, (-)-lirinidine, and 2-hydroxy-1-methoxy-6a,7-dehydroaporphine showed potent inhibition of melanogenesis. Comparison of the inhibitory activities of synthetic related alkaloids facilitated characterization of the structure-activity relationships of aporphine- and benzylisoquinoline-type alkaloids. In addition, 3-30 μM nuciferine and N-methylasimilobine inhibited the expression of tyrosinase mRNA, 3-30 μM N-methylasimilobine inhibited the expression of TRP-1 mRNA, and 10-30 μM nuciferine inhibited the expression of TRP-2 mRNA.

  12. Chemical constituents and antioxidant activity of essential oil and organic extract from the peel and kernel parts of Citrus japonica Thunb. (kumquat) from Iran.

    PubMed

    Nouri, Amrah; Shafaghatlonbar, Ali

    2016-01-01

    The constituents of essential oils and organic extracts from peel and kernels of Citrus japonica were analysed by GC and GC/MS. The content of essential oil in peel and kernel was 1.1 and 0.8% based on dry weight. The essential oil of C. japonica peel and kernel was characterised by a higher amount of limonene (51.0 and 47.1%) and germacrene D (12.1 and 6.3%), and the hexane extracts of its peel and kernel were characterised by a higher amount of dodecanol-1(12.9 and 20.8%) and linolenic acid (13.1 and 16.3%), respectively. The antioxidant activities of oils were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) method. The results indicate that both oils from different parts of C. japonica possess considerable antioxidant activity. The fruit peel and kernel essential oil could thus be useful in the industries, chiefly in the food and pharmaceutical industries.

  13. Laboratory and Simulated Field Bioassays to Evaluate Larvicidal Activity of Pinus densiflora Hydrodistillate, Its Constituents and Structurally Related Compounds against Aedes albopictus, Aedes aegypti and Culex pipiens pallens in Relation to Their Inhibitory Effects on Acetylcholinesterase Activity.

    PubMed

    Lee, Dong Chan; Ahn, Young-Joon

    2013-05-30

    The toxicity of Pinus densiflora (red pine) hydrodistillate, its 19 constituents and 28 structurally related compounds against early third-instar larvae of Aedes albopictus (Ae. albopictus), Aedes aegypti (Ae. aegypti) and Culex pipiens palles (Cx. p. pallens) was examined using direct-contact bioassays. The efficacy of active compounds was further evaluated in semi-field bioassays using field-collected larval Cx. p. pallens. Results were compared with those of two synthetic larvicides, temephos and fenthion. In laboratory bioassays, Pinus densiflora hydrodistillate was found to have 24 h LC50 values of 20.33, 21.01 and 22.36 mg/L against larval Ae. albopictus, Ae. aegypti and Cx. p. pallens respectively. Among the identified compounds, thymol, δ-3-carene and (+)-limonene exhibited the highest toxicity against all three mosquito species. These active compounds were found to be nearly equally effective in field trials as well. In vitro bioassays were conducted to examine the acetylcholinesterase (AChE) inhibitory activity of 10 selected compounds. Results showed that there is a noticeable correlation between larvicidal activity and AChE inhibitory activity. In light of global efforts to find alternatives for currently used insecticides against disease vector mosquitoes, Pinus densiflora hydrodistillate and its constituents merit further research as potential mosquito larvicides.

  14. [Effects of Schisandra chinensis (Wuweizi) constituents on the activity of hepatic microsomal CYP450 isozymes in rats detected by using a cocktail probe substrates method].

    PubMed

    Wang, Bao-Lian; Hu, Jin-Ping; Sheng, Li; Li, Yan

    2011-08-01

    Effects of constituents from Schisandra chinensis (Wuweizi) on six liver microsomal CYP450 isozymes (CYP1A2, CYP2C6, CYP2C11, CYP2D2, CYP2E1 and CYP3A1/2) were studied in rats in vivo and in vitro. The in vitro incubation was conducted using liver microsomes of rats after multiple dosing of alcoholic/water extract from Schisandra chinensis. A HPLC-MS method was applied to determine the metabolites formation of six CYP450s probe substrates (phenacetin-CYP1A2, dextromethorphan-CYP2D2, diclofenac sodium-CYP2C6, mephenytoin-CYP2C11, chlorzoxazone-CYP2E1 and midazolam-CYP3A1/2) in rat liver microsomal incubations. The activity of CYP450 isozymes were represented by the formation of metabolites. Alcoholic extract of Schisandra chinensis (28-120 microg x mL(-1)) showed significant inhibitory effect on six CYP450 isozymes to a certain extent in vitro. Multiple dosing of Schisandra chinensis alcoholic extract (1.5 g x kg(-1), qd x 7d) had significant induction on CYP2E1 and CYP3A1/2, inhibition on CYP2D2 and CYP2C11, and no effect on CYP2C6 and CYP1A2. Water extract of Schisandra chinensis (100-500 microg x mL(-1)) also exhibited inhibition on the activity of CYP450 isozymes in vitro, whereas multiple administrations (1.5 g x kg(-1), qd x 7d) had significant induction of CYP2E1 and inhibition on CYP2D2, no effect on CYP2C6, CYP3A1/2, CYP1A2 or CYP2C11. The results suggested that the constituents from Schisandra chinensis exhibited the inhibition and induction on six rat liver microsomal CYP450 isozymes to a certain extent in vivo and in vitro. The possibility of interaction between Schisandra chinensis and coadministrative drugs will be considered base on the levels and subtype of CYP450 involved in the drug metabolism.

  15. Active thermal isolation for temperature responsive sensors

    NASA Technical Reports Server (NTRS)

    Martinson, Scott D. (Inventor); Gray, David L. (Inventor); Carraway, Debra L. (Inventor); Reda, Daniel C. (Inventor)

    1994-01-01

    The detection of flow transition between laminar and turbulent flow and of shear stress or skin friction of airfoils is important in basic research for validation of airfoil theory and design. These values are conventionally measured using hot film nickel sensors deposited on a polyimide substrate. The substrate electrically insulates the sensor and underlying airfoil but is prevented from thermally isolating the sensor by thickness constraints necessary to avoid flow contamination. Proposed heating of the model surface is difficult to control, requires significant energy expenditures, and may alter the basic flow state of the airfoil. A temperature responsive sensor is located in the airflow over the specified surface of a body and is maintained at a constant temperature. An active thermal isolator is located between this temperature responsive sensor and the specific surface of the body. The total thickness of the isolator and sensor avoid any contamination of the flow. The temperature of this isolator is controlled to reduce conductive heat flow from the temperature responsive sensor to the body. This temperature control includes (1) operating the isolator at the same temperature as the constant temperature of the sensor; and (2) establishing a fixed boundary temperature which is either less than or equal to, or slightly greater than the sensor constant temperature. The present invention accordingly thermally isolates a temperature responsive sensor in an energy efficient, controllable manner while avoiding any contamination of the flow.

  16. Antimalarial activity and safety assessment of Flueggea virosa leaves and its major constituent with special emphasis on their mode of action.

    PubMed

    Singh, Shiv Vardan; Manhas, Ashan; Kumar, Yogesh; Mishra, Sonali; Shanker, Karuna; Khan, Feroz; Srivastava, Kumkum; Pal, Anirban

    2017-03-05

    A clinical emergency stands due to the appearance of drug resistant Plasmodium strains necessitate novel and effective antimalarial chemotypes, where plants seem as the prime option, especially after the discovery of quinine and artemisinin. The present study was aimed towards bioprospecting leaves of Flueggea virosa for its antimalarial efficacy and active principles. Crude hydro-ethanolic extract along with solvent derived fractions were tested in vitro against Plasmodium falciparum CQ sensitive (3D7) and resistant (K1) strains, where all the fractions exhibited potential activity (IC50 values <10μg/mL) against both the strains. Interestingly, under in vivo conditions against P. berghei in Swiss mice, preferential chemo-suppression was recorded for crude hydro-ethanolic extract (77.38%) and ethyl acetate fraction (86.09%) at the dose of 500mg/kg body weight. Additionally, ethyl acetate fraction was found to be capable of normalizing the host altered pharmacological parameters and enhanced oxidative stress augmented during the infection. The bioactivity guided fractionation lead to the isolation of bergenin as a major and active constituent (IC50, 8.07±2.05μM) of ethyl acetate fraction with the inhibition of heme polymerization pathway of malaria parasite being one of the possible chemotherapeutic target. Furthermore, bergenin exhibited a moderate antimalarial activity against P. berghei and also ameliorated parasite induced systemic inflammation in host (mice). Safe toxicity profile elucidated through in vitro cytotoxicity and in silico ADME/T predications evidently suggest that bergenin possess drug like properties. Hence, the present study validates the traditional usage of F. indica as an antimalarial remedy and also insists for further chemical modifications of bergenin to obtain more effective antimalarial chemotypes.

  17. Chemical constituents and free radical scavenging activity of corn pollen collected from Apis mellifera hives compared to floral corn pollen at Nan, Thailand

    PubMed Central

    2012-01-01

    Background Bee pollen is composed of floral pollen mixed with nectar and bee secretion that is collected by foraging honey (Apis sp.) and stingless bees. It is rich in nutrients, such as sugars, proteins, lipids, vitamins and flavonoids, and has been ascribed antiproliferative, anti-allergenic, anti-angiogenic and free radical scavenging activities. This research aimed at a preliminary investigation of the chemical constituents and free radical scavenging activity in A. mellifera bee pollen. Methods Bee pollen was directly collected from A. mellifera colonies in Nan province, Thailand, in June, 2010, whilst floral corn (Zea mays L.) pollen was collected from the nearby corn fields. The pollen was then sequentially extracted with methanol, dichloromethane (DCM) and hexane, and each crude extract was tested for free radical scavenging activity using the DPPH assay, evaluating the percentage scavenging activity and the effective concentration at 50% (EC50). The most active crude fraction from the bee pollen was then further enriched for bioactive components by silica gel 60 quick and adsorption or Sephadex LH-20 size exclusion chromatography. The purity of all fractions in each step was observed by thin layer chromatography and the bioactivity assessed by the DPPH assay. The chemical structures of the most active fractions were analyzed by nuclear magnetic resonance. Results The crude DCM extract of both the bee corn pollen and floral corn pollen provided the highest active free radical scavenging activity of the three solvent extracts, but it was significantly (over 28-fold) higher in the bee corn pollen (EC50 = 7.42 ± 0.12 μg/ml), than the floral corn pollen (EC50 = 212 ± 13.6% μg/ml). After fractionation to homogeneity, the phenolic hydroquinone and the flavone 7-O-R-apigenin were found as the minor and major bioactive compounds, respectively. Bee corn pollen contained a reasonably diverse array of nutritional components, including biotin (56.7 μg/100

  18. Stereoselective Effects of Abused “Bath Salt” Constituent 3,4-Methylenedioxypyrovalerone in Mice: Drug Discrimination, Locomotor Activity, and Thermoregulation

    PubMed Central

    Gannon, Brenda M.; Williamson, Adrian; Suzuki, Masaki; Rice, Kenner C.

    2016-01-01

    3,4-Methylenedioxypyrovalerone (MDPV) is a common constituent of illicit “bath salts” products. MDPV is a chiral molecule, but the contribution of each enantiomer to in vivo effects in mice has not been determined. To address this, mice were trained to discriminate 10 mg/kg cocaine from saline, and substitutions with racemic MDPV, S(+)-MDPV, and R(−)-MDPV were performed. Other mice were implanted with telemetry probes to monitor core temperature and locomotor responses elicited by racemic MDPV, S(+)-MDPV, and R(−)-MDPV under a warm (28°C) or cool (20°C) ambient temperature. Mice reliably discriminated the cocaine training dose from saline, and each form of MDPV fully substituted for cocaine, although marked potency differences were observed such that S(+)-MDPV was most potent, racemic MDPV was less potent than the S(+) enantiomer, and R(−)-MDPV was least potent. At both ambient temperatures, locomotor stimulant effects were observed after doses of S(+)-MDPV and racemic MDPV, but R(−)-MDPV did not elicit locomotor stimulant effects at any tested dose. Interestingly, significant increases in maximum core body temperature were only observed after administration of racemic MDPV in the warm ambient environment; neither MDPV enantiomer altered core temperature at any dose tested, at either ambient temperature. These studies suggest that all three forms of MDPV induce biologic effects, but R(−)-MDPV is less potent than S(+)-MDPV and racemic MDPV. Taken together, these data suggest that the S(+)-MDPV enantiomer is likely responsible for the majority of the biologic effects of the racemate and should be targeted in therapeutic efforts against MDPV overdose and abuse. PMID:26769917

  19. Metabolic responses to simulated extravehicular activity

    NASA Technical Reports Server (NTRS)

    Williamson, Rebecca C.; Sharer, Peter J.; Webbon, Bruce W.; Rendon, Lisa R.

    1992-01-01

    Automatic control of the liquid cooling garment (LCG) worn by astronauts during extravehicular activity (EVA) would more efficiently regulate astronaut thermal comfort and improve astronaut productivity. An experiment was conducted in which subjects performed exercise profiles on a unique, supine upper body ergometer to elicit physiological and thermal responses similar to those achieved during zero-g EVAs. Results were analyzed to quantify metabolic rate, various body temperatures, and other heat balance parameters. Such data may lead to development of a microprocessor-based system to automatically maintain astronaut heat balance during extended EVAs.

  20. Inhibitory Activities of Stauntonia hexaphylla Leaf Constituents on Rat Lens Aldose Reductase and Formation of Advanced Glycation End Products and Antioxidant

    PubMed Central

    Hwang, Seung Hwan; Kwon, Shin Hwa; Kim, Set Byeol

    2017-01-01

    Stauntonia hexaphylla (Thunb.) Decne. (Lardizabalaceae) leaves (SHL) have been used traditionally as analgesics, sedatives, diuretics, and so on, in China. To date, no data have been reported on the inhibitory effect of SHL and its constituents on rat lens aldose reductase (RLAR) and advanced glycation end products (AGEs). Therefore, the inhibitory effect of compounds isolated from SHL extract on RLAR and AGEs was investigated to evaluate potential treatments of diabetic complications. The ethyl acetate (EtOAC) fraction of SHL extract showed strong inhibitory activity on RLAR and AGEs; therefore, EtOAc fraction (3.0 g) was subjected to Sephadex LH-20 column chromatography, for further fractionation, with 100% MeOH solvent system to investigate its effect on RLAR and AGEs. Phytochemical investigation of SHL led to the isolation of seven compounds. Among the isolated compounds, chlorogenic acid, calceolarioside B, luteolin-3′-O-β-D-glucopyranoside, quercetin-3-O-β-D-glucopyranoside, and luteolin-7-O-β-D-glucopyranoside exhibited significant inhibitory activity against RLAR with IC50 in the range of 7.34–23.99 μM. In addition, 3-(3,4-dihydroxyphenyl) propionic acid, neochlorogenic acid, and luteolin-3′-O-β-D-glucopyranoside exhibited the most potent inhibitory activity against formation of AGEs, with an IC50 value of 115.07–184.06 μM, compared to the positive control aminoguanidine (820.44 μM). Based on these findings, SHL dietary supplements could be considered for the prevention and/or treatment of diabetes complication. PMID:28326319

  1. Self-Assembly of the Toll-Like Receptor Agonist Macrophage-Activating Lipopeptide MALP-2 and of Its Constituent Peptide.

    PubMed

    Castelletto, Valeria; Kirkham, Steven; Hamley, Ian W; Kowalczyk, Radoslaw; Rabe, Martin; Reza, Mehedi; Ruokolainen, Janne

    2016-02-08

    The self-assembly of the macrophage-activating lipopeptide MALP-2 in aqueous solution has been investigated and is compared to that of the constituent peptide GNNDESNISFKEK. MALP-2 is a toll-like receptor agonist lipopeptide with diverse potential biomedical applications and its self-assembly has not previously been examined. It is found to self-assemble, above a critical aggregation concentration (cac), into remarkable "fibre raft" structures, based on lateral aggregation of β-sheet based bilayer tapes. Peptide GNNDESNISFKEK also forms β-sheet structures above a cac, although the morphology is distinct, comprising highly extended and twisted tape structures. A detailed insight into the molecular packing within the MALP-2 raft and GNNDESNISFKEK nanotape structures is obtained through X-ray diffraction and small-angle X-ray scattering. These results point to the significant influence of the attached lipid chains on the self-assembly motif, which lead to the raft structure for the lipopeptide assemblies.

  2. Trisomy 21 consistently activates the interferon response

    PubMed Central

    Sullivan, Kelly D; Lewis, Hannah C; Hill, Amanda A; Pandey, Ahwan; Jackson, Leisa P; Cabral, Joseph M; Smith, Keith P; Liggett, L Alexander; Gomez, Eliana B; Galbraith, Matthew D; DeGregori, James; Espinosa, Joaquín M

    2016-01-01

    Although it is clear that trisomy 21 causes Down syndrome, the molecular events acting downstream of the trisomy remain ill defined. Using complementary genomics analyses, we identified the interferon pathway as the major signaling cascade consistently activated by trisomy 21 in human cells. Transcriptome analysis revealed that trisomy 21 activates the interferon transcriptional response in fibroblast and lymphoblastoid cell lines, as well as circulating monocytes and T cells. Trisomy 21 cells show increased induction of interferon-stimulated genes and decreased expression of ribosomal proteins and translation factors. An shRNA screen determined that the interferon-activated kinases JAK1 and TYK2 suppress proliferation of trisomy 21 fibroblasts, and this defect is rescued by pharmacological JAK inhibition. Therefore, we propose that interferon activation, likely via increased gene dosage of the four interferon receptors encoded on chromosome 21, contributes to many of the clinical impacts of trisomy 21, and that interferon antagonists could have therapeutic benefits. DOI: http://dx.doi.org/10.7554/eLife.16220.001 PMID:27472900

  3. Cerebral blood flow response to functional activation

    PubMed Central

    Paulson, Olaf B; Hasselbalch, Steen G; Rostrup, Egill; Knudsen, Gitte Moos; Pelligrino, Dale

    2010-01-01

    Cerebral blood flow (CBF) and cerebral metabolic rate are normally coupled, that is an increase in metabolic demand will lead to an increase in flow. However, during functional activation, CBF and glucose metabolism remain coupled as they increase in proportion, whereas oxygen metabolism only increases to a minor degree—the so-called uncoupling of CBF and oxidative metabolism. Several studies have dealt with these issues, and theories have been forwarded regarding the underlying mechanisms. Some reports have speculated about the existence of a potentially deficient oxygen supply to the tissue most distant from the capillaries, whereas other studies point to a shift toward a higher degree of non-oxidative glucose consumption during activation. In this review, we argue that the key mechanism responsible for the regional CBF (rCBF) increase during functional activation is a tight coupling between rCBF and glucose metabolism. We assert that uncoupling of rCBF and oxidative metabolism is a consequence of a less pronounced increase in oxygen consumption. On the basis of earlier studies, we take into consideration the functional recruitment of capillaries and attempt to accommodate the cerebral tissue's increased demand for glucose supply during neural activation with recent evidence supporting a key function for astrocytes in rCBF regulation. PMID:19738630

  4. Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways

    PubMed Central

    Hou, Yue; Li, Guoxun; Wang, Jian; Pan, Yingni; Jiao, Kun; Du, Juan; Chen, Ru; Wang, Bing; Li, Ning

    2017-01-01

    The EtOAc extract of Coreopsis tinctoria Nutt. significantly inhibited LPS-induced nitric oxide (NO) production, as judged by the Griess reaction, and attenuated the LPS-induced elevation in iNOS, COX-2, IL-1β, IL-6 and TNF-α mRNA levels, as determined by quantitative real-time PCR, when incubated with BV-2 microglial cells. Immunohistochemical results showed that the EtOAc extract significantly decreased the number of Iba-1-positive cells in the hippocampal region of LPS-treated mouse brains. The major effective constituent of the EtOAc extract, okanin, was further investigated. Okanin significantly suppressed LPS-induced iNOS expression and also inhibited IL-6 and TNF-α production and mRNA expression in LPS-stimulated BV-2 cells. Western blot analysis indicated that okanin suppressed LPS-induced activation of the NF-κB signaling pathway by inhibiting the phosphorylation of IκBα and decreasing the level of nuclear NF-κB p65 after LPS treatment. Immunofluorescence staining results showed that okanin inhibited the translocation of the NF-κB p65 subunit from the cytosol to the nucleus. Moreover, okanin significantly inhibited LPS-induced TLR4 expression in BV-2 cells. In summary, okanin attenuates LPS-induced activation of microglia. This effect may be associated with its capacity to inhibit the TLR4/NF-κB signaling pathways. These results suggest that okanin may have potential as a nutritional preventive strategy for neurodegenerative disorders. PMID:28367982

  5. Resveratrol regulates gene transcription via activation of stimulus-responsive transcription factors.

    PubMed

    Thiel, Gerald; Rössler, Oliver G

    2017-03-01

    Resveratrol (trans-3,4',5-trihydroxystilbene), a polyphenolic phytoalexin of grapes and other fruits and plants, is a common constituent of our diet and of dietary supplements. Many health-promoting benefits have been connected with resveratrol in the treatment of cardiovascular diseases, cancer, diabetes, inflammation, neurodegeneration, and diseases connected with aging. To explain the pleiotropic effects of resveratrol, the molecular targets of this compound have to be identified on the cellular level. Resveratrol induces intracellular signal transduction pathways which ultimately lead to changes in the gene expression pattern of the cells. Here, we review the effect of resveratrol on the activation of the stimulus-responsive transcription factors CREB, AP-1, Egr-1, Elk-1, and Nrf2. Following activation, these transcription factors induce transcription of delayed response genes. The gene products of these delayed response genes are ultimately responsible for the changes in the biochemistry and physiology of resveratrol-treated cells. The activation of stimulus-responsive transcription factors may explain many of the intracellular activities of resveratrol. However, results obtained in vitro may not easily be transferred to in vivo systems.

  6. Multivariate data analysis to evaluate the fingerprint peaks responsible for the cytotoxic activity of Mallotus species.

    PubMed

    Tistaert, C; Chataigné, G; Dejaegher, B; Rivière, C; Nguyen Hoai, N; Chau Van, M; Quetin-Leclercq, J; Vander Heyden, Y

    2012-12-01

    The Mallotus genus comprises numerous species used as traditional medicines in oriental countries and provides scientists a broad basis in the search for pharmacologically active constituents. In this paper, the cytotoxicity of 39 Mallotus extracts, different in species, part of the plant used, origin, and harvest season, is evaluated combining cytotoxicity assays with fingerprint technology and data handling tools. At first, the antiproliferative activity of the plant extracts is analyzed both on a non-cancerous cell line (WI-38--human lung fibroblast) and on a cancerous cell line (HeLa human cervix carcinoma). The results are linked to a data set of high-performance liquid chromatographic fingerprint profiles of the samples using multivariate calibration techniques. The regression coefficients of the multivariate model are then evaluated to indicate those peaks potentially responsible for the cytotoxic activity of the Mallotus extracts. In a final step, the cytotoxic extracts are analyzed by HPLC-MS and the indicated peaks identified.

  7. In Vitro and In Vivo Efficacy Studies of Lavender angustifolia Essential Oil and Its Active Constituents on the Proliferation of Human Prostate Cancer.

    PubMed

    Zhao, Yunqi; Chen, Ran; Wang, Yun; Qing, Chen; Wang, Wei; Yang, Yixin

    2016-05-05

    Lavandula angustifolia is the most widely cultivated Lavandula species. The extraction of its flower and leaves has been used as herbal medicine. In this study, the in vitro antitumor activities were tested on human prostate cancer PC-3 and DU145 cell lines. Flow cytometry technology was applied to study apoptosis induction and cell cycle arrest. The PC-3 cell line was used to establish subcutaneous xenograft tumors in nude mice. Paraffin sections from xenograft tumor specimens were used in the TUNEL (terminal deocynucleotide transferase dUTP nick end labeling) assay and an immunohistochemistry assay to detect cell proliferation markers Ki67 and PCNA. Lavender essential oil, linalool, and linalyl acetate showed stronger inhibitory effect on PC-3 cells than on DU145 cells. The apoptotic cell populations observed in PC-3 cells treated with lavender essential oil, linalool, and linalyl acetate were 74.76%, 67.11%, and 56.14%, respectively. The PC-3 cells were mainly arrested in the G2/M phase. In the xenograft model with PC-3 cell transplantation, essential oil and linalool significantly suppressed tumor growth. The immunosignals of Ki67 and PCNA in the essential oil, linalool, and linalyl acetate treatment groups were significantly lower than that of the control group in xenograft tumor sections. The TUNEL assay indicated that each of the 3 phytochemicals significantly induced apoptosis compared to the control group. This study provides novel insight and evidence on the antiproliferative effect of L angustifolia essential oil and its major constituents on human prostate cancer. The antitumor effect was associated with cell proliferation inhibition and apoptosis induction in xenograft tumors.

  8. The Protective Effect of α-Hederin, the Active Constituent of Nigella sativa, on Lung Inflammation and Blood Cytokines in Ovalbumin Sensitized Guinea Pigs.

    PubMed

    Keyhanmanesh, Rana; Saadat, Saeideh; Mohammadi, Mostafa; Shahbazfar, Amir-Ali; Fallahi, Maryam

    2015-11-01

    In the present study, the preventive effect of two different concentrations of α-hederin, the active constituent of Nigella sativa, on lung inflammation and blood cytokines in ovalbumin sensitized guinea pigs was examined. Forty eight male adult guinea pigs were divided into control (C), sensitized (S) and sensitized pretreated groups; with thymoquinone (S+TQ), low dose (S+LAH) and high dose of α-hederin (S+HAH) and inhaled fluticasone propionate (S+FP). The lung histopathology and blood levels of IL-4, IFN-γ and IL-17 were assessed. Compared to sensitized animals, all pathological changes improved significantly in pretreated groups (p < 0.001 to p < 0.05). These improvements in α-hederin pretreated groups were similar to S+TQ and S+FP groups except cellular infiltration in S+LAH and S+HAH groups which was lower than S+TQ group (p < 0.05). The blood IL-4 and IL-17 levels in S+HAH groups showed a significant decrease compared to S group (p < 0.05) which were similar to S+TQ and S+FP groups. The level of IFN-γ in S+LAH and S+HAH groups increased significantly compared to S group (p < 0.05) which was higher than S+FP group (p < 0.05). Blood IL-4 in S+HAH group was significantly lower than S+LAH group (p < 0.05). In conclusion, α-hederin could attenuate the lung inflammation and improve the changes of cytokines like thymoquinone and fluticasone in used dosages.

  9. Thymoquinone, an active constituent of Nigella sativa seeds, binds with bilirubin and protects mice from hyperbilirubinemia and cyclophosphamide-induced hepatotoxicity.

    PubMed

    Laskar, Amaj A; Khan, Masood A; Rahmani, Arshad H; Fatima, Sana; Younus, Hina

    2016-08-01

    Some reports indicate that thymoquinone (TQ), the main constituent of Nigella sativa seeds, is hepatoprotective. The aim of this study was to determine whether TQ is able to bind directly to bilirubin, and whether TQ or liposomal formulation of TQ (Lip-TQ) can reduce cyclophosphamide (CYP)-induced liver toxicity, serum bilirubin level in mice. The binding of TQ with bilirubin was studied by UV-VIS, fluorescence and Near-UV CD spectroscopy. Inhibition of binding of bilirubin to erythrocytes by TQ was also examined. To increase the in vivo efficacy, Lip-TQ was prepared and used against CYP-induced toxicity. The protective role of TQ or Lip-TQ against CYP-induced toxicity was assessed by determining the liver function parameters, the levels of superoxide dismutase (SOD) and catalase (CAT), and histological studies. It was found that TQ binds to bilirubin and significantly inhibits the binding of bilirubin to erythrocytes. Lip-TQ (10 mg/kg) significantly reduced the levels of aspartate transaminase (AST) from 254 ± 48 to 66 ± 18 IU/L (P < 0.001), alanine transaminase (ALT) from 142 ± 28 to 47.8 ± 16 IU/L (P < 0.05) and serum bilirubin from 2.8 ± 0.50 to 1.24 ± 0.30 mg/dl (P < 0.05). Treatment with Lip-TQ reduced the CYP-induced inflammation and hemorrhage in liver tissues. Moreover, treatment with free or Lip-TQ protected the activity of SOD and CAT in CYP-injected mice. Therefore, TQ can reduce the level of bilirubin in systemic circulation in disease conditions that lead to hyperbilirubinemia and liver toxicity and hence may be used as a supplement in the treatment of liver ailments.

  10. Triterpenoids isolated from apple peels have potent antiproliferative activity and may be partially responsible for apple's anticancer activity.

    PubMed

    He, Xiangjiu; Liu, Rui Hai

    2007-05-30

    Bioactivity-guided fractionation of apple peels was used to determine the chemical identity of bioactive constituents. Thirteen triterpenoids were isolated, and their chemical structures were identified. Antiproliferative activities of the triterpenoids against human HepG2 liver cancer cells, MCF-7 breast cancer cells, and Caco-2 colon cancer cells were evaluated. Most of the triterpenoids showed high potential anticancer activities against the three human cancer cell lines. Among the compounds isolated, 2alpha-hydroxyursolic acid, 2alpha-hydroxy-3beta-{[(2E)-3-phenyl-1-oxo-2-propenyl]oxy}olean-12-en-28-oic acid, and 3beta-trans-p-coumaroyloxy-2alpha-hydroxyolean-12-en-28-oic acid showed higher antiproliferative activity toward HepG2 cancer cells. Ursolic acid, 2alpha-hydroxyursolic acid, and 3beta-trans-p-coumaroyloxy-2alpha-hydroxyolean-12-en-28-oic acid exhibited higher antiproliferative activity against MCF-7 cancer cells. All triterpenoids tested showed antiproliferative activity against Caco-2 cancer cells, especially 2alpha-hydroxyursolic acid, maslinic acid, 2alpha-hydroxy-3beta-{[(2E)-3-phenyl-1-oxo-2-propenyl]oxy}olean-12-en-28-oic acid, and 3beta-trans-p-coumaroyloxy-2alpha-hydroxyolean-12-en-28-oic acid, which displayed much higher antiproliferative activities. These results showed the triterpenoids isolated from apple peels have potent antiproliferative activity and may be partially responsible for the anticancer activities of whole apples.

  11. Antibacterial constituents from Melodinus suaveolens.

    PubMed

    Li, Jiang-Ling; Lunga, Paul-Keilah; Zhao, Yun-Li; Qin, Xu-Jie; Yang, Xing-Wei; Liu, Ya-Ping; Luo, Xiao-Dong

    2015-04-01

    To investigate the non-alkaloidal chemical constituents of the stems and leaves of Melodinus suaveolens and their antibacterial activities. Compounds were isolated and purified by repeated silica gel, Sephadex LH-20, RP18, and preparative HPLC. Their structures were elucidated by comparison with published spectroscopic data, as well as on the basis of extensive spectroscopic analysis. The antibacterial screening assays were performed by the dilution method. Fourteen compounds were isolated, and identified as lycopersene (1), betulinic aldehyde (2), 3β-acetoxy-22,23,24,25,26,27-hexanordammaran-20-one (3), 3a-acetyl-2, 3, 5-trimethyl-7a-hydroxy-5-(4,8,12-trimethyl-tridecanyl)-1,3a,5,6,7,7a-hexahydro-4-oxainden-1-one (4), 3β-hydroxy-28-norlup-20(29)-ene-17β-hydroperoxide (5), 3β-hydroxy-28-norlup-20(29)-ene-17α-hydroperoxide (6), β-sitosterol (7), 28-nor-urs-12-ene-3β, 17β-diol (8), α-amyrin (9), ergosta-4,6,8(14),22-tetraen-3-one (10), 3β-hydroxy-urs-11-en-28,13β-olide (11), betulin (12), obtusalin (13), and ursolic acid (14). Among the isolates, compounds 1, 2, 6, 8, 10, and 14 showed potent antibacterial activities against the four bacteria. This is the first report of the antibacterial activity of the constituents of Melodinus suaveolens.

  12. Banisteriopsis caapi, a unique combination of MAO inhibitory and antioxidative constituents for the activities relevant to neurodegenerative disorders and Parkinson’s disease

    PubMed Central

    Samoylenko, Volodymyr; Rahman, Md. Mostafizur; Tekwani, Babu L.; Tripathi, Lalit M.; Wang, Yan-Hong; Khan, Shabana I.; Khan, Ikhlas A.; Miller, Loren S.; Joshi, Vaishali C.; Muhammad, Ilias

    2009-01-01

    Aim of the study Parkinson’s disease is a neurological disorder mostly effecting the elder population of the world. Currently there is no definitive treatment or cure for this disease. Therefore, in this study the composition and constituents of the aqueous extract of B. caapi for monoamine oxidases (MAO) inhibitory and antioxidant activities were assessed, which are relevant to the prevention of neurological disorders, including Parkinsonism. Materials and methods The aqueous extract of B. caapi stems was standardized and then fractionated using reversed-phase (RP) chromatography. Pure compounds were isolated either by reversed-phase (RP) chromatography or centrifugal preparative TLC, using a Chromatotron®. Structure elucidation was carried out by 1D and 2D NMR, Mass, IR and Circular Dichroism spectroscopy and chemical derivatization. Chemical profiling of the extract was carried out with RP-HPLC. The inhibitory activity of MAO-A, MAO-B, acetylcholinesterase, butyrylcholinesterase and catechol-O-methyl transferase enzymes, as well as antioxidant and cytotoxic activities of both B. caapi extract and isolated compounds were evaluated. Results An examination of the aqueous extracts of B. caapi cultivar Da Vine yielded two new alkaloidal glycosides, named banistenoside A (1) and banistenoside B (2), containing “azepino[1,2-a]tetrahydro-β-carboline” unique carbon framework. One additional new natural tetrahydronorharmine (4), four known β-carbolines harmol (3), tetrahydroharmine (5), harmaline (6) and harmine (7), two known proanthocyanidines (−)-epicatechin (8) and (−)-procyanidin B2 (9), and a new disaccharide β-D-fructofuranosyl-(2→5)-fructopyranose (14) together with known sacharose (15) and β-D-glucose (16) were also isolated. In addition, the acetates of 1, 2, 8, 9, 14 and 15 (compounds 10–13, 17, 18) were also prepared. Harmaline (6) and harmine (7) showed potent in vitro inhibitory activity against recombinant human brain monoamine oxidase

  13. Identification of Major Active Ingredients Responsible for Burn Wound Healing of Centella asiatica Herbs.

    PubMed

    Wu, Fang; Bian, Difei; Xia, Yufeng; Gong, Zhunan; Tan, Qian; Chen, Jiaojiao; Dai, Yue

    2012-01-01

    Centella asiatica herbs have been prescribed as a traditional medicine for wound healing in China and Southeast Asia for a long time. They contain many kinds of triterpenoid compounds, mainly including glycosides (asiaticoside and madecassoside) and corresponding aglycones (asiatic acid and madecassic acid). To identify which is the major active constituent, a comprehensive and comparative study of these compounds was performed. In vitro, primary human skin fibroblasts, originating from healthy human foreskin samples, were treated with various concentrations of asiaticoside, madecassoside, asiatic acid, and madecassic acid, respectively. Cell proliferation, collagen synthesis, MMP-1/TIMP-1 balance, and TGF-β/Smad signaling pathway were investigated. In vivo, mice were orally administered with the four compounds mentioned above for two weeks after burn injury. The speed and quality of wound healing, as well as TGF-β(1) levels in skin tissues, were examined. Interestingly, in contrast to prevalent postulations, asiaticoside and madecassoside themselves, rather than their corresponding metabolites asiatic acid and madecassic acid, are recognized as the main active constituents of C. asiatica herbs responsible for burn wound healing. Furthermore, madecassoside is more effective than asiaticoside (P = 0.0446 for procollagen type III synthesis in vitro, P = 0.0057 for wound healing speed, and P = 0.0491 for wound healing pattern in vivo, correspondingly).

  14. Human platelet glycoprotein Ia. One component is only expressed on the surface of activated platelets and may be a granule constituent

    SciTech Connect

    Bienz, D.; Clemetson, K.J.

    1989-01-05

    Glycoprotein Ia (GP Ia) is a relatively minor component of human blood platelets thought to be a receptor involved in collagen-induced platelet activation. However, some difficulties exist with the definition of this glycoprotein. The expression of GP Ia on resting (prostacyclin analogue-treated) and thrombin-activated platelets was compared by surface labeling with /sup 125/I-lactoperoxidase. Intact platelets or platelets solubilized in sodium dodecyl sulfate were labeled with periodate/(/sup 3/H)NaBH/sub 4/. Analysis on two-dimensional isoelectric focusing/sodium dodecyl sulfate-polyacrylamide gel electrophoresis gels showed that GP Ia is very poorly labeled in resting platelets. After activation a new spot (GP Ia*) appears with the same relative molecular mass as GP Ia under reducing conditions. GP Ia and Ia* can be clearly separated by two-dimensional nonreduced/reduced gel electrophoresis. Therefore, two glycoproteins which have been termed GP Ia exist in platelets with similar molecular weight and pI under reducing conditions. One of these (GP Ia*) is only surface-labeled when platelets are activated, indicating that it is only exposed on the surface of activated platelets. Supernatant from activated platelets contains this glycoprotein as well as other granule components. This glycoprotein is missing in platelets from two patients with collagen-response defects.

  15. Building a Constituency for Children.

    ERIC Educational Resources Information Center

    Hale, Margie

    One of the goals of the West Virginia Task Force on Children, Youth and Families is to build a constituency for children. Two critical factors in building a constituency for children are a shared vision and influential leaders. The four principles used by the Task Force for building a constituency are: (1) defining a regional target for organizing…

  16. Artemisia princeps Pamp. Essential oil and its constituents eucalyptol and α-terpineol ameliorate bacterial vaginosis and vulvovaginal candidiasis in mice by inhibiting bacterial growth and NF-κB activation.

    PubMed

    Trinh, Hien-Trung; Lee, In-Ah; Hyun, Yang-Jin; Kim, Dong-Hyun

    2011-12-01

    To investigate the inhibitory effects of Artemisia princeps Pamp. (family Asteraceae) essential oil (APEO) and its main constituents against bacterial vaginosis and vulvovaginal candidiasis, their antimicrobial activities against Gardnerella vaginalis and Candida albicans in vitro and their anti-inflammatory effects against G. vaginalis-induced vaginosis and vulvovaginal candidiasis were examined in mice. APEO and its constituents eucalyptol and α-terpineol were found to inhibit microbe growths. α-Terpineol most potently inhibited the growths of G. vaginalis and C. albicans with MIC values of 0.06 and 0.125 % (v/v), respectively. The antimicrobial activity of α-terpineol was found to be comparable to that of clotrimazole. Intravaginal treatment with APEO, eucalyptol, or α-terpineol significantly decreased viable G. vaginalis and C. albicans numbers in the vaginal cavity and myeloperoxidase activity in mouse vaginal tissues compared with controls. These agents also inhibited the expressions of proinflammatory cytokines (IL-1 β, IL-6, TNF- α), COX-2, iNOS, and the activation of NF- κB and increased expression of the anti-inflammatory cytokine IL-10. In addition, they inhibited the expressions of proinflammatory cytokines and the activation of NF- κB in lipopolysaccharide-stimulated peritoneal macrophages, and α-terpineol most potently inhibited the expressions of proinflammatory cytokines and NF- κB activation. Based on these findings, APEO and its constituents, particularly α-terpineol, ameliorate bacterial vaginosis and vulvovaginal candidiasis by inhibiting the growths of vaginal pathogens and the activation of NF- κB.

  17. Dose Response Data for Hormonally Active Chemicals ...

    EPA Pesticide Factsheets

    The shape of the dose response curve in the low dose region has been debated since the late 1940s. The debate originally focused on linear no threshold (LNT) vs threshold responses in the low dose range for cancer and noncancer related effects. For noncancer effects the default assumption is that noncancer effects generally display threshold rather than LNT responses. More recently, claims have arisen that the chemicals, like endocrine disrupters (EDS), which act via high affinity, low capacity nuclear receptors, may display LNT or nonmonotonic low dose responses: responses that could be missed in multigenerational guideline toxicity testing. This presentation will discuss LNT, threshold and nonmonotonic dose response relationships from case studies of chemicals that disrupt reproductive development and function via the ER, AR and AhR pathways and will include in vitro and in vivo multigenerational data. The in vivo studies in this discussion include only robust, well designed, comprehensive studies that administered the chemical via a relevant route(s) of exposure over a broad dose response range, including low dose(s) in the microgram/kg/d range. The chemicals include ethinyl estradiol, estradiol, genistein, bisphenol a, trenbolone, finasteride, flutamide, phthalate esters and 2,3,7,8 TCDD. The objective is to critically evaluate the data from well done studies in this field to address concerns that current multigenerational reproductive test gui

  18. Cytotoxic activity of secondary metabolites derived from Artemisia annua L. towards cancer cells in comparison to its designated active constituent artemisinin.

    PubMed

    Efferth, Thomas; Herrmann, Florian; Tahrani, Ahmed; Wink, Michael

    2011-08-15

    Artemisia annua L. (sweet wormwood, qinhao) has traditionally been used in Chinese medicine. The isolation of artemisinin from Artemisia annua and its worldwide accepted application in malaria therapy is one of the showcase success stories of phytomedicine during the past decades. Artemisinin-type compounds are also active towards other protozoal or viral diseases as well as cancer cells in vitro and in vivo. Nowadays, Artemisia annua tea is used as a self-reliant treatment in developing countries. The unsupervised use of Artemisia annua tea has been criticized to foster the development of artemisinin resistance in malaria and cancer due to insufficient artemisinin amounts in the plant as compared to standardized tablets with isolated artemisinin or semisynthetic artemisinin derivatives. However, artemisinin is not the only bioactive compound in Artemisia annua. In the present investigation, we analyzed different Artemisia annua extracts. Dichloromethane extracts were more cytotoxic (range of IC₅₀: 1.8-14.4 μg/ml) than methanol extracts towards Trypanosoma b. brucei (TC221 cells). The range of IC₅₀ values for HeLa cancer cells was 54.1-275.5 μg/ml for dichloromethane extracts and 276.3-1540.8 μg/ml for methanol extracts. Cancer and trypanosomal cells did not reveal cross-resistance among other compounds of Artemisia annua, namely the artemisinin-related artemisitene and arteanuine B as well as the unrelated compounds, scopoletin and 1,8-cineole. This indicates that cells resistant to one compound retained sensitivity to another one. These results were also supported by microarray-based mRNA expression profiling showing that molecular determinants of sensitivity and resistance were different between artemisinin and the other phytochemicals investigated.

  19. Effect of Alpha-Hederin, the active constituent of Nigella sativa, on miRNA-126, IL-13 mRNA levels and inflammation of lungs in ovalbumin-sensitized male rats

    PubMed Central

    Fallahi, Maryam; Keyhanmanesh, Rana; Khamaneh, Amir Mahdi; Ebrahimi Saadatlou, Mohammad Ali; Saadat, Saeideh; Ebrahimi, Hadi

    2016-01-01

    Objective: In previous studies the therapeutic effects of Nigella sativa have been demonstrated on asthmatic animals. In the present study, the preventive effect of single dose of alpha-hederin, its active constituent, has been evaluated on lung inflammation and some inflammatory mediators in lungs of ovalbumin sensitized rat in order to elicit its mechanism. Materials and Methods: Forty rats were randomly grouped in 4 groups; control (C), sensitized (S), sensitized pretreated groups with thymoquinone (3 mg/kg i.p., S+TQ) and alpha-hederin (0.02 mg/kg i.p., S+AH). Levels of IL-13 mRNA and miRNA-126 in lung tissue and its pathological changes in each group were assessed. Results: Elevated levels of miRNA-126, IL-13 mRNA and pathological changes were observed in the sensitized group compared to the control group (p<0.001 to p<0.05). All of these factors were significantly reduced in S+TQ and S+AH groups in comparison to S group (p<0.001 to p<0.05). Although alpha-hederin decreased the levels of miRNA-126, IL-13 mRNA and pathological changes in comparison with thymoquinone, the results were statistically not significant. Conclusion: The results suggested that alpha-hederin had preventive effect on sensitized rats like thymoquinone. It may intervene in miRNA-126 expression, which consequently could interfere with IL-13 secretion pathway leading to a reduction in inflammatory responses. PMID:27247924

  20. Synthesis of Amaryllidaceae Constituents and Unnatural Derivatives.

    PubMed

    Ghavre, Mukund; Froese, Jordan; Pour, Milan; Hudlicky, Tomas

    2016-05-04

    This update covers the syntheses of Amaryllidaceae alkaloids since the publication of the last major review in 2008. A short summary of past syntheses and their step count is provided for the major constituents; pancratistatin, 7-deoxypancratistatin, narciclasine, lycoricidine, lycorine, and for other natural constituents, as well as for unnatural derivatives. Discussion of biological activities is provided for unnatural derivatives. Future prospects and further developments in this area are covered at the end of the review. The literature is covered to the end of August 2015.

  1. The cytotoxic constituents from marine-derived streptomyces 3320#

    NASA Astrophysics Data System (ADS)

    Ren, Hong; Gu, Qianqun; Cui, Chengbin; Zhu, Weiming

    2006-01-01

    The present work studies the chemical constituents from marine-derived streptomyces 3320# and their antitumor activities. The n-BuOH extract of the ferment broth of 3320# was chromatographed on silica gel, Sephadex LH-20, ODS columns and HPLC to separate the compounds with antitoumor activities. Their structures were identified using IR, UV, NMR, MS spectroscopic techniques and compared with published data. The antitumor activities of the isolates were assayed using SRB method and flow cytometry assay, accompanied with the morphological observation of the cells under light microscope against mammalian tsFT210 cells. Ten compounds, cyclo-(Ala-Leu) 1, cyclo-(Ala-Ile) 2, cyclo-(Ala-Val) 3, cyclo-(Phe- Pro) 4, cyclo-(Phe-Gly) 5, cyclo-(Leu-Pro) 6, 1-methyl-1, 2, 3, 4-tetrahydro-β-carboline-3-carboxylic acid 7, N-(4-hydroxyphenethyl) acetamide 8, 4-methyoxy-1-(2-hydroxy) ethylbenzene 9 and uridine 10, were isolated from the ferment broth of streptomyces 3320#. Among them, compounds 6, 7, 8 and 10 showed potent cytotoxicity against the tsFT210 cell with the IC50 values of 3.6, 7.2, 5.2 and 1.6 mmol L-1, respectively. Compounds 8, 10 also exhibited apoptosis inducing activity under 2.0 mmol L-1. Compounds 6, 7, 8 and 10 are the principle bioactive constituents responsible for the antitumor activities of marine streptomyces 3320#. Compound 7 was isolated from this species for the first time.

  2. Rotor Flapping Response to Active Control

    NASA Technical Reports Server (NTRS)

    Nguyen, Khanh; Johnson, Wayne

    2004-01-01

    Rotor active control using higher harmonic blade pitch has been proposed as a means to reduce both rotor radiated noise and airframe vibration and to enhance rotor performance. The higher harmonic input, however, can affect rotor thrust and cyclic flapping - the basic trim characteristics of the rotor. Some of the trim changes can negate the active control benefits. For example, wind tunnel test results of a full scale BO-105 rotor with individual-blade control indicate some rotor performance improvements, accompanied with changes in rotor trim, using two-per-rev blade pitch input. The observed performance benefits could therefore be a simple manifestation of the trim change rather than an efficient redistribution of the rotor airloads. More recently, the flight test of the BO-105 helicopter equip,ped with individual-blade-control actuators also reported trim changes whenever the two-per-rev blade pitch for noise reduction was activated. The pilot had to adjust the trim control to maintain the aircraft under a constant flight path. These two cases highlight the, importance of trim considerations in the application of active control to rotorcraft.

  3. Arctigenin but not arctiin acts as the major effective constituent of Arctium lappa L. fruit for attenuating colonic inflammatory response induced by dextran sulfate sodium in mice.

    PubMed

    Wu, Xin; Yang, Yan; Dou, Yannong; Ye, Jun; Bian, Difei; Wei, Zhifeng; Tong, Bei; Kong, Lingyi; Xia, Yufeng; Dai, Yue

    2014-12-01

    The crude powder of the fruit of Arctium lappa L. (ALF) has previously been reported to attenuate experimental colitis in mice. But, its main effective ingredient and underlying mechanisms remain to be identified. In this study, ALF was extracted with ethanol, and then successively fractionated into petroleum ether, ethyl acetate, n-butanol and water fraction. Experimental colitis was induced by dextran sulfate sodium (DSS) in mice. Among the four fractions of ALF, the ethyl acetate fraction showed the most significant inhibition of DSS-induced colitis in mice. The comparative studies of arctigenin and arctiin (the two main ingredients of ethyl acetate fraction) indicated that arctigenin rather than arctiin could reduce the loss of body weight, disease activity index and histological damage in the colon. Arctigenin markedly recovered the loss of intestinal epithelial cells (E-cadherin-positive cells) and decreased the infiltration of neutrophils (MPO-positive cells) and macrophages (CD68-positive cells). Arctigenin could down-regulate the expressions of TNF-α, IL-6, MIP-2, MCP-1, MAdCAM-1, ICAM-1 and VCAM-1 at both protein and mRNA levels in colonic tissues. Also, it markedly decreased the MDA level, but increased SOD activity and the GSH level. Of note, the efficacy of arctigenin was comparable or even superior to that of the positive control mesalazine. Moreover, it significantly suppressed the phosphorylation of MAPKs and the activation of NF-κB, including phosphorylation of IκBα and p65, p65 translocation and DNA binding activity. In conclusion, arctigenin but not arctiin is the main active ingredient of ALF for attenuating colitis via down-regulating the activation of MAPK and NF-κB pathways.

  4. Effects of Concanavalin A, fed as a constituent of Jack bean (Canavalia ensiformis L.) seeds, on the humoral immune response and performance of broiler chickens.

    PubMed

    Mendez, A; Vargas, R E; Michelangeli, C

    1998-02-01

    An experiment was conducted to investigate the effects of the lectin, Concanavalin A (Con A), contained in raw Jack bean (JB) (Canavalia ensiformis, L.) seeds on the immunological response of broilers. A maize-soybean meal basal diet was prepared to which either 2.5, 5, or 10% of ground raw Jack bean (RJB) seeds was added. The RJB seeds contained 24 g Con A/kg on a dry matter basis, as measured by rocket immunoelectrophoresis. Similar diets were prepared by using the same levels of JB after toasting at 190 C for 16 min. In addition, the basal diet was pair-fed to groups of chicks at the level of feed intake of chicks fed the 10% RJB diet. Each diet was fed to six groups of six chicks for 6 wk. At 5 wk, 15 of chicks from each diet were immunized against Brucella abortus (BA) and the anti-BA antibody titers were determined 1 wk later by ELISA. Antibody production against Con A was also measured by the same method. Binding of Con A to intestinal villi and subsequent endocytosis were confirmed by microscopic examination using a specific peroxidase-antiperoxidase-staining technique. Performance was recorded weekly. Feed intake and weight gain were reduced (P < 0.05) only by the diet containing 10% RJB, indicating that broiler chicks can tolerate daily intakes of 100 mg of Con A over 6 wk without affecting growth. Toasted JB diets supported adequate chick performance. The antibody response to BA did not differ with dietary treatment. Serum from chicks fed raw JB also contained antibodies against Con A. The bursa of Fabricius, thymus, spleen, and pancreas dry weights, as a percentage of dry body weight, were not affected by the experimental diets. The data indicated that Con A binds to the cells of the gastrointestinal tract, passes into the general circulation and, eventually, elicits an immunological response without affecting the production of antibodies to BA.

  5. Chemical constituents of fugitive dust.

    PubMed

    Van Pelt, R Scott; Zobeck, Ted M

    2007-07-01

    Wind erosion selectively winnows the fine, most chemically concentrated portions of surface soils and results in the inter-regional transport of fugitive dust containing plant nutrients, trace elements and other soil-borne contaminants. We sampled and analyzed surface soils, sediments in transport over eroding fields, and attic dust from a small area of the Southern High Plains of Texas to characterize the physical nature and chemical constituents of these materials and to investigate techniques that would allow relatively rapid, low cost techniques for estimating the chemical constituents of fugitive dust from an eroding field. From chemical analyses of actively eroding sediments, it would appear that Ca is the only chemical species that is enriched more than others during the process of fugitive dust production. We found surface soil sieved to produce a sub-sample with particle diameters in the range of 53-74 microm to be a reasonably good surrogate for fugitive dust very near the source field, that sieved sub-samples with particle diameters <10 microm have a crustal enrichment factor of approximately 6, and that this factor, multiplied by the chemical contents of source soils, may be a reasonable estimator of fugitive PM(10) chemistry from the soils of interest. We also found that dust from tractor air cleaners provided a good surrogate for dust entrained by tillage and harvesting operations if the chemical species resulting from engine wear and exhaust were removed from the data set or scaled back to the average of enrichment factors noted for chemical species with no known anthropogenic sources. Chemical analyses of dust samples collected from attics approximately 4 km from the nearest source fields indicated that anthropogenic sources of several environmentally important nutrient and trace element species are much larger contributors, by up to nearly two orders of magnitude, to atmospheric loading and subsequent deposition than fugitive dust from eroding

  6. Ionospheric Response Due to Seismic Activity

    NASA Astrophysics Data System (ADS)

    Sharma, Dinesh Kumar

    2016-07-01

    Signatures of the seismic activity in the ionospheric F2 region have been studied by analyzing the measurement of electron and ion temperatures during the occurrence of earthquake. The ionospheric electron and ion temperatures data recorded by the RPA payload aboard the Indian SROSS-C2 satellite during the period from January 1995 to December 2000 were used for the altitude range 430-630 km over Indian region. The normal day's electron and ion temperatures have been compared to the temperatures recorded during the seismic activity. The details of seismic events were obtained from USGS earthquake data information website. It has been found that the average electron temperature is enhanced during the occurrence of earthquakes by 1.2 to 1.5 times and this enhancement was for ion temperature ranging from 1.1to 1.3 times over the normal day's average temperatures. The above careful quantitative analysis of ionospheric electron and ion temperatures data shows the consistent enhancement in the ionospheric electron and ion temperatures. It is expected that the seismogenic vertical electrical field propagates up to the ionospheric heights and induces Joule heating that may cause the enhancement in ionospheric temperatures.

  7. Comparison of two extraction methods for evaluation of volatile constituents patterns in commercial whiskeys Elucidation of the main odour-active compounds.

    PubMed

    Caldeira, M; Rodrigues, F; Perestrelo, R; Marques, J C; Câmara, J S

    2007-11-15

    An analytical procedure based on manual dynamic headspace solid-phase microextraction (HS-SPME) method and the conventional extraction method by liquid-liquid extraction (LLE), were compared for their effectiveness in the extraction and quantification of volatile compounds from commercial whiskey samples. Seven extraction solvents covering a wide range of polarities and two SPME fibres coatings, has been evaluated. The highest amounts extracted, were achieved using dichloromethane (CH2Cl2) by LLE method (LLE(CH2Cl2)) and using a CAR/PDMS fibre (SPME(CAR/PDMS)) in HS-SPME. Each method was used to determine the responses of 25 analytes from whiskeys and calibration standards, in order to provide sensitivity comparisons between the two methods. Calibration curves were established in a synthetic whiskey and linear correlation coefficient (r) were greater than 0.9929 for LLE(CH2Cl2) and 0.9935 for SPME(CAR/PDMS), for all target compounds. Recoveries greater than 80% were achieved. For most compounds, precision (expressed by relative standard deviation, R.S.D.) are very good, with R.S.D. values lower than 14.78% for HS-SPME method and than 19.42% for LLE method. The detection limits ranged from 0.13 to 19.03 microg L(-1) for SPME procedure and from 0.50 to 12.48 microg L(-1) for LLE. A tentative study to estimate the contribution of a specific compound to the aroma of a whiskey, on the basis of their odour activity values (OAV) was made. Ethyl octanoate followed by isoamyl acetate and isobutyl alcohol, were found the most potent odour-active compounds.

  8. Enzyme activity control by responsive redoxpolymers.

    PubMed

    Nagel, Birgit; Warsinke, Axel; Katterle, Martin

    2007-06-05

    A new thermoresponsive poly-N-isopropylacrylamide (PNIPAM)-ferrocene polymer was synthesized and characterized. PNIPAMFoxy bears additional oxirane groups which were used for attachment by a self-assembly process on a cysteamine-modified gold electrode to create a thin hydrophilic film. The new redox polymer enabled electrical communication between the cofactor pyrrolinoquinoline quinone (PQQ) of soluble glucose dehydrogenase (sGDH) and the electrode for sensitive detection of this enzyme as a prospective protein label. The temperature influence on the redox polymer/enzyme complex was investigated. An inverse temperature response behavior of surface bound PNIPAMFoxy compared to the soluble polymer was found and is discussed in detail. The highest efficiency of mediated electron transfer for the immobilized PNIPAMFoxy with sGDH was observed at 24 degrees C, which was twice as high as that of its soluble counterpart. A steady-state electrooxidation current densitiy of 4.5 microA.cm-2 was observed in the presence of 10 nM sGDH and 5 mM glucose. A detection limit of 0.5 nM of soluble PQQ-sGDH was obtained.

  9. Motor cortex activity predicts response alternation during sensorimotor decisions

    PubMed Central

    Pape, Anna-Antonia; Siegel, Markus

    2016-01-01

    Our actions are constantly guided by decisions based on sensory information. The motor cortex is traditionally viewed as the final output stage in this process, merely executing motor responses based on these decisions. However, it is not clear if, beyond this role, the motor cortex itself impacts response selection. Here, we report activity fluctuations over motor cortex measured using MEG, which are unrelated to choice content and predict responses to a visuomotor task seconds before decisions are made. These fluctuations are strongly influenced by the previous trial's response and predict a tendency to switch between response alternatives for consecutive decisions. This alternation behaviour depends on the size of neural signals still present from the previous response. Our results uncover a response-alternation bias in sensorimotor decision making. Furthermore, they suggest that motor cortex is more than an output stage and instead shapes response selection during sensorimotor decision making. PMID:27713396

  10. New Benzo[c]phenanthridine and Benzenoid Derivatives, and Other Constituents from Zanthoxylum ailanthoides: Effects on Neutrophil Pro-Inflammatory Responses

    PubMed Central

    Chung, Ching-Yi; Hwang, Tsong-Long; Kuo, Liang-Mou; Kuo, Wen-Lung; Cheng, Ming-Jen; Wu, Yi-Hsiu; Sung, Ping-Jyun; Chung, Mei-Ing; Chen, Jih-Jung

    2013-01-01

    A new benzo[c]phenanthridine, oxynorchelerythrine (1), and two new benzenoid derivatives, methyl 4-(2-hydroxy-4-methoxy-3-methyl-4-oxobutoxy)benzoate (2) and (E)-methyl 4-(4-((Z)-3-methoxy-3-oxoprop-1-enyl)phenoxy)-2-methylbut-2-enoate (3), have been isolated from the twigs of Zanthoxylum ailanthoides, together with 11 known compounds (4–14). The structures of these new compounds were determined through spectroscopic and MS analyses. Among the isolated compounds, decarine (4), (−)-syringaresinol (6), (+)-episesamin (8), glaberide I (9), (−)-dihydrocubebin (10), and xanthyletin (11) exhibited potent inhibition (IC50 values ≤ 4.79 μg/mL) of superoxide anion generation by human nutrophils in response to N-formyl-l-methionyl-l-leucyl-l-phenylalanine/cytochalasin B (fMLP/CB). Compounds 4, 8, and 11 also inhibited fMLP/CB-induced elastase release with IC50 values ≤ 5.48 μg/mL. PMID:24232457

  11. Cell wall protein and glycoprotein constituents of Aspergillus fumigatus that bind to polystyrene may be responsible for the cell surface hydrophobicity of the mycelium.

    PubMed

    Peñalver, M C; Casanova, M; Martínez, J P; Gil, M L

    1996-07-01

    Cell surface hydrophobicity (CSH) of Aspergillus fumigatus grown both in complex medium (yeast extract/peptone/dextrose; YPD) and minimal (Vogel's N) medium was monitored by assessing attachment of polystyrene microspheres to the cell surface. It was found that mature mycelium was hydrophobic. Treatment of intact mycelium with beta-mercaptoethanol (beta ME) abolished binding of the microspheres to hyphal elements, and coating of the microspheres with beta ME extracts from mycelium inhibited their attachment to intact mycelial cells. A. fumigatus mycelium was tagged in vivo with biotin and treated with beta ME. The beta ME extracts were analysed by SDS-PAGE and Western blotting with both peroxidase-conjugated-ExtrAvidin and concanavalin A (ConA). This procedure allowed identification of cell wall surface proteins and glycoproteins. Rabbit polyclonal antisera were raised against beta ME extracts obtained from cells grown in YPD and Vogel's N media. These antisera defined some major cell-wall-bound antigens. SDS-PAGE and Western blotting analysis of the cell wall material released by beta ME and adsorbed on polystyrene microspheres revealed about 19 protein species with apparent molecular masses ranging from 20 to 70 kDa, and two high-molecular-mass glycoproteins of 115 and 210 kDa. Treatment of cells grown in YPD, but not those grown in Vogel's N medium, with beta ME released a 55 kDa polypeptide able to adsorb to polystyrene microspheres that was detectable with the antisera. The ability to bind to polystyrene particles exhibited by several protein and glycoprotein species released by beta ME treatment suggested that these cell wall moieties possess exposed hydrophobic domains that could be responsible for the CSH of mycelium.

  12. Response-restriction analysis: II. Alteration of activity preferences.

    PubMed Central

    Hanley, Gregory P; Iwata, Brian A; Roscoe, Eileen M; Thompson, Rachel H; Lindberg, Jana S

    2003-01-01

    We used response-restriction (RR) assessments to identify the preferences of 7 individuals with mental retardation for a variety of vocational and leisure activities. We subsequently increased their engagement in nonpreferred activities using several procedures: response restriction per se versus a Premack-type contingency (Study 1), supplemental reinforcement for engagement in target activities (Study 2), and noncontingent pairing of reinforcers with nonpreferred activities (Study 3). Results indicated that preferences are not immutable and can be altered through a variety of relatively benign interventions and that the results of RR assessments may be helpful in determining which types of procedures may be most effective on an individual basis. PMID:12723867

  13. An Active Metamaterial Platform for Chiral Responsive Optoelectronics.

    PubMed

    Kang, Lei; Lan, Shoufeng; Cui, Yonghao; Rodrigues, Sean P; Liu, Yongmin; Werner, Douglas H; Cai, Wenshan

    2015-08-05

    Chiral-selective non-linear optics and optoelectronic signal generation are demonstrated in an electrically active photonic metamaterial. The metamaterial reveals significant chiroptical responses in both harmonic generation and the photon drag effect, correlated to the resonance behavior in the linear regime. The multifunctional chiral metamaterial with dual electrical and optical functionality enables transduction of chiroptical responses to electrical signals for integrated photonics.

  14. Pythium infection activates conserved plant defense responses in mosses

    Technology Transfer Automated Retrieval System (TEKTRAN)

    The moss Physcomitrella patens (P. patens) is a useful model to study abiotic stress responses since it is highly tolerant to drought, salt and osmotic stress. However, little is known about the defense mechanisms activated in this moss after pathogen assault. Here the induction of defense responses...

  15. 78 FR 68053 - Agency Information Collection Activities OMB Responses

    Federal Register 2010, 2011, 2012, 2013, 2014

    2013-11-13

    ... From the Federal Register Online via the Government Publishing Office ENVIRONMENTAL PROTECTION AGENCY Agency Information Collection Activities OMB Responses AGENCY: Environmental Protection Agency...) responses to Agency Clearance requests, in compliance with the Paperwork Reduction Act (44 U.S.C. 3501...

  16. Acoustic cues to Nehiyawewin constituency

    NASA Astrophysics Data System (ADS)

    Cook, Clare; Muehlbauer, Jeff

    2005-04-01

    This study examines how speakers use acoustic cues, e.g., pitch and pausing, to establish syntactic and semantic constituents in Nehiyawewin, an Algonquian language. Two Nehiyawewin speakers autobiographies, which have been recorded, transcribed, and translated by H. C. Wolfart in collaboration with a native speaker of Nehiyawewin, provide natural-speech data for the study. Since it is difficult for a non-native-speaker to reliably distinguish Nehiyawewin constituents, an intermediary is needed. The transcription provides this intermediary through punctuation marks (commas, semi-colons, em-dashes, periods), which have been shown to consistently mark constituency structure [Nunberg, CSLI 1990]. The acoustic cues are thus mapped onto the punctuated constituents, and then similar constituents are compared to see what acoustic cues they share. Preliminarily, the clearest acoustic signal to a constituent boundary is a pitch drop preceding the boundary and/or a pitch reset on the syllable following the boundary. Further, constituent boundaries marked by a period consistently end on a low pitch, are followed by a pitch reset of 30-90 Hz and have an average pause of 1.9 seconds. I also discuss cross-speaker cues, and prosodic cues that do not correlate to punctuation, with implications for the transcriptional view of orthography [Marckwardt, Oxford 1942].

  17. Identification of mosquito biting deterrent constituents from the Indian folk remedy plant Jatropha curcas.

    PubMed

    Cantrell, Charles L; Ali, Abbas; Duke, Stephen O; Khan, Ikhlas

    2011-07-01

    An investigation of the Indian folk remedy plant Jatropha curcas L., was performed to identify the constituents responsible for the mosquito biting deterrent activity of the oil. J. curcas seed oil is burned in oil lamps in India and parts of Africa to repel biting insects, primarily mosquitoes. The seed oil was thoroughly analyzed by 1H NMR, 13C NMR, high-performance liquid chromatography-refractive index, and gas chromatography-flame ionization detection to identify the constituents in the oil. Identified constituents, both free fatty acids and triglycerides, were evaluated for activity in Aedes aegypti (L.) (Diptera: Culicidae) biting deterrent assays. Furthermore, an oil condensation trap was used to demonstrate that free fatty acids or triglycerides are partially volatilized during the combustion process. These compounds were found to be responsible for the biting deterrency of the burned oil. Specifically, oleic, palmitic, linoleic, and stearic acids were all active at 25 nmol/cm2 above that of solvent control in Ae. aegypti biting deterrent assays. Oleic, palmitic, and linoleic acids were all more active than stearic acid in the same bioassay. Evaluation of the triglycerides containing each of these fatty acids revealed that tripalmitin, tristearin, trilinolein, and triolein all demonstrated significant activity above a solvent control at 10 microg/cm2, whereas tripalmitin was the most active. Due to literature reports suggesting larvicidal activity of the oil, J. curcas seed oil and its free fatty acid constituents also were evaluated against 1-d-old Ae. aegypti larvae up to 500 ppm. Oleic acid was the only fatty acid having larvicidal activity against 1-d-old Ae. aegypti larvae, with an LD50 of 47.9 ppm.

  18. Anti-Tumor Action, Clinical Biochemistry Profile and Phytochemical Constituents of a Pharmacologically Active Fraction of S. crispus in NMU-Induced Rat Mammary Tumour Model.

    PubMed

    Yaacob, Nik Soriani; Yankuzo, Hassan Muhammad; Devaraj, Sutha; Wong, Jimmy Ka Ming; Lai, Choon-Sheen

    2015-01-01

    Cancer patients seek alternative remedies such as traditional medicinal plants for safe and effective treatment and help overcome the side effects of conventional therapy. Current knowledge indicates that extracts of Strobilanthes crispus of the Acanthaceae family exhibit potent anticancer properties in vitro and are non-toxic in vivo. S. crispus was also reported to be protective against chemical hepatocarcinogenesis. We previously showed that a bioactive fraction of S. crispus leaves also synergized with tamoxifen to cause apoptosis of human breast cancer cell lines without damaging non-malignant epithelial cells. The present study aimed to evaluate the antitumor effect of S. crispus dichloromethane fraction (F3) using N-methyl-N-Nitrosourea (NMU)-induced rat mammary tumor model. Tumor regression was observed in 75% of the rats following 8-week oral administration of F3 with no secondary tumour formation and no signs of anemia or infection. However, no improvement in the liver and renal function profiles was observed. Major constituents of F3 were identified as lutein, 131-hydroxy-132-oxo-pheophytin a, campesterol, stigmasterol, β-sitosterol, pheophytin a and 132-hydroxy-pheophytin a. These compounds however, may not significantly contribute to the antitumor effect of F3.

  19. Anti-Tumor Action, Clinical Biochemistry Profile and Phytochemical Constituents of a Pharmacologically Active Fraction of S. crispus in NMU-Induced Rat Mammary Tumour Model

    PubMed Central

    Yaacob, Nik Soriani; Yankuzo, Hassan Muhammad; Devaraj, Sutha; Wong, Jimmy Ka Ming; Lai, Choon-Sheen

    2015-01-01

    Cancer patients seek alternative remedies such as traditional medicinal plants for safe and effective treatment and help overcome the side effects of conventional therapy. Current knowledge indicates that extracts of Strobilanthes crispus of the Acanthaceae family exhibit potent anticancer properties in vitro and are non-toxic in vivo. S. crispus was also reported to be protective against chemical hepatocarcinogenesis. We previously showed that a bioactive fraction of S. crispus leaves also synergized with tamoxifen to cause apoptosis of human breast cancer cell lines without damaging non-malignant epithelial cells. The present study aimed to evaluate the antitumor effect of S. crispus dichloromethane fraction (F3) using N-methyl-N-Nitrosourea (NMU)-induced rat mammary tumor model. Tumor regression was observed in 75% of the rats following 8-week oral administration of F3 with no secondary tumour formation and no signs of anemia or infection. However, no improvement in the liver and renal function profiles was observed. Major constituents of F3 were identified as lutein, 131-hydroxy-132-oxo-pheophytin a, campesterol, stigmasterol, β-sitosterol, pheophytin a and 132-hydroxy-pheophytin a. These compounds however, may not significantly contribute to the antitumor effect of F3. PMID:26000968

  20. Chemical composition and acaricidal activity of the essential oil of Baccharis dracunculifolia De Candole (1836) and its constituents nerolidol and limonene on larvae and engorged females of Rhipicephalus microplus (Acari: Ixodidae).

    PubMed

    de Assis Lage, Tiago Coelho; Montanari, Ricardo Marques; Fernandes, Sergio Antonio; de Oliveira Monteiro, Caio Márcio; de Oliveira Souza Senra, Tatiane; Zeringota, Viviane; da Silva Matos, Renata; Daemon, Erik

    2015-01-01

    Baccharis dracunculifolia DC (common name "alecrim-do-campo" in Brazil) is a plant with widespread distribution in South America that is the botanical origin of green propolis. The aim of this study was to evaluate the chemical composition and acaricidal activity of the essential oil of B. dracunculifolia and its constituents nerolidol and limonene on unengorged larvae and engorged females of Rhipicephalus microplus (Acari: Ixodidae). The essential oil yield was 0.8% of dry mass and the major constituents were nerolidol (22.3%), germacrene D (7.2%), limonene (6.9%), β-pinene (6.7) and bicyclogermacrene (6.5%). The acaricidal activity of the essential oil and the pure compounds nerolidol and (R)-(+)-limonene were assessed in the laboratory through the modified larval packet test (LPT) and the female immersion test (FIT). In the LPT, the essential oil and nerolidol were both active, causing more than 90% mortality at concentrations from 15.0 and 10.0 mg mL(-1), respectively, whereas (R)-(+)-limonene was not active. In the FIT, the oil and nerolidol caused reduction in the quantity and quality of eggs produced, with control percentages of 96.3% and 90.3% at concentrations of 60.0 and 50.0 mg mL(-1), respectively. It can be concluded that the essential oil obtained from the aerial parts of B. dracunculifolia and its major component nerolidol have high activity on R. microplus larvae and engorged females.

  1. Activated oxygen alters cerebral microvascular responses in newborn pigs

    SciTech Connect

    Leffler, C.W.; Busiia, D.W.; Armstead, W.M.; Mirro, R.; Thelin, O. )

    1990-02-26

    In piglets, cerebral ischemia/reperfusion blocks prostanoid dependent cerebral vasodilation to hypercapnia (CO{sub 2}) and hypotension but not prostanoid independent dilation to isoproterenol (Isu) or constriction to norepinephrine (NE). Ischemia/reperfusion increases activated-O{sub 2} production by piglet brains. Using cranial windows in piglets, the authors investigated the hypothesis that activated oxygen can block prostanoid dependent cerebral vasodilator responses to CO{sub 2} and hypotension without altering responses to Isu and NE. Exposure to an activated oxygen generating system of xanthine oxidase, hypoxanthine, and Fe that made about 3 times the activated-O{sub 2} on the brain surface as ischemia/reperfusion caused reversible pial arteriolar dilation. After exposure, pial arteriolar dilation was reduced to CO{sub 2} and hypotension but not to Isu. NE constrictor responses were also unaltered. H{sub 2}O{sub 2} or H{sub 2}O{sub 2} + Fe caused constriction followed by reversible dilation. After exposure, pial arteriolar dilation in response to CO{sub 2} and hypotension was not altered. However, addition of xanthine oxidase and hypoxanthine with H{sub 2}O{sub 2} and Fe totally eliminated pial arteriolar dilator responses to CO{sub 2} and hypotension but did not decrease dilation caused by Isu or constriction caused by NE. The authors conclude that activated oxygen could produce the altered prostanoid dependent pial arteriolar responses observed following ischemia in piglets.

  2. Identification of methysticin as a potent and non-toxic NF-kappaB inhibitor from kava, potentially responsible for kava's chemopreventive activity.

    PubMed

    Shaik, Ahmad Ali; Hermanson, David Lee; Xing, Chengguo

    2009-10-01

    Nuclear factor-kappaB (NF-kappaB) is a transcription factor that plays an essential role in cancer development. The results of our recent chemopreventive study demonstrate that kava, a beverage in the South Pacific Islands, suppresses NF-kappaB activation in lung adenoma tissues, potentially a mechanism responsible for kava's chemopreventive activity. Methysticin is identified as a potent NF-kappaB inhibitor in kava with minimum toxicity. Other kava constituents, including four kavalactones of similar structures to methysticin, demonstrate minimum activities in inhibiting NF-kappaB.

  3. Atmospheric Constituent Explorer System (ACES)

    NASA Astrophysics Data System (ADS)

    Darrach, M. R.; Madzunkov, S.; Neidholdt, E.; Simcic, J.

    2016-10-01

    We report on the Atmospheric Constituent Explorer System (ACES), a mass spectrometer based instrument for atmospheric probe missions (e.g. Venus and ice giant) that can determine abundances and isotopic ratios of the noble-gases and trace species.

  4. Larvicidal constituents of Zingiber officinale (ginger) against Anisakis simplex.

    PubMed

    Lin, Rong-Jyh; Chen, Chung-Yi; Lee, June-Der; Lu, Chin-Mei; Chung, Li-Yu; Yen, Chuan-Min

    2010-11-01

    In this study, we investigated the anthelmintic activity of [10]-shogaol, [6]-shogaol, [10]-gingerol and [6]-gingerol, compounds isolated from the roots of Zingiber officinale L., Zingiberaceae (ginger), against Anisakis simplex. The above compounds kill or reduce spontaneous movement in A. simplex larvae. The maximum lethal efficacy of [10]-shogaol and [10]-gingerol was approximately 80% and 100%, respectively. We further examined the time course of compound-induced loss of mobility in A. simplex. The results showed that various concentrations of [10]-shogaol, [6]-shogaol, [10]-gingerol and [6]-gingerol have maximum effects on loss of spontaneous movement from 24 to 72 h. In addition, the time course of mortality and the percentage of loss of spontaneous movements were ascertained to determine the minimum effective doses of [10]-gingerol and [10]-shogaol. [10]-Gingerol exhibited a larger maximum larvicidal effect and greater loss of spontaneous movement than [10]-shogaol and albendazole. In addition, these constituents of Zingiber officinale showed effects against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and peroxyl radicals. These constituents of Zingiber officinale are responsible for its larvicidal activity against A. simplex.

  5. Presence of cholinergic and calcium antagonist constituents in Saussurea lappa explains its use in constipation and spasm.

    PubMed

    Gilani, Anwar H; Shah, Abdul J; Yaeesh, S

    2007-06-01

    This study was carried out to provide a scientific basis for the traditional use of Saussurea lappa, in constipation and spasms. Isolated tissue preparations were used to see if the aqueous-methanol crude extract of the S. lappa root (Sl.Cr) contains gut stimulatory and inhibitory constituents. In isolated guinea-pig ileum, a quiescent preparation, Sl.Cr caused a concentration-dependent (0.3-5.0 mg/mL) spasmogenic effect, with the maximum effect reaching 91% of the acetylcholine maximum. A further increase in concentration caused a declining effect, indicating the presence of spasmolytic constituent(s). The spasmolytic effect was more marked in the spontaneously contracting rabbit jejunum and in the atropinized preparations. The spasmolytic effect was mediated through calcium channel blocking (CCB) activity, as evident by its inhibitory effect against high K(+) (80 mm)-induced contraction and displacement of the Ca(++) concentration-response curves to the right. These data indicate that the crude extract of Sl.Cr contains gut stimulatory constituent(s) of cholinergic-type providing a scientific basis for its use in constipation. The presence of spasmolytic constituents of CCB-type more evident in the spontaneous contracting gut preparation may explain its use in spasms.

  6. Screening of Panamanian Plants for Cosmetic Properties, and HPLC-Based Identification of Constituents with Antioxidant and UV-B Protecting Activities

    PubMed Central

    Guldbrandsen, Niels; De Mieri, Maria; Gupta, Mahabir; Liakou, Eleni; Pratsinis, Harris; Kletsas, Dimitris; Chaita, Eliza; Aligiannis, Nektarios; Skaltsounis, Alexios-Leandros; Hamburger, Matthias

    2015-01-01

    A library of 600 taxonomically diverse Panamanian plant extracts was screened for DPPH scavenging and UV-B protective activities, and the methanolic extracts of Mosquitoxylum jamaicense, Combretum cacoucia, and Casearia commersionia were submitted to HPLC-based activity profiling. The compounds located in the active time windows were isolated and identified as gallic acid derivatives and flavonoids. Gallic acid methyl ester (3) and digallic acid derivatives (2, 6) showed the highest DPPH scavenging activity (<10 μg/mL), while protocatechuic acid (7) and isoquercitrin (10) exhibited the highest UV-B protective properties. PMID:26839809

  7. Asymmetric frontal cortical activity and negative affective responses to ostracism.

    PubMed

    Peterson, Carly K; Gravens, Laura C; Harmon-Jones, Eddie

    2011-06-01

    Ostracism arouses negative affect. However, little is known about variables that influence the intensity of these negative affective responses. Two studies fill this void by incorporating work on approach- and withdrawal-related emotional states and their associated cortical activations. Study 1 found that following ostracism anger related directly to relative left frontal cortical activation. Study 2 used unilateral hand contractions to manipulate frontal cortical activity prior to an ostracizing event. Right-hand contractions, compared to left-hand contractions, caused greater relative left frontal cortical activation during the hand contractions as well as ostracism. Also, right-hand contractions caused more self-reported anger in response to being ostracized. Within-condition correlations revealed patterns of associations between ostracism-induced frontal asymmetry and emotive responses to ostracism consistent with Study 1. Taken together, these results suggest that asymmetrical frontal cortical activity is related to angry responses to ostracism, with greater relative left frontal cortical activity being associated with increased anger.

  8. Chemical constituents and bioactivities of Panax ginseng (C. A. Mey.).

    PubMed

    Ru, Wenwen; Wang, Dongliang; Xu, Yunpeng; He, Xianxian; Sun, Yang-En; Qian, Liyan; Zhou, Xiangshan; Qin, Yufeng

    2015-02-01

    Ginseng, Panax ginseng (C. A. Mey.), is a well-known Chinese traditional medicine in the Far East and has gained popularity in the West during the last decade. There is extensive literature on the chemical constituents and bioactivities of ginseng. In this paper we compiled the chemical constituents isolated and detected from ginseng including polysaccharides, ginsenosides, peptides, polyacetylenic alcohols, fatty acids, etc. Meanwhile we summarized the biological activities of ginseng, which have been reported over the past few decades, including: anti-aging activity, anti-diabetic activity, immunoregulatory activity, anti-cancer activity, neuroregulation activity, wound and ulcer healing activity, etc. Nevertheless, further studies to exploit other kinds of constituents and new biological activities of ginseng are still necessary to facilitate research and development in the future.

  9. 20 CFR 665.300 - What are rapid response activities and who is responsible for providing them?

    Code of Federal Regulations, 2010 CFR

    2010-04-01

    ... 20 Employees' Benefits 3 2010-04-01 2010-04-01 false What are rapid response activities and who is responsible for providing them? 665.300 Section 665.300 Employees' Benefits EMPLOYMENT AND TRAINING... INVESTMENT ACT Rapid Response Activities § 665.300 What are rapid response activities and who is...

  10. 20 CFR 665.300 - What are rapid response activities and who is responsible for providing them?

    Code of Federal Regulations, 2014 CFR

    2014-04-01

    ... 20 Employees' Benefits 4 2014-04-01 2014-04-01 false What are rapid response activities and who is responsible for providing them? 665.300 Section 665.300 Employees' Benefits EMPLOYMENT AND TRAINING... WORKFORCE INVESTMENT ACT Rapid Response Activities § 665.300 What are rapid response activities and who...

  11. Reward anticipation enhances brain activation during response inhibition.

    PubMed

    Rosell-Negre, Patricia; Bustamante, Juan Carlos; Fuentes-Claramonte, Paola; Costumero, Víctor; Benabarre, Sergio; Barros-Loscertales, Alfonso

    2014-06-01

    The chance to achieve a reward starts up the required neurobehavioral mechanisms to adapt our thoughts and actions in order to accomplish our objective. However, reward does not equally reinforce everybody but depends on interindividual motivational dispositions. Thus, immediate reward contingencies can modulate the cognitive process required for goal achievement, while individual differences in personality can affect this modulation. We aimed to test the interaction between inhibition-related brain response and motivational processing in a stop signal task by reward anticipation and whether individual differences in sensitivity to reward (SR) modulate such interaction. We analyzed the cognitive-motivational interaction between the brain pattern activation of the regions involved in correct and incorrect response inhibition and the association between such brain activations and SR scores. We also analyzed the behavioral effects of reward on both reaction times for the "go" trials before and after correct and incorrect inhibition in order to test error prediction performance and postinhibition adjustment. Our results show enhanced activation during response inhibition under reward contingencies in frontal, parietal, and subcortical areas. Moreover, activation of the right insula and the left putamen positively correlates with the SR scores. Finally, the possibility of reward outcome affects not only response inhibition performance (e.g., reducing stop signal reaction time), but also error prediction performance and postinhibition adjustment. Therefore, reward contingencies improve behavioral performance and enhance brain activation during response inhibition, and SR is related to brain activation. Our results suggest the conditions and factors that subserve cognitive control strategies in cognitive motivational interactions during response inhibition.

  12. Baseline Brain Activity Predicts Response to Neuromodulatory Pain Treatment

    PubMed Central

    Jensen, Mark P.; Sherlin, Leslie H.; Fregni, Felipe; Gianas, Ann; Howe, Jon D.; Hakimian, Shahin

    2015-01-01

    Objectives The objective of this study was to examine the associations between baseline electroencephalogram (EEG)-assessed brain oscillations and subsequent response to four neuromodulatory treatments. Based on available research, we hypothesized that baseline theta oscillations would prospectively predict response to hypnotic analgesia. Analyses involving other oscillations and the other treatments (meditation, neurofeedback, and both active and sham transcranial direct current stimulation) were viewed as exploratory, given the lack of previous research examining brain oscillations as predictors of response to these other treatments. Design Randomized controlled study of single sessions of four neuromodulatory pain treatments and a control procedure. Methods Thirty individuals with spinal cord injury and chronic pain had their EEG recorded before each session of four active treatments (hypnosis, meditation, EEG biofeedback, transcranial direct current stimulation) and a control procedure (sham transcranial direct stimulation). Results As hypothesized, more presession theta power was associated with greater response to hypnotic analgesia. In exploratory analyses, we found that less baseline alpha power predicted pain reduction with meditation. Conclusions The findings support the idea that different patients respond to different pain treatments and that between-person treatment response differences are related to brain states as measured by EEG. The results have implications for the possibility of enhancing pain treatment response by either 1) better patient/treatment matching or 2) influencing brain activity before treatment is initiated in order to prepare patients to respond. Research is needed to replicate and confirm the findings in additional samples of individuals with chronic pain. PMID:25287554

  13. Instruction-based response activation depends on task preparation.

    PubMed

    Liefooghe, Baptist; De Houwer, Jan; Wenke, Dorit

    2013-06-01

    An increasing number of studies have demonstrated that a response in one task can be activated automatically on the basis merely of instructed stimulus-response (S-R) mappings belonging to another task. Such instruction-based response activations are considered to be evidence for the formation of S-R associations on the basis of the S-R mappings for an upcoming, but not yet executed, task. A crucial but somewhat neglected assumption is that instructed S-R associations are formed only under conditions that impose a sufficient degree of task preparation. Accordingly, in the present study we investigated the relation between task preparation and the instruction-based task-rule congruency effect, which is an index of response activation on the basis of instructions. The results from two experiments demonstrated that merely instructed S-R mappings of a particular task only elicit instruction-based response activations when that task is prepared for to a sufficient degree. Implications are discussed for the representation of instructed S-R mappings in working memory.

  14. Patterning of sympathetic nerve activity in response to vestibular stimulation

    NASA Technical Reports Server (NTRS)

    Kerman, I. A.; McAllen, R. M.; Yates, B. J.

    2000-01-01

    Growing evidence suggests a role for the vestibular system in regulation of autonomic outflow during postural adjustments. In the present paper we review evidence for the patterning of sympathetic nerve activity elicited by vestibular stimulation. In response to electrical activation of vestibular afferents, firing of sympathetic nerves located throughout the body is altered. However, activity of the renal nerve is most sensitive to vestibular inputs. In contrast, high-intensity simultaneous activation of cutaneous and muscle inputs elicits equivalent changes in firing of the renal, superior mesenteric and lumbar colonic nerves. Responses of muscle vasoconstrictor (MVC) efferents to vestibular stimulation are either inhibitory (Type I) or are comprised of a combination of excitation and inhibition (Type II). Interestingly, single MVC units located in the hindlimb exhibited predominantly Type I responses while those located in the forelimb and face exhibited Type II responses. Furthermore, brachial and femoral arterial blood flows were dissociated in response to vestibular stimulation, such that brachial vascular resistance increased while femoral resistance decreased. These studies demonstrate that vestibulosympathetic reflexes are patterned according to both the anatomical location and innervation target of a particular sympathetic nerve, and can lead to distinct changes in local blood flow.

  15. Veratri Nigri Rhizoma et Radix (Veratrum nigrum L.) and Its Constituent Jervine Prevent Adipogenesis via Activation of the LKB1-AMPKα-ACC Axis In Vivo and In Vitro

    PubMed Central

    Park, Jinbong; Jeon, Yong-Deok; Kim, Hye-Lin; Kim, Dae-Seung; Han, Yo-Han; Jung, Yunu; Youn, Dong-Hyun; Kang, JongWook; Yoon, Daeyeon; Jeong, Mi-Young; Lee, Jong-Hyun; Hong, Seung-Heon; Lee, Junhee; Um, Jae-Young

    2016-01-01

    This study was performed in order to investigate the antiobese effects of the ethanolic extract of Veratri Nigri Rhizoma et Radix (VN), a herb with limited usage, due to its toxicology. An HPLC analysis identified jervine as a constituent of VN. By an Oil Red O assay and a Real-Time RT-PCR assay, VN showed higher antiadipogenic effects than jervine. In high-fat diet- (HFD-) induced obese C57BL/6J mice, VN administration suppressed body weight gain. The levels of peroxisome proliferator-activated receptor gamma (PPARγ), CCAAT-enhancer-binding protein alpha (C/EBPα), adipocyte fatty-acid-binding protein (aP2), adiponectin, resistin, and LIPIN1 were suppressed by VN, while SIRT1 was upregulated. Furthermore, VN activated phosphorylation of the liver kinase B1- (LKB1-) AMP-activated protein kinase alpha- (AMPKα-) acetyl CoA carboxylase (ACC) axis. Further investigation of cotreatment of VN with the AMPK agonist AICAR or AMPK inhibitor Compound C showed that VN can activate the phosphorylation of AMPKα in compensation to the inhibition of Compound C. In conclusion, VN shows antiobesity effects in HFD-induced obese C57BL/6J mice. In 3T3-L1 adipocytes, VN has antiadipogenic features, which is due to activating the LKB1-AMPKα-ACC axis. These results suggest that VN has a potential benefit in preventing obesity. PMID:27143989

  16. Veratri Nigri Rhizoma et Radix (Veratrum nigrum L.) and Its Constituent Jervine Prevent Adipogenesis via Activation of the LKB1-AMPKα-ACC Axis In Vivo and In Vitro.

    PubMed

    Park, Jinbong; Jeon, Yong-Deok; Kim, Hye-Lin; Kim, Dae-Seung; Han, Yo-Han; Jung, Yunu; Youn, Dong-Hyun; Kang, JongWook; Yoon, Daeyeon; Jeong, Mi-Young; Lee, Jong-Hyun; Hong, Seung-Heon; Lee, Junhee; Um, Jae-Young

    2016-01-01

    This study was performed in order to investigate the antiobese effects of the ethanolic extract of Veratri Nigri Rhizoma et Radix (VN), a herb with limited usage, due to its toxicology. An HPLC analysis identified jervine as a constituent of VN. By an Oil Red O assay and a Real-Time RT-PCR assay, VN showed higher antiadipogenic effects than jervine. In high-fat diet- (HFD-) induced obese C57BL/6J mice, VN administration suppressed body weight gain. The levels of peroxisome proliferator-activated receptor gamma (PPARγ), CCAAT-enhancer-binding protein alpha (C/EBPα), adipocyte fatty-acid-binding protein (aP2), adiponectin, resistin, and LIPIN1 were suppressed by VN, while SIRT1 was upregulated. Furthermore, VN activated phosphorylation of the liver kinase B1- (LKB1-) AMP-activated protein kinase alpha- (AMPKα-) acetyl CoA carboxylase (ACC) axis. Further investigation of cotreatment of VN with the AMPK agonist AICAR or AMPK inhibitor Compound C showed that VN can activate the phosphorylation of AMPKα in compensation to the inhibition of Compound C. In conclusion, VN shows antiobesity effects in HFD-induced obese C57BL/6J mice. In 3T3-L1 adipocytes, VN has antiadipogenic features, which is due to activating the LKB1-AMPKα-ACC axis. These results suggest that VN has a potential benefit in preventing obesity.

  17. Water-quality assessment of the Delmarva Peninsula, Delaware, Maryland, and Virginia; effects of agricultural activities on, and distribution of, nitrate and other inorganic constituents in the surficial aquifer

    USGS Publications Warehouse

    Hamilton, P.A.; Denver, J.M.; Phillips, P.J.; Shedlock, R.J.

    1993-01-01

    Agricultural applications of inorganic fertilizers and manure have changed the natural chemical com- position of water in the surficial aquifer through- out the Delmarva Peninsula. Nitrate, derived from nitrification of ammonia in inorganic fertilizers and manure, is the dominant anion in agricultural areas. Concentrations of nitrate in 185 water samples collected in agricultural areas ranged from 0.4 to 48 mg/L as nitrogen, with a median concen- tration of 8.2 mg/L as nitrogen. Nitrate concen- trations exceeded the U.S. Environmental Protection Agency's maximum contaminant level for drinking water of 10 mg/L as nitrogen in about 33% of the 185 water samples. Groundwater affected by agricultural activities contains significantly higher concentrations of dissolved constituents than does natural groundwater. Concentrations of calcium and magnesium are higher because of liming of soils, and concentrations of potassium and chloride are higher because of applications of potash, a supple- ment to the nitrogen-based fertilizers. Alkalinity concentrations commonly are decreased because the bicarbonate ion is consumed in buffering reactions with acid that is produced during nitrification. Effects of agricultural activities on groundwater quality are not limited to the near-surface parts of the aquifer underlying farm fields. Elevated concentrations are common in aerobic water at or near the base of the aquifer, 80 to 100 ft below land surface. The median concentration of nitrate in water beneath agricultural areas collected from 24 wells deeper than 80 ft below land surface was 8.5 mg/L as nitrogen, and concentrations in 9 of these water samples exceeded the maximum contaminant level. Regional variations in concentrations of nitrate and other agriculture related constituents in the surficial aquifer in the Delmarva Peninsula depend on a number of factors that include geomorphology, geology, soils, land use, and groundwater-flow patterns. (USGS)

  18. Bactericidal activities of plant essential oils and some of their isolated constituents against Campylobacter jejuni, Escherichia coli, Listeria monocytogenes, and Salmonella enterica.

    PubMed

    Friedman, Mendel; Henika, Philip R; Mandrell, Robert E

    2002-10-01

    An improved method of sample preparation was used in a microplate assay to evaluate the bactericidal activity levels of 96 essential oils and 23 oil compounds against Campylobacter jejuni, Escherichia coli O157:H7, Listeria monocytogenes, and Salmonella enterica obtained from food and clinical sources. Bactericidal activity (BA50) was defined as the percentage of the sample in the assay mixture that resulted in a 50% decrease in CFU relative to a buffer control. Twenty-seven oils and 12 compounds were active against all four species of bacteria. The oils that were most active against C. jejuni (with BA50 values ranging from 0.003 to 0.009) were marigold, ginger root, jasmine, patchouli, gardenia, cedarwood, carrot seed, celery seed, mugwort, spikenard, and orange bitter oils; those that were most active against E. coli (with BA50 values ranging from 0.046 to 0.14) were oregano, thyme, cinnamon, palmarosa, bay leaf, clove bud, lemon grass, and allspice oils; those that were most active against L monocytogenes (with BA50 values ranging from 0.057 to 0.092) were gardenia, cedarwood, bay leaf, clove bud, oregano, cinnamon, allspice, thyme, and patchouli oils; and those that were most active against S. enterica (with BA50 values ranging from 0.045 to 0.14) were thyme, oregano, cinnamon, clove bud, allspice, bay leaf, palmarosa, and marjoram oils. The oil compounds that were most active against C. jejuni (with BA50 values ranging from 0.003 to 0.034) were cinnamaldehyde, estragole, carvacrol, benzaldehyde, citral, thymol, eugenol, perillaldehyde, carvone R, and geranyl acetate; those that were most active against E. coli (with BA50 values ranging from 0.057 to 0.28) were carvacrol, cinnamaldehyde, thymol, eugenol, salicylaldehyde, geraniol, isoeugenol, citral, perillaldehyde, and estragole; those that were most active against L monocytogenes (with BA50 values ranging from 0.019 to 0.43) were cinnamaldehyde, eugenol, thymol, carvacrol, citral, geraniol, perillaldehyde

  19. Antioxidant activity and phytochemical constituent of two plants used to manage foot and mouth disease in the Far North Region of Cameroon

    PubMed Central

    Vougat, Ronald Romuald Bebey Ngom; Foyet, Harquin Simplice; Ziebe, Roland; Garabed, Rebecca B.

    2015-01-01

    Aim: Plants used in the Far North Region of Cameroon by livestock farmers to manage foot and mouth disease (FMD) in cattle and the phytochemical composition and antioxidant potentials of two of them (Boscia senegalensis [BS] and Tapinanthus dodoneifolius [TD]) were investigated in this study. Materials and Methods: Ethno veterinary data were collected from 325 livestock farmers using semi-structured interviews from September 2011 to April 2012. The 2,2-diphenyl-picrylhydrazyl radical scavenging activity and total phenolic content (TPC) were first performed with five different solvents to choose the best extract of each plant based on these two factors. To achieve our aim, the ferric iron reducing activity, hydroxyl radical scavenging activity (HRSA), free radical scavenging activity (FRSA), vitamin E and iron content were analyzed on extracts selected using current techniques. Results: The results showed that 12 plants of 8 different families are regularly used by farmers to manage FMD. It also demonstrated that acetone extract of TD and methanolic extract of BS are the extracts which showed the best total antioxidant activity (AA) and the best TPC. In general, TD show the best AA during the HRSA and FRSA analysis compared with BS. Similarly, TD content more phenolic compounds and tannins than BS. Both plants contain proteins, saponins, tannins, phenols, alkaloid, and polyphenols which are known to have many biological activities. Conclusion: These results support the AA of both plants and can justify their use by herders to treat FMD which is often followed by many secondary diseases. PMID:26401383

  20. Anti-inflammatory activity of edible brown alga Saccharina japonica and its constituents pheophorbide a and pheophytin a in LPS-stimulated RAW 264.7 macrophage cells.

    PubMed

    Islam, Md Nurul; Ishita, Ishrat Jahan; Jin, Seong Eun; Choi, Ran Joo; Lee, Chan Mee; Kim, Yeong Shik; Jung, Hyun Ah; Choi, Jae Sue

    2013-05-01

    Anti-inflammatory activity of Saccharina japonica and its active components was evaluated via in vitro inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide (NO) production, inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) expression in RAW 264.7 murine macrophage cells. Since the methanolic extract of S. japonica showed strong anti-inflammatory activity, it was fractionated with several solvents. Among the fractions, the ethyl acetate fraction demonstrated the highest inhibition of LPS-induced NO production (IC50=25.32μg/mL), followed by the CH2Cl2 fraction (IC50=75.86μg/mL). Considering the yield and anti-inflammatory potential together, the CH2Cl2 fraction was selected for chromatographic separation to yield two active porphyrin derivatives, pheophorbide a and pheophytin a, together with an inactive fucoxanthin. In contrast to fucoxanthin, pheophorbide a and pheophytin a showed dose-dependent inhibition against LPS-induced NO production at nontoxic concentrations in RAW 264.7 cells. Both compounds also suppressed the expression of iNOS proteins, while they did not inhibit the COX-2 expression in LPS-stimulated macrophages. These results indicate that pheophorbide a and pheophytin a are two important candidates of S. japonica as anti-inflammatory agents which can inhibit the production of NO via inhibition of iNOS protein expression. Thus, these compounds hold great promise for use in the treatment of various inflammatory diseases.

  1. In vitro antiplasmodial activity of extract and constituents from Esenbeckia febrifuga, a plant traditionally used to treat malaria in the Brazilian Amazon.

    PubMed

    Dolabela, Maria Fâni; Oliveira, Salma G; Nascimento, José Maria; Peres, José Maria; Wagner, Hildebert; Póvoa, Marinete Marins; de Oliveira, Alaíde Braga

    2008-05-01

    Esenbeckia febrifuga (Rutaceae) is a plant traditionally used to treat malaria in the Brazilian Amazon region. Ethanol extract of stems displayed a good antiplasmodial activity against Plasmodium falciparum strains W-2 (IC(50) 15.5+/-0.71 microg/ml) and 3 D7 (IC(50) 21.0+/-1.4 microg/ml). Two coumarins (bergaptene 1 and isopimpinellin 2), five alkaloids (flindersiamine 3, kokusaginine 4, skimmiamine 5, gamma-fagarine 6 and 1-hydroxy-3-methoxy-N-methylacridone, 7), besides a limonoid (rutaevine 8), have been isolated for the first time from this species. Antiplasmodial activity of compounds 3, 5-8 has been evaluated in vitro against P. falciparum strains (W-2 and 3D7) and the furoquinolines 5 and 6 were the most potent displaying IC(50) values <50 microg/ml; flindersiamine (3) showed a weak activity while alkaloid 7 and rutaevine (8) were inactive (IC(50)>100 microg/ml).

  2. Circulatory response and autonomic nervous activity during gum chewing.

    PubMed

    Hasegawa, Yoko; Sakagami, Joe; Ono, Takahiro; Hori, Kazuhiro; Zhang, Min; Maeda, Yoshinobu

    2009-08-01

    Mastication has been proven to enhance the systemic circulation, with circulatory responses seeming to be largely regulated by autonomic nervous activity via a more complex regulatory system than those of other activities. However, few studies have examined the relationships between changes in autonomic nervous activity and the systemic circulation that are induced by masticatory movement. We investigated changes in the systemic circulation and autonomic nervous activity during gum chewing to clarify the influence of mastication. Electrocardiograms, arterial blood pressure, and masseter electromyograms were taken while chewing gum continuously as indicators of systemic circulation in 10 healthy subjects with normal dentition. Cardiac sympathetic activity and vagus nervous activity, as well as vasomotor sympathetic nervous activity, were evaluated by fluctuation analysis of heart rate and blood pressure. Repeated analysis of variance and multiple comparisons were performed to determine chronological changes in each indicator during gum chewing. Gum chewing increased the heart rate and the mean arterial pressure. Although cardiac sympathetic activity and vagus nervous activity showed significant changes, vasomotor sympathetic nervous activity did not. These results suggest that changes in the autonomic nervous activity of the heart are mainly involved in the enhancement of systemic circulation with gum chewing. This explains some characteristics of autonomic nervous regulation in masticatory movement.

  3. Experience with family activation of rapid response teams.

    PubMed

    Bogert, Soudi; Ferrell, Carmen; Rutledge, Dana N

    2010-01-01

    Condition H allows family activation of a rapid response team in a hospital setting. Systematic implementation of Condition H at a 500-bed Magnet community hospital led to varied types of calls, all of which met the policy criteria. Many communication issues were discovered through this process.

  4. Educating for Political Activity: A Younger Generational Response

    ERIC Educational Resources Information Center

    Mac an Ghaill, Mairtin

    2010-01-01

    This paper is a response to Professor Chitty's "Educational Review" Guest Lecture article, "Educating for political activity". I address the three sections of his paper: a global and national-based politics of war, corporate manipulation and parliamentary scandals. This provides a basis to draw upon empirical material from a…

  5. Dynamics of lung macrophage activation in response to helminth infection

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Most of our understanding of the development and phenotype of alternatively activated macrophages (AAM) has been obtained from studies investigating the response of bone marrow- and peritoneal-derived cells to IL-4 or IL-13 stimulation. Comparatively little is known about the development of the AAM...

  6. Chemical constituents of marijuana: the complex mixture of natural cannabinoids.

    PubMed

    Elsohly, Mahmoud A; Slade, Desmond

    2005-12-22

    The cannabis plant (Cannabis sativa L.) and products thereof (such as marijuana, hashish and hash oil) have a long history of use both as a medicinal agent and intoxicant. Over the last few years there have been an active debate regarding the medicinal aspects of cannabis. Currently cannabis products are classified as Schedule I drugs under the Drug Enforcement Administration (DEA) Controlled Substances act, which means that the drug is only available for human use as an investigational drug. In addition to the social aspects of the use of the drug and its abuse potential, the issue of approving it as a medicine is further complicated by the complexity of the chemical make up of the plant. This manuscript discusses the chemical constituents of the plant with particular emphasis on the cannabinoids as the class of compounds responsible for the drug's psychological properties.

  7. The grammar of visual narrative: Neural evidence for constituent structure in sequential image comprehension

    PubMed Central

    Cohn, Neil; Jackendoff, Ray; Holcomb, Phillip J.; Kuperberg, Gina R.

    2014-01-01

    Constituent structure has long been established as a central feature of human language. Analogous to how syntax organizes words in sentences, a narrative grammar organizes sequential images into hierarchic constituents. Here we show that the brain draws upon this constituent structure to comprehend wordless visual narratives. We recorded neural responses as participants viewed sequences of visual images (comics strips) in which blank images either disrupted individual narrative constituents or fell at natural constituent boundaries. A disruption of either the first or the second narrative constituent produced a left-lateralized anterior negativity effect between 500-700ms. Disruption of the second constituent also elicited a posteriorly-distributed positivity (P600) effect. These neural responses are similar to those associated with structural violations in language and music. These findings provide evidence that comprehenders use a narrative structure to comprehend visual sequences and that the brain engages similar neurocognitive mechanisms to build structure across multiple domains. PMID:25241329

  8. The grammar of visual narrative: Neural evidence for constituent structure in sequential image comprehension.

    PubMed

    Cohn, Neil; Jackendoff, Ray; Holcomb, Phillip J; Kuperberg, Gina R

    2014-11-01

    Constituent structure has long been established as a central feature of human language. Analogous to how syntax organizes words in sentences, a narrative grammar organizes sequential images into hierarchic constituents. Here we show that the brain draws upon this constituent structure to comprehend wordless visual narratives. We recorded neural responses as participants viewed sequences of visual images (comics strips) in which blank images either disrupted individual narrative constituents or fell at natural constituent boundaries. A disruption of either the first or the second narrative constituent produced a left-lateralized anterior negativity effect between 500 and 700ms. Disruption of the second constituent also elicited a posteriorly-distributed positivity (P600) effect. These neural responses are similar to those associated with structural violations in language and music. These findings provide evidence that comprehenders use a narrative structure to comprehend visual sequences and that the brain engages similar neurocognitive mechanisms to build structure across multiple domains.

  9. A Comprehensive Review on the Phytochemical Constituents and Pharmacological Activities of Pogostemon cablin Benth.: An Aromatic Medicinal Plant of Industrial Importance.

    PubMed

    Swamy, Mallappa Kumara; Sinniah, Uma Rani

    2015-05-12

    Pogostemon cablin Benth. (patchouli) is an important herb which possesses many therapeutic properties and is widely used in the fragrance industries. In traditional medicinal practices, it is used to treat colds, headaches, fever, nausea, vomiting, diarrhea, abdominal pain, insect and snake bites. In aromatherapy, patchouli oil is used to relieve depression, stress, calm nerves, control appetite and to improve sexual interest. Till now more than 140 compounds, including terpenoids, phytosterols, flavonoids, organic acids, lignins, alkaloids, glycosides, alcohols, aldehydes have been isolated and identified from patchouli. The main phytochemical compounds are patchouli alcohol, α-patchoulene, β-patchoulene, α-bulnesene, seychellene, norpatchoulenol, pogostone, eugenol and pogostol. Modern studies have revealed several biological activities such as antioxidant, analgesic, anti-inflammatory, antiplatelet, antithrombotic, aphrodisiac, antidepressant, antimutagenic, antiemetic, fibrinolytic and cytotoxic activities. However, some of the traditional uses need to be verified and may require standardizing and authenticating the bioactivity of purified compounds through scientific methods. The aim of the present review is to provide comprehensive knowledge on the phytochemistry and pharmacological activities of essential oil and different plant extracts of patchouli based on the available scientific literature. This information will provide a potential guide in exploring the use of main active compounds of patchouli in various medical fields.

  10. Anti-adipogenic activity of the edible brown alga Ecklonia stolonifera and its constituent fucosterol in 3T3-L1 adipocytes.

    PubMed

    Jung, Hyun Ah; Jung, Hee Jin; Jeong, Hyun Young; Kwon, Hyun Ju; Kim, Min-Sun; Choi, Jae Sue

    2014-06-01

    Fucosterol is a sterol metabolite of brown algae and regulates genes involved with cholesterol homeostasis. As a part of our continuous search for anti-obesity agents from natural marine sources, the anti-adipogenic activities of Ecklonia stolonifera and its sterol, fucosterol, were evaluated for the inhibition of adipocyte differentiation and lipid formation. Oil Red O staining was used to evaluate triglyceride contents in 3T3-L1 pre-adipocytes primed by differentiation medium (DM) I and DM II. The methanolic extract of E. stolonifera showed strong anti-adipogenic activity, and was thus fractionated with several solvents. Among the tested fractions, the dichloromethane (CH2Cl2) fraction was found to be the most active fraction, with significant inhibition (40.5 %) of intracellular lipid accumulation at a non-toxic concentration, followed by the ethyl acetate fraction (30.2 %) at the same concentration, while the n-butanol and water fractions did not show inhibitory activity within the tested concentrations. The strong anti-adipogenic CH2Cl2-soluble fraction was further purified by a repeated chromatography to yield fucosterol. Fucosterol reduced lipid contents in a concentration-dependent manner without showing any cytotoxicity. Fucosterol treatment also yielded a decrease in the expression of the adipocyte marker proteins peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT/enhancer-binding protein α (C/EBPα) in a concentration-dependent manner. Taken together, these results suggest that fucosterol inhibits expression of PPARγ and C/EBPα, resulting in a decrease of lipid accumulation in 3T3-L1 pre-adipocytes, indicating that the potential use of E. stolonifera and its bioactive fucosterol as an anti-obesity agent.

  11. Carnosol, a Constituent of Zyflamend, Inhibits Aryl Hydrocarbon Receptor-Mediated Activation of CYP1A1 and CYP1B1 Transcription and Mutagenesis

    PubMed Central

    Mohebati, Arash; Guttenplan, Joseph B.; Kochhar, Amit; Zhao, Zhong-Lin; Kosinska, Wieslawa; Subbaramaiah, Kotha; Dannenberg, Andrew J.

    2012-01-01

    The aryl hydrocarbon receptor (AhR), a ligand-activated member of the basic-helix-loop-helix family of transcription factors, plays a significant role in polycyclic aromatic hydrocarbon (PAH) induced carcinogenesis. In the upper aerodigestive tract of humans, tobacco smoke, a source of PAHs, activates the AhR leading to increased expression of CYP1A1 and CYP1B1, which encode proteins that convert PAHs to genotoxic metabolites. Inhibitors of Hsp90 ATPase cause a rapid decrease in levels of AhR, an Hsp90 client protein, and thereby block PAH-mediated induction of CYP1A1 and CYP1B1. The main objective of this study was to determine whether Zyflamend, a polyherbal preparation, suppressed PAH-mediated induction of CYP1A1 and CYP1B1 and inhibited DNA adduct formation and mutagenesis. We also investigated whether carnosol, one of multiple phenolic antioxidants in Zyflamend, had similar inhibitory effects. Treatment of cell lines derived from oral leukoplakia (MSK-Leuk1) and skin (HaCaT) with benzo[a]pyrene (B[a]P), a prototypic PAH, induced CYP1A1 and CYP1B1 transcription, resulting in enhanced levels of message and protein. Both Zyflamend and carnosol suppressed these effects of B[a]P. Notably, both Zyflamend and carnosol inhibited Hsp90 ATPase activity and caused a rapid reduction in AhR levels. The formation of B[a]P induced DNA adducts and mutagenesis were also inhibited by Zyflamend and carnosol. Collectively, these results show that Zyflamend and carnosol inhibit Hsp90 ATPase leading to reduced levels of AhR, suppression of B[a]P-mediated induction of CYP1A1 and CYP1B1 and inhibition of mutagenesis. Carnosol-mediated inhibition of Hsp90 ATPase activity can help explain the chemopreventive activity of herbs such as Rosemary, which contain this phenolic antioxidant. PMID:22374940

  12. Phase response curves in the characterization of epileptiform activity

    NASA Astrophysics Data System (ADS)

    Perez Velazquez, J. L.; Galán, R. F.; Dominguez, L. Garcia; Leshchenko, Y.; Lo, S.; Belkas, J.; Erra, R. Guevara

    2007-12-01

    Coordinated cellular activity is a major characteristic of nervous system function. Coupled oscillator theory offers unique avenues to address cellular coordination phenomena. In this study, we focus on the characterization of the dynamics of epileptiform activity, based on some seizures that manifest themselves with very periodic rhythmic activity, termed absence seizures. Our approach consists in obtaining experimentally the phase response curves (PRCs) in the neocortex and thalamus, and incorporating these PRCs into a model of coupled oscillators. Phase preferences of the stationary states and their stability are determined, and these results from the model are compared with the experimental recordings, and interpreted in physiological terms.

  13. Fractionation of muscle activity in rapid responses to startling cues

    PubMed Central

    Dean, Lauren R.

    2017-01-01

    Movements in response to acoustically startling cues have shorter reaction times than those following less intense sounds; this is known as the StartReact effect. The neural underpinnings for StartReact are unclear. One possibility is that startling cues preferentially invoke the reticulospinal tract to convey motor commands to spinal motoneurons. Reticulospinal outputs are highly divergent, controlling large groups of muscles in synergistic patterns. By contrast the dominant pathway in primate voluntary movement is the corticospinal tract, which can access small groups of muscles selectively. We therefore hypothesized that StartReact responses would be less fractionated than standard voluntary reactions. Electromyogram recordings were made from 15 muscles in 10 healthy human subjects as they carried out 32 varied movements with the right forelimb in response to startling and nonstartling auditory cues. Movements were chosen to elicit a wide range of muscle activations. Multidimensional muscle activity patterns were calculated at delays from 0 to 100 ms after the onset of muscle activity and subjected to principal component analysis to assess fractionation. In all cases, a similar proportion of the total variance could be explained by a reduced number of principal components for the startling and the nonstartling cue. Muscle activity patterns for a given task were very similar in response to startling and nonstartling cues. This suggests that movements produced in the StartReact paradigm rely on similar contributions from different descending pathways as those following voluntary responses to nonstartling cues. NEW & NOTEWORTHY We demonstrate that the ability to activate muscles selectively is preserved during the very rapid reactions produced following a startling cue. This suggests that the contributions from different descending pathways are comparable between these rapid reactions and more typical voluntary movements. PMID:28003416

  14. Effects of ginger and its pungent constituents on transient receptor potential channels.

    PubMed

    Kim, Young-Soo; Hong, Chan Sik; Lee, Sang Weon; Nam, Joo Hyun; Kim, Byung Joo

    2016-12-01

    Ginger extract is used as an analeptic in herbal medicine and has been reported to exert antioxidant effects. Transient receptor potential (TRP) canonical 5 (TRPC5), TRP cation channel, subfamily M, member 7 (TRPM7; melastatin 7), and TRP cation channel, subfamily A, member 1 (TRPA1; ankyrin 1) are non-selective cation channels that are modulated by reactive oxygen/nitrogen species (ROS/RNS) and subsequently control various cellular processes. The aim of this study was to evaluate whether ginger and its pungent constituents modulate these channels and exert antioxidant effects. It was found that TRPC5 and TRPA1 currents were modulated by ginger extract and by its pungent constituents, [6]-gingerol, zingerone and [6]-shogaol. In particular, [6]-shogaol markedly and dose-dependently inhibited TRPC5 currents with an IC50 of value of ~18.3 µM. Furthermore, the strong dose-dependent activation of TRPA1 currents by [6]-shogaol was abolished by A‑967079 (a selective TRPA1 inhibitor). However, ginger extract and its pungent constituents had no effect on TRPM7 currents. These results suggest the antioxidant effects of ginger extract and its pungent constituents are mediated through TRPC5 and TRPA1, and that [6]-shogaol is predominantly responsible for the regulation of TRPC5 and TRPA1 currents by ginger extract.

  15. Activation of DNA damage response signaling by condensed chromatin.

    PubMed

    Burgess, Rebecca C; Burman, Bharat; Kruhlak, Michael J; Misteli, Tom

    2014-12-11

    The DNA damage response (DDR) occurs in the context of chromatin, and architectural features of chromatin have been implicated in DNA damage signaling and repair. Whereas a role of chromatin decondensation in the DDR is well established, we show here that chromatin condensation is integral to DDR signaling. We find that, in response to DNA damage chromatin regions transiently expand before undergoing extensive compaction. Using a protein-chromatin-tethering system to create defined chromatin domains, we show that interference with chromatin condensation results in failure to fully activate DDR. Conversely, forced induction of local chromatin condensation promotes ataxia telangiectasia mutated (ATM)- and ATR-dependent activation of upstream DDR signaling in a break-independent manner. Whereas persistent chromatin compaction enhanced upstream DDR signaling from irradiation-induced breaks, it reduced recovery and survival after damage. Our results demonstrate that chromatin condensation is sufficient for activation of DDR signaling and is an integral part of physiological DDR signaling.

  16. Humpback Dolphin (Genus Sousa) Behavioural Responses to Human Activities.

    PubMed

    Piwetz, Sarah; Lundquist, David; Würsig, Bernd

    2015-01-01

    Humpback dolphins (genus Sousa) use shallow, near-shore waters throughout their range. This coastal distribution makes them vulnerable to recreational and commercial disturbances, especially near heavily populated and industrialized areas. Most research focusing on Sousa and human activities has emphasized direct impacts and threats, involving injury and death, with relatively little focus on indirect effects on dolphins, such as changes in behaviour that may lead to deleterious effects. Understanding behaviour is important in resolving human-wildlife conflict and is an important component of conservation. This chapter gives an overview of animal behavioural responses to human activity with examples from diverse taxa; reviews the scientific literature on behavioural responses of humpback dolphins to human activity throughout their range, including marine vessel traffic, dolphin tourism, cetacean-fishery interactions, noise pollution, and habitat alteration; and highlights information and data gaps for future humpback dolphin research to better inform behaviour-based management decisions that contribute to conservation efforts.

  17. Potential Antidepressant Constituents of Nigella sativa Seeds

    PubMed Central

    Elkhayat, Ehab S.; Alorainy, Mohammad S.; El-Ashmawy, Ibrahim M.; Fat’hi, Shawkat

    2016-01-01

    Background: Nigella sativa Linn. is well known seed in the Middle East, Asia, and the Far East as a natural remedy for many ailments and as a flavoring agent proclaimed medicinal usage dating back to the ancient Egyptians, Greeks, and Romans. An authentic saying of the Prophet Muhammad (Peace Be Upon Him) about black seed is also quoted in Al-Bukhari. Objective: This study was carried out to evaluate the antidepressant effect and isolate the potential antidepressant constituents of the polar extract of N. sativa seeds. Materials and Methods: The antidepressant effect was evaluated through the immobility duration in tail suspension and forced swim tests (FSTs). Albino mice were orally treated with N. sativa polar extract and its RP-18 column chromatography fractions (50 and 100 mg/kg,). Results: The polar extract and two of its sub-fractions were significantly able to decrease the immobility time of mice when subjected to both tail suspension and FSTs, the effects are comparable to standard drug (Sertraline, 5 mg/kg). However, these treatments did not affect the number of crossings and rearing in the open field test. Phytochemical investigation of the two active fractions led to the isolation of quercetin-3-O-α-L-rhamnopyranoside 1, quercetin-7-O-β-D-gluco- pyranoside 2, tauroside E 3, and sapindoside B as the potential antidepressant constituents. SUMMARY Phytochemical and biological evaluation the antidepressant constituents in Nigella sativa using the tail suspension and forced swim methods afforded the isolation and identification of quercetin-3-O-α-L rhamnopyranoside, quercetin-7-O-β-D gluco pyranoside, tauroside E, and sapindoside B as the potential antidepressant constituents in the polar extract of N. sativa. The isolated compounds were identified through extensive NMR analysis (1D, 2D, ESI MS). Abbreviations used: TST: Tail suspension test, FST: Forced swim test, OFT: An Open field test PMID:27041854

  18. Comparison of volatile constituents, and antioxidant and antibacterial activities of the essential oils of Thymus caucasicus, T. kotschyanus and T. vulgaris.

    PubMed

    Asbaghian, Shiva; Shafaghat, Ali; Zarea, Khalil; Kasimov, Fakhraddin; Salimi, Farshid

    2011-01-01

    A comparison of the chemical composition, and antioxidant and antibacterial activities of the essential oils obtained from the aerial parts of Thymus caucasicus, T. kotschyanus, and T vulgaris was carried out. The oils, obtained by hydrodistillation, were analyzed by GC and GC/MS. Twenty, 29 and 22 compounds representing 94.8%, 96.6% and 98.2% of the essential oils of T. caucasicus, T. kotschyanus and T. vulgaris, respectively, have been identified. The oil of T. caucasicus was characterized by 1,8-cineol (21.5%), thymol (12.6%), beta-fenchyl alcohol (8.7%), nerolidol (7.8%), terpinolene (7.2%), alpha-pinene (7.0%) and myrcene (6.8%). In the oil of T. kotschyanus, carvacrol (24.4%), beta-caryophyllene (14.5%), gamma-terpinene (12.4%), alpha-phellandrene (10.8%), p-cymene (9.8%) and thymol (6.8%) were the predominant compounds, whereas the main components of T. vulgaris oil were thymol (43.8%), p-cymene (15.2%), germacrene-D (11.7%), terpinolene (3.4%), carvacrol (3.2%), beta-caryophyllene (2.8%) and alpha-thujene (2.2%). In all three plants oil, hydrocarbon monoterpenes predominated over sesquiterpenes. Antioxidant activities were assessed by determining IC50 values in the DPPH radical scavenging assay. Antibacterial activity was determined by measuring minimum inhibitory concentration (MIC) using the broth dilution method. The essential oils of T. caucasicus, T. kotschyanus and T. vulgaris showed free radical scavenging and antibacterial activity.

  19. Effect of cinnamon, clove and some of their constituents on the Na(+)-K(+)-ATPase activity and alanine absorption in the rat jejunum.

    PubMed

    Kreydiyyeh, S I; Usta, J; Copti, R

    2000-09-01

    The effect of a water extract of some spices on the in vitro activity of the rat jejunal Na(+)-K(+)-ATPase was investigated. Extracts of nutmeg, cinnamon, clove, cumin, coriander, turmeric and caraway all inhibited the ATPase, while anise seed and white pepper exerted no significant effects. The extracts of clove and cinnamon had the most potent inhibitory effect on the intestinal ATPase as compared to extracts of other spices. They also inhibited the in vitro Na(+)-K(+)-ATPase activity in a crude kidney homogenate and the activity of an isolated dog kidney Na(+)-K(+)-ATPase. The alcoholic extract of cinnamon, compared to the aqueous extract, had a stronger inhibitory action on the jejunal enzyme and a lower IC(50) value, which was not significantly different from the one observed with cinnamaldehyde, the major volatile oil present cinnamon, suggesting that in alcoholic extracts cinnamaldehyde is the major inhibitory component. The IC(50) values of eugenol, aqueous clove extract and ethanolic clove extract all fell within the same range and were not significantly different from each other, suggesting that eugenol is the major inhibitory component in both alcoholic and aqueous extracts. Based on the IC(50) values, the order of sensitivity of the enzyme to the spices extracts is as follows: isolated dog kidney ATPase>rat kidney ATPase>rat intestine ATPase. The aqueous extracts of clove and cinnamon also significantly lowered the absorption of alanine from the rat intestine. It was concluded that the active principle(s) in clove and cinnamon can permeate the membrane of the enterocytes and inhibit the Na(+)-K(+)-ATPase that provides the driving force for many transport processes.

  20. Delphinid behavioral responses to incidental mid-frequency active sonar.

    PubMed

    Henderson, E Elizabeth; Smith, Michael H; Gassmann, Martin; Wiggins, Sean M; Douglas, Annie B; Hildebrand, John A

    2014-10-01

    Opportunistic observations of behavioral responses by delphinids to incidental mid-frequency active (MFA) sonar were recorded in the Southern California Bight from 2004 through 2008 using visual focal follows, static hydrophones, and autonomous recorders. Sound pressure levels were calculated between 2 and 8 kHz. Surface behavioral responses were observed in 26 groups from at least three species of 46 groups out of five species encountered during MFA sonar incidents. Responses included changes in behavioral state or direction of travel, changes in vocalization rates and call intensity, or a lack of vocalizations while MFA sonar occurred. However, 46% of focal groups not exposed to sonar also changed their behavior, and 43% of focal groups exposed to sonar did not change their behavior. Mean peak sound pressure levels when a behavioral response occurred were around 122 dB re: 1 μPa. Acoustic localizations of dolphin groups exhibiting a response gave insight into nighttime movement patterns and provided evidence that impacts of sonar may be mediated by behavioral state. The lack of response in some cases may indicate a tolerance of or habituation to MFA sonar by local populations; however, the responses that occur at lower received levels may point to some sensitization as well.

  1. Nonconscious activation of placebo and nocebo pain responses

    PubMed Central

    Jensen, Karin B.; Kaptchuk, Ted J.; Kirsch, Irving; Raicek, Jacqueline; Lindstrom, Kara M.; Berna, Chantal; Gollub, Randy L.; Ingvar, Martin; Kong, Jian

    2012-01-01

    The dominant theories of human placebo effects rely on a notion that consciously perceptible cues, such as verbal information or distinct stimuli in classical conditioning, provide signals that activate placebo effects. However, growing evidence suggest that behavior can be triggered by stimuli presented outside of conscious awareness. Here, we performed two experiments in which the responses to thermal pain stimuli were assessed. The first experiment assessed whether a conditioning paradigm, using clearly visible cues for high and low pain, could induce placebo and nocebo responses. The second experiment, in a separate group of subjects, assessed whether conditioned placebo and nocebo responses could be triggered in response to nonconscious (masked) exposures to the same cues. A total of 40 healthy volunteers (24 female, mean age 23 y) were investigated in a laboratory setting. Participants rated each pain stimulus on a numeric response scale, ranging from 0 = no pain to 100 = worst imaginable pain. Significant placebo and nocebo effects were found in both experiment 1 (using clearly visible stimuli) and experiment 2 (using nonconscious stimuli), indicating that the mechanisms responsible for placebo and nocebo effects can operate without conscious awareness of the triggering cues. This is a unique experimental verification of the influence of nonconscious conditioned stimuli on placebo/nocebo effects and the results challenge the exclusive role of awareness and conscious cognitions in placebo responses. PMID:23019380

  2. Chemical constituents and antifilarial activity of Lantana camara against human lymphatic filariid Brugia malayi and rodent filariid Acanthocheilonema viteae maintained in rodent hosts.

    PubMed

    Misra, Namita; Sharma, Mithilesh; Raj, Kanwal; Dangi, Anil; Srivastava, Sudhir; Misra-Bhattacharya, Shailja

    2007-02-01

    Lymphatic filariasis continues to be a major health problem in tropical and subtropical countries. A macrofilaricidal agent capable of eliminating adult filarial parasites is urgently needed. In the present study, we report the antifilarial activity in the extract of stem portion of the plant Lantana camara. The crude extract at 1 g/kg for 5 days by oral route killed 43.05% of the adult Brugia malayi parasites and sterilized 76% of surviving female worms in the rodent model Mastomys coucha. A 34.5% adulticidal activity along with sterilization of 66% of female worms could be demonstrated in the chloroform fraction. Remarkable antifilarial activity was observed in the adult B. malayi transplanted gerbil model where up to 80% of the adult worms could be killed at the same dose and all the surviving female parasites were found sterilized. The extract was also found effective against a subcutaneous rodent filariid Acanthocheilonema viteae maintained in Mastomys coucha, where it exerted strong microfilaricidal (95.04%) and sterilization (60.66%) efficacy with mild macrofilaricidal action. Two compounds, oleanonic acid and oleanolic acid, isolated from hexane and chloroform fractions showed LC100 at 31.25 and 62.5 mug/ml, respectively, on B. malayi in vitro. This is the first ever report on the antifilarial efficacy of Lantana camara.

  3. Comparative analysis of chemical constituents, antimicrobial and antioxidant activities of ethylacetate extracts of Polygonum cuspidatum and its endophytic actinomycete, Streptomyces sp. A0916.

    PubMed

    Wang, Lei; Qiu, Peng; Long, Xiu-Feng; Zhang, Shuai; Zeng, Zhi-Gang; Tian, Yong-Qiang

    2016-02-01

    The present study investigated the chemical composition of ethylacetate extracts from an endophytic actinomycete Streptomyces sp. A0916 and its host Polygonum cuspidatum. A comparative analysis of the antimicrobial and antioxidant properties of the extracts was also conducted. 32 compounds of P. cuspidatum and 23 compounds of Streptomyces sp. A0916 were isolated and identified by GC/MS. Antimicrobial activities of the extracts were evaluated using eight microbial strains (3 Gram-positive bacteria, 3 Gram-negative bacteria, and 2 fungi). The Streptomyces sp. A0916 extracts showed a wide range of antimicrobial activities and presented greater antimicrobial effectiveness than the P. cuspidatum extracts. The minimum inhibitory concentration (MIC) of Streptomyces sp. A0916 extracts against the ampicillin-resistant strain Enterococcus faecium SIIA843 was 32 μg·mL(-1). Furthermore, the extracts had greater antimicrobial effect against Gram-positive bacteria than Gram-negative bacteria. Finally, the antioxidant activity of the Streptomyces sp. A0916 extracts was equal to that of the P. cuspidatum extracts. In conclusion, our results suggest that the endophytic actinomycetes of the medicinal plants are an important source of bioactive substances.

  4. In vitro biological assessment of berberis vulgaris and its active constituent, berberine: antioxidants, anti-acetylcholinesterase, anti-diabetic and anticancer effects

    PubMed Central

    2013-01-01

    Background Berberis vulgaris is a well known plant with traditional herbal medical history. The aims of this study was to bioscreen and compare the in vitro biological activity (antioxidant, cholinergic, antidaibetic and the anticancer) of barberry crude extract and berberine active compound. Methods The effect of B. vulgaris extract and berberine chloride on cellular thiobarbituric acid reactive species (TBARS) formation, diphenyle–α-picrylhydrazyl (DPPH) oxidation, cellular nitric oxide (NO) radical scavenging capability, superoxide dismutase (SOD), glutathione peroxidase (GPx), acetylcholinesterase (AChE) and α-gulcosidase activities were spectrophotometrically determined. On the other hand, the effect of extract and berberine as anticancer was estimated on three different cell lines which were MCF-7, HepG-2, and Caco-2 cells by using neutral red uptake assay which compared with control normal cells (PBMC). Results Our results showed that barberry crude extract contains 0.6 mg berberine/mg crude extract. Barberry extract showed potent antioxidative capacity through decreasing TBARS, NO and the oxidation of DPPH that associated with GPx and SOD hyperactivation. Inhibitory effect of berberis crude extract on α-glucosidase was more potent than that of berberine chloride, while both had the same AChE inhibitory effect. Besides, different concentrations of both berberine chloride and barberry ethanolic extract showed to have no growth inhibitory effect on normal blood cells (PBMC). Otherwise, both berberine chloride and barberry ethanolic extract showed to have inhibitory effect on the growth of breast, liver and colon cancer cell lines (MCF7, HepG2 and CACO-2, respectively) at different incubation times starting from 24 hrs up to 72 hrs and the inhibitory effect increased with time in a dose dependant manner. Conclusion This work demonstrates the potential of the barberry crude extract and its active alkaloid, berberine, on suppressing lipid peroxidation

  5. Photoactivated Spatiotemporally-Responsive Nanosensors of in Vivo Protease Activity.

    PubMed

    Dudani, Jaideep S; Jain, Piyush K; Kwong, Gabriel A; Stevens, Kelly R; Bhatia, Sangeeta N

    2015-12-22

    Proteases play diverse and important roles in physiology and disease, including influencing critical processes in development, immune responses, and malignancies. Both the abundance and activity of these enzymes are tightly regulated and highly contextual; thus, in order to elucidate their specific impact on disease progression, better tools are needed to precisely monitor in situ protease activity. Current strategies for detecting protease activity are focused on functionalizing synthetic peptide substrates with reporters that emit detection signals following peptide cleavage. However, these activity-based probes lack the capacity to be turned on at sites of interest and, therefore, are subject to off-target activation. Here we report a strategy that uses light to precisely control both the location and time of activity-based sensing. We develop photocaged activity-based sensors by conjugating photolabile molecules directly onto peptide substrates, thereby blocking protease cleavage by steric hindrance. At sites of disease, exposure to ultraviolet light unveils the nanosensors to allow proteases to cleave and release a reporter fragment that can be detected remotely. We apply this spatiotemporally controlled system to probe secreted protease activity in vitro and tumor protease activity in vivo. In vitro, we demonstrate the ability to dynamically and spatially measure metalloproteinase activity in a 3D model of colorectal cancer. In vivo, veiled nanosensors are selectively activated at the primary tumor site in colorectal cancer xenografts to capture the tumor microenvironment-enriched protease activity. The ability to remotely control activity-based sensors may offer a valuable complement to existing tools for measuring biological activity.

  6. Microwave-assisted efficient extraction of different parts of Hippophae rhamnoides for the comparative evaluation of antioxidant activity and quantification of its phenolic constituents by reverse-phase high-performance liquid chromatography (RP-HPLC).

    PubMed

    Sharma, Upendra K; Sharma, Kapil; Sharma, Nandini; Sharma, Abhishek; Singh, Harsh P; Sinha, Arun K

    2008-01-23

    The outcome of different extraction procedures (microwave, ultrasound, Soxhlet, and maceration) on the antioxidant activity of seeds, leaves, pulp, and fruits of Hippophae rhamnoides (sea buckthorn or SBT) was investigated by two different bioassays: 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) and 2,2'-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assays. The SBT extracts were found to possess strong antioxidant activity measured in terms of TEAC (2.03-182.13 and 6.97-282.75 mg/g) with ABTS and DPPH assays, respectively. In general, the antioxidant capacity of microwave-assisted extracts was found to be significantly higher than those obtained by ultrasound-assisted extraction (UAE) and maceration while being slightly higher than Soxhlet extracts. Further, microwave extracts of seeds were found to possess maximum antioxidant capacity followed by leaves, fruits, and pulp. Also, the chemical composition of extracts, studied in terms of the total phenolic content, was found to be in the range of 1.9-23.5 mg/g Gallic acid equivalent (GAE), which indicates a strong correlation between antioxidant activity and phenolic content present in the SBT. In addition, some of its bioactive phenolic constituents, such as rutin ( 1), quercetin-3- O-galactoside ( 2), quercetin ( 3), myricetin ( 4), kaempferol ( 5), and isorhamnetin ( 6), were also quantified in different extracts by reverse-phase high-performance liquid chromatography (RP-HPLC).

  7. Guava fruit extract and its triterpene constituents have osteoanabolic effect: Stimulation of osteoblast differentiation by activation of mitochondrial respiration via the Wnt/β-catenin signaling.

    PubMed

    Porwal, Konica; Pal, Subhashis; Dev, Kapil; China, Shyamsundar Pal; Kumar, Yogesh; Singh, Chandan; Barbhuyan, Tarun; Sinha, Neeraj; Sanyal, Sabyasachi; Trivedi, Arun Kumar; Maurya, Rakesh; Chattopadhyay, Naibedya

    2017-03-08

    The aim of this study was to evaluate the skeletal effect of guava triterpene-enriched extract (GE) in rats and identify osteogenic compounds thereof, and determine their modes of action. In growing female rats, GE at 250 mg/kg dose increased parameters of peak bone mass including femur length, bone mineral density (BMD) and biomechanical strength, suggesting that GE promoted modeling-directed bone growth. GE also stimulated bone regeneration at the site of bone injury. In adult osteopenic rats (osteopenia induced by ovariectomy, OVX) GE completely restored the lost bones at both axial and appendicular sites, suggesting a strong osteoanabolic effect. Serum metabolomics studies showed changes in several metabolites (some of which are related to bone metabolism) in OVX compared with ovary-intact control and GE treatment to OVX rats reversed those. Out of six abundantly present triterpenes in GE, ursolic acid (UA) and 2α-hydroxy ursolic acid (2α-UA) induced osteogenic differentiation in vitro as did GE by activating Wnt/β-catenin pathway assessed by phosphorylation of GSK-3β. Over-expressing of constitutively active GSK-3β (caGSK-3β) in osteoblasts abolished the differentiation-promoting effect of GE, UA and 2α-UA. All three increased both glycolysis and mitochondrial respiration but only rotenone (inhibitor of mitochondrial electron transfer) and not 2-deoxyglucose (to block glycolysis) inhibited osteoblast differentiation. In addition, caGSK-3β over-expression attenuated the enhanced mitochondrial respiration caused by GE, UA and 2α-UA. We conclude that GE has osteoanabolic effect which is contributed by UA and 2α-UA, and involve activation of canonical Wnt signaling which in turn modulates cellular energy metabolism leading to osteoblast differentiation.

  8. Crocins, the active constituents of Crocus sativus L., counteracted apomorphine-induced performance deficits in the novel object recognition task, but not novel object location task, in rats.

    PubMed

    Pitsikas, Nikolaos; Tarantilis, Petros A

    2017-02-17

    Schizophrenia is a chronic mental disease that affects nearly 1% of the population worldwide. Several lines of evidence suggest that the dopaminergic (DAergic) system might be compromised in schizophrenia. Specifically, the mixed dopamine (DA) D1/D2 receptor agonist apomorphine induces schizophrenia-like symptoms in rodents, including disruption of memory abilities. Crocins are among the active components of saffron (dried stigmas of Crocus sativus L. plant) and their implication in cognition is well documented. The present study investigated whether crocins counteract non-spatial and spatial recognition memory deficits induced by apomorphine in rats. For this purpose, the novel object recognition task (NORT) and the novel object location task (NOLT) were used. The effects of compounds on mobility in a locomotor activity chamber were also investigated in rats. Post-training peripheral administration of crocins (15 and 30mg/kg) counteracted apomorphine (1mg/kg)-induced performance deficits in the NORT. Conversely, crocins did not attenuate spatial recognition memory deficits produced by apomorphine in the NOLT. The present data show that crocins reversed non-spatial recognition memory impairments produced by dysfunction of the DAergic system and modulate different aspects of memory components (storage and/or retrieval). The effects of compounds on recognition memory cannot be attributed to changes in locomotor activity. Further, our findings illustrate a functional interaction between crocins and the DAergic system that may be of relevance for schizophrenia-like behavioral deficits. Therefore, the utilization of crocins as an adjunctive agent, for the treatment of cognitive deficits observed in schizophrenic patients should be further investigated.

  9. Two primes priming: does feature integration occur before response activation?

    PubMed

    Grainger, Julianne E; Scharnowski, Frank; Schmidt, Thomas; Herzog, Michael H

    2013-07-17

    Responses to a target can be sped up or slowed down by a congruent or incongruent prime, respectively. Even though presentations are rapid, the prime and the target are thought to activate motor responses in strict sequence, with prime activation preceding target activation. In feature fusion, the opposite seems to be the case. For example, a vernier offset to the left is immediately followed by a vernier offset to the right at the same location. The two verniers are not perceived as two elements in sequence but as a single, aligned vernier. Here, we ask the question as to how features are integrated: before or after motor activation? We presented two vernier primes with opposite offset directions preceding a single vernier target. No priming effect occurred when the vernier primes were presented at the same location, indicating that verniers integrate before motor activation. There was also no priming effect when the primes were presented simultaneously at different locations, indicating that there is an integration stage different from the perceptual fusion stage. When the second prime is delayed, it determines priming, even for very long delays. To explain these long integration times, we argue that there is a buffer preceding motor activation.

  10. The Haida Gwaii Diabetes Project: planned response activity outcomes.

    PubMed

    Heffernan, Clare; Herbert, Carol; Grams, Garry D.; Grzybowski, Stefan; Wilson, Mary Ann; Calam, Betty; Brown, Diane

    1999-11-01

    A 1992 chart review in the Haida Village of Skidegate, Haida Gwaii/Queen Charlotte Islands, Canada, revealed that 17% of the unscreened population aged 35 or over have been diagnosed with diabetes. The Haida Gwaii Diabetes Project was designed to develop a culturally sensitive community-based participatory action approach to the management of noninsulin-dependent diabetes (NIDDM). Phase One included obtaining community support, conducting a chart review, holding clinics to measure biophysical indicators, conducting focus groups, and planning response activities with the communities. A list of activities was developed, based on the focus group results. In addition, the project team developed a set of operating principles that ensured and reinforced collaboration. Phase Two included implementing and monitoring planned response activities, and holding exit clinics. The best attended activities were trials of traditional herbal medicine and traditional diet, and an exercise programme. While participation levels were not high enough for causal conclusions, a significant decrease in total cholesterol (0.45; P = 0.005) and rise in HDL (-0.097; P = 0.05) was found for participants for whom paired values were available. Diabetes intervention research in First Nations settings involves small numbers of participants, making it difficult to quantitatively assess outcomes. To increase participation it is advisable to open activities to the whole community, to tie planned activities into other scheduled community events, and to share findings concerning managing illnesses of acculturation with other communities.

  11. The prolactin responses to active and passive heating in man.

    PubMed

    Low, David; Purvis, Alison; Reilly, Thomas; Cable, N Tim

    2005-11-01

    The aim of this study was to compare the prolactin and blood pressure responses at identical core temperatures during active and passive heat stresses, using prolactin as an indirect marker of central fatigue. Twelve male subjects cycled to exhaustion at 60% maximal oxygen uptake (VO2peak) in a room maintained at 33 degrees C (active). In a second trial they were passively heated (passive) in a water bath (41.56 +/- 1.65 degrees C) until core temperature was equal to the core temperature observed at exhaustion during the active trial. Blood samples were taken from an indwelling venous cannula for the determination of serum prolactin during active heating and at corresponding core temperatures during passive heating. Core temperature was not significantly different between the two methods of heating and averaged 38.81 +/- 0.53 and 38.82 +/- 0.70 degrees C (data expressed as means +/- s.d.) at exhaustion during active heating and at the end of passive heating, respectively (P > 0.05). Mean arterial blood pressure was significantly lower throughout passive heating (active, 73 +/- 9 mmHg; passive, 62 +/- 12 mmHg; P < 0.01). Despite the significantly reduced blood pressure responses during passive heating, during both forms of heating the prolactin response was the same (active, 14.9 +/- 12.6 ng ml(-1); passive, 13.3 +/- 9.6 ng ml(-1); n.s.). These results suggest that thermoregulatory, i.e. core temperature, and not cardiovascular afferents provide the key stimulus for the release of prolactin, an indirect marker of central fatigue, during exercise in the heat.

  12. Characterization of the volatile constituents in the essential oil of Pistacia lentiscus L. from different origins and its antifungal and antioxidant activity.

    PubMed

    Barra, Andrea; Coroneo, Valentina; Dessi, Sandro; Cabras, Paolo; Angioni, Alberto

    2007-08-22

    Essential oil (EO) from aerial parts (leaves, juvenile branches, and flowers when present) of Pistacia lentiscus L. growing wild in five localities of Sardinia (Italy) was extracted by steam-distillation (SD) and analyzed by gas chromatography (GC), FID, and GC-ion trap mass spectrometry (ITMS). Samples of P. lentiscus L. were harvested between April and October to study the seasonal chemical variability of the EO. A total of 45 compounds accounting for 97.5-98.4% of the total EO were identified, and the major compounds were alpha-pinene (14.8-22.6%), beta-myrcene (1-19.4%), p-cymene (1.6-16.2%), and terpinen-4-ol (14.2-28.3%). The yields of EO (v/dry w) ranged between 0.09 and 0.32%. Similar content of the major compounds was found in samples from different origins and seasonal variability was also observed. The EOs were tested for their antifungal activity against Aspergillus flavus, Rhizoctonia solani, Penicillium commune, Fusarium oxysporum. Two samples were weakly effective against Aspergillus flavus. Furthermore, terpinenol and alpha-terpineol, two of the major components of EO of Pistacia lentiscus L., totally inhibited the mycelian growth of A. flavus. Quite good antioxidant activity of the EO was also found.

  13. Electrically active bioceramics: a review of interfacial responses.

    PubMed

    Baxter, F R; Bowen, C R; Turner, I G; Dent, A C E

    2010-06-01

    Electrical potentials in mechanically loaded bone have been implicated as signals in the bone remodeling cycle. Recently, interest has grown in exploiting this phenomenon to develop electrically active ceramics for implantation in hard tissue which may induce improved biological responses. Both polarized hydroxyapatite (HA), whose surface charge is not dependent on loading, and piezoelectric ceramics, which produce electrical potentials under stress, have been studied in order to determine the possible benefits of using electrically active bioceramics as implant materials. The polarization of HA has a positive influence on interfacial responses to the ceramic. In vivo studies of polarized HA have shown polarized samples to induce improvements in bone ingrowth. The majority of piezoelectric ceramics proposed for implant use contain barium titanate (BaTiO(3)). In vivo and in vitro investigations have indicated that such ceramics are biocompatible and, under appropriate mechanical loading, induce improved bone formation around implants. The mechanism by which electrical activity influences biological responses is yet to be clearly defined, but is likely to result from preferential adsorption of proteins and ions onto the polarized surface. Further investigation is warranted into the use of electrically active ceramics as the indications are that they have benefits over existing implant materials.

  14. Oral anti-inflammatory activity of cannabidiol, a non-psychoactive constituent of cannabis, in acute carrageenan-induced inflammation in the rat paw.

    PubMed

    Costa, Barbara; Colleoni, Mariapia; Conti, Silvia; Parolaro, Daniela; Franke, Chiara; Trovato, Anna Elisa; Giagnoni, Gabriella

    2004-03-01

    Cannabidiol, the major non-psychoactive component of marijuana, has various pharmacological actions of clinical interest. It is reportedly effective as an anti-inflammatory and anti-arthritic in murine collagen-induced arthritis. The present study examined the anti-inflammatory and anti-hyperalgesic effects of cannabidiol, administered orally (5-40 mg/kg) once a day for 3 days after the onset of acute inflammation induced by intraplantar injection of 0.1 ml carrageenan (1% w/v in saline) in the rat. At the end of the treatment prostaglandin E2 (PGE2) was assayed in the plasma, and cyclooxygenase (COX) activity, production of nitric oxide (NO; nitrite/nitrate content), and of other oxygen-derived free radicals (malondialdehyde) in inflamed paw tissues. All these markers were significantly increased following carrageenan. Thermal hyperalgesia, induced by carrageenan and assessed by the plantar test, lasted 7 h. Cannabidiol had a time- and dose-dependent anti-hyperalgesic effect after a single injection. Edema following carrageenan peaked at 3 h and lasted 72 h; a single dose of cannabidiol reduced edema in a dose-dependent fashion and subsequent daily doses caused further time- and dose-related reductions. There were decreases in PGE2 plasma levels, tissue COX activity, production of oxygen-derived free radicals, and NO after three doses of cannabidiol. The effect on NO seemed to depend on a lower expression of the endothelial isoform of NO synthase. In conclusion, oral cannabidiol has a beneficial action on two symptoms of established inflammation: edema and hyperalgesia.

  15. Focused-ion-beam-fabricated Au nanorods coupled with Ag nanoparticles used as surface-enhanced Raman scattering-active substrate for analyzing trace melamine constituents in solution.

    PubMed

    Sivashanmugan, Kundan; Liao, Jiunn-Der; Liu, Bernard Haochih; Yao, Chih-Kai

    2013-10-24

    A well-ordered Au-nanorod array with a controlled tip ring diameter (Au_NRsd) was fabricated using the focused ion beam method. Au_NRsd was then coupled with Ag nanoparticles (Ag NPs) to bridge the gaps among Au nanorods. The effect of surface-enhanced Raman scattering (SERS) on Au_NRsd and Ag NPs/Au_NRsd was particularly verified using crystal violet (CV) as the molecular probe. Raman intensity obtained from a characteristic peak of CV on Au_NRsd was estimated by an enhancement factor of ≈10(7) in magnitude, which increased ≈10(12) in magnitude for that on Ag NPs/Au_NRsd. A highly SERS-active Ag NPs/Au_NRsd was furthermore applied for the detection of melamine (MEL) at very low concentrations. Raman-active peaks of MEL (10(-3) to 10(-12)M) in water or milk solution upon Au_NRsd or Ag NPs/Au_NRsd were well distinguished. The peaks at 680 and 702 cm(-1) for MEL molecules were found suitable to be used as the index for sensing low-concentration MEL in a varied solution, while that at 1051 cm(-1) was practical to interpret MEL molecules in water or milk solution bonded with Au (i.e., Au_NRsd) or Ag (i.e., Ag NPs/Au_NRsd) surface. At the interface of Ag NPs/Au_NRsd and MEL molecules in milk solution, a laser-induced electromagnetic field or hotspot effect was produced and competent to sense low-concentration MEL molecules interacting with Ag and Au surfaces. Accordingly, Ag NPs/Au_NRsd is very promising to be used as a fast and sensitive tool for screening MEL in complex matrices such as adulteration in e.g., food and pharmaceutical products.

  16. Response Activation in Overlapping Tasks and the Response-Selection Bottleneck

    ERIC Educational Resources Information Center

    Schubert, Torsten; Fischer, Rico; Stelzel, Christine

    2008-01-01

    The authors investigated the impact of response activation on dual-task performance by presenting a subliminal prime before the stimulus in Task 2 (S2) of a psychological refractory period (PRP) task. Congruence between prime and S2 modulated the reaction times in Task 2 at short stimulus onset asynchrony despite a PRP effect. This Task 2…

  17. Antiproliferative activity and induction of apoptosis in human colon cancer cells treated in vitro with constituents of a product derived from Pistacia lentiscus L. var. chia.

    PubMed

    Balan, K V; Prince, J; Han, Z; Dimas, K; Cladaras, M; Wyche, J H; Sitaras, N M; Pantazis, P

    2007-04-01

    In this report, we demonstrate that a 50% ethanol extract of the plant-derived product, Chios mastic gum (CMG), contains compounds which inhibit proliferation and induce death of HCT116 human colon cancer cells in vitro. CMG-treatment induces cell arrest at G(1), detachment of the cells from the substrate, activation of pro-caspases-8, -9 and -3, and causes several morphological changes typical of apoptosis in cell organelles. These events, furthermore, are time- and dose-dependent, but p53- and p21-independent. Apoptosis induction by CMG is not inhibited in HCT116 cell clones expressing high levels of the anti-apoptotic protein, Bcl-2, or dominant-negative FADD, thereby indicating that CMG induces cell death via a yet-to-be identified pathway, unrelated to the death receptor- and mitochondrion-dependent pathways. The findings presented here suggest that CMG (a) induces an anoikis form of cell death in HCT116 colon cancer cells that includes events associated with caspase-dependent pathways; and (b) might be developed into a chemotherapeutic agent for the treatment of human colon and other cancers.

  18. Collateral response to activation of potassium channels in vivo.

    PubMed

    Lamping, K G

    1998-04-01

    Activation of ATP-sensitive K+ channels is involved in the coronary vascular response to decreases in perfusion pressure and ischemia. Since activation of ATP-sensitive K+ channels in collateral vessels may be important in determining flow to collateral-dependent myocardium, the ability of collaterals to respond to activation of the channel was tested. In the beating heart of dogs, we compared responses of non-collaterals less than 100 microns in diameter to collaterals of similar size using computer-controlled stroboscopic epi-illumination of the left ventricle coupled to a microscope-video system. Aprikalim, a selective activator of ATP-sensitive K+ channels (0.1-10 microM) produced similar dose-dependent dilation of non-collaterals and collaterals. Relaxation was decreased by inhibition of ATP-sensitive K+ channels with glibenclamide, but not by inhibition of nitric oxide synthase with nitro-L-arginine. Bradykinin (10-100 microM) produced similar dilation of non-collaterals and collaterals which was decreased by nitro-L-arginine but not glibenclamide. Thus, in microvascular collaterals, relaxation to both nitric oxide and activation of ATP-sensitive K+ channels is similar to non-collaterals.

  19. Reduced brain activation in violent adolescents during response inhibition.

    PubMed

    Qiao, Yi; Mei, Yi; Du, XiaoXia; Xie, Bin; Shao, Yang

    2016-02-18

    Deficits in inhibitory control have been linked to aggression and violent behaviour. This study aimed to observe whether violent adolescents show different brain activation patterns during response inhibition and to ascertain the roles these brain regions play. A self-report method and modified overt aggression scale (MOAS) were used to evaluate violent behaviour. Functional magnetic resonance imaging was performed in 22 violent adolescents and 17 matched healthy subjects aged 12 to 18 years. While scanning, a go/no-go task was performed. Between-group comparisons revealed that activation in the bilateral middle and superior temporal gyrus, hippocampus, and right orbitofrontal area (BA11) regions were significantly reduced in the violent group compared with the control group. Meanwhile, the violent group had more widespread activation in the prefrontal cortex than that observed in the control group. Activation of the prefrontal cortex in the violent group was widespread but lacking in focus, failing to produce intensive activation in some functionally related regions during response inhibition.

  20. Effects of three activities on annoyance responses to recorded flyovers

    NASA Technical Reports Server (NTRS)

    Gunn, W. J.; Shepherd, W. T.; Fletcher, J. L.

    1975-01-01

    Subjects participated in an experiment in which they were engaged in TV viewing, telephone listening, or reverie (no activity) for a 1/2-hour session. During the session, they were exposed to a series of recorded aircraft sounds at the rate of one flight every 2 minutes. Within each session, four levels of flyover noise, separated by 5dB increments, were presented several times in a Latin Square balanced sequence. The peak level of the noisiest flyover in any session was fixed at 95, 90, 85, 75, or 70 dBA. At the end of the test session, subjects recorded their responses to the aircraft sounds, using a bipolar scale which covered the range from 'very pleasant' to 'extremely annoying'. Responses to aircraft noises were found to be significantly affected by the particular activity in which the subjects were engaged. Furthermore, not all subjects found the aircraft sounds to be annoying.

  1. Innate response activator B cells: origins and functions

    PubMed Central

    Swirski, Filip K.

    2015-01-01

    Innate response activator (IRA) B cells are a subset of B-1a derived B cells that produce the growth factors granulocyte macrophage colony stimulating factor and IL-3. In mouse models of sepsis and pneumonia, B-1a B cells residing in serosal sites recognize bacteria, migrate to the spleen or lung, and differentiate to IRA B cells that then contribute to the host response by amplifying inflammation and producing polyreactive IgM. In atherosclerosis, IRA B cells accumulate in the spleen, where they promote extramedullary hematopoiesis and activate classical dendritic cells. In this review, we focus on the ontogeny and function of IRA B cells in acute and chronic inflammation. PMID:25957266

  2. Vestibular Activation Habituates the Vasovagal Response in the Rat

    PubMed Central

    Cohen, Bernard; Martinelli, Giorgio P.; Xiang, Yongqing; Raphan, Theodore; Yakushin, Sergei B.

    2017-01-01

    Vasovagal syncope is a significant medical problem without effective therapy, postulated to be related to a collapse of baroreflex function. While some studies have shown that repeated static tilts can block vasovagal syncope, this was not found in other studies. Using anesthetized, male Long–Evans rats that were highly susceptible to generation of vasovagal responses, we found that repeated activation of the vestibulosympathetic reflex (VSR) with ±2 and ±3 mA, 0.025 Hz sinusoidal galvanic vestibular stimulation (sGVS) caused incremental changes in blood pressure (BP) and heart rate (HR) that blocked further generation of vasovagal responses. Initially, BP and HR fell ≈20–50 mmHg and ≈20–50 beats/min (bpm) into a vasovagal response when stimulated with Sgv\\S in susceptible rats. As the rats were continually stimulated, HR initially rose to counteract the fall in BP; then the increase in HR became more substantial and long lasting, effectively opposing the fall in BP. Finally, the vestibular stimuli simply caused an increase in BP, the normal sequence following activation of the VSR. Concurrently, habituation caused disappearance of the low-frequency (0.025 and 0.05 Hz) oscillations in BP and HR that must be present when vasovagal responses are induced. Habituation also produced significant increases in baroreflex sensitivity (p < 0.001). Thus, repeated low-frequency activation of the VSR resulted in a reduction and loss of susceptibility to development of vasovagal responses in rats that were previously highly susceptible. We posit that reactivation of the baroreflex, which is depressed by anesthesia and the disappearance of low-frequency oscillations in BP and HR are likely to be critically involved in producing resistance to the development of vasovagal responses. SGVS has been widely used to activate muscle sympathetic nerve activity in humans and is safe and well tolerated. Potentially, it could be used to produce similar habituation of

  3. Photodynamic therapy for cancer and activation of immune response

    NASA Astrophysics Data System (ADS)

    Mroz, Pawel; Huang, Ying-Ying; Hamblin, Michael R.

    2010-02-01

    Anti-tumor immunity is stimulated after PDT for cancer due to the acute inflammatory response, exposure and presentation of tumor-specific antigens, and induction of heat-shock proteins and other danger signals. Nevertheless effective, powerful tumor-specific immune response in both animal models and also in patients treated with PDT for cancer, is the exception rather than the rule. Research in our laboratory and also in others is geared towards identifying reasons for this sub-optimal immune response and discovering ways of maximizing it. Reasons why the immune response after PDT is less than optimal include the fact that tumor-antigens are considered to be self-like and poorly immunogenic, the tumor-mediated induction of CD4+CD25+foxP3+ regulatory T-cells (T-regs), that are able to inhibit both the priming and the effector phases of the cytotoxic CD8 T-cell anti-tumor response and the defects in dendritic cell maturation, activation and antigen-presentation that may also occur. Alternatively-activated macrophages (M2) have also been implicated. Strategies to overcome these immune escape mechanisms employed by different tumors include combination regimens using PDT and immunostimulating treatments such as products obtained from pathogenic microorganisms against which mammals have evolved recognition systems such as PAMPs and toll-like receptors (TLR). This paper will cover the use of CpG oligonucleotides (a TLR9 agonist found in bacterial DNA) to reverse dendritic cell dysfunction and methods to remove the immune suppressor effects of T-regs that are under active study.

  4. Suppression of inflammatory reactions by terpinen-4-ol, a main constituent of tea tree oil, in a murine model of oral candidiasis and its suppressive activity to cytokine production of macrophages in vitro.

    PubMed

    Ninomiya, Kentaro; Hayama, Kazumi; Ishijima, Sanae A; Maruyama, Naho; Irie, Hiroshi; Kurihara, Junichi; Abe, Shigeru

    2013-01-01

    The onset of oral candidiasis is accompanied by inflammatory symptoms such as pain in the tongue, edema or tissue damage and lowers the quality of life (QOL) of the patient. In a murine oral candidiasis model, the effects were studied of terpinen-4-ol (T-4-ol), one of the main constituents of tea tree oil, Melaleuca alternifolia, on inflammatory reactions. When immunosuppressed mice were orally infected with Candida albicans, their tongues showed inflammatory symptoms within 24 h after the infection, which was monitored by an increase of myeloperoxidase activity and macrophage inflammatory protein-2 in their tongue homogenates. Oral treatment with 50 µL of 40 mg/mL terpinen-4-ol 3h after the Candida infection clearly suppressed the increase of these inflammatory parameters. In vitro analysis of the effects of terpinen-4-ol on cytokine secretion of macrophages indicated that 800 µg/mL of this substance significantly inhibited the cytokine production of the macrophages cultured in the presence of heat-killed C. albicans cells. Based on these findings, the role of the anti-inflammatory action of T-4-ol in its therapeutic activity against oral candidiasis was discussed.

  5. Viruses and the DNA Damage Response: Activation and Antagonism.

    PubMed

    Luftig, Micah A

    2014-11-01

    Viruses must interact with their hosts in order to replicate; these interactions often provoke the evolutionarily conserved response to DNA damage, known as the DNA damage response (DDR). The DDR can be activated by incoming viral DNA, during the integration of retroviruses, or in response to the aberrant DNA structures generated upon replication of DNA viruses. Furthermore, DNA and RNA viral proteins can induce the DDR by promoting inappropriate S phase entry, by modifying cellular DDR factors directly, or by unintentionally targeting host DNA. The DDR may be antiviral, although viruses often require proximal DDR activation of repair and recombination factors to facilitate replication as well as downstream DDR signaling suppression to ensure cell survival. An unintended consequence of DDR attenuation during infection is the long-term survival and proliferation of precancerous cells. Therefore, the molecular basis for DDR activation and attenuation by viruses remains an important area of study that will likely provide key insights into how viruses have evolved with their hosts.

  6. Activation of the DNA Damage Response by RNA Viruses

    PubMed Central

    Ryan, Ellis L.; Hollingworth, Robert; Grand, Roger J.

    2016-01-01

    RNA viruses are a genetically diverse group of pathogens that are responsible for some of the most prevalent and lethal human diseases. Numerous viruses introduce DNA damage and genetic instability in host cells during their lifecycles and some species also manipulate components of the DNA damage response (DDR), a complex and sophisticated series of cellular pathways that have evolved to detect and repair DNA lesions. Activation and manipulation of the DDR by DNA viruses has been extensively studied. It is apparent, however, that many RNA viruses can also induce significant DNA damage, even in cases where viral replication takes place exclusively in the cytoplasm. DNA damage can contribute to the pathogenesis of RNA viruses through the triggering of apoptosis, stimulation of inflammatory immune responses and the introduction of deleterious mutations that can increase the risk of tumorigenesis. In addition, activation of DDR pathways can contribute positively to replication of viral RNA genomes. Elucidation of the interactions between RNA viruses and the DDR has provided important insights into modulation of host cell functions by these pathogens. This review summarises the current literature regarding activation and manipulation of the DDR by several medically important RNA viruses. PMID:26751489

  7. Identification of antibacterial constituents from the indigenous Australian medicinal plant Eremophila duttonii F. Muell. (Myoporaceae).

    PubMed

    Smith, Joshua E; Tucker, David; Watson, Kenneth; Jones, Graham Lloyd

    2007-06-13

    This paper reports on the isolation and identification of antibacterial constituents from the indigenous Australian medicinal plant Eremophila duttonii F. Muell. (Myoporaceae). Preparations derived from this plant are used by indigenous populations in the topical treatment of minor wounds, otitis and ocular complaints, and as a gargle for sore throat. Several authors have reported extracts of this plant to effect rapid bacteriolysis and inhibit growth of a wide range of Gram-positive micro-organisms. In other studies involving screening of native medicinal plants for antibacterial activity, extracts of Eremophila duttonii have been reported to consistently exhibit the highest potency amongst all species included. From a hexane extract, we identified two diterpenes of the serrulatane class, the principal constituents responsible for antibacterial activity and present as major constituents of the resinous leaf cuticle: serrulat-14-en-7,8,20-triol (1) and serrulat-14-en-3,7,8,20-tetraol (2). In addition, a hydroxylated furanosesquiterpene with mild antibacterial activity which appeared to be a novel compound was isolated from the extract and tentatively identified as 4-hydroxy-4-methyl-1-(2,3,4,5-tetrahydro-5-methyl[2,3'-bifuran]-5-yl) pentan-2-one. Minimum inhibitory concentrations for each of the compounds against three Gram-positive bacteria: Staphylococcus aureus (ATCC 29213), Staphylococcus epidermidis (ATCC 12228) and Streptococcus pneumoniae (ARL 10582), were determined using a micro-titre plate broth dilution assay.

  8. Placebo-Activated Neural Systems are Linked to Antidepressant Responses

    PubMed Central

    Peciña, Marta; Bohnert, Amy S. B.; Sikora, Magdalena; Avery, Erich T.; Langenecker, Scott A.; Mickey, Brian J.; Zubieta, Jon-Kar

    2016-01-01

    Importance High placebo responses have been observed across a wide range of pathologies, severely impacting drug development. Objective Here we examined neurochemical mechanisms underlying the formation of placebo effects in patients with Major Depressive Disorder (MDD). Participants Thirty-five medication-free MDD patients. Design and Intervention We performed a single-blinded two-week cross-over randomized controlled trial of two identical oral placebos (described as having either “active” or “inactive” fast-acting antidepressant-like effects) followed by a 10-week open-label treatment with a selective serotonin reuptake inhibitor (SSRI) or in some cases, another agent as clinically indicated. The volunteers were studied with PET and the μ-opioid receptor (MOR)-selective radiotracer [11C]carfentanil after each 1-week “inactive” and “active” oral placebo treatment. In addition, 1 mL of isotonic saline was administered intravenously (i.v.) within sight of the volunteer during PET scanning every 4 min over 20 min only after the 1-week active placebo treatment, with instructions that the compound may be associated with the activation of brain systems involved in mood improvement. This challenge stimulus was utilized to test the individual capacity to acutely activate endogenous opioid neurotransmision under expectations of antidepressant effect. Setting A University Health System. Main Outcomes and Measures Changes in depressive symptoms in response to “active” placebo and antidepressant. Baseline and activation measures of MOR binding. Results Higher baseline MOR binding in the nucleus accumbens (NAc) was associated with better response to antidepressant treatment (r=0.48; p=0.02). Reductions in depressive symptoms after 1-week of “active” placebo treatment, compared to the “inactive”, were associated with increased placebo-induced μ-opioid neurotransmission in a network of regions implicated in emotion, stress regulation, and the

  9. Corporate responsibility for childhood physical activity promotion in the UK.

    PubMed

    Leone, Liliana; Ling, Tom; Baldassarre, Laura; Barnett, Lisa M; Capranica, Laura; Pesce, Caterina

    2016-12-01

    The alarming epidemic of obesity and physical inactivity at paediatric age urges societies to rise to the challenge of ensuring an active lifestyle. As one response to this, business enterprises are increasingly engaged in promoting sport and physical activity (PA) initiatives within the frame of corporate social responsibility (CSR). However, comparative analyses among industry sectors of CSR strategies for PA promotion with a particular focus on children are still lacking. This study aimed to explore (i) what are the CSR strategies for PA promotion adopted in different industry sectors and (ii) whether corporate engagement in promoting PA for children is supportive of children's rights to play and be physically active. Corporate pledges pertaining to CSR initiatives to promote PA were analysed. The hypothesis was that companies from different sectors employ different CSR strategies and that companies with a higher profile as regard to public health concerns for children tend to legitimate their action by adopting a compensatory strategy. Results show that the issue of PA promotion is largely represented within CSR commitments. CSR strategies for PA promotion vary across industry sectors and the adoption of a compensatory strategy for rising childhood obesity allows only a limited exploitation of the potential of CSR commitments for the provision of children's rights to play and be physically active. Actors within the fields of public health ethics, human rights and CSR should be considered complementary to develop mainstreaming strategies and improve monitoring systems of PA promotion in children.

  10. Cinobufagin Modulates Human Innate Immune Responses and Triggers Antibacterial Activity

    PubMed Central

    Xie, Shanshan; Spelmink, Laura; Codemo, Mario; Subramanian, Karthik; Pütsep, Katrin

    2016-01-01

    The traditional Chinese medicine Chan-Su is widely used for treatment of cancer and cardiovascular diseases, but also as a remedy for infections such as furunculosis, tonsillitis and acute pharyngitis. The clinical use of Chan-Su suggests that it has anti-infective effects, however, the mechanism of action is incompletely understood. In particular, the effect on the human immune system is poorly defined. Here, we describe previously unrecognized immunomodulatory activities of cinobufagin (CBG), a major bioactive component of Chan-Su. Using human monocyte-derived dendritic cells (DCs), we show that LPS-induced maturation and production of a number of cytokines was potently inhibited by CBG, which also had a pro-apoptotic effect, associated with activation of caspase-3. Interestingly, CBG triggered caspase-1 activation and significantly enhanced IL-1β production in LPS-stimulated cells. Finally, we demonstrate that CBG upregulates gene expression of the antimicrobial peptides (AMPs) hBD-2 and hBD-3 in DCs, and induces secretion of HNP1-3 and hCAP-18/LL-37 from neutrophils, potentiating neutrophil antibacterial activity. Taken together, our data indicate that CBG modulates the inflammatory phenotype of DCs in response to LPS, and triggers an antibacterial innate immune response, thus proposing possible mechanisms for the clinical effects of Chan-Su in anti-infective therapy. PMID:27529866

  11. Infrared measurements of atmospheric constituents

    NASA Technical Reports Server (NTRS)

    Murcray, David G.; Murcray, Frank J.; Goldman, Aaron; Rinsland, Curtis P.; Camy-Peyret, C.; Flaud, J. M.

    1990-01-01

    The objective of this program is to obtain data concerning the concentration versus altitude of various constituents of interest in the photochemistry of the stratospheric ozone layer. Data pertinent to this objective are obtained using balloon-borne instruments to measure the atmospheric transmission and emission in the mid infrared. In addition to obtaining constituent profile information, the spectral data obtained are also used to identify absorption or emission features which may interfere with the retrieval of constituent data from satellite instruments using lower spectral resolution. The spectral resolution obtained with the solar spectral system is 0.0025 cm(exp -1) and represents about a factor of 5 greater resolution than any solar spectra previously obtained in this spectral region. As a result of the increase in spectral resolution, a large number of features are observed in these spectra which were not observed in previous studies. Identification and analysis of these features is in progress. The results of this analysis to date shows a number of HNO3 features which have not been observed before, and these occur where they will interfere with the retrieval of other constituents. An example of the interference is the occurrence of features in the 780.2 cm(exp -1) region which overlap the ClONO2 feature which will be used for retrieval of ClONO2 by the CLAES instrument on UARS. A number of features due to COF2 were also identified in the 1250 cm(exp -1) region which may interfere with retrieval of N2O5.

  12. Emotion potentiates response activation and inhibition in masked priming

    PubMed Central

    Bocanegra, Bruno R.; Zeelenberg, René

    2012-01-01

    Previous studies have shown that emotion can have 2-fold effects on perception. At the object-level, emotional stimuli benefit from a stimulus-specific boost in visual attention at the relative expense of competing stimuli. At the visual feature-level, recent findings indicate that emotion may inhibit the processing of small visual details and facilitate the processing of coarse visual features. In the present study, we investigated whether emotion can boost the activation and inhibition of automatic motor responses that are generated prior to overt perception. To investigate this, we tested whether an emotional cue affects covert motor responses in a masked priming task. We used a masked priming paradigm in which participants responded to target arrows that were preceded by invisible congruent or incongruent prime arrows. In the standard paradigm, participants react faster, and commit fewer errors responding to the directionality of target arrows, when they are preceded by congruent vs. incongruent masked prime arrows (positive congruency effect, PCE). However, as prime-target SOAs increase, this effect reverses (negative congruency effect, NCE). These findings have been explained as evidence for an initial activation and a subsequent inhibition of a partial response elicited by the masked prime arrow. Our results show that the presentation of fearful face cues, compared to neutral face cues, increased the size of both the PCE and NCE, despite the fact that the primes were invisible. This is the first demonstration that emotion prepares an individual's visuomotor system for automatic activation and inhibition of motor responses in the absence of visual awareness. PMID:23162447

  13. Sensor web enables rapid response to volcanic activity

    USGS Publications Warehouse

    Davies, Ashley G.; Chien, Steve; Wright, Robert; Miklius, Asta; Kyle, Philip R.; Welsh, Matt; Johnson, Jeffrey B.; Tran, Daniel; Schaffer, Steven R.; Sherwood, Robert

    2006-01-01

    Rapid response to the onset of volcanic activity allows for the early assessment of hazard and risk [Tilling, 1989]. Data from remote volcanoes and volcanoes in countries with poor communication infrastructure can only be obtained via remote sensing [Harris et al., 2000]. By linking notifications of activity from ground-based and spacebased systems, these volcanoes can be monitored when they erupt.Over the last 18 months, NASA's Jet Propulsion Laboratory (JPL) has implemented a Volcano Sensor Web (VSW) in which data from ground-based and space-based sensors that detect current volcanic activity are used to automatically trigger the NASA Earth Observing 1 (EO-1) spacecraft to make highspatial-resolution observations of these volcanoes.

  14. A Paradox of Syntactic Priming: Why Response Tendencies Show Priming for Passives, and Response Latencies Show Priming for Actives

    PubMed Central

    Segaert, Katrien; Menenti, Laura; Weber, Kirsten; Hagoort, Peter

    2011-01-01

    Speakers tend to repeat syntactic structures across sentences, a phenomenon called syntactic priming. Although it has been suggested that repeating syntactic structures should result in speeded responses, previous research has focused on effects in response tendencies. We investigated syntactic priming effects simultaneously in response tendencies and response latencies for active and passive transitive sentences in a picture description task. In Experiment 1, there were priming effects in response tendencies for passives and in response latencies for actives. However, when participants' pre-existing preference for actives was altered in Experiment 2, syntactic priming occurred for both actives and passives in response tendencies as well as in response latencies. This is the first investigation of the eff