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1

Furofuran lignans display schistosomicidal and trypanocidal activities.  

PubMed

Parasitic diseases continue to be a major worldwide health problem, and there is an urgent need for development of therapeutic drugs. This paper describes synthesis of dehydrodiferulic acid dilactone 1 and dehydrodisinapic acid dilactone 2 furofuran lignans by oxidative coupling of ferulic and sinapic acids, respectively. Their schistosomicidal, trypanocidal, and leishmanicidal activities were evaluated in vitro against Schistosoma mansoni adult worms, trypomastigote and amastigotes forms of Trypanosoma cruzi, and promastigote forms of Leishmania amazonensis. Compound 1 did not display significant schistosomicidal activity, but it presented potent trypanocidal activity, since it induced death of trypomastigotes and amastigotes with IC50/24h of 9.3?M and 7.3?M, respectively. Compound 2 had slight trypanocidal and schistosomicidal activities. None of the compounds were active against L. amazonensis. These results demonstrated that furofuran lignans are potentially useful for anti-parasitic drugs development and should be further investigated. PMID:25200100

Andrade e Silva, Márcio Luis; Esperandim, Viviane Rodrigues; Ferreira, Daniele da Silva; Magalhăes, Lizandra Guidi; Lima, Thais Coelho; Cunha, Wilson Roberto; Nanayakkara, Dhammika N P; Pereira, Ana Carolina; Bastos, Jairo Kenupp

2014-11-01

2

A new schistosomicidal and antioxidative phenylpropanoid from Astragalus englerianus.  

PubMed

A new phenylpropanoid, (E)-2,3,4-trimethoxy-5-(1-propenyl)phenol (1), along with five known aromatic compounds (2-6), was isolated from the methanol extract of roots of Astragalus englerianus. Their structures were elucidated based on the analyses of extensive spectroscopic data and comparison of their physicochemical properties. Compounds 1 and 2 were evaluated schistosomicidal activities, and all the isolated compounds were tested for their antioxidant activities in vitro. Compound 1 showed significant schistosomicidal activity with worm mortality rates of 66.7% and 83.3% within 12 and 24 h in a drug-containing (1.16 mM) RPMI 1640 medium, respectively. Also, compound 1 exhibited excellent antioxidant activity (2,2-diphenyl-1-(2,4,6-trinitrophenyl)hydrazyl free radical-scavenging capability) with an IC50 value of 81.3 ± 1.3 ?M. PMID:25391647

Xiao, Chao-Jiang; Zhang, Yu; Qiu, Lin; Xu, Wei; Zhao, Ming-Zao; Dong, Xiang; Jiang, Bei

2014-11-12

3

Schistosomicidal and Antioxidant Flavonoids from Astragalus englerianus.  

PubMed

Astragalus englerianus is a close relative of the traditional Chinese medicine plant Radix Astragali (Huang-qi) and is mainly distributed in Yunnan. It has been traditionally used as a substitute of "Huang-qi" for reducing fatigue and enhancing immunity by local folks. A phytochemical study of the methanol extract of the roots led to the isolation of three new flavonoids including one aurone (1) and two chalcones (2 and 3), as well as two known flavonoids (4 and 5). Their structures were elucidated based on the analyses of extensive spectroscopic data and comparison of their physicochemical properties. This is the first report on the occurrence of ?-hydroxydihydrochalcone, 2',5'-dioxygenchalcones, and 2',5'-dioxygenaurone in the genus Astragalus. All the isolated compounds were tested in vitro for their schistosomicidal and antioxidant activities. Compounds 2 and 4 showed schistosomicidal activities with worm mortality rates of 100?% within 12?h in a drug-containing (0.70 and 0.77?mM, respectively) RPMI 1640 medium. Compounds 1 and 2 exhibited antioxidant activities in 2,2-diphenyl-1-(2,4,6-trinitrophenyl)hydrazyl free radical scavenging assays, with IC50 values of 35.9?±?1.1 and 12.2?±?1.1?µM, respectively. PMID:25371983

Xiao, Chao-Jiang; Zhang, Yu; Qiu, Lin; Dong, Xiang; Jiang, Bei

2014-12-01

4

In Vitro and In Vivo Anti-Schistosomal Activity of the Alkylphospholipid Analog Edelfosine  

PubMed Central

Background Schistosomiasis is a parasitic disease caused by trematodes of the genus Schistosoma. Five species of Schistosoma are known to infect humans, out of which S. haematobium is the most prevalent, causing the chronic parasitic disease schistosomiasis that still represents a major problem of public health in many regions of the world and especially in tropical areas, leading to serious manifestations and mortality in developing countries. Since the 1970s, praziquantel (PZQ) is the drug of choice for the treatment of schistosomiasis, but concerns about relying on a single drug to treat millions of people, and the potential appearance of drug resistance, make identification of alternative schistosomiasis chemotherapies a high priority. Alkylphospholipid analogs (APLs), together with their prototypic molecule edelfosine (EDLF), are a family of synthetic antineoplastic compounds that show additional pharmacological actions, including antiparasitic activities against several protozoan parasites. Methodology/Principal Findings We found APLs ranked edelfosine> perifosine> erucylphosphocholine> miltefosine for their in vitro schistosomicidal activity against adult S. mansoni worms. Edelfosine accumulated mainly in the worm tegument, and led to tegumental alterations, membrane permeabilization, motility impairment, blockade of male-female pairing as well as induction of apoptosis-like processes in cells in the close vicinity to the tegument. Edelfosine oral treatment also showed in vivo schistosomicidal activity and decreased significantly the egg burden in the liver, a key event in schistosomiasis. Conclusions/Significance Our data show that edelfosine is the most potent APL in killing S. mansoni adult worms in vitro. Edelfosine schistosomicidal activity seems to depend on its action on the tegumental structure, leading to tegumental damage, membrane permeabilization and apoptosis-like cell death. Oral administration of edelfosine diminished worm and egg burdens in S. mansoni-infected CD1 mice. Here we report that edelfosine showed promising antischistosomal properties in vitro and in vivo. PMID:25302497

Yepes, Edward; Varela-M, Rubén E.; López-Abán, Julio; Dakir, E. L. Habib; Mollinedo, Faustino; Muro, Antonio

2014-01-01

5

The schistosomicidal and toxic effects of some ??-di(p-aminophenoxy)alkanes and related monoamines  

PubMed Central

An account is given of the results obtained with a number of p-aminophenoxyalkanes which were examined for activity against Schistosoma mansoni in mice and for the presence of retinotoxicity in cats. The first compound to be found active, 1:5-di(p-aminophenoxy)-pentane dihydrochloride (M & B 968A), was modified in a variety of ways in an attempt to increase its activity and to eliminate its ocular effects. It was found that a p-aminophenoxyalkyl group was common to all the active compounds, but that the rest of the molecule could be any of several different groups, including alkoxy, phenoxy, and phenyl groups, without diminishing the activity. Although at least one p-aminophenoxyalkyl group was essential for schistosomicidal activity, ocular toxicity was also shown by a p-aminophenylalkyl derivative in which the ether linkage was absent. PMID:13584723

Collins, R. F.; Davis, M.; Edge, N. D.; Hill, J.

1958-01-01

6

Application and evaluation of a molecular approach for detection of the schistosomicidal effect of Mirazid® (myrrh) in the murine model  

PubMed Central

The conventional PCR technique was used for studying the schistosomicidal effect of Mirazid® in the murine model. Results of the molecular study were compared with the parasitological results (ova and worm count). The used PCR technique was more sensitive than the Kato-Katz thick smears. Mirazid® showed some schistosomicidal effects against murine Schistosoma mansoni. However, it was not efficient enough to cure any of the studied mice.

Lotfy, Wael M.; Nageh, Aly M.; Hussein, Neveen A.; Hassan, Ashraf A.

2012-01-01

7

Spotlight on the in vitro effect of artemisinin-naphthoquine phosphate on Schistosoma mansoni and its snail host Biomphalaria alexandrina.  

PubMed

Malaria and schistosomiasis are the two most important parasitic diseases in the tropics and sub-tropics with geographic overlap. Efforts have been made for developing new schistosomicidal drugs, or testing existing drugs originally used for non-related diseases. The antimalarial artemisinin-naphthoquine phosphate combination (CO-ArNp) was recently reported to be a promising novel antischistosomal therapy with potent in vivo activity against Schistosoma mansoni. In this work, we report the in vitro dose- and time-response effect of CO-ArNp against the Egyptian strain of S. mansoni, and its snail host, Biomphalaria alexandrina. Incubation of adult S. mansoni with CO-ArNp at 40 or 20?g/ml for 48 or 72h killed all worms. Exposure of S. mansoni miracidia and cercariae to the molluscicidal LC50 of CO-ArNp (16.8?g/ml) resulted in 100% mortality of the free larval stages within 90 and 15min, respectively. Moreover, incubation of adult B. alexandrina snails with this drug combination killed all snails at 40?g/ml within 24h. Scanning electron microscope revealed marked morphological and tegumental alterations on the different stages of the parasite and its snail soft tissue. Our study highlights the schistosomicidal and molluscicidal effects of artemisinin-naphthoquine phosphate. No doubt more studies are needed to clarify its potential value to control schistosomiasis. PMID:25291045

El-Beshbishi, Samar N; Bardicy, Samia El; Tadros, Menerva; Ayoub, Magda; Taman, Amira

2015-01-01

8

In vitro activity of penicillins against anaerobes.  

PubMed

The in vitro susceptibility of 162 anaerobic isolates from clinical material were tested to pencillin G, BL-P1654, and carbenicillin. Penicillin G and BL-P1654 showed good activity against Bacteroides fragilis, but only 60% of strains were susceptible to carbenicillin at achievable blood levels (128 mug/ml). PMID:1041215

Tally, F P; Jacobus, N V; Bartlett, J G; Gorbach, S L

1975-04-01

9

Anthelmintic activity of crude extract and essential oil of Tanacetum vulgare (Asteraceae) against adult worms of Schistosoma mansoni.  

PubMed

Schistosomiasis, a parasitic disease caused by trematode flatworms of the genus Schistosoma, affects more than 200 million people worldwide, and its control is dependent on a single drug, praziquantel. Tanacetum vulgare (Asteraceae) is used in folk medicine as a vermifuge. This study aimed to investigate the in vitro schistosomicidal activity of the crude extract (TV) and the essential oil (TV-EO) from the aerial parts of T. vulgare. TV-EO was obtained by hydrodistillation and analyzed by GC/MS, which allowed the identification of ?-thujone (84.13%) as the major constituent. TV and TV-EO, at 200 ?g/mL, decreased motor activity and caused 100% mortality of all adult worms. At 100 and 50 ?g/mL, only TV caused death of all adult worms, while TV-EO was inactive. TV (200 ?g/mL) was also able to reduce viability and decrease production of developed eggs. Confocal laser scanning microscopy showed morphological alterations in the tegument of the S. mansoni surface after incubation with TV (50 and 100 ?g/mL). Quantitative analysis on the schistosomes tegument showed that TV caused changes in the numbers of tubercles of S. mansoni male worms in a dose-dependent manner. The findings suggest that T. vulgare is a potential source of schistosomicidal compounds. PMID:24672320

Godinho, Loyana Silva; Aleixo de Carvalho, Lara Soares; Barbosa de Castro, Clarissa Campos; Dias, Mirna Meana; Pinto, Priscila de Faria; Crotti, Antônio Eduardo Miller; Pinto, Pedro Luiz Silva; de Moraes, Josué; Da Silva Filho, Ademar A

2014-01-01

10

In vitro activity of the EWS oncogene transcriptional activation domain.  

PubMed

Aberrant chromosomal fusion of the Ewings sarcoma oncogene (EWS) to several different cellular partners gives rise to the Ewing's family of oncogenic proteins [EWS fusion proteins (EFPs)] and associated tumors (EFTs). EFPs are potent transcriptional activators dependent on the N-terminal region of EWS [the EWS activation domain (EAD)], and this function is thought to be central to EFT oncogenesis and maintenance. Thus, EFPs are promising therapeutic targets, and detailed molecular studies of the EAD will be pivotal for exploring this potential. For many reasons, the molecular mechanism of EAD action is poorly understood and one major obstacle to progress is the lack of an in vitro transcription assay. Using well-characterized EAD-dependent activators and soluble nuclear extracts, we have attempted to recapitulate EAD transcriptional activity in vitro. We report that while the EAD activates transcription strongly in vitro, the effect of EAD mutations is strikingly different from that observed in vivo. Our results therefore suggest that crude soluble extracts do not support bona fide EAD activity in vitro, and we discuss our findings in relation to future assay development and potential mechanisms of EAD action. PMID:19290668

Ng, King Pan; Li, Kim K C; Lee, Kevin A W

2009-04-01

11

Acidosis activates complement system in vitro.  

PubMed

We investigated the in vitro effect of different forms of acidosis (pH 7.0) on the formation of anaphylatoxins C3a and C5a. Metabolic acidosis due to addition of hydrochloric acid (10 micromol/ml blood) or lactic acid (5.5 micromol/ml) to heparin blood (N=12) caused significant activation of C3a and C5a compared to control (both p=0.002). Respiratory acidosis activated C3a (p=0.007) and C5a (p=0.003) compared to normocapnic controls. Making blood samples with lactic acidosis hypocapnic resulted in a median pH of 7.37. In this respiratory compensated metabolic acidosis, C3a and C5a were not increased. These experiments show that acidosis itself and not lactate trigger for activation of complement components C3 and C5. PMID:9927235

Emeis, M; Sonntag, J; Willam, C; Strauss, E; Walka, M M; Obladen, M

1998-01-01

12

Original article In vitro cholesterol-lowering activity  

E-print Network

Original article In vitro cholesterol-lowering activity of Lactobacillus plantarum of these microorganisms. One of the most studied properties is the cholesterol-lowering activity of bacteria and five Lactobacillus paracasei strains isolated from cheese were studied in vitro for their cholesterol

Paris-Sud XI, Université de

13

In Vitro Evaluation of TLR4 Agonist Activity: Formulation Effects  

PubMed Central

Effective in vitro evaluation of vaccine adjuvants would allow higher throughput screening compared to in vivo studies. However, vaccine adjuvants comprise a wide range of structures and formulations ranging from soluble TLR agonists to complex lipid-based formulations. The effects of formulation parameters on in vitro bioactivity assays and the correlations with in vivo adjuvant activity is not well understood. In the present work, we employ the Limulus amebocyte lysate assay and a human macrophage cellular cytokine production assay to demonstrate the differences in in vitro bioactivity of four distinct formulations of the synthetic TLR4 agonist GLA: an aqueous nanosuspension (GLA-AF), an oil-in-water emulsion (GLA-SE), a liposome (GLA-LS), and an alum-adsorbed formulation (GLA-Alum). Furthermore, we demonstrate the importance of the localization of GLA on in vitro potency. By comparing to previous published reports on the in vivo bioactivity of these GLA-containing formulations, we conclude that the most potent activators of the in vitro systems may not be the most potent in vivo adjuvant formulations. Furthermore, we discuss the formulation considerations which should be taken into account when interpreting data from in vitro adjuvant activity assays. PMID:24121074

Misquith, Ayesha; Millie Fung, H. W.; Dowling, Quinton M.; Guderian, Jeffrey A.; Vedvick, Thomas S.; Fox, Christopher B.

2013-01-01

14

In vitro antioxidant activity of Anthriscus cerefolium L. (Hoffm.) extracts  

Microsoft Academic Search

Standardised aqueous extracts of chervil (Anthriscus cerefolium L. Hoffm.) (Apiacae) were investigated for antioxidant effect. Numerous in vitro test methods were used to determine whether the extracts, from different vegetative parts (root, herb) had H-donor, metal binding, reductive, free radical scavenging and membrane protective activity. Apiin was used as a reference material. The herb extract showed better activity in all

Szabolcs Fejes; Anna Blázovics; Andrea Lugasi; Éva Lemberkovics; Gizella Petri; Ágnes Kéry

2000-01-01

15

In Vitro Activity of Thimerosal against Ocular Pathogenic Fungi  

Microsoft Academic Search

The in vitro activity of thimerosal versus those of amphotericin B and natamycin was assessed against 244 ocular fungal isolates. The activity of thimerosal against Fusarium spp., Aspergillus spp., and Alternaria alternata was 256 times, 512 times, and 128 times, respectively, greater than that of natamycin and 64 times, 32 times, and 32 times, respectively, greater than that of amphotericin

Yan Xu; Guangren Pang; Dongqing Zhao; Chuanwen Gao; Lutan Zhou; Shengtao Sun; Bingliang Wang

2010-01-01

16

ASSESSMENT OF IN VITRO ANDROGENIC ACTIVITY IN KRAFT MILL EFFLUENT  

EPA Science Inventory

Detection of In Vitro Androgenic Activity in Feedlot Effluent. Lambright, CS 1 , Guillette, LJ, Jr.2, Gray, LE, Jr.1 , 1USEPA, NHEERL, RTP, NC, 2 University of Florida, Dept. of Zoology, Gainesville FL Recent studies have shown the presence of androgenic activity in water...

17

Peroxynitrite Decreases Rabbit Tissue Factor Activity In Vitro  

Microsoft Academic Search

Tissue factor (TF) is a primary initiator of physiological coagulation in vivo. Peroxynitrite (OONO), a molecule formed from nitric oxide (NO) and superoxide (O2 · ), decreases human TF activity in vitro. Coagulopathy has been associated with hepatoenteric ischemia- reperfusion known to involve formation of OONO. Further, circulating TF activity decreases in rabbits after hepatoenteric ischemia-reperfusion. We hypothesized that exposure

Vance G. Nielsen; John P. Crow

2004-01-01

18

In Vitro Activity of AR-709 against Streptococcus pneumoniae?  

PubMed Central

We investigated the in vitro activity of AR-709, a novel diaminopyrimidine antibiotic currently in development for treatment of community-acquired upper and lower respiratory tract infections, against 151 Streptococcus pneumoniae strains from various European countries. AR-709 showed excellent activity against both drug-susceptible and multidrug-resistant pneumococci. PMID:18180358

Jansen, W. T. M.; Verel, A.; Verhoef, J.; Milatovic, D.

2008-01-01

19

In vitro antibacterial activity of different clotrimazole formulations.  

PubMed

The antibacterial activity of two different clotrimazole formulations was tested in vitro. A neutral vaginal tablet with 100 mg active ingredient has a partial bactericidal effect on gram-positive bacteria. A new formula containing 500 mg clotrimazole and lactic acid, designed for a one-dose therapy of vulvovaginal mycoses, shows an improved bactericidal activity against gram-positive bacteria and, owing to the lactic acid content, a broad bactericidal effect on gram-negative species. PMID:7160238

Schaller, K

1982-01-01

20

In Vitro Antibacterial Activity of Essential Oils against Streptococcus pyogenes  

PubMed Central

Streptococcus pyogenes plays an important role in the pathogenesis of tonsillitis. The present study was conducted to evaluate the in vitro antibacterial activities of 18 essential oils chemotypes from aromatic medicinal plants against S. pyogenes. Antibacterial activity of essential oils was investigated using disc diffusion method. Minimum Inhibitory Concentration of essential oils showing an important antibacterial activity was measured using broth dilution method. Out of 18 essential oils tested, 14 showed antibacterial activity against S. pyogenes. Among them Cinnamomum verum, Cymbopogon citratus, Thymus vulgaris CT thymol, Origanum compactum, and Satureja montana essential oils exhibited significant antibacterial activity. The in vitro results reported here suggest that, for patients suffering from bacterial throat infections, if aromatherapy is used, these essential oils, considered as potential antimicrobial agents, should be preferred. PMID:23662123

Sfeir, Julien; Lefrançois, Corinne; Baudoux, Dominique; Derbré, Séverine; Licznar, Patricia

2013-01-01

21

Genotoxicity of acrylamide in vitro: Acrylamide is not metabolically activated in standard in vitro systems.  

PubMed

The recent finding that acrylamide (AA), a genotoxic rodent carcinogen, is formed during the frying or baking of a variety of foods raises human health concerns. AA is known to be metabolized by cytochrome P450 2E1 (CYP2E1) to glycidamide (GA), which is responsible for AA's in vivo genotoxicity and probable carcinogenicity. In in-vitro mammalian cell tests, however, AA genotoxicity is not enhanced by rat liver S9 or a human liver microsomal fraction. In an attempt to demonstrate the in vitro expression of AA genotoxicity, we employed Salmonella strains and human cell lines that overexpress human CYP2E1. In the umu test, however, AA was not genotoxic in the CYP2E1-expressing Salmonella strain or its parental strain. Moreover, a transgenic human lymphoblastoid cell line overexpressing CYP2E1 (h2E1v2) and its parental cell line (AHH-1) both showed equally weak cytotoxic and genotoxic responses to high (>1 mM) AA concentrations. The DNA adduct N7-GA-Gua, which is detected in liver following AA treatment in vivo, was not substantially formed in the in vitro system. These results indicate that AA was not metabolically activated to GA in vitro. Thus, AA is not relevantly genotoxic in vitro, although its in vivo genotoxicity was clearly demonstrated. PMID:20209648

Koyama, Naoki; Yasui, Manabu; Oda, Yoshimitsu; Suzuki, Satoshi; Satoh, Tetsuo; Suzuki, Takuya; Matsuda, Tomonari; Masuda, Shuichi; Kinae, Naohide; Honma, Masamitsu

2011-01-01

22

In vitro screening of Indian medicinal plants for antiplasmodial activity  

Microsoft Academic Search

Plants traditionally used in India to treat fever or malaria were examined in vitro for antiplasmodial properties against Plasmodium falciparum. Of 80 analysed ethanol extracts, from 47 species, significant effects were found for 31 of the extracts. These represent 23 different species from 20 families. Of the active species 20 were tested against P. falciparum for the first time. The

Henrik Toft Simonsen; Jesper Brćndegaard Nordskjold; Ulla Wagner Smitt; Ulf Nyman; Pushpangadan Palpu; Prabhakar Joshi; George Varughese

2001-01-01

23

In vitro antiprotozoal activity of the leaves of Artemisia ludoviciana  

Microsoft Academic Search

The inhabitants of Northeast of Mexico use an infusion of leaves from Artemisia ludoviciana as an antidiarrheal remedy. The aqueous, methanol, acetone and hexane leaf extracts from mature plants were found to be active in vitro against the parasitic protozoa Entamoeba histolytica and Giardia lamblia.

Salvador Said Fernández; Monica Celina Ramos Guerra; Benito David Mata Cárdenas; Javier Vargas Villarreal; Licet Villarreal Trevińo

2005-01-01

24

In vitro antiprotozoal activity of the leaves of Artemisia ludoviciana.  

PubMed

The inhabitants of Northeast of Mexico use an infusion of leaves from Artemisia ludoviciana as an antidiarrheal remedy. The aqueous, methanol, acetone and hexane leaf extracts from mature plants were found to be active in vitro against the parasitic protozoa Entamoeba histolytica and Giardia lamblia. PMID:15975735

Said Fernández, Salvador; Ramos Guerra, Monica Celina; Mata Cárdenas, Benito David; Vargas Villarreal, Javier; Villarreal Trevińo, Licet

2005-07-01

25

In vitro anticancer activity of Anemopsis californica  

PubMed Central

Three different extract conditions (aqueous, EtOH and EtOAc) of four different parts (bracts, leaves, roots and stems) of the plant Anemopsis californica (A. californica) were evaluated for their effect on the growth and migration of human colon cancer cells, HCT-8, and the breast cancer cell lines Hs 578T and MCF-7/AZ. Our aim was to identify potential anticancer activity in crude A. californica extracts, given that this plant is used by Native Americans to treat a variety of diseases, including cancer. Our results demonstrated that for each of the cell lines tested, the majority of ethyl acetate extracts of all the plant parts are more toxic than the aqueous and ethanol extracts. Furthermore, significant growth inhibitory activity against the three cell lines was found for the ethyl acetate extract of the roots, while the aqueous extract of the roots influenced the migratory capacity of the three cell lines. This study provides evidence for the anticancer properties of A. californica when extracted in water and ethyl acetate, and supports the importance for further purification of the crude extracts and isolation of potential new anticancer compounds through bio-guided fractionation. PMID:21941602

KAMINSKI, CATHERINE N.; FERREY, SETH L.; LOWREY, TIMOTHY; GUERRA, LEO; VAN SLAMBROUCK, SEVERINE; STEELANT, WIM F.A.

2010-01-01

26

In vitro antimicrobial activity of olive leaves.  

PubMed

We investigated the antimicrobial effect of olive leaves against bacteria and fungi. The microorganisms tested were inoculated in various concentrations of olive leaf water extract. Olive leaf 0.6% (w/v) water extract killed almost all bacteria tested, within 3 h. Dermatophytes were inhibited by 1.25% (w/v) plant extract following a 3-day exposure whereas Candida albicans was killed following a 24 h incubation in the presence of 15% (w/v) plant extract. Olive leaf extract fractions, obtained by dialysis, that showed antimicrobial activity consisted of particles smaller than 1000 molecular rate cutoffs. Scanning electron microscopic observations of C. albicans, exposed to 40% (w/v) olive leaf extract, showed invaginated and amorphous cells. Escherichia coli cells, subjected to a similar treatment but exposed to only 0.6% (w/v) olive leaf extract showed complete destruction. These findings suggest an antimicrobial potential for olive leaves. PMID:12870202

Markin, D; Duek, L; Berdicevsky, I

2003-04-01

27

In vitro antifungal activity of Rhazya stricta.  

PubMed

Rhazya stricta is a small glabrous shrub, widely distributed throughout Western Asia from Yemen to Arabia, to the North West Province of India and abundantly found in various regions of Pakistan. Larvicidal and antifungal studies of polar and non polar aerial parts extracts of Rhazya stricta were performed using brine shrimps larvae for larvicidal study and for antifungal study microorganisms, Trichophyton longifusis, Aspergillus flavus, Candida albicans, Microsporum canis and Fusarium solani were used respectively. The methanol fraction showed significant cytotoxicity with LC50 17.809 microg/ml, having mortality rate 73.33% at highest dose. While pet-ether, chloroform and carbon tetrachloride possessed moderate to low cytotoxicity with their LC50 values 49.077 microg/ml, 95.859 microg/ml and 80.489 microg/ml respectively, ethyl acetate fraction showed no cytotoxicity. Results of antifungal studies showed that fractionated samples of methanol and chloroform possessed significant antifungal activities against, Trichophyton longifusis, Aspergillus flavus, Candida albicans and Fusarium solani respectively. Due to these promising results, further in vivo studies over R. stricta must be conducted. PMID:17604249

Khan, Saifullah; Khan, Gul Majid

2007-10-01

28

In Vitro Phytotoxicity and Antioxidant Activity of Selected Flavonoids  

PubMed Central

The knowledge of flavonoids involved in plant-plant interactions and their mechanisms of action are poor and, moreover, the structural characteristics required for these biological activities are scarcely known. The objective of this work was to study the possible in vitro phytotoxic effects of 27 flavonoids on the germination and early radical growth of Raphanus sativus L. and Lepidium sativum L., with the aim to evaluate the possible structure/activity relationship. Moreover, the antioxidant activity of the same compounds was also evaluated. Generally, in response to various tested flavonoids, germination was only slightly affected, whereas significant differences were observed in the activity of the various tested flavonoids against radical elongation. DPPH test confirms the antioxidant activity of luteolin, quercetin, catechol, morin, and catechin. The biological activity recorded is discussed in relation to the structure of compounds and their capability to interact with cell structures and physiology. No correlation was found between phytotoxic and antioxidant activities. PMID:22754304

De Martino, Laura; Mencherini, Teresa; Mancini, Emilia; Aquino, Rita Patrizia; De Almeida, Luiz Fernando Rolim; De Feo, Vincenzo

2012-01-01

29

In vitro antimicrobial activity of novel azaphenothiazine derivatives.  

PubMed

Antimicrobial activity in vitro of a series of novel azaphenothiazine derivatives containing a quinoline moiety was investigated using Gram-positive (Staphylococcus aureus, Enterococcus faecalis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) strains as well as in Candida albicans yeast. The examined compounds showed the highest activity against Enterococcus faecalis and Escherichia coli whereas activity against Pseudomonas aeruginosa was the lowest. Compound 1d demonstrates the highest activity against all tested bacterial strains. Compounds 1c, 1h and 1k with various substituents (CH3, OH, NH2) at C11 position of the quinobenzothiazine ring, did not exhibit activity against any tested bacterial strain. Only compounds 1m and 1n with long aliphatic chains at the quinoline nitrogen atom showed antifungal activity. Correlations between antimicrobial activity and chemical structure of the tested compounds were observed. PMID:23285676

Zieba, Andrzej; Czuba, Zenon Pawe?; Król, Wojciech

2012-01-01

30

Antimalarial activity of plumbagin in vitro and in animal models  

PubMed Central

Background Plumbagin is the major active constituent in several plants including Plumbago indica Linn. (root). This compound has been shown to exhibit a wide spectrum of biological and pharmacological activities. The present study aimed to evaluate the in vitro and in vivo antimalarial activity of plumbagin including its acute and subacute toxicity in mice. Methods In vitro antimalarial activity of plumbagin against K1 and 3D7 Plasmodium falciparum clones were assessed using SYBR Green I based assay. In vivo antimalarial activity was investigated in Plasmodium berghei-infected mouse model (a 4-day suppressive test). Results Plumbagin exhibited promising antimalarial activity with in vitro IC50 (concentration that inhibits parasite growth to 50%) against 3D7 chloroquine-sensitive P. falciparum and K1 chloroquine-resistant P. falciparum clones of 580 (270–640) and 370 (270–490) nM, respectively. Toxicity testing indicated relatively low toxicity at the dose levels up to 100 (single oral dose) and 25 (daily doses for 14 days) mg/kg body weight for acute and subacute toxicity, respectively. Chloroquine exhibited the most potent antimalarial activity in mice infected with P. berghei ANKA strain with respect to its activity on the reduction of parasitaemia on day 4 and the prolongation of survival time. Conclusions Plumbagin at the dose of 25 mg/kg body weight given for 4 days was safe and produced weak antimalarial activity. Chemical derivatization of the parent compound or preparation of modified formulation is required to improve its systemic bioavailability. PMID:24410949

2014-01-01

31

In vitro antioxidant activity of Anthriscus cerefolium L. (Hoffm.) extracts.  

PubMed

Standardised aqueous extracts of chervil (Anthriscus cerefolium L. Hoffm.) (Apiacae) were investigated for antioxidant effect. Numerous in vitro test methods were used to determine whether the extracts, from different vegetative parts (root, herb) had H-donor, metal binding, reductive, free radical scavenging and membrane protective activity. Apiin was used as a reference material. The herb extract showed better activity in all experiments than the root extract. The present results underline that the wateric chervil extracts have antioxidant and anti-lipoperoxidant activity. PMID:10722209

Fejes, S; Blázovics, A; Lugasi, A; Lemberkovics, E; Petri, G; Kéry, A

2000-03-01

32

In vitro evaluation of the antimicrobial activities of selected lozenges.  

PubMed

The in vitro antimicrobial activities of 10 lozenges (Merothol, Merocets, Merocaine, Strepsils (two varieties), Dequacaine, Dequacets, Zensyls, Tyrozets, and Labosept) were determined by use of a microtiter counting method with Streptococcus pyogenes, Staphylococcus aureus, and Candida albicans as the test organisms. Merothol, Merocets, Merocaine, and both Strepsils formulations all reduced the counts of both S. aureus and S. pyogenes suspensions by approximately 6 log cycles within 5 and 20 min, respectively. Merothol, Merocets, and Merocaine also caused a reduction in the counts of the C. albicans suspension approximately 5 log cycles within 40 min, but no other lozenge formulation showed rapid and marked activity against C. albicans. Dequacaine and Dequacets showed marked but much slower activities against this yeast. Zensyls caused an approximately 6-log-cycle reduction in bacterial counts within 40 min, and Dequacaine, Dequacets, and Tyrozets showed marked but slower antibacterial activities. This work confirmed by a statistically sound in vitro method the in vivo antibacterial activities reported for Merothol, Merocets, and Merocaine, demonstrated equivalent antibacterial activities for Strepsils, and indicated that Merothol, Merocets, and Merocaine also showed marked activities against C. albicans. PMID:8308699

Richards, R M; Xing, D K

1993-12-01

33

In vitro antioxidant activity of Retama monosperma (L.) Boiss.  

PubMed

The relationship between the antioxidant activity and the phenolic contents (total polyphenol, flavonoid and condensed tannin) of Retama monosperma (Fabaceae), used commonly in the traditional medicine of Mediterranean regions, was investigated. The antioxidant activities of the various fractions (toluene, chloroform, ethyl acetate and butanol) of the hydromethanolic extract of the seeds, stems and flowers have been evaluated using in vitro 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) radical scavenging activities and Phosphomolybdic acid assays and were compared to ascorbic acid. A significant high Pearson's correlations between flavonoid content and antioxidant activities (r = 0.91) with Phosphomolybdic acid assays and (r = - 0.79) with IC50 DPPH radical scavenging activities. However, there was no correlation between condensed tannin and antioxidant activities. The results obtained in the present study indicate that the ethyl acetate fraction of seeds is a potential source of natural antioxidant for R. monosperma. PMID:25033217

Belmokhtar, Zoubir; Harche, Meriem Kaid

2014-01-01

34

Studies on the activities of rumen microorganisms in vitro  

E-print Network

EXTRACTS ON THE DIGESTION OF CELLULOSE BE RUMEN MICROORGANISMS INTRODUCTION Page Review of Literature Collection of Numen Samples Processing of Rumen Samples Measurement of the Activity of Rurren Yiicroorgan~ s'". s Procedure for ~vt-, c Incubation... Experiments Determination of Cellulose Digestion 'reparation of M. souite Bean Extracts Fractionanicn of' Mesouite Bean Extract" 9 l5 RFS'JLT DISC'JSSION SUMMARY FART II, DETERMINATIONS OF PUMINAL pH AND IN VITRO CFILULOSE DIGESTION ON CATTLE...

Johnson, Carl Edward

2012-06-07

35

In vitro and ex vivo antiangiogenic activity of Salvia officinalis.  

PubMed

Angiogenesis is a key process in the promotion of cancer and its metastasis. Herein, the antiangiogenic activity of Salvia officinalis extract and its fractions was investigated. S. officinalis aerial parts were extracted with ethanol and its successive hexane, ethyl acetate, n-butanol and aqueous fractions were evaluated for their antiangiogenic activities using human umbilical vein endothelial cells (HUVEC) capillary tube formation and rat aorta models in a three-dimensional collagen matrix. Furthermore, antimigrative effects of the fractions were assessed using a wound healing model. The ethanol extract of S. officinalis (ESO) potently inhibited capillary tube formation in HUVEC and rat aorta models of angiogenesis, and its hexane fraction (HSO) exerted the highest inhibitory effect. In addition, the ethanol extract of S. officinalis and its hexane fraction showed a dose-dependent inhibitory activity on the migration of the endothelial cells in the wound healing model. Furthermore, ESO inhibited endothelial cell proliferation at 50-200 ?g/mL in a dose-dependent manner. These findings indicated some new pharmacological activities of S. officinalis such as antiangiogenic in vitro and ex vivo, and antimigrative activity in vitro. Therefore, S. officinalis could be a candidate as a useful herb with therapeutic or preventive activity against angiogenesis related disorders. PMID:20878705

Keshavarz, Maryam; Mostafaie, Ali; Mansouri, Kamran; Bidmeshkipour, Ali; Motlagh, Hamid Reza Mohammadi; Parvaneh, Shahram

2010-10-01

36

In vitro anti-quorum sensing activity of phytol.  

PubMed

Anti-quorum sensing activity of the diterpene phytol was evaluated in vitro for the first time. This compound (at three sub-MIC concentrations - 0.5, 0.25 and 0.125 MIC, respectively) reduced the formation of Pseudomonas aeruginosa PAO1 biofilm in the range of 74.00-84.33% exhibiting higher activity than the both positive controls used, streptomycin and ampicillin. Phytol (0.5 MIC) also effectively reduced P. aeruginosa twitching and flagella motility. Indeed, the bacteria treated were incapable of producing a twitching zone and had almost round, smooth and regular colony edges. Finally, the tested compound (0.5 MIC) exhibited good P. aeruginosa pyocyanin inhibitory activity (51.94%) practically to the same extent as streptomycin (52.09%). According to the experimental data obtained, this phytol property may inspire design of medical foods targeting P. aeruginosa quorum sensing activity. PMID:25103916

Pejin, Boris; Ciric, Ana; Glamoclija, Jasmina; Nikolic, Milos; Sokovic, Marina

2015-02-01

37

[Antitumor activity of the root of Euphorbia helioscopic in vitro].  

PubMed

Antitumor activity of the aquatic extract the root of Euphorbia helioscopia L (EWE) in Vitro were studied. Viable cells count, MTT staining and colonal formation assays of three kinds of cancer cells were used to assess the antitumor activity. Determined by viable cells count, the IC50 values of EWE against 7721, Hela, MKN-45 cells were 1.26, 1.98, 1.72 mg/ml respectively (72 h). Determined MTT staining, the IC50 values EWE against 7721, Hela, MKN-45 cells were 1.43, 1.67, 0.97 mg/ml. Determined by colonal formation, the inhibition rate of EWE (4 mg/ml) against 7721, Hela, MKN-45 cells were 59.8%, 66.4%, 70.5%. The results indicated that EWE had obvious antitumor activity. PMID:12575050

Cai, Y; Wang, J; Liang, B

1999-02-01

38

In vitro antioxidant activities of Solanum surattense leaf extract  

PubMed Central

Objective To evaluate the antioxidant activity of alcoholic leaf-extract of Solanum surattense (Solanaceae) (S. surattense). Methods Leaf extract were tested for in vitro free radical scavenging assays, such as hydroxyl radical and hydrogen peroxide, inhibition of superoxide anion radical and 2, 2-diphenyl-1-picryl hydrazyl radical (DPPH), total antioxidant activity and reducing ability. Further, total phenolic content of S. surattense was analyzed. Results S. surattense extract effectively scavenged free radicals at all different concentrations and showed its potent antioxidant activity. Further, these effects were in a dose dependent manner. Results were compared to standard antioxidants such as butylated hydroxytoluene, ascorbic acid and ?-tocopherol. Conclusions S. surattense have strong antioxidant potential. Further the study validates the therapeutic benefits of the Indian system of medicine. PMID:23570013

Muruhan, Sridevi; Selvaraj, Senthil; Viswanathan, Pugalendi Kodukkur

2013-01-01

39

Semiautomated assessment of in vitro activity of potential antileishmanial drugs.  

PubMed

We have compared the in vitro activity of six agents against macrophage-contained Leishmania tropica amastigotes determined by the conventional Giemsa staining procedure, with the activity determined by the semiautomated assessment of incorporation of radiolabeled uracil into the nucleic acid of the organisms. Although the mean 50% effective dose of Pentostam by Giemsa staining (4.1 micrograms/ml) was somewhat higher than that by uracil incorporation (2.8 micrograms/ml), the ED50S for the other two clinical agents (pentamidine, 0.035 versus 0.037 micrograms/ml; amphotericin B, 0.67 versus 0.70 micrograms/ml) and for three promising experimental agents (ketoconazole, 11.3 versus 11.3 micrograms/ml; the 8-aminoquinoline WR 6026, 1.6 versus 1.5 micrograms/ml formycin B, 0.018 versus 0.017 micrograms/ml) were virtually identical. The radiolabeling technique has several advantages over the Giemsa staining procedure. These include the need for relatively few macrophages, rapid and objective data generation, and viability of the test organism being measured. The successful application of the radiolabeling technique to at least six different chemical classes of compounds suggests that it would be useful for the routine assessment of antileishmanial activity in vitro. PMID:3002244

Berman, J D; Gallalee, J V

1985-12-01

40

Synthesis and in vitro antimalarial activity of sulfone endoperoxides.  

PubMed

A series of 4,8-dimethyl-4-phenylsulfonylmethyl-2,3-dioxabicyclo[3.3.1]+ ++nonanes, carrying a variety of substituents at position-8 (4) were prepared by a short and efficient method from R-(+)-limonene. Key reactions include thiol oxygen cooxidation, and alkylation and acylation of a sterically hindered tertiary alcohol compatible with the endoperoxy functionality. Some of compounds 4, which are structurally related to yingzhaosu A (2), were found to exhibit in vitro antimalarial activity comparable to that of artemisinin (1) and superior to that of arteflene (3). PMID:9871509

Bachi, M D; Korshin, E E; Ploypradith, P; Cumming, J N; Xie, S; Shapiro, T A; Posner, G H

1998-04-21

41

In Vitro and In Vivo Osteogenic Activity of Largazole.  

PubMed

Due to their capability of modifying chromatin structure and thereby regulating gene transcription, histone deacetylases (HDACs) have been reported to play important roles in osteogenesis and considered a promising potential therapeutic target for bone diseases, including osteoporosis. We showed that the novel marine-derived HDAC inhibitor largazole exhibits in vitro and in vivo osteogenic activity. Largazole significantly induced the expression of ALP and OPN. The osteogenic activity of largazole was mediated through the increased expression of Runx2 and BMPs. Importantly, largazole showed in vivo bone-forming efficacy in the mouse calvarial bone formation assay and the rabbit calvarial bone fracture healing model. The dual action of largazole to stimulate bone formation and inhibit bone resorption would be a useful feature in drug development for bone-related disorders. PMID:21666868

Lee, Su-Ui; Kwak, Han Bok; Pi, Sung-Hee; You, Hyung-Keun; Byeon, Seong Rim; Ying, Yongcheng; Luesch, Hendrik; Hong, Jiyong; Kim, Seong Hwan

2011-03-10

42

In vitro screening of medicinal plant extracts for macrofilaricidal activity.  

PubMed

Methanolic extracts of 20 medicinal plants were screened at 1-10 mg/ml for in vitro macrofilaricidal activity by worm motility assay against adult Setaria digitata, the cattle filarial worm. Four plant extracts showed macrofilaricidal activity by worm motility at concentrations below 4 mg/ml and an incubation period of 100 min. Complete inhibition of worm motility and subsequent mortality was observed at 3, 2, 1 and 1 mg/ml, respectively, for Centratherum anthelminticum, Cedrus deodara, Sphaeranthus indicus and Ricinus communis. 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide (MTT) reduction assay was carried out at 1 mg ml(-1) and 4-h incubation period, and the results showed that C. deodara, R. communis, S. indicus and C. anthelminticum exhibited 86.56, 72.39, 61.20 and 43.15% inhibition respectively in formazan formation compared to the control. PMID:17013649

Nisha, Mathew; Kalyanasundaram, M; Paily, K P; Abidha; Vanamail, P; Balaraman, K

2007-02-01

43

In Vitro Anti-rotaviral Activity of Achillea kellalensis  

PubMed Central

Background Achillea kellalensis, which is frequently used by Chaharmahal va Bakhtiarians residing in, Southwest of Iran, as a traditional herbal medicine for the treatment of acute diarrhea, has been selected to examine its antiviral activities against bovine rotavirus and cell toxicity activity in MA-104 cells. Objectives The aim of this study was to evaluate the in vitro cytotoxic and anti-rotavirus properties of crude extracts of A. kellalensis. Materials and Methods The dried and powdered flowers of Achillea kellalensis were extracted with hot water and ethanol 50% (v/v). The cell viability and toxicity of the extracts were evaluated on MA-104 cells using four methods; trypan blue dye, NR, crystal violet and MTT assay. The in vitro anti-rotavirus properties were determined via four different assays, in order to evaluate the direct inhibition and/or the inhibition of viral replication. Results Cytotoxicity of two A. kellalensis extracts showed different concentrations. Hydro-alcoholic extract had low CC50 at 600 µg/mL by the NR assay while the aqueous extract had high CC50 at 1000µg/mL by the crystal violet method. In the simultaneous treatment assay and post treatment assay, the extracts were able to prevent viral replication and inhibit the viral CPE on MA-104 cells at 10 TCID50, but the extracts did not exhibit direct antiviral activity on rotavirus adsorption. The effective concentration (EC50) of both extracts was observed to be 100 µg/mL. Conclusions These results indicate that A. kellalensis extracts exert potent anti-rotaviral activity only after viral adsorption. The two extracts from A. kellalensis showed a good selectivity index. Also these results suggest that extracts prepared from the flowers of A. kellalensis may be potential anti-rotaviral agents in vivo and be useful in veterinary medicine. PMID:24624203

Taherkhani, Reza; Farshadpour, Fatemeh; Makvandi, Manoochehr

2013-01-01

44

In vitro activity of combinations of ceftazidime-avibactam in in vitro checkerboard assays.  

PubMed

To evaluate the in vitro effects of the combination of ceftazidime and avibactam on the MICs of both compounds, checkerboard assays were performed for 81 clinical strains, including 55 Enterobacteriaceae strains (32 Klebsiella pneumoniae, 19 Escherichia coli, 1 Citrobacter freundii and 3 Enterobacter cloacae) and 26 strains of Pseudomonas aeruginosa, all with known resistance mechanisms such as ESBLs and carbapenemases, phenotypically or molecularly determined. Phenotypically ceftazidime-resistant strains (n=69) were analysed in more detail. For the Enterobacteriaceae a concentration dependent effect of avibactam was found for most strains with a maximum effect of avibactam at a concentration of 4 mg/L, which decreased all ceftazidime MICs to ? 4 mg/L. Avibactam alone also showed antibacterial activity (MIC50 and MIC90 being 8 and 16 mg/L respectively). For the ceftazidime-resistant P. aeruginosa strains, considerable inhibition of ?-lactamases by avibactam was acquired at a concentration of 4 mg/L, which decreased all ceftazidime MICs except one to ? 8 mg/L (the CLSI and EUCAST susceptible breakpoint). Increasing the concentration of avibactam further decreased MICs, resulting in a maximum effect for most strains at 8 to 16 mg/L. In summary, for most strains, tested addition of avibactam of 4 mg/L restored the antibacterial activity of ceftazidime to a level comparable to wild-type strains, indicating full inhibition, and strains became susceptible according to EUCAST and CLSI criteria. Based on these in vitro data, avibactam is a promising inhibitor of different ?-lactamases including ESBLs and carbapenemases. PMID:25487794

Berkhout, Johanna; Melchers, Maria J; van Mil, Anita C; Nichols, Wright W; Mouton, Johan W

2014-12-01

45

Antimicrobial activities of silver dressings: an in vitro comparison.  

PubMed

A range of silver-coated or -impregnated dressings are now commercially available for use but comparative data on their antimicrobial efficacies are limited. The antibacterial activities of five commercially available silver-coated/impregnated dressings were compared against nine common burn-wound pathogens, namely methicillin-sensitive and -resistant Staphylococcus aureus (MRSA), Enterococcus faecalis, Pseudomonas aeruginosa, Escherichia coli, Enterobacter cloacae, Proteus vulgaris, Acinetobacter baumannii and a multi-drug-efflux-positive Acinetobacter baumannii (BM4454), using a broth culture method. The rapidity and extent of killing of these pathogens under in vitro conditions were evaluated. All five silver-impregnated dressings investigated exerted bactericidal activity, particularly against Gram-negative bacteria, including Enterobacter species, Proteus species and E. coli. The spectrum and rapidity of action, however, ranged widely for different dressings. Acticoat and Contreet had a broad spectrum of bactericidal activities against both Gram-positive and -negative bacteria. Contreet was characterized by a very rapid bactericidal action and achieved a reduction of > or =10,000 c.f.u. ml(-1) in the first 30 min for Enterobacter cloacae, Proteus vulgaris, Pseudomonas aeruginosa and Acinetobacter baumanii. Other dressings demonstrated a narrower range of bactericidal activities. Understanding the characteristics of these dressings may enable them to be targeted more appropriately according to the specific requirements for use of a particular dressing, as in for prophylaxis in skin grafting or for an infected wound with MRSA. PMID:16388031

Ip, Margaret; Lui, Sau Lai; Poon, Vincent K M; Lung, Ivan; Burd, Andrew

2006-01-01

46

Silver and Gold Nanoparticles Alter Cathepsin Activity In vitro  

NASA Astrophysics Data System (ADS)

Nanomaterials are being incorporated into many biological applications for use as therapeutics, sensors, or labels. Silver nanomaterials are being utilized for biological implants and wound dressings as an antiviral material, whereas gold nanomaterials are being used as biological labels or sensors due to their surface properties and biocompatibility. Cytotoxicity data of these materials are becoming more prevalent; however, little research has been performed to understand how the introduction of these materials into cells affects cellular processes. Here, we demonstrate the impact that silver and gold nanoparticles have on cathepsin activity in vitro. Cathepsins are important cellular proteases that are imperative for proper immune system function. We have selected to examine gold and silver nanoparticles due to the increased use of these materials in biological applications. This manuscript depicts how both of these types of nanomaterials affect cathepsin activity, which could impact the host's immune system and its ability to respond to pathogens. Cathepsin B activity decreases in a dose-dependent manner with all nanoparticles tested. Alternatively, the impact of nanoparticles on cathepsin L activity depends greatly on the type and size of the material.

Speshock, Janice L.; Braydich-Stolle, Laura K.; Szymanski, Eric R.; Hussain, Saber M.

2010-12-01

47

Silver and Gold Nanoparticles Alter Cathepsin Activity In vitro  

NASA Astrophysics Data System (ADS)

Nanomaterials are being incorporated into many biological applications for use as therapeutics, sensors, or labels. Silver nanomaterials are being utilized for biological implants and wound dressings as an antiviral material, whereas gold nanomaterials are being used as biological labels or sensors due to their surface properties and biocompatibility. Cytotoxicity data of these materials are becoming more prevalent; however, little research has been performed to understand how the introduction of these materials into cells affects cellular processes. Here, we demonstrate the impact that silver and gold nanoparticles have on cathepsin activity in vitro. Cathepsins are important cellular proteases that are imperative for proper immune system function. We have selected to examine gold and silver nanoparticles due to the increased use of these materials in biological applications. This manuscript depicts how both of these types of nanomaterials affect cathepsin activity, which could impact the host's immune system and its ability to respond to pathogens. Cathepsin B activity decreases in a dose-dependent manner with all nanoparticles tested. Alternatively, the impact of nanoparticles on cathepsin L activity depends greatly on the type and size of the material.

Speshock, Janice L.; Braydich-Stolle, Laura K.; Szymanski, Eric R.; Hussain, Saber M.

2011-12-01

48

Human filarial Wolbachia lipopeptide directly activates human neutrophils in vitro  

PubMed Central

The host inflammatory response to the Onchocerca volvulus endosymbiont, Wolbachia, is a major contributing factor in the development of chronic pathology in humans (onchocerciasis/river blindness). Recently, the toll-like pattern recognition receptor motif of the major inflammatory ligands of filarial Wolbachia, membrane-associated diacylated lipoproteins, was functionally defined in murine models of pathology, including mediation of neutrophil recruitment to the cornea. However, the extent to which human neutrophils can be activated in response to this Wolbachia pattern recognition motif is not known. Therefore, the responses of purified peripheral blood human neutrophils to a synthetic N-terminal diacylated lipopeptide (WoLP) of filarial Wolbachia peptidoglycan-associated lipoprotein (PAL) were characterized. WoLP exposure led to a dose-dependent activation of healthy, human neutrophils that included gross morphological alterations and modulation of surface expressed integrins involved in tethering, rolling and extravasation. WoLP exposure induced chemotaxis but not chemokinesis of neutrophils, and secretion of the major neutrophil chemokine, interleukin 8. WoLP also induced and primed the respiratory burst, and enhanced neutrophil survival by delay of apoptosis. These results indicate that the major inflammatory motif of filarial Wolbachia lipoproteins directly activates human neutrophils in vitro and promotes a molecular pathway by which human neutrophils are recruited to sites of Onchocerca parasitism. PMID:24909063

Tamarozzi, F; Wright, H L; Johnston, K L; Edwards, S W; Turner, J D; Taylor, M J

2014-01-01

49

Recruitment of Perisomatic Inhibition during Spontaneous Hippocampal Activity In Vitro  

PubMed Central

It was recently shown that perisomatic GABAergic inhibitory postsynaptic potentials (IPSPs) originating from basket and chandelier cells can be recorded as population IPSPs from the hippocampal pyramidal layer using extracellular electrodes (eIPSPs). Taking advantage of this approach, we have investigated the recruitment of perisomatic inhibition during spontaneous hippocampal activity in vitro. Combining intracellular and extracellular recordings from pyramidal cells and interneurons, we confirm that inhibitory signals generated by basket cells can be recorded extracellularly, but our results suggest that, during spontaneous activity, eIPSPs are mostly confined to the CA3 rather than CA1 region. CA3 eIPSPs produced the powerful time-locked inhibition of multi-unit activity expected from perisomatic inhibition. Analysis of the temporal dynamics of spike discharges relative to eIPSPs suggests significant but moderate recruitment of excitatory and inhibitory neurons within the CA3 network on a 10 ms time scale, within which neurons recruit each other through recurrent collaterals and trigger powerful feedback inhibition. Such quantified parameters of neuronal interactions in the hippocampal network may serve as a basis for future characterisation of pathological conditions potentially affecting the interactions between excitation and inhibition in this circuit. PMID:23805227

Molter, Colin; Mehidi, Amine; Szabadics, Janos; Leinekugel, Xavier

2013-01-01

50

In vitro analysis of iron chelating activity of flavonoids.  

PubMed

Flavonoids have been demonstrated to possess miscellaneous health benefits which are, at least partly, associated with iron chelation. In this in vitro study, 26 flavonoids from different subclasses were analyzed for their iron chelating activity and stability of the formed complexes in four patho/physiologically relevant pH conditions (4.5, 5.5, 6.8, and 7.5) and compared with clinically used iron chelator deferoxamine. The study demonstrated that the most effective iron binding site of flavonoids represents 6,7-dihydroxy structure. This site is incorporated in baicalein structure which formed, similarly to deferoxamine, the complexes with iron in the stoichiometry 1:1 and was not inferior in all tested pH to deferoxamine. The 3-hydroxy-4-keto conformation together with 2,3-double bond and the catecholic B ring were associated with a substantial iron chelation although the latter did not play an essential role at more acidic conditions. In agreement, quercetin and myricetin possessing all three structural requirements were similarly active to baicalein or deferoxamine at the neutral conditions, but were clearly less active in lower pH. The 5-hydroxy-4-keto site was less efficient and the complexes of iron in this site were not stable at the acidic conditions. Isolated keto, hydroxyl, methoxyl groups or an ortho methoxy-hydroxy groups were not associated with iron chelation at all. PMID:21450273

Mlad?nka, P?emysl; Macáková, Kate?ina; Filipský, Tomáš; Zatloukalová, Libuše; Jahodá?, Lud?k; Bovicelli, Paolo; Silvestri, Ilaria Proietti; Hrdina, Radomír; Saso, Luciano

2011-05-01

51

Influence of gold nanoparticles on platelets functional activity in vitro  

NASA Astrophysics Data System (ADS)

Now in the leading biomedical centers of the world approved new technology of laser photothermal destruction of cancer cells using plasmon gold nanoparticles. Investigations of influence of gold nanoparticles on white rat platelets aggregative activity in vitro have been made. Platelet aggregation was investigated in platelet rich plasma (PRP) with help of laser analyzer 230 LA <>, Russia). Aggregation inductor was ADP solution in terminal concentration 2.5 micromole (<>, Russia). Gold nanoshells soluted in salt solution were used for experiments. Samples of PRP were incubated with 50 or 100 ?l gold nanoshells solution in 5 minute, after that we made definition ADP induced platelet aggregation. We found out increase platelet function activity after incubation with nanoparticles solution which shown in maximum ADP-induced aggregation degree increase. Increase platelet function activity during intravenous nanoshells injection can be cause of thrombosis on patients. That's why before clinical application of cancer cell destruction based on laser photothermal used with plasmon gold nanoparticles careful investigations of thrombosis process and detail analyze of physiological blood parameters are very necessary.

Akchurin, Garif G.; Akchurin, George G.; Ivanov, Alexey N.; Kirichuk, Vyacheslav F.; Terentyuk, George S.; Khlebtsov, Boris N.; Khlebtsov, Nikolay G.

2008-02-01

52

Lethal Factor Active-Site Mutations Affect Catalytic Activity In Vitro  

PubMed Central

The lethal factor (LF) protein of Bacillus anthracis lethal toxin contains the thermolysin-like active-site and zinc-binding consensus motif HEXXH (K. R. Klimpel, N. Arora, and S. H. Leppla, Mol. Microbiol. 13:1093–1100, 1994). LF is hypothesized to act as a Zn2+ metalloprotease in the cytoplasm of macrophages, but no proteolytic activities have been previously shown on any target substrate. Here, synthetic peptides are hydrolyzed by LF in vitro. Mass spectroscopy and peptide sequencing of isolated cleavage products separated by reverse-phase high-pressure liquid chromatography indicate that LF seems to prefer proline-containing substrates. Substitution mutations within the consensus active-site residues completely abolish all in vitro catalytic functions, as does addition of 1,10-phenanthroline, EDTA, and certain amino acid hydroxamates, including the novel zinc metalloprotease inhibitor ZINCOV. In contrast, the protease inhibitors bestatin and lysine CMK, previously shown to block LF activity on macrophages, did not block LF activity in vitro. These data provide the first direct evidence that LF may act as an endopeptidase. PMID:9573135

Hammond, S. E.; Hanna, P. C.

1998-01-01

53

In vitro antimicrobial activity of ethanolic fractions of Cryptolepis sanguinolenta  

PubMed Central

Background Following claims that some plants have antimicrobial activities against infectious microbes, the in vitro antimicrobial activities of different solvent fractions of ethanolic extract of Cryptolepis sanguinolenta were evaluated against eight standard bacteria and clinical isolates. Methods The solvent partitioning protocol involving ethanol, petroleum ether, chloroform, ethyl acetate and water, was used to extract various fractions of dried pulverized Cryptolepis sanguinolenta roots. Qualitative phyto-constituents screening was performed on the ethanol extract, chloroform fraction and the water fraction. The Kirby Bauer disk diffusion method was employed to ascertain the antibiogram of the test organisms while the agar diffusion method was used to investigate the antimicrobial properties of the crude plant extracts. The microplate dilution method aided in finding the MICs while the MBCs were obtained by the method of Nester and friends. The SPSS 16.0 version was used to analyze the percentages of inhibitions and bactericidal activities. Results The phytochemical screening revealed the presence of alkaloids, reducing sugars, polyuronides, anthocyanosides and triterpenes. The ethanol extract inhibited 5 out of 8 (62.5%) of the standard organisms and 6 out of 8 (75%) clinical isolates. The petroleum ether fraction inhibited 4 out of 8 (50%) of the standard microbes and 1 out of 8 (12.5%) clinical isolates. It was also observed that the chloroform fraction inhibited the growth of all the organisms (100%). Average inhibition zones of 14.0?±?1.0?mm to 24.67?±?0.58?mm was seen in the ethyl acetate fraction which halted the growth of 3 (37.5%) of the standard organisms. Inhibition of 7 (87.5%) of standard strains and 6 (75%) of clinical isolates were observed in the water fraction. The chloroform fraction exhibited bactericidal activity against all the test organisms while the remaining fractions showed varying degrees of bacteriostatic activity. Conclusion The study confirmed that fractions of Cryptolepis sanguinolenta have antimicrobial activity. The chloroform fraction had the highest activity, followed by water, ethanol, petroleum ether and ethyl acetate respectively. Only the chloroform fraction exhibited bactericidal activity and further investigations are needed to ascertain its safety and prospects of drug development. PMID:22709723

2012-01-01

54

Amino ozonides exhibit in vitro activity against Echinococcus multilocularis metacestodes.  

PubMed

Artemisinin is an antimalarial sesquiterpene lactone that contains a 1,2,4-trioxane heterocycle. Dihydroartemisinin and artesunate demonstrated activity against Echinococcus multilocularis metacestodes in vitro but were not effective in a mouse model. In this study, the in vitro effects of a small library of synthetic ozonides (1,2,4-trioxolanes) were investigated. Initial compound screening against E. multilocularis metacestodes was performed at 20?M, and selected ozonides were further assessed in dose-response studies in metacestode cultures and mammalian cells. Transmission electron microscopy (TEM) was employed to characterise compound-induced structural alterations. At 20?M, the most potent ozonides (OZ401, OZ455, OZ491 and OZ494) led to death of ca. 60-100% of the parasites. Subsequent dose-response experiments demonstrated that OZ401, OZ455 and OZ491, which contain an aminopropylether substructure, were the most potent, with 50% inhibitory concentrations ranging from 11?M to 14?M. Cytotoxicity for these three ozonides, assessed in human foreskin fibroblasts, rat hepatoma cells and green monkey epithelial kidney (Vero) cells, was evident only at high concentrations. TEM demonstrated that OZ401 and OZ491 treatment induced considerable metabolic impairment in metacestodes at 1 day post exposure. At Day 3 post exposure, the germinal layer was severely distorted, although some intact cells were still visible, demonstrating that not all cell types in the parasite tissue were equally affected. Complete destruction of the germinal layer was noted at 5 days post exposure. Synthetic ozonides could represent interesting leads that will be further investigated in a suitable in vivo model of E. multilocularis infection. PMID:24239405

Küster, Tatiana; Kriegel, Nadja; Stadelmann, Britta; Wang, Xiaofang; Dong, Yuxiang; Vennerstrom, Jonathan L; Keiser, Jennifer; Hemphill, Andrew

2014-01-01

55

Candida Species Exhibit Differential In Vitro Hemolytic Activities  

PubMed Central

A total of 80 Candida isolates representing 14 species were examined for their respective responses to an in vitro hemolytic test. A modification of a previously described plate assay system where the yeasts are incubated on glucose (3%)-enriched sheep blood agar in a carbon dioxide (5%)-rich environment for 48 h was used to evaluate the hemolytic activity. A group of eight Candida species which included Candida albicans (15 isolates), C. dubliniensis (2), C. kefyr (2), C. krusei (4), C. zeylanoides (1), C. glabrata (34), C. tropicalis (5), and C. lusitaniae (2) demonstrated both alpha and beta hemolysis at 48 h postinoculation. Only alpha hemolysis was detectable in four Candida species, viz., C. famata (3), C. guilliermondii (4), C. rugosa (1), and C. utilis (1), while C. parapsilosis (5) and C. pelliculosa (1) failed to demonstrate any hemolytic activity after incubation for 48 h or longer. This is the first study to demonstrate the variable expression profiles of hemolysins by different Candida species. PMID:11474025

Luo, Gang; Samaranayake, Lakshman P.; Yau, Joyce Y. Y.

2001-01-01

56

Quantitative comparisons of in vitro assays for estrogenic activities.  

PubMed Central

Substances that may act as estrogens show a broad chemical structural diversity. To thoroughly address the question of possible adverse estrogenic effects, reliable methods are needed to detect and identify the chemicals of these diverse structural classes. We compared three assays--in vitro estrogen receptor competitive binding assays (ER binding assays), yeast-based reporter gene assays (yeast assays), and the MCF-7 cell proliferation assay (E-SCREEN assay)--to determine their quantitative agreement in identifying structurally diverse estrogens. We examined assay performance for relative sensitivity, detection of active/inactive chemicals, and estrogen/antiestrogen activities. In this examination, we combined individual data sets in a specific, quantitative data mining exercise. Data sets for at least 29 chemicals from five laboratories were analyzed pair-wise by X-Y plots. The ER binding assay was a good predictor for the other two assay results when the antiestrogens were excluded (r(2) is 0.78 for the yeast assays and 0.85 for the E-SCREEN assays). Additionally, the examination strongly suggests that biologic information that is not apparent from any of the individual assays can be discovered by quantitative pair-wise comparisons among assays. Antiestrogens are identified as outliers in the ER binding/yeast assay, while complete antagonists are identified in the ER binding and E-SCREEN assays. Furthermore, the presence of outliers may be explained by different mechanisms that induce an endocrine response, different impurities in different batches of chemicals, different species sensitivity, or limitations of the assay techniques. Although these assays involve different levels of biologic complexity, the major conclusion is that they generally provided consistent information in quantitatively determining estrogenic activity for the five data sets examined. The results should provide guidance for expanded data mining examinations and the selection of appropriate assays to screen estrogenic endocrine disruptors. Images Figure 1 Figure 2 Figure 3 Figure 4 Figure 5 Figure 6 Figure 7 PMID:10964792

Fang, H; Tong, W; Perkins, R; Soto, A M; Prechtl, N V; Sheehan, D M

2000-01-01

57

In vitro antimicrobial activity of Medilox® super-oxidized water  

PubMed Central

Aim Super-oxidized water is one of the broad spectrum disinfectants, which was introduced recently. There are many researches to find reliable chemicals which are effective, inexpensive, easy to obtain and use, and effective for disinfection of microorganisms leading hospital infections. Antimicrobial activity of super-oxidized water is promising. The aim of this study was to investigate the in-vitro antimicrobial activity of different concentrations of Medilox® super-oxidized water that is approved by the Food and Drug Administration (FDA) as high level disinfectant. Material and methods In this study, super-oxidized water obtained from Medilox® [Soosan E & C, Korea] device, which had been already installed in our hospital, was used. Antimicrobial activities of different concentrations of super-oxidized water (1/1, 1/2, 1/5, 1/10, 1/20, 1/50, 1/100) at different exposure times (1, 2, 5, 10, 30 min) against six ATCC strains, eight antibiotic resistant bacteria, yeasts and molds were evaluated using qualitative suspension test. Dey-Engley Neutralizing Broth [Sigma-Aldrich, USA] was used as neutralizing agent. Results Medilox® was found to be effective against all standard strains (Acinetobacter baumannii 19606, Escherichia coli 25922, Enterococcus faecalis 29212, Klebsiella pneumoniae 254988, Pseudomonas aeruginosa 27853, Staphylococcus aureus 29213), all clinical isolates (Acinetobacter baumannii, Escherichia coli, vancomycin-resistant Enterococcus faecium, Klebsiella pneumoniae, Pseudomonas aeruginosa, methicillin-resistant Staphylococcus aureus, Bacillus subtilis, Myroides spp.), and all yeastsat 1/1 dilution in ??1 minute. It was found to be effective on Aspergillus flavus at 1/1 dilution in ??2 minutes and on certain molds in ??5 minutes. Conclusion Medilox® super-oxidized water is a broad spectrum, on-site producible disinfectant, which is effective on bacteria and fungi and can be used for the control of nosocomial infection. PMID:25023905

2014-01-01

58

Psoralen activates cartilaginous cellular functions of rat chondrocytes in vitro.  

PubMed

Abstract Context: Psoralen, an active ingredient from Fructus Psoraleae (FP), is used in Traditional Chinese Medicine (TCM) to treat bone diseases. However, the effect of psoralen on cartilage is unknown. Objective: To investigate the effects of psoralen on chondrocytes isolated from rats. Materials and methods: Chondrocytes were treated with different concentrations of psoralen (1, 10, and 100??M) in vitro at 3-d and 9-d intervals. MTS assay, Alcian blue colorimetry, western blotting, and qRT-PCR, respectively, were used to evaluate the effects of psoralen on cell viability, glycosaminoglycan (GAG) synthesis, collagen synthesis, and cartilage-specific gene expression. Results: Psoralen dosages of 1-10??M exhibited low cytotoxicity toward chondrocytes. However, a dosage of 100??M suppressed the proliferation of chondrocytes. Different concentrations of psoralen treatments on chondrocytes revealed that GAG and Type II collagen synthesis increased, especially at 100??M, by 0.39-fold and 0.48-fold, respectively, on day 3, and by 0.51-fold and 0.56-fold, respectively, on day 9. Similarly, gene expression of Type II collagen, aggrecan, and SOX-9 were all up-regulated on days 3 and 9, particularly aggrecan which increased significantly by 9.37-fold and 7.32-fold at 100??M. Additionally, Type I collagen was inhibited both in gene expression and in protein synthesis. Conclusion: The results showed that psoralen promotes cartilaginous extracellular matrix (ECM) synthesis, as well as increased cartilaginous gene expression, and it may be a useful bioactive component for activating the cartilaginous cellular functions of chondrocytes. PMID:25471084

Xu, Kang; Pan, Xin; Sun, Yanjun; Xu, Wei; Njunge, Lucy; Yang, Li

2014-12-01

59

Genistein and daidzein modulate in vitro rat uterine contractile activity.  

PubMed

The present study investigated the effect of genistein, daidzein and estradiol on in vitro rat uterine responsiveness to oxytocin (OT) and PGF(2)alpha or luprostiol (L). In a first experiment, animals were either sham-operated (SH; n=5), or ovariectomized (OVX; n=20) and orally treated for three months with either genistein (G; n=5; 10 microg/g BW/d) or daidzein (D; n=5; 10 microg/g BW/d) or 17 alpha-ethinylestradiol (E; n=5; 23 microg/kg BW/d) or untreated (OVX; n=5). At necropsy, the basal uterine tension was lower in OVX, G and D than in SH, the highest value being measured in E. Oxytocin (10(-12); 10(-11) M) or PGF(2)alpha (10(-12); 10(-9) M) induced an increase in SH, but not in OVX, E and G. In D, only the highest doses were efficient. In a second experiment, 20 intact animals were s.c. injected with either genistein (G; n=5; 10 microg/g BW) or daidzein (D; n=5; 10 microg/g BW) or estradiol benzoate (E; n=5; 23 microg/kg BW) or vehicle (C: controls; n=5), and killed 24 h later. In C and E, OT (10(-15) to 10(-10) M) or L (10(-12) to 10(-7) M) stimulated uterine contractile activity in a dose-dependent manner until a maximal level. On the opposite, in G and D, contractile agents (except the highest luprostiol doses) did not stimulate myometrium contractions. Moreover, radioligand binding assays showed that genistein or daidzein inhibited the specific binding of [(3)H] estradiol to the calf uterus estrogen receptor (ER). Therefore, it could be postulated that both genistein and daidzein might bind to the rat uterus ER, inducing either anti-estrogenic or very weak estrogenic effects (depending on the experimental conditions) on in vitro uterine responsiveness to OT and PGF(2)alpha or luprostiol. PMID:11226836

Picherit, C; Dalle, M; Néliat, G; Lebecque, P; Davicco, M J; Barlet, J P; Coxam, V

2000-12-15

60

Danthron activates AMP-activated protein kinase and regulates lipid and glucose metabolism in vitro  

PubMed Central

Aim: To discover the active compound on AMP-activated protein kinase (AMPK) activation and investigate the effects of the active compound 1,8-dihydroxyanthraquinone (danthron) from the traditional Chinese medicine rhubarb on AMPK-mediated lipid and glucose metabolism in vitro. Methods: HepG2 and C2C12 cells were used. Cell viability was determined using MTT assay. Real-time PCR was performed to measure the gene expression. Western blotting assay was applied to investigate the protein phosphorylation level. Enzymatic assay kits were used to detect the total cholesterol (TC), triglyceride (TG) and glucose contents. Results: Danthron (0.1, 1, and 10 ?mol/L) dose-dependently promoted the phosphorylation of AMPK and acetyl-CoA carboxylase (ACC) in both HepG2 and C2C12 cells. Meanwhile, danthron treatment significantly reduced the lipid synthesis related sterol regulatory element-binding protein 1c (SREBP1c) and fatty acid synthetase (FAS) gene expressions, and the TC and TG levels. In addition, danthron treatment efficiently increased glucose consumption. The actions of danthron on lipid and glucose metabolism were abolished or reversed by co-treatment with the AMPK inhibitor compound C. Conclusion: Danthron effectively reduces intracellular lipid contents and enhanced glucose consumption in vitro via activation of AMPK signaling pathway. PMID:23770982

Zhou, Rong; Wang, Ling; Xu, Xing; Chen, Jing; Hu, Li-hong; Chen, Li-li; Shen, Xu

2013-01-01

61

IN VITRO AND IN VIVO DEVELOPMENTAL COMPETENCE OF OVULATED AND IN VITRO MATURED PORCINE OOCYTES ACTIVATED BY ELECTRICAL ACTIVATION  

Technology Transfer Automated Retrieval System (TEKTRAN)

The objective of this study was to evaluate the in vitro and in vivo developmental competence of parthenogenetic (parthenote) pig embryos derived from ovulated and in vitro matured (IVM) oocytes. A total of four experiments were carried out. These demonstrated that the mean blastocyst rates from s...

62

Antioxidant, Antibacterial and Antischistosomal Activities of Extracts from Grateloupia livida (Harv). Yamada  

PubMed Central

The present study was designated to evaluate the antioxidant, antibacterial and antischistosomal activities of Grateloupia livida (GL) extracts in vitro. A GL Ethanol extract (EE) was separated into petroleum ether (PE), ethyl acetate (EA), n-butyl alcohol (BuOH) and aqueous (AQ) fractions to fractionate the polar and non-polar compounds in the EE. Extracts antioxidant activities were evaluated in vitro by DPPH radical-scavenging, deoxyribose radical scavenging, and ?-carotene bleaching assays, all using butylated hydroxytoluene (BHT) as the reference antioxidant compound. The most effective antioxidant properties were observed in the PE fraction in all three assays. Antimicrobial testing showed that the PE fraction exhibited broad-spectrum antimicrobial activity, with the PE fraction also exhibiting strong activity against the human pathogenic trematode S. japonicum adult worm. In order to investigate the relationships between bioactivity and chemical composition, the chemical composition of the PE fraction was analyzed by gas chromatography-mass spectrometry (GC-MS). In total, 25 components were identified in the PE fraction, most of which have known antioxidant and antimicrobial activities. However, none of the compounds have reported activity against Schistosoma, suggesting that the schistosomicidal activity of the PE fraction may be related to minor constituents present in the extract, or governed by more intricate synergistic or additive relationships. Finally, fractions with the greatest biological activity displayed neither cellular cytotoxicity, at concentrations up to 100 ug/ml, or acute oral toxicity in mice, at doses up to 2000 mg/kg. Based on antioxidant, antimicrobial, antischistosomal activities, and low toxicity, the PE fraction possesses properties useful for food preservation and overall improvement of human health. PMID:24312216

Yao, Fen; Chen, Weizhou; Zhong, Shuping; Zheng, Fuchun; Shi, Ganggang

2013-01-01

63

Processed tart cherry products--comparative phytochemical content, in vitro antioxidant capacity and in vitro anti-inflammatory activity.  

PubMed

Processing of fruits and vegetables affects their phytochemical and nutrient content. Tart cherries are commercially promoted to possess antioxidant and anti-inflammatory activity. However, processing affects their phytochemical content and may affect their related health benefits. The current study compares the in vitro antioxidant capacity and anti-inflammatory cyclooxygenase activity of processed tart cherry (Prunus cerasus) products-cherry juice concentrate, individually quick-frozen cherries, canned cherries, and dried cherries. Cherry products were analyzed for total anthocyanin and proanthocyanidin content and profile. On a per serving basis, total anthocyanins were highest in frozen cherries and total proanthocyanidins were highest in juice concentrate. Total phenolics were highest in juice concentrate. Juice concentrate had the highest oxygen radical absorbance capacity (ORAC) and peroxynitrite radical averting capacity (NORAC). Dried cherries had the highest hydroxyl radical averting capacity (HORAC) and superoxide radical averting capacity (SORAC). Processed tart cherry products compared very favorably to the U.S. Dept. of Agriculture-reported ORAC of other fresh and processed fruits. Inhibition of in vitro inflammatory COX-1 activity was greatest in juice concentrate. In summary, all processed tart cherry products possessed antioxidant and anti-inflammatory activity, but processing differentially affected phytochemical content and in vitro bioactivity. On a per serving basis, juice concentrate was superior to other tart cherry products. PMID:23163942

Ou, Boxin; Bosak, Kristen N; Brickner, Paula R; Iezzoni, Dominic G; Seymour, E Mitchell

2012-05-01

64

Agelasine F from a Philippine Agelas sp. sponge exhibits in vitro antituberculosis activity.  

PubMed

Marine sponge samples were collected in Baler, Aurora, Philippines, and extracts were tested for in vitro antituberculosis activity. An orange Agelas sp. sponge yielded the known compound, agelasine F, which inhibited some drug resistant strains of Mycobacterium tuberculosis in vitro at concentrations as low as 3.13 micrograms/ml. Activity against M. tuberculosis residing within macrophages required concentrations of 13-22 micrograms/ml which was below the IC50 for Vero cells (34 micrograms/ml). PMID:10865457

Mangalindan, G C; Talaue, M T; Cruz, L J; Franzblau, S G; Adams, L B; Richardson, A D; Ireland, C M; Concepcion, G P

2000-05-01

65

Antimalarial activity in vitro of Cochlospermum tinctorium tubercle extracts  

Microsoft Academic Search

Resistance of Plasmodium falciparum to current antimalarial compounds has drastically increased during the last few years and is now a major public health problem. We have studied plants traditionally used in Africa against malaria. Extracts of the tubercles of Cochlospermum tinctorium A. Rich, commonly used in Burkina Faso, were tested in vitro on 2 strains of P. falciparum, one (FcB1-Colombia)

F. Benoit; A. Valentin; Y. Pélissier; C. Marion; Z. Dakuyo; M. Mallié; J.-M. Bastide

1995-01-01

66

In vitro antioxidant activity of polysaccharide from Gardenia jasminoides ellis  

USGS Publications Warehouse

A water-soluble polysaccharide, GP, was isolated from Gardenia jasminoides Ellis through hot water extraction followed by ethanol precipitation. The in vitro free radicals scavenging tests exhibited that GP has significant scavenging abilities especially for ABTS, DPPH, and hydroxyl radicals, which suggests that the polysaccharide GP is a novel antioxidant. ?? 2011 Academic Journals.

Fan, Y.; Ge, Z.; Luo, A.

2011-01-01

67

In Vitro Fungicidal Activities of Voriconazole, Itraconazole, and Amphotericin B against Opportunistic Moniliaceous and Dematiaceous Fungi  

Microsoft Academic Search

The NCCLS proposed standard M38-P describes standard parameters for testing the fungistatic antifungal activities (MICs) of established agents against filamentous fungi (molds); however, standard conditions are not available for testing their fungicidal activities (minimum fungicidal or lethal concentrations (MFCs)). This study evaluated the in vitro fungistatic and fungicidal activities of voriconazole, itraconazole, and amphotericin B against 260 common and emerging

ANA ESPINEL-INGROFF

2001-01-01

68

In vitro studies on antiradical and antioxidant activities of fenugreek ( Trigonella foenum graecum) seeds  

Microsoft Academic Search

An extract of fenugreek (Trigonella foenum graecum) seeds was isolated and evaluated for antioxidant activity using various in vitro assay systems. The seed extract exhibited scavenging of hydroxyl radicals (OH) and inhibition of hydrogen peroxide-induced lipid peroxidation in rat liver mitochondria. The OH scavenging activity of the extract was evaluated by pulse radiolysis and the deoxyribose system. The antimutagenic activity

S. Kaviarasan; G. H. Naik; R. Gangabhagirathi; C. V. Anuradha; K. I. Priyadarsini

2007-01-01

69

In vitro cultures of Bituminaria bituminosa: pterocarpan, furanocoumarin and isoflavone production and cytotoxic activity evaluation.  

PubMed

Bituminaria bituminosa L. is known for producing several compounds with considerable pharmaceutical interest, such as phenylpropanoids, furanocoumarins and pterocarpans. In vitro cultures of seedlings, shoots, and callus have been produced to obtain plant materials useful for the production of these metabolites. The secondary metabolite profile was evaluated by HPLC-DAD. The extracts of all the in vitro material contained the flavonoid daidzein, while plicatin B, erybraedin C and bitucarpin A were found only in the extracts of the in vitro shoots and in wild shoots. The furanocoumarins angelicin and psoralen were found in in vivo and in vitro plants, but in the callus were not detectable. The extracts were also tested for cytotoxic activity in HeLa cell culture; the highest level of cytotoxicity was found in in vitro shoot extracts. PMID:24868860

D'Angiolillo, Francesca; Pistellia, Laura; Noccioli, Cecilia; Ruffoni, Barbara; Piaggi, Simona; Scarpato, Roberto; Pistelli, Luisa

2014-04-01

70

In Vitro Antioxidant Activities of Sulfated Derivatives of Polysaccharides Extracted from Auricularia auricular  

PubMed Central

In this research, two types of sulfated polysaccharide derivatives were successfully synthesized. Their antioxidant activities were investigated by employing various established in vitro systems. In addition, the degree of sulfation was evaluated using ion-chromatography and IR spectra. The results verify that, when employing scavenging superoxide radical tests, both the sulfation of acid Auricularia auricular polysaccharides (SAAAP) and the sulfation of neutral Auricularia auricular polysaccharides (SNAAP) derivatives possessed considerable antioxidant activity and had a more powerful antioxidant competence than that of the native non-sulfated polysaccharides (AAAP and NAAP). On the other hand, AAAP and NAAP exhibited stronger activity on scavenging both the hydroxyl radical and lipid peroxidation. Available data obtained with in vitro measurements indicates that the sulfated groups of AAAP and NAAP played an important role on antioxidant activity. In sum, the research demonstrates that the antioxidant activity of sulfated polysaccharide derivatives in vitro has a potential significance for seeking new natural antioxidant protective agents. PMID:21686185

Zhang, Hua; Wang, Zhen-Yu; Yang, Lin; Yang, Xin; Wang, Xue; Zhang, Zhi

2011-01-01

71

miRNA studies in in vitro and in vivo activated hepatic stellate cells  

PubMed Central

AIM: To understand which and how different miRNAs are implicated in the process of hepatic stellate cell (HSC) activation. METHODS: We used microarrays to examine the differential expression of miRNAs during in vitro activation of primary HSCs (pHSCs). The transcriptome changes upon stable transfection of rno-miR-146a into an HSC cell line were studied using cDNA microarrays. Selected differentially regulated miRNAs were investigated by quantitative real-time polymerase chain reaction during in vivo HSC activation. The effect of miRNA mimics and inhibitor on the in vitro activation of pHSCs was also evaluated. RESULTS: We found that 16 miRNAs were upregulated and 26 were downregulated significantly in 10-d in vitro activated pHSCs in comparison to quiescent pHSCs. Overexpression of rno-miR-146a was characterized by marked upregulation of tissue inhibitor of metalloproteinase-3, which is implicated in the regulation of tumor necrosis factor-? activity. Differences in the regulation of selected miRNAs were observed comparing in vitro and in vivo HSC activation. Treatment with miR-26a and 29a mimics, and miR-214 inhibitor during in vitro activation of pHSCs induced significant downregulation of collagen type?I?transcription. CONCLUSION: Our results emphasize the different regulation of miRNAs in in vitro and in vivo activated pHSCs. We also showed that miR-26a, 29a and 214 are involved in the regulation of collagen type I mRNA. PMID:21734783

Maubach, Gunter; Lim, Michelle Chin Chia; Chen, Jinmiao; Yang, Henry; Zhuo, Lang

2011-01-01

72

Luliconazole demonstrates potent in vitro activity against dermatophytes recovered from patients with onychomycosis.  

PubMed

The in vitro activities of luliconazole, amorolfine, ciclopirox, and terbinafine were determined against 320 dermatophyte isolates from large toenails of onychomycosis patients enrolled into an ongoing phase 2b/3 clinical study. The geometric mean MIC for luliconazole was 0.00022 ?g/ml against all isolates, compared to 0.0194 to 0.3107 ?g/ml for the three other agents. The in vitro potency of luliconazole was maintained regardless of the dermatophyte species. PMID:24709260

Wiederhold, Nathan P; Fothergill, Annette W; McCarthy, Dora I; Tavakkol, Amir

2014-06-01

73

Inhibition of house fly microsomal aldrin epoxidase activity by juvenile hormone analogs in vitro  

E-print Network

INHIBITION OF HOUSE FLY MICROSOMAL ALDRIN EPOXIDASE ACTIVITY BY JUVENILE HORMONE ANALOGS IN VITRO A Thesis by GEORGE ELLIS SPATES, JR. Submitted to the Graduate College of Texas A&M University in partial fulfillment of the requirement... for the degree of MASTER OF SCIENCE August 1974 Major Subject: Entomology INHIBITION OF HOUSE FLY MICROSOMAL ALDRIN EXPOXIDASE ACTIVLTY BY JUVENI'LE HORMONE ANALOGS IN VITRO A Theseus by GEORGE ELLIS SPATES, JR. Approved as to style and content by: 1...

Spates, George Ellis

1974-01-01

74

Appraisal of in vitro and in vivo antioxidant activity potential of cornelian cherry leaves.  

PubMed

The antioxidant activity of the 80% methanolic extract of Cornus mas L. leaves (CMM) was evaluated by various methods both in vitro and in vivo. In vitro screening tests indicated that CMM had high antioxidant activity in terms of free radical scavenging and metal reducing activity. In vivo antioxidant activity studies in normal healthy rats demonstrated that the total antioxidant capacity of liver homogenates were increased, although no changes were observed in the activities of antioxidant enzymes superoxide dismutase, catalase and glutathione peroxidase or in the level of lipid peroxidation. Studies on CCl4-treated rats also showed that CMM restored the activities of antioxidant enzymes, lowered the level of lipid peroxidation and elevated the total antioxidant capacities of both the total blood and liver homogenates of the animals. Further activity-guided fractionation studies led to the isolation of gallic acid, a well-known antioxidant, as one of the active components. PMID:24035707

Celep, Engin; Ayd?n, Ahmet; K?rm?z?bekmez, Hasan; Yesilada, Erdem

2013-12-01

75

In Vitro Activity of SCH-56592 and Comparison with Activities of Amphotericin B and Itraconazole against Aspergillus spp  

Microsoft Academic Search

In this study, we investigated the in vitro activity of SCH-56592 (SCH), a new triazole antifungal agent. We compared the activity of SCH with those of itraconazole (ITZ) and amphotericin B (AB) against 60 clinical isolates of Aspergillus spp. by using a microtiter format. Incubation was done at 37°C for 48 h, and MIC endpoints (no growth) were read visually.

KAREN L. OAKLEY; CAROLINE B. MOORE; DAVID W. DENNING

1997-01-01

76

Design, synthesis and in vitro antitumor activity evaluation of novel 4-pyrrylamino quinazoline derivatives  

PubMed Central

Here we describe the design and synthesis of two series of 4-pyrrylamino quinazolines as new analogues of the EGFR inhibitor Gefitinib. In vitro antitumor activity of these novel compounds against pancreatic (Miapaca2) and prostate (DU145) cancer cell lines was evaluated. Compared with the parental Gefitinib, all the 18 derivatives show a greatly increased cytotoxicity to cancer cells. In vitro kinase inhibitory activity on EGFR was also investigated. Among them, compounds GI-6, GII-4, GII-6, GII-8, and GII-9 are more potential RTK inhibitors. Based on these results, we propose simple structure-activity relationship to provide information for designing and developing more potent antitumor agents. PMID:21895983

Wu, Xiaoqing; Li, Mingdong; Tang, Wenhua; Zheng, Youguang; Lian, Jiqin; Xu, Liang; Ji, Min

2011-01-01

77

Macrophage activation and leishmanicidal activity by galactomannan and its oxovanadium (IV/V) complex in vitro.  

PubMed

Compounds that activate macrophage antimicrobial activity are potential targets for treatment of leishmaniasis. The present study investigated the in vitro immunomodulatory effects of a galactomannan (GALMAN-A) isolated from seeds of Mimosa scabrella and its oxovanadium (IV/V) complex (GALMAN-A:VO(2+)/VO(3+)) on macrophage activity. GALMAN-A increased nitric oxide levels by ~33% at a concentration of 250?g/ml, while GALMAN-A:VO(2+)/VO(3+) decreased nitric oxide levels by ~33% at a concentration of 50?g/ml. Furthermore, GALMAN-A increased interleukin-1 beta (IL-1?) and interleukin-6 (IL-6) levels by 5.5 and 2.3 times, respectively, at a concentration of 25?g/ml; at the same concentration, GALMAN-A:VO(2+)/VO(3+) promoted an increase in IL-1? and IL-6 production by 8 and 5.5 times, respectively. However, neither GALMAN-A nor GALMAN-A:VO(2+)/VO(3+) affected tumor necrosis factor alpha (TNF-?) or interleukin-10 (IL-10) levels. Importantly, both GALMAN-A and GALMAN-A:VO(2+)/VO(3+) exhibited leishmanicidal activity on amastigotes of Leishmania (L.) amazonensis, reaching ~60% activity at concentrations of 100 and 25?g/ml, respectively. These results indicate that GALMAN-A is three times more potent and its oxovanadium complex is twelve times more potent than Glucantime (300?g/ml), which is the drug of choice in leishmaniasis treatment. The IC50 value for GALMAN-A:VO(2+)/VO(3+) was 74.4?g/ml (0.58?g/ml of vanadium). Thus, the significant activation of macrophages and the noted leishmanicidal effect demonstrate the need for further studies to clarify the mechanisms of action of these compounds. PMID:24169303

Adriazola, Izabela Ono; Evangelista do Amaral, Alex; Amorim, Juliana Carolina; Correia, Beatriz Lourenço; Petkowicz, Carmen Lúcia Oliveira; Mercę, Ana Lucia Ramalho; Noleto, Guilhermina Rodrigues

2014-03-01

78

Telomerase activity reconstituted in vitro with purified human telomerase reverse transcriptase and human telomerase RNA component.  

PubMed

Telomerase is a specialized reverse transcriptase that catalyzes elongation of the telomeric tandem repeat, TTAGGG, by addition of this sequence to the ends of existing telomeres. Human telomerase reverse transcriptase (hTERT) has been identified as a catalytic enzyme involved in telomere elongation that requires telomerase RNA, human telomerase RNA component (hTR), as an RNA template. We established a new method to express and purify soluble insect-expressed recombinant hTERT. The partially purified FLAG-hTERT retained the catalytic activity of telomerase in a complementation assay in vitro to exhibit telomerase activity in telomerase-negative TIG3 cell extract and in a reconstitution assay with FLAG-hTERT and purified hTR in vitro. FLAG-hTERT (D712A) with a mutation in the VDV motif exhibited no telomerase activity, confirming the authentic catalytic activity of FLAG-hTERT. The reconstituted complex of FLAG-hTERT and hTR in vitro was detected by electrophoretic mobility shift assay, and its activity was stimulated by more than 30-fold by TIG3 cell extract. This suggested that some cellular component(s) in the extract facilitated the reconstituted telomerase activity in vitro. Geldanamycin had no effect on the reconstituted activity but partially reduced the stimulated activity of the reconstituted telomerase by the TIG3 cell extract, suggesting that Hsp90 may contribute to the stimulatory effect of the cellular components. PMID:10811633

Masutomi, K; Kaneko, S; Hayashi, N; Yamashita, T; Shirota, Y; Kobayashi, K; Murakami, S

2000-07-21

79

In vitro antioxidant activity of Holarrhena antidysenterica Wall. methanolic leaf extract  

PubMed Central

Antioxidative potential of methanolic leaf extract of Holarrhena antidysenterica was evaluated using hydroxyl radical, superoxide anion scavenging and reducing power assays. The antioxidant activity of the methanol extract increased in a concentration-dependent manner. The extract showed significant reactive oxygen species (ROS) scavenging activity in all in vitro antioxidant assays and contained high level of total phenolic content PMID:24826020

Ganapathy, P. S. Sujan; Ramachandra, Y. L.; Rai, S. Padmalatha

2011-01-01

80

In vitro fertilization and artificial activation of eggs of the direct-developing anuran Eleutherodactylus coqui  

Microsoft Academic Search

Although much is known about the reproductive biology of pond-breeding frogs, there is comparatively little information about terrestrial-breeding anurans, a highly successful and diverse group. This study investigates the activation and in vitro fertilization of eggs of the Puerto Rican coqui frog obtained by hormonally induced ovulation. We report that spontaneous activation occurs in 34% of eggs, probably in response

Esteban Toro; Scott F Michael

2004-01-01

81

In vitro and In vivo Wound Healing-Promoting Activities of Human Cathelicidin LL37  

Microsoft Academic Search

The human antimicrobial peptide LL-37 plays an important role in host defense against infection. In addition to its antimicrobial action, other activities have been described in eukaryotic cells that may contribute to the healing response. In this study, we demonstrated that in vitro human cathelicidin activates migration of the human keratinocyte cell line HaCaT, involving phenotypic changes related to actin

Marta Carretero; María J Escámez; Marta García; Blanca Duarte; Almudena Holguín; Luisa Retamosa; Jose L Jorcano; Marcela del Río; Fernando Larcher

2008-01-01

82

In vitro Antifungal Activity of Thai Herb and Spice Extracts against Food Spoilage Fungi  

Microsoft Academic Search

The screening of Thai herbs and spices was carried out to investigate their in vitro antifungal activity against Aspergillus niger, A. oryzaeand Penicilliumsp. by using agar well diffusion method. Of thirteen plants tested, crude ethanol extracts of three, namely Piper betel, Boesenbergia pandurata, Andrographis paniculata exhibited antifungal activity against all test microorganisms. Penicillium sp. was more resistant to the extracts

Penkhae Wanchaitanawong; Piyamat Chaungwanit; Ngamtip Poovarodom; Sunee Nitisinprasert

83

Serum suppression of lymphocyte activation in vitro in acquired immunodeficiency disease  

Microsoft Academic Search

Sera from nine men and one woman having the recently described acquired immunodeficiency disease syndrome (AID) were studied for effects on healthy control lymphocyte activationin vitro by two T-lymphocyte activators, phytohemagglutinin (PHA) and allogeneic lymphocytes in the mixed lymphocyte culture (MLC) reaction. Selected sera were also tested for blocking of endogenous natural killer (NK) activity against the K562 tumor target.

Susanna Cunningham-Rundles; Mary Ann Michelis; Henry Masur

1983-01-01

84

Synthesis and Biological Evaluation of 1,4-Naphthoquinones and Quinoline-5,8-diones as Antimalarial and Schistosomicidal Agents  

PubMed Central

Improving the solubility of polysubstituted 1,4-naphthoquinone derivatives was achieved by introducing nitrogen in two different positions of the naphthoquinone core, at C-5 and at C-8 of menadione through a two-step, straightforward synthesis based on the regioselective hetero-Diels-Alder reaction. The antimalarial and the antischistosomal activities of these polysubstituted aza-1,4-naphthoquinone derivatives were evaluated and led to the selection of distinct compounds for antimalarial versus antischistosomal action. The AgII-assisted oxidative radical decarboxylation of the phenyl acetic acids using AgNO3 and ammonium peroxodisulfate was modified to generate the 3-picolinyl-menadione with improved pharmacokinetic parameters, high antimalarial effects and capacity to inhibit the formation of ?-hematin. PMID:22777178

Lanfranchi, Don Antoine; Cesar-Rodo, Elena; Bertrand, Benoît; Huang, Hsin-Hung; Day, Latasha; Johann, Laure; Elhabiri, Mourad; Becker, Katja; Williams, David L.

2012-01-01

85

Bromelain enzyme from pineapple: in vitro activity study under different micropropagation conditions.  

PubMed

The aim of this work was to evaluate the activity of bromelain in pineapple plants (Ananas comosus var. Comosus), Pérola cultivar, produced in vitro in different culture conditions. This enzyme, besides its pharmacological effects, is also employed in food industries, such as breweries and meat processing. In this work, the enzymatic activity was evaluated in the tissues of leaves and stems of plants grown in culture medium without plant growth regulator. The most significant levels of bromelain were observed in leaf tissue after 4 months of culture in vitro in medium with a filter paper bridge, followed by medium gelled by the agar. The results of this study, regarding the different structures of the pineapple (leaves and stems) in vitro showed that the activity of bromelain varied depending on the culture conditions, the time and structure of which was quantified, ensuring a viable strategy in the production of seedlings with high levels of bromelain in subsequent phases of micropropagation. PMID:22736274

Vilanova Neta, Jaci Lima; da Silva Lédo, Ana; Lima, Aloisio André Bonfim; Santana, José Carlos Curvelo; Leite, Nadjma Souza; Ruzene, Denise Santos; Silva, Daniel Pereira; de Souza, Roberto Rodrigues

2012-09-01

86

Vaccinia virus late transcription is activated in vitro by cellular heterogeneous nuclear ribonucleoproteins.  

PubMed

Vaccinia virus gene expression is temporally regulated, and three gene classes have been identified: early, intermediate, and late. Several virus-encoded proteins and an activity designated VLTF-X are required for maximum transcription in vitro of a template containing a late promoter. VLTF-X is present in both cytoplasmic and nuclear extracts prepared from uninfected mammalian cells and co-purifies with a late promoter DNA-binding activity. Here, extensive purification of VLTF-X has revealed that heterogeneous nuclear ribonucleoproteins A2/B1 and RBM3 co-purified with in vitro late transcription stimulation. Overexpression and purification of these proteins from Escherichia coli demonstrated that they both complemented for VLTF-X activity in in vitro transcription reactions. These studies identify two host cell factors potentially contributing to poxvirus replication in vivo. PMID:11546759

Wright, C F; Oswald, B W; Dellis, S

2001-11-01

87

Bioprotective properties of Dragon's blood resin: In vitro evaluation of antioxidant activity and antimicrobial activity  

PubMed Central

Background Food preservation is basically done to preserve the natural characteristics and appearance of the food and to increase the shelf life of food. Food preservatives in use are natural, chemical and artificial. Keeping in mind the adverse effects of synthetic food preservatives, there is a need to identify natural food preservatives. The aims of this study were to evaluate in vitro antioxidant and antimicrobial activities of Dragon's blood resin obtained from Dracaena cinnabari Balf f., with a view to develop safer food preservatives. Methods In this study, three solvents of varying polarity were used to extract and separate the medium and high polarity compounds from the non-polar compounds of the Dragon's blood resin. The extracts were evaluated for their antimicrobial activity against the food borne pathogens. The antioxidant activities of the extracts were assessed using DPPH and ABTS radical scavenging, FRAP, metal chelating and reducing power assays. Total phenolics, flavonoids and flavonols of extracts were also estimated using the standard methods. Results Phytochemical analysis of extracts revealed high phenolic content in CH2Cl2 extract of resin. Free radical scavenging of CH2Cl2 extract was found to be highest which is in good correlation with its total phenolic content. All test microorganisms were also inhibited by CH2Cl2 extract. Conclusions Our result provide evidence that CH2Cl2 extract is a potential source of natural antioxidant compounds and exhibited good inhibitory activity against various food borne pathogens. Thus, CH2Cl2 extract of Dragon's blood resin could be considered as possible source of food preservative. PMID:21329518

2011-01-01

88

In vitro and in vivo activities of Peganum harmala extract against Leishmania major  

PubMed Central

BACKGROUND: In vitro and in vivo antileishmanial activities of crude hydroalcoholic extract of peganum harmala seeds were investigated against Leishmania major. METHODS: The extract of aerial parts of P harmala was obtained by maceration. The in vitro experiments were performed on promastigotes to assess antileishmanial activity of the extract using amphotericin B as a reference. The in vivo studies were carried out on cutaneous leishmaniasis in outbred mice to evaluate the effects of topical application of the ointment-based extract. RESULTS: The in vitro experiments showed a concentration-dependent decrease of parasites number caused by the extract with an IC50 value of 59.4 ?g/ml. In vivo studies demonstrated a significant post-treatment decrease in the lesion size and parasite count in infected animals, compared to placebo and control groups. High performance liquid chromatography (HPLC) of the crude extract demonstrated the existence of harmaline and harmine as beta-carboline alkaloids. CONCLUSIONS: P harmala seeds extract showed significant in vitro and in vivo antileishmanial activities. Most biological activity of the extract could be attributed to its beta-carboline content. However, another alkaloid of P harmala seeds extract, peganine, has also been reported to have antileishmanial activity. These beneficial effects can be attributed to the cumulative effects of various biologically active components present in it. PMID:22279479

Rahimi-Moghaddam, Parvaneh; Ebrahimi, Soltan Ahmed; Ourmazdi, Hourmazd; Selseleh, Monawar; Karjalian, Maryam; Haj-Hassani, Giti; Alimohammadian, Mohammad Hossein; Mahmoudian, Massoud; Shafiei, Massoumeh

2011-01-01

89

In vitro and in vivo activities of SM101, a mixture of metampicillin and sulbactam  

Microsoft Academic Search

SM-101 is a mixture of metampicillin and sulbactam(2?1). The antibacterial activities of SM-101 were compared with those of\\u000a metampicillin, piperacillin and Augmentin. It showed powerful antibacterial activities against major strains. ExceptP. aeruginosa andS. marcescens, thein vitro antibacterial activity of SM-101 was higher than those of metampicillin, piperacillin and Augmentin againstStaphylococcus spp.,Streptococcus spp.,Morganella morganii, E. coli, andProteus spp. The ED50 values

Keum-Hwa Choi; Sook-Kyung Kim; Moon-Chang Baek; Byong-Kak Kim; Dong-Young Lee; Eung-Chil Choi

1995-01-01

90

How Much In Vitro Cholesterol Reducing Activity of Lactobacilli Predicts Their In Vivo Cholesterol Function?  

PubMed Central

Background: Based on literature, in vitro cholesterol removal of lactic acid bacteria has been accounted for their in vivo cholesterol reduction. But recently it has been proposed that such in vitro characteristic may not be directly relevant to their in vivo activity. The objective of this study was to find how much in vitro cholesterol reducing potential of Lactobacillus plantarum A7 (LA7), a native strain isolated from an infant fecal flora, reflects its in vivo efficiency. LA7 previously showed serum cholesterol reducing capability in mice subjected to fatty diet. Here, we investigate whether the given strain is capable of in vitro cholesterol assimilation or consumption. Method: LA7 was cultured in whole milk and de-Man–Rogosa–Sharpe (MRS) added with water-soluble cholesterol. Colorimetric method was adopted for cholesterol determination in both cultured media during incubation period. Results: No cholesterol assimilation was detected by growth and incubation of the active culture in either of the medium. Thus, in vivo cholesterol function of LA7 was not caused by cholesterol consumption. A comprehensive review of literature on the related studies also showed that there are other documented studies which evidenced the uncertainty of the direct relation between in vitro and in vivo studies. Conclusion: Cholesterol removal from the cultured media may not be considered as an appropriate integral index for selection of Lactobacillus strains with cholesterol-lowering activity. PMID:23671771

Madani, Golnoush; Mirlohi, Maryam; Yahay, Mahmoud; Hassanzadeh, Akbar

2013-01-01

91

In vitro antimalarial activity of prenylated flavonoids from Erythrina fusca.  

PubMed

Ethyl acetate (EtOAc) extract from the stem bark of Erythrina fusca showed a antimalarial activity against the multi-drug-resistant strain (K1) of Plasmodium falciparum, and six flavonoids, lupinifolin (1), citflavanone (2), erythrisenegalone (3), lonchocarpol A (4), liquiritigenin (5), and 8-prenyldaidzein (6), were isolated from the extract. Diprenylated flavanone 4 showed a notable antimalarial activity (IC(50); 1.6 microg/mL); however 1 and 3 did not show the activity, even though these compounds possessed prenylated substitution. PMID:18404327

Khaomek, Pranorm; Ichino, Chikara; Ishiyama, Aki; Sekiguchi, Hitomi; Namatame, Miyuki; Ruangrungsi, Nijsiri; Saifah, Ekarin; Kiyohara, Hiroaki; Otoguro, Kazuhiko; Omura, Satoshi; Yamada, Haruki

2008-04-01

92

Botulinum toxin suppression of CNS network activity in vitro.  

PubMed

The botulinum toxins are potent agents which disrupt synaptic transmission. While the standard method for BoNT detection and quantification is based on the mouse lethality assay, we have examined whether alterations in cultured neuronal network activity can be used to detect the functional effects of BoNT. Murine spinal cord and frontal cortex networks cultured on substrate integrated microelectrode arrays allowed monitoring of spontaneous spike and burst activity with exposure to BoNT serotype A (BoNT-A). Exposure to BoNT-A inhibited spike activity in cultured neuronal networks where, after a delay due to toxin internalization, the rate of activity loss depended on toxin concentration. Over a 30?hr exposure to BoNT-A, the minimum concentration detected was 2?ng/mL, a level consistent with mouse lethality studies. A small proportion of spinal cord networks, but not frontal cortex networks, showed a transient increase in spike and burst activity with exposure to BoNT-A, an effect likely due to preferential inhibition of inhibitory synapses expressed in this tissue. Lastly, prior exposure to human-derived antisera containing neutralizing antibodies prevented BoNT-A induced inhibition of network spike activity. These observations suggest that the extracellular recording from cultured neuronal networks can be used to detect and quantify functional BoNT effects. PMID:24688538

Pancrazio, Joseph J; Gopal, Kamakshi; Keefer, Edward W; Gross, Guenter W

2014-01-01

93

Botulinum Toxin Suppression of CNS Network Activity In Vitro  

PubMed Central

The botulinum toxins are potent agents which disrupt synaptic transmission. While the standard method for BoNT detection and quantification is based on the mouse lethality assay, we have examined whether alterations in cultured neuronal network activity can be used to detect the functional effects of BoNT. Murine spinal cord and frontal cortex networks cultured on substrate integrated microelectrode arrays allowed monitoring of spontaneous spike and burst activity with exposure to BoNT serotype A (BoNT-A). Exposure to BoNT-A inhibited spike activity in cultured neuronal networks where, after a delay due to toxin internalization, the rate of activity loss depended on toxin concentration. Over a 30?hr exposure to BoNT-A, the minimum concentration detected was 2?ng/mL, a level consistent with mouse lethality studies. A small proportion of spinal cord networks, but not frontal cortex networks, showed a transient increase in spike and burst activity with exposure to BoNT-A, an effect likely due to preferential inhibition of inhibitory synapses expressed in this tissue. Lastly, prior exposure to human-derived antisera containing neutralizing antibodies prevented BoNT-A induced inhibition of network spike activity. These observations suggest that the extracellular recording from cultured neuronal networks can be used to detect and quantify functional BoNT effects. PMID:24688538

Pancrazio, Joseph J.; Gopal, Kamakshi; Keefer, Edward W.; Gross, Guenter W.

2014-01-01

94

In vitro determination of the spermicidal activity of plant saponins.  

PubMed

The plant kingdom might yield an effective antifertility drug. A Mentha arvensis L. (Labiatae) fraction with uterotonic activity was isolated, and was found to be active on the nonpregnant as well as the pregnant rat uterus. According to folklore medicine, the Mexican plant Montanoa tomentosa Cerv. (zoapatle) possesses antifertility activity in women. The effect of various isolated preparations from this plant on early pregnancy were investigated in serveral rodent species including the mouse, rat hamster, and guinea pig. It was concluded that zoapatle plant extracts possess unique antifertility activity. Lin-Hsim and coworkers isolated fractions from Aristolochia molissima Hanceith contrceptive activity in female mice. Saponins of some plants were used in contraceptive formulations either as foaming agents or as spermicidal substances. Elbary and Nour investigated the spermicidal effects of saponins isolated from the following plants: Gypsophila paniculata L., Saponaria officinalis L., Enterolobium cyclocarpum, Griseb., Terminalia horrida Steud., Melilotus sicula Vitm., and Ruscus hypoglossum L. All of the saponins tested possessed spermicidal activity. Jain and coworkers isolated 2 new saponins in Pittosporum nilghrense with spermicidal effects. In this paper we have determined the spermicidal activity of saponins isolated from some Yugoslav plants, which in that aspect have not been investigated. The results are illustrated in the table. They show that all of the saponins tested were spermicidal in dependence on their nature. Saponins of Primula vulgaris Huds. and Cyclamen persicum Mill. immobilized human spermatozoa within a period of 20 s at a dilution 1:1000. Saponin of Gypsophila paniculata L. was spermicidal at dilution 1:20. These findings show that saponins isolated from some Yugoslav plants may be useful spermicides of natural origin. PMID:4080814

Primorac, M; Sekulovi?, D; Antoni?, S

1985-08-01

95

In vitro activity of Amazon plant extracts against Enterococcus faecalis.  

PubMed

Previous studies analyzing 2,200 plant extracts indicated anti-enterococcal activity in 25 extracts obtained from Brazilian forests' plants. In the present study, these extracts were subjected to microdilution broth assay (MDBA) and disk diffusion assay (DDA) using planktonic Enterococcus faecalis ATCC(®) 29212™ and were submitted to phytochemical analysis in TLC and HPLC. Three extracts obtained from Ipomoea alba (MIC < 40 ?g/mL), Diclinanona calycina (MIC ? 40 ?g/mL) and Moronobea coccinea (40 < MIC < 80 ?g/mL; MBC = 80 ?g/mL) showed significant bactericidal activity in the MDBA and four extracts obtained from I. alba (14.04 ± 0.55 mm diameter) S. globulifera (14.43 ± 0.33 mm and 12.18 ± 0.28 mm diameter) and Connarus ruber var. ruber (13.13 ± 0.18 mm diameter) were active in DDA. Residues H2O obtained from Psidium densicomum (mean of 16.78 mm diameter) and from Stryphnodendron pulcherrimum (mean of 15.97 mm diameter) have shown an improved antibacterial activity after fractionation if compared to that obtained from the respective crude extracts. Antioxidant activity was observed in some residues of the active extracts. TLC analysis showed that phenolic compounds are likely to be found in active extracts. Three molecules were isolated from S. globulifera and were identified by (13)C NMR lupeol, ?-amyrin and 3?-hydroxyglutin-5-ene. The present chemical and biological findings suggest that these extracts are a potential source of new anti-Enterococcus compounds to be introduced in endodontic therapy. PMID:25477906

de Castilho, Adriana Lígia; da Silva, Juliana Paola Correa; Saraceni, Cintia Helena Coury; Díaz, Ingrit Elida Collantes; Paciencia, Mateus Luís Barradas; Varella, Antonio Drauzio; Suffredini, Ivana Barbosa

2014-01-01

96

In vitro activities of four xyloglucan endotransglycosylases from Arabidopsis  

NASA Technical Reports Server (NTRS)

Xyloglucan endotransglycosylases (XETs) are encoded by a gene family in Arabidopsis thaliana. These enzymes modify a major structural component of the plant cell wall, xyloglucan, and therefore may influence plant growth and development. We have produced four Arabidopsis XETs (TCH4, Meri-5, EXGT and XTR9) using the baculovirus/insect cell system and compared their biochemical activities. TCH4, as previously demonstrated, and the other three proteins are capable of carrying out transglycosylation of xyloglucans. The K(m) for XLLGol acceptor oligosaccharide is in the range of 20-40 microM for all the XETs except XTR9, which has a Km of 5 microM and is significantly inhibited by high levels of XLLGol. All four enzymes are most active between pH 6.0 and 6.5. TCH4 and XTR9 have temperature optima of 18 degrees C, whereas Meri-5 and EXGT are most active at 28 and 37 degrees C, respectively. Although the activity levels of three of the XETs are not influenced by the presence of fucose on the xyloglucan polymer, XTR9 has a clear preference for non-fucosylated xyloglucan polymer. The four XETs show a marked preference for XLLGol over either XXFGol or XXXGol as acceptor oligosaccharide. All four XETs are glycosylated; however, only the activities of TCH4 and Meri-5 are affected by the removal of the N-glycan with PNGase F. These four enzymes most likely function solely as transglycosylases because xyloglucan endoglucanase activity was not apparent. Subtle differences in biochemical activities may influence the physiological functions of the distinct XETs in vivo.

Campbell, P.; Braam, J.; McIntire, L. V. (Principal Investigator)

1999-01-01

97

In vitro activity of Amazon plant extracts against Enterococcus faecalis  

PubMed Central

Previous studies analyzing 2,200 plant extracts indicated anti-enterococcal activity in 25 extracts obtained from Brazilian forests’ plants. In the present study, these extracts were subjected to microdilution broth assay (MDBA) and disk diffusion assay (DDA) using planktonic Enterococcus faecalis ATCC® 29212™ and were submitted to phytochemical analysis in TLC and HPLC. Three extracts obtained from Ipomoea alba (MIC < 40 ?g/mL), Diclinanona calycina (MIC ? 40 ?g/mL) and Moronobea coccinea (40 < MIC < 80 ?g/mL; MBC = 80 ?g/mL) showed significant bactericidal activity in the MDBA and four extracts obtained from I. alba (14.04 ± 0.55 mm diameter) S. globulifera (14.43 ± 0.33 mm and 12.18 ± 0.28 mm diameter) and Connarus ruber var. ruber (13.13 ± 0.18 mm diameter) were active in DDA. Residues H2O obtained from Psidium densicomum (mean of 16.78 mm diameter) and from Stryphnodendron pulcherrimum (mean of 15.97 mm diameter) have shown an improved antibacterial activity after fractionation if compared to that obtained from the respective crude extracts. Antioxidant activity was observed in some residues of the active extracts. TLC analysis showed that phenolic compounds are likely to be found in active extracts. Three molecules were isolated from S. globulifera and were identified by 13C NMR lupeol, ?-amyrin and 3?-hydroxyglutin-5-ene. The present chemical and biological findings suggest that these extracts are a potential source of new anti-Enterococcus compounds to be introduced in endodontic therapy. PMID:25477906

de Castilho, Adriana Lígia; da Silva, Juliana Paola Correa; Saraceni, Cintia Helena Coury; Díaz, Ingrit Elida Collantes; Paciencia, Mateus Luís Barradas; Varella, Antonio Drauzio; Suffredini, Ivana Barbosa

2014-01-01

98

In Vitro Anthelmintic Activity of Baliospermum montanum Muell. Arg roots  

PubMed Central

Alcohol and aqueous extracts from the roots of Baliospermum montanum Muell. Arg were investigated for their anthelmintic activity against Pheretima posthuma and Ascardia galli. Various concentrations (10-100 mg/ml) of each extract were tested in the bioassay, which involved determination of time of paralysis and time of death of the worms. Both the extracts exhibited significant anthelmintic activity at highest concentration of 100 mg/ml. Piperazine citrate (10 mg/ml) was included as standard reference and distilled water as control. PMID:20390101

Mali, R. G.; Wadekar, R. R.

2008-01-01

99

Impact of antibacterial drugs on human serum paraoxonase-1 (hPON1) activity: an in vitro study  

PubMed Central

Objective To investigate the in vitro effects of the antibacterial drugs, meropenem trihydrate, piperacillin sodium, and cefoperazone sodium, on the activity of human serum paraoxonase (hPON1). Methods hPON1 was purified from human serum using simple chromatographic methods, including DEAE-Sephadex anion exchange and Sephadex G-200 gel filtration chromatography. Results The three antibacterial drugs decreased in vitro hPON1 activity. Inhibition mechanisms meropenem trihydrate was noncompetitive while piperacillin sodium and cefoperazone sodium were competitive. Conclusions Our results showed that antibacterial drugs significantly inhibit hPON1 activity, both in vitro, with rank order meropenem trihydrate piperacillin sodium cefoperazone sodium in vitro. PMID:25183328

Söyüt, Hakan; Kaya, Elif Duygu; Beydemir, ?ükrü

2014-01-01

100

In vitro assessment of antioxidant activity of Newbouldia laevis  

Microsoft Academic Search

Poverty, drug resistance and other factors including increasing difficulty in the control of mosquitoes (the vector of the causative organism of malaria), have led to a growing interest in phytochemical research. The antioxidant activity of Newbouldia laevis stem bark was investigated. Air dried stem bark of N. laevis was powdered and extracted with 95 % v\\/v methanol by maceration, and

O. E. Ogunlana; O. O. Ogunlana

2008-01-01

101

Inhibition of catalase activity in vitro by diesel exhaust particles  

SciTech Connect

The effect of diesel exhaust particles (DEP) on the activity of catalase, an intracellular anti-oxidant, was investigated because H{sub 2}O{sub 2} is a cytotoxic oxidant, and catalase released from alveolar cells is an important antioxidant in the epithelial lining fluid in the lung. DEP inhibited the activity of bovine liver catalase dose-dependently, to 25-30% of its original value. The inhibition of catalase by DEP was observed only in the presence of anions such as Cl{sup {minus}}, Br{sup {minus}}, or thiocyanate. Other anions, such as CH{sub 3}COO{sup {minus}} or SO{sub 4}{sup {minus}}, and cations such as K{sup +}, Na{sup +}, Mg{sup 2+}, or Fe{sup 2+}, did not affect the activity of catalase, even in the presence of DEP extract. Catalase from guinea pig alveolar cells and catalase from red blood cells were also inhibited by DEP extracts, as was catalase from bovine liver. These results suggest that DEP taken up in the lung and located on alveolar spaces might cause cell injury by inhibiting the activity of catalase in epithelial lining fluid, enhancing the toxicity of H{sub 2}O{sub 2} generated from cells in addition to that of O{sub 2}{sup {minus}} generated by the chemical reaction of DEP with oxygen. 10 refs., 6 figs.

Mori, Yoki; Murakami, Sumika; Sagae, Toshiyuki [Health Sciences Univ. of Hokkaido (Japan)] [and others] [Health Sciences Univ. of Hokkaido (Japan); and others

1996-02-09

102

In vitro anti-MRSA activity of carvone with gentamicin  

PubMed Central

Carvone is one of the naturally occurring monoterpenes, the largest class of secondary metabolites in plants, and exists in two enantiomers, R-carvone (R-car) and S-car. The objective of this study was to investigate the antimicrobial activity of R-car and S-car with gentamicin (GET) against methicillin-resistant Staphylococcus aureus (MRSA). MRSA is a major human pathogen that causes serious problems, including hospital-acquired pneumonia, abscesses and surgical wound infections. Nosocomial MRSA infections often exhibit multidrug resistance. In the present study, antimicrobial susceptibility testing was performed with R-car, S-car and GET using the broth microdilution method. Minimal inhibitory concentration values for R- and S-car against six different strains of S. aureus ranged between 500 and 1,000 ?g/ml. Anti-MRSA activity was evaluated using the checkerboard and time-kill assays to investigate the potential synergistic effects of different combinations of the carvone enantiomers and GET. R-car plus S-car, R-car plus GET and S-car plus GET exhibited significant synergistic activity against MRSA. These findings suggest that the single-agent anti-MRSA activities of R-car, S-car and GET are effectively increased through combination therapy. This study showed that carvone may be a potential adjuvant antimicrobial agent. PMID:24669246

MUN, SU-HYUN; KANG, OK-HWA; JOUNG, DAE-KI; KIM, SUNG-BAE; CHOI, JANG-GI; SHIN, DONG-WON; KWON, DONG-YEUL

2014-01-01

103

In vitro anti- Helicobacter pylori activity of Greek herbal medicines  

Microsoft Academic Search

In this paper, we have studied the anti-Helicobacter pylori effect of 70 Greek plant extracts and a number of commercially available herbs used traditionally in folk medicine against gastric ailments, peptic ulcer included. The extracts of Anthemis melanolepis, Cerastium candidissimum, Chamomilla recutita, Conyza albida, Dittrichia viscosa, Origanum vulgare and Stachys alopecuros have been proved active against one standard strain and

George Stamatis; Panayiotis Kyriazopoulos; Stamatina Golegou; Aris Basayiannis; Spyros Skaltsas; Helen Skaltsa

2003-01-01

104

In vitro and in vivo activities of sparfloxacin, other quinolones, and tetracyclines against Chlamydia trachomatis.  

PubMed Central

Sparfloxacin was more potent than other quinolones (tosufloxacin, lomefloxacin, ciprofloxacin, ofloxacin, fleroxacin, enoxacin, and norfloxacin) and as potent as minocycline and doxycycline in activity against Chlamydia trachomatis in vitro and in vivo. Sparfloxacin was more bactericidal than minocycline against C. trachomatis D/UW-3/Cx. PMID:1317145

Nakata, K; Maeda, H; Fujii, A; Arakawa, S; Umezu, K; Kamidono, S

1992-01-01

105

INFLUENCE OF CCL4 BIOTRANSFORMATION ON THE ACTIVATION OF RAT LIVER PHOSPHOLIPASE C IN VITRO  

EPA Science Inventory

The Influence of CCl4 Biotransforrnation on the Activation of Rat Liver Phospholipase C in Vitro. Coleman, J.F., Condie, L.W. AND LAMB, R.G. (1988). Toxicol. Appl Pharmacol. 95, 200-207. Carbon tetrachloride (CCL4) biotransformation and covalent binding was measured in l000g live...

106

Synergistic in vitro antimalarial activity of plant extracts used as traditional herbal remedies in Mali  

Microsoft Academic Search

In Mali, where malaria is endemic, plants are extensively used for treating periodic fevers and malaria. According to the advice of traditional medicine, plants are often mixed during the preparation of febrifugal decoctions. In previous studies, we demonstrated the potent in vitro antimalarial activity of extracts isolated from four plants commonly used in traditional remedies: Mitragyna inermis (Willd.) O. Kuntze,

N. Azas; N. Laurencin; F. Delmas; C. Di Giorgio; M. Gasquet; M Laget; P. Timon-David

2002-01-01

107

In vitro antiplasmodial activity of medicinal plants native to or naturalised in South Africa  

Microsoft Academic Search

The increasing prevalence and distribution of malaria has been attributed to a number of factors, one of them being the emergence and spread of drug resistant parasites. Efforts are now being directed towards the discovery and development of new chemically diverse antimalarial agents. The present study reports on the in vitro antiplasmodial activity of 134 plant taxa native to or

Cailean Clarkson; Vinesh J Maharaj; Neil R Crouch; Olwen M Grace; Pamisha Pillay; Motlalepula G Matsabisa; Niresh Bhagwandin; Peter J Smith; Peter I Folb

2004-01-01

108

Covalently immobilized thrombomodulin inhibits coagulation and complement activation of artificial surfaces in vitro  

Microsoft Academic Search

Thrombomodulin (TM) serves as the endothelial cell receptor for thrombin and alters its characteristics from pro- to anticoagulant. Additionally, it promotes the formation of activated protein C. We evaluated the conservation of the overall outcome of these functions in recombinant TM linked to artificial surfaces by incubation with human whole blood in vitro.TM was covalently immobilized through poly(ethylene glycol) (PEG)

C Sperling; K Salchert; U Streller; C Werner

2004-01-01

109

“In vitro” antifungal activity of ozonized sunflower oil on yeasts from onychomycosis  

PubMed Central

The “in vitro” antifungal activity of ozonized sunflower oil (Bioperoxoil®) was tested on 101 samples of yeasts originating from onychomycosis using the disk diffusion method. The oil was efficacious against several clinical fungal strains: Candida parapsilosis, Candida albicans, Trichosporon asahii, Candida tropicalis and Candida guilliermondii. PMID:24031958

Guerrer, L.V.; Cunha, K. C.; Nogueira, M. C. L.; Cardoso, C. C.; Soares, M. M. C. N.; Almeida, M. T. G.

2012-01-01

110

IN VITRO ANDROGENIC ACTIVITY OF KRAFT MILL EFFLUENT IS ASSOCIATED WITH MASCULINIZATION OF FEMALE FISH  

EPA Science Inventory

In Vitro Androgenic Activity of Kraft Mill Effluent is Associated with Masculinization of Female Fish. Lambright, CS 1 , Parks, LG 1, Orlando, E 2, Guillette, LJ, Jr.2, Ankley, G 3, Gray, LE, Jr.1 , 1USEPA, NHEERL, RTP, NC, 2 University of Florida, Dept. of Zoology, Gainesville ...

111

SPME determination of volatile aldehydes for evaluation of in-vitro antioxidant activity  

Microsoft Academic Search

The in-vitro antioxidant activity of natural (essential oils, vitamin E) or synthetic substances (tert-butyl hydroxy anisole (BHA), Trolox) has been evaluated by monitoring volatile carbonyl compounds released in model lipid systems subjected to peroxidation. The procedure employed methodology previously developed for the determination of carbonyl compounds as their pentafluorophenylhydrazine derivatives which were quantified, with high sensitivity, by means of capillary

Elena E. Stashenko; Miguel A. Puertas; Jairo R. Martínez

2002-01-01

112

In vitro antifungal activity of phenylheptatriyne from Bidens cernua L. against yeasts  

Microsoft Academic Search

In vitro antifungal activity of phenylheptatriyne from Bidens cernua L. (Asteraceae) was studied using broth macrodilution method against 125 strains of yeasts including 104 clinical and other isolates of Candida spp. (C. albicans, C. krusei, C. tropicalis, C. guilliermondii, C. parapsilosis, C. glabrata, C. inconspicua), 16 strains of basidiomycetous yeasts (Cryptococcus neoformans, C. albidus, Trichosporon cutaneum, Rhodotorula glutinis) and five

N. P. Rybalchenko; V. A. Prykhodko; S. S. Nagorna; N. N. Volynets; A. N. Ostapchuk; V. V. Klochko; T. V. Rybalchenko; L. V. Avdeeva

2010-01-01

113

In vitro antioxidant activities of the methanol extracts of four Helichrysum species from Turkey  

Microsoft Academic Search

This study was designed to examine the in vitro antioxidant activities of the methanol extracts of four Helichrysum species (Helichrysum noeanum Boiss., H. chionophilum Boiss. & Bal., H. plicatum DC. subsp. plicatum, H. arenarium (L.) Moench. subsp. aucheri (Boiss.) Davis & Kuphicha). The extracts were screened for their possible antioxidant activitiy by two complementary test systems, namely DPPH free radical-scavenging

Bektas Tepe; Munevver Sokmen; H. Askin Akpulat; Atalay Sokmen

2005-01-01

114

In vitro metabolism and bioavailability tests for the predictive toxicology of endocrine active substances  

EPA Science Inventory

Legislation and prospective legislative proposals internationally (may) require that chemicals are tested for their ability to disrupt the hormonal systems of animals. Chemicals found to test positive in vitro are considered to be endocrine active substances (EAS) and may be puta...

115

In vitro activity of tigecycline against 2423 clinical isolates and comparison of the available interpretation breakpoints  

Microsoft Academic Search

MICs to tigecycline and 12 antimicrobials were performed by microdilution method, against 2423 nonduplicate pathogens recently isolated in 17 Greek hospitals. The Food and Drug Administration (FDA) and European Committee on Antimicrobial Susceptibility Testing (EUCAST) criteria were used comparatively for interpretation of tigecycline MICs. Tigecycline exhibited potent in vitro activity against the majority of the isolates tested. (MIC90 values of

Joseph Papaparaskevas; Leonidas S. Tzouvelekis; Athanassios Tsakris; Theodore E. Pittaras; Nicholas J. Legakis

2010-01-01

116

EFFECT OF WATER POLLUTANTS AND OTHER CHEMICALS UPON THE ACTIVITY OF LIPASE 'IN VITRO'  

EPA Science Inventory

Lipase preparations were treated in vitro with 100 chemicals of various classes, many of which are environmental pollutants, to determine their effect upon enzyme activity. The greatest inhibition was caused by mercuric ion and certain heavy metal cations; almost as inhibiting we...

117

Glutathione S-transferases interact with AMP-activated protein kinase: evidence for S-glutathionylation and activation in vitro.  

PubMed

AMP-activated protein kinase (AMPK) is a cellular and whole body energy sensor with manifold functions in regulating energy homeostasis, cell morphology and proliferation in health and disease. Here we apply multiple, complementary in vitro and in vivo interaction assays to identify several isoforms of glutathione S-transferase (GST) as direct AMPK binding partners: Pi-family member rat GSTP1 and Mu-family members rat GSTM1, as well as Schistosoma japonicum GST. GST/AMPK interaction is direct and involves the N-terminal domain of the AMPK ?-subunit. Complex formation of the mammalian GSTP1 and -M1 with AMPK leads to their enzymatic activation and in turn facilitates glutathionylation and activation of AMPK in vitro. GST-facilitated S-glutathionylation of AMPK may be involved in rapid, full activation of the kinase under mildly oxidative physiological conditions. PMID:23741294

Klaus, Anna; Zorman, Sarah; Berthier, Alexandre; Polge, Cécile; Ramirez, Sacnicte; Michelland, Sylvie; Sčve, Michel; Vertommen, Didier; Rider, Mark; Lentze, Nicolas; Auerbach, Daniel; Schlattner, Uwe

2013-01-01

118

In vitro fertilization and artificial activation of eggs of the direct-developing anuran Eleutherodactylus coqui.  

PubMed

Although much is known about the reproductive biology of pond-breeding frogs, there is comparatively little information about terrestrial-breeding anurans, a highly successful and diverse group. This study investigates the activation and in vitro fertilization of eggs of the Puerto Rican coqui frog obtained by hormonally induced ovulation. We report that spontaneous activation occurs in 34% of eggs, probably in response to mechanical stress during oviposition. Artificial activation, as evidenced by the slow block to polyspermy and the onset of zygote division, was elicited both by mechanical stimulation and calcium ionophore exposure in 64% and 83% of the cases, respectively. Finally, one in vitro fertilization protocol showed a 27% success rate, despite the fact that about one third of all unfertilized eggs obtained by hormone injection auto-activate. We expect these findings to aid in the conservation effort of Eleutherodactylus frogs, the largest vertebrate genus. PMID:15296510

Toro, Esteban; Michael, Scott F

2004-08-01

119

In vitro inhibition of lysine decarboxylase activity by organophosphate esters.  

PubMed

Organophosphate esters (OPEs), a major group of organophosphorus flame retardants, are regarded as emerging environmental contaminants of health concern. Amino acid decarboxylases catalyze the conversion of amino acids into polyamines that are essential for cell proliferation, hypertrophy and tissue growth. In this paper, inhibitory effect of twelve OPEs with aromatic, alkyl or chlorinated alkyl substituents on the activity of lysine decarboxylase (LDC) was assessed quantitatively with an economic and label-free fluorescence sensor and cell assay. The sensor comprises a macrocyclic host (cucurbit[7]uril) and a fluorescent dye (acridine orange) reporter. The twelve OPEs were found to vary in their capacity to inhibit LDC activity. Alkyl group substituted OPEs had no inhibitory effect. By contrast, six OPEs substituted with aromatic or chlorinated alkyl groups inhibited LDC activity significantly with IC50 ranging from 1.32 ?M to 9.07 ?M. Among them, the inhibitory effect of tri-m-cresyl phosphate (TCrP) was even more effective as an inhibitor than guanosine 5'-diphosphate-3'-diphosphate (ppGpp) (1.60 ?M), an LDC natural inhibitor in vivo. Moreover, at non-cytotoxic concentrations, these six OPEs showed perceptible inhibitory effects on LDC activity in PC12 living cells, and led to a marked loss in the cadaverine content. Molecular docking analysis of the LDC/OPE complexes revealed that different binding modes contribute to the difference in their inhibitory effect. Our finding suggested that LDC, as a new potential biological target of OPEs, might be implicated in toxicological and pathogenic mechanism of OPEs. PMID:25264276

Wang, Sufang; Wan, Bin; Zhang, Lianying; Yang, Yu; Guo, Liang-Hong

2014-12-01

120

In vitro activity of systemic antifungal agents against Malassezia furfur.  

PubMed Central

The activity of four antifungal agents against 15 systemic (blood and vascular catheter) and 10 superficial (skin) Malassezia furfur isolates was evaluated. MIC ranges were similar for the two groups of organisms: amphotericin B, 0.3 to 2.5 micrograms/ml; flucytosine, greater than 100 micrograms/ml; miconazole, 0.4 to 1.5 micrograms/ml; and ketoconazole, 0.025 to 0.4 micrograms/ml. PMID:3619430

Marcon, M J; Durrell, D E; Powell, D A; Buesching, W J

1987-01-01

121

In vitro antimicrobial activity of Persian shallot (Allium hirtifolium).  

PubMed

Allium hirtifolium is a Persian native plant grown in cool mountain slopes of Iran. It has been used as a spice in Iran for many years. According to the literature review, there are no considerable reports on the antimicrobial properties of this plant. In this study, the antimicrobial activity of Persian shallot hydroalcoholic extract and F1 fraction of the plant (containing amino acid derivatives and/or other cationic compounds) was investigated on some Gram positive cocci and bacilli, Gram negative bacilli, two protozoa, a yeast and a fungus. Excellent activity against Candida albicans (MIC = 64 microg/ml, MBC = 128 microg/ml), Leishmania infantum (MIC = 0.2 mg/ml on the first day of study) and Trichomonas vaginalis (MIC = 5 microg/ml in PSDE form) and a moderate activity against Bacillus spp and Pseudomonas aeroginosa (MIC = 128 microg/ml) was observed. The results showed that this plant contains some anti-trichomonas and anti-leishmania components. PMID:23210319

Soroush, Setareh; Taherikalani, Morovat; Asadollahi, Parisa; Asadollahi, Khairollah; Taran, Mojtaba; Emaneini, Mohammad; Alizadeh, Sajjad

2012-01-01

122

In vitro antiviral activity of sulfated Auricularia auricula polysaccharides.  

PubMed

Total Auricularia auricula polysaccharide (AAP(t)) was prepared by extracting and removing the proteins. Column chromatography was used to further graded it into AAP(1) and AAP(2). Three AAPs were modified by chlorosulfonic acid-pyridine method to obtain three sulfated AAPs (sAAPs), sAAP(t), sAAP(1) and sAAP(2), respectively. Three sAAPs and Newcastle disease virus (NDV) were added into cultivation system of chicken embryo fibroblast (CEF) in three manners, pre-, post- and simultaneous-adding polysaccharide with NDV respectively, taking three non-modified AAPs as control. Their anti-viral activities were compared by MTT method. The results showed that sAAPs and AAPs at a certain concentration could significantly inhibit the cellular infectivity of NDV in three manners. The effects of sAAPs were better than that of AAPs. It indicated that sulfated modification could enhance the antiviral activity of AAP. sAAP(1) and sAAP(t) possessed stronger activity and would be as the component of a new-type antiviral drug. PMID:22939338

Nguyen, The Luong; Chen, Jin; Hu, Yuanliang; Wang, Deyun; Fan, Yunpeng; Wang, Junmin; Abula, Saifuding; Zhang, Jing; Qin, Tao; Chen, Xingying; Chen, Xiaolan; Khakame, Shem Kakai; Dang, Bao Khanh

2012-10-15

123

In vitro antiplasmodial activity of 18 plants used in Congo Brazzaville traditional medicine  

Microsoft Academic Search

Sixty-six extracts of 18 plants commonly used by traditional healers in Congo Brazzaville for the treatment of malaria have been investigated for in vitro antiplasmodial activity. Ethanolic and dichloromethane extracts of 7 among the 18 studied plants were moderately active (10?g\\/ml

S. F. Mbatchi; B. Mbatchi; J. T. Banzouzi; T. Bansimba; G. F. Nsonde Ntandou; J.-M. Ouamba; A. Berry; F. Benoit-Vical

2006-01-01

124

Topical Activity of Ascorbic Acid: From in vitro Optimization to in vivo Efficacy  

Microsoft Academic Search

We present here a new cosmetic formula system containing 3% ascorbic acid based on an optimized oil-in-water (O\\/W) emulsion. This formulation demonstrated a good long-term stability of the active ingredient and also of the emulsion itself. It could be deduced from in vitro release studies that this O\\/W emulsion enabled a better release of the hydrophilic active agent than an

T. Raschke; U. Koop; H.-J. Düsing; A. Filbry; K. Sauermann; S. Jaspers; H. Wenck; K.-P. Wittern

2004-01-01

125

In Vitro Activities of Ravuconazole (BMS-207147) against 541 Clinical Isolates of Cryptococcus neoformans  

Microsoft Academic Search

The in vitro activities of the new triazole, ravuconazole (BMS-207147), were compared to those of fluconazole and itraconazole against 541 clinical isolates of Cryptococcus neoformans. Isolates were obtained from cerebro- spinal fluid (396), blood (116), and miscellaneous clinical specimens (29). Overall, ravuconazole (MIC at which 90% of the isolates are inhibited (MIC90), 0.25 mg\\/ml) was more active than either itraconazole

T. Yamazumi; M. A. Pfaller; S. A. Messer; A. Houston; R. J. Hollis; R. N. Jones

2000-01-01

126

Comparative In Vitro Activities of Fluconazole, Voriconazole, and MXP-4509 Against Romanian Blood Yeast Isolates  

Microsoft Academic Search

The aim of the study was to evaluate the antifungal activity of a new triazole formulation against 182 clinical isolates of\\u000a yeasts recovered from blood cultures in three tertiary hospitals in Romania and to compare its activity with those of fluconazole\\u000a and voriconazole. In vitro susceptibility was assessed by following the guidelines of AFST-EUCAST E. Def. 7.1. The distribution\\u000a of

Mihai Mare?; Valentin N?stas?; Florina Moraru Ramona; Bogdan Doroftei; Alina ?tefanache

127

In vitro activity of temocillin against extended spectrum b-lactamase-producing Escherichia coli  

Microsoft Academic Search

Objectives: Temocillin is a semi-synthetic 6-a-methoxy derivative of ticarcillin. It is highly stable to most bacterial b-lactamases. However, data concerning its activity against extended-spectrum b-lactamase (ESBL)-producing Enterobacteriaceae are limited. We have analysed the in vitro activity of temocillin against clinical isolates of ESBL-producing Escherichia coli over the past 4 years in a university hospital in Brussels, Belgium. Methods: Strains were

Hector Rodriguez-Villalobos; Vincent Malaviolle; Joelle Frankard; Ricardo de Mendon; Claire Nonhoff; Marc J. Struelens

2006-01-01

128

Nicking and joining activity of banana bunchy top virus replication protein in vitro  

Microsoft Academic Search

The major open reading frame of banana bunchy top virus (BBTV) DNA-1 encodes a putative repli- cation initiation protein (Rep). In vitro, a fusion protein of BBTV Rep linked to a maltose-binding protein exhibited both site-specific nicking and joining activities. These activities were dependent on the presence of Mg2M or Mn2M, but did not require ATP. The fusion protein specifically

Gregory J. Hafner; Mark R. Stafford; Lindsay C. Wolter; Robert M. Harding; James L. Dale

129

Similar activity of mecamylamine stereoisomers in vitro and in vivo  

PubMed Central

A previous characterization of mecamylamine stereoisomers using nicotinic acetylcholine receptors expressed in Xenopus oocytes revealed only small differences between the activity of the R and S forms of mecamylamine. However, that work was limited in the breadth of receptor subtypes tested, especially in regard to the discrimination of high and low sensitivity receptors, which differ in the ratios of alpha and beta subunits. We report new data using subunit concatamers, which produce uniform populations of high-sensitivity or low-sensitivity receptors, as well as alpha2, alpha5, and alpha6-containing receptors, which were not studied previously. Consistent with previous studies, we found that beta4-containing receptors were most sensitive to mecamylamine and that the IC50 values for the inhibition of net charge were lower than for inhibition of peak currents. No large differences were seen between the activities of the mecamylamine isomers. Additionally, a previously reported potentiation of high-sensitivity ?4?2 receptors by S-mecamylamine could not be reproduced in the oocyte system, even with mutants that had greatly reduced sensitivity to mecamylamine inhibition or when the selective agonist TC-2559 was used. In vivo studies suggested that the R-isomer might be somewhat more potent than the S isomer at blocking CNS effects of nicotine. Although the potency difference was no more than a factor of two, it is consistent with lower LD50 estimates previously reported for the R isomer. Our results significantly extend knowledge of the nicotinic acetylcholine receptor activity profile of mecamylamine and support the hypothesis that these effects are not strongly stereoisomer selective. PMID:24161916

Papke, Roger L.; Stokes, Clare; Muldoon, Pretal; Damaj, M. Imad

2014-01-01

130

Lack of activity of cadmium in in vitro estrogenicity assays.  

PubMed

Prompted by reports about strong estrogenic effects of cadmium, attempts were made to reproduce these observations using the yeast estrogen screen (YES) and the E-Screen assays. For the first time, possible activation of the Src/MAPK pathway was also investigated. In the YES, only a slight activation (10% of a maximal effect) of the estrogen receptor alpha (ERalpha) was observed at cadmium concentrations between 5 x 10(-7) M and 5 x 10(-6) M. In the E-Screen assay, carried out by two laboratories, the heavy metal was without observable cell proliferative effects when tested in the range between 6 x 10(-11) M and 1 x 10(-5) M. However, in both assays, cadmium led to a reduction of the effects of 17beta-estradiol (E2). Treatment of MCF-7 human breast cancer cells with 1 x 10(-7) M cadmium failed to induce phosphorylation of Src and the MAP kinases Erk1 and Erk2-effects shown to occur with E2 and epidermal growth factor (EGF). In summary, we were unable to confirm the strong estrogenicity of cadmium reported recently by a number of laboratories. This apparent absence of effects in our hands is not due to a lack of uptake of the metal or to effective protection against cadmium by high levels of glutathione or metallothionein, since toxicity and an antagonism of E2 responses were observed both in the YES and the E-Screen. PMID:16716372

Silva, Elisabete; Lopez-Espinosa, Maria José; Molina-Molina, José-Manuel; Fernández, Marieta; Olea, Nicolas; Kortenkamp, Andreas

2006-10-01

131

A cyclic enkephalin analog with high in vitro opiate activity.  

PubMed Central

A conformationally restricted analog of [Leu5]enkephalin was synthesized by cyclization of the COOH-terminal carboxyl group of leucine to the gamma-amino moiety of alpha, gamma-diaminobutyric acid (A2bu) substituted in position 2 of the peptide. Relative to [Leu5]enkephalin, the cyclic analog with D configuration in position 2, H-Tyr-cyclo(-N gamma-D-A2bu-Gly-Phe-Leu-), was 17.5 times more potent in the guinea pig ileum assay and twice as potent in the rat brain receptor binding assay, whereas its diastereomer H-Tyr-cyclo(-N gamma-L-A2bu-Gly-Phe-Leu-) showed low activity. The cyclic D isomer was also slightly more active than the open-chain reference compound [D-Nva2, Leu5]enkephalinamide in both assays, and it proved to be highly resistant to degradation by brain "enkephalinases." The steric constraints introduced in H-Tyr-cyclo(-N gamma-D-A2bu-Gly-Phe-Leu-) were shown to prevent the realization of most of the conformational features ascribed to linear enkephalin in solution or in the crystalline state and permitted an assessment of proposed models of the conformation of enkephalin when it is bound to the receptor. Images PMID:6261242

DiMaio, J; Schiller, P W

1980-01-01

132

Review on in vivo and in vitro methods evaluation of antioxidant activity  

PubMed Central

A good number of abstracts and research articles (in total 74) published, so far, for evaluating antioxidant activity of various samples of research interest were gone through where 407 methods were come across, which were repeated from 29 different methods. These were classified as in vitro and in vivo methods. And those are described and discussed below in this review article. In the later part of this review article, frequency of in vitro as well as in vivo methods is analyzed with a bar diagram. Solvents are important for extracting antioxidants from natural sources. Frequency of solvents used for extraction is also portrayed and the results are discussed in this article. As per this review there are 19 in vitro methods and 10 in vivo methods that are being used for the evaluation of antioxidant activity of the sample of interest. DPPH method was found to be used mostly for the in vitro antioxidant activity evaluation purpose while LPO was found as mostly used in vivo antioxidant assay. Ethanol was with the highest frequency as solvent for extraction purpose. PMID:24936134

Alam, Md. Nur; Bristi, Nusrat Jahan; Rafiquzzaman, Md.

2012-01-01

133

In Vitro Activity of Ceftaroline against 623 Diverse Strains of Anaerobic Bacteria ?  

PubMed Central

The in vitro activities of ceftaroline, a novel, parenteral, broad-spectrum cephalosporin, and four comparator antimicrobials were determined against anaerobic bacteria. Against Gram-positive strains, the activity of ceftaroline was similar to that of amoxicillin-clavulanate and four to eight times greater than that of ceftriaxone. Against Gram-negative organisms, ceftaroline showed good activity against ?-lactamase-negative strains but not against the members of the Bacteroides fragilis group. Ceftaroline showed potent activity against a broad spectrum of anaerobes encountered in respiratory, skin, and soft tissue infections. PMID:20100877

Citron, D. M.; Tyrrell, K. L.; Merriam, C. V.; Goldstein, E. J. C.

2010-01-01

134

Novel antifungal activity of purpurin against Candida species in vitro.  

PubMed

The antifungal activity of purpurin (1,2,4-trihydroxy-9,10-anthraquinone), a natural red anthraquinone pigment in madder root (Rubia tinctorum L.), was evaluated by a broth microdilution assay against a total of 24 Candida isolates representing six species. The minimum inhibitory concentration (MIC) range of purpurin was 1.28-5.12 ?g/ml. Mechanistic studies using the rhodamine 6G extrusion assay indicated that purpurin inhibited the energy-dependent efflux pumps of the Candida isolates in a dose-dependent manner. Furthermore, purpurin demonstrated a dose-dependent depolarization of mitochondrial membrane potential, one of the biochemical checkpoints regulating cell death in eukaryotic cells, suggesting a possible linkage between purpurin antifungal mechanism and Candida apoptosis. PMID:20392152

Kang, Kai; Fong, Wing-Ping; Tsang, Paul Wai-Kei

2010-11-01

135

Neuromuscular Activity of Micrurus laticollaris (Squamata: Elapidae) Venom in Vitro  

PubMed Central

In this work, we have examined the neuromuscular activity of Micrurus laticollaris (Mexican coral snake) venom (MLV) in vertebrate isolated nerve-muscle preparations. In chick biventer cervicis preparations, the MLV induced an irreversible concentration- and time-dependent (1–30 µg/mL) neuromuscular blockade, with 50% blockade occurring between 8 and 30 min. Muscle contractures evoked by exogenous acetylcholine were completely abolished by MLV, whereas those of KCl were also significantly altered (86% ± 11%, 53% ± 11%, 89% ± 5% and 89% ± 7% for one, three, 10 and 30 µg of venom/mL, respectively; n = 4; p < 0.05). In mouse phrenic nerve-diaphragm preparations, MLV (1–10 µg/mL) promoted a slight increase in the amplitude of twitch-tension (3 µg/mL), followed by neuromuscular blockade (n = 4); the highest concentration caused complete inhibition of the twitches (time for 50% blockade = 26 ± 3 min), without exhibiting a previous neuromuscular facilitation. The venom (3 µg/mL) induced a biphasic modulation in the frequency of miniature end-plate potentials (MEPPs)/min, causing a significant increase after 15 min, followed by a decrease after 60 min (from 17 ± 1.4 (basal) to 28 ± 2.5 (t15) and 12 ± 2 (t60)). The membrane resting potential of mouse diaphragm preparations pre-exposed or not to d-tubocurarine (5 µg/mL) was also significantly less negative with MLV (10 µg/mL). Together, these results indicate that M. laticollaris venom induces neuromuscular blockade by a combination of pre- and post-synaptic activities. PMID:24445448

Carbajal-Saucedo, Alejandro; Floriano, Rafael Stuani; Dal Belo, Cháriston André; Olvera-Rodríguez, Alejandro; Alagón, Alejandro; Rodrigues-Simioni, Léa

2014-01-01

136

Neuromuscular activity of Micrurus laticollaris (Squamata: Elapidae) venom in vitro.  

PubMed

In this work, we have examined the neuromuscular activity of Micrurus laticollaris (Mexican coral snake) venom (MLV) in vertebrate isolated nerve-muscle preparations. In chick biventer cervicis preparations, the MLV induced an irreversible concentration- and time-dependent (1-30 µg/mL) neuromuscular blockade, with 50% blockade occurring between 8 and 30 min. Muscle contractures evoked by exogenous acetylcholine were completely abolished by MLV, whereas those of KCl were also significantly altered (86% ± 11%, 53% ± 11%, 89% ± 5% and 89% ± 7% for one, three, 10 and 30 µg of venom/mL, respectively; n = 4; p < 0.05). In mouse phrenic nerve-diaphragm preparations, MLV (1-10 µg/mL) promoted a slight increase in the amplitude of twitch-tension (3 µg/mL), followed by neuromuscular blockade (n = 4); the highest concentration caused complete inhibition of the twitches (time for 50% blockade = 26 ± 3 min), without exhibiting a previous neuromuscular facilitation. The venom (3 µg/mL) induced a biphasic modulation in the frequency of miniature end-plate potentials (MEPPs)/min, causing a significant increase after 15 min, followed by a decrease after 60 min (from 17 ± 1.4 (basal) to 28 ± 2.5 (t15) and 12 ± 2 (t60)). The membrane resting potential of mouse diaphragm preparations pre-exposed or not to d-tubocurarine (5 µg/mL) was also significantly less negative with MLV (10 µg/mL). Together, these results indicate that M. laticollaris venom induces neuromuscular blockade by a combination of pre- and post-synaptic activities. PMID:24445448

Carbajal-Saucedo, Alejandro; Floriano, Rafael Stuani; Dal Belo, Cháriston André; Olvera-Rodríguez, Alejandro; Alagón, Alejandro; Rodrigues-Simioni, Léa

2014-01-01

137

Progress of in vitro factor VIII coagulant activity from 0 to 8 hours after reconstitution  

PubMed Central

Background Continuous infusion of factor VIII (FVIII) is a more cost-effective method for treating hemophilia A than intermittent bolus injection. However, there is currently no specific data in Korea about the progress of in vitro FVIII coagulant activity (FVIII:C) after reconstitution from its lyophilized form. Methods Three commercial FVIII concentrate products (two recombinant FVIII and one plasma-derived) were used. In vitro FVIII:C was measured at 0, 2, 4, 6, and 8 hours following reconstitution in both the indoor light-exposed and light-shielded groups. Results For the three drugs, in vitro FVIII:C decreased over the 8 hours following reconstitution (P<0.001). The decline of FVIII:C was linear (P<0.001). In vitro FVIII:C for the indoor light-exposed groups was 95.3±1.9% and 90.6±2.5% after 4 and 8 hours following reconstitution, respectively, compared to baseline activity. In the light-shielded group, FVIII:C was 95.4±1.1% and 90.9±1.7% of the baseline activity after 4 and 8 hours, respectively. There was no statistical difference between FVIII:C in the indoor light-exposed and light-shielded groups (P=0.849). Conclusion In vitro FVIII:C decreased after reconstitution, but activity was maintained at over 90% of the baseline value during 8 hours. Exposure to indoor light did not accelerate the loss of FVIII:C over the experimental time. This result indicates that CI with FVIII is available in 8-hour intervals, with no indoor light-exposure precautions needed. PMID:25548761

Shim, Ye Jee; Lee, Kun Soo; Kim, Uk Hyun; Suh, Jin Kyung; Baik, Sae Yun

2014-01-01

138

In vitro - in vivo correlations for endocrine activity of a mixture of currently used pesticides  

SciTech Connect

Two pesticide mixtures were investigated for potential endocrine activity. Mix 3 consisted of bitertanol, propiconazole, and cypermethrin, and Mix 5 included malathion and terbuthylazine in addition to the three pesticides in Mix 3. All five single pesticides and the two mixtures were investigated for their ability to affect steroidogenesis in vitro in H295R cells. The pesticides alone and both mixtures affected steroidogenesis with both mixtures causing increase in progesterone and decrease in testosterone. For Mix 5 an increase in estradiol was seen as well, indicating increased aromatase activity. The two mixtures were also investigated in pregnant rats dosed from gestational day 7 to 21, followed by examination of dams and fetuses. Decreased estradiol and reduced placental testosterone were seen in dams exposed to Mix 5. Also a significant increase in aromatase mRNA-levels in female adrenal glands was found for Mix5. However, either of the two mixtures showed any effects on fetal hormone levels in plasma or testis, or on anogenital distance. Overall, potential aromatase induction was found for Mix 5 both in vitro and in vivo, but not for Mix 3, an effect likely owed to terbuthylazine in Mix 5. However, the hormonal responses in vitro were only partly reflected in vivo, probably due to some toxicokinetic issues, as the pesticide levels in the amniotic fluid also were found to be negatively affected by the number of compounds present in the mixtures. Nonetheless, the H295R assay gives hints on conceivable interference with steroidogenesis, thus generating hypotheses on in vivo effects. - Highlights: • The study examines the endocrine disrupting potential of mixtures of pesticides. • All single pesticides and both mixtures affected steroidogenesis in vitro. • Potential aromatase induction was found for Mix 5 both in vitro and in vivo. • The hormonal responses in vitro were only partly reflected in vivo.

Taxvig, Camilla, E-mail: camta@food.dtu.dk [Division of Toxicology and Risk Assessment, National Food Institute, Technical University of Denmark, Mřrkhřj Bygade 19, DK-2860 Sřborg (Denmark); Hadrup, Niels; Boberg, Julie; Axelstad, Marta [Division of Toxicology and Risk Assessment, National Food Institute, Technical University of Denmark, Mřrkhřj Bygade 19, DK-2860 Sřborg (Denmark); Bossi, Rossana [Department of Environmental Science, Aarhus University, DK-4000 Roskilde (Denmark); Bonefeld-Jřrgensen, Eva Cecilie [Department of Public Health, University of Aarhus, DK-8000 Aarhus C (Denmark); Vinggaard, Anne Marie [Division of Toxicology and Risk Assessment, National Food Institute, Technical University of Denmark, Mřrkhřj Bygade 19, DK-2860 Sřborg (Denmark)

2013-11-01

139

Relationship between in vivo activity and in vitro measures of function and stability of a protein  

SciTech Connect

The in vivo activities of mutant proteins are readily measured and can potentially be used to estimate changes in in vitro properties such as stability or function, but this connection has not been rigorously established. Gene V protein is a small protein produced by bacteriophage f1 that binds to single-stranded DNA and to RNA and for which fitness can be assayed both in vivo and in vitro. We have assembled a large number of temperature-sensitive mutants of the gene V protein of bacteriophage f1 and measured their ability to support phage growth and replication in vivo. We have also purified many of these mutant gene V proteins and measured their stabilities and ssDNA binding affinities in vitro. Mutations at surface residues frequently yielded temperature-sensitive mutants, but remarkably, no overall correlation between in vivo activity and in vitro measures of either stability or function was found for this group. Mutations at buried residues often lead to the temperature-sensitive phenotype. At buried sites temperature sensitivity was strongly correlated with in vitro stability changes, but not with in vitro ssDNA binding affinity. The implication of these observations for protein engineering efforts is that phenotypes conferred by amino acid substitutions at buried sites can be used to identify mutants whose stabilities fall into ranges of interest, while phenotypes of mutants with surface substitutions may be much less readily interpreted, even in the case of a single-stranded-DNA-binding protein. 54 refs., 3 figs., 2 tabs.

Sandberg, W.S.; Schlunk, P.M.; Zabin, H.G. [Univ. of Chicago, IL (United States)] [and others

1995-09-19

140

Gamma radiation effects on phenolics, antioxidants activity and in vitro digestion of pistachio ( Pistachia vera) hull  

NASA Astrophysics Data System (ADS)

The effect of gamma radiation (10, 20, 30, 40, 50 and 60 kGy) on tannin, total phenolics, antioxidants activity and in vitro digestion of pistachio hulls has been investigated in this study. The possibility of using the radial diffusion method based on software measurement of the rings area has also been investigated in this study. The software based method in radial diffusion method showed a higher r2 (0.995) value when compared to the traditional method. Irradiation reduced the tannin content ( P<0.01) and activity of antioxidants ( P<0.05) of pistachio hull extracts but increased the total phenolic content ( P<0.05). There was no effect of gamma irradiation on the in vitro digestion of the pistachio hull. Irradiation decreased the digestion rate of the pistachio hull at the dose of 40 kGy when compared to the control. This study showed that gamma irradiation decreased tannin and antioxidants activity of pistachio hull.

Behgar, M.; Ghasemi, S.; Naserian, A.; Borzoie, A.; Fatollahi, H.

2011-09-01

141

In vitro screening of two Nigerian medicinal plants (Vernonia amygdalina and Annona senegalensis) for anthelmintic activity.  

PubMed

Vernonia amygdalina and Annona senegalensis, two plants used by local/smallholder livestock farmers in Nigeria as anthelmintic were screened for in vitro anthelmintic activity using Haemonchus contortus eggs. The extract of V. amygdalina did not show any significant activity at concentrations up to 11.2mg/ml. The extract of A. senegalensis showed significant (P<0.001) reduction in egg hatch at a concentration of 7.1mg/ml. The in vitro fecal culture of eggs with A. senegalensis showed significant (P<0.001) reductions in larval recovery with increasing concentrations from 1 to 10% ((w/w) in fecal culture) when whole ground plant material was used. Although traditional veterinary healers and local livestock farmers claim both plants are effective as anthelmintics, our result indicate that only A. senegalensis showed promising anthelmintic activity especially with use of ground whole plant materials as used by some farmers. PMID:12651218

Alawa, C B I; Adamu, A M; Gefu, J O; Ajanusi, O J; Abdu, P A; Chiezey, N P; Alawa, J N; Bowman, D D

2003-04-01

142

In vitro propagation of Withania somnifera and isolation of withanolides with immunosuppressive activity.  

PubMed

Withania somnifera plantlets were produced in vitro from the shoot-tip of aseptically germinated seedlings. Culture conditions were optimized using different plant growth regulators which gave rise to 120 shoots from a single bud. The plantlets were then transferred to pots and maintained in greenhouse for 4 months. 90% of these in vitro propagated plantlets survived and showed normal growth. Leaves from these plants were used for isolation of the withanolides. Methanolic extract of leaves from plantlets growing in tissue culture and those transferred to the greenhouse were evaluated for immunomodulatory activity. While the extract from greenhouse samples showed potent immunosuppressive activity, those from tissue cultures samples did not show any activity. Fractionation and characterization of withanolides, using HPLC, NMR, MS methods revealed the presence of withaferin A in the greenhouse samples. Our results indicate that Withania species may require longer time and better differentiation and also natural environment for the production of withaferin A. PMID:11301861

Furmanowa, M; Gajdzis-Kuls, D; Ruszkowska, J; Czarnocki, Z; Obidoska, G; Sadowska, A; Rani, R; Upadhyay, S N

2001-03-01

143

Antioxidant activity of glycoprotein purified from Undaria pinnatifida measured by an in vitro digestion model.  

PubMed

The present study was performed to investigate the chemical composition and antioxidant activity of glycoprotein purified from Undaria pinnatifida Harvey (UPGP). On SDS-PAGE, UPGP migrated as a single band with a molecular weight of approximately 10 kDa and confirmed by staining with Schiff's reagent as glycoprotein. It consists of a carbohydrate component (42.53%) and protein component (57.47%). Amino acid profile, FT-IR spectrum and enzymatic glycosylation analysis suggested that protein is linked with carbohydrate by O-glycosylation. UPGP showed dose-dependent antioxidant activities as detected by different assays before and after in vitro digestion. The IC50 values of undigested UPGP were 0.25 ± 0.03, 0.08 ± 0.005, 0.69 ± 0.12, and 0.25 ± 0.08 mg/mL for DPPH, ABTS, FRAP, and NO, respectively. Following in vitro digestion, the antioxidant activities of UPGP were decreased during the gastric phase compared to those of undigested UPGP, with an increase occurring during the duodenal phase in all assays. However, the reducing power was unchanged after in vitro digestion. Furthermore, UPGP showed protective activity against oxidative DNA damage both undigested, after saliva and duodenal phase of digestion. These results indicate that the antioxidant and DNA protection activities of UPGP may be pH-dependent and assay specific. PMID:24060280

Rafiquzzaman, S M; Kim, Eun-Young; Kim, Yu-Ri; Nam, Taek-Jeong; Kong, In-Soo

2013-11-01

144

In vitro activities of natural products against oral Candida isolates from denture wearers  

PubMed Central

Background Candida-associated denture stomatitis is a frequent infectious disease. Treatment of this oral condition is difficult because failures and recurrences are common. The aim of this study was to test the in vitro antifungal activity of pure constituents of essentials oils. Methods Eight terpenic derivatives (carvacrol, farnesol, geraniol, linalool, menthol, menthone, terpinen-4-ol, and ?-terpineol), a phenylpropanoid (eugenol), a phenethyl alcohol (tyrosol) and fluconazole were evaluated against 38 Candida isolated from denture-wearers and 10 collection Candida strains by the CLSI M27-A3 broth microdilution method. Results Almost all the tested compounds showed antifungal activity with MIC ranges of 0.03-0.25% for eugenol and linalool, 0.03-0.12% for geraniol, 0.06-0.5% for menthol, ?-terpineol and terpinen-4-ol, 0.03-0.5% for carvacrol, and 0.06-4% for menthone. These compounds, with the exception of farnesol, menthone and tyrosol, showed important in vitro activities against the fluconazole-resistant and susceptible-dose dependent Candida isolates. Conclusions Carvacrol, eugenol, geraniol, linalool and terpinen-4-ol were very active in vitro against oral Candida isolates. Their fungistatic and fungicidal activities might convert them into promising alternatives for the topic treatment of oral candidiasis and denture stomatitis. PMID:22118215

2011-01-01

145

Inhibition of the activation of heat shock factor in vivo and in vitro by flavonoids.  

PubMed Central

Transcriptional activation of human heat shock protein (HSP) genes by heat shock or other stresses is regulated by the activation of a heat shock factor (HSF). Activated HSF posttranslationally acquires DNA-binding ability. We previously reported that quercetin and some other flavonoids inhibited the induction of HSPs in HeLa and COLO 320DM cells, derived from a human colon cancer, at the level of mRNA accumulation. In this study, we examined the effects of quercetin on the induction of HSP70 promoter-regulated chloramphenicol acetyltransferase (CAT) activity and on the binding of HSF to the heat shock element (HSE) by a gel mobility shift assay with extracts of COLO 320DM cells. Quercetin inhibited heat-induced CAT activity in COS-7 and COLO 320DM cells which were transfected with plasmids bearing the CAT gene under the control of the promoter region of the human HSP70 gene. Treatment with quercetin inhibited the binding of HSF to the HSE in whole-cell extracts activated in vivo by heat shock and in cytoplasmic extracts activated in vitro by elevated temperature or by urea. The binding of HSF activated in vitro by Nonidet P-40 was not suppressed by the addition of quercetin. The formation of the HSF-HSE complex was not inhibited when quercetin was added only during the binding reaction of HSF to the HSE after in vitro heat activation. Quercetin thus interacts with HSF and inhibits the induction of HSPs after heat shock through inhibition of HSF activation. Images PMID:1321338

Hosokawa, N; Hirayoshi, K; Kudo, H; Takechi, H; Aoike, A; Kawai, K; Nagata, K

1992-01-01

146

Inhibition of the activation of heat shock factor in vivo and in vitro by flavonoids.  

PubMed

Transcriptional activation of human heat shock protein (HSP) genes by heat shock or other stresses is regulated by the activation of a heat shock factor (HSF). Activated HSF posttranslationally acquires DNA-binding ability. We previously reported that quercetin and some other flavonoids inhibited the induction of HSPs in HeLa and COLO 320DM cells, derived from a human colon cancer, at the level of mRNA accumulation. In this study, we examined the effects of quercetin on the induction of HSP70 promoter-regulated chloramphenicol acetyltransferase (CAT) activity and on the binding of HSF to the heat shock element (HSE) by a gel mobility shift assay with extracts of COLO 320DM cells. Quercetin inhibited heat-induced CAT activity in COS-7 and COLO 320DM cells which were transfected with plasmids bearing the CAT gene under the control of the promoter region of the human HSP70 gene. Treatment with quercetin inhibited the binding of HSF to the HSE in whole-cell extracts activated in vivo by heat shock and in cytoplasmic extracts activated in vitro by elevated temperature or by urea. The binding of HSF activated in vitro by Nonidet P-40 was not suppressed by the addition of quercetin. The formation of the HSF-HSE complex was not inhibited when quercetin was added only during the binding reaction of HSF to the HSE after in vitro heat activation. Quercetin thus interacts with HSF and inhibits the induction of HSPs after heat shock through inhibition of HSF activation. PMID:1321338

Hosokawa, N; Hirayoshi, K; Kudo, H; Takechi, H; Aoike, A; Kawai, K; Nagata, K

1992-08-01

147

Titanium nanotubes activate genes related to bone formation in vitro  

PubMed Central

Background: Titanium is used worldwide to make osseointegrable devices, thanks to its favorable characteristics as mechanical proprieties and biocompatibility, demonstrated by in vivo studies with animal models and clinical trials over a forty-year period. However, the exact genetic effect of the titanium layer on cells is still not well characterized. Materials and Methods: To investigate how titanium nanotubes stimulate osteoblasts differentiation and proliferation, some osteoblast genes (SP7, RUNX2, COL3A1, COL1A1, ALPL, SPP1 and FOSL1) were analyzed by quantitative Real Time RT- PCR. Results: After 15 days, osteoblasts cultivated on titanium naotube showed the up-regulation of bone related genes SP7, ENG, FOSL1 and SPP1 and the down-regulation of RUNX2, COL3A1, COL1A1, and ALPL. After 30 days of treatment, the bone related genes SP7, ENG, FOSL1 and RUNX2 were up-regulated while COL3A1, COL1A1, ALPL and SPP1 were down-regulated. Conclusions: Our results, demonstrates that titanium nanotubes can lead to osteoblast differentiation and extracellular matrix deposition and mineralization in dental pulp stem cells by the activation of osteoblast related genes SPP1, FOSL1 and RUNX2. PMID:23814577

Pozio, Alfonso; Palmieri, Annalisa; Girardi, Ambra; Cura, Francesca; Carinci, Francesco

2012-01-01

148

Screening of selected medicinal plants for in vitro antidermatophytic activity.  

PubMed

Different solvent extracts of leaves of Achyranthes aspera, Aegle marmelos, Cleistanthus collinus, Curcuma aromatica and Strychnos nux-vomica were screened against dermatophytes viz., Trichophyton mentagrophytes, T. rubrum, Microsporum gypseum, M. canis and Epidermophyton floccossum var. nigricans. The mean zones of inhibition were between 7.1 and 26.5mm. Minimum inhibitory concentrations (MIC) and minimum fungicidal concentrations (MFC) were from 7.81 to 500 and from 15.62 to 1000?g/mL respectively. The highest mean zone of inhibition (26.5mm), the lowest MIC value (7.81?g/ml) and the lowest MFC (15.62?g/ml) were observed in ethyl acetate extract of A. aspera against T. rubrum. The standard antifungal drug ketoconazole (10?g/disc) was used as the positive control and mean zones of inhibition were from 23 to 29mm. Further separation of active principle from ethyl acetate extract of A. aspera is under progress. PMID:24135649

Kalaivanan, C; Chandrasekaran, M; Venkatesalu, V

2013-12-01

149

Antioxidative and in vitro antiproliferative activity of Arctium lappa root extracts  

PubMed Central

Background Arctium lappa, known as burdock, is widely used in popular medicine for hypertension, gout, hepatitis and other inflammatory disorders. Pharmacological studies indicated that burdock roots have hepatoprotective, anti-inflammatory, free radical scavenging and antiproliferative activities. The aim of this study was to evaluate total phenolic content, radical scavenging activity by DPPH and in vitro antiproliferative activity of different A. lappa root extracts. Methods Hot and room temperature dichloromethanic, ethanolic and aqueous extracts; hydroethanolic and total aqueous extract of A. lappa roots were investigated regarding radical scavenging activity by DPPH, total phenolic content by Folin-Ciocalteau method and antiproliferative in vitro activity was evaluated in human cancer cell lines. The hydroethanolic extract analyzed by high-resolution electrospray ionization mass spectroscopy. Results Higher radical scavenging activity was found for the hydroethanolic extract. The higher phenolic contents were found for the dichloromethane, obtained both by Soxhlet and maceration extraction and hydroethanolic extracts. The HRESI-MS demonstrated the presence of arctigenin, quercetin, chlorogenic acid and caffeic acid compounds, which were identified by comparison with previous data. The dichloromethane extracts were the only extracts that exhibited activity against cancer cell lines, especially for K562, MCF-7 and 786-0 cell lines. Conclusions The hydroethanolic extracts exhibited the strongest free radical scavenging activity, while the highest phenolic content was observed in Soxhlet extraction. Moreover, the dichloromethanic extracts showed selective antiproliferative activity against K562, MCF-7 and 786-0 human cancer cell lines. PMID:21429215

2011-01-01

150

Antiviral activity of glycyrrhizin against hepatitis C virus in vitro.  

PubMed

Glycyrrhizin (GL) has been used in Japan to treat patients with chronic viral hepatitis, as an anti-inflammatory drug to reduce serum alanine aminotransferase levels. GL is also known to exhibit various biological activities, including anti-viral effects, but the anti-hepatitis C virus (HCV) effect of GL remains to be clarified. In this study, we demonstrated that GL treatment of HCV-infected Huh7 cells caused a reduction of infectious HCV production using cell culture-produced HCV (HCVcc). To determine the target step in the HCV lifecycle of GL, we used HCV pseudoparticles (HCVpp), replicon, and HCVcc systems. Significant suppressions of viral entry and replication steps were not observed. Interestingly, extracellular infectivity was decreased, and intracellular infectivity was increased. By immunofluorescence and electron microscopic analysis of GL treated cells, HCV core antigens and electron-dense particles had accumulated on endoplasmic reticulum attached to lipid droplet (LD), respectively, which is thought to act as platforms for HCV assembly. Furthermore, the amount of HCV core antigen in LD fraction increased. Taken together, these results suggest that GL inhibits release of infectious HCV particles. GL is known to have an inhibitory effect on phospholipase A2 (PLA2). We found that group 1B PLA2 (PLA2G1B) inhibitor also decreased HCV release, suggesting that suppression of virus release by GL treatment may be due to its inhibitory effect on PLA2G1B. Finally, we demonstrated that combination treatment with GL augmented IFN-induced reduction of virus in the HCVcc system. GL is identified as a novel anti-HCV agent that targets infectious virus particle release. PMID:23874843

Matsumoto, Yoshihiro; Matsuura, Tomokazu; Aoyagi, Haruyo; Matsuda, Mami; Hmwe, Su Su; Date, Tomoko; Watanabe, Noriyuki; Watashi, Koichi; Suzuki, Ryosuke; Ichinose, Shizuko; Wake, Kenjiro; Suzuki, Tetsuro; Miyamura, Tatsuo; Wakita, Takaji; Aizaki, Hideki

2013-01-01

151

Antiviral Activity of Glycyrrhizin against Hepatitis C Virus In Vitro  

PubMed Central

Glycyrrhizin (GL) has been used in Japan to treat patients with chronic viral hepatitis, as an anti-inflammatory drug to reduce serum alanine aminotransferase levels. GL is also known to exhibit various biological activities, including anti-viral effects, but the anti-hepatitis C virus (HCV) effect of GL remains to be clarified. In this study, we demonstrated that GL treatment of HCV-infected Huh7 cells caused a reduction of infectious HCV production using cell culture-produced HCV (HCVcc). To determine the target step in the HCV lifecycle of GL, we used HCV pseudoparticles (HCVpp), replicon, and HCVcc systems. Significant suppressions of viral entry and replication steps were not observed. Interestingly, extracellular infectivity was decreased, and intracellular infectivity was increased. By immunofluorescence and electron microscopic analysis of GL treated cells, HCV core antigens and electron-dense particles had accumulated on endoplasmic reticulum attached to lipid droplet (LD), respectively, which is thought to act as platforms for HCV assembly. Furthermore, the amount of HCV core antigen in LD fraction increased. Taken together, these results suggest that GL inhibits release of infectious HCV particles. GL is known to have an inhibitory effect on phospholipase A2 (PLA2). We found that group 1B PLA2 (PLA2G1B) inhibitor also decreased HCV release, suggesting that suppression of virus release by GL treatment may be due to its inhibitory effect on PLA2G1B. Finally, we demonstrated that combination treatment with GL augmented IFN-induced reduction of virus in the HCVcc system. GL is identified as a novel anti-HCV agent that targets infectious virus particle release. PMID:23874843

Matsumoto, Yoshihiro; Matsuura, Tomokazu; Aoyagi, Haruyo; Matsuda, Mami; Hmwe, Su Su; Date, Tomoko; Watanabe, Noriyuki; Watashi, Koichi; Suzuki, Ryosuke; Ichinose, Shizuko; Wake, Kenjiro; Suzuki, Tetsuro; Miyamura, Tatsuo; Wakita, Takaji; Aizaki, Hideki

2013-01-01

152

Structural features of endocrine active chemicals - A comparison of in vivo and in vitro data.  

PubMed

Studies on reproductive toxicity need high numbers of test animals. Therefore, we investigated whether chemical structural features (SF) in combination with in vitro data on specific adverse outcome pathways (AOP) may be used for predicting reproductive toxicity of untested chemicals. Using the OECD Toolbox and expert judgment, we identified 89 structure groups for 275 chemicals for which the results of prenatal developmental toxicity or multigeneration studies were present in the Fraunhofer database on Fertility and Developmental Toxicity in experimental animals (FeDTex) database. Likewise, we evaluated 220 chemicals which had been tested in reporter gene assays on endocrine ((anti)estrogenic and (anti)androgenic) properties in the CALUX® test battery. There was a large spread of effect levels for substances within the chemical structure groups for both, in vivo and in vitro results. The groups of highest concern (diphenyl derivatives, planar conjugated systems with fused rings, phenols and organophosphates) correlated quite well, however, between the in vivo and in vitro data on estrogenic activity. For the 56 chemicals represented in both databases, lowest effect doses in vivo correlated well with the estrogenic activity in vitro. These results suggest that a panel of assays covering relevant AOPs and data on metabolism and toxicokinetics may allow prediction of relative reproductive or development toxicity potency within the identified chemical structure groups. PMID:25461902

Lewin, Geertje; Escher, Sylvia E; van der Burg, Bart; Simetska, Nelly; Mangelsdorf, Inge

2014-10-22

153

In vitro anti-HIV-1 activity of salicylidene acylhydrazide compounds.  

PubMed

Salicylidene acylhydrazide compounds have been shown to inhibit bacterial pathogens, including Chlamydia and Neisseria gonorrhoeae. If such compounds could also target HIV-1, their potential use as topical microbicides to prevent sexually transmitted infections would be considerable. In this study, the in vitro anti-HIV-1 activity, cytotoxicity and mechanism of action of several salicylidene acylhydrazides were determined. Inhibitory activity was assessed using TZM-bl cells and primary peripheral blood mononuclear cells (PBMCs) as targets for HIV-1 infection. Antiviral activity was measured against cell-free and cell-associated virus and in vaginal fluid and semen simulants. Since the antibacterial activity of salicylidene acylhydrazides is reversible by Fe(2+), the ability of Fe(2+) and other cations to reverse the anti-HIV-1 activity of the compounds was determined. Real-time PCR was also employed to determine the stage affected in the HIV-1 replication cycle. Four compounds with 50% inhibitory concentrations against HIV-1 of 1-7 ?M were identified. In vitro toxicity varied but was generally limited. Activity was similar against three R5 clade B primary isolates and whether the target for virus replication was TZM-bl cells or PBMCs. Compounds inhibited cell-free and cell-associated virus and were active in vaginal fluid and semen simulants. Fe(2+), but not other cations, reversed the anti-HIV-1 effect. Finally, the inhibitory effect of the compounds occurred at a post-integration step. In conclusion, salicylidene acylhydrazides were identified with in vitro anti-HIV-1 activity in the micromolar range. The activity of these compounds against other sexually transmitted pathogens makes them potential candidates to formulate for use as a broad-spectrum topical genital microbicide. PMID:22819150

Forthal, Donald N; Phan, Tran B; Slepenkin, Anatoly V; Landucci, Gary; Chu, Hencelyn; Elofsson, Mikael; Peterson, Ellena

2012-10-01

154

Antioxidant activities of Indigofera cassioides Rottl. Ex. DC. using various in vitro assay models  

PubMed Central

Objective To evaluate the antioxidant potential of methanolic leaf extract of Indigofera cassioides (MEIC) using various in vitro antioxidant assay systems. Methods Antioxidant and free radical scavenging activity of MEIC was assayed by using different in vitro models like ABTS, DPPH, nitric oxide, superoxide, hydrogen peroxide and hydroxyl radical. Reductive ability of the extract was tested by the complex formation with potassium ferricyanide. Further total phenol and flavonoid contents of the crude extract were also determined. Rutin and ascorbic acid were used as standards. Results MEIC exhibited potent and concentration dependent free radical scavenging activity in all the tested models. Reductive ability was also found to increase with increase in MEIC concentration. Total phenol and flavonoid content determination showed that the extract is rich in phenols and flavonoids. Conclusions All the results of the in vitro antioxidant assays reveal potent antioxidant and free radical scavenging activity of the leaves of Indigofera cassioides, equivalent to that of standard ascorbic acid and rutin. This potent antioxidant activity may be attributed to its high phenolic and flavonoid contents. PMID:23569910

Kumar, R Senthil; Rajkapoor, B; Perumal, P

2012-01-01

155

Oxidative stress biomarkers and acetylcholinesterase activity in human erythrocytes exposed to clomazone (in vitro)  

PubMed Central

The aim of this study was to investigate the effect of clomazone herbicide on oxidative stress biomarkers and acetylcholinesterase activity in human erythrocytes in in vitro conditions. The activity of catalase (CAT), superoxide dismutase (SOD) and acetylcholinesterase (AChE), as well as the levels of thiobarbituric acid reactive substances (TBARS) and reduced glutathione (GSH) were measured in human erythrocytes exposed (in vitro) to clomazone at varying concentrations in the range of 0, 100, 250 and 500 µg/L for 1 h at 37 °C.TBARS levels were significantly higher in erythrocytes incubated with clomazone at 100, 250 and 500 µg/L. However, erythrocyte CAT and AChE activities were decreased at all concentrations tested. SOD activity was increased only at 100 µg/L of clomazone. GSH levels did not change with clomazone exposure. These results clearly showed clomazone to induce oxidative stress and AChE inhibition in human erythrocytes (in vitro). We, thus, suggest a possible role of ROS on toxicity mechanism induced by clomazone in humans. PMID:22058656

Santi, Adriana; Menezes, Charlene; Duarte, Marta Maria F.; Leitemperger, Jossiele; Lópes, Thais; Loro, Vania L.

2011-01-01

156

In Vitro Antiproliferative and Antioxidant Activities and Total Phenolic Contents of the Extracts of Melastoma malabathricum Leaves  

Microsoft Academic Search

The present study aims to determine the in vitro antiproliferative and antioxidant activities of various extracts from the leaves of Melastoma malabathricum using various established in vitro assays. The aqueous extract inhibited the proliferation of Caov-3 and HL-60 cell lines, while the chloroform extract exhibited antiproliferative activity against the Caov-3, HL-60, and CEM-SS cell lines. The methanol extract demonstrated antiproliferative activity against

Z. A. Zakaria; M. S. Rofiee; A. M. Mohamed; L. K. Teh; M. Z. Salleh

157

In vitro antimycoplasmal activity of six Jordanian medicinal plants against three Mycoplasma species.  

PubMed

The in vitro effect of six Jordanian traditional medicine plant methanolic extracts were tested against 32 isolates of Mycoplasma species; Mycoplasma mycoides subsp. mycoides LC (6), Mycoplasma capricolum subsp. capricolum (8) and M. putrefaciens (18), all isolated from either nasal swabs or milk, from sheep and goats in different regions in Jordan. All Mycoplasma species showed susceptibility to Artemisia herba-alba and Artemisia arborescens with MIC ranges from 3.125-12.5 mg/ml. Allium sativum and Punica grantum showed limited activity against some Mycoplasma isolates. Olea europea and Citrullus colocynthis showed no in vitro activity against any of the Mycoplasma species tested. Artemisia herba-alba and Artemisia arborescens may therefore be useful for the treatment of mycoplasma infections. PMID:17969714

Al-Momani, W; Abu-Basha, E; Janakat, S; Nicholas, R A J; Ayling, R D

2007-10-01

158

Antifungal activity of hypothemycin against Peronophythora litchii in vitro and in vivo.  

PubMed

The antifungal activity of a natural resorcylic acid lactone, hypothemycin (HPM), against Peronophythora litchii in vitro and in vivo was investigated. HPM treatment substantially suppressed spore germination of P. litchi, with the inhibition rate of 100% when 0.78 ?g/mL HPM was applied. Similarly, mycelial growth of P. litchii was efficiently inhibited. Furthermore, HPM caused the ultrastructural modifications of P. litchii, including the disruption of the cell wall and the endomembrane system, especially the plasma membrane, mitochondria, and vacuoles, which led to the destruction of the cellular integrity. Moreover, application of HPM significantly reduced decay and suppressed peel browning of postharvest litchi fruit inoculated with P. litchii during storage at 28 °C. Overall, these findings suggested that HPM exhibited excellent antifungal activity against P. litchii both in vitro and in vivo, which could be helpful for the storage of harvest litchi fruit. PMID:24106914

Xu, Liangxiong; Xue, Jinghua; Wu, Ping; Wang, Duoduo; Lin, Lijing; Jiang, Yueming; Duan, Xuewu; Wei, Xiaoyi

2013-10-23

159

Sulfated modification of longan polysaccharide and its immunomodulatory and antitumor activity in vitro.  

PubMed

A water-soluble polysaccharide fraction (LP1) was prepared from Dimocarpus longan Lour. by hot water extraction, DEAE-cellulose and Sephadex G-100 chromatography. Its sulfated derivative (LP1-S) was prepared by the sulfuric acid method. Preliminary tests in vitro showed LP1 and LP1-S could stimulate murine lymphocytes proliferation, increase pinocytic activity of murine macrophages and production of nitric oxide (NO), interleukin 6 (IL-6), IL-1? and tumor necrosis factor-alpha (TNF-?) in macrophages. Furthermore, LP1-S exhibited higher antiproliferative activity against human nasopharyngeal carcinoma HONE1 cells in vitro than LP1, which might be caused by the sulfate group in its structures. These results indicated that the LP1-S might be useful for developing safe antitumor drugs or health food. PMID:24680807

Jiang, Jie; Meng, Fa-Yan; He, Zhou; Ning, Yuan-Ling; Li, Xue-Hua; Song, Hui; Wang, Jing; Zhou, Rui

2014-06-01

160

Sericins exhibit ROS-scavenging, anti-tyrosinase, anti-elastase, and in vitro immunomodulatory activities.  

PubMed

Some biological properties of Bombyx mori sericins from twenty strains were investigated, fourteen fed with artificial diet, two with fresh mulberry leaves and four with both diets. Sericin exhibited ROS-scavenging, anti-tyrosinase and anti-elastase properties, the strain significantly influenced these properties, while diet only influenced the anti-tyrosinase activity. Sericins were clustered into 5 groups and one sericin from each group was further studied: sericins showed anti-proliferative activity on in vitro stimulated peripheral blood mononuclear cells; some strains decreased in vitro secretion of IFN?, while no effects were observed on TNF? and IL10 release. Therefore, a mixture of sericins extracted from the most promising strains may be useful for dermatological and cosmetic use. PMID:23541552

Chlapanidas, Theodora; Faragň, Silvio; Lucconi, Giulia; Perteghella, Sara; Galuzzi, Marta; Mantelli, Melissa; Avanzini, Maria Antonietta; Tosca, Marta Cecilia; Marazzi, Mario; Vigo, Daniele; Torre, Maria Luisa; Faustini, Massimo

2013-07-01

161

Cadmium restores in vitro splicing activity inhibited by zinc-depletion.  

PubMed

Zinc (Zn)-depletion inhibits the second step of RNA splicing, namely exon-ligation. To investigate the effects of cadmium (Cd) and other metal ions on RNA splicing inhibited by Zn-depletion, we measured in vitro splicing activities in the presence of these metals. Zn-depletion in the splicing reaction mixture was achieved by addition of a Zn-chelator, 1,10-phenanthroline. Cd(II) at 1, 5 and 10 microM restored the splicing activity to 2, 24 and 72% of that in the control reaction mixture, while higher concentrations of Cd(II) decreased the splicing activity, and more than 50 microM Cd(II) showed a complete absence of spliced products. Hg(II) also restored the splicing activity, albeit to a lesser extent, since 5 and 10 microM Hg(II) restored the splicing activity to 3 and 4% of the control value. The other metal ions examined in this study, Co(II), Cu(II), Mg(II) and Mn(II), did not show any restoration of the splicing activity. We concluded that Cd(II) could restore the in vitro splicing activity inhibited by Zn-depletion, although higher concentrations of Cd(II) prevented progress of the RNA splicing reaction. These results suggest that Cd(II) has a bifunctional property regarding RNA splicing, and is stimulatory at low concentrations and inhibitory at high concentrations. PMID:16645842

Lee, Myeong Jin; Ayaki, Hitoshi; Goji, Junko; Kitamura, Keiko; Nishio, Hisahide

2006-10-01

162

The protective role of AMP-activated protein kinase in alpha-synuclein neurotoxicity in vitro.  

PubMed

In the present study, we investigated the role of the main intracellular energy sensor, AMP-activated protein kinase (AMPK), in the in vitro neurotoxicity of ?-synuclein (ASYN), one of the key culprits in the pathogenesis of Parkinson's disease. The loss of viability in retinoic acid-differentiated SH-SY5Y human neuroblastoma cells inducibly overexpressing wild-type ASYN was associated with the reduced activation of AMPK and its activator LKB1, as well as AMPK target Raptor. ASYN-overexpressing rat primary neurons also displayed lower activity of LKB1/AMPK/Raptor pathway. Restoration of AMPK activity by metformin or AICAR reduced the in vitro neurotoxicity of ASYN overexpression, acting independently of the prosurvival kinase Akt or the induction of autophagic response. The conditioned medium from ASYN-overexpressing cells, containing secreted ASYN, as well as dopamine-modified or nitrated recombinant ASYN oligomers, all inhibited AMPK activation in differentiated SH-SY5Y cells and reduced their viability, but not in the presence of metformin or AICAR. The RNA interference-mediated knockdown of AMPK increased the sensitivity of SH-SY5Y cells to the harmful effects of secreted ASYN. AMPK-dependent protection from extracellular ASYN was also observed in rat neuron-like pheochromocytoma cell line PC12. These data demonstrate the protective role of AMPK against the toxicity of both intracellular and extracellular ASYN, suggesting that modulation of AMPK activity may be a promising therapeutic strategy in Parkinson's disease. PMID:24269733

Dulovic, Marija; Jovanovic, Maja; Xilouri, Maria; Stefanis, Leonidas; Harhaji-Trajkovic, Ljubica; Kravic-Stevovic, Tamara; Paunovic, Verica; Ardah, Mustafa T; El-Agnaf, Omar M A; Kostic, Vladimir; Markovic, Ivanka; Trajkovic, Vladimir

2014-03-01

163

In Vitro and In Vivo Antifungal Activities of T-2307, a Novel Arylamidine?  

PubMed Central

The in vitro and in vivo antifungal activities of T-2307, a novel arylamidine, were evaluated and compared with those of fluconazole, voriconazole, micafungin, and amphotericin B. T-2307 exhibited broad-spectrum activity against clinically significant pathogens, including Candida species (MIC range, 0.00025 to 0.0078 ?g/ml), Cryptococcus neoformans (MIC range, 0.0039 to 0.0625 ?g/ml), and Aspergillus species (MIC range, 0.0156 to 4 ?g/ml). Furthermore, T-2307 exhibited potent activity against fluconazole-resistant and fluconazole-susceptible-dose-dependent Candida albicans strains as well as against azole-susceptible strains. T-2307 exhibited fungicidal activity against some Candida and Aspergillus species and against Cryptococcus neoformans. In mouse models of disseminated candidiasis, cryptococcosis, and aspergillosis, the 50% effective doses of T-2307 were 0.00755, 0.117, and 0.391 mg·kg?1·dose?1, respectively. This agent was considerably more active than micafungin and amphotericin B against candidiasis and than amphotericin B against cryptococcosis, and its activity was comparable to the activities of micafungin and amphotericin B against aspergillosis. The results of preclinical in vitro and in vivo evaluations performed thus far indicate that T-2307 could represent a potent injectable agent for the treatment of candidiasis, cryptococcosis, and aspergillosis. PMID:18227186

Mitsuyama, Junichi; Nomura, Nobuhiko; Hashimoto, Kyoko; Yamada, Eio; Nishikawa, Hiroshi; Kaeriyama, Makoto; Kimura, Akiko; Todo, Yozo; Narita, Hirokazu

2008-01-01

164

Characterization of VIP1 activity as a transcriptional regulator in vitro and in planta  

PubMed Central

VIP1 (VirE2 interacting protein 1), initially discovered as a host protein involved in Agrobacterium-plant cell DNA transfer, is a transcription factor of the basic leucine-zipper (bZIP) domain family that regulates several defence-related genes in Arabidopsis. We have developed assays to assess VIP1 binding to its DNA target in vitro and transcriptional activation efficiency in planta. Several point mutations in the VIP1 response element VRE affected the VIP1 activity, and a strong correlation between VIP1-VRE binding and transcriptional activation levels was observed. Promoter activation by VIP1 was influenced by bacterial and plant proteins known to interact with VIP1 during Agrobacterium infection, i.e., VirE2, VirF and VIP2. VirF, an F-box protein, strongly decreased VIP1 transcriptional activation ability, but not its binding to VRE in vitro, most likely by triggering proteasomal degradation of VIP1. Finally, activation of a VRE-containing promoter was observed in dividing cells, probably resulting from activation of endogenous VIP1. PMID:23942522

Lacroix, Benoît; Citovsky, Vitaly

2013-01-01

165

Curcuminoid derivatives enhance telomerase activity in an in vitro TRAP assay.  

PubMed

The length of telomeres controls the life span of eukaryotic cells. Telomerase maintains the length of telomeres in certain eukaryotic cells, such as germline cells and stem cells, and allows these cells to evade replicative senescence. Here, we report for the first time a number of curcuminoid derivatives that enhance telomerase activity in an in vitro TRAP assay. A preliminary analysis of structure-activity relationships found that the minimal requirement for this enhanced telomerase activity is a curcuminoid core with at least one n-pentylpyridine side chain, while curcuminoids with two such side chains exhibit even greater activity. The finding here might lead to a new class of telomerase activators that act directly or indirectly on telomerase, rather than through the reactivation of the telomerase reverse transcriptase (TERT) gene associated with other telomerase activators found in the literature. PMID:25305686

Taka, Thanachai; Changtam, Chatchawan; Thaichana, Pak; Kaewtunjai, Navakoon; Suksamrarn, Apichart; Lee, T Randall; Tuntiwechapikul, Wirote

2014-11-15

166

In vitro antiplasmodial and cytotoxicity activities of 14 medicinal plants from Kenya  

Microsoft Academic Search

Organic and aqueous extracts obtained from 14 Kenyan medicinal plants were screened for their antimalarial properties on two strains of Plasmodium falciparum (K1 chloroquine resistant and NF54 chloroquine sensitive). Dichloromethane extracts had the highest activities with IC50 ranging from 1.4 to 35.2 ?g\\/ml. These extracts together with methanol extract of Turraea robusta were tested for their cytotoxicity properties in vitro on

Beatrice N. Irungu; Geoffrey M. Rukunga; Geoffrey M. Mungai; Charles N. Muthaura

2007-01-01

167

In vitro activity of tigecycline as a therapeutic option against multidrug-resistant Acinetobacter spp.  

PubMed

The study was performed to detect the in vitro activity of tigecycline in multidrug-resistant Acinetobacter isolates from patients in Hacettepe University Adult Hospital, Turkey. The microorganisms were isolated from clinical specimens of patients with respiratory and bloodstream infections. Thirty (66.7%) of the 45 inpatients were in ICUs. In vitro activity of imipenem, meropenem, ceftazidime, ciprofloxacin and aztreonam in 124 Acinetobacter species isolated was evaluated by microdilution test. Overall, 51 (41%) Acinetobacter spp. were found to be resistant to > or = 3 antibiotics belonging to different antimicrobial classes and defined as multidrug-resistant (MDR). Among the MDR Acinetobacter spp. 32 (62.7%) were Acinetobacter baumannii and 19 (37.3%) Acinetobacter lwoffii. In vitro activity of tigecycline against MDR isolates were studied by E-test. Each MDR isolate was also tested for metallo-beta-lactamase (MBL) production using CLSI guidelines. Forty-five (88.2%) of the isolates were found to produce MBL. The MIC90s of all antimicrobial agents tested except tigecycline were > or = 64 microg/ml whereas the MIC50, and MIC90 of tigecycline were found 1 microg/ml and 1.5 microg/ml, respectively. ERIC-PCR results revealed that bloodstream and respiratory isolates had nine and six different patterns, respectively. In conclusion, tigecycline has been shown to have potent in vitro activity against MDR Acinetobacter spp. and might be of therapeutic value in the treatment of infections due to MDR Acinetobacter spp., including those harbouring MBLs. Further clinical trials are needed to confirm the efficacy of tigecycline in the management of MDR Acinetobacter infections. PMID:19123310

Eser, Ozgen Köseo?lu; Ergin, Alper; Tunçkanat, Ferda; Hasçelik, Gül?en

2008-10-01

168

Comparative in vitro activity of gemifloxacin, ciprofloxacin, levofloxacin and ofloxacin in a North American surveillance study  

Microsoft Academic Search

The in vitro activity of gemifloxacin, a new fluoroquinolone, was compared to three marketed fluoroquinolones; ciprofloxacin, levofloxacin and ofloxacin against over 4,000 recent clinical isolates covering 29 species isolated in the United States and Canada between 1997–1999. Based on MIC90s, gemifloxacin was the most potent fluoroquinolone tested against a majority of Gram-positive isolates: Streptococcus pneumoniae, penicillin resistant S. pneumoniae, macrolide

D. J Hoban; S. K Bouchillon; J. L Johnson; G. G Zhanel; D. L Butler; L. A Miller; J. A Poupard

2001-01-01

169

In vitro analysis of STAT5 activation by granulocyte-macrophage colony-stimulating factor  

Microsoft Academic Search

Background: The granulocyte-macrophage colony-sti- mulating factor (GM-CSF) receptor activates multiple and complex signalling pathways in response to GM- CSF stimulation. Biochemical studies suggested that signalling pathways are transmitted through protein\\/ protein interactions, but how these biochemical cascades are initiated and transmitted in response to cytokine stimulation is largely unknown. Results: To investigate these events biochemically, we established an in vitro

Yoshiko Sakurai; Ken-ichi Arai; Sumiko Watanabe

2000-01-01

170

In vitro propagation of the medicinal plant Ziziphora tenuior L. and evaluation of its antioxidant activity.  

PubMed

Ziziphora tenuior L. (Lamiaceae) is an aromatic herb used for its medicinal values against fungi, bacteria. Micropropagation can be used for large-scale multiplication of essential oil producing plants thus avoiding an overexploitation of natural resources. This work aims to develop a reliable protocol for the in vitro propagation of Z. tenuior, and to compare the antioxidant activity between in vitro propagated and wild plants. The explants were sterilized and cultured on MS medium containing different concentrations of growth regulators naphthalene acetic acid (NAA) or indole-3-butyric acid (IBA) with 0.5 mg/L of kinetin (Kin) callus formation was 70.2% after 45 days of incubation in dark on medium supplemented with 1.5 mg/L of NAA. After one month of callus culture on medium supplemented with 2 mg/L BA the shoot number was 5.12 and for the multiplication stage. The shoot number was 4.21 and length was 6.17 cm on medium supplemented with 1 mg/L Kin + 0.1 mg/L NAA. DPPH• reagent was used to test the antioxidant activity. The aqueous and methanol extracts of in vitro plants which were treated with 1.5 and 1 mg/L of kin plus 0.1 mg/L of NAA showed a strong DPPH• scavenging activity where IC50 was 0.307 and 0.369 mg/ml, respectively, while the IC50 of aqueous and methanol extracts of wild plants was 0.516 and 9.229 mg/ml, respectively. Our results suggested that plant growth regulators and in vitro culture conditions increased the antioxidant activity. PMID:25183942

Dakah, Abdulkarim; Zaid, Salim; Suleiman, Mohamad; Abbas, Sami; Wink, Michael

2014-09-01

171

In vitro propagation of the medicinal plant Ziziphora tenuior L. and evaluation of its antioxidant activity  

PubMed Central

Ziziphora tenuior L. (Lamiaceae) is an aromatic herb used for its medicinal values against fungi, bacteria. Micropropagation can be used for large-scale multiplication of essential oil producing plants thus avoiding an overexploitation of natural resources. This work aims to develop a reliable protocol for the in vitro propagation of Z. tenuior, and to compare the antioxidant activity between in vitro propagated and wild plants. The explants were sterilized and cultured on MS medium containing different concentrations of growth regulators naphthalene acetic acid (NAA) or indole-3-butyric acid (IBA) with 0.5 mg/L of kinetin (Kin) callus formation was 70.2% after 45 days of incubation in dark on medium supplemented with 1.5 mg/L of NAA. After one month of callus culture on medium supplemented with 2 mg/L BA the shoot number was 5.12 and for the multiplication stage. The shoot number was 4.21 and length was 6.17 cm on medium supplemented with 1 mg/L Kin + 0.1 mg/L NAA. DPPH• reagent was used to test the antioxidant activity. The aqueous and methanol extracts of in vitro plants which were treated with 1.5 and 1 mg/L of kin plus 0.1 mg/L of NAA showed a strong DPPH• scavenging activity where IC50 was 0.307 and 0.369 mg/ml, respectively, while the IC50 of aqueous and methanol extracts of wild plants was 0.516 and 9.229 mg/ml, respectively. Our results suggested that plant growth regulators and in vitro culture conditions increased the antioxidant activity. PMID:25183942

Dakah, Abdulkarim; Zaid, Salim; Suleiman, Mohamad; Abbas, Sami; Wink, Michael

2014-01-01

172

In Vitro Activity of BAY 12-8039, a New Fluoroquinolone, against Mycoplasmas  

Microsoft Academic Search

The in vitro activity of the fluoroquinolone BAY 12-8039 against 66 strains of different mycoplasma species and 30 strains of Ureaplasma urealyticum was compared with those of three other antimicrobial agents. BAY 12-8039 at 0.5 mg\\/ml inhibited 100% of all the mycoplasmal and ureaplasmal strains tested. The minimal bactericidal concentrations of BAY 12-8039 increased only two- to eightfold compared to

C. M. BEBEAR; H. RENAUDIN; A. BOUDJADJA; Universitede Bordeaux; Bayer Pharma

1998-01-01

173

Application of modified in vitro screening procedure for identifying herbals possessing sulfonylurea-like activity  

Microsoft Academic Search

We describe here the application of a modified in vitro procedure for identifying herbs potentially possessing sulfonylurea-like activity. The procedure consists of the combination of an SUR1 receptor binding assay and an insulin secretion assay in cultures of HIT-T15 cells. This procedure could be used as an initial step in identifying new safe and efficacious agents for the management of

Y Rotshteyn; S. W Zito

2004-01-01

174

In Vitro and In Vivo Activities of a New Cephalosporin, FR264205, against Pseudomonas aeruginosa  

Microsoft Academic Search

FR264205 is a novel parenteral 3-aminopyrazolium cephalosporin. This study evaluated the in vitro and in vivo activities of FR264205 against Pseudomonas aeruginosa. The MIC of FR264205 at which 90% of 193 clinical isolates of P. aeruginosa were inhibited was 1 g\\/ml, 8- to 16-fold lower than those of ceftazidime (CAZ), imipenem (IPM), and ciprofloxacin (CIP). FR264205 also exhibited this level

Shinobu Takeda; Toru Nakai; Yoshimi Wakai; Fumiaki Ikeda; Kazuo Hatano

2007-01-01

175

In vitro activity of beta-lactam antibiotics against CTX-M-producing Escherichia coli  

Microsoft Academic Search

Beta-lactam antibiotics have been discussed as options for the treatment of infections caused by multiresistant extended-spectrum\\u000a beta-lactamase (ESBL)-producing bacteria if the minimum inhibitory concentration (MIC) is low. The objective of this study\\u000a was to investigate the in vitro activity of different beta-lactam antibiotics against CTX-M-producing Escherichia coli. A total of 198 isolates of E. coli with the ESBL phenotype were

M. Tärnberg; Ĺ. Östholm-Balkhed; H.-J. Monstein; A. Hällgren; H. Hanberger; L. E. Nilsson

176

In vitro activity of tigecycline against multidrug-resistant Enterobacteriaceae isolates from a Belgian hospital  

Microsoft Academic Search

Bacterial resistance among Gram-negative pathogens is a challenging clinical problem. Tigecycline has been developed specifically\\u000a to overcome resistance. The aim of this study was to assess the in vitro activity of tigecycline against ESBL-producing Escherichia coli, ESBL-producing Klebsiella spp., and multidrug-resistant Enterobacter spp. Between May 2007 and March 2008, 26 strains of ESBL-producing Escherichia coli, 10 strains of ESBL-producing Klebsiella

R. Naesens; J. P. Ursi; J. Van Schaeren; A. Jeurissen

2009-01-01

177

In vitro activation of dibromoacetonitrile to cyanide: role of xanthine oxidase  

Microsoft Academic Search

Dibromoacetonitrile (DBAN) is a disinfection byproduct of chlorination of drinking water. Epidemiological studies indicate that it might present a potential hazard to human health. The present work provides evidence for DBAN activation to cyanide (CN-) by the hypoxanthine (HX)\\/xanthine oxidase (XO)\\/iron (Fe) system in vitro. Optimum conditions for the oxidation of DBAN to CN-were characterized. Addition of the sulfhydryl compounds

Ahmed M. Mohamadin; Ashraf B. Abdel-Naim

2003-01-01

178

In Vitro Activity of OPT-80 Tested against Clinical Isolates of Toxin-Producing Clostridium difficile?  

PubMed Central

Agar dilution antimicrobial susceptibility testing (CLSI, M11-A7, 2007) performed for 208 toxin-producing clinical isolates of Clostridium difficile resulted in OPT-80 MICs ranging from 0.06 to 1 ?g/ml, with 90% of the isolates inhibited by a concentration of 0.5 ?g/ml. The in vitro activity of OPT-80 was independent of the susceptibilities of isolates to nine other antimicrobial agents. PMID:18725442

Karlowsky, James A.; Laing, Nancy M.; Zhanel, George G.

2008-01-01

179

In vitro evaluation of the antimicrobial activity of chlorhexidine and sodium hypochlorite  

Microsoft Academic Search

The aim of this study was to investigate in vitro the antimicrobial activity of 0.2%, 1%, and 2% chlorhexidine gluconate (CHX gel and CHX liquid), against endodontic pathogens and compare the results with the ones achieved by 0.5%, 1%, 2.5%, 4%, and 5.25% sodium hypochlorite (NaOCl). A broth dilution test was performed, and the timing for irrigants to kill microbial

Morgana Eli Vianna; Brenda P. F. A Gomes; Vanessa Bellocchio Berber; Alexandre Augusto Zaia; Caio Cezar Randi Ferraz; Francisco José de Souza-Filho

2004-01-01

180

In vitro and in vivo Activities of a New Lead Compound I2906 against Mycobacterium tuberculosis  

Microsoft Academic Search

Background: Due to the long duration of treatment and the emergence of multidrug-resistant strains, new antitubercular agents are urgently needed. I2906, as a novel lead, was screened and tested for efficacy in vitro and in vivo. Methods:To determine the efficacy of I2906,the minimum inhibitory concentrations against Mycobacterium tuberculosis and cytotoxicity were tested, and its in vivo activities were assessed by

Jingning Lu; Jun Yue; Jing Wu; Rusong Luo; Zhidong Hu; Jianrong Li; Yun Bai; Zhijiao Tang; Qiaoyang Xian; Xuelian Zhang; Honghai Wang

2010-01-01

181

In vitro and in vivo immunosuppressive activity of Spica Prunellae ethanol extract on the immune responses in mice  

Microsoft Academic Search

The immunosuppressive activity of the ethanol extract of Spica Prunellae (Prunella vulgaris fruiting spikes) (EESP) consisting of a mixture of triterpenoids, flavonoids, tannins and polysaccharide was studied on the immune responses in mice. The effects of EESP on mice splenocyte proliferation in vitro were measured. EESP significantly suppressed concanavalin A (Con A)- and lipopolysaccharide (LPS)-stimulated splenocyte proliferation in vitro in

Hong-Xiang Sun; Feng Qin; Yuan-Jiang Pan

2005-01-01

182

Quantitative studies on the in vitro metabolic activation of dimethylnitrosamine by rat liver postmitochondrial supernatant.  

PubMed Central

The metabolic activation of dimethylnitrosamine (DMN) to mutagenic and/or cytotoxic intermediates in vitro has been characterized and the relationship between DMN demethylase and ethoxyresorufin-O-deethylase (EROD) or ethylmorphine-N-demethylase (EMND) has been evaluated. A mammalian assay system which uses the postmitochondrial supernatant (S-15 fraction) prepared from a rat liver homogenate as an enzyme source and V79 Chinese hamster cells as targets for chemically induced damage was used. The enzyme pattern of the S-15 fraction was altered by pretreatment of experimental animals in vivo and/or by the use of enzyme inhibitors in vitro. The results of these studies indicate that the concentration of S-15 fraction in the reaction mixture can markedly influence the degree of DMN-induced cytotoxicity when it is metabolized in vitro and that the degree of DMN-induced cytotoxicity and mutagenicity are linearly related. The degree of cytotoxicity and mutagenicity induced in V79 cells by DMN does not correlate with EROD activity (a measure of 3-methylcholanthrene-inducible mixed-function oxidases) nor with EMND activity (a measure of phenobarbital-inducible mixed function oxidases) in the S-15 fraction. PMID:6499815

Doolittle, D J; Goodman, J I

1984-01-01

183

Nanostructured Systems Containing Rutin: In Vitro Antioxidant Activity and Photostability Studies  

NASA Astrophysics Data System (ADS)

The improvement of the rutin photostability and its prolonged in vitro antioxidant activity were studied by means of its association with nanostructured aqueous dispersions. Rutin-loaded nanocapsules and rutin-loaded nanoemulsion showed mean particle size of 124.30 ± 2.06 and 124.17 ± 1.79, respectively, polydispersity index below 0.20, negative zeta potential, and encapsulation efficiency close to 100%. The in vitro antioxidant activity was evaluated by the formation of free radical ·OH after the exposure of hydrogen peroxide to a UV irradiation system. Rutin-loaded nanostructures showed lower rutin decay rates [(6.1 ± 0.6) 10-3 and (5.1 ± 0.4) 10-3 for nanocapsules and nanoemulsion, respectively] compared to the ethanolic solution [(35.0 ± 3.7) 10-3 min-1] and exposed solution [(40.1 ± 1.7) 10-3 min-1] as well as compared to exposed nanostructured dispersions [(19.5 ± 0.5) 10-3 and (26.6 ± 2.6) 10-3, for nanocapsules and nanoemulsion, respectively]. The presence of the polymeric layer in nanocapsules was fundamental to obtain a prolonged antioxidant activity, even if the mathematical modeling of the in vitro release profiles showed high adsorption of rutin to the particle/droplet surface for both formulations. Rutin-loaded nanostructures represent alternatives to the development of innovative nanomedicines.

Almeida, Juliana S.; Lima, Fernanda; Ros, Simoní Da; Bulhőes, Luis O. S.; de Carvalho, Leandro M.; Beck, Ruy C. R.

2010-10-01

184

beta-Glucuronidase activities of intestinal bacteria determined both in vitro and in vivo in gnotobiotic rats.  

PubMed Central

The beta-glucuronidase activities of bacterial strains isolated from the rat intestinal tract were studied both in vitro in culture media and in vivo in the intestinal contents of gnotobiotic rats. Only 50 of 407 strains tested were found to be positive in vitro. They belonged to the three genera Clostridium, Peptostreptococcus, and Staphylococcus. The in vitro-negative strains were also negative in vivo. The beta-glucuronidase activities of the beta-glucuronidase activities of the positive strains were generally greater in vivo than in vitro. The highest in vivo activities were found in the intact bacterial cells and in the soluble fractions prepared from disrupted pellets. There was a discrepancy between the activities obtained from both conventional and gnotobiotic rats harboring selected positive strains, suggesting that the main beta-glucuronidase-positive strains have not yet been isolated from the intestines of conventional rats. PMID:3994372

Gadelle, D; Raibaud, P; Sacquet, E

1985-01-01

185

Dibutyltin Activates MAP kinases in Human Natural Killer Cells, in vitro  

PubMed Central

Previous studies have shown that dibutyltin (DBT) interferes with the function of human natural killer (NK) cells, diminishing their capacity to destroy tumor cells, in vitro. DBT is a widespread environmental contaminant and has been found in human blood. As NK cells are our primary immune defense against tumor cells, it is important to understand the mechanism by which DBT interferes with their function. The current study examines the effects of DBT exposures on key enzymes in the signaling pathway that regulates NK responsiveness to tumor cells. These include several protein tyrosine kinases (PTKs), mitogen activated protein kinases (MAPKs) and mitogen activated protein kinase kinases (MAP2Ks). The results showed that in vitro exposures of NK cells to DBT had no effect on PTKs. However, exposures to DBT for as little as 10 min were able to increase the phosphorylation (activation) of the MAPKs. The DBT-induced activations of these MAPKs, appears to be due to DBT-induced activations of the immediate upstream activators of the MAPKs, MAP2Ks. The results suggest that DBT-interference with the MAPK signaling pathway is a consequence of DBT exposures, which could account for DBT-induced decreases in NK function. PMID:20333459

Odman-Ghazi, Sabah O.; Abraha, Abraham; Isom, Erica Taylor; Whalen, Margaret M.

2010-01-01

186

In vitro antioxidant activity of hydro alcoholic extract from the fruit pulp of Cassia fistula Linn.  

PubMed

The present study is aimed to investigate antioxidant activity of the extracts of Cassia fistula Linn. (Leguminosae) fruit pulp. Cassia fistula Linn., a Indian Laburnum, is widely cultivated in various countries and different continents including Asia, Mauritius, South Africa, Mexico, China, West Indies, East Africa and Brazil as an ornamental tree for its beautiful bunches of yellow flowers and also used in traditional medicine for several indications. The primary phytochemical study and in vitro antioxidant study was performed on hydro alcoholic extract of fruit pulp. Phytochemical screening of the plant has shown the presence of phenolic compounds, fatty acids, flavonoids, tannins and glycosides. Phenolic content was measured using Folin-Ciocalteu reagent and was calculated as gallic acid equivalents. Antiradical activity of hydro alcoholic extract was measured by DPPH (2,2-diphenyl-1- picrylhydrazyl) assay and was compared to ascorbic acid. Ferric reducing power of the extract was also evaluated by Oyaizu method. In the present study, three methods were used for evaluation of antioxidant activity. First two methods were for direct measurement of radical scavenging activity and third method to evaluate the reducing power. Results indicate that hydro alcoholic fruit pulp extracts have marked amount of total phenols which could be responsible for the antioxidant activity. These in vitro assays indicate that this plant extract is a significant source of natural antioxidant, Cassia fistula fruit pulp extract shows lower activity in DPPH and total phenol content as compared with standard which might be helpful in preventing the progress of various oxidative stresses. PMID:24250133

Bhalodia, Nayan R; Nariya, Pankaj B; Acharya, R N; Shukla, V J

2013-04-01

187

In Vitro and In Vivo Activities of CS-758 (R-120758), a New Triazole Antifungal Agent  

PubMed Central

The activity of CS-758 (R-120758), a new triazole antifungal agent, was evaluated and compared with those of fluconazole, itraconazole, and amphotericin B in vitro and with those of fluconazole and itraconazole in vivo. CS-758 exhibited potent in vitro activity against clinically important fungi. The activity of CS-758 against Candida spp. was superior to that of fluconazole and comparable or superior to those of itraconazole and amphotericin B. CS-758 retained potent activity against Candida albicans strains with low levels of susceptibility to fluconazole (fluconazole MIC, 4 to 32 ?g/ml). Against Aspergillus spp. and Cryptococcus neoformans, the activity of CS-758 was at least fourfold superior to those of the other drugs tested. CS-758 also exhibited potent in vivo activity against murine systemic infections caused by C. albicans, C. neoformans, Aspergillus fumigatus, and Aspergillus flavus. The 50% effective doses against these infections were 0.41 to 5.0 mg/kg of body weight. These results suggest that CS-758 may be useful in the treatment of candidiasis, cryptococcosis, and aspergillosis. PMID:11796343

Kamai, Yasuki; Harasaki, Tamako; Fukuoka, Takashi; Ohya, Satoshi; Uchida, Katsuhisa; Yamaguchi, Hideyo; Kuwahara, Shogo

2002-01-01

188

In vitro and in vivo antibacterial activities of a new quinolone, OPC-17116.  

PubMed Central

The in vitro and in vivo antibacterial activities of OPC-17116 were compared with those of ofloxacin, enoxacin, ciprofloxacin, and tosufloxacin. The MICs of OPC-17116 for 90% of the strains tested were 0.125 to 8 micrograms/ml against gram-positive bacteria such as members of the genera Staphylococcus, Streptococcus, and Enterococcus: less than or equal to 0.063 to 16 micrograms/ml against members of the family Enterobacteriaceae; and less than or equal to 0.063 to 16 micrograms/ml against glucose-nonfermentative bacilli such as Pseudomonas aeruginosa. The activity of OPC-17116 against gram-positive organisms was comparable to that of tosufloxacin and higher than those of other reference drugs. The in vitro activity of OPC-17116 against gram-negative bacteria was similar to those of the reference drugs. In experimental systemic infections in mice with various organisms, the efficacy of OPC-17116 was similar to that of tosufloxacin and greater than those of ofloxacin, enoxacin, and ciprofloxacin. In a pyelonephritic model in mice with P. aeruginosa KU-1, OPC-17116 was as active as ciprofloxacin and more active than ofloxacin, enoxacin, and tosufloxacin. In respiratory tract infections in mice with Staphylococcus aureus Smith, Streptococcus pneumoniae TMS 3, and Klebsiella pneumoniae 3K25, the efficacy of OPC-17116 was generally greater than that of tosufloxacin. The peak level of OPC-17116 in the lungs of mice was 10 times higher than that in serum and was significantly greater than levels in lung achieved with an equivalent dose of the other quinolones. The therapeutic efficacy of OPC-17116 may depend not only on its in vitro activity but also on its high concentration in tissue. PMID:1320364

Imada, T; Miyazaki, S; Nishida, M; Yamaguchi, K; Goto, S

1992-01-01

189

In Vitro Antibacterial Activity of three Indian Spices Against Methicillin-Resistant Staphylococcus aureus  

PubMed Central

Objective To explore the in vitro antibacterial activity of ethanolic extracts of cinnamon (Cinnamomum zeylanicum; CIN), clove (Syzygium aromaticum, CLV) and cumin (Cuminum cyminum, CMN) against clinical isolates of methicillin resistant Staphylococcus aureus (MRSA), from Kolkata, India. Methods The CIN, CLV and CMN were tested for their antibacterial activity against MRSA by in vitro methods. Minimum inhibitory concentration (MIC) values of the three extracts were determined, and time-kill studies were performed in order to investigate the bactericidal activity of the extracts (at the MIC level) for the isolates. The killing efficacy of the extracts was determined at various concentrations. Results The zone diameter of inhibition (ZDI) obtained due to CIN, CLV and CMN ranged between 22-27 mm, 19-23 mm and 9-15 mm, respectively; while the MICs, for the isolates, were in the range of 64-256, 64-512 and 128-512 µg/ml, respectively. When tested for their MIC levels; the CIN and CLV were found to be bactericidal after 6 hrs of incubation, while CMN showed bactericidal activity after 24 hrs. However, when tested at various concentrations; CIN, CLV and CMN displayed bactericidal activity against S. aureus, after 24 hrs of incubation, at 200, 200 and 300 µg/ml, respectively. Conclusion The C. zeylanicum and S. aromaticum showed the strongest in vitro antibacterial activity followed by C. cyminum against MRSA, and such findings could be considered a valuable support in the treatment of infection and may contribute to the development of potential antimicrobial agents for inclusion in anti- S. aureus regimens. PMID:22125725

Mandal, Shayamapda; Saha, Krishnendu; Pal, Nishith Kumar

2011-01-01

190

Redispersible liposomal-N-acetylcysteine powder for pulmonary administration: development, in vitro characterization and antioxidant activity.  

PubMed

Liposomal dry powders of N-acetylcysteine (SD-NAC-Lip) were developed for pulmonary administration. Liposomes were prepared by reverse phase evaporation and spray dried using lactose (10%, w/w) as drying adjuvant. The powders were characterized according to process yield, drug content, residual water content, particle size distribution, morphology and redispersion behavior. In vitro aerosol performance was evaluated using an eight-stage Andersen Cascade Impactor. Moreover, in vitro antioxidant activity was determined by measuring thiobarbituric acid reactive species (TBARS) present in the lungs of healthy Wistar rats after induction of oxidation by iron/EDTA. The spray-drying process had a high yield (71%±2), drug content (mg/g) according to the expected value, moisture content below 9%, geometric mean diameter under 3?m with span value lower than 1. Spherical particles were observed by scanning electron microscopy. Liposomal dry-powders were able to recover the nanometric size of the original dispersion after their redispersion in aqueous medium, as shown by laser diffraction and transmission electron microscopy. Furthermore, the powders presented aerodynamic diameter of about 7?m and respirable fraction above 30%, indicating suitable properties for pulmonary use. The encapsulation of N-acetylcysteine in liposomes was essential to maintain its in vitro antioxidant activity after the drying process. In addition, the powder containing the encapsulated drug had better in vitro antioxidant activity than the liquid and solid formulations containing the non-encapsulated drug, which makes it a good candidate for the treatment of pulmonary diseases associated with oxidative stress. PMID:25263567

Ourique, Aline Ferreira; Chaves, Paula Dos Santos; Souto, Gabriele Dadalt; Pohlmann, Adriana Raffin; Guterres, Silvia Stanisçuaski; Beck, Ruy Carlos Ruver

2014-12-18

191

Diphenyl diselenide in vitro and in vivo activity against the oomycete Pythium insidiosum.  

PubMed

This study evaluated the in vitro activity of diphenyl diselenide against 19 Pythium insidiosum isolates and the in vivo therapeutic response of rabbits with experimentally induced pythiosis. In vitro: susceptibility tests were performed using the broth macrodilution method in accordance with the CLSI document M38-A2. The criteria for interpretation were as follows: MIC-1 and MIC-2 (inhibition of 90% and 100% of mycelium growth, respectively) and the minimum fungicide concentration (MIC-3). In vivo: twenty rabbits were divided into four groups with five animals each and treated for 40 consecutive days: groups 1 and 2 (experimentally induced pythiosis) were treated with diphenyl diselenide (10mg/kg/day) and canola oil (1 mL/kg/day), respectively; groups 3 and 4 (controls) were treated with canola oil (1 mL/kg/day) and diphenyl diselenide (10mg/kg/day), respectively. Toxicity was evaluated using biochemical and haematological parameters. In vitro susceptibility tests showed that 89.4% of isolates had a MIC-1 ? 0.5 ?g/mL, 84.2% of isolates had a MIC-2 ? 1.0 ?g/mL and 94.7% of isolates had a MIC-3 ? 2.0 ?g/mL. The in vivo assay suggested that this compound has a fungistatic activity, and the biochemical and haematological parameters indicated that there was no renal, hepatic or haematological toxicity. The comparison of the unsaturated iron binding capacity levels between animals with and without pythiosis suggested the involvement of iron metabolism in the pathogenesis of pythiosis. This study demonstrated the absence of detectable toxicity caused by diphenyl diselenide and the in vitro fungicidal and in vivo fungistatic activities of this drug, which makes it an option for future therapeutic approaches in the treatment of pythiosis. PMID:22055205

Loreto, Erico Silva; Alves, Sydney Hartz; Santurio, Janio Morais; Nogueira, Cristina Wayne; Zeni, Gilson

2012-04-23

192

Identification and Validation of Soy Peptides with In-vitro Hemagglutination Activity  

Microsoft Academic Search

We previously demonstrated that different enzyme hydrolysates of soybean agglutinin (SBA), ?-conglycinin and glycinin-rich\\u000a fractions had in-vitro hemagglutination activities. In the present study, the three proteins were subjected to trypsin hydrolysis,\\u000a and N-acetyl-d-galactosamine (GalNAc)-agarose beads were used to isolate the active peptides. Matrix Assisted Laser Desorption\\/Ionization\\u000a Time-of-Flight (MALDI?TOF) Mass Spectrometry (MS) was used to determine the mass of the peptides

Yating Ma; Tong Wang

2011-01-01

193

Effect of Nano red elemental selenium on GPx activity of broiler chick kidney cells in vitro  

Microsoft Academic Search

A new selenium source, Nano red elemental selenium (Nano-Se) was used to study the effect on the GPx activity of broiler chick\\u000a kidney cells (BCKC)in vitro, Sodium selenite (Na2SeO3) and seleno-1-methionine (Se-Met) were used as the controls. The results showed that the effects of three kinds of Se forms\\u000a on the GPx activity of BCKC were accordant (p>0.05) compared with

Xu Bao-hua; Xu Zi-rong; Xia Mei-sheng; Hu Cai-hong; Deng Yue-song; Xiong Li

2003-01-01

194

A humanized anti-M2 scFv shows protective in vitro activity against influenza  

SciTech Connect

M2 is one of the most conserved influenza proteins, and has been widely prospected as a potential universal vaccine target, with protection predominantly mediated by antibodies. In this paper we describe the creation of a humanized single chain Fv from 14C2, a potent monoclonal antibody against M2. We show that the humanized scFv demonstrates similar activity to the parental mAb: it is able to recognize M2 in its native context on cell surfaces and is able to show protective in vitro activity against influenza, and so represents a potential lead antibody candidate for universal prophylactic or therapeutic intervention in influenza.

Bradbury, Andrew M [Los Alamos National Laboratory; Velappan, Nileena [Los Alamos National Laboratory; Schmidt, Jurgen G [Los Alamos National Laboratory

2008-01-01

195

In vitro antifungal activity of phenylheptatriyne from Bidens cernua L. against yeasts.  

PubMed

In vitro antifungal activity of phenylheptatriyne from Bidens cernua L. (Asteraceae) was studied using broth macrodilution method against 125 strains of yeasts including 104 clinical and other isolates of Candida spp. (C. albicans, C. krusei, C. tropicalis, C. guilliermondii, C. parapsilosis, C. glabrata, C. inconspicua), 16 strains of basidiomycetous yeasts (Cryptococcus neoformans, C. albidus, Trichosporon cutaneum, Rhodotorula glutinis) and five standard reference strains of Candida species. Phenylheptatriyne has shown significant activity against investigated strains, and the Minimal Inhibitory Concentrations for Candida spp. were determined as 12.5-50 microg/ml and for basidiomycetous yeasts as 12.5-100 microg/ml. PMID:19837144

Rybalchenko, N P; Prykhodko, V A; Nagorna, S S; Volynets, N N; Ostapchuk, A N; Klochko, V V; Rybalchenko, T V; Avdeeva, L V

2010-07-01

196

In Vitro Activity of Mirincamycin (U24729A) against Plasmodium falciparum Isolates from Gabon?  

PubMed Central

We assessed the in vitro activity of mirincamycin, a lincosamide antibiotic, against Plasmodium falciparum clinical isolates from Gabon. Growth was determined by HRP2 enzyme-linked immunosorbent assay using an adapted protocol with a prolonged incubation time (6 days) to account for antibiotic-induced delayed death. Mirincamycin's cis and trans isomers are more active (median 50% inhibitory concentrations [IC50s], 3.2 nM and 2.6 nM) than the comparator drugs clindamycin (IC50, 12 nM) and doxycycline (IC50, 720 nM), and therefore, further clinical development is promising. PMID:19841147

Held, Jana; Westerman, Richard; Kremsner, Peter G.; Mordmüller, Benjamin

2010-01-01

197

Synthesis and in vitro antibacterial activity of oxazolidine LBM-415 analogs as peptide deformylase inhibitors.  

PubMed

The drug resistant bacteria pose a severe threat to human health. The increasing resistance of those pathogens to traditional antibacterial therapy renders the identification of new antibacterial agents with novel antibacterial mechanisms an urgent need. In this study, a series of (2S)-N-substituted-1-[(formyhydroxyamino)methyl]-1-oxohexyl]-2-oxazolidinecarboxamides were designed, synthesized and evaluated for in vitro antibacterial activity. Most of these compounds displayed good activities against Gram-positive organisms comparable to reference agent LBM-415. PMID:21288715

Yu, Linliang; Zhou, Weicheng; Wang, Zhenyu

2011-03-01

198

In vitro hypoglycemic activity of methanolic extract of some indigenous plants.  

PubMed

Pakistan is rich in medicinally important plants and has ancient herbal treatment methods. Present work is based on the study of six indigenous plants Eugenia jambolana, Lawsonia inermis, Momordica charantia, Morus alba, Nigella sativa and Trigonella foenum graecum which show the inhibitory effect of glucose utilization, and are in use as hypoglycemic agents of varying degree in traditional system of medicine. The glucose uptake activity of (methanolic extracts) of these plants was tested in vitro and glucose was estimated by glucose oxidase method. The results in three different media revealed that, hypoglycemic activity is more prominent in neutral and basic media as compared to acidic medium. PMID:17604247

Arayne, M Saeed; Sultana, Najma; Mirza, Agha Zeeshan; Zuberi, M Hashim; Siddiqui, Farhan Ahmed

2007-10-01

199

In vitro xanthine oxidase inhibitory and in vivo hypouricemic activity of herbal coded formulation (Gouticin).  

PubMed

Currently, natural products have been used in treating gouty arthritis and are recognized as xanthine oxidase inhibitors. Current study was designed to evaluate in vitro xanthine oxidase inhibitory potential of Gouticin and its ingredients extracts and in vivo hypouricemic activity of gouticin tablet 500 mg twice daily. Ethanol extracts of Gouticin and its ingredients were evaluated in vitro, at 200, 100, 50, 25 ? g/ml concentrations for xanthine oxidase inhibitory activity. IC(50) values of Gouticin and its ingredients were estimated. Further, in vivo therapeutic effect of Gouticin was investigated in comparison with allopathic medicine (Allopurinol) to treat gout. Total patients were 200 that were divided into test and control group. Herbal coded medicine (Gouticin) was given to test group and allopathic medicine allopurinol was administered to control group. In vitro, Gouticin has the highest percent inhibition at 96% followed by Allopurinol with 93% inhibition. In vivo study, mean serum uric acid level of patients was 4.62 mg/dl and 5.21mg/dl by use of Gouticin and Allopurinol at end of therapy. The study showed that herbal coded formulation gouticin and its ingredients are potential sources of natural xanthine oxidase inhibitors. Gouticin 500 mg twice daily is more effective than the allopurinol 300mg once daily in the management of gout. PMID:24811815

Akram, Muhammad; Usmanghani, Khan; Ahmed, Iqbal; Azhar, Iqbal; Hamid, Abdul

2014-05-01

200

Hepatoprotective activity of Sapindus mukorossi and Rheum emodi extracts: In vitro and in vivo studies  

PubMed Central

AIM: To study the hepatoprotective capacity of Sapindus mukorossi (S. mukorossi) and Rheum emodi (R. emodi) extracts in CCl4 treated male rats. METHODS: The dried powder of S. mukorossi and R. emodi was extracted successively with petroleum ether, benzene, chloroform, and ethanol and concentrated in vacuum. Primary rat hepatocyte monolayer cultures were used for in vitro studies. In vivo, the hepatoprotective capacity of the extract of the fruit pericarp of S. mukorossi and the rhizomes of R. emodi was analyzed in liver injured CCl4-treated male rats. RESULTS: In vitro: primary hepatocytes monolayer cultures were treated with CCl4 and extracts of S. mukorossi & R. emodi. A protective activity could be demonstrated in the CCl4 damaged primary monolayer culture. In vivo: extracts of the fruit pericarp of S. mukorossi (2.5 mg/mL) and rhizomes of R. emodi (3.0 mg/mL) were found to have protective properties in rats with CCl4 induced liver damage as judged from serum marker enzyme activities. CONCLUSION: The extracts of S. mukorossi and R. emodi do have a protective capacity both in vitro on primary hepatocytes cultures and in in vivo in a rat model of CCl4 mediated liver injury. PMID:18442207

Ibrahim, Mohammed; Khaja, Mohammed Nane; Aara, Anjum; Khan, Aleem Ahmed; Habeeb, Mohammed Aejaz; Devi, Yalavarthy Prameela; Narasu, Mangamoori Lakshmi; Habibullah, Chitoor Mohammed

2008-01-01

201

Specialization of the DNA-Cleaving Activity of a Group I Ribozyme Through In Vitro Evolution  

NASA Technical Reports Server (NTRS)

In an earlier study, an in vitro evolution procedure was applied to a large population of variants of the Tetrahymena group 1 ribozyme to obtain individuals with a 10(exp 5)-fold improved ability to cleave a target single-stranded DNA substrate under simulated physiological conditions. The evolved ribozymes also showed a twofold improvement, compared to the wild-type, in their ability to cleave a single-stranded RNA substrate. Here, we report continuation of the in vitro evolution process using a new selection strategy to achieve both enhanced DNA and diminished RNA-cleavage activity. Our strategy combines a positive selection for DNA cleavage with a negative selection against RNA binding. After 36 "generations" of in vitro evolution, the evolved population showed an approx. 100-fold increase in the ratio of DNA to RNA-cleavage activity. Site-directed mutagenesis experiment confirmed the selective advantage of two covarying mutations within the catalytic core of ribozyme that are largely responsible for this modified behavior. The population of ribozymes has now undergone a total of 63 successive generations of evolution, resulting in an average 28 mutations relative to the wild-type that are responsible for the altered phenotype.

Tsang, Joyce; Joyce, Gerald F.

1996-01-01

202

Synthesis and in vitro anthelmintic activity against Nippostrongylus brasiliensis of new 2-amino-4-hydroxy-delta-valerolactam derivatives.  

PubMed

The synthesis of a series of 2-amino-4-hydroxy-delta-valerolactam derivatives is described (compounds 4 to 10). These compounds showed a high anthelmintic in vitro activity against the Nippostrongylus brasiliensis model. PMID:9580122

Gordon, S; Costa, L; Incerti, M; Manta, E; Saldańa, J; Domínguez, L; Mariezcurrena, R; Suescun, L

1997-10-01

203

In vitro assays for assessment of androgenic and estrogenic activity of defined mixtures and complex environment samples  

EPA Science Inventory

Point sources of potentially endocrine active compounds to aquatic environments such as waste water treatment plants, pulp and paper mills, and animal feeding operations invariably contain complex mixtures of chemicals. The current study investigates the use of targeted in vitro ...

204

In vitro immunomodulatory activity of Bo-yang-hwan-o-tang.  

PubMed

Bo-yang-hwan-o-tang (BHT), an herbal decoction has been mainly used for improvement of blood flow in oriental medicine. Its in vivo immunomodulation was recently demonstrated but the effective mechanisms have not been described. This study was carried out to evaluate in vitro immunomodulatory activity of BHT. Water extract of BHT significantly promoted in vitro proliferative responses of mouse spleen cells (SPC) and also further enhanced the proliferation of SPC stimulated with anti-CD3 antibody. Unexpectedly, addition of BHT extract did not affect proliferation of both resting and CD3-activated T cells, whereas it showed a strong mitogenic activity on B cells. Flow cytometric analysis of CFSE-stained SPC showed that BHT-mediated enhancement of CD3-activated SPC proliferation is due to T cell, but not B cell, division. Mixed culture experiment combining T and mitomycin C-treated B cells demonstrated that BHT-mediated enhancement of CD3-activated T cell proliferation was dependent on the presence of B cells. However, B cell-derived factors were not involved in BHT effect on T cell proliferation. In the presence of B cells, BHT treatment resulted in a great enhancement in IL-2 production of CD3-activated T cells, and BHT effect on T cell proliferation was completely abrogated by addition of exogenous IL-2, indicating that IL-2 plays a critical role in BHT-mediated enhancement of CD3-activated T cell proliferation. Taken together, our data revealed that BHT possesses a potent B cell mitogenic activity and also can enhance activated T cell response through B cell regulation. PMID:15658611

Kim, Young-Hyun; Ha, Jong-Cheon; Do, Jeong-Su; Choi, Youn-Hwa; Choo, Young Kug; Woo, Won-Hong; Yi, Ho Keun; Hwang, Pyung Han; Nam, Sang-Yun

2004-01-01

205

Antibody C region influences TGN1412-like functional activity in vitro.  

PubMed

The unexpected outcome of the clinical trial of the superagonistic CD28 mAb TGN1412 (IgG4?) continues to stimulate interest. We show that TGN1412 binds similarly to human and cynomolgus macaque Fc?R, eliminating the possibility that differences in Fc-mediated interactions with Fc?R contributed to the failure of preclinical testing in macaques to predict toxicity in humans. The influence of the Fc domain and C region structure on the in vitro functional activity of TGN1412 was investigated using F(ab')(2) and Fab fragments derived from TGN1412 recovered from the trial and recombinant TGN1412 subclass variants and mutants. Superagonistic activity, as measured by cytokine release and proliferation, was assessed by exposing PBMCs to immobilized mAbs/fragments or to aqueous mAbs/fragments in the presence of HUVEC monolayers. Removing the Fc generally curtailed or abolished PBMC activation. However, eliminating detectable Fc?R-binding of the IgG4 by mutation (L235E) did not abrogate activity. Stabilizing the "wild-type" IgG4 hinge (S228P) enhanced activity without increasing Fc?R binding, which could only partially be explained by inhibition of Fab arm-exchange. Subclass switching the IgG4 mAb to IgG1 decreased activity, whereas switching to IgG2 markedly increased activity. We conclude that the C region strongly influences in vitro CD28-mediated superagonistic signaling. Superagonism requires an intact Fc, as shown by the absence of activity of TGN1412 Fab and F(ab')(2) fragments, but, notably, appears to be relatively independent of Fc?R-binding properties. We propose that the Fc, potentially through restricting flexibility, maintains a favorable V region conformation to allow superagonistic activity. These findings have important implications for Ab design strategies. PMID:23150712

Ball, Christina; Fox, Bernard; Hufton, Simon; Sharp, Giles; Poole, Stephen; Stebbings, Richard; Eastwood, David; Findlay, Lucy; Parren, Paul W H I; Thorpe, Robin; Bristow, Adrian; Thorpe, Susan J

2012-12-15

206

Pharmacological Activity of Retinoic Acid Receptor Alpha-Selective Antagonists in Vitro and in Vivo  

PubMed Central

Oral administration of a retinoic acid receptor (RAR) pan-antagonist reversibly inhibits spermatogenesis. Given the importance of RAR? in regulating spermatogenesis, we identified two RAR?-selective antagonists by transactivation and transactivation competition assays and asked whether they effectively inhibit spermatogenesis. Although these two antagonists were potent in vitro, they displayed poor in vivo activity in mice when administered orally. Testicular weights were normal, and morphological analysis revealed normal spermatid alignment and sperm release. In vitro drug property analyses were performed with one of these antagonists and compared with the pan-antagonist. We showed that the discrepancies may be explained by several factors, including high plasma protein binding, faster hepatic metabolism relative to the pan-antagonist, and only moderate permeability. The conclusion of poor oral bioavailability was supported by more pronounced defects in mice when the antagonist was administered intravenously versus intraperitoneally. These results are crucial for designing new RAR?-selective antagonists for pharmaceutical application. PMID:24040487

2013-01-01

207

Characterization of calcium responses and electrical activity in differentiating mouse neural progenitor cells in vitro.  

PubMed

In vitro methods for developmental neurotoxicity (DNT) testing have the potential to reduce animal use and increase insight into cellular and molecular mechanisms underlying chemical-induced alterations in the development of functional neuronal networks. Mouse neural progenitor cells (mNPCs) differentiate into nervous system-specific cell types and have proven valuable to detect DNT using biochemical and morphological techniques. We therefore investigated a number of functional neuronal parameters in primary mNPCs to explore their applicability for neurophysiological in vitro DNT testing. Immunocytochemistry confirmed that mNPCs express neuronal, glial, and progenitor markers at various differentiation durations (1, 7, 14, and 21 days). Because intracellular calcium ([Ca(2+)]i) plays an essential role in neuronal development and function, we measured stimulus-evoked changes in [Ca(2+)]i at these differentiation durations using the Ca(2+)-responsive dye Fura-2. Increases in [Ca(2+)]i (averages ranging from 65 to 226 nM) were evoked by depolarization, ATP, l-glutamic acid, acetylcholine, and dopamine (up to 87%, 57%, 93%, 28%, and 37% responding cells, respectively) and to a lesser extent by serotonin and gamma-aminobutyric acid (both up to 10% responding cells). Notably, the changes in percentage of responsive cells and their response amplitudes over time indicate changes in the expression and functionality of the respective neurotransmitter receptors and related calcium signaling pathways during in vitro differentiation. The development of functional intercellular signaling pathways was confirmed using multielectrode arrays, demonstrating that mNPCs develop electrical activity within 1-2 weeks of differentiation (55% active wells at 14 days of differentiation; mean spike rate of 1.16 spikes/s/electrode). The combined data demonstrate that mNPCs develop functional neuronal characteristics in vitro, making it a promising model to study chemical-induced effects on the development of neuronal function. PMID:24241723

de Groot, Martje W G D M; Dingemans, Milou M L; Rus, Katinka H; de Groot, Aart; Westerink, Remco H S

2014-02-01

208

In vitro antioxidant and cytotoxic activities of essential oil of Feronia elephantum Correa  

PubMed Central

Objective To analyse the chemical composition and evaluation of antioxidant, cytotoxic and DNA fragmentation activities of essential oil of Feronia elephantum Correa. Methods Chemical composition analysis of hydrodistilled essential oil was determined by gas chromatography-mass spectrometry and in vitro antioxidant activity of oil was determined by DPPH free radical, hydroxyly radical scavenging, metal chelating and prevention of deoxyribose degradation. Cytotoxicity and DNA fragmentation activities against breast cancer cells (MCF-7) were also analyzed. Results Gas chromatography-mass spectrometry analysis revealed the presence of 24 compounds with caryophyllene oxide (62.29%) as major compound. A considerable antioxidant, cyotoxic and DNA fragmentation activities of oils was observed. Conclusions The result of this study clearly indicates oil could be useful for food preservation and preparation. PMID:25182553

Thirugnanasampandan, Ramaraj; David, Delma

2014-01-01

209

Medicinal activities of the leaves of Musa sapientum var. sylvesteris in vitro  

PubMed Central

Objective This study is to investigate the medicinal value of methanolic extract of the leaves of Musa sapientum var. sylvesteris in Bangladesh. Methods Several biochemical assays, thin layer chormatogarphy and ultra-violet spectroscopy were used to detect the presence of various types of compounds in this extract. Antioxidant effects were measured by DPPH scavenging assay, total reducing assay and hydrogen peroxide scavenging assay. Receptor binding activities and hydrogen peroxide induced hemolysis assay were performed by hemagglutination assay and hemolysis assay using erythrocytes. Disk diffusion assay was performed to show the antibacterial effect of the extract. Results Methanolic extract of the leaves showed antioxidant and antibacterial activity in vitro. The extract showed hemaglutination inhibition activities and hydrogen peroxide induced hemolysis inhibition activity of human red blood cells. Conclusion Musa sapientum var. sylvesteris can be an useful medicinal plant. PMID:23730561

Sahaa, Repon Kumer; Acharyaa, Srijan; Shovon, Syed Sohidul Haque; Royb, Priyanka

2013-01-01

210

Molecular analysis of human papillomavirus virus-like particle activated langerhans cells in vitro.  

PubMed

Langerhans cells (LC) are the resident antigen-presenting cells in human epithelium, and are therefore responsible for initiating immune responses against human papillomaviruses (HPV) entering the epithelial and mucosal layers in vivo. Upon proper pathogenic stimulation, LC become activated causing an internal signaling cascade that results in the up-regulation of co-stimulatory molecules and the release of inflammatory cytokines. Activated LC then migrate to lymph nodes where they interact with antigen-specific T cells and initiate an adaptive T-cell response. However, HPV manipulates LC in a suppressive manner that alters these normal maturation responses. Here, in vitro LC activation assays for the detection of phosphorylated signaling intermediates, the up-regulation of activation-associated surface markers, and the release of inflammatory cytokines in response to HPV particles are described. PMID:25348303

Woodham, Andrew W; Raff, Adam B; Da Silva, Diane M; Kast, W Martin

2015-01-01

211

In vitro antiprotozoal and cytotoxic activity of ethnopharmacologically selected guinean plants.  

PubMed

Based on an ethnobotanical survey, 41 Guinean plant species widely used in the traditional treatment of fever and/or malaria were collected. From these, 74 polar and apolar extracts were prepared and tested for their in vitro antiprotozoal activity along with their cytotoxicity on MRC-5 cells. A potent activity (IC50 activity (IC50 8.1?µg/mL) against Leishmania infantum. The selectivity index of the active samples varied from 0.08 to >?100. These results may validate at least in part the traditional use of some of the plant species. PMID:25180493

Traore, Mohammed Sahar; Diane, Sere; Diallo, Mamadou Saliou Telly; Balde, Elhadj Saďdou; Balde, Mamadou Aliou; Camara, Aďssata; Diallo, Abdoulaye; Keita, Abdoulaye; Cos, Paul; Maes, Louis; Pieters, Luc; Balde, Aliou Mamadou

2014-10-01

212

Activities of Z-ajoene against tumour and viral spreading in vitro.  

PubMed

Z-ajoene is a garlic-derived compound with known anti-tumour properties. This report argues in favour of pro-apoptotic and cell cycle blockage activities of Z-ajoene on various cell lines involving activation of the p53-family gene products, p53, p63 and p73, at indicated doses. According to its known anti-proteasome activity, Z-ajoene induced a downregulation of MHC-class I expression at the surface of treated cells but did not impair their recognition by CD8+ T cells. We further demonstrated a new activity of Z-ajoene against human cytomegalovirus spreading in vitro that was mediated by an increased number of apoptotic cells after infection. Altogether our data point at the ubiquitous efficiency of Z-ajoene as a new compound to fight against cancers of various origins including those that put up viruses. PMID:17521297

Terrasson, Jerome; Xu, Bo; Li, Min; Allart, Sophie; Davignon, Jean-Luc; Zhang, Li-he; Wang, Kui; Davrinche, Christian

2007-06-01

213

Studies of the inhibition of serum pseudocholinesterase activity in vitro by commonly used drugs.  

PubMed

We studied the effect of 17 commonly used drugs, including prescription and over-the-counter medications, on the activity of serum pseudocholinesterase (PCE) in vitro. Normal pooled human serum was incubated for 120 minutes at 37 degrees C with therapeutic serum concentrations of prescription and over-the-counter drugs, and the postincubation PCE activity was measured. Morphine, quinidine, and thioridazine depressed PCE activity by more than 5% while no or negligible effect was noted following incubation with acetaminophen, chlordiazepoxide, chlorpromazine, desipramine, doxepin, imipramine, methamphetamine, nortriptyline, phenobarbital, phenytoin, procainamide, salicylic acid, theophylline, and valproic acid. Depression of PCE activity can prolong the half-life of coadministered agents with metabolism mediated by PCE. PMID:16040293

Bailey, David N; Briggs, John R

2005-08-01

214

Expression of porcine protegrin-1 in Pichia pastoris and its anticancer activity in vitro  

PubMed Central

Protegrin-1 (PG-1), a ?-hairpin antimicrobial peptide (AMP), is amongst the shortest AMPs in sequence length while remaining active against a variety of microorganisms. The aim of this study was produce recombinant PG-1 and investigate its anticancer activity. A DNA sequence encoding the mature PG-1, fused with a 6His-tag, was cloned into the pPICZ?-A vector and transformed into Pichia pastoris. Expression was induced following culture for ~96 h with 1% methanol at 28°C, and ~15.6 mg PG-1 was expressed in 100 ml culture medium. Following purification using a Ni-chelating Sepharose column, ~20 mg pure active PG-1 was obtained from 500 ml culture broth supernatant. The expressed PG-1/6His exhibited strong dose- and time-dependent anticancer activity against HepG2 cells in vitro.

NIU, MINGFU; CHAI, SHUMAO; YOU, XIAOYAN; WANG, WENHUI; QIN, CUILI; GONG, QIANG; ZHANG, TINGTING; WAN, PENG

2015-01-01

215

In vitro Antiproliferative Activity of Benzopyranone Derivatives in Comparison with Standard Chemotherapeutic Drugs  

PubMed Central

SUMMARY The cytotoxic activities of five new benzopyranone derivatives containing basic amino side chain are described. Their cytotoxicities against ER (+) MCF-7 and ER (?) MDA-MB-231 human breast cancer cell lines, and Ishikawa human endometrial cell line were determined after 72 h drug exposure employing CellTiter-Glo assay at concentrations ranging from 0.01 – 1.0 × 105 nM. The antiproliferative activities of these compounds were compared to tamoxifen (TAM), 4-hydroxytamoxifen (4-OHT, active metabolite of tamoxifen) and raloxifene (RAL). In vitro results indicated that compounds 9, 10, 12 and 13 were more potent than TAM against the human breast cancer cell lines with IC50 < 20 µM. The in silico structure-activity relationships of these compounds and their binding mode within the estrogen receptor (ER) binding site using AutoDock vina are discussed. PMID:21290426

Musa, Musiliyu A.; Cooperwood, John S.; Khan, M. Omar F.; Rahman, Taufiq

2012-01-01

216

The ruthenium compound KP1339 potentiates the anticancer activity of sorafenib in vitro and in vivo?  

PubMed Central

KP1339 is a promising ruthenium-based anticancer compound in early clinical development. This study aimed to test the effects of KP1339 on the in vitro and in vivo activity of the multi-kinase inhibitor sorafenib, the current standard first-line therapy for advanced hepatoma. Anticancer activity of the parental compounds as compared to the drug combination was tested against a panel of cancer cell lines with a focus on hepatoma. Combination of KP1339 with sorafenib induced in the majority of all cases distinctly synergistic effects, comprising both sorafenib-resistant as well as sorafenib-responsive cell models. Several mechanisms were found to underlie these multifaceted synergistic activities. Firstly, co-exposure induced significantly enhanced accumulation levels of both drugs resulting in enhanced apoptosis induction. Secondly, sorafenib blocked KP1339-mediated activation of P38 signalling representing a protective response against the ruthenium drug. In addition, sorafenib treatment also abrogated KP1339-induced G2/M arrest but resulted in check point-independent DNA-synthesis block and a complete loss of the mitotic cell populations. The activity of the KP1339/sorafenib combination was evaluated in the Hep3B hepatoma xenograft. KP1339 monotherapy led to a 2.4-fold increase in life span and, thus, was superior to sorafenib, which induced a 1.9-fold prolonged survival. The combined therapy further enhanced the mean survival by 3.9-fold. Synergistic activity was also observed in the VM-1 melanoma xenograft harbouring an activating braf mutation. Together, our data indicate that the combination of KP1339 with sorafenib displays promising activity in vitro and in vivo especially against human hepatoma models. PMID:23790465

Heffeter, Petra; Atil, Bihter; Kryeziu, Kushtrim; Groza, Diana; Koellensperger, Gunda; Körner, Wilfried; Jungwirth, Ute; Mohr, Thomas; Keppler, Bernhard K.; Berger, Walter

2013-01-01

217

In vitro activities of amphotericin B deoxycholate and liposomal amphotericin B against 604 clinical yeast isolates  

PubMed Central

We determined the in vitro antifungal activity of liposomal amphotericin B (L-AmB) against 604 clinical yeast isolates. Amphotericin B deoxycholate (D-AmB) was tested in parallel against all the isolates. Susceptibility testing was performed according to the Clinical and Laboratory Standards Institute (CLSI) M27-A3 method. Overall, L-AmB was highly active against the isolates (mean MIC, 0.42 µg ml?1; MIC90, 1 µg ml?1; 97.2?% of MICs were ?1 µg ml?1) and comparable to D-AmB (mean MIC, 0.48 µg ml?1; MIC90, 1 µg ml?1; 97.3?% of MICs were ?1 µg ml?1). The in vitro activity of D-AmB and L-AmB was correlated (R2?=?0.61; exp(b), 2.3; 95?% CI, 2.19–2.44, P<0.001). Candida albicans (mean MICs of D-AmB and L-AmB, 0.39 µg ml?1 and 0.31 µg ml?1, respectively) and Candida parapsilosis (mean MICs of D-AmB and L-AmB, 0.38 µg ml?1 and 0.35 µg ml?1, respectively) were the species most susceptible to the agents tested, while Candida krusei (currently named Issatchenkia orientalis) (mean MICs of D-AmB and L-AmB, 1.27 µg ml?1 and 1.13 µg ml?1, respectively) was the least susceptible. The excellent in vitro activity of L-AmB may have important implications for empirical treatment approaches and support its role in treatment of a wide range of invasive infections due to yeasts. PMID:25210203

Lovero, Grazia; Coretti, Caterina; De Giglio, Osvalda; Martinelli, Domenico; Bedini, Andrea; Delia, Mario; Rosato, Antonio; Codeluppi, Mauro; Caggiano, Giuseppina

2014-01-01

218

In vitro activities of amphotericin B deoxycholate and liposomal amphotericin B against 604 clinical yeast isolates.  

PubMed

We determined the in vitro antifungal activity of liposomal amphotericin B (L-AmB) against 604 clinical yeast isolates. Amphotericin B deoxycholate (D-AmB) was tested in parallel against all the isolates. Susceptibility testing was performed according to the Clinical and Laboratory Standards Institute (CLSI) M27-A3 method. Overall, L-AmB was highly active against the isolates (mean MIC, 0.42 µg ml(-1); MIC90, 1 µg ml(-1); 97.2?% of MICs were ?1 µg ml(-1)) and comparable to D-AmB (mean MIC, 0.48 µg ml(-1); MIC90, 1 µg ml(-1); 97.3?% of MICs were ?1 µg ml(-1)). The in vitro activity of D-AmB and L-AmB was correlated (R(2)?=?0.61; exp(b), 2.3; 95?% CI, 2.19-2.44, P<0.001). Candida albicans (mean MICs of D-AmB and L-AmB, 0.39 µg ml(-1) and 0.31 µg ml(-1), respectively) and Candida parapsilosis (mean MICs of D-AmB and L-AmB, 0.38 µg ml(-1) and 0.35 µg ml(-1), respectively) were the species most susceptible to the agents tested, while Candida krusei (currently named Issatchenkia orientalis) (mean MICs of D-AmB and L-AmB, 1.27 µg ml(-1) and 1.13 µg ml(-1), respectively) was the least susceptible. The excellent in vitro activity of L-AmB may have important implications for empirical treatment approaches and support its role in treatment of a wide range of invasive infections due to yeasts. PMID:25210203

Montagna, Maria Teresa; Lovero, Grazia; Coretti, Caterina; De Giglio, Osvalda; Martinelli, Domenico; Bedini, Andrea; Delia, Mario; Rosato, Antonio; Codeluppi, Mauro; Caggiano, Giuseppina

2014-12-01

219

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

PubMed

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 3?-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. PMID:25219673

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

2015-01-01

220

In vitro Antioxidant and Antibacterial Activities of Methanol Extract of Kyllinga nemoralis  

PubMed Central

The present study was designed to evaluate the antioxidant and antibacterial activity of methanol extract of Kyllinga nemoralis. Six different in vitro antioxidant assays including 2,2-diphenyl-1-picrylhydrazyl, hydroxyl radical, superoxide anion radical, hydrogen peroxide radical, ferric reducing antioxidant power assay and reducing power were carried out to ensure the scavenging effect of the plant on free radicals. In addition, total antioxidant capacity assay, total phenolic contents, tannins, flavonoids and flavonol contents of the plant were also analysed by the standard protocols. Kyllinga nemoralis exhibited high antioxidant activity on 2,2-diphenyl-1-picrylhydrazyl assay (IC50= 90 ?g/ml), superoxide radical scavenging assay (IC50= 180 ?g/ml) and hydrogen peroxide radical scavenging assay (IC50= 200 ?g/ml), compared with standards. These observations provide comprehensible supporting evidence for the antioxidant potential of the plant extract. Reducing power (IC50= 213.16 ?g/ml) and hydroxyl radical scavenging activity (IC50= 223 ?g/ml) of the plant extract was remarkable. The methanol extract of K. nemoralis exhibited significant antimicrobial activity against Gram-positive human pathogenic bacteria. Standard in vitro antioxidant assays assessed the electron donating ability of the plant extract in scavenging free radicals. The inhibitory effect of the plant extract against bacterial pathogens may be due to the presence of phytochemicals. Thus, the results suggest that Kyllinga nemoralis is a potential source of antioxidants and could serve as the base for drug development. PMID:24843192

Sindhu, T.; Rajamanikandan, S.; Srinivasan, P.

2014-01-01

221

Cholecalciferol synthesized after UV-activation of 7-dehydrocholesterol onto titanium implants inhibits osteoclastogenesis in vitro.  

PubMed

UV-activated 7-dehydrocholesterol (7-DHC) has been successfully used as a biocompatible coating for titanium (Ti) implants producing active vitamin D with positive effect on osteoblast differentiation. Since an osseointegrating implant must promote bone formation while delay resorption, here we determine the effect of this coating on the pre-osteoclast cell line RAW 264.7. Moreover, D3 synthesis was optimized by (1) the supplementation with VitE of the 7-DHC coating to reduce 7-DHC oxidation and (2) the addition of an incubation step (48 h at 23°C) after UV-irradiation to favor isomerization. In vitro results with RAW264.7 cells showed no cytotoxic effect of the coatings and a significant decrease of osteoclastogenesis. Indeed, TRAP immunostaining suggested an inhibition of Trap-positive multinucleated cells and the mRNA levels of different phenotypic, fusion, and activity markers were reduced, particularly with 7-DHC:VitE. In conclusion, we demonstrate an improvement of the D3 synthesis from UV-activated 7-DHC when combined with VitE and show that these implants inhibit osteoclastogenesis in vitro. © 2014 Wiley Periodicals, Inc. J Biomed Mater Res Part A, 2014. PMID:25369149

Satué, María; Ramis, Joana M; Monjo, Marta

2014-11-01

222

The Ability to Associate with Activation Domains in vitro is not Required for the TATA Box-Binding Protein to Support Activated Transcription in vivo  

NASA Astrophysics Data System (ADS)

The TATA box-binding protein (TBP) interacts in vitro with the activation domains of many viral and cellular transcription factors and has been proposed to be a direct target for transcriptional activators. We have examined the functional relevance of activator-TBP association in vitro to transcriptional activation in vivo. We show that alanine substitution mutations in a single loop of TBP can disrupt its association in vitro with the activation domains of the herpes simplex virus activator VP16 and of the human tumor suppressor protein p53; these mutations do not, however, disrupt the transcriptional response of TBP to either activation domain in vivo. Moreover, we show that a region of VP16 distinct from its activation domain can also tightly associate with TBP in vitro, but fails to activate transcription in vivo. These data suggest that the ability of TBP to interact with activation domains in vitro is not directly relevant to its ability to support activated transcription in vivo.

Tansey, William P.; Herr, Winship

1995-11-01

223

The ability to associate with activation domains in vitro is not required for the TATA box-binding protein to support activated transcription in vivo.  

PubMed Central

The TATA box-binding protein (TBP) interacts in vitro with the activation domains of many viral and cellular transcription factors and has been proposed to be a direct target for transcriptional activators. We have examined the functional relevance of activator-TBP association in vitro to transcriptional activation in vivo. We show that alanine substitution mutations in a single loop of TBP can disrupt its association in vitro with the activation domains of the herpes simplex virus activator VP16 and of the human tumor suppressor protein p53; these mutations do not, however, disrupt the transcriptional response of TBP to either activation domain in vivo. Moreover, we show that a region of VP16 distinct from its activation domain can also tightly associate with TBP in vitro, but fails to activate transcription in vivo. These data suggest that the ability of TBP to interact with activation domains in vitro is not directly relevant to its ability to support activated transcription in vivo. Images Fig. 1 Fig. 2 Fig. 3 Fig. 4 PMID:7479838

Tansey, W P; Herr, W

1995-01-01

224

Comparison of the Antiviral Activities of Alkoxyalkyl and Alkyl Esters of Cidofovir against Human and Murine Cytomegalovirus Replication In Vitro  

PubMed Central

Alkoxyalkyl esters of cidofovir (CDV) have substantially greater antiviral activity and selectivity than unmodified CDV against herpesviruses and orthopoxviruses in vitro. Enhancement of antiviral activity was also noted when cyclic CDV was esterified with alkoxyalkanols. In vitro antiviral activity of the most active analogs against human cytomegalovirus (HCMV) and orthopoxviruses was increased relative to CDV up to 1,000- or 200-fold, respectively. Alkyl chain length and linker structure are important potential modifiers of antiviral activity and selectivity. In this study, we synthesized a series of alkoxyalkyl esters of CDV or cyclic CDV with alkyl chains from 8 to 24 atoms and having linker moieties of glycerol, propanediol, and ethanediol. We also synthesized alkyl esters of CDV which lack the linker to determine if the alkoxyalkyl linker moiety is required for activity. The new compounds were evaluated in vitro against HCMV and murine CMV (MCMV). CDV or cyclic CDV analogs both with and without linker moieties were highly active against HCMV and MCMV, and their activities were strongly dependent on chain length. The most active compounds had 20 atoms esterified to the phosphonate of CDV. Both alkoxypropyl and alkyl esters of CDV provided enhanced antiviral activities against CMV in vitro. Thus, the oxypropyl linker moiety is not required for enhanced activity. CDV analogs having alkyl ethers linked to glycerol or ethanediol linker groups also demonstrated increased activity against CMV. PMID:15673748

Wan, William B.; Beadle, James R.; Hartline, Caroll; Kern, Earl R.; Ciesla, Stephanie L.; Valiaeva, Nadejda; Hostetler, Karl Y.

2005-01-01

225

Evaluation of the in vitro activity of levornidazole, its metabolites and comparators against clinical anaerobic bacteria.  

PubMed

This study evaluated the in vitro anti-anaerobic activity and spectrum of levornidazole, its metabolites and comparators against 375 clinical isolates of anaerobic bacteria, including Gram-negative bacilli (181 strains), Gram-negative cocci (11 strains), Gram-positive bacilli (139 strains) and Gram-positive cocci (44 strains), covering 34 species. Minimum inhibitory concentrations (MICs) of levornidazole, its five metabolites and three comparators against these anaerobic isolates were determined by the agar dilution method. Minimum bactericidal concentrations (MBCs) of levornidazole and metronidazole were measured against 22 strains of Bacteroides fragilis. Levornidazole showed good activity against B. fragilis, other Bacteroides spp., Clostridium difficile, Clostridium perfringens and Peptostreptococcus magnus, evidenced by MIC90 values of 0.5, 1, 0.25, 2 and 1mg/L, respectively. The activity of levornidazole and the comparators was poor for Veillonella spp. Generally, levornidazole displayed activity similar to or slightly higher than that of metronidazole, ornidazole and dextrornidazole against anaerobic Gram-negative bacilli, Gram-positive bacilli and Gram-positive cocci, especially B. fragilis. Favourable anti-anaerobic activity was also seen with levornidazole metabolites M1 and M4 but not M2, M3 or M5. For the 22 clinical B. fragilis strains, MBC50 and MBC90 values of levornidazole were 2mg/L and 4mg/L, respectively. Both MBC50/MIC50 and MBC90/MIC90 ratios of levornidazole were 4, similar to those of metronidazole. Levornidazole is an important anti-anaerobic option in clinical settings in terms of its potent and broad-spectrum in vitro activity, bactericidal property, and the anti-anaerobic activity of its metabolites M1 and M4. PMID:25301712

Hu, Jiali; Zhang, Jing; Wu, Shi; Zhu, Demei; Huang, Haihui; Chen, Yuancheng; Yang, Yang; Zhang, Yingyuan

2014-12-01

226

Comparison of In Vitro Activities of Camptothecin and Nitidine Derivatives against Fungal and Cancer Cells  

PubMed Central

The activities of a series of camptothecin and nitidine derivatives that might interact with topoisomerase I were compared against yeast and cancer cell lines. Our findings reveal that structural modifications to camptothecin derivatives have profound effects on the topoisomerase I-drug poison complex in cells. Although the water-soluble anticancer agents topotecan and irinotecan are less active than the original structure, camptothecin, other derivatives or analogs with substitutions that increase compound solubility have also increased antifungal activities. In fact, a water-soluble prodrug appears to penetrate into the cell and release its active form; the resulting effect in complex with Cryptococcus neoformans topoisomerase I is a fungicidal response and also potent antitumor activity. Some of the compounds that are not toxic to wild-type yeast cells are extremely toxic to the yeast cells when the C. neoformans topoisomerase I target is overexpressed. With the known antifungal mechanism of a camptothecin-topoisomerase I complex as a cellular poison, these findings indicate that drug entry may be extremely important for antifungal activity. Nitidine chloride exhibits antifungal activity against yeast cells through a mechanism(s) other than topoisomerase I and appears to be less active than camptothecin analogs against tumor cells. Finally, some camptothecin analogs exhibit synergistic antifungal activity against yeast cells in combination with amphotericin B in vitro. Our results suggest that camptothecin and/or nitidine derivatives can exhibit potent antifungal activity and that the activities of camptothecin derivatives with existing antifungal drugs may be synergistic against pathogenic fungi. These new compounds, which exhibit potent antitumor activities, will likely require further structural changes to find more selective activity against fungal versus mammalian cells to hold promise as a new class of antifungal agents. PMID:10582872

Del Poeta, Maurizio; Chen, Shih-Fong; Von Hoff, Daniel; Dykstra, Christine C.; Wani, Mansukh C.; Manikumar, Govindarajan; Heitman, Joseph; Wall, Monroe E.; Perfect, John R.

1999-01-01

227

In Vitro and In Vivo Activity of a Novel Antifungal Small Molecule against Candida Infections  

PubMed Central

Candida is the most common fungal pathogen of humans worldwide and has become a major clinical problem because of the growing number of immunocompromised patients, who are susceptible to infection. Moreover, the number of available antifungals is limited, and antifungal-resistant Candida strains are emerging. New and effective antifungals are therefore urgently needed. Here, we discovered a small molecule with activity against Candida spp. both in vitro and in vivo. We screened a library of 50,240 small molecules for inhibitors of yeast-to-hypha transition, a major virulence attribute of Candida albicans. This screening identified 20 active compounds. Further examination of the in vitro antifungal and anti-biofilm properties of these compounds, using a range of Candida spp., led to the discovery of SM21, a highly potent antifungal molecule (minimum inhibitory concentration (MIC) 0.2 – 1.6 µg/ml). In vitro, SM21 was toxic to fungi but not to various human cell lines or bacterial species and was active against Candida isolates that are resistant to existing antifungal agents. Moreover, SM21 was relatively more effective against biofilms of Candida spp. than the current antifungal agents. In vivo, SM21 prevented the death of mice in a systemic candidiasis model and was also more effective than the common antifungal nystatin at reducing the extent of tongue lesions in a mouse model of oral candidiasis. Propidium iodide uptake assay showed that SM21 affected the integrity of the cell membrane. Taken together, our results indicate that SM21 has the potential to be developed as a novel antifungal agent for clinical use. PMID:24465737

Yuen, Kwok Yong; Wang, Yu; Yang, Dan; Samaranayake, Lakshman Perera

2014-01-01

228

In vitro and in silico antidiabetic activity of pyran ester derivative isolated from Tragia cannabina  

PubMed Central

Objective To investigate the in vitro antidiabetic effects of isolated 4-Oxo-4H-pyran-2,6-dicarboxylic acid bis-[6-methyl-heptyl] ester from the chloroform extract of root of Tragia cannabina (T. cannabina) and AMP kinase activation property of the isolated compound. Methods The roots of T. cannabina were collected and extracted with ethanol [95% v/v] then chromatographed over silica gel 60-120 mesh of column length 100 cm and diameter 3 cm. Elution was carried out with solvents and solvent mixtures of increasing polarities. Then the chloroform extract was used for isolation. In vitro antidiabetic activity was performed with fertile eggs of White Leghorn chicks by induction of diabetes by streptozotocin. Results The isolated pyran ester binds very efficiently within the active pocket of AMPK with the formation of hydrogen bond and consuming less binding energy, which is good when compared to orientation of standard drug metformin. In in vitro antidiabetic evaluation by streptozotocin treated chick embryo the administration of isolated compound at a doses of 0.5 mg/egg and 1 mg/egg produced a significant reduction in the blood glucose levels in a dose dependant manner (P<0.01). The blood glucose level of diabetic control was (244.20±12.64) mg/dL, whereas it was (207.40±2.43) mg/dL (P<0.001) for isolated compound 0.5 mg/egg and 174.800±2.410 mg/dL (P<0.001) for 1 mg/ egg of the isolated compound. Conclusions The significant glucose levels were reduced (P<0.01) after administration of the pyran ester isolated from T. cannabina to streptozotocin treated chick embryo. PMID:25183128

Sivajothi, Vaiyapuri; Dakappa, Shruthi Shirur

2014-01-01

229

In vitro antioxidant activity and effect of Parkia biglobosa bark extract on mitochondrial redox status.  

PubMed

Aqueous-methanolic extract of Parkia biglobosa bark (PBB) was screened for its polyphenolic constituents, in vitro antioxidant activity, and effect on mitochondria redox status. The in vitro antioxidant activity was assessed by using the scavenging abilities and the reducing powers of 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) diammonium salt radical cation against Fe(3+). Subsequently, the ability of PBB to inhibit lipid peroxidation induced by FeSO(4) (10 ?m) and its metal-chelating potential were investigated. The effects of the extract on basal reactive oxygen species (ROS) generation and on the mitochondrial membrane potential (??m) in isolated mitochondria were determined by using 2', 7'-dichlorodihydrofluorescin (DCFH) oxidation and safranin fluorescence, respectively. PBB mitigated the Fe(II)-induced lipid peroxidation in rat tissues and showed dose-dependent scavenging of DPPH (IC(50): 98.33 ± 10.0 ?g/mL) and ABTS. (trolox equivalent antioxidant concentration, TEAC value = 0.05), with considerable ferric-reducing and moderate metal-chelating abilities. PBB caused slight decreases in both the liver and the brain mitochondria potentials and resulted in a significant decrease (p < 0.001) in DCFH oxidation. Screening for polyphenolics using high-performance liquid chromatography coupled to a diode array detector (HPLC-DAD) revealed the presence of caffeic acid, gallic acid, catechin, epigalocatechin, rutin, and quercetin. These results demonstrate for the first time the considerable in vitro antioxidant activity and favorable effect of PBB on mitochondria redox status and provide justification for the use of the plant in ethnomedicine. PMID:25151454

Komolafe, Kayode; Olaleye, Tolulope Mary; Omotuyi, Olaposi Idowu; Boligon, Aline Augusti; Athayde, Margareth Linde; Akindahunsi, Akintunde Afolabi; Teixeira da Rocha, Joao Batista

2014-08-01

230

Characterisation of Fasciola hepatica cytochrome c peroxidase as an enzyme with potential antioxidant activity in vitro.  

PubMed

Cytochrome c peroxidase oxidises hydrogen peroxide using cytochrome c as the electron donor. This enzyme is found in yeast and bacteria and has been also described in the trematodes Fasciola hepatica and Schistosoma mansoni. Using partially purified cytochrome c peroxidase samples from Fasciola hepatica we evaluated its role as an antioxidant enzyme via the investigation of its ability to protect against oxidative damage to deoxyribose in vitro. A system containing FeIII-EDTA plus ascorbate was used to generate reactive oxygen species superoxide radical, H2O2 as well as the hydroxyl radical. Fasciola hepatica cytochrome c peroxidase effectively protected deoxyribose against oxidative damage in the presence of its substrate cytochrome c. This protection was proportional to the amount of enzyme added and occurred only in the presence of cytochrome c. Due to the low specific activity of the final partially purified sample the effects of ascorbate and calcium chloride on cytochrome c peroxidase were investigated. The activity of the partially purified enzyme was found to increase between 10 and 37% upon reduction with ascorbate. However, incubation of the partially purified enzyme with 1 mM calcium chloride did not have any effect on enzyme activity. Our results showed that Fasciola hepatica CcP can protect deoxyribose from oxidative damage in vitro by blocking the formation of the highly toxic hydroxyl radical (.OH). We suggest that the capacity of CcP to inhibit .OH-formation, by efficiently removing H2O2 from the in vitro oxidative system, may extend the biological role of CcP in response to oxidative stress in Fasciola hepatica. PMID:10404259

Campos, E G; Hermes-Lima, M; Smith, J M; Prichard, R K

1999-05-01

231

In vitro and in vivo activity of a novel antifungal small molecule against Candida infections.  

PubMed

Candida is the most common fungal pathogen of humans worldwide and has become a major clinical problem because of the growing number of immunocompromised patients, who are susceptible to infection. Moreover, the number of available antifungals is limited, and antifungal-resistant Candida strains are emerging. New and effective antifungals are therefore urgently needed. Here, we discovered a small molecule with activity against Candida spp. both in vitro and in vivo. We screened a library of 50,240 small molecules for inhibitors of yeast-to-hypha transition, a major virulence attribute of Candida albicans. This screening identified 20 active compounds. Further examination of the in vitro antifungal and anti-biofilm properties of these compounds, using a range of Candida spp., led to the discovery of SM21, a highly potent antifungal molecule (minimum inhibitory concentration (MIC) 0.2-1.6 µg/ml). In vitro, SM21 was toxic to fungi but not to various human cell lines or bacterial species and was active against Candida isolates that are resistant to existing antifungal agents. Moreover, SM21 was relatively more effective against biofilms of Candida spp. than the current antifungal agents. In vivo, SM21 prevented the death of mice in a systemic candidiasis model and was also more effective than the common antifungal nystatin at reducing the extent of tongue lesions in a mouse model of oral candidiasis. Propidium iodide uptake assay showed that SM21 affected the integrity of the cell membrane. Taken together, our results indicate that SM21 has the potential to be developed as a novel antifungal agent for clinical use. PMID:24465737

Wong, Sarah Sze Wah; Kao, Richard Yi Tsun; Yuen, Kwok Yong; Wang, Yu; Yang, Dan; Samaranayake, Lakshman Perera; Seneviratne, Chaminda Jayampath

2014-01-01

232

In vitro antioxidant and H+, K+-ATPase inhibition activities of Acalypha wilkesiana foliage extract  

PubMed Central

Aims: The aim of this study was to evaluate the antioxidant activty and anti-acid property of Acalypha wilkesiana foliage extract. Materials and Methods: Hot and cold aqueous extracts were prepared from healthy leaves of A. wilkesiana. Free radical scavenging activity and H+, K+-ATPase inhibition activities of aqueous foliage extracts was screened by in vitro models. Statistical Analysis Used: All experiments were performed in triplicate and results are expressed as mean ± SEM. Results: A. wilkesiana hot aqueous extract (AWHE) showed significant antioxidants and free radical scavenging activity. Further, AWHE has shown a potent H+, K+-ATPase inhibitory activity (IC50: 51.5 ± 0.28 ?g/ml) when compare to standard proton pump inhibitor omeprazole (56.2 ± 0.64 ?g/ml); however, latter activity is equal to A. wilkesiana cold aqueous extract (AWCE). Quantitative analysis of AWHE has revealed more content of phenols and flavonoids; this is found to be the reason for good antioxidant activity over AWCE. Molecular docking was carried out against H+, K+-ATPase enzyme crystal structure to validate the anti-acid activity of A. wilkesiana major phytochemicals. Conclusions: The present study indicates that the constituents of AWHE and AWCE have good antacid and free radical scavenging activity. PMID:24082698

Prakash Gupta, Rajesh Kashi; Pradeepa; Hanumanthappa, Manjunatha

2013-01-01

233

Radical scavenging activities of Heracleum aquilegifolium Wight (Apiaceae) fruit oils in vitro.  

PubMed

The fruits of Heracleum aquilegifolium Wight (Apiaceae) were collected from Western Ghats of the Indian Peninsula. The essential oils were extracted by hydrodistillation. The chemical composition of the essential oils was analysed by gas chromatography and gas chromatography-mass spectrometry (GC-MS). Beta-Pinene (22.3%), 1,8-cineole (20.3%), and beta-phellandrene (12.4%) were the main components of H. aquilegifolium fruit oils. The antioxidant properties of essential oils of H. aquilegifolium were examined by different procedures namely reducing power ability, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, nitric oxide radical scavenging activity, hydrogen peroxide scavenging activity, hydroxyl radical scavenging activity, superoxide anion scavenging activity, and metal chelating activity. The antioxidant activities were compared with those of synthetic antioxidants and standard drugs such as butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), ascorbic acid, alpha-tocopherol, curcumin, and quercetin. The study confirmed the possible antioxidant potential of essential oils tested with various in vitro antioxidant methods. The presence of monoterpenes in combination with other components in the oils could be responsible for the activity. PMID:21319706

Karuppusamy, Subbiah; Muthuraja, Gurunathan

2010-01-01

234

In Vitro ?-Amylase Inhibition and Antioxidant Activities of Methanolic Extract of Amaranthus Caudatus Linn  

PubMed Central

Objectives The present study was aimed to investigate the ?-amylase inhibition and antioxidant activities of methanolic extract of Amaranthus caudatus Linn (MeAc). Methods Methanolic extract of Amaranthus caudatus was screened for ?-amylase inhibition activity by CNPG3 method (2-chloro-p-nitrophenyl-?-D-maltotrioside) and antioxidant activity was evaluated by 1,1-diphenyl-2-picryl-hydrazile (DPPH) free radical scavenging, superoxide dismutase (SOD) scavenging, hydroxyl free radical scavenging, nitric oxide (NO) radical scavenging, and 2.2’-azinobis-3-ethylbenzothiazole-6-sulfonic acid (ABTS) radical scavenging assays. MeAc was also screened for non enzymatic hemoglycosylation. Results The methanolic extract of Amaranthus caudatus showed potent ?-amylase inhibition activity (IC50 19.233 µg/ml). MeAc showed significant antioxidant activity in all the in vitro antioxidant models. Furthermore, the MeAc was found to be extremely effective in scavenging ABTS radical activity (IC50 48.75±1.1 µg/ml) when compared to DPPH (IC50 77.5±0.4 µg/ml), SOD (IC50 62.5±2.1 µg/ml), hydroxyl (IC50 88.50±1.8 µg/ml) and NO (IC50 67.5±2.2 µg/ml) scavenging activity. Conclusions The methanolic extract of A. caudatus showed potent ?-amylase inhibition and antioxidant activities. PMID:22043408

Kumar, Ashok; Khan, Saleemulla

2011-01-01

235

Effect of neurotransmitters on NADPH-cytochrome P450 reductase in vitro activity.  

PubMed

Three neurotransmitters, namely adrenaline, serotonin and tryptamine inhibit the in vitro activity of several cytochrome P450 (CYP) isozymes (CYP1A2, CYP2C9, CYP2D6 and CYP3A). In order to test whether this effect is related to inhibition of the CYP-coupled NADPH reductase activity, we assayed the potential inhibitory effect of these neurotransmitters and their main metabolites on the NADPH reductase activity. Of the five compounds analyzed: tryptamine, tryptophol, serotonin, 5-hydroxytryptamine and adrenaline, only adrenaline significantly decreased NADPH reductase activity at the fixed concentration of 500 microM. However, the effect became negligible when adrenaline concentration was decreased to 100 microM: whereas a high inhibitory effect was observed in CYP2D6, CYP2C9 and CYP3A4 enzyme activities, the NADPH reductase activity remains unchanged. This study indicates that the effect of these endogenous neurotransmitters on CYP enzymes is not related to changes in the reductase activity. In the light of these findings further studies on the inhibitory effect of these neurotransmitters on CYP enzymes can be designed ruling out the modulation of the coupled NADPH reductase activity as a confounding factor. PMID:19356039

Gervasini, Guillermo; Martinez, Carmen; Benitez, Julio; Agúndez, Jose A G

2007-08-01

236

Synthesis of isatin thiosemicarbazones derivatives: in vitro anti-cancer, DNA binding and cleavage activities.  

PubMed

New derivatives of thiosemicarbazone Schiff base with isatin moiety were synthesized L1-L6. The structures of these compounds were characterized based on the spectroscopic techniques. Compound L6 was further characterized by XRD single crystal. The interaction of these compounds with calf thymus (CT-DNA) exhibited high intrinsic binding constant (k(b)=5.03-33.00×10(5) M(-1)) for L1-L3 and L5 and (6.14-9.47×10(4) M(-1)) for L4 and L6 which reflect intercalative activity of these compounds toward CT-DNA. This result was also confirmed by the viscosity data. The electrophoresis studies reveal the higher cleavage activity of L1-L3 than L4-L6. The in vitro anti-proliferative activity of these compounds against human colon cancer cell line (HCT 116) revealed that the synthesized compounds (L3, L6 and L2) exhibited good anticancer potency. PMID:24607427

Ali, Amna Qasem; Teoh, Siang Guan; Salhin, Abdussalam; Eltayeb, Naser Eltaher; Khadeer Ahamed, Mohamed B; Abdul Majid, A M S

2014-05-01

237

Radiolabeling of intact dosage forms by neutron activation: effects on in vitro performance  

SciTech Connect

Compressed tablets containing various quantities of stable isotopes of Ba, Er, and Sm for use in neutron activation studies were evaluated for the effect of stable isotope incorporation on tablet hardness and disintegration times. At concentrations likely to be used in scintigraphic studies employing neutron activation as a radiolabeling method, no significant effect on in vitro parameters were observed. While the incorporation of stable isotopes influenced tablet hardness to a greater degree than disintegration time, irradiation of tablets in a neutron flux of 4.4 x 10(13) n/cm2 sec had a direct effect on tablet disintegration time. Thus, future neutron activation studies should focus on minimizing the amount of stable isotope to be incorporated with the formulation while using the shortest feasible irradiation time.

Parr, A.; Jay, M.

1987-12-01

238

In vitro evaluation of synergistic activity between ciprofloxacin and broad snouted caiman serum against Escherichia coli.  

PubMed

The in vitro synergistic activity between ciprofloxacin and serum of broad snouted caiman on Escherichia coli was studied. The estimated MIC value of ciprofloxacin was 0.0188?µg/ml, and two assays of kill curve during 5 hours were performed: the first one in a standard culture medium and the second one in the presence of caiman serum. Different concentrations of ciprofloxacin were tested. Ciprofloxacin showed higher values of bacterial elimination rate in the presence of caiman serum in all concentrations tested. The combined activity of sub-inhibitory concentrations of ciprofloxacin and the humoral immune factors present in caiman serum determined an increase in the bacterial elimination observed in this assay. We suggest that the antibacterial activity of complement and natural antibodies present in caiman serum, which can bind to both Gram-negative and Gram-positive bacteria and acting through the classical complement pathway, can inhibit bacterial growth of Escherichia coli by lysis. PMID:25468795

Siroski, P A; Russi, N B; Ortega, H H; Formentini, E A

2015-02-01

239

In Vitro Activity of Moxifloxacin against 923 Anaerobes Isolated from Human Intra-Abdominal Infections  

PubMed Central

The in vitro activity of moxifloxacin against 923 recent anaerobic isolates obtained from pretreatment cultures in patients with complicated intra-abdominal infections was studied using the CLSI M11-A-6 agar dilution method. Moxifloxacin was active against 87% (96 of 110) Bacteroides fragilis strains at ?1 ?g/ml and 87% (79 of 90) B. thetaiotaomicron strains at ?2 ?g/ml. Species variation was seen, with B. uniformis, B. vulgatus, Clostridium clostridioforme, and C. symbiosum being least susceptible and accounting for most of the resistant isolates; excluding the aforementioned four resistant species, 86% (303 of 363) of Bacteroides species isolates and 94% (417 of 450) of all other genera and species were susceptible to ?2 ?g/ml of moxifloxacin. Overall, moxifloxacin was active against 763 of 923 (83%) of strains at ?2 ?g/ml, supporting its use as a monotherapy for some community-acquired intra-abdominal infections. PMID:16377680

Goldstein, Ellie J. C.; Citron, Diane M.; Warren, Yumi A.; Tyrrell, Kerin L.; Merriam, C. Vreni; Fernandez, Helen

2006-01-01

240

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

PubMed

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. PMID:25306376

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

2015-03-01

241

In vitro antimicrobial activity of orbifloxacin against Staphylococcus intermedius isolates from canine skin and ear infections.  

PubMed

The objective of the study was to evaluate the in vitro activity of orbifloxacin against Staphylococcus intermedius strains isolated in France from canine skin and ear infections. The minimum inhibitory concentrations (MICs) of orbifloxacin against 240 field S. intermedius isolates (69 skin and 171 ear isolates) ranged from 0.016 to 8 mg l(-1), with MIC50 and MIC90 equal to 0.5 and 1 mg l(-1), respectively. Only one strain, a pyoderma isolate was resistant (MIC=8 mg l(-1)). Orbifloxacin was tested at different concentrations for killing rate against five isolates obtained from pyoderma cases and against a reference strain (Staphylococcus aureus ATCC 29213). Orbifloxacin expressed a concentration-dependent bactericidal activity against the S. aureus reference strain, but a time-dependent bactericidal activity against S. intermedius. Orbifloxacin induced bactericidal effect against the S. intermedius strains tested with concentrations equal to or two times MIC. PMID:15120955

Ganičre, Jean-Pierre; Médaille, Christine; Etoré, Florence

2004-08-01

242

Synthesis of isatin thiosemicarbazones derivatives: In vitro anti-cancer, DNA binding and cleavage activities  

NASA Astrophysics Data System (ADS)

New derivatives of thiosemicarbazone Schiff base with isatin moiety were synthesized L1-L6. The structures of these compounds were characterized based on the spectroscopic techniques. Compound L6 was further characterized by XRD single crystal. The interaction of these compounds with calf thymus (CT-DNA) exhibited high intrinsic binding constant (kb = 5.03-33.00 × 105 M-1) for L1-L3 and L5 and (6.14-9.47 × 104 M-1) for L4 and L6 which reflect intercalative activity of these compounds toward CT-DNA. This result was also confirmed by the viscosity data. The electrophoresis studies reveal the higher cleavage activity of L1-L3 than L4-L6. The in vitro anti-proliferative activity of these compounds against human colon cancer cell line (HCT 116) revealed that the synthesized compounds (L3, L6 and L2) exhibited good anticancer potency.

Ali, Amna Qasem; Teoh, Siang Guan; Salhin, Abdussalam; Eltayeb, Naser Eltaher; Khadeer Ahamed, Mohamed B.; Majid, A. M. S. Abdul

243

In vitro antiplasmodial, antiamoebic, and cytotoxic activities of a series of bisbenzylisoquinoline alkaloids.  

PubMed Central

Twenty-four bisbenzylisoquinoline alkaloids were screened for antiplasmoidal, antiamoebic, and cytotoxic activities by use of in vitro microtests. Eight of the alkaloids had antiplasmodial activity, with a 50% inhibitory concentration (IC50) of less than 1 microM against a multidrug-resistant strain of Plasmodium falciparum (chloroquine had an IC50 of 0.2 microM). The three alkaloids most active against Entamoeba histolytica, aromoline, isotrilobine, and insularine, had IC50s of 5 to 11.1 microM (metronidazole had an IC50 of 1.87 microM). None of the 24 bisbenzylisoquinoline alkaloids exhibited significant cytotoxicity against the KB cell line, the most toxic being berbamine, with an IC50 of 17.8 microM (the IC50 of podophyllotoxin was 0.008 microM). Bisbenzylisoquinoline alkaloids merit further investigation as potential novel antimalarial agents. PMID:8141587

Marshall, S J; Russell, P F; Wright, C W; Anderson, M M; Phillipson, J D; Kirby, G C; Warhurst, D C; Schiff, P L

1994-01-01

244

In vitro human fecal microbial metabolism of Forsythoside A and biological activities of its metabolites.  

PubMed

The present study aimed to investigate the metabolism of Forsythoside A (FTA) by human fecal bacteria to clarify the relationship between its intestinal metabolism and its pharmacological activities. FTA was incubated with human fecal microflora in vitro to investigate its metabolic process, and highly sensitive and specific ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS) was performed using MetaboLynx software for metabolite analysis. Caffeic acid (CA) and hydroxytyrosol (HT) were obtained by hydrolysis of FTA, and CA was further hydrogenated to form 3,4-dihydroxybenzenepropionic acid (DCA). The anticomplementary, antimicrobial and antiendotoxin activities of FTA and its metabolites by human fecal microflora were evaluated in vitro with a hemolysis assay, the agar disc-diffusion method, the MIC value and the gel clot LAL assay, respectively. The metabolites showed higher biological activity than FTA, especially HT and DCA. Orally administered FTA may be metabolized to HT and DCA, and the pharmacological effects of FTA may be dependent on intestinal bacterial metabolism. PMID:25281775

Xing, Shihua; Peng, Ying; Wang, Mengyue; Chen, Daofeng; Li, Xiaobo

2014-12-01

245

?-noradrenergic receptor activation specifically modulates the generation of sighs in vivo and in vitro  

PubMed Central

The pre-Bötzinger complex (preBötC), an area that is critical for generating breathing (eupnea), gasps and sighs is continuously modulated by catecholamines. These amines and the generation of sighs have also been implicated in the regulation of arousal. Here we studied the catecholaminergic modulation of sighs not only in anesthetized freely breathing mice (in vivo), but also in medullary slice preparations that contain the preBötC and that generate fictive eupneic and sigh rhythms in vitro. We demonstrate that activating ?-noradrenergic receptors (?-NR) specifically increases the frequency of sighs, while eupnea remains unaffected both in vitro and in vivo. ?-NR activation specifically increased the frequency of intrinsically bursting pacemaker neurons that rely on persistent sodium current (INap). By contrast, all parameters of bursting pacemakers that rely on the non-specific cation current (ICAN) remained unaffected. Moreover, riluzole, which blocks bursting in INap pacemakers abolished sighs altogether, while flufenamic acid (FFA) which blocks the ICAN current did not alter the sigh-increasing effect caused by ?-NR. Our results suggest that the selective ?-NR action of sighs may result from the modulation of INap pacemaker activity and that disturbances in noradrenergic system may contribute to abnormal arousal response. The ?-NR action on the preBötC may be an important mechanism in modulating behaviors that are specifically associated with sighs, such as the regulation of the early events leading to the arousal response. PMID:24273495

Viemari, Jean-Charles; Garcia, Alfredo J.; Doi, Atsushi; Elsen, Gina; Ramirez, Jan-Marino

2013-01-01

246

Functional analysis of HPV-like particle-activated Langerhans cells in vitro.  

PubMed

Langerhans cells (LCs) are antigen-presenting cells responsible for initiating an immune response against human papillomaviruses (HPVs) entering the epithelial layer in vivo as they are the first immune cell that HPV comes into contact with. LCs become activated in response to foreign antigens, which causes internal signaling resulting in the increased expression of co-stimulatory molecules and the secretion of inflammatory cytokines. Functionally activated LCs are then capable of migrating to the lymph nodes where they interact with antigen-specific T cells and initiate an adaptive T-cell response in vivo. However, HPV has evolved in a manner that suppresses LC function, and thus the induction of antigen-specific T cells is hindered. While many methods exist to monitor the activity of LCs in vitro, the migration and induction of cytotoxic T cells is ultimately indicative of a functional immune response. Here, methods in analyzing functional migration and induction of antigen-specific T cells after stimulation of LCs with HPV virus-like particles in vitro are described. PMID:25348318

Yan, Lisa; Woodham, Andrew W; Da Silva, Diane M; Kast, W Martin

2015-01-01

247

Bactericidal Activity of Soymilk Fermentation Broth by In Vitro and Animal Models  

PubMed Central

Abstract Soybean fermentation broth (SFB) exhibits potent antibacterial activity against different species of bacteria in in vitro assays and animal models. Four isoflavone compounds—daidzin, genistin, genistein, and daidzein—of SFB were analyzed and quantified by high-performance liquid chromatography. In the in vitro test, daidzin and daidzein had more potent antibacterial activity than genistin. The minimum inhibition concentration values for these bacteria of SFB ranged from 1.25% to 5%, and the minimum bactericidal concentration values of strains ranged from 2.5% to 10%, depending on the species or strain. Vancomycin-resistant Entercoccus faecalis (VRE) strains were also tested for susceptibility to SFB in two species of animal model: the Sprague–Dawley rat and the BALB/c mouse. SFB-fed Sprague–Dawley rats showed excellent elimination efficiency against VRE, close to 99% compared with the phosphate-buffered saline–fed control group. In the BALB/c mouse model, SFB antibacterial activity was 65–80% against VRE compared with the control. In conclusion, SFB contains natural antibacterial substances such as daidzin, genistin, and daidzein that inhibit bacterial growth. PMID:22468646

Chin, Yi-Ping; Tsui, Ko-Chung; Chen, Mei-Chieh; Wang, Cheng-Yi; Yang, Chin-Yuh

2012-01-01

248

Bactericidal activity of soymilk fermentation broth by in vitro and animal models.  

PubMed

Soybean fermentation broth (SFB) exhibits potent antibacterial activity against different species of bacteria in in vitro assays and animal models. Four isoflavone compounds-daidzin, genistin, genistein, and daidzein-of SFB were analyzed and quantified by high-performance liquid chromatography. In the in vitro test, daidzin and daidzein had more potent antibacterial activity than genistin. The minimum inhibition concentration values for these bacteria of SFB ranged from 1.25% to 5%, and the minimum bactericidal concentration values of strains ranged from 2.5% to 10%, depending on the species or strain. Vancomycin-resistant Entercoccus faecalis (VRE) strains were also tested for susceptibility to SFB in two species of animal model: the Sprague-Dawley rat and the BALB/c mouse. SFB-fed Sprague-Dawley rats showed excellent elimination efficiency against VRE, close to 99% compared with the phosphate-buffered saline-fed control group. In the BALB/c mouse model, SFB antibacterial activity was 65-80% against VRE compared with the control. In conclusion, SFB contains natural antibacterial substances such as daidzin, genistin, and daidzein that inhibit bacterial growth. PMID:22468646

Chin, Yi-Ping; Tsui, Ko-Chung; Chen, Mei-Chieh; Wang, Cheng-Yi; Yang, Chin-Yuh; Lin, Yuh-Ling

2012-06-01

249

Bluetongue Virus VP1 Polymerase Activity In Vitro: Template Dependency, Dinucleotide Priming and Cap Dependency  

PubMed Central

Background Bluetongue virus (BTV) protein, VP1, is known to possess an intrinsic polymerase function, unlike rotavirus VP1, which requires the capsid protein VP2 for its catalytic activity. However, compared with the polymerases of other members of the Reoviridae family, BTV VP1 has not been characterized in detail. Methods and Findings Using an in vitro polymerase assay system, we demonstrated that BTV VP1 could synthesize the ten dsRNAs simultaneously from BTV core-derived ssRNA templates in a single in vitro reaction as well as genomic dsRNA segments from rotavirus core-derived ssRNA templates that possess no sequence similarity with BTV. In contrast, dsRNAs were not synthesized from non-viral ssRNA templates by VP1, unless they were fused with specific BTV sequences. Further, we showed that synthesis of dsRNAs from capped ssRNA templates was significantly higher than that from uncapped ssRNA templates and the addition of dinucleotides enhanced activity as long as the last base of the dinucleotide complemented the 3? -terminal nucleotide of the ssRNA template. Conclusions We showed that the polymerase activity was stimulated by two different factors: cap structure, likely due to allosteric effect, and dinucleotides due to priming. Our results also suggested the possible presence of cis-acting elements shared by ssRNAs in the members of family Reoviridae. PMID:22110731

Matsuo, Eiko; Roy, Polly

2011-01-01

250

Epithelial Cells as Active Player In Fibrosis: Findings from an In Vitro Model  

PubMed Central

Kidney fibrosis, a scarring of the tubulo-interstitial space, is due to activation of interstitial myofibroblasts recruited locally or systemically with consecutive extracellular matrix deposition. Newly published clinical studies correlating acute kidney injury (AKI) to chronic kidney disease (CKD) challenge this pathological concept putting tubular epithelial cells into the spotlight. In this work we investigated the role of epithelial cells in fibrosis using a simple controlled in vitro system. An epithelial/mesenchymal 3D cell culture model composed of human proximal renal tubular cells and fibroblasts was challenged with toxic doses of Cisplatin, thus injuring epithelial cells. RT-PCR for classical fibrotic markers was performed on fibroblasts to assess their modulation toward an activated myofibroblast phenotype in presence or absence of that stimulus. Epithelial cell lesion triggered a phenotypical modulation of fibroblasts toward activated myofibroblasts as assessed by main fibrotic marker analysis. Uninjured 3D cell culture as well as fibroblasts alone treated with toxic stimulus in the absence of epithelial cells were used as control. Our results, with the caveats due to the limited, but highly controllable and reproducible in vitro approach, suggest that epithelial cells can control and regulate fibroblast phenotype. Therefore they emerge as relevant target cells for the development of new preventive anti-fibrotic therapeutic approaches. PMID:23457584

Moll, Solange; Ebeling, Martin; Weibel, Franziska; Farina, Annarita; Araujo Del Rosario, Andrea; Hoflack, Jean Christophe; Pomposiello, Silvia; Prunotto, Marco

2013-01-01

251

New formula herbal pellets demonstrate a uniform and stable release of the active ingredients in vitro.  

PubMed

The aim of this study was to evaluate the effect of different capsule filling manufacturing techniques and storage conditions on the release of the active ingredients from herbal capsules during the dissolution test in vitro. Different techniques for the preparation of the original mixture of dry extracts were applied, and subsequently capsules with six different fillings were prepared. The stability of the capsules was evaluated in different long-term storage conditions, registering changes in the water content (loss of drying), capsule disintegration time, and phenolic compounds dissolution test in vitro. The baseline of phenolic compounds release in the control capsules (filled with the mixture of the powder of dry herbal extracts) was the highest, compared to other capsule groups, yet during long-term storage, these capsules accumulated too much moisture, which impeded capsule disintegration time and phenolic compounds release. The study showed that moisture and temperature changes occurring during the storage of the preparation had a negative effect on the release of phenolic compounds from herbal capsules. Capsules filled with pellets demonstrated a uniform and stable release of the active ingredients in different long-term storage conditions, which indicates that the manufacturing technology of dry herbal extracts affects the stability of the active ingredients. PMID:23923396

Pranskuniene, Zivile; Bernatoniene, Jurga; Kalveniene, Zenona; Masteikova, Ruta; Mekas, Tauras; Velziene, Saule; Ivanauskas, Kostas; Suchockas, Vytautas; Mintauckiene, Inesa; Savickas, Arunas

2013-01-01

252

In vitro and in vivo immunomodulatory activity of sulfated polysaccharides from Enteromorpha prolifera.  

PubMed

Water-soluble sulfated polysaccharides extracted from Enteromorpha prolifera and fractionated using ion-exchange chromatography (crude, F(1), F(2) and F(3) fractions) were investigated to determine their in vitro and in vivo immunomodulatory activities. The sulfated polysaccharides, especially the F(1) and F(2) fractions, stimulated a macrophage cell line, Raw 264.7, inducing considerable nitric oxide (NO) and various cytokine production via up-regulated mRNA expression. The in vivo experiment results show that the sulfated polysaccharides (the crude and F(2) fractions) significantly increased Con A-induced splenocyte proliferation, revealing their potential comitogenic activity. In addition, IFN-? and IL-2 secretions were considerably increased by the F(2) fraction without altering the release of IL-4 and IL-5. This implies that the F(2) fraction can activate T cells by up-regulating Th-1 response and that Th-1 cells might be the main target cells of the F(2) fraction. These in vitro and in vivo results suggest that the sulfated polysaccharides are strong immunostimulators. PMID:21907732

Kim, Jin-Kyung; Cho, Myoung Lae; Karnjanapratum, Supatra; Shin, Il-Shik; You, Sang Guan

2011-12-01

253

Alkali extraction and in vitro antioxidant activity of Monascus mycelium polysaccharides.  

PubMed

In the present work, alkali extraction technology was used to optimize the extraction of Monascus mycelium polysaccharides for the first time. The extracting parameters of alkali extracted Monascus mycelium polysaccharides were optimized by Box-Behnken design (BBD). The optimum conditions were extraction temperature 49 °C, alkali concentration 7%, solvent/material ratio 23:1 (ml/g) and extraction time 2.3 h with an enhanced yield of 10.1%, compared with the yield 4.76% of hot water extraction, indicating that alkali extraction is a more efficient way. In order to discuss the biological activity of alkali extracted polysaccharides, we compared the in vitro antioxidant activity of alkali extracted polysaccharides (AMP) with hot water extracted polysaccharides (HMP). The result showed that AMP have the similar capability of scavenging both superoxide radical and 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical of HMP in vitro. Therefore, alkali extraction technology is not only a high-efficiency way to extract AMP, but also can retain the natural antioxidant activities of AMP, which can be used in pharmaceutical and food industries. PMID:24966417

Wang, Pengrong; Chen, Danfeng; Jiang, Donghua; Dong, Xiameng; Chen, Panpan; Lin, Yaoxue

2014-07-01

254

Polyoxygenated Steroids from the Octocoral Leptogorgia punicea and in Vitro Evaluation of Their Cytotoxic Activity  

PubMed Central

Five new polyoxygenated marine steroids—punicinols A–E (1–5)—were isolated from the gorgonian Leptogorgia punicea and characterized by spectroscopic methods (IR, MS, 1H, 13C and 2-D NMR). The five compounds induced in vitro cytotoxic effects against lung cancer A549 cells, while punicinols A and B were the most active, with IC50 values of 9.7 ?M and 9.6 ?M, respectively. The synergistic effects of these compounds with paclitaxel, as well as their effects on cell cycle distribution and their performance in the clonogenic assay, were also evaluated. Both compounds demonstrated significant synergistic effects with paclitaxel. PMID:25486111

Moritz, Maria Izabel G.; Marostica, Lucas Lourenço; Bianco, Éverson M.; Almeida, Maria Tereza R.; Carraro, Joăo L.; Cabrera, Gabriela M.; Palermo, Jorge A.; Simőes, Cláudia M. O.; Schenkel, Eloir P.

2014-01-01

255

Polyoxygenated Steroids from the Octocoral Leptogorgia punicea and in Vitro Evaluation of Their Cytotoxic Activity.  

PubMed

Five new polyoxygenated marine steroids-punicinols A-E (1-5)-were isolated from the gorgonian Leptogorgia punicea and characterized by spectroscopic methods (IR, MS, 1H, 13C and 2-D NMR). The five compounds induced in vitro cytotoxic effects against lung cancer A549 cells, while punicinols A and B were the most active, with IC50 values of 9.7 ?M and 9.6 ?M, respectively. The synergistic effects of these compounds with paclitaxel, as well as their effects on cell cycle distribution and their performance in the clonogenic assay, were also evaluated. Both compounds demonstrated significant synergistic effects with paclitaxel. PMID:25486111

Moritz, Maria Izabel G; Marostica, Lucas Lourenço; Bianco, Everson M; Almeida, Maria Tereza R; Carraro, Joăo L; Cabrera, Gabriela M; Palermo, Jorge A; Simőes, Cláudia M O; Schenkel, Eloir P

2014-12-01

256

Chemical composition and possible in vitro phytotoxic activity of Helichrsyum italicum (Roth) Don ssp. italicum.  

PubMed

The chemical composition of the essential oil of Helichrysum italicum (Roth) Don ssp. italicum, collected in the National Park of Cilento and Diano Valley, Southern Italy, was studied by means of GC and GC/MS. Forty four compounds of 45 constituents were identified in the oil, mainly oxygenated sesquiterpenes. The essential oil was evaluated for its potential in vitro phytotoxic activity against germination and early radicle elongation of radish and garden cress. The radicle elongation of radish was significantly inhibited at the highest doses tested, while germination of both seeds was not affected. PMID:21904272

Mancini, Emilia; De Martino, Laura; Marandino, Aurelio; Scognamiglio, Maria Rosa; De Feo, Vincenzo

2011-01-01

257

In vitro synergistic activity between bismuth subcitrate and various antimicrobial agents against Campylobacter pyloridis (C. pylori).  

PubMed Central

The in vitro interactions between bismuth subcitrate and a variety of antimicrobial agents against 12 Campylobacter pyloridis (C. pylori) isolates were studied by the agar dilution checkerboard technique. The combination of bismuth subcitrate with the older quinolone, oxolinic acid, produced synergistic activity against all strains. This observation, however, could not be extended to the (aryl) fluoroquinolones, norfloxacin, ofloxacin, and difloxacin, since synergy was rare or absent when bismuth subcitrate was combined with these antibiotics. Among the other antimicrobial agents tested, rifampin and the beta-lactams frequently showed showed MICs for C. pyloridis similar to those of bismuth subcitrate. PMID:3674850

Van Caekenberghe, D L; Breyssens, J

1987-01-01

258

[In vitro study of the cytotoxic activity of sipunculid leukocytes towards allogeneic and xenogenic erythrocytes].  

PubMed

A cell mediated cytotoxic reaction analogous to that known in Vertebrates is induced in vitro by leukocytes of sipunculid worms (coelomata invertebrates). Xenogenic or allogenic erythrocytes are employed as target cells. A cytotoxic effect always occurs when killer leukocytes react against xenogenic cells. A cytotoxic activity against allogenic erythrocytes occurs in all cases when donors of leukocytes and donors of erythrocytes arise from stations far apart (Roscoff and Arcachon). Between stations near each other (4 miles apart) a cytotoxic effect is noticed only in one case out of three. No reaction is noticed between Sipunculus nudus from the same station. PMID:825267

Boiledieu, D; Valembois, P

1976-07-19

259

Ceruminal diffusion activities and ceruminolytic characteristics of otic preparations – an in-vitro study  

PubMed Central

Background An in-vitro setup was established in order to determine a) the diffusion activities of eight otic preparations (Aurizon®, Eas Otic®, Epi Otic®, Otifree®, Otomax®, Panolog®, Posatex®, Surolan®) through synthetic cerumen, and b) the ceruminolytic capacity and impregnation effects of these products. The main lipid classes of canine cerumen produced with moderate, non-purulent otitis externa were determined by thin layer chromatography and were subsequently used to produce a standardised synthetic cerumen (SCC). SCC was filled into capillary tubes, all of which were loaded with six commercially available multipurpose otic medications and two ear cleaners, each mixed with two markers in two experimental setups. These two marker compounds (Oil red O and marbofloxacin) were chosen, since they exhibit different physicochemical drug characteristics by which it is possible to determine and verify the diffusion activity of different types of liquids (i.e. the otic preparations). A synthetic cerumen described in the literature (JSL) was also used for comparison as its lipid composition was different to SCC. The diffusion activities of the otic preparations through both types of synthetic cerumen were studied over 24 hours. A second in-vitro experiment determined both the ceruminolytic activity and impregnation effect of the otic preparations by comparing the weight loss or weight gain after repeated incubation of JSL. Results Canine cerumen is mainly composed of triglycerides, sterol esters, fatty acid esters and squalene. The diffusion experiments showed a high diffusion efficacy along with a high impregnation effect for one test product. All the other products exhibited a lower diffusion activity with a mild to moderate impregnation effect. A mild ceruminolytic activity was observed for the two ear cleaners but not for any of the otic medications. Conclusions The present study demonstrates that there are significant differences in the diffusion characteristics and ceruminolytic properties of the eight tested otic preparations. PMID:23574753

2013-01-01

260

In Vitro and In Vivo Antibacterial Activities of Omadacycline, a Novel Aminomethylcycline  

PubMed Central

Omadacycline is the first intravenous and oral 9-aminomethylcycline in clinical development for use against multiple infectious diseases including acute bacterial skin and skin structure infections (ABSSSI), community-acquired bacterial pneumonia (CABP), and urinary tract infections (UTI). The comparative in vitro activity of omadacycline was determined against a broad panel of Gram-positive clinical isolates, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE), Lancefield groups A and B beta-hemolytic streptococci, penicillin-resistant Streptococcus pneumoniae (PRSP), and Haemophilus influenzae (H. influenzae). The omadacycline MIC90s for MRSA, VRE, and beta-hemolytic streptococci were 1.0 ?g/ml, 0.25 ?g/ml, and 0.5 ?g/ml, respectively, and the omadacycline MIC90s for PRSP and H. influenzae were 0.25 ?g/ml and 2.0 ?g/ml, respectively. Omadacycline was active against organisms demonstrating the two major mechanisms of resistance, ribosomal protection and active tetracycline efflux. In vivo efficacy of omadacycline was demonstrated using an intraperitoneal infection model in mice. A single intravenous dose of omadacycline exhibited efficacy against Streptococcus pneumoniae, Escherichia coli, and Staphylococcus aureus, including tet(M) and tet(K) efflux-containing strains and MRSA strains. The 50% effective doses (ED50s) for Streptococcus pneumoniae obtained ranged from 0.45 mg/kg to 3.39 mg/kg, the ED50s for Staphylococcus aureus obtained ranged from 0.30 mg/kg to 1.74 mg/kg, and the ED50 for Escherichia coli was 2.02 mg/kg. These results demonstrate potent in vivo efficacy including activity against strains containing common resistance determinants. Omadacycline demonstrated in vitro activity against a broad range of Gram-positive and select Gram-negative pathogens, including resistance determinant-containing strains, and this activity translated to potent efficacy in vivo. PMID:24295985

Macone, A. B.; Caruso, B. K.; Leahy, R. G.; Donatelli, J.; Weir, S.; Draper, M. P.; Levy, S. B.

2014-01-01

261

In vitro and in vivo antibacterial activities of omadacycline, a novel aminomethylcycline.  

PubMed

Omadacycline is the first intravenous and oral 9-aminomethylcycline in clinical development for use against multiple infectious diseases including acute bacterial skin and skin structure infections (ABSSSI), community-acquired bacterial pneumonia (CABP), and urinary tract infections (UTI). The comparative in vitro activity of omadacycline was determined against a broad panel of Gram-positive clinical isolates, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE), Lancefield groups A and B beta-hemolytic streptococci, penicillin-resistant Streptococcus pneumoniae (PRSP), and Haemophilus influenzae (H. influenzae). The omadacycline MIC90s for MRSA, VRE, and beta-hemolytic streptococci were 1.0 ?g/ml, 0.25 ?g/ml, and 0.5 ?g/ml, respectively, and the omadacycline MIC90s for PRSP and H. influenzae were 0.25 ?g/ml and 2.0 ?g/ml, respectively. Omadacycline was active against organisms demonstrating the two major mechanisms of resistance, ribosomal protection and active tetracycline efflux. In vivo efficacy of omadacycline was demonstrated using an intraperitoneal infection model in mice. A single intravenous dose of omadacycline exhibited efficacy against Streptococcus pneumoniae, Escherichia coli, and Staphylococcus aureus, including tet(M) and tet(K) efflux-containing strains and MRSA strains. The 50% effective doses (ED50s) for Streptococcus pneumoniae obtained ranged from 0.45 mg/kg to 3.39 mg/kg, the ED50s for Staphylococcus aureus obtained ranged from 0.30 mg/kg to 1.74 mg/kg, and the ED50 for Escherichia coli was 2.02 mg/kg. These results demonstrate potent in vivo efficacy including activity against strains containing common resistance determinants. Omadacycline demonstrated in vitro activity against a broad range of Gram-positive and select Gram-negative pathogens, including resistance determinant-containing strains, and this activity translated to potent efficacy in vivo. PMID:24295985

Macone, A B; Caruso, B K; Leahy, R G; Donatelli, J; Weir, S; Draper, M P; Tanaka, S K; Levy, S B

2014-01-01

262

14-3-3 Facilitates Ras-Dependent Raf-1 Activation In Vitro and In Vivo  

PubMed Central

14-3-3 proteins complex with many signaling molecules, including the Raf-1 kinase. However, the role of 14-3-3 in regulating Raf-1 activity is unclear. We show here that 14-3-3 is bound to Raf-1 in the cytosol but is totally displaced when Raf-1 is recruited to the plasma membrane by oncogenic mutant Ras, in vitro and in vivo. 14-3-3 is also displaced when Raf-1 is targeted to the plasma membrane. When serum-starved cells are stimulated with epidermal growth factor, some recruitment of 14-3-3 to the plasma membrane is evident, but 14-3-3 recruitment correlates with Raf-1 dissociation and inactivation, not with Raf-1 recruitment. In vivo, overexpression of 14-3-3 potentiates the specific activity of membrane-recruited Raf-1 without stably associating with the plasma membrane. In vitro, Raf-1 must be complexed with 14-3-3 for efficient recruitment and activation by oncogenic Ras. Recombinant 14-3-3 facilitates Raf-1 activation by membranes containing oncogenic Ras but reduces the amount of Raf-1 that associates with the membranes. These data demonstrate that the interaction of 14-3-3 with Raf-1 is permissive for recruitment and activation by Ras, that 14-3-3 is displaced upon membrane recruitment, and that 14-3-3 may recycle Raf-1 to the cytosol. A model that rationalizes many of the apparently discrepant observations on the role of 14-3-3 in Raf-1 activation is proposed. PMID:9632779

Roy, Sandrine; McPherson, Robert A.; Apolloni, Ann; Yan, Jun; Lane, Annette; Clyde-Smith, Jodi; Hancock, John F.

1998-01-01

263

Comparison of in vitro activities of meropenem productions on Klebsiella pneumoniae isolated from hospitalized patients  

PubMed Central

Purpose: Antimicrobial activities of meropenem products on Klebsiella pneumoniae isolates were determined. Methods: 212 non-duplicated Klebsiella pneumoniae isolates were examined for in vitro meropenem susceptibility test by using the following disks, which were made from Meronem (AstraZeneca, UK), Exipenem (Exir, Iran) and Meroxan (DAANA, Iran) powders. MIC50 and MIC90 for meropenem antibiotics were determined. Results: Meronem had good activities against most isolates of Klebsiella pneumoniae, and only a few strains had a rather high MIC. Exipenem and Meroxan showed a similar activity with Meronem. Conclusion: Regarding the comparison of two internal generic meropenem products with the external Meronem product have shown that they are equivalents in terms of microbiological activity, as measured using the disk diffusion and MIC. In developing countries, we suggested preparing disks with antibiotic powders that can be an equivalent function in microbiological activity with standard disks. In addition, since it demonstrated significant antimicrobial activity against the Klebsiella pneumoniae. For use of Exipenem and Meroxan in vivo, it would be better to perform additional testing (activity against different species, stability etc.). PMID:25152857

Akhi, Mohammad Taghi; Asghari, Babak; Nahaei, Mohammed Reza; Memar, Mohammad Yousef; Lari, Abdolaziz Rastegar; Naghili, Behrooz; Pirzadeh, Tahereh

2014-01-01

264

Influence of pulmonary surfactant on in vitro bactericidal activities of amoxicillin, ceftazidime, and tobramycin.  

PubMed Central

The influence of a natural pulmonary surfactant on antibiotic activity was investigated to assess the possible use of exogenous surfactant as a vehicle for antibiotic delivery to the lung. The influence of surfactant on the bactericidal activity of amoxicillin was tested against Staphylococcus aureus and Streptococcus pneumoniae, and the influence of surfactant on the activities of ceftazidime and tobramycin was tested against Klebsiella pneumoniae, Pseudomonas aeruginosa, S. aureus, and S. pneumoniae. In vitro antibiotic activity was determined by killing curve studies in media with and without surfactant. Amoxicillin and ceftazidime activities were not changed in the presence of surfactant, except for a decreased killing rate of S. pneumoniae by ceftazidime in medium with additional rabbit serum. In contrast, killing curves with low concentrations of tobramycin (0.25x and 1x the MIC) showed a decreased level of activity of tobramycin against all pathogens tested in the presence of surfactant. With higher tobramycin concentrations (4x the MIC) killing rates were decreased less or were unchanged in the presence of surfactant. Concluding from the results of the study, both amoxicillin and ceftazidime can be combined with surfactant without the loss of activity. For mixing surfactant with tobramycin, dosages should be adjusted to overcome the partial inactivation of tobramycin by surfactant. PMID:7726491

van 't Veen, A; Mouton, J W; Gommers, D; Kluytmans, J A; Dekkers, P; Lachmann, B

1995-01-01

265

Uridine 5?-Triphosphate Promotes In Vitro Schwannoma Cell Migration through Matrix Metalloproteinase-2 Activation  

PubMed Central

In response to peripheral nerve injury, Schwann cells adopt a migratory phenotype and modify the extracellular matrix to make it permissive for cell migration and axonal re-growth. Uridine 5?-triphosphate (UTP) and other nucleotides are released during nerve injury and activate purinergic receptors expressed on the Schwann cell surface, but little is known about the involvement of purine signalling in wound healing. We studied the effect of UTP on Schwannoma cell migration and wound closure and the intracellular signaling pathways involved. We found that UTP treatment induced Schwannoma cell migration through activation of P2Y2 receptors and through the increase of extracellular matrix metalloproteinase-2 (MMP-2) activation and expression. Knockdown P2Y2 receptor or MMP-2 expression greatly reduced wound closure and MMP-2 activation induced by UTP. MMP-2 activation evoked by injury or UTP was also mediated by phosphorylation of all 3 major mitogen-activated protein kinases (MAPKs): JNK, ERK1/2, and p38. Inhibition of these MAPK pathways decreased both MMP-2 activation and cell migration. Interestingly, MAPK phosphorylation evoked by UTP exhibited a biphasic pattern, with an early transient phosphorylation 5 min after treatment, and a late and sustained phosphorylation that appeared at 6 h and lasted up to 24 h. Inhibition of MMP-2 activity selectively blocked the late, but not the transient, phase of MAPK activation. These results suggest that MMP-2 activation and late MAPK phosphorylation are part of a positive feedback mechanism to maintain the migratory phenotype for wound healing. In conclusion, our findings show that treatment with UTP stimulates in vitro Schwannoma cell migration and wound repair through a MMP-2-dependent mechanism via P2Y2 receptors and MAPK pathway activation. PMID:24905332

Martiańez, Tania; Segura, Mňnica; Figueiro-Silva, Joana; Grijota-Martinez, Carmen; Trullas, Ramón; Casals, Núria

2014-01-01

266

In vitro and in vivo activities of pterostilbene against Candida albicans biofilms.  

PubMed

Pterostilbene (PTE) is a stilbene-derived phytoalexin that originates from several natural plant sources. In this study, we evaluated the activity of PTE against Candida albicans biofilms and explored the underlying mechanisms. In 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) reduction assays, biofilm biomass measurement, confocal laser scanning microscopy, and scanning electron microscopy, we found that ?16 ?g/ml PTE had a significant effect against C. albicans biofilms in vitro, while it had no fungicidal effect on planktonic C. albicans cells, which suggested a unique antibiofilm effect of PTE. Then we found that PTE could inhibit biofilm formation and destroy the maintenance of mature biofilms. At 4 ?g/ml, PTE decreased cellular surface hydrophobicity (CSH) and suppressed hyphal formation. Gene expression microarrays and real-time reverse transcription-PCR showed that exposure of C. albicans to 16 ?g/ml PTE altered the expression of genes that function in morphological transition, ergosterol biosynthesis, oxidoreductase activity, and cell surface and protein unfolding processes (heat shock proteins). Filamentation-related genes, especially those regulated by the Ras/cyclic AMP (cAMP) pathway, including ECE1, ALS3, HWP1, HGC1, and RAS1 itself, were downregulated upon PTE treatment, indicating that the antibiofilm effect of PTE was related to the Ras/cAMP pathway. Then, we found that the addition of exogenous cAMP reverted the PTE-induced filamentous growth defect. Finally, with a rat central venous catheter infection model, we confirmed the in vivo activity of PTE against C. albicans biofilms. Collectively, PTE had strong activities against C. albicans biofilms both in vitro and in vivo, and these activities were associated with the Ras/cAMP pathway. PMID:24514088

Li, De-Dong; Zhao, Lan-Xue; Mylonakis, Eleftherios; Hu, Gan-Hai; Zou, Yong; Huang, Tong-Kun; Yan, Lan; Wang, Yan; Jiang, Yuan-Ying

2014-01-01

267

In Vitro and In Vivo Activities of Pterostilbene against Candida albicans Biofilms  

PubMed Central

Pterostilbene (PTE) is a stilbene-derived phytoalexin that originates from several natural plant sources. In this study, we evaluated the activity of PTE against Candida albicans biofilms and explored the underlying mechanisms. In 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) reduction assays, biofilm biomass measurement, confocal laser scanning microscopy, and scanning electron microscopy, we found that ?16 ?g/ml PTE had a significant effect against C. albicans biofilms in vitro, while it had no fungicidal effect on planktonic C. albicans cells, which suggested a unique antibiofilm effect of PTE. Then we found that PTE could inhibit biofilm formation and destroy the maintenance of mature biofilms. At 4 ?g/ml, PTE decreased cellular surface hydrophobicity (CSH) and suppressed hyphal formation. Gene expression microarrays and real-time reverse transcription-PCR showed that exposure of C. albicans to 16 ?g/ml PTE altered the expression of genes that function in morphological transition, ergosterol biosynthesis, oxidoreductase activity, and cell surface and protein unfolding processes (heat shock proteins). Filamentation-related genes, especially those regulated by the Ras/cyclic AMP (cAMP) pathway, including ECE1, ALS3, HWP1, HGC1, and RAS1 itself, were downregulated upon PTE treatment, indicating that the antibiofilm effect of PTE was related to the Ras/cAMP pathway. Then, we found that the addition of exogenous cAMP reverted the PTE-induced filamentous growth defect. Finally, with a rat central venous catheter infection model, we confirmed the in vivo activity of PTE against C. albicans biofilms. Collectively, PTE had strong activities against C. albicans biofilms both in vitro and in vivo, and these activities were associated with the Ras/cAMP pathway. PMID:24514088

Li, De-Dong; Zhao, Lan-Xue; Mylonakis, Eleftherios; Hu, Gan-Hai; Zou, Yong; Huang, Tong-Kun; Yan, Lan

2014-01-01

268

In vitro activity of cefquinome, a new cephalosporin, compared with other cephalosporin antibiotics.  

PubMed

The in vitro activity of cefquinome, a new aminothiazolyl cephalosporin with a C-3 bicyclic pyridinium group, was compared with ceftazidime, cefpirome, and cefepime. Cefquinome inhibited members of the Enterobacteriaceae at less than or equal to 0.5 microgram/ml for Escherichia coli, Klebsiella pneumoniae, K. oxytoca, Citrobacter diversus, Salmonella Shigella, Proteus mirabilis, Morganella, and Providencia. Although most Citrobacter freundii and Enterobacter cloacae were inhibited by less than 2 micrograms/ml, some strains resistant to ceftazidime were resistant, [minimum inhibitory concentration (MIC) greater than 16 micrograms/ml]. Serratia marcescens were inhibited by less than 1 microgram/ml and Pseudomonas aeruginosa by 8 micrograms/ml similar to the activity of cefepime. The majority of Haemophilus influenzae and Neisseria gonorrhoeae were inhibited by less than 0.25 microgram/ml. Most enterococci had cefquinome MICs of 4-8 micrograms/ml. Cefquinome was extremely active against group-A streptococci and Streptococcus pneumoniae with MICs less than 0.12 microgram/ml. 90% of methicillin-susceptible Staphylococcus aureus 90% were inhibited by 2 micrograms/ml. Overall, the in vitro activity of cefquinome was comparable with aminothiazolyl cephalosporins. It inhibited some Enterobacter and Citrobacter freundii resistant to ceftazidime as did cefpirome and cefepime. Cefquinome was not destroyed by the common plasmid beta-lactamases TEM-1, TEM-2, SHV-1, or by the chromosomal beta-lactamases of Klebsiella, Branhamella, and Pseudomonas, but it was hydrolyzed by TEM-3, TEM-5, and TEM-9. Its activity was not adversely decreased in different medium or protein, and minimum bactericidal concentrations (MBCs) for most species except for Enterobacter were within a dilution of MICs. PMID:1611848

Chin, N X; Gu, J W; Fang, W; Neu, H C

1992-01-01

269

In vitro and in vivo antiproliferative and trypanocidal activities of ruthenium NO donors  

PubMed Central

Background and purpose: Many compounds liberating NO (NO donors) have been used as therapeutic agents. Here we test two ruthenium nitrosyls, which release NO when activated by biological reducing agents, for their effects in vitro and in vivo against Trypanasoma cruzi, the agent responsible for the American trypanosomiasis (Chagas' disease). Experimental approach: Ruthenium NO donors were incubated with a partially drug-resistant strain of T. cruzi and the anti-proliferative and trypanocidal activities evaluated. In a mouse model of acute Chagas' disease, trypanocidal activity was evaluated by measuring parasitemia, survival rate of infected mice and elimination of amastigotes in myocardial tissue. Key results: In vitro, the observed anti-proliferative and trypanocidal activities of trans-[Ru(NO)(NH3)4isn](BF4)3 and trans-[Ru(NO)(NH3)4imN](BF4)3 were due to NO liberated upon reduction of these nitrosyls. Ru(NO)isn had a lower IC50epi (67 ?M) than the NO donor, sodium nitroprusside (IC50epi=244 ?M) and Ru(NO)imN (IC50try=52 ?M) was more potent than gentian violet (IC50try=536 ?M), currently used in the treatment of blood. Both ruthenium nitrosyls eliminated, in vivo, extracellular as well as intracellular forms of T. cruzi in the bloodstream and myocardial tissue and allowed survival of up to 80% of infected mice at a dose (100 nmol kg?1 day?1) much lower than the optimal dose for benznidazole (385 ?mol kg?1 day?1). Conclusions and implications: Our data strongly suggest that NO liberated is responsible for the anti-proliferative and trypanocidal activities of the ruthenium NO donors and that these compounds are promising leads for novel and effective anti-parasitic drugs. PMID:17603548

Silva, J J N; Osakabe, A L; Pavanelli, W R; Silva, J S; Franco, D W

2007-01-01

270

Assessment of Antioxidant Activities of Eugenol by in vitro and in vivo Methods  

PubMed Central

Summary Reactive oxygen species are implicated in many human diseases and aging process. Much of the evidence is based on experimental data indicating increasing rates of lipid peroxidation in disease states and the ameliorating effects of antioxidants. It is becoming increasingly evident that the natural antioxidants, which have basically a phenolic structure, play an important role in protecting tissues against free radical damage. Eugenol (4-allyl-2 methoxyphenol), is one among such naturally occurring phenolic compounds. The antioxidant activity of eugenol is evaluated by the extent of protection offered against free radical mediated lipid peroxidation using both in vitro and in vivo studies. The in vitro lipid peroxidation is induced in mitochondria by (Fe(II)-ascorbate) or (Fe(II) + H2O2). The lipid peroxidation is assessed colorimetrically by measuring the formation of thiobarbituric acid reactive substances (TBARS) following the reaction of oxidized lipids with TBA. Eugenol inhibits both iron and Fenton reagent mediated lipid peroxidation. The inhibitory activity of eugenol is about five fold higher than ?-tocopherol and about ten fold less than the synthetic antioxidant, BHT. The in vivo antioxidant activity of eugenol is evaluated by the determination of certain biochemical parameters (SGOT, Cyt.P450, glucose-6-phosphatase), peroxidation products and histopathological examination of •CCl3 radical induced hepatotoxicity in rats. Eugenol significantly inhibits the rise in SGOT activity and cell necrosis without protecting the endoplasmic reticulum (ER) damage as assessed by its failure to prevent a decrease in glucose-6-phosphatase activity. The protective action of eugenol has been found to be due to interception of secondary radicals derived from ER lipids rather than interfering with primary radicals of CCl4 (•CCl3/CCl3OO•). PMID:20013178

Nagababu, Enika; Rifkind, Joseph M.; Sesikeran, Boindala; Lakshmaiah, Nakka

2011-01-01

271

In vitro activity of origanum vulgare essential oil against candida species  

PubMed Central

The aim of this study was to evaluate the in vitro activity of the essential oil extracted from Origanum vulgare against sixteen Candida species isolates. Standard strains tested comprised C. albicans (ATCC strains 44858, 4053, 18804 and 3691), C. parapsilosis (ATCC 22019), C. krusei (ATCC 34135), C. lusitaniae (ATCC 34449) and C. dubliniensis (ATCC MY646). Six Candida albicans isolates from the vaginal mucous membrane of female dogs, one isolate from the cutaneous tegument of a dog and one isolate of a capuchin monkey were tested in parallel. A broth microdilution technique (CLSI) was used, and the inoculum concentration was adjusted to 5 x 106 CFU mL-1. The essential oil was obtained by hydrodistillation in a Clevenger apparatus and analyzed by gas chromatography. Susceptibility was expressed as Minimal Inhibitory Concentration (MIC) and Minimal Fungicidal Concentration (MFC). All isolates tested in vitro were sensitive to O. vulgare essential oil. The chromatographic analysis revealed that the main compounds present in the essential oil were 4-terpineol (47.95%), carvacrol (9.42%), thymol (8.42%) and ?-terpineol (7.57%). C. albicans isolates obtained from animal mucous membranes exhibited MIC and MFC values of 2.72 ?L mL-1 and 5 ?L mL-1, respectively. MIC and MFC values for C. albicans standard strains were 2.97 ?L mL-1 and 3.54 ?L mL-1, respectively. The MIC and MFC for non-albicans species were 2.10 ?L mL-1 and 2.97 ?L mL-1, respectively. The antifungal activity of O. vulgare essential oil against Candida spp. observed in vitro suggests its administration may represent an alternative treatment for candidiasis. PMID:24031471

Cleff, Marlete Brum; Meinerz, Ana Raquel; Xavier, Melissa; Schuch, Luiz Filipe; Schuch, Luiz Filipe; Araújo Meireles, Mário Carlos; Alves Rodrigues, Maria Regina; de Mello, Joăo Roberto Braga

2010-01-01

272

The Immunological Enhancement Activity of Propolis Flavonoids Liposome In Vitro and In Vivo  

PubMed Central

The aim of this study was to investigate and assess the effects of propolis flavonoids liposome imposed on the immune system by comparing it to propolis flavonoids and blank liposome. In vitro, the effects of the above drugs on macrophages were assessed by measuring the phagocytic function and cytokine production. In vivo, the immunological adjuvant activity of propolis flavonoids liposome was compared with those of propolis flavonoids and blank liposome. The results showed that in vitro propolis flavonoids liposome can significantly enhance the phagocytic function of macrophages and the release of IL-1?, IL-6, and IFN-?. In addition, subcutaneous administration of propolis flavonoids liposome with ovalbumin to mice could effectively activate the cellular and humoral immune response, including inducing higher level concentrations of IgG, IL-4, and IFN-? in serum and the proliferation rates of splenic lymphocytes. These findings provided valuable information regarding the immune modulatory function of propolis flavonoids liposome and indicated the possibility of use of propolis flavonoids liposome as a potential adjuvant. PMID:25383082

Tao, Yang; Wang, Deqing; Hu, Yuanliang; Huang, Yee; Yu, Yun; Wang, Deyun

2014-01-01

273

In vitro metabolism of pyripyropene A and ACAT inhibitory activity of its metabolites.  

PubMed

Pyripyropene A (PPPA, 1) of fungal origin, a selective inhibitor of acyl-CoA:cholesterol acyltransferase 2 (ACAT2), proved orally active in atherogenic mouse models. The in vitro metabolites of 1 in liver microsomes and plasma of human, rabbit, rat and mouse were analyzed by ultra fast liquid chromatography and liquid chromatography/tandem mass spectrometry. In the liver microsomes from all species, successive hydrolysis occurred at the 1-O-acetyl residue, then at the 11-O-acetyl residue of 1, while the 7-O-acetyl residue was resistant to hydrolysis. Furthermore, dehydrogenation of the newly generated 11-alcoholic hydroxyl residue occurred in human and mouse-liver microsomes, while oxidation of the pyridine ring occurred in human and rabbit liver microsomes. On the other hand, hydrolysis of the 7-O-acetyl residue proceeded only in the mouse plasma. These data indicated that the in vitro metabolic profiles of 1 have subtle differences among animal species. All of the PPPA metabolites observed in liver microsomes and plasma markedly decreased ACAT2 inhibitory activity. These findings will help us to synthesize new PPPA derivatives more effective in in vivo study than 1.The Journal of Antibiotics advance online publication, 9 July 2014; doi:10.1038/ja.2014.91. PMID:25005817

Matsuda, Daisuke; Ohshiro, Taichi; Ohtawa, Masaki; Yamazaki, Hiroyuki; Nagamitsu, Tohru; Tomoda, Hiroshi

2014-07-01

274

In vitro activity of Alkanna frigida extracts in comparison with glucantime against Leishmania major  

PubMed Central

Background and Objectives Current chemotherapies of cutaneous leihmaniasis have faced to some problems and limitations; Development of new leishmanicidal drugs from different sources like herbal plants, are crucially important. The objective of the present study was evaluation of in vitro activity of Alkanna frigida extracts in comparison with glucantime against Leishmania major. Materials and Methods L. major promastigotes were exposed to different concentrations of the A. frigida extracts, processed by ethyl acetate, ethanol, hexane and chloroform. The inhibitory effect, as the IC50, were calculated after 24, 48 and 72 hours by linear regression analysis values of the concentrations employed. Results The significant inhibition was observed after 24 and 48 hours with different concentrations of compounds (p < 0.05 in all tests). All extracts had potent activity against proliferation of the promastigotes, comparing to the untreated negative control. It could compete with the glucantime efficacy in some concentrations. Ethyl acetate and ethanol extractions showed potent IC50 value, 106 µg/ml and 86 µg/ml, respectively. Hexane and chloroform extractions had poor efficacy after 24 hours; however, the efficacy increased after 48 and 72 hours. Conclusion The results indicated that the A. frigida has appropriate inhibitory effects on the growth of L. major promastigotes in vitro and can be of herbal targets for further investigation in vivo. PMID:23825738

Jafari, Fariba; Nourian, Abbasali; Fazaeli, Asghar; Yazdinezhad, Alireza; Haniloo, Ali

2013-01-01

275

Antimicrobial activity of artemisinin and precursor derived from in vitro plantlets of Artemisia annua L.  

PubMed

Artemisia annua L., a medicinal herb, produces secondary metabolites with antimicrobial property. In Malaysia due to the tropical hot climate, A. annua could not be planted for production of artemisinin, the main bioactive compound. In this study, the leaves of three in vitro A. annua L. clones were, extracted and two bioactive compounds, artemisinin and a precursor, were isolated by thin layer chromatography. These compounds were found to be effective in inhibiting the growth of Gram-positive and Gram-negative bacteria but not Candida albicans. Their antimicrobial activity was similar to that of antibactericidal antibiotic streptomycin. They were found to inhibit the growth of the tested microbes at the minimum inhibition concentration of 0.09?mg/mL, and toxicity test using brine shrimp showed that even the low concentration of 0.09?mg/mL was very lethal towards the brine shrimps with 100% mortality rate. This study hence indicated that in vitro cultured plantlets of A. annua can be used as the alternative method for production of artemisinin and its precursor with antimicrobial activities. PMID:24575401

Appalasamy, Suganthi; Lo, Kiah Yann; Ch'ng, Song Jin; Nornadia, Ku; Othman, Ahmad Sofiman; Chan, Lai-Keng

2014-01-01

276

Antimicrobial Activity of Artemisinin and Precursor Derived from In Vitro Plantlets of Artemisia annua L.  

PubMed Central

Artemisia annua L., a medicinal herb, produces secondary metabolites with antimicrobial property. In Malaysia due to the tropical hot climate, A. annua could not be planted for production of artemisinin, the main bioactive compound. In this study, the leaves of three in vitro A. annua L. clones were, extracted and two bioactive compounds, artemisinin and a precursor, were isolated by thin layer chromatography. These compounds were found to be effective in inhibiting the growth of Gram-positive and Gram-negative bacteria but not Candida albicans. Their antimicrobial activity was similar to that of antibactericidal antibiotic streptomycin. They were found to inhibit the growth of the tested microbes at the minimum inhibition concentration of 0.09?mg/mL, and toxicity test using brine shrimp showed that even the low concentration of 0.09?mg/mL was very lethal towards the brine shrimps with 100% mortality rate. This study hence indicated that in vitro cultured plantlets of A. annua can be used as the alternative method for production of artemisinin and its precursor with antimicrobial activities. PMID:24575401

Appalasamy, Suganthi; Lo, Kiah Yann; Ch'ng, Song Jin; Nornadia, Ku; Othman, Ahmad Sofiman; Chan, Lai-Keng

2014-01-01

277

Evaluation of the immunomodulatory activities of royal jelly components in vitro.  

PubMed

In this work the effect of different components isolated from royal jelly (RJ) was studied using an in vitro rat T-cell proliferation assay. We found that lower concentrations of MEL 174 (final water extract of RJ) and MEL 147 (3-10-dihydroxydecanoic acid) stimulated T-cell proliferation, triggered by concanavalin A (Con-A) and the process was followed by an increase in the production of interleukin-2 (IL-2). Higher concentrations of MEL 174, MEL 247 (dry powder of RJ) and MEL 138 (trans-10-hydroxydec-2-enoic acid) inhibited T-cell proliferation. The inhibition of T-cell proliferation in the presence of MEL 174 was followed by a decrease in IL-2 production, which was partly abrogated by exogenous IL-2, a decrease in nitric oxide (NO) production and increased apoptosis. In conclusion, our results showed the complexity of biological activity of RJ and suggest that its water extract possesses the most potent immunomodulatory activity in vitro. PMID:18075862

Gasic, Sonja; Vucevic, Dragana; Vasilijic, Sasa; Antunovic, Mirjana; Chinou, Ioanna; Colic, Miodrag

2007-01-01

278

Transferrin mediated solid lipid nanoparticles containing curcumin: enhanced in vitro anticancer activity by induction of apoptosis.  

PubMed

Photodegradation and low bioavailability are major hurdles for the therapeutic use of curcumin. Aim of the present study was to formulate transferrin-mediated solid lipid nanoparticles (Tf-C-SLN) to increase photostability, and enhance its anticancer activity against MCF-7 breast cancer cells. Tf-C-SLN were prepared by homogenization method and characterized by size, zeta potential, entrapment efficiency and stability, transmission electron microscopy (TEM), X-ray diffraction (XRD) and in vitro release study. Microplate analysis and flow cytometry techniques were used for cytotoxicity and apoptosis study. The physical characterization showed the suitability of method of preparation. TEM and XRD study revealed the spherical nature and entrapment of curcumin in amorphous form, respectively. The cytotoxicity, ROS and cell uptake was found to be increased considerably with Tf-C-SLN compared to curcumin solubilized surfactant solution (CSSS) and curcumin-loaded SLN (C-SLN) suggesting the targeting effect. AnnexinV-FITC/PI double staining, DNA analysis and reduced mitochondrial potential confirmed the apoptosis. The flow cytometric studies revealed that the anticancer activity of curcumin is enhanced with Tf-C-SLN compared to CSSS and C-SLN, and apoptosis is the mechanism underlying the cytotoxicity. The present study indicated the potential of Tf-C-SLN in enhancing the anticancer effect of curcumin in breast cancer cells in vitro. PMID:20655375

Mulik, Rohit S; Mönkkönen, Jukka; Juvonen, Risto O; Mahadik, Kakasaheb R; Paradkar, Anant R

2010-10-15

279

Neonatal Phosphate Nutrition Alters in Vivo and in Vitro Satellite Cell Activity in Pigs  

PubMed Central

Satellite cell activity is necessary for postnatal skeletal muscle growth. Severe phosphate (PO4) deficiency can alter satellite cell activity, however the role of neonatal PO4 nutrition on satellite cell biology remains obscure. Twenty-one piglets (1 day of age, 1.8 ± 0.2 kg BW) were pair-fed liquid diets that were either PO4 adequate (0.9% total P), supra-adequate (1.2% total P) in PO4 requirement or deficient (0.7% total P) in PO4 content for 12 days. Body weight was recorded daily and blood samples collected every 6 days. At day 12, pigs were orally dosed with BrdU and 12 h later, satellite cells were isolated. Satellite cells were also cultured in vitro for 7 days to determine if PO4 nutrition alters their ability to proceed through their myogenic lineage. Dietary PO4 deficiency resulted in reduced (P < 0.05) sera PO4 and parathyroid hormone (PTH) concentrations, while supra-adequate dietary PO4 improved (P < 0.05) feed conversion efficiency as compared to the PO4 adequate group. In vivo satellite cell proliferation was reduced (P < 0.05) among the PO4 deficient pigs, and these cells had altered in vitro expression of markers of myogenic progression. Further work to better understand early nutritional programming of satellite cells and the potential benefits of emphasizing early PO4 nutrition for future lean growth potential is warranted. PMID:22822445

Alexander, Lindsey S.; Seabolt, Brynn S.; Rhoads, Robert P.; Stahl, Chad H.

2012-01-01

280

In vitro analysis of finasteride activity against Candida albicans urinary biofilm formation and filamentation.  

PubMed

Candida albicans is the 3rd most common cause of catheter-associated urinary tract infections, with a strong propensity to form drug-resistant catheter-related biofilms. Due to the limited efficacy of available antifungals against biofilms, drug repurposing has been investigated in order to identify novel agents with activities against fungal biofilms. Finasteride is a 5-?-reductase inhibitor commonly used for the treatment of benign prostatic hyperplasia, with activity against human type II and III isoenzymes. We analyzed the Candida Genome Database and identified a C. albicans homolog of type III 5-?-reductase, Dfg10p, which shares 27% sequence identity and 41% similarity to the human type III 5-?-reductase. Thus, we investigated finasteride for activity against C. albicans urinary biofilms, alone and in combination with amphotericin B or fluconazole. Finasteride alone was highly effective in the prevention of C. albicans biofilm formation at doses of ?16 mg/liter and the treatment of preformed biofilms at doses of ?128 mg/liter. In biofilm checkerboard analyses, finasteride exhibited synergistic activity in the prevention of biofilm formation in a combination of 4 mg/liter finasteride with 2 mg/liter fluconazole. Finasteride inhibited filamentation, thus suggesting a potential mechanism of action. These results indicate that finasteride alone is highly active in the prevention of C. albicans urinary biofilms in vitro and has synergistic activity in combination with fluconazole. Further investigation of the clinical utility of finasteride in the prevention of urinary candidiasis is warranted. PMID:25049253

Chavez-Dozal, Alba A; Lown, Livia; Jahng, Maximillian; Walraven, Carla J; Lee, Samuel A

2014-10-01

281

Telomere Length and Telomerase Activity in Bovine Pre-implantation Embryos In Vitro.  

PubMed

Telomeres are specialized structures that cap the ends of chromosomes and help to maintain genomic integrity and stability. Telomeres undergo dynamic changes during embryo development, which also represents an important stage for telomere elongation through telomerase enzyme activity. The objectives of this study were to examine changes in telomere length and telomerase activity from the early oocyte, through to the blastocysts stage of development, and the expression of factors with the potential to directly regulate telomeres. In vitro-produced bovine embryos were lysed and analysed for either relative telomere length, or telomerase activity using quantitative real-time PCR protocols. Our results reveal that relative telomere length is the shortest in the presumptive zygote stage of development and gradually increases to the blastocyst stage. We also demonstrate that differences between the mean telomere lengths throughout these stages are statistically significant (p < 0.05). Telomerase activity in the stages examined appears relatively constant until the blastocyst, where the highest level of activity is detected, leading to a significant difference in telomerase activity across embryonic stages (p < 0.005). Bovine telomerase RNA component (bTERC) expression levels were highest in the blastocyst, TERF1 transcripts showed little change in expression, and TERF2 expression decreased in the blastocysts (p < 0.05). Our results suggest that a complex integration of telomere-related RNA and proteins influences the regulatory mechanisms involved in 'reprogramming' of telomeres during early embryonic stages. PMID:25469445

Gilchrist, Gc; Kurjanowicz, P; Mereilles, Fv; King, Wa; LaMarre, J

2015-02-01

282

In vitro hemolytic activity of Lonomia obliqua caterpillar bristle extract on human and Wistar rat erythrocytes.  

PubMed

Human accidental envenomation caused by skin contact with the bristles of Lonomia obliqua caterpillar causes coagulation and fibrinolysis disorders. Alterations of hematologic parameters are observed only in severe cases of envenomation, but with no clinical evidence of intravascular hemolysis. However, since we have observed intravascular hemolysis in preliminary studies using Wistar rats as an experimental model for investigating L. obliqua envenomation, the objective of the present study was to investigate the in vitro hemolytic activity of the bristle extract of L. obliqua caterpillars on human and rat erythrocytes. Our results showed that the bristle extract has indirect and direct hemolytic activity on human and rat erythrocytes, although direct hemolytic activity was only observed at higher bristle extract concentrations. We also observed that the bristle extract has a proteolytic activity on band 3 of human and rat erythrocyte membranes. Thus, crude L. obliqua bristle extract was found to contain at least two components with hemolytic activity on erythrocytes, a phospholipase enzyme and another protein with a direct activity on the erythrocyte membrane. PMID:12782083

Seibert, Carla Simone; Shinohara, Elvira Maria Guerra; Sano-Martins, Ida Sigueko

2003-06-01

283

Cholecystokinin activates pancreatic calcineurin-NFAT signaling in vitro and in vivo.  

PubMed

Elevated endogenous cholecystokinin (CCK) release induced by protease inhibitors leads to pancreatic growth. This response has been shown to be mediated by the phosphatase calcineurin, but its downstream effectors are unknown. Here we examined activation of calcineurin-regulated nuclear factor of activated T-cells (NFATs) in isolated acinar cells, as well as in an in vivo model of pancreatic growth. Western blotting of endogenous NFATs and confocal imaging of NFATc1-GFP in pancreatic acini showed that CCK dose-dependently stimulated NFAT translocation from the cytoplasm to the nucleus within 0.5-1 h. This shift in localization correlated with CCK-induced activation of NFAT-driven luciferase reporter and was similar to that induced by a calcium ionophore and constitutively active calcineurin. The effect of CCK was dependent on calcineurin, as these changes were blocked by immunosuppressants FK506 and CsA and by overexpression of the endogenous protein inhibitor CAIN. Parallel NFAT activation took place in vivo. Pancreatic growth was accompanied by an increase in nuclear NFATs and subsequent elevation in expression of NFAT-luciferase in the pancreas, but not in organs unresponsive to CCK. The changes also required calcineurin, as they were blocked by FK506. We conclude that CCK activates NFATs in a calcineurin-dependent manner, both in vitro and in vivo. PMID:17978097

Gurda, Grzegorz T; Guo, LiLi; Lee, Sae-Hong; Molkentin, Jeffery D; Williams, John A

2008-01-01

284

Cholecystokinin Activates Pancreatic Calcineurin-NFAT Signaling In Vitro and In Vivo  

PubMed Central

Elevated endogenous cholecystokinin (CCK) release induced by protease inhibitors leads to pancreatic growth. This response has been shown to be mediated by the phosphatase calcineurin, but its downstream effectors are unknown. Here we examined activation of calcineurin-regulated nuclear factor of activated T-cells (NFATs) in isolated acinar cells, as well as in an in vivo model of pancreatic growth. Western blotting of endogenous NFATs and confocal imaging of NFATc1-GFP in pancreatic acini showed that CCK dose-dependently stimulated NFAT translocation from the cytoplasm to the nucleus within 0.5–1 h. This shift in localization correlated with CCK-induced activation of NFAT-driven luciferase reporter and was similar to that induced by a calcium ionophore and constitutively active calcineurin. The effect of CCK was dependent on calcineurin, as these changes were blocked by immunosuppressants FK506 and CsA and by overexpression of the endogenous protein inhibitor CAIN. Parallel NFAT activation took place in vivo. Pancreatic growth was accompanied by an increase in nuclear NFATs and subsequent elevation in expression of NFAT-luciferase in the pancreas, but not in organs unresponsive to CCK. The changes also required calcineurin, as they were blocked by FK506. We conclude that CCK activates NFATs in a calcineurin-dependent manner, both in vitro and in vivo. PMID:17978097

Guo, LiLi; Lee, Sae-Hong; Molkentin, Jeffery D.; Williams, John A.

2008-01-01

285

SCE-129, Antipseudomonal Cephalosporin: In Vitro and In Vivo Antibacterial Activities  

PubMed Central

SCE-129 [3-(4-carbamoyl-1-pyridiniomethyl)-7?-(d-?-sulfophenylacetamido)-ceph-3-em-4-carboxylate monosodium salt], a new semisynthetic cephalosporin, shows potent in vitro antibacterial activities against Pseudomonas aeruginosa and some gram-positive bacteria, whereas it shows lower activity against many gram-negative rods. Against clinical isolates of P. aeruginosa this cephalosporin exhibited higher activity than did carbenicillin, and against the strains of Staphylococcus aureus, SCE-129 had similar activity to carbenicillin. Variations in pH, addition of horse serum, and type of growth medium had no significant effects on the activity of the cephalosporin; however, the inoculum size had some effect on the activity. SCE-129 is an effective bactericidal agent against P. aeruginosa and S. aureus. The protective effects of SCE-129 in mice infected with P. aeruginosa and S. aureus were more potent than those of carbenicillin. The protective effects of SCE-129 on Pseudomonas infection in mice varied according to the dosage schedule and the challenge dose. In a multiple dose schedule, a smaller amount of SCE-129 was necessary than that in a single dose schedule. The effects of SCE-129 after subcutaneous or intraperitoneal administration were more potent than were those by intravenous administration. No protective effect was observed by oral administration. PMID:417670

Tsuchiya, Kanji; Kondo, Masahiro; Nagatomo, Hiroshi

1978-01-01

286

In Vitro and Ex Vivo Activities of Minocycline and EDTA against Microorganisms Embedded in Biofilm on Catheter Surfaces  

Microsoft Academic Search

Minocycline-EDTA (M-EDTA) flush solution has been shown to prevent catheter-related infection and colonization in a rabbit model and in hemodialysis patients. We undertook this study in order to determine the activities of M-EDTA against organisms embedded in fresh biofilm (in vitro) and mature biofilm (ex vivo). For the experiment with the in vitro model, a modified Robbin's device (MRD) was

Issam Raad; Ioannis Chatzinikolaou; Gassan Chaiban; Hend Hanna; Ray Hachem; Tanya Dvorak; Guy Cook; William Costerton

2003-01-01

287

In vitro Activation of heme oxygenase-2 by menadione and its analogs  

PubMed Central

Background Previously, we reported that menadione activated rat, native heme oxygenase-2 (HO-2) and human recombinant heme oxygenase-2 selectively; it did not activate spleen, microsomal heme oxygenase-1. The purpose of this study was to explore some structure–activity relationships of this activation and the idea that redox properties may be an important aspect of menadione efficacy. Methods Heme oxygenase activity was determined in vitro using rat spleen and brain microsomes as the sources of heme oxygenase-1 and ?2, respectively, as well as recombinant, human heme oxygenase-2. Results Menadione analogs with bulky aliphatic groups at position-3, namely vitamins K1 and K2, were not able to activate HO-2. In contrast, several compounds with similar bulky but less lipophilic moieties at position-2 (and ?3) were able to activate HO-2 many fold; these compounds included polar, rigid, furan-containing naphthoquinones, furan-benzoxazine naphthoquinones, 2-(aminophenylphenyl)-3-piperidin-1-yl naphthoquinones. To explore the idea that redox properties might be involved in menadione efficacy, we tested analogs such as 1,4-dimethoxy-2-methylnaphthalene, pentafluoromenadione, monohalogenated naphthoquinones, ?-tetralone and 1,4-naphthoquinone. All of these compounds were inactive except for 1,4-naphthoquinone. Menadione activated full-length recombinant human heme oxygenase-2 (FL-hHO-2) as effectively as rat brain enzyme, but it did not activate rat spleen heme oxygenase. Conclusions These observations are consistent with the idea that naphthoquinones such as menadione bind to a receptor in HO-2 and activate the enzyme through a mechanism that may involve redox properties. PMID:24533775

2014-01-01

288

Xenobiotic metabolizing enzyme activities in cells used for testing skin sensitization in vitro.  

PubMed

For ethical and regulatory reasons, in vitro tests for scoring potential toxicities of cosmetics are essential. A test strategy for investigating potential skin sensitization using two human keratinocytic and two human dendritic cell lines has been developed (Mehling et al. Arch Toxicol 86:1273–1295, 2012). Since prohaptens may be metabolically activated in the skin, information on xenobiotic metabolizing enzyme (XME) activities in these cell lines is of high interest. In this study, XME activity assays, monitoring metabolite or cofactor, showed the following: all three passages of keratinocytic (KeratinoSens® and LuSens) and dendritic (U937 und THP-1) cells displayed N-acetyltransferase 1 (NAT1) activities (about 6–60 nmol/min/mg S9-protein for acetylation of para-aminobenzoic acid). This is relevant since reactive species of many cosmetics are metabolically controlled by cutaneous NAT1. Esterase activities of about 1–4 nmol fluorescein diacetate/min/mg S9-protein were observed in all passages of investigated keratinocytic and about 1 nmol fluorescein diacetate/min/mg S9-protein in dendritic cell lines. This is also of practical relevance since many esters and amides are detoxified and others activated by cutaneous esterases. In both keratinocytic cell lines, activities of aldehyde dehydrogenase (ALDH) were observed (5–17 nmol product/min/mg cytosolic protein). ALDH is relevant for the detoxication of reactive aldehydes. Activities of several other XME were below detection, namely the investigated cytochrome P450-dependent alkylresorufin O-dealkylases 7-ethylresorufin O-deethylase, 7-benzylresorufin O-debenzylase and 7-pentylresorufin O-depentylase (while NADPH cytochrome c reductase activities were much above the limit of quantification), the flavin-containing monooxygenase, the alcohol dehydrogenase as well as the UDP glucuronosyl transferase activities. PMID:23958860

Fabian, E; Vogel, D; Blatz, V; Ramirez, T; Kolle, S; Eltze, T; van Ravenzwaay, B; Oesch, F; Landsiedel, R

2013-09-01

289

Anticancer activity of litchi fruit pericarp extract against human breast cancer in vitro and in vivo  

SciTech Connect

Litchi fruit pericarp (LFP) extract contains significant amounts of polyphenolic compounds and exhibits powerful antioxidative activity against fat oxidation in vitro. The purpose of this study is to confirm the anticancer activity of LFP extract on human breast cancer in vitro and in vivo, and to elucidate the mechanism of its activity. Human breast cancer cells were tested in vitro for cytotoxicity, colony formation inhibition, BrdU incorporation, and gene expression profiling after treatment with LFP extract. Seven nude mice bearing human breast infiltrating duct carcinoma orthotopically were tested for its anticancer activity and expression of caspase-3 in vivo by oral administration of 0.3% (0.3 mg/ml) of LFP water-soluble crude ethanolic extract (CEE) for 10 weeks. LFP extract demonstrated a dose- and time-dependent inhibitory effect on cell growth (IC{sub 5} = 80 {mu}g/ml), and it significantly inhibited colony formation and BrdU incorporation of human breast cancer cells. Oligonucleotide microarray analysis identified 41(1.22%) up-regulated and 129 (3.84%) down-regulated genes after LFP water-soluble CEE treatment; the predominantly up-regulated genes were involved in various biological functions including cell cycle regulation and cell proliferation, apoptosis, signal transduction and transcriptional regulation, and extracellular matrix/adhesion molecules; and down-regulated genes were mainly associated with adhesion, invasion, and malignancy of cancer cells. A 40.70% tumor mass volume reduction and significant increase of casepase-3 protein expression were observed in vivo experiment. The findings in this study suggested that LFP extract might have potential anticancer activity on both ER positive and negative breast cancers, which could be attributed, in part, to its DNA damage effect, proliferating inhibition and apoptosis induction of cancer cells through up-regulation and down-regulation of multiple genes involved in cell cycle regulation and cell proliferation, apoptosis, signal transduction and transcriptional regulation, motility and invasiveness of cancer cells; ADP-ribosyltransferase (NAD+; poly (ADP-ribose) polymerase)-like 1 (ADPRTL1), Cytochrome P450, subfamily I (CYP1A1) and Hyaluronan-mediated motility receptor (HMMR) might be the main molecular targets at which LFP water-soluble CEE acted.

Wang Xiujie [Division of Experimental Oncology, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China)]. E-mail: xiujiewang@yahoo.com; Yuan Shulan [Division of Experimental Oncology, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China); Wang Jing [Division of Experimental Oncology, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China); Lin Ping [Division of Experimental Oncology, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China); Liu Guanjian [Department of Clinical Epidemiology, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China); Lu Yanrong [Division of Experimental Oncology, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China); Zhang Jie [Division of Experimental Oncology, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China); Wang, Wendong [Department of Pathology of Public Health School, Sichuan University, Chengdu 610041, Sichuan Province (China); Wei Yuquan [Division of Biotherapy, National Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, Sichuan Province (China)]. E-mail: yuquanwei@mail.sc.cninfo.net

2006-09-01

290

Ethnopharmacological in vitro studies on Austria's folk medicine—An unexplored lore in vitro anti-inflammatory activities of 71 Austrian traditional herbal drugs?  

PubMed Central

Ethnopharmacological relevance In Austria, like in most Western countries, knowledge about traditional medicinal plants is becoming scarce. Searching the literature concerning Austria's ethnomedicine reveals its scant scientific exploration. Aiming to substantiate the potential of medicinal plants traditionally used in Austria, 63 plant species or genera with claimed anti-inflammatory properties listed in the VOLKSMED database were assessed for their in vitro anti-inflammatory activity. Material and methods 71 herbal drugs from 63 plant species or genera were extracted using solvents of varying polarities and subsequently depleted from the bulk constituents, chlorophylls and tannins to avoid possible interferences with the assays. The obtained 257 extracts were assessed for their in vitro anti-inflammatory activity. The expression of the inflammatory mediators E-selectin and interleukin-8 (IL-8), induced by the inflammatory stimuli tumor necrosis factor alpha (TNF-?) and the bacterial product lipopolysaccharide (LPS) was measured in endothelial cells. The potential of the extracts to activate the nuclear factors PPAR? and PPAR? and to inhibit TNF-?-induced activation of the nuclear factor-kappa B (NF-?B) in HEK293 cells was determined by luciferase reporter gene assays. Results In total, extracts from 67 of the 71 assessed herbal drugs revealed anti-inflammatory activity in the applied in vitro test systems. Thereby, 30 could downregulate E-selectin or IL-8 gene expression, 28 were strong activators of PPAR? or PPAR? (inducing activation of more than 2-fold at a concentration of 10 µg/mL) and 21 evoked a strong inhibition of NF-?B (inhibition of more than 80% at 10 µg/mL). Conclusion Our research supports the efficacy of herbal drugs reported in Austrian folk medicine used for ailments associated with inflammatory processes. Hence, an ethnopharmacological screening approach is a useful tool for the discovery of new drug leads. PMID:23770053

Vogl, Sylvia; Picker, Paolo; Mihaly-Bison, Judit; Fakhrudin, Nanang; Atanasov, Atanas G.; Heiss, Elke H.; Wawrosch, Christoph; Reznicek, Gottfried; Dirsch, Verena M.; Saukel, Johannes; Kopp, Brigitte

2013-01-01

291

In vitro biological activities and fatty acid profiles of Pistacia terebinthus fruits and Pistacia khinjuk seeds.  

PubMed

This study reports in vitro anticholinesterase, antioxidant and antimicrobial effects of the n-hexane, dichloromethane, ethanol and ethanol-water extracts prepared from Pistacia terebinthus L. fruits and Pistacia khinjuk Stocks seeds as well as their total phenolic and flavonoid contents, and fatty acid compositions. Ethanol and ethanol-water extracts of both species exhibited higher anticholinesterase activity than galanthamine. Among ABTS, DPPH and CUPRAC assays, the highest antioxidant capacity of the extracts was found in the last one. P. terebinthus ethanol extract being rich in flavonoid content showed the best cupric reducing effect. All extracts possessed no antimicrobial activity. The main fatty acid in P. terebinthus fruits (52.52%) and P. khinjuk seeds (59.44%) was found to be oleic acid. Our results indicate that P. terebinthus fruits and P. khinjuk seeds could be a good source of anticholinesterase compounds, and could be phytochemically investigated. PMID:25115646

Hac?bekiro?lu, I??l; Y?lmaz, Pelin Köseo?lu; Ha?imi, Nesrin; K?l?nç, Ersin; Tolan, Veysel; Kolak, Ufuk

2014-08-12

292

Synthesis, characterization, in vitro anti-proliferative and hemolytic activity of hydroxyapatite.  

PubMed

Hydroxyapatite (Ca10(PO4)6(OH)2, HAP) nanoparticles are widely used in several biomedical applications due to its compositional similarities to bone mineral, excellent biocompatibility and bioactivity, osteoconductivity. In this present investigation, HAP nanoparticles synthesized by precipitation technique using calcium nitrate and di-ammonium phosphate. The crystalline nature and the functional group analysis are confirmed using X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and Fourier transform Raman spectroscopy (FT-Raman) respectively. The morphological observations are ascertained from field emission electron scanning electron microscope (FE-SEM) and transmission electron microscope (TEM). In vitro anti-proliferative and hemolytic activities are carried out on the synthesized HAP samples and the studies reveals that HAP have mild activity against erythrocytes. PMID:24650878

Palanivelu, R; Ruban Kumar, A

2014-06-01

293

Flavonoid glycosides from Chromolaena odorata leaves and their in vitro cytotoxic activity.  

PubMed

Two new flavonoid glycosides, (1, 2), and eleven known compounds, (3-13), were isolated from from a 70% EtOH extract of the leaves of Chromolaena odorata (Asteraceae). Their structures were elucidated by 1D and 2D NMR spectroscopic interpretation as well as by chemical studies. The newly isolated compounds were tested in vitro for their cytotoxic activities against the LLC and HL-60 cancer cell lines. Compound 1 showed cytotoxicity against LLC and HL-60 cancer cell lines with IC(50) values of 28.2 and 11.6 µM, respectively. Compound 2 exhibited significant cytotoxic activity in the inhibition of HL-60 cancer cell lines with IC(50) value of 10.8 µM. PMID:21212562

Hung, Tran Manh; Cuong, To Dao; Dang, Nguyen Hai; Zhu, Shu; Long, Pham Quoc; Komatsu, Katsuko; Min, Byung Sun

2011-01-01

294

In vitro bactericidal activity of aminoglycosides, including the next-generation drug plazomicin, against Brucella spp.  

PubMed

Plazomicin is a next-generation aminoglycoside with a potentially unique set of clinical characteristics compared with other aminoglycosides. This study assessed the minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) of plazomicin against 15 clinical isolates as well as three reference strains representing Brucella abortus, Brucella melitensis and Brucella suis. These data were compared with those obtained for six other aminoglycosides and two aminocyclitols. Plazomicin and gentamicin were the only drugs demonstrating bactericidal activity towards two of the three Brucella spp., whilst plazomicin was the only drug exhibiting bactericidal activity against B. suis. This is the first study to assess the bactericidal nature of plazomicin against Brucella spp. in vitro. PMID:25459738

Olsen, Steven C; Carlson, Steve A

2015-01-01

295

In vitro activity of antimicrobial agents against Pseudomonas tolaasii, pathogen of cultivated button mushroom.  

PubMed

In vitro antibacterial activity tests of seven biofungicides (Ekstrasol, Bisolbisan, Bisolbifit, Serenade, Sonata, Timorex, F-Stop) and two disinfectants (colloidal silver alone and in combination with hydrogen peroxide) against the Pseudomonas tolaasii strain (NS3B6) were carried out by the disc-diffusion, broth microdilution and broth macrodilution method. Biofungicides tested in this study did not exhibit any antimicrobial activity in neither one of the methods used. Disc diffusion method revealed high sensitivity of the tested P. tolaasii strain to Ecocute based on colloidal silver and hydrogen peroxide. Both microdilution and macrodilution methods identified the same MICs and MBCs of Ecocute (0.19 mg/L) for P. tolaasii strain. MICs and MBCs values of silver alone were much higher (10 mg/L) compared to silver in combination with hydrogen peroxide. PMID:22375589

Todorovi?, Biljana; Milijasevi?-Mar?i?, Svetlana; Poto?nik, Ivana; Stepanovi?, Miloš; Rekanovi?, Emil; Nikoli?-Bujanovi?, Ljiljana; Cekerevac, Milan

2012-01-01

296

Inhibitory Activities of Cudrania tricuspidata Leaves on Pancreatic Lipase In Vitro and Lipolysis In Vivo  

PubMed Central

To identify effective herb to treat obesity, we screened 115 herbal extracts for inhibition of porcine pancreatic lipase (triacylg-ycerol acylhydrolase, EC 3.1.1.3) activity in vitro. Of the extracts tested, Cudrania tricuspidata leaves exhibited the most pronounced inhibitory effect on lipase activity with an IC50 value of 9.91??g/mL. Antilipid absorption effects of C. tricuspidata leaves were examined in rats after oral administration of lipid emulsions containing 50 or 250?mg??C. tricuspidata/kg body weight. Plasma triacylglycerol levels 2?h after the oral administration of emulsions containing C. tricuspidata were significantly reduced compared to the untreated group (P < 0.05). These results suggest that C. tricuspidata leaves may be useful for the treatment of obesity. PMID:23365603

Kim, Young Sook; Lee, Youngseop; Kim, Junghyun; Sohn, Eunjin; Kim, Chan Sik; Lee, Yun Mi; Jo, Kyuhyung; Shin, Sodam; Song, Yoojin; Kim, Joo Hwan; Kim, Jin Sook

2012-01-01

297

Antibacterial activity of aqueous extracts of Indian chewing sticks on dental plaque: An in vitro study.  

PubMed

The anti-microbial efficacy of aqueous extracts of Indian chewing sticks against different kinds of plaque bacteria in vitro was investigated. Supra-gingival plaque is cultured and subjected to the antibacterial activity of the aqueous extracts of chewing sticks (Neem, Acacia, Pongamia glabra, Achyranthes aspera, Streblus asper) separately. The results of the study demonstrate that all the five chewing sticks under study possess inhibitory potential against bacteria present in dental plaque mainly on aerobes. The antibacterial efficacy of aqueous extracts has antibacterial effects and could be used as a therapeutic agent and therefore, it appears to be potent anti-microbial agents that could be considered as a medicinal plant. Results of this study showed chewing sticks contained antibacterial agents, but the concentration and composition of the active substances differed among the plants. PMID:25210357

Rao, Dola Srinivasa; Penmatsa, Tanuja; Kumar, Alapati Kranthi; Reddy, M Narendra; Gautam, Nalam Sai; Gautam, Nalam Radhika

2014-07-01

298

In Vitro Activities of Three Nonfluorinated Quinolones against Representative Bacterial Isolates  

PubMed Central

In vitro susceptibility tests were performed to document the inhibitory activities of three nonfluorinated quinolone (NFQ) compounds (PGE 9262932, PGE 9509924, and PGE 4175997) compared to those of ciprofloxacin, levofloxacin, and trovafloxacin against 3,030 bacterial isolates. The spectra of the NFQ agents included most gram-positive species as well as quinolone-susceptible Enterobacteriaceae. Ciprofloxacin-resistant, methicillin-resistant Staphylococcus aureus strains were inhibited by the NFQ series at ?1.0 ?g/ml. The NFQ compounds were not very active against Pseudomonas aeruginosa and most other nonfermentative gram-negative bacilli. Against other species, the potency of the NFQ agents was similar to that of trovafloxacin. Continued investigation of the NFQ compounds seems to be warranted. PMID:11353655

Barry, Arthur L.; Fuchs, Peter C.; Brown, Steven D.

2001-01-01

299

Chemical composition and in vitro antimicrobial activity of the essential oil of Cyclotrichium leucotrichum from Iran.  

PubMed

The objective of this study was to investigate in vitro antimicrobial activity and composition of the essential oil of Cyclotrichium leucotrichum growing wild in Iran. The essential oil was obtained by hydro-distillation and analysed by GC-FID and GC/MS. Fifty-nine components representing 98.9% of the total oil were characterised. The essential oil which has 1,8-cineol (14.8%), elemol (12.6%), spathulenol (9.4%), E-caryophyllene (5.7%) and hinesol (5.7%) as its main components, exhibited moderate activity against seven bacteria and a yeast, Candida albicans, with minimum inhibitory concentration values ranging from 0.5 to 64 mg mL(-1) and minimum bactericidal concentration values ranging from 2 to >64 mg mL(-1), respectively. The best inhibitory effects were against three gram-positive bacteria and tested yeast, C. albicans. PMID:22455838

Mirjalili, M H; Hadian, J; Aliahmadi, A; Kanani, M R; Sonboli, A

2013-01-01

300

Endophytic fungi diversity of aquatic/riparian plants and their antifungal activity in vitro.  

PubMed

Two hundred and fourteen endophytic fungi were isolated from 500 segments of aquatic/riparian plants Ottelia acuminata, Myriophyllum verticillatum, Equisetum arvense, Cardamine multijuga, and Impatiens chinensis. They were identified to 31 taxa in which Cladosporium, Fusarium, and Geotrichum were the dominant genera. Among all isolates, 169 (79%) were anamorphic fungi, 1 (0.5%) was an teleomorphic ascomycete and 44 (21%) were sterile mycelia. There were significant differences in the colonization frequency of endophytes between the five plant species (X~2=51.128, P<0.001, Chi-square test). The riparian plants harboured more endophytes than the submerged plants. The antifungal activity of these isolates against Fusarium solani and Phytophthora nicotianae in vitro were tested and 28 (13.1%) isolates showed antifungal activities with more than 30% growth inhibition rate against the two pathogens. PMID:20221722

Li, Hai-Yan; Zhao, Chun-An; Liu, Chen-Jian; Xu, Xiao-Fei

2010-02-01

301

Augmentation of natural killer cell activity in vitro against tumor cells by wild plants from Jordan.  

PubMed

Thirteen aqueous extracts prepared from Jordanian plants, that are currently used in traditional medicine to treat various types of cancer, were tested in mice for their ability to augment natural killer (NK) cell function in vitro in generating cytotoxicity against YAC tumor targets. Lymphoid cells at a concentration of 5x10(6)/ml were incubated in medium alone or in medium containing different dilutions of either plant extract or purified interferon alpha for 20 h and tested for NK activity. Maximum NK activity (62. 3%) was obtained at 1:50 dilution of Nigella sativum fresh aqueous extract, 48.5% at 1:100 dilution for Allium sativum (and 38.3% at 1:50 dilution for Onopordum acanthium. Fresh aqueous plant extracts appeared to be more potent than old dried aqueous extract or ethanolic extracts. NK augmentation by plant extracts using nylon wool non-adherent spleen cells was slightly higher than the whole spleen cells. PMID:10904146

Abuharfeil, N M; Maraqa, A; Von Kleist, S

2000-07-01

302

Coffee with cinnamon - impact of phytochemicals interactions on antioxidant and anti-inflammatory in vitro activity.  

PubMed

This paper evaluates the potential bioaccessibility and interactions between antiradical and anti-inflammatory compounds from coffee and cinnamon. Results obtained for whole plant material extracts were compared with those for chlorogenic and cinnamic acids (the main bioactive constituents of the study material). All samples, coffee, cinnamon and a mixture of the two showed abilities to scavenge free radicals and to inhibit lipoxygenase (LOX) activity. Both activities increased after simulated gastrointestinal digestion. In the mixture antiradical phytochemicals acted antagonistically - isoboles adopted the convex form. The same interactions were determined for chemical standards. The water-extractable LOX inhibitors acted synergistically - the isobole curve was "concave". The same type of interaction was determined for standard compounds. Interestingly, after digestion in vitro a slight antagonism in the action of LOX inhibitors was observed. The results show that the food matrix and/or its changes during digestion may play an important role in creating the biological properties. PMID:24874360

Durak, Agata; Gawlik-Dziki, Urszula; Pecio, Lukasz

2014-11-01

303

Impact of fibroblast activation protein on osteosarcoma cell lines in vitro  

PubMed Central

Fibroblast activation protein (FAP) or seprase, which belongs to the group type II integral serine proteases, is an integral membrane serine peptidase. Previous studies have demonstrated that FAP has an effect on tumor growth, proliferation and invasion. However, the cellular functional role that FAP plays in osteosarcoma (OS) remains unknown. The aim of the present study was to investigate the activities of FAP in OS cell lines. The gene expression of FAP was knocked down through a hammerhead ribozyme transgene, and the various functions between the knockdown cells and their control cells were tested using a series of functional assays in vitro. The results indicated that knockdown of FAP markedly reduced the ability of cellular growth, matrix adhesion, migration and invasion in MG-63 and HOS cell lines compared with the control cells (P<0.05). In conclusion, FAP influences OS cells and may play a role in OS tumor progression and metastasis. PMID:24520291

DING, LIXIANG; YE, LIN; XU, JIANLI; JIANG, WEN G.

2014-01-01

304

Antiviral activity of Folium isatidis derived extracts in vitro and in vivo.  

PubMed

Folium isatidis is a native Chinese herbaceous plant widely used for medicinal purposes for thousands of years. However, few studies have focused on the leaves of Isatis indigotica. In this report, we isolated a series of four fractions (I-IV) from Folium isatidis and explored the antiviral activity of each tested extract. The extracts were active against a panel of RNA and DNA viruses in vitro, namely influenza A virus (IAV), coxsackie virus B3 (CVB3), respiratory syncytial virus (RSV), and adenovirus type 7 (Ad-7). Oral administration of 200 mg/kg/d of fraction III in mice exerted strong antiviral effects in viral replication, accompanied by prolonged survival rate, attenuated lung tissue damage as well as significant reductions in pulmonary virus titers and lung index. Our results provide the first biochemical evidence that Folium isatidis and its extracts could be used as potential antiviral agent in the postexposure prophylaxis for multiple viral infections. PMID:23895163

Deng, You-Ping; Liu, Yuan-Yuan; Liu, Zhao; Li, Jin; Zhao, Ling-Min; Xiao, Hong; Ding, Xiao-Hua; Yang, Zhan-Qiu

2013-01-01

305

Antibacterial activity of aqueous extracts of Indian chewing sticks on dental plaque: An in vitro study  

PubMed Central

The anti-microbial efficacy of aqueous extracts of Indian chewing sticks against different kinds of plaque bacteria in vitro was investigated. Supra-gingival plaque is cultured and subjected to the antibacterial activity of the aqueous extracts of chewing sticks (Neem, Acacia, Pongamia glabra, Achyranthes aspera, Streblus asper) separately. The results of the study demonstrate that all the five chewing sticks under study possess inhibitory potential against bacteria present in dental plaque mainly on aerobes. The antibacterial efficacy of aqueous extracts has antibacterial effects and could be used as a therapeutic agent and therefore, it appears to be potent anti-microbial agents that could be considered as a medicinal plant. Results of this study showed chewing sticks contained antibacterial agents, but the concentration and composition of the active substances differed among the plants. PMID:25210357

Rao, Dola Srinivasa; Penmatsa, Tanuja; Kumar, Alapati Kranthi; Reddy, M. Narendra; Gautam, Nalam Sai; Gautam, Nalam Radhika

2014-01-01

306

Selection of a T7 promoter mutant with enhanced in vitro activity by a novel multi-copy bead display approach for in vitro evolution.  

PubMed

In vitro evolution of nucleic acids and proteins is a powerful strategy to optimize their biological and physical properties. To select proteins with the desired phenotype from large gene libraries, the proteins need to be linked to the gene they are encoded by. To facilitate selection of the desired phenotype and isolation of the encoding DNA, a novel bead display approach was developed, in which each member of a library of beads is first linked to multiple copies of a clonal gene variant by emulsion polymerase chain reaction. Beads are transferred to a second emulsion for an in vitro transcription-translation reaction, in which the protein encoded by each bead's amplicon covalently binds to the bead present in the same picoliter reactor. The beads then contain multiple copies of a clonal gene variant and multiple molecules of the protein encoded by the bead's gene variant and serve as the unit of selection. As a proof of concept, we screened a randomized library of the T7 promoter for high expression levels by flow cytometry and identified a T7 promoter variant with an ~10-fold higher in vitro transcriptional activity, confirming that the multi-copy bead display approach can be efficiently applied to in vitro evolution. PMID:23074193

Paul, Siddhartha; Stang, Alexander; Lennartz, Klaus; Tenbusch, Matthias; Überla, Klaus

2013-01-01

307

In vitro antiplasmodial and phytochemical study of five Artemisia species from Iran and in vivo activity of two species  

Microsoft Academic Search

The extract from Artemisia annua, containing artemisinin, has been proven active against multidrug resistant Plasmodium falciparum in previous studies. The purpose of this paper was to study five Artemisia species from Iran for their in vitro and in vivo antimalarial property and detection of artemisinin in the active species by chromatographic and spectroscopic methods including\\u000a nuclear magnetic resonance (NMR) spectroscopy.

Ali Ramazani; Soroush Sardari; Sedigheh Zakeri; Behrouz Vaziri

2010-01-01

308

In Vitro Activities of Nontraditional Antimicrobials against Multiresistant Acinetobacter baumannii Strains Isolated in an Intensive Care Unit Outbreak  

Microsoft Academic Search

Fifteen multiresistant Acinetobacter baumannii isolates from patients in intensive care units and 14 nonout- break strains were tested to determine in vitro activities of nontraditional antimicrobials, including cefepime, meropenem, netilmicin, azithromycin, doxycycline, rifampin, sulbactam, and trovafloxacin. The latter five drugs were further tested against four of the strains for bactericidal or bacteriostatic activity by performing kill-curve studies at 0.5, 1,

MARIA D. APPLEMAN; HOWARD BELZBERG; DIANE M. CITRON; PETER N. R. HESELTINE; ALBERT E. YELLIN; JAMES MURRAY; THOMAS V. BERNE

2000-01-01

309

Antiviral activity of Avicennia marina against herpes simplex virus type 1 and vaccine strain of poliovirus (An in vitro study)  

Microsoft Academic Search

Avicenniaceae family is a member of true mangrove plants which has one genus, 11 species and several subspecies. Avicennia marina is the most current species among these plants in Iranian mangrove forest. Regarding to the presence of many active biological constituents in this plant and their applications in traditional and alternative medicine, the in vitro antiviral activity of its leaf

Keivan Zandi; Marzieh Taherzadeh; Ramin Yaghoubi; Saeed Tajbakhsh; Zahra Rastian; Moradali Fouladvand

2009-01-01

310

In vitro activity of the trinem sanfetrinem (GV104326) against gram-positive organisms.  

PubMed Central

The in vitro activity of the trinem sanfetrinem (formerly GV104326) (GV) was compared with that of vancomycin, ampicillin, and/or nafcillin against 287 gram-positive bacteria, including methicillin-resistant Staphylococcus aureus and multiresistant enterococci, by the agar and microbroth dilution methods. GV demonstrated 2 to 16 times more activity than ampicillin and nafcillin against the majority of these organisms. The MIC range of GV was 16 to 64 micrograms/ml for 19 Enterococcus faecium strains that were highly resistant to ampicillin (ampicillin MIC range, 64 to 512 micrograms/ml) and vancomycin resistant and 0.25 to 32 micrograms/ml for resistant Rhodococcus spp. Similar activities (+/-1 dilution) were observed by either the agar or the broth microdilution method. GV demonstrated bactericidal activity against a beta-lactamase-producing Enterococcus faecalis strain and against two methicillin-susceptible Staphylococcus aureus strains in 10(5)-CFU/ml inocula. Synergy between GV and gentamicin was observed against an E. faecalis strain that lacked high-level gentamicin resistance. The activity of GV suggests this compound warrants further study. PMID:8878596

Singh, K V; Coque, T M; Murray, B E

1996-01-01

311

In vitro cancer cell growth inhibition and antioxidant activity of Bombax ceiba (Bombacaceae) flower extracts.  

PubMed

The flowers of Bombax ceiba were investigated for their chemical composition, antioxidant effects and antiproliferative activity against seven human cancer cell lines. The antiproliferative responses of diethyl ether (DE) and light petroleum (PE) extracts were evaluated by sulforhodamine B (SRB) assay against MCF-7, HeLa, COR-L23, C32, A375, ACHN, and LNCaP cells in comparison with a human normal cell line, 142BR. Moreover, extracts were characterized by GC-MS analysis and tested for their antioxidant properties by different in vitro systems, namely DPPH, Fe-chelating activity and beta-carotene bleaching test. Both PE and DE extracts showed the highest antiproliferative activity against human renal adenocarcinoma (ACHN) in a concentration-dependent manner. PE extract showed the highest radical scavenging activity against the DPPH radical, while DE extract was more active in the beta-carotene bleaching test. The presence of beta-sitosterol and some fatty acids may contribute to the bioactivity of B. ceiba flower extracts. PMID:25026723

Tundis, Rosa; Rashed, Khaled; Said, Ataa; Menichini, Francesco; Loizzo, Monica R

2014-05-01

312

In vitro Effect of Verapamil on Platelet Activation Induced by ADP, Collagen or Thrombin.  

PubMed

We studied the effects in Vitro of the calcium channel blocker verapamil (0.1, 0.2 or 0.3 mM) on platelet aggregation, on cytoplasmic Ca(+ +) levels and on TxB(2) production after activation of platelets with adenosine diphosphate (ADP) (100 µM), collagen (20 µg/ml) or thrombin (1 U/ml). A Platelet Ionized Calcium Aggregometer was used and washed, aequorin loaded platelets were employed. The drug was able to inhibit similarly and always significantly aggregation, Ca(+ +) fluxes and TxB(2) production when collagen was the agonist. Furthermore, inhibition of aggregation and TxB(2) production was significant at all the concentrations tested when platelets were activated by ADP or thrombin, but in this case inhibition of Ca (+ +) fluxes was observed only with the higher concentrations of the drug (0.2 or 0.3 mM). Hence, with these two last agonists inhibition of Ca(+ +) movements was less pronounced than inhibition of aggregation or TxB(2) production. These data suggest that platelet activation by collagen depends directly and almost exclusively on Ca(+ +) fluxes through biological membranes, while activation by ADP or thrombin is less strictly related to Ca(+ +) movements. Indeed, with these last two agonists verapamil may inhibit platelet activation also by calcium-independent mechanism(s). PMID:21043728

Brocchieri, A; Pacchiarini, L; Saporiti, A; Grignani, G

1995-01-01

313

Studies on in vitro paraquat and diquat removal by activated carbon.  

PubMed

The adsorption characteristics of paraquat and diquat onto activated carbon in vitro were discussed for the primary treatment of acute poisoning by accidental, suicidal or homicidal ingestion of paraquat containing herbicides. Paraquat was adsorbed onto activated carbon more abundantly and more rapidly in physiological saline solution than that in artificial gastric juice and distilled water. Most suitable solvent for paraquat removal by activated carbon was physiological saline solution (0.9% sodium chloride solution). No significant correlation was observed between the ability of paraquat removal and the properties of adsorbent. Paraquat was preferentially adsorbed onto activated carbon in the mixed solution. The adsorption abilities by activated carbon (the removal ratio, the amount adsorbed and the adsorption rate) for paraquat were larger than those for diquat, and it was enhanced by added sodium chloride and added magnesium sulfate. Enhancing effect for adsorption removal was proportional to the saline concentration. As addition of salts into carbon suspension enhanced the adsorption ability, it will contribute to the effective treatment of acute poisoning. PMID:7940530

Terada, H; Miyoshi, T; Imaki, M; Nakamura, T; Tanada, S

1994-06-01

314

In vitro antiplasmodial activity of benzophenones and xanthones from edible fruits of Garcinia species.  

PubMed

Species of Garcinia have been used to combat malaria in traditional African and Asian medicines, including Ayurveda. In the current study, we have identified antiplasmodial benzophenone and xanthone compounds from edible Garcinia species by testing for in vitro inhibitory activity against Plasmodium falciparum. Whole fruits of Garcinia xanthochymus, G. mangostana, G. spicata, and G. livingstonei were extracted and tested for antiplasmodial activity. Garcinia xanthochymus was subjected to bioactivity-guided fractionation to identify active partitions. Purified benzophenones (1-9) and xanthones (10-18) were then screened in the plasmodial lactate dehydrogenase assay and tested for cytotoxicity against mammalian (Vero) cells. The benzophenones guttiferone E (4), isoxanthochymol (5), and guttiferone H (6), isolated from G. xanthochymus, and the xanthones ?-mangostin (15), ?-mangostin (16), and 3-isomangostin (17), known from G. mangostana, showed antiplasmodial activity with IC50 values in the range of 4.71-11.40 µM. Artemisinin and chloroquine were used as positive controls and exhibited IC50 values in the range of 0.01-0.24 µM. The identification of antiplasmodial benzophenone and xanthone compounds from G. xanthochymus and G. mangostana provides evidence for the antiplasmodial activity of Garcinia species and warrants further investigation of these fruits as dietary sources of chemopreventive compounds. PMID:24963617

Lyles, James T; Negrin, Adam; Khan, Shabana I; He, Kan; Kennelly, Edward J

2014-06-01

315

Inhibition mechanism of lanthanum ion on the activity of horseradish peroxidase in vitro  

NASA Astrophysics Data System (ADS)

In order to understand the inhibition mechanism of lanthanum ion (La 3+) on the activity of horseradish peroxidase (HRP), the effects of La 3+ on the activity, electron transfer and conformation of HRP in vitro were investigated by using cyclic voltammetry (CV), atomic force microscopy (AFM), circular dichroism (CD), high performance liquid chromatography (HPLC), matrix-assisted laser desorption/ionization time-of-flight mass spectroscopy (MALDI-TOF/MS) and inductively coupled plasma mass spectrometry (ICP-MS). It was found that La 3+ can combine with the amide groups of the polypeptide chain in HRP molecule, forming the complex of La 3+ and HRP (La-HRP). The formation of the La-HRP complex causes the destruction of the native structure of HRP molecule, leading to the decrease in the non-planarity of the porphyrin ring in the heme group of HRP molecule, and then in the exposure extent of active center, Fe(III) of the porphyrin ring of HRP molecule. Thus, the direct electrochemical and catalytic activities of HRP are decreased. It is a possible inhibition mechanism of La 3+ on the activity of peroxidase.

Guo, Shaofen; Wang, Lihong; Lu, Aihua; Lu, Tianhong; Ding, Xiaolan; Huang, Xiaohua

2010-02-01

316

In vitro and in vivo activities of anti-influenza virus compound T-705.  

PubMed

T-705 (6-fluoro-3-hydroxy-2-pyrazinecarboxamide) has been found to have potent and selective inhibitory activity against influenza virus. In an in vitro plaque reduction assay, T-705 showed potent inhibitory activity against influenza A, B, and C viruses, with 50% inhibitory concentrations (IC(50)s) of 0.013 to 0.48 microg/ml, while it showed no cytotoxicity at concentrations up to 1,000 microg/ml in Madin-Darby canine kidney cells. The selectivity index for influenza virus was more than 2,000. It was also active against a neuraminidase inhibitor-resistant virus and some amantadine-resistant viruses. T-705 showed weak activity against non-influenza virus RNA viruses, with the IC(50)s being higher for non-influenza virus RNA viruses than for influenza virus, and it had no activity against DNA viruses. Orally administered T-705 at 100 mg/kg of body weight/day (four times a day) for 5 days significantly reduced the mean pulmonary virus yields and the rate of mortality in mice infected with influenza virus A/PR/8/34 (3 x 10(2) PFU). These results suggest that T-705 may be a compound that is useful and highly selective against influenza virus infections and that has a mode of action different from those of commercially available drugs, such as amantadine, rimantadine, and neuraminidase inhibitors. PMID:11897578

Furuta, Y; Takahashi, K; Fukuda, Y; Kuno, M; Kamiyama, T; Kozaki, K; Nomura, N; Egawa, H; Minami, S; Watanabe, Y; Narita, H; Shiraki, K

2002-04-01

317

In vitro and ex vivo activity of peptide deformylase inhibitors against Mycobacterium tuberculosis H37Rv.  

PubMed

Bacterial peptide deformylase (PDF) catalyses removal of the N-terminal formyl group of proteins and is essential for protein maturation, growth and survival of bacteria. Thus, PDF appears to be a good antimycobacterial drug target. In the present study, various well-known PDF inhibitors, such as BB-3497, actinonin, 1,10-phenanthroline, hydroxylamine hydrochloride and galardin, were selected to evaluate their inhibitory activity against Mycobacterium tuberculosis. All compounds were found to be active against M. tuberculosis, with MIC(90) values (lowest drug concentration at which 90% of growth was inhibited on the basis of CFU enumeration) ranging from 0.2 mg/L to 74 mg/L. BB-3497 and 1,10-phenanthroline exhibited potent in vitro antimycobacterial activity, and also showed synergism with isoniazid and rifampicin. All compounds showed a bacteriostatic mode of inhibition. Under ex vivo conditions and short-course chemotherapy, BB-3497 and actinonin were found to be significantly active, with BB-3497 exhibiting comparable efficacy to that of isoniazid. Collectively, promising activities of PDF inhibitors such as BB-3497 and actinonin suggest their potential use against M. tuberculosis. PMID:19505802

Sharma, Anshika; Sharma, Sadhna; Khuller, G K; Kanwar, A J

2009-09-01

318

Effects of interleukin-2 and interleukin-2-activated cells on in vitro myelopoiesis.  

PubMed Central

Lymphokine-activated killer (LAK) cells from human peripheral blood mononuclear cells cultured with recombinant interleukin-2 (IL-2) have been used clinically in adoptive immunotherapy for cancer patients. To study the influence of LAK cells and IL-2 on haematopoiesis, an in vitro assay system for colony formation of granulocyte-macrophage progenitor cells (GM-CFC) was used. LAK cells from cultures of either human peripheral blood (PB) or human bone marrow (BM) mononuclear cells were both inhibitory to allogeneic BM-derived GM-CFC. Inhibitory activity could be transferred with supernatants from co-cultures of LAK cells and BM targets, but also from the IL-2 activated PB- or BM-derived cells alone. The inhibitory activity from the initially non-cytotoxic/non-inhibitory BM population was rapidly induced by IL-2 activation, and preceded the generation of cytotoxic LAK cells in the culture. These experiments show that inhibition of haematopoietic progenitor cells by IL-2 is not dependent on generation of cytotoxic LAK cells, but rather the result of IL-2-induced cytokine production. We conclude that the synergistic action of interferon-gamma (IFN-gamma) and tumour necrosis factor-alpha (TNF-alpha) may contribute to inhibition, but that also other cytokines are responsible for the observed inhibition of BM-derived GM-CFC. PMID:2118847

Clerigue, M; Pisa, P; Tsai, L; Hanson, M

1990-01-01

319

In vitro evaluation of antimicrobial activity of the freshwater sponge Ochridaspongia rotunda (Arndt, 1937).  

PubMed

The antimicrobial activity of five crude extracts (aqueous, methanol, ethyl acetate, acetone and methylene chloride) of the freshwater sponge Ochridaspongia rotunda (Arndt, 1937) was evaluated in vitro by using microdilution method against eight bacterial and eight fungal strains for the first time. The extracts were proven to be active in varying degrees against all the bacteria and fungi tested. O. rotunda methanol extract exhibited the highest antibacterial activity (minimum inhibitory concentration (MIC) 7.5-15.0 ?g/mL and minimum bactericidal concentration 15-30 ?g/mL), while its acetone extract exhibited the most promising antifungal activity (MIC 7.5-45.0 ?g/mL and minimum fungicidal concentration 15-60 ?g/mL). The extracts were more effective against the bacteria and fungi screened compared with the positive controls (streptomycin and ampicillin for bacteria and bifonazole and ketoconazole for fungi, respectively). According to the experimental data obtained, this deepwater sponge species may be considered as a gold mine of new antimicrobial substances with significant and broad-range activity. PMID:24804931

Pejin, Boris; Talevski, Aleksandra; Ciric, Ana; Glamoclija, Jasmina; Nikolic, Milos; Talevski, Trajce; Sokovic, Marina

2014-01-01

320

In vitro screening of traditional medicines for anti-HIV activity: memorandum from a WHO meeting.  

PubMed Central

Many plant products are being used by patients with acquired immunodeficiency syndrome (AIDS) in some countries without any scientific proof that they possess anti-HIV (human immunodeficiency virus) activity. Traditional healers are now offering their remedies for scientific evaluation, and a few studies provide information on the inhibitory activity against HIV of plants such as Viola yedoensis, Arctium lappa, Epimedium grandiflorum, Glycyrrhiza uralensis and Castanospermum australe. Natural products can be selected for biological screening based on ethnomedical use, random collection or a chemotaxonomic approach (i.e., screening of species of the same botanical family for similar compounds), but the follow-up and selection of plants based on literature leads would seem to be the most cost-effective way of identifying plants with anti-HIV activity. No single in vitro screening methodology for anti-HIV activity is ideal and confirmatory assays in multiple systems are needed to examine completely the potential use of a compound. To promote further research in traditional medicine and AIDS, appropriate institutions will be identified where the different activities for the scientific evaluation of plants and their extracts for possible treatment of AIDS can be carried out. PMID:2633879

1989-01-01

321

Phosphorylated H2AX in parthenogenetically activated, in vitro fertilized and cloned bovine embryos.  

PubMed

Summary In vitro embryo production methods induce DNA damage in the embryos. In response to these injuries, histone H2AX is phosphorylated (?H2AX) and forms foci at the sites of DNA breaks to recruit repair proteins. In this work, we quantified the DNA damage in bovine embryos undergoing parthenogenetic activation (PA), in vitro fertilization (IVF) or somatic cell nuclear transfer (SCNT) by measuring ?H2AX accumulation at different developmental stages: 1-cell, 2-cell and blastocyst. At the 1-cell stage, IVF embryos exhibited a greater number of ?H2AX foci (606.1 ± 103.2) and greater area of ?H2AX staining (12923.6 ± 3214.1) than did PA and SCNT embryos. No differences at the 2-cell stage were observed among embryo types. Although PA, IVF and SCNT were associated with different blastocyst formation rates (31.1%, 19.7% and 8.3%, P < 0.05), no differences in the number of ?H2AX foci or area were detected among the treatments. ?H2AX is detected in bovine preimplantation embryos produced by PA, IVF and SCNT; the amount of DNA damage was comparable among those embryos developing to the blastocyst stage among different methods for in vitro embryo production. While IVF resulted in increased damage at the 1-cell embryo stage, no difference was observed between PA and SCNT embryos at any developmental stage. The decrease in the number of double-stranded breaks at the blastocyst stage seems to indicate that DNA repair mechanisms are functional during embryo development. PMID:24735637

Pereira, A F; Melo, L M; Freitas, V J F; Salamone, D F

2014-04-15

322

An in Vitro Antimicrobial Activity of Ten Iranian-Made Toothpastes  

PubMed Central

Background: Antimicrobial agents have been used as a chemotherapeutic agent to improve oral health. This in vitro study was carried out to determine the antimicrobial activity of ten Iranian-made toothpastes against commonly found bacteria in the oral cavity. Methods: The microorganisms used in this study were Streptococcus mutans, Streptococcus sanguis, Actinomyces viscosus and Candida albicans. Sterile discs impregnated with 10 Iranian-made toothpastes; Paveh, Saviz, Latifeh II, Bath, Darugar II, Darugar I, Close up, Tage, Pooneh III and Nasim, which were separately used on agar plates. Crest Cavity Protection toothpaste and Sterile pyrogenfree distilled water were used as positive and negative controls, respectively. The samples were tested in triplicate, at full strength, 1:1 and 1:3 dilutions. Inhibition zones were measured in millimeter after 48 hr. The data were analyzed by the ANOVA and t-test. Results: All tested toothpastes demonstrated an antimicrobial activity. The antimicrobial activity of Bath on S. mutans, Paveh on S. sanguis, Paveh, Saviz, Latifeh III and Darugar II on C. albicans were similar to the activity of Crest Cavity Protection. The antimicrobial activity of Pooneh III and Nasim on S. mutans, Bath on S. sanguis and A. viscosus, and Bath and Pooneh III on C. albicans were significantly higher and the others were significantly lower than the positive control. While, the activity of Crest Cavity Protection was the same as Pooneh III, it showed a weaker activity compared with Bath. Conclusion: Apart from Bath and Pooneh III, the other Iranian-made toothpastes tested in this study showed a lower antimicrobial activity compared to Crest Cavity Protection. PMID:21528037

Sadeghi, Mostafa; Assar, Shokrollah

2009-01-01

323

Vaticanol C, a resveratrol tetramer, activates PPAR? and PPAR?/? in vitro and in vivo  

PubMed Central

Background Appropriate long-term drinking of red wine is associated with a reduced risk of cardiovascular disease. Resveratrol, a well-known SIRT1 activator is considered to be one of the beneficial components contained in red wine, and also developed as a drug candidate. We previously demonstrated that resveratrol protects brain against ischemic stroke in mice through a PPAR?-dependent mechanism. Here we report the different effects of the oligomers of resveratrol. Methods We evaluated the activation of PPARs by ?-viniferin, a resveratrol dimer, and vaticanol C, a resveratrol tetramer, in cell-based reporter assays using bovine arterial endothelial cells, as well as the activation of SIRT1. Moreover, we tested the metabolic action by administering vaticanol C with the high fat diet to wild-type and PPAR?-knockout male mice for eight weeks. Results We show that vaticanol C activates PPAR? and PPAR?/? in cell-based reporter assays, but does not activate SIRT1. ?-Viniferin shows a similar radical scavenging activity as resveratrol, but neither effects on PPARs and SIRT-1. Eight-week intake of vaticanol C with a high fat diet upregulates hepatic expression of PPAR?-responsive genes such as cyp4a10, cyp4a14 and FABP1, and skeletal muscle expression of PPAR?/?-responsive genes, such as UCP3 and PDK4 (pyruvate dehydrogenase kinase, isoform 4), in wild-type, but not PPAR?-knockout mice. Conclusion Vaticanol C, a resveratrol tetramer, activated PPAR? and PPAR?/? in vitro and in vivo. These findings indicate that activation of PPAR? and PPAR?/? by vaticanol C may be a novel mechanism, affording beneficial effects against lifestyle-related diseases. PMID:20504373

2010-01-01

324

In Vitro and In Vivo Activities of Chios Mastic Gum Extracts and Constituents against Helicobacter pylori?  

PubMed Central

The extracts and pure major constituents of Chios mastic gum (resin of Pistacia lentiscus var. chia) were tested for their activities against Helicobacter pylori. A total mastic extract without polymer (TMEWP) was prepared after removal of the contained insoluble polymer in order to ameliorate solubility and enhance in vivo activity. Administration of TMEWP to H. pylori SS1-infected mice over the period of 3 months with an average dose of 0.75 mg/day led to an approximately 30-fold reduction in the H. pylori colonization (1.5 log CFU/g of tissue). However, no attenuation in the H. pylori-associated chronic inflammatory infiltration and the activity of chronic gastritis was observed. To further characterize potential active mastic constituents, the TMEWP was separated into an acidic and a neutral fraction. Both were extensively characterized by nuclear magnetic resonance and mass spectroscopy to elucidate the structure of the components contained within each fraction. After chromatographic separation, the acid fraction gave the major triterpenic acids, while the neutral fraction gave several triterpenic alcohols and aldehydes. Mastic extracts and isolated pure triterpenic acids were tested for in vitro activity against a panel of 11 H. pylori clinical strains. The acid fraction was found to be the most active extract (minimum bactericidal concentration [MBC], 0.139 mg/ml), and the most active pure compound was isomasticadienolic acid (MBC, 0.202 mg/ml [0.443 mM]). Our results show that administration of TMEWP may be effective in reducing H. pylori colonization and that the major triterpenic acids in the acid extract may be responsible for such an activity. PMID:17116667

Paraschos, Sotirios; Magiatis, Prokopios; Mitakou, Sofia; Petraki, Kalliopi; Kalliaropoulos, Antonios; Maragkoudakis, Petros; Mentis, Andreas; Sgouras, Dionyssios; Skaltsounis, Alexios-Leandros

2007-01-01

325

Comparative study of the in vitro inflammatory activity of three nickel salts on keratinocytes.  

PubMed

Nickel, the allergen of contact dermatitis, induces the in vitro production of inflammation markers such as intracellular adhesion molecule-1, interleukin-1 and tumour necrosis factor-alpha by keratinocytes. The purpose of our study was to compare the effect in vitro of different nickel salts on keratinocyte activation in order to determine whether this process depends on the nature of the salt used. Cultured keratinocytes were incubated with three nickel salts for 24 h in MCDB153 medium without hydrocortisone. Nickel gluconate, nickel sulphate and nickel chloride were each used at four concentrations: 5.10(-5) M, 1.10(-4) M and 1.10 (-3) M. Keratinocyte activation was studied through the production of three inflammation markers: intracellular adhesion molecule-1, tumour necrosis factor-alpha and very late antigen-3 (an integrin with increased expression during contact dermatitis). Marker production was detected by immunocytochemistry and flow cytometry. Tumour necrosis factor-alpha production and intracellular adhesion molecule-1 and very late antigen-3 expression increased with addition of the three nickel salts, becoming maximal for nickel gluconate 1.10(-4) M. In a subsequent experiment, zinc gluconate (an anti-inflammatory molecule) at 9 micrograms/ml reduced the very late antigen-3 expression induced by nickel gluconate 1.10(-4) M. Therefore, this study enabled us to determine the concentration of a nickel salt (nickel gluconate) inducing optimal keratinocyte activation in our culture conditions and also indicated the potential interest of very late antigen-3 as an inflammation marker. PMID:9602219

Sainte-Marie, I; Jumbou, O; Tenaud, I; Dreno, B

1998-05-01

326

Antioxidant activity of Smoke Shield in-vitro and in-vivo.  

PubMed

Smoke Shield is a proprietory formulation containing extract of turmeric (Curcuma longa), obtained by supercritical carbon dioxide gas extraction and post-supercritical hydroethanolic extraction, together with extracts of green tea and other spices whose presence synergistically increases the activity of turmeric. This study evaluates the antioxidant potentials of Smoke Shield in-vitro and in experimental animals, as well as in human models. Smoke Shield was found to scavenge superoxide radicals generated by photoreduction of riboflavin (50% inhibitory concentration = 91 microg mL(-1)) and hydroxyl radicals generated by Fenton reaction (50% inhibitory concentration = 95 microg mL(-1)) and reduced lipid peroxidation. Administration of Smoke Shield to mice was found to elevate antioxidant enzymes such as catalase and superoxide dismutase in blood as well as in liver and kidney. Glutathione-S-transferase activity was found to be significantly elevated in liver and kidney of animals treated with Smoke Shield. Glutathione levels were also significantly elevated in blood. Glutathione reductase was significantly elevated in kidney. Administration of Smoke Shield decreased the lipid peroxidation in serum, liver and kidney, as well as reduced the levels of conjugated dienes and hydroperoxides. Administration of Smoke Shield to smokers was found to increase the superoxide dismutase and glutathione in blood and decrease glutathione peroxidase. Smoke Shield inhibited phase I enzymes as represented by aniline-hydroxylase and aminopyrenedemethylase in-vitro. These results indicate that Smoke Shield has potent antioxidant activity, could inhibit phase I enzymes and increase detoxifying enzymes, which makes it an effective chemoprotective herbal formulation. PMID:12841947

Sreekanth, Kavitha Sivaraman; Sabu, Mandumpal Chacko; Varghese, Leyon; Manesh, Chittezhath; Kuttan, Girija; Kuttan, Ramadasan

2003-06-01

327

In Vitro and In Vivo Activity of an Organic Tellurium Compound on Leishmania (Leishmania) chagasi  

PubMed Central

Tellurium compounds have shown several biological properties and recently the leishmanicidal effect of one organotellurane was demonstrated. These findings led us to test the effect of the organotellurium compound RF07 on Leishmania (Leishmania) chagasi, the agent of visceral leishmaniasis in Latin America. In vitro assays were performed in L. (L.) chagasi-infected bone marrow derived macrophages treated with different concentrations of RF07. In in vivo experiments Golden hamsters were infected with L. (L.) chagasi and injected intraperitoneally with RF07 whereas control animals received either Glucantime or PBS. The effect of RF07 on cathepsin B activity of L. (L.) chagasi amastigotes was assayed spectrofluorometrically using fluorogenic substrates. The main findings were: 1) RF07 showed significant leishmanicidal activity against intracellular parasites at submicromolar concentrations (IC50 of 529.7±26.5 nM), and the drug displayed 10-fold less toxicity to macrophages (CC50 of 5,426±272.8 nM); 2) kinetics assays showed an increasing leishmanicidal action of RF07 at longer periods of treatment; 3) one month after intraperitoneal injection of RF07 L. (L.) chagasi-infected hamsters showed a reduction of 99.6% of parasite burden when compared to controls that received PBS; 4) RF07 inhibited the cathepsin B activity of L. (L.) chagasi amastigotes. The present results demonstrated that the tellurium compound RF07 is able to destroy L. (L.) chagasi in vitro and in vivo at concentrations that are non toxic to the host. We believe these findings support further study of the potential of RF07 as a possible alternative for the chemotherapy of visceral leishmaniasis. PMID:23144968

Pimentel, Isabella Aparecida Salerno; Paladi, Carolina de Siqueira; Katz, Simone; Júdice, Wagner Alves de Souza; Cunha, Rodrigo L. O. R.; Barbiéri, Clara Lúcia

2012-01-01

328

Protective activity of guanosine in an in vitro model of Parkinson's disease.  

PubMed

Parkinson's disease (PD) is a pathological condition characterized by a progressive neurodegeneration of dopaminergic neurons with the consequent reduction of dopamine content in the substantia nigra. The neurotoxin 6-hydroxydopamine (6-OHDA) is widely used to mimic the neuropathology of PD in both in vivo and in vitro experimental models. We found that, as expected, in dopaminergic human SH-SY5Y neuroblastoma cells the toxin reduced cell viability causing programmed cell death as assessed by an increase in DNA fragmentation. We also examined, in these cells, the activation/inactivation of several pro and anti apoptotic signaling pathways by 6-OHDA including p-38 kinase (p-38), c-Jun N-terminal kinase (JNK), protein kinase B (also known as Akt), glycogen synthase kinase-3? (GSK3?), and Bcl-2 protein. Guanine-based purines, exert neuroprotective effects and we previously reported that guanosine activates cell survival pathways including PI3K/Akt/PKB signaling in different kinds of cells including glia and neuroblastoma cells. In the present study we found that guanosine (300 µM) protected SH-SY5Y neuroblastoma cells when they were exposed to 6-OHDA, promoting their survival. Guanosine reduced the 6-OHDA mediated activation of p-38 and JNK. Moreover the nucleoside potentiated the early increase in the phosphorylation of the anti-apoptotic kinase Akt and the increase in the expression of the anti-apoptotic Bcl-2 protein induced by 6-OHDA. In summary our results show that guanosine results to be neuroprotective in a recognized in vitro model of PD thus suggesting that it could represent a new potential pharmacological tool to be studied in the therapeutic approach to PD. PMID:23241934

Giuliani, P; Romano, S; Ballerini, P; Ciccarelli, R; Petragnani, N; Cicchitti, S; Zuccarini, M; Jiang, S; Rathbone, M P; Caciagli, F; Di Iorio, P

2012-12-01

329

Shc depletion stimulates brown fat activity in vivo and in vitro.  

PubMed

Adipose tissue is an important metabolic organ that integrates a wide array of homeostatic processes and is crucial for whole-body insulin sensitivity and energy metabolism. Brown adipose tissue (BAT) is a key thermogenic tissue with a well-established role in energy expenditure. BAT dissipates energy and protects against both hypothermia and obesity. Thus, BAT stimulation therapy is a rational strategy for the looming pandemic of obesity, whose consequences and comorbidities have a huge impact on the aged. Shc-deficient mice (ShcKO) were previously shown to be lean, insulin sensitive, and resistant to high-fat diet and obesity. We investigated the contribution of BAT to this phenotype. Insulin-dependent BAT glucose uptake was higher in ShcKO mice. Primary ShcKO BAT cells exhibited increased mitochondrial respiration; increased expression of several mitochondrial and lipid-oxidative enzymes was observed in ShcKO BAT. Levels of brown fat-specific markers of differentiation, UCP1, PRDM16, ELOVL3, and Cox8b, were higher in ShcKO BAT. In vitro, Shc knockdown in BAT cell line increased insulin sensitivity and metabolic activity. In vivo, pharmacological stimulation of ShcKO BAT resulted in higher energy expenditure. Conversely, pharmacological inhibition of BAT abolished the improved metabolic parameters, that is the increased insulin sensitivity and glucose tolerance of ShcKO mice. Similarly, in vitro Shc knockdown in BAT cell lines increased their expression of UCP1 and metabolic activity. These data suggest increased BAT activity significantly contributes to the improved metabolic phenotype of ShcKO mice. PMID:25257068

Tomilov, Alexey; Bettaieb, Ahmed; Kim, Kyoungmi; Sahdeo, Sunil; Tomilova, Natalia; Lam, Adam; Hagopian, Kevork; Connell, Michelle; Fong, Jennifer; Rowland, Douglas; Griffey, Stephen; Ramsey, Jon; Haj, Fawaz; Cortopassi, Gino

2014-12-01

330

Virtual Screening Analysis and In-vitro Xanthine Oxidase Inhibitory Activity of Some Commercially Available Flavonoids  

PubMed Central

Allopurinol, the xanthine oxidase inhibitor, is the only drug available for the treatment of gout. We examined the xanthine oxidase inhibitory activity of some commercially available flavonoids such asepigallocatechin, acacatechin, myricetin, naringenin, daidzein and glycitein by virtual screening and in-vitro studies. The interacting residues within the complex model and their contact types were identified. The virtual screening analysis were carried out using AutoDock 4.2 and in-vitro xanthine oxidase inhibitory activity was carried out using xanthine as the substrate. In addition, enzyme kinetics was performed using LineweaverBurkplot analysis. Allopurinol, a known xanthine oxidase inhibitor was used as the standard. The docking energy ofglycitein was found to be -8.49 kcal/mol which was less than that of the standard (-4.47 kcal/ mol). All the selected flavonoids were found to exhibit lower binding energy (-8.08 to -6.03 kcal/ mol) than allopurinol. The docking results confirm that flavonoids showed greater inhibition of xanthine oxidase due to their active binding sites and lesser binding energies compared to allopurinol. This may be attributed to the presence of benzopyran ring in the flavonoids. In the xanthine oxidase assay, IC50 value of glycitein was found to be 12±0.86 ?g/mL, whereas that of allopurinol was 24±0.28 ?g/mL. All the remaining compounds exhibited IC50 values ranging between 22±0.64 to 62±1.18 ?g/mL. In the enzyme kinetic studies, flavonoids showed competitive type of enzyme inhibition. It can be concluded that flavonoids could be a promising remedy for the treatment of gout and related inflammatory disorders. Further in-vivo studies are required to develop potential compounds with lesser side effects. PMID:24250638

Umamaheswari, Muthuswamy; Madeswaran, Arumugam; Asokkumar, Kuppusamy

2013-01-01

331

Mechanism of Action and Capsid-Stabilizing Properties of VHHs with an In Vitro Antipolioviral Activity  

PubMed Central

ABSTRACT Previously, we reported on the in vitro antiviral activity of single-domain antibody fragments (VHHs) directed against poliovirus type 1. Five VHHs were found to neutralize poliovirus type 1 in an in vitro setting and showed 50% effective concentrations (EC50s) in the nanomolar range. In the present study, we further investigated the mechanism of action of these VHHs. All five VHHs interfere at multiple levels of the viral replication cycle, as they interfere both with attachment of the virus to cells and with viral uncoating. The latter effect is consistent with their ability to stabilize the poliovirus capsid, as observed in a ThermoFluor thermal shift assay, in which the virus is gradually heated and the temperature causing 50% of the RNA to be released from the capsid is determined, either in the presence or in the absence of the VHHs. The VHH-capsid interactions were also seen to induce aggregation of the virus-VHH complexes. However, this observation cannot yet be linked to their mechanism of action. Cryo-electron microscopy (cryo-EM) reconstructions of two VHHs in complex with poliovirus type 1 show no conformational changes of the capsid to explain this aggregation. On the other hand, these reconstructions do show that the binding sites of VHHs PVSP6A and PVSP29F overlap the binding site for the poliovirus receptor (CD155/PVR) and span interfaces that are altered during receptor-induced conformational changes associated with cell entry. This may explain the interference at the level of cell attachment of the virus as well as their effect on uncoating. IMPORTANCE The study describes the mechanism of neutralization and the capsid-stabilizing activity of five single-domain antibody fragments (VHHs) that have an in vitro neutralizing activity against poliovirus type 1. The results show that the VHHs interfere at multiple levels of the viral replication cycle (cell attachment and viral uncoating). These mechanisms are possibly shared by some conventional antibodies and may therefore provide some insight into the natural immune responses. Since the binding sites of two VHHs studied by cryo-EM are very similar to that of the receptor, the VHHs can be used as probes to study the authentic virus-cell interaction. The structures and conclusions in this study are original and raise interesting findings regarding virus-receptor interactions and the order of key events early in infection. PMID:24501405

Schotte, Lise; Strauss, Mike; Thys, Bert; Halewyck, Hadewych; Filman, David J.; Bostina, Mihnea; Rombaut, Bart

2014-01-01

332

Biological extraction of realgar by Acidithiobacillus ferrooxidans and its in vitro and in vivo antitumor activities.  

PubMed

Acidithiobacillus ferrooxidans is a Gram-negative, chemolithoautotrophic bacterium involved in metal bioleaching. It is used for the extraction of coarse medical realgar, which is converted into an aqueous solution. To prove its feasibility as an anticancer drug candidate, extracted realgar (ER/Af) was evaluated for its antitumor activities both in vitro and in vivo. In cytotoxicity tests, ER/Af displayed significant inhibition on cell proliferation of HepG2, SMMC7721, and H22 cells in a time and dose dependent manner. Remarkable tumor growth inhibition and survival time prolongation effects, along with no obvious toxicity, were observed in antitumor experiments against H22 cell-bearing mice. Apoptosis induction was also confirmed as one of the mechanisms involved in the efficacy of ER/Af both in vitro and in vivo. The most important observation is that ER/Af showed high selective affinity to tumor tissues with about eight-fold higher arsenic accumulations at the tumor site of mice than those of the arsenic trioxide (ATO)-treated group at the same dose (57.8 +/- 3.34 microg/g dry tissue vs. 7.6 +/- 0.88 microg/g dry tissue). In conclusion, A. ferrooxidans could be successfully used for the extraction of realgar and ER/Af was proved to be a promising anticancer drug candidate, which is valuable for further study and clinical trials. PMID:20645754

Zhang, Xu; Xie, Qin-Jian; Wang, Xin; Wang, Bo; Li, Hong-Yu

2010-01-01

333

In vitro germicidal activity of teat dips against Nocardia asteroides and other udder pathogens.  

PubMed

Nine commercial teat dip formulations containing 1.94% linear dodecylbenzene sulfonic acid, or 1% available iodine from nonylphenoxypoly (ethyleneoxy) ethanol-iodine complex, or .5% chlorhexidine acetate were tested for contamination with aerobic and anaerobic bacteria and their in vitro germicidal activity against Staphylococcus aureus, Streptococcus agalactiae, Escherichia coli, and Nocardia asteroides. All products were free of bacteria when neutralized samples were tested on blood agar or liquid thioglycollate media. To test for in vitro efficacy, each teat dip preparation was mixed with a suspension of one of the pathogenic test organisms containing 10(8) bacteria/ml (final concentration) for .5 to 15 min. Viable bacteria were evaluated by direct plating of neutralized aliquots and by filtration techniques. All products were effective against E. coli, Staph. aureus, and Strep. agalactiae. With N. asteroides, the direct plating method gave equivocal results. The filtration experiments indicated that all teat dips containing dodecylbenzene sulfonic acid and nonylphenoxypoly (ethyleneoxy) ethanol-iodine complex were effective against all four pathogens. Three of the teat dips containing chlorhexidine acetate were ineffective against N. asteroides. The fourth teat dip, containing chlorhexidine acetate and an emollient, was partially effective. PMID:1597578

Larocque, L; Malik, S S; Landry, D A; Presseault, S; Sved, S; Matula, T

1992-05-01

334

Acute lipopolysaccharide exposure facilitates epileptiform activity via enhanced excitatory synaptic transmission and neuronal excitability in vitro  

PubMed Central

Growing evidence indicates brain inflammation has been involved in the genesis of seizures. However, the direct effect of acute inflammation on neuronal circuits is not well known. Lipopolysaccharide (LPS) has been used extensively to stimulate brain inflammatory responses both in vivo and in vitro. Here, we observed the contribution of inflammation induced by 10 ?g/mL LPS to the excitability of neuronal circuits in acute hippocampal slices. When slices were incubated with LPS for 30 minutes, significant increased concentration of tumor necrosis factor ? and interleukin 1? were detected by enzyme-linked immunosorbent assay. In electrophysiological recordings, we found that frequency of epileptiform discharges and spikes per burst increased 30 minutes after LPS application. LPS enhanced evoked excitatory postsynaptic currents but did not modify evoked inhibitory postsynaptic currents. In addition, exposure to LPS enhanced the excitability of CA1 pyramidal neurons, as demonstrated by a decrease in rheobase and an increase in action potential frequency elicited by depolarizing current injection. Our observations suggest that acute inflammation induced by LPS facilitates epileptiform activity in vitro and that enhancement of excitatory synaptic transmission and neuronal excitability may contribute to this facilitation. These results may provide new clues for treating seizures associated with brain inflammatory disease. PMID:25170268

Gao, Fei; Liu, Zhiqiang; Ren, Wei; Jiang, Wen

2014-01-01

335

New in vitro method for evaluating antiviral activity of acyclic nucleoside phosphonates against plant viruses.  

PubMed

A new method was developed for testing antiviral compounds against plant viruses based on rapidly growing brassicas in vitro on liquid medium. This method enables exchange of media containing tested chemicals in various concentrations and simultaneous evaluation of their phytotoxicity and antiviral activity. While using ribavirin as a standard for comparison, phytotoxicity and ability of the acyclic nucleotide analogues (R)-PMPA, PMEA, PMEDAP, and (S)-HPMPC to eliminate ssRNA Turnip yellow mosaic virus (TYMV) were evaluated by this method. Double antibody sandwich ELISA and real-time PCR were used for relative quantification of viral protein and nucleic acid in plants. Ribavirin had the most powerful antiviral effect against TYMV. On the other hand, (R)-PMPA and PMEA had no antiviral effect and almost no phytotoxicity compared to the control. (S)-HPMPC and PMEDAP showed moderate antiviral effect, accompanied by higher phytotoxicity. The tested compounds can be screened within 6-9 weeks in contrast to the 6 months for traditionally used explants on solid medium. The method enables large-scale screening of potential antivirals for in vitro elimination of viruses from vegetatively propagated crops and ornamentals. PMID:20933018

Spak, J; Holý, A; Pavingerová, D; Votruba, I; Spaková, V; Petrzik, K

2010-12-01

336

In vitro and in vivo anthelmintic activity of Euphorbia helioscopia L.  

PubMed

The anthelmintic potentials of the aqueous and methanol extracts of Euphorbia helioscopia were investigated. In folklore medicine, E. helioscopia (Euphorbiaceae) is used in the treatment of various gastrointestinal ailments and diseases. A worm motility inhibition (WMI) assay and egg hatch assay (EHA) were used for in vitro assessment, and a faecal egg count reduction (FECR) assay was used for an in vivo study. The in vitro study revealed anthelmintic effects of crude methanolic extracts of E. helioscopia on live Haemonchus contortus worms as evident from their paralysis and/or death at 8h after exposure, different concentrations (12.5 mg ml(-1), 25 mg ml(-1) and 50 mg ml(-1)) of aqueous and methanolic extracts were used against H. contortus which exhibited dose-dependent anthelmintic effects on H. contortus. Aqueous and methanolic extracts of aerial parts (stem, leaves and flowers) of E. helioscopia were found to have very low percent inhibitory egg hatching as compared to levamisole. It is concluded that the entire plant of E. helioscopia possesses significant anthelmintic activity and could be a potential alternative for treating cases of helminth infections in ruminants. PMID:22633018

Lone, Bashir A; Chishti, M Z; Bhat, Fayaz Ahmad; Tak, Hidayatullah; Bandh, Suhaib A

2012-10-26

337

Synthesis and Antifungal Activity In Vitro of Isoniazid Derivatives against Histoplasma capsulatum var. capsulatum  

PubMed Central

Histoplasmosis is a severe infection that affects millions of patients worldwide and is endemic in the Americas. Amphotericin B (AMB) and itraconazole are highly effective for the treatment of severe and milder forms of the disease, but AMB is toxic, and the bioavailability of itraconazole is erratic. Therefore, it is important to investigate new classes of drugs for histoplasmosis treatment. In this study, a series of nine isoniazid hydrazone derivatives were synthesized and evaluated for their antifungal activities in vitro against the dimorphic fungus Histoplasma capsulatum var. capsulatum. The drugs were tested by microdilution in accordance with CLSI guidelines. The compound N?-(1-phenylethylidene)isonicotinohydrazide had the lowest MIC range of all the compounds for the yeast and filamentous forms of H. capsulatum. The in vitro synergy of this compound with AMB against the planktonic and biofilm forms of H. capsulatum cells was assessed by the checkerboard method. The effects of this hydrazone on cellular ergosterol content and membrane integrity were also investigated. The study showed that the compound alone is able to reduce the ergosterol content of planktonic cells and can alter the membrane permeability of the fungus. Furthermore, the compound alone or in combination with AMB showed inhibitory effects against mature biofilms of H. capsulatum. N?-(1-Phenylethylidene)isonicotinohydrazide alone or combined with AMB might be of interest in the management of histoplasmosis. PMID:24514090

de Farias Marques, Francisca Jakelyne; de Aguiar Cordeiro, Rebecca; da Silva, Marcos Reinaldo; Donato Maia Malaquias, Angela; Silva de Melo, Charlline Vládia; Mafezoli, Jair; Ferreira de Oliveira, Maria da Conceiçăo; Nogueira Brilhante, Raimunda Sâmia; Gadelha Rocha, Marcos Fábio; Pinheiro Gomes Bandeira, Tereza de Jesus; Costa Sidrim, José Júlio

2014-01-01

338

Contact Lenses Wettability In Vitro: Effect of Surface-Active Ingredients  

PubMed Central

Purpose To investigate the release of surface-active agents (surfactants) from unworn soft contact lenses and their influence on the lens surface wettability in vitro. Methods Surface tension (ST) of blister pack solutions was measured by pendant-drop technique. STs at the air-aqueous interface and contact angles (CAs) of four conventional and seven silicone hydrogel (SiH) soft contact lenses (SCLs) were evaluated in a dynamic-cycling regime using a modified captive-bubble tensiometer-goniometer. Measurements were performed immediately after removal from blister packs, and after soaking in a glass vial filled with a surfactant-free solution, which was replaced daily for one week. Lens surface wettability was expressed as adhesion energy (AE) according to Young’s equation. Results STs of all blister pack solutions were lower than the reference ST of pure water (72.5 mN/m), indicating the presence of surfactants. When lenses were depleted of surfactants by soaking, the STs of all studied lenses and advancing CAs of selected lenses increased (p < 0.001). Receding CAs of all studied lenses were 12° ± 5° and were not affected by the presence of surfactants. For most of the conventional lenses, the surface wettability was largely dependent on surfactants, and reduced significantly after surfactant depletion. In contrast, most SiH lenses exhibited stable and self-sustained surface wettability in vitro. Conclusions The manufacturer-added surfactants affected wetting properties of all studied SCLs, although to different degrees. PMID:20400924

Lin, Meng C.; Svitova, Tatyana F.

2010-01-01

339

Hemodynamic flow improves rat hepatocyte morphology, function, and metabolic activity in vitro  

PubMed Central

In vitro primary hepatocyte systems typically elicit drug induction and toxicity responses at concentrations much higher than corresponding in vivo or clinical plasma Cmax levels, contributing to poor in vitro-in vivo correlations. This may be partly due to the absence of physiological parameters that maintain metabolic phenotype in vivo. We hypothesized that restoring hemodynamics and media transport would improve hepatocyte architecture and metabolic function in vitro compared with nonflow cultures. Rat hepatocytes were cultured for 2 wk either in nonflow collagen gel sandwiches with 48-h media changes or under controlled hemodynamics mimicking sinusoidal circulation within a perfused Transwell device. Phenotypic, functional, and metabolic parameters were assessed at multiple times. Hepatocytes in the devices exhibited polarized morphology, retention of differentiation markers [E-cadherin and hepatocyte nuclear factor-4? (HNF-4?)], the canalicular transporter [multidrug-resistant protein-2 (Mrp-2)], and significantly higher levels of liver function compared with nonflow cultures over 2 wk (albumin ?4-fold and urea ?5-fold). Gene expression of cytochrome P450 (CYP) enzymes was significantly higher (fold increase over nonflow: CYP1A1: 53.5 ± 10.3; CYP1A2: 64.0 ± 15.1; CYP2B1: 15.2 ± 2.9; CYP2B2: 2.7 ± 0.8; CYP3A2: 4.0 ± 1.4) and translated to significantly higher basal enzyme activity (device vs. nonflow: CYP1A: 6.26 ± 2.41 vs. 0.42 ± 0.015; CYP1B: 3.47 ± 1.66 vs. 0.4 ± 0.09; CYP3A: 11.65 ± 4.70 vs. 2.43 ± 0.56) while retaining inducibility by 3-methylcholanthrene and dexamethasone (fold increase over DMSO: CYP1A = 27.33 and CYP3A = 4.94). These responses were observed at concentrations closer to plasma levels documented in vivo in rats. The retention of in vivo-like hepatocyte phenotype and metabolic function coupled with drug response at more physiological concentrations emphasizes the importance of restoring in vivo physiological transport parameters in vitro. PMID:23485712

Simmers, M. B.; Deering, T. G.; Berry, D. J.; Feaver, R. E.; Hastings, N. E.; Pruett, T. L.; LeCluyse, E. L.; Blackman, B. R.; Wamhoff, B. R.

2013-01-01

340

Stimulatory action of itopride hydrochloride on colonic motor activity in vitro and in vivo.  

PubMed

We investigated the effects of itopride hydrochloride (itopride, N-[4-[2-(dimethylamino)ethoxy]benzyl]-3,4-dimethoxybenzamide hydrochloride), a gastroprokinetic agent, on the colonic motor activity in vitro and in vivo, in comparison with benzamides, cisapride hydrate (cisapride), and mosapride citrate (mosapride). Itopride stimulated both peristaltic and segmental motility induced by applying intraluminal pressure to the isolated guinea pig colon. Although cisapride and mosapride enhanced the segmental motility, they markedly reduced the peristaltic motility. In conscious dogs with implanted strain gauge force transducers, itopride stimulated contractile activity in the gastrointestinal tract from the stomach to the colon. Cisapride stimulated contractile activity in the gastric antrum, ileum, and ascending colon. Mosapride stimulated contractile activity only in the gastric antrum and ileum. In guinea pigs and rats, itopride accelerated colonic luminal transit. On the other hand, cisapride and mosapride failed to enhance colonic transit. These results demonstrate that itopride has a stimulatory action on colonic peristalsis, propelling colonic luminal contents, different from that of cisapride and mosapride. Therefore, itopride may be a useful drug for the treatment of functional bowel disorders such as functional constipation. PMID:12724347

Tsubouchi, Tadashi; Saito, Takaharu; Mizutani, Fujie; Yamauchi, Toshie; Iwanaga, Yuji

2003-08-01

341

In vitro antiviral activity of chestnut and quebracho woods extracts against avian reovirus and metapneumovirus.  

PubMed

Field evidences have suggested that a natural extract, containing tannins, could be effective against poultry enteric viral infections. Moreover previous studies have shown that vegetable tannins can have antiviral activity against human viruses. Based on this knowledge three different Chestnut (Castanea spp.) wood extracts and one Quebracho (Schinopsis spp.) wood extract, all containing tannins and currently used in the animal feed industry, were tested for in vitro antiviral activity against avian reovirus (ARV) and avian metapneumovirus (AMPV). The MTT assay was used to evaluate the 50% cytotoxic compounds concentration (CC(50)) on Vero cells. The antiviral properties were tested before and after the adsorption of the viruses to Vero cells. Antiviral activities were expressed as IC(50) (concentration required to inhibit 50% of viral cytopathic effect). CC(50)s of tested compounds were > 200 microg/ml. All compounds had an extracellular antiviral effect against both ARV and AMPV with IC(50) values ranging from 25 to 66 microg/ml. Quebracho extract had also evident intracellular anti-ARV activity (IC(50) 24 microg/ml). These preliminary results suggest that the examined vegetable extracts might be good candidates in the control of some avian virus infections. Nevertheless further in vivo experiments are required to confirm these findings. PMID:19435637

Lupini, C; Cecchinato, M; Scagliarini, A; Graziani, R; Catelli, E

2009-12-01

342

Activity and synergistic interactions of stilbenes and antibiotic combinations against bacteria in vitro.  

PubMed

The synergistic antibacterial activity of two stilbenes [3,4',5-trihydroxystilbene (1) and 3,5-dihydroxy-4-isopropylstilbene(2)] purified from a Bacillus sp. N strain associated with entomopathogenic nematode Rhabditis (Oscheius) in combination with ciprofloxacin and cefotaxime was investigated. The activity of the stilbenes and standard antibiotics on bacteria were determined using the macrodilution method. The minimum inhibitory concentration and minimum bactericidal concentration of the stilbenes was compared with that of the standard antibiotics. The antibacterial activities of stilbenes against pathogenic bacteria were assessed using the checkerboard and time-kill methods to evaluate the synergistic effects of stilbenes in treatment with ciprofloxacin or cefotaxime. The results of the present study showed that the combination effects of both stilbenes with ciprofloxacin were synergistic (FIC index <0.5). Whereas stilbene 2 with cefotaxime recorded additive. Furthermore, time-kill study showed that the growth of the tested bacteria was completely attenuated with 12-24 h of treatment with 50:50 ratios of stilbenes and antibiotics. These results suggest that stilbenes combined with antibiotics may be microbiologically beneficial and not antagonistic. These findings have potential implications in delaying the development of resistance as the antibacterial effect is achieved with lower concentrations of both drugs (antibiotics and stilbenes). The in vitro synergistic activity of stilbenes and antibiotics against bacteria is reported here for the first time. PMID:22806752

Kumar, S Nishanth; Siji, J V; Nambisan, Bala; Mohandas, C

2012-11-01

343

In vitro Anti-Toxoplasma gondii Activity of Root Extract/Fractions of Eurycoma longifolia Jack  

PubMed Central

Background Toxoplasma gondii infection causes toxoplasmosis, an infectious disease with worldwide prevalence. The limited efficiency of drugs against this infection, their side effects and the potential appearance of resistant strains make the search of novel drugs an essential need. We examined Eurycoma longifolia root extract and fractions as potential sources of new compounds with high activity and low toxicity. The main goal of this study was to investigate the anti-T. gondii activity of crude extract (TACME) and four fractions (TAF 273, TAF 355, TAF 191 and TAF 401) from E. longifolia, with clindamycin as the positive control. Methods In vitro toxoplasmacidal evaluation was performed using Vero cells as host for T. gondii. Light microscopy technique was used to study in situ antiparasitic activity. Results Significant anti-T. gondii activity was observed with clindamycin (EC50?=?0.016 ?g/ml), follow by TAF 355 (EC50?=?0.369 ?g/ml) and TAF 401 (EC50?=?0.882 ?g/ml). Light microscopy revealed that most Vero cells were infected after 3 h of exposure to T. gondii. After 36 h of exposure to the E. longifolia fraction, the host Vero cells showed no visible intracellular parasite and no remarkable morphological changes. Conclusions Our study demonstrated that TAF 355 and TAF401 fractions may be the sources of new anti-T. gondii compounds. PMID:22781137

2012-01-01

344

A topological study of repetitive co-activation networks in in vitro cortical assemblies  

NASA Astrophysics Data System (ADS)

To address the issue of extracting useful information from large data-set of large scale networks of neurons, we propose an algorithm that involves both algebraic-statistical and topological tools. We investigate the electrical behavior of in vitro cortical assemblies both during spontaneous and stimulus-evoked activity coupled to Micro-Electrode Arrays (MEAs). Our goal is to identify core sub-networks of repetitive and synchronous patterns of activity and to characterize them. The analysis is performed at different resolution levels using a clustering algorithm that reduces the network dimensionality. To better visualize the results, we provide a graphical representation of the detected sub-networks and characterize them with a topological invariant, i.e. the sequence of Betti numbers computed on the associated simplicial complexes. The results show that the extracted sub-populations of neurons have a more heterogeneous firing rate with respect to the entire network. Furthermore, the comparison of spontaneous and stimulus-evoked behavior reveals similarities in the identified clusters of neurons, indicating that in both conditions similar activation patterns drive the global network activity.

Pirino, Virginia; Riccomagno, Eva; Martinoia, Sergio; Massobrio, Paolo

2015-02-01

345

A topological study of repetitive co-activation networks in in vitro cortical assemblies.  

PubMed

To address the issue of extracting useful information from large data-set of large scale networks of neurons, we propose an algorithm that involves both algebraic-statistical and topological tools. We investigate the electrical behavior of in vitro cortical assemblies both during spontaneous and stimulus-evoked activity coupled to Micro-Electrode Arrays (MEAs). Our goal is to identify core sub-networks of repetitive and synchronous patterns of activity and to characterize them. The analysis is performed at different resolution levels using a clustering algorithm that reduces the network dimensionality. To better visualize the results, we provide a graphical representation of the detected sub-networks and characterize them with a topological invariant, i.e. the sequence of Betti numbers computed on the associated simplicial complexes. The results show that the extracted sub-populations of neurons have a more heterogeneous firing rate with respect to the entire network. Furthermore, the comparison of spontaneous and stimulus-evoked behavior reveals similarities in the identified clusters of neurons, indicating that in both conditions similar activation patterns drive the global network activity. PMID:25559130

Pirino, Virginia; Riccomagno, Eva; Martinoia, Sergio; Massobrio, Paolo

2015-01-01

346

Water-soluble extracts from defatted sesame seed flour show antioxidant activity in vitro.  

PubMed

Defatted white and gold sesame seed flour, recovered as a byproduct after sesame oil extraction, was extracted with 70% ethanol to obtain polar-soluble crude extracts. The in vitro antioxidant activity of the extract was evaluated by DPPH free radical scavenging activity and oxygen radical absorbing capacity (ORAC). The polar-soluble crude extracts of both sesame seed types exhibited good antioxidant capacity, especially by the ORAC method with 34,720 and 21,700?mol Trolox equivalent/100g of white and gold sesame seed extract, respectively. HPLC, butanol extraction, and UPLC-MS analyses showed that different compounds contributed to the antioxidant activity of the polar-soluble crude extracts. Sesaminol glycosides were identified in the butanol-soluble fractions; whereas, purified water-soluble fraction contained ferulic and vanillic acids. This study shows that hydrophilic antioxidants in the purified water-soluble fraction contributed to the antioxidant activity of white and gold sesame seed polar-soluble crude extracts. PMID:25577085

Ben Othman, Sana; Katsuno, Nakako; Kanamaru, Yoshihiro; Yabe, Tomio

2015-05-15

347

In vitro antimicrobial activity of 20 selected climber species from the Bignoniaceae family.  

PubMed

Hydroalcoholic and aqueous extracts of some climber species from the Bignoniaceae family that grow in the north of Argentina were evaluated for in vitro antibacterial activity against Gram-positive and Gram-negative strains. By means of bioautography and disc diffusion methods, it could be determined that all infusions were not active, whereas the hydroalcoholic extracts of seven species were able to inhibit bacterial growth. The minimum inhibitory concentration and minimum bactericidal concentration observed were between 62.5 and 1000 ?g gallic acid equivalent (GAE)/mL and between 125 and 1000 ?g GAE/mL, respectively. The tested extracts were more active against Gram-positive microorganisms. Time-kill experiments indicated that all extracts have bacteriostatic activity. Phytochemical screening showed the presence of terpenoids, phenols and flavonoids. The amount of phenolic compounds and flavonoids was higher in tinctures when compared with infusions. These results suggest the presence of antibacterial substances in the hydroalcoholic extracts, which could be used for the treatment of infections. PMID:23577749

Torres, Carola Analía; Zampini, Iris Catiana; Nuńez, María Beatriz; Isla, María Inés; Castro, Marcela Paola; Gonzalez, Ana María

2013-01-01

348

In vitro activity of antibiotic combinations against Pseudomonas aeruginosa biofilm and planktonic cultures.  

PubMed

In order to investigate the hypothesis that the combination of clarithromycin with other antibacterial agents offers a successful treatment in the eradication of Pseudomonas aeruginosa biofilm, we first determined the activity of eight antimicrobial agents against planktonic cultures of P. aeruginosa isolates by the microdilution technique. Second, we determined the in vitro effects of these antimicrobial agents individually and in combination against planktonic cultures and pre-formed biofilms of P. aeruginosa PA01. Drug combinations with marked activity were tested on biofilms of clinical isolates. The percentages of planktonic culture survival and biofilm persistence were determined using spectrophotometry and scanning electron microscopy, respectively. Bacterial enumeration was used as a more quantitative method to assess the viability of bacteria in the biofilm. Among the antibacterial agents tested, tobramycin and polymyxin B had the strongest activity against planktonic cultures when tested alone. Synergistic activity was observed for the combination chitosan/tobramycin against planktonic cultures but not biofilms, and for the combination tobramycin/clarithromycin against biofilms but not planktonic cultures. The results suggest that the combination clarithromycin/tobramycin may be successful for eradicating infections involving bacterial biofilms such as in cystic fibrosis patients chronically infected by P. aeruginosa. Further studies on representative isolates in vivo are warranted to support these results. PMID:18280117

Tré-Hardy, Marie; Vanderbist, Francis; Traore, Hamidou; Devleeschouwer, Michel Jean

2008-04-01

349

Effect of aqueous extract and fractions of Fagonia arabica on in vitro anticoagulant activity.  

PubMed

Fagonia arabica (FA) is a deobstruent and blood purifier, which possesses thrombolytic and antioxidant activities. In this study, the anticoagulant effects of FA and its derived fractions were evaluated. Plasma recalcification was performed with multisolvent extracts of FA and then with extracts prepared successively with increasing polarity of the solvents. Aqueous extract was the most potent anticoagulant extract, which was fractionated by thin-layer chromatography and column chromatography. Five fractions collected were checked for their anticoagulation effect. The most potent fraction was screened for phytoconstituents. Aqueous extract of FA is the most active anticoagulant (31 minutes). Results were statistically significant when compared to heparin (38 minutes) and saline (4.04 minutes; P > .001). The Fifth fraction (FA5), the most potent fraction (27 minutes), was found positive for flavonoids, saponin, tannin, triterpenoids, carbohydrates, reducing sugar, and monosaccharides. Aqueous FA and fraction FA5 were most active in in vitro anticoagulation, and any of the phytochemicals identified could be considered the active component. PMID:23814169

Chourasia, Sweta R; Kashyap, Rajpal Singh; Deopujari, Jayant Y; Purohit, Hemant J; Taori, Girdhar M; Daginawala, Hatim F

2014-11-01

350

In vitro assessment of antioxidant activity of tyrosol, resveratrol and their acetylated derivatives.  

PubMed

Consumption of phenolic compounds is associated with beneficial effects in humans even though many of them are poorly absorbed. The aim of this study was to investigate the in vitro antioxidant activity of tyrosol (T), resveratrol (R) and their acetylated derivatives (AcD), as increased lipophilicity has been reported to improve absorption. The chemically synthesized AcDs were evaluated by their ability to scavenge DPPH radicals, inhibit non-enzymatic linoleic acid peroxidation, inhibit human serum oxidation in the presence of copper ions and inhibit lipoxygenase activity. T showed an inhibitory effect only in serum oxidation, where the T-acetylated at aromatic-OH was the most active. The T-acetylated at aliphatic-OH and 3,5-diacetyl-R exhibited the most powerful effect in non-enzymatic linoleic acid peroxidation with IC50 values 2.4mM±0.21 and 0.055mM±0.0018, respectively. In all other tests R was the most potent among all its AcD and T. Increasing lipophilicity by acetylation improves antioxidant activity of phenolic compounds in non-enzymatic lipid peroxidation assays. PMID:25660873

Vlachogianni, Ioanna C; Fragopoulou, Elizabeth; Kostakis, Ioannis K; Antonopoulou, Smaragdi

2015-06-15

351

Passive and active in vitro resorption of calcium and magnesium phosphate cements by osteoclastic cells.  

PubMed

Biocements are clinically applied materials for bone replacement in non-load-bearing defects. Depending on their final composition, cements can be either resorbed or remain stable at the implantation site. Degradation can occur by two different mechanisms, by simple dissolution (passive) or after osteoclastic bone remodeling (active). This study investigated both the passive and active in vitro resorption behavior of brushite (CaHPO??· 2H?O), monetite (CaHPO?), calcium-deficient hydroxyapatite (CDHA; Ca?(PO?)?HPO?OH), and struvite (MgNH?PO??·?6H?O) cements. Passive resorption was measured by incubating the cement samples in a cell culture medium, whereas active resorption was determined during the surface culture of multinuclear osteoclastic cells derived from RAW 264.7 macrophages. Osteoclast formation was confirmed by showing tartrate resistant acid phosphatase (TRAP) activity on CDHA, brushite, and monetite surfaces, as well as by measuring calcitonin receptor (CT-R) expression as an osteoclast-specific protein by Western blot analysis for struvite ceramics. An absence of passive degradation and only marginally active degradation of <0.01% were found for CDHA matrices. For the secondary calcium phosphates brushite and monetite, active degradation was predominant with a cumulative Ca˛+ release of 2.02 (1.20) ?mol during 13 days, whereas passive degradation released only 0.788 (0.04) ?mol calcium ions into the medium. The struvite cement was the most degradable with a passive (active) release of 9.26 (2.92) Mg˛+ ions and a total weight loss of 4.7% over 13 days of the study. PMID:20673025

Grossardt, Christian; Ewald, Andrea; Grover, Liam M; Barralet, Jake E; Gbureck, Uwe

2010-12-01

352

In vitro ?-glucosidase inhibitory activity of phenolic constituents from aerial parts of Polygonum hyrcanicum  

PubMed Central

Background and the purpose of the study The early stage of diabetes mellitus type 2 is associated with postprandial hyperglycemia. Hyperglycemia is believed to increase the production of free radicals and reactive oxygen species, leading to oxidative tissue damage. In an effort of identifying herbal drugs which may become useful in the prevention or mitigation of diabetes, biochemical activities of Polygonum hyrcanicum and its constituents were studied. Methods Hexane, ethylacetate and methanol extracts of P. hyrcanicum were tested for ?-glucosidase inhibitory, antioxidant and radical scavenging properties. Active constituents were isolated and identified from the methanolic extract in an activity guided approach. Results A methanolic extract from flowering aerial parts of the plant showed notable ?-glucosidase inhibitory activity (IC50?=?15 ?g/ml). Thirteen phenolic compounds involving a cinnamoylphenethyl amide, two flavans, and ten flavonols and flavonol 3-O-glycosides were subsequently isolated from the extract. All constituents showed inhibitory activities while compounds 3, 8 and 11 (IC50?=?0.3, 1.0, and 0.6 ?M, respectively) were the most potent ones. The methanol extract also showed antioxidant activities in DPPH (IC50?=?76 ?g/ml) and FRAP assays (1.4 mmol ferrous ion equivalent/g extract). A total phenol content of 130 mg/g of the extract was determined by Folin-Ciocalteu reagent. Conclusion This study shows that P. hyrcanicum contains phenolic compounds with in vitro activity that can be useful in the context of preventing or mitigating cellular damages linked to diabetic conditions. PMID:23351720

2012-01-01

353

Buffer nitrogen solubility, in vitro ruminal partitioning of nitrogen and in vitro ruminal biological activity of tannins in leaves of four fodder tree species.  

PubMed

This study explores the chemical composition, buffer N solubility, in vitro ruminal N degradability and in vitro ruminal biological activity of tannins in leaves from Gliricidia sepium, Leucaena leucocephala, Morus alba and Trichanthera gigantea trees. These tree leaves are a potential protein source for ruminants, but their site-influenced nutritive value is largely unknown. Leucaena leucocephala leaves had the highest N content (42.1 g/kg DM), while T. gigantea leaves had the least (26.1 g/kg DM). Leucaena leucocephala had the highest buffer solubility index (20%), while 10% of the total N in leaves of the other three species was soluble. The rapidly fermentable N fraction 'a' was highest in M. alba leaves (734.9 g/kg DM) and least in T. gigantea leaves (139.5 g/kg DM). The rate of fermentation (c) was highest for M. alba (7%/hours) leaves. No significant correlations were recorded between buffer solubility index of N and in vitro ruminal N degradability parameters: a, b, and c. The highest response to tannin inactivation using polyethylene glycol, in terms of percentage increase in 36-hours cumulative gas production, was recorded in M. alba (39%) and T. gigantea (38%) leaves. It was concluded that buffer solubility of N is not a good indicator of ruminal N degradation in the leaves of these tree species. Leaves of M. alba could be more valuable as a source of rapidly fermentable N when animals are offered low-protein, high-fibre diets compared with other tree species evaluated in the current study. However, when feeding M. alba leaves, the role of tannins must be considered because these secondary plant compounds showed significant in vitro ruminal biological activity. PMID:24750263

Cudjoe, N; Mlambo, V

2014-08-01

354

The Novel Arylamidine T-2307 Maintains In Vitro and In Vivo Activity against Echinocandin-Resistant Candida albicans.  

PubMed

We evaluated the in vitro and in vivo activities of the investigational arylamidine T-2307 against echinocandin-resistant Candida albicans. T-2307 demonstrated potent in vitro activity, and daily subcutaneous doses between 0.75 and 6 mg/kg of body weight significantly improved survival and reduced fungal burden compared to placebo control and caspofungin (10 mg/kg/day) in mice with invasive candidiasis caused by an echinocandin-resistant strain. Thus, T-2307 may have potential use in the treatment of echinocandin-resistant C. albicans infections. PMID:25451054

Wiederhold, Nathan P; Najvar, Laura K; Fothergill, Annette W; Bocanegra, Rosie; Olivo, Marcos; McCarthy, Dora I; Kirkpatrick, William R; Fukuda, Yoshiko; Mitsuyama, Junichi; Patterson, Thomas F

2015-02-01

355

In vivo and in vitro techniques to determine the biological activity of food allergens.  

PubMed

Methods for determination of the biological activity of food allergens comprise both determination of the allergenic potency, i.e. the capability to elicit an allergic reaction in an already sensitized individual, and the allergenic potential, i.e. the risk for sensitizing a hitherto non-allergic individual. Several methods are discussed for determination of potency including the double-blinded placebo-controlled food challenge, skin testing, in vitro effector cell assays such as basophil histamine release, and IgE-based techniques such as RAST and RAST inhibition. No reliable methods have yet been developed which can predict the allergenic potential of a food or a food allergen. The progress in the areas of stability studies and animal models for food allergy are discussed. PMID:11419727

Poulsen, L K

2001-05-25

356

Production, structural elucidation and in vitro antitumor activity of trehalose lipid biosurfactant from Nocardia farcinica strain.  

PubMed

The objective of this study was to isolate and identify the chemical structure of a biosurfactant produced by Nocardia farcinica strain BN26 isolated from soil, and evaluate its in vitro antitumor activity on a panel of human cancer cell lines. Strain BN26 was found to produce glycolipid biosurfactant on n-hexadecane as the sole carbon source. The biosurfactant was purified using medium pressure liquid chromatography and characterized as trehalose lipid tetraester (THL) by nuclear magnetic resonance (NMR) spectroscopy and mass spectrometry (MS). Subsequently, the cytotoxic effects of THL on cancer cell lines BV-173, KE-37 (SKW-3), HL-60, HL-60/DOX and JMSU-1 were evaluated by MTT assay. The results showed that THL caused concentration dependent cytotoxicity on all human tumor cell lines investigated. PMID:25370728

Christova, Nelly; Lang, Siegmund; Wray, Victor; Kaloyanov, Kaloyan; Konstantinov, Spiro; Stoineva, Ivanka

2014-11-01

357

Preparation and antitubercular activities in vitro and in vivo of novel Schiff bases of isoniazid.  

PubMed

Structural modification of the frontline antitubercular isonicotinic acid hydrazide (INH) provides lipophilic adaptations (3-46) of the drug in which the hydrazine moiety of the parent compound has been chemically blocked from the deactivating process of N(2)-acetylation by N-arylaminoacetyl transferases. As a class, these compounds show high levels of activity against Mycobacterium tuberculosis in vitro and in tuberculosis-infected macrophages. They provide strong protection in tuberculosis-infected mice and have low toxicity. With some representatives of this class achieving early peak plasma concentrations approximately three orders of magnitude above minimum inhibitory concentration, they may serve as tools for improving our understanding of INH-based treatment modalities, particularly for those patients chronically underdosed in conventional INH therapy. PMID:19524330

Hearn, Michael J; Cynamon, Michael H; Chen, Michaeline F; Coppins, Rebecca; Davis, Jessica; Joo-On Kang, Helen; Noble, Abigail; Tu-Sekine, Becky; Terrot, Marianne S; Trombino, Daniella; Thai, Minh; Webster, Eleanor R; Wilson, Rebecca

2009-10-01

358

Designed, synthetically accessible bryostatin analogues potently induce activation of latent HIV reservoirs in vitro  

NASA Astrophysics Data System (ADS)

Bryostatin is a unique lead in the development of potentially transformative therapies for cancer, Alzheimer's disease and the eradication of HIV/AIDS. However, the clinical use of bryostatin has been hampered by its limited supply, difficulties in accessing clinically relevant derivatives, and side effects. Here, we address these problems through the step-economical syntheses of seven members of a new family of designed bryostatin analogues using a highly convergent Prins-macrocyclization strategy. We also demonstrate for the first time that such analogues effectively induce latent HIV activation in vitro with potencies similar to or better than bryostatin. Significantly, these analogues are up to 1,000-fold more potent in inducing latent HIV expression than prostratin, the current clinical candidate for latent virus induction. This study provides the first demonstration that designed, synthetically accessible bryostatin analogues could serve as superior candidates for the eradication of HIV/AIDS through induction of latent viral reservoirs in conjunction with current antiretroviral therapy.

Dechristopher, Brian A.; Loy, Brian A.; Marsden, Matthew D.; Schrier, Adam J.; Zack, Jerome A.; Wender, Paul A.

2012-09-01

359

Preparation and antitubercular activities in vitro and in vivo of novel Schiff bases of isoniazid  

PubMed Central

Structural modification of the frontline antitubercular isonicotinic acid hydrazide (INH) provides lipophilic adaptations (3-46) of the drug in which the hydrazine moiety of the parent compound has been chemically blocked from the deactivating process of N2-acetylation by N-arylaminoacetyl transferases. As a class, these compounds show high levels of activity against Mycobacterium tuberculosis in vitro and in tuberculosis-infected macrophages. They provide strong protection in tuberculosis-infected mice and have low toxicity. With some representatives of this class achieving early peak plasma concentrations approximately three orders of magnitude above minimum inhibitory concentration, they may serve as tools for improving our understanding of INH-based treatment modalities, particularly for those patients chronically underdosed in conventional INH therapy. PMID:19524330

Hearn, Michael J.; Cynamon, Michael H.; Chen, Michaeline F.; Coppins, Rebecca; Davis, Jessica; Kang, Helen Joo-On; Noble, Abigail; Tu-Sekine, Becky; Terrot, Marianne S.; Trombino, Daniella; Thai, Minh; Webster, Eleanor R.; Wilson, Rebecca

2009-01-01

360

In vitro anticancer activity of extracts of Mentha Spp. against human cancer cells.  

PubMed

In vitro anticancer potential of methanolic and aqueous extracts of whole plants of Mentha arvensis, M. longifolia, M. spicata and M. viridis at concentration of 100 ?g/ml was evaluated against eight human cancer cell lines--A-549, COLO-205, HCT-116, MCF-7, NCI-H322, PC-3, THP-1 and U-87MG from six different origins (breast, colon, glioblastoma, lung, leukemia and prostate) using sulphorhodamine blue (SRB) assay. Methanolic extracts of above-mentioned Mentha Spp. displayed anti-proliferative effect in the range of 70-97% against four human cancer cell lines, namely COLO-205, MCF-7, NCI-H322 and THP-1; however, aqueous extracts were found to be active against HCT-116 and PC-3. The results indicate that Mentha Spp. contain certain constituents with cytotoxic properties which may find use in developing anticancer agents. PMID:25630112

Sharma, Vikas; Hussain, Shabir; Gupta, Moni; Saxena, Ajit Kumar

2014-10-01

361

Antimutagenic activities of naturally occurring polyamines in Chinese hamster ovary cell in vitro  

SciTech Connect

Spermine and spermidine, ubiquitous polyamines present in bacteria and animal cells, are also involved in cell growth. Since they interact with the double helix, they can stabilize the DNA molecule. Recent evidence of the antimutagenic and anticarcinogenic capacity of spermine has focused attention on the he mechanism(s) by which such agents can protect cells from induced damages. In the present paper the authors show the ability of spermine and spermidine to decrease the level of sister chromatid exchanges induced in Chinese hamster ovary cells cultivated in vitro, by treating them with Psoralen + UVA irradiation (able to induce mainly monoadducts and DNA cross-links). Two different mechanisms of polyamine action can be invoked to explain the preservative activity of this class of agents.

Cozzi, R.; Perticone, P.; Bona, R.; Polani, S. (Univ. La Sapienza, Rome (Italy))

1991-01-01

362

Degradation and antioxidant activities of peptides and zinc-peptide complexes during in vitro gastrointestinal digestion.  

PubMed

The degradation characteristics of three peptides (Ser-Met, Asn-Cys-Ser, and glutathione) and their zinc-peptide complexes were studied using a two-stage in vitro digestion model. Enzyme-resistant peptides and zinc-peptide complexes, antioxidant activities, and free amino acids released by digestive enzymes, were measured in this study. The results revealed that the three peptides and their zinc-peptide complexes were resistant to pepsin but not to pancreatin. Pancreatin can partly hydrolyse both peptides and zinc-peptide complexes, but more than half of them remaining in their original form after gastrointestinal digestion. The coordination of zinc improved the enzymatic resistance of the peptide due to lower solubility of complexes and affected the hydrolytic site of pepsin and pancreatin. Zinc-Asn-Cys-Ser, which is highly resistant to enzymatic hydrolysis and maintains Zn in a soluble form, may have potential to improve Zn bioavailability. PMID:25466083

Wang, Chan; Li, Bo; Wang, Bo; Xie, Ningning

2015-04-15

363

Synthesis, spectroscopic characterization, antineoplastic, in vitro-cytotoxic, and antibacterial activities of mononuclear ruthenium(II) complexes  

Microsoft Academic Search

The synthesis, antineoplastic, cytotoxic, and antibacterial activities of Ru(II) complexes derived from quinazoline and thiosemicarbazone ligands are reported. These complexes have been prepared and characterized by UV-Vis, IR, H-NMR, FAB-mass spectroscopy, and elemental analysis. The ligands and resulting complexes were subjected to in vivo antineoplastic activity against a transplantable murine tumor cell line Ehrlich ascites carcinoma (EAC) and in vitro cytotoxic activity

Sreekanth Thota; Mohammad Imran; Manasa Udugula; Subhas Somalingappa Karki; Narasimha Kanjarla; Rajeshwar Yerra; Jan Balzarini; Erik De Clercq

2012-01-01

364

In Vitro Activities of Ertapenem (MK-0826) against Clinical Bacterial Isolates from 11 North American Medical Centers  

PubMed Central

This study compared the in vitro activities of the new long-half-life carbapenem ertapenem (also known as MK-0826 and L-749,345) with those of imipenem, amoxicillin-clavulanate, and ciprofloxacin against 5,558 recent clinical isolates from 11 North American medical centers. We confirmed the greater activity of ertapenem than of imipenem against the Enterobacteriaceae and the greater activity of imipenem against pseudomonads and gram-positive bacteria. PMID:11353653

Fuchs, Peter C.; Barry, Arthur L.; Brown, Steven D.

2001-01-01

365

A Facile Synthesis, In vitro Antiinflammatory and Antioxidant activity of Novel Benzimidazolylpyrano[2,3-d][1,3]thiazolocarbonitriles  

PubMed Central

The synthesis benzimidazolylpyrano [2,3-d] [1,3] thiazolocarbonitriles (5a-j) were achieved by cyclocondensation of arylidene amino-benzo[d]imidazole-2-thiols (3a-j) with mercaptoacetic acid followed by cyclization with 2-(phenylmethylene)malononitrile. Further more, the present study aimed at the evaluation of in vitro antiinflammatory activity and antioxidant activity of synthetic compounds. All tested compounds showed appreciable activity against the standard drugs.

Malladi, S. R.; Anisetti, R.; Rao, P. R.

2014-01-01

366

Silica-induced NLRP3 inflammasome activation in vitro and in rat lungs.  

PubMed

RationaleMineral particles in the lung cause inflammation and silicosis. In myeloid and bronchial epithelial cells the inflammasome plays a role in responses to crystalline silica. Thioredoxin (TRX) and its inhibitory protein TRX-interacting protein link oxidative stress with inflammasome activation. We investigated inflammasome activation by crystalline silica polymorphs and modulation by TRX in vitro, as well as its localization and the importance of silica surface reactivity in rats.MethodsWe exposed bronchial epithelial cells and differentiated macrophages to silica polymorphs quartz and cristobalite and measured caspase-1 activity as well as the release of IL-1beta, bFGF and HMGB1; including after TRX overexpression or treatment with recombinant TRX. Rats were intratracheally instilled with vehicle control, Dörentruper quartz (DQ12) or DQ12 coated with polyvinylpyridine N-oxide. At days 3, 7, 28, 90, 180 and 360 five animals per treatment group were sacrificed. Hallmarks of silicosis were assessed with Haematoxylin-eosin and Sirius Red stainings. Caspase-1 activity in the bronchoalveolar lavage and caspase-1 and IL-1ß localization in lung tissue were determined using Western blot and immunohistochemistry (IHC).ResultsSilica polymorphs triggered secretion of IL-1ß, bFGF and HMGB1 in a surface reactivity dependent manner. Inflammasome readouts linked with caspase-1 enzymatic activity were attenuated by TRX overexpression or treatment. At day 3 and 7 increased caspase-1 activity was detected in BALF of the DQ12 group and increased levels of caspase-1 and IL-1ß were observed with IHC in the DQ12 group compared to controls. DQ12 exposure revealed silicotic nodules at 180 and 360 days. Particle surface modification markedly attenuated the grade of inflammation and lymphocyte influx and attenuated the level of inflammasome activation, indicating that the development of silicosis and inflammasome activation is determined by crystalline silica surface reactivity.ConclusionOur novel data indicate the pivotal role of surface reactivity of crystalline silica to activate the inflammasome in cultures of both epithelial cells and macrophages. Inhibitory capacity of the antioxidant TRX to inflammasome activation was evidenced. DQ12 quartz exposure induced acute and chronic functional activation of the inflammasome in the heterogeneous cell populations of the lung in associated with its crystalline surface reactivity. PMID:25406505

Peeters, Paul M; Eurlings, Irene M J; Perkins, Timothy N; Wouters, Emiel F; Schins, Roel P F; Borm, Paul J A; Drommer, Wolfgang; Reynaert, Niki L; Albrecht, Catrin

2014-11-19

367

In vitro antibacterial activity of Camellia sinensis extract against cariogenic microorganisms  

PubMed Central

Context: Dental caries, a ubiquitous multifactorial infectious disease, is primarily caused by microorganisms like Streptococcus mutans and Lactobacillus acidophilus. Use of antimicrobials is an important strategy to curb cariogenic microorganisms. Aim: The aim was to evaluate the in vitro antimicrobial activity of C. sinensis extract on S. mutans and L. acidophilus. Study Setting and Design: Experimental design, in vitro study, lab setting. Materials and Methods: Aqueous, acetone and ethanolic extracts of C. sinensis were subjected to antioxidant analysis. The ethanolic extract was used for assessment of antimicrobial properties. Ethanolic green tea extract at ten different concentrations and 0.2% chlorhexidine was used. Microbiological investigations were carried out to determine the minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and zone of Inhibition of the test and control agents against S. mutans and L. acidophilus. Statistical Analysis: Kruskall–Wallis and Mann–Whitney U-test. Results: MIC of green tea extract on S. mutans and L. acidophilus was found to be 0.2% and 0.3% respectively, MBC was found to be 0.8% and 0.9%, respectively. The mean zone of inhibition for 30 ?l containing 300 ?g of ethanolic extract of green tea and control against S. mutans were 18.33 mm and 14.67 mm, respectively. The mean zone of inhibition for 30 ?l containing 300 ?g of ethanolic extract of green tea and control against L. acidophilus were 12.67 mm and 7.33 mm, respectively. Conclusion: Green tea has antibacterial activity against predominant cariogenic bacteria namely S. mutans and L. acidophilus. PMID:25538470

Anita, P.; Sivasamy, Shyam; Madan Kumar, P. D.; Balan, I. Nanda; Ethiraj, Sumathi

2014-01-01

368

Human immunodeficiency virus type 2 preintegration complexes: activities in vitro and response to inhibitors.  

PubMed Central

We have established an assay for the function of preintegration complexes (PICs) of human immunodeficiency virus type 2 (HIV-2) to investigate the integration mechanism and to develop additional methods for screening candidate integration inhibitors. We partially purified HIV-2 PICs and found that they were competent to integrate viral cDNA into target DNA in vitro. Analysis of the structure of integration products on Southern blots revealed forms consistent with those expected for authentic integration products and circular forms containing one and two long terminal repeats. To determine whether in vitro products had the detailed structure expected of integration products formed in vivo, we recovered product molecules and analyzed junctions between viral DNA and target DNA. In the integration junctions of all nine molecules examined, we observed the 5-bp duplication of target sequence characteristic of integration in vivo. We investigated the possible role in integration of Vpx, a protein present in HIV-2 but not HIV-1 and known to be present in viral cores. Although association of Vpx with viral cDNA was detectable, our studies revealed no obvious role of Vpx in integration since the activities of PICs from Vpx- virions were indistinguishable from those of wild type. We have also investigated the use of HIV-2 PICs as tools to screen candidate HIV inhibitors. Assays with HIV-2 PICs, like assays with HIV-1 PICs, were less sensitive to many small molecule inhibitors than were reactions with purified integrase only. Comparing results of assays with PICs from HIV-1 and HIV-2 may be particularly useful, since inhibitors active against both may be more widely useful and less vulnerable to escape mutants. PMID:9060709

Hansen, M S; Bushman, F D

1997-01-01

369

In vitro assay for osteoinductive activity of different demineralized freeze-dried bone allograft  

PubMed Central

Purpose Various bone graft materials have been used for periodontal tissue regeneration. Demineralized freeze-dried bone allograft (DFDBA) is a widely used bone substitute. The current widespread use of DFDBA is based on its potential osteoinductive ability. Due to the lack of verifiable data, the purpose of this study was to assess the osteoinductive activity of different DFDBAs in vitro. Methods Sarcoma osteogenic (SaOS-2) cells (human osteoblast-like cells) were exposed to 8 mg/mL and 16 mg/mL concentrations of three commercial types of DFDBA: Osseo+, AlloOss, and Cenobone. The effect of these materials on cell proliferation was determined using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay. The osteoinductive ability was evaluated using alizarin red staining, and the results were confirmed by evaluating osteogenic gene expression using reverse transcription polymerase chain reaction (RT-PCR). Results In the SaOS-2 cells, an 8 mg/mL concentration of Osseo+ and Cenobone significantly increased cell proliferation in 48 hours after exposure (P<0.001); however, in these two bone materials, the proliferation of cells was significantly decreased after 48 hours of exposure with a 16 mg/mL concentration (P<0.001). The alizarin red staining results demonstrated that the 16 mg/mL concentration of all three tested DFDBA induced complete morphologic differentiation and mineralized nodule production of the SaOS-2 cells. The RT-PCR results revealed osteopontin gene expression at a 16 mg/mL concentration of all three test groups, but not at an 8 mg/mL concentration. Conclusions These commercial types of DFDBA are capable of decreasing proliferation and increasing osteogenic differentiation of the SaOS-2 cell line and have osteoinductive activity in vitro. PMID:23346466

Vaziri, Shahram; Vahabi, Surena; Torshabi, Maryam

2012-01-01

370

Total alkaloids of Rubus alceifolius Poir shows anti-angiogenic activity in vivo and in vitro.  

PubMed

Total alkaloids is an active ingredient of the natural plant Rubus alceifolius Poir, commonly used for the treatment of various cancers. Antitumor effects may be mediated through anti-angiogenic mechanisms. As such, the goal of the present study was to investigate and evaluate the effect of total alkaloids in Rubus alceifolius Poir (TARAP) on tumor angiogenesis and investigate the underlying molecular mechanisms of TARAP action in vivo and in vitro. A chick embryo chorioallantoic membrane (CAM) assay was used to assess angiogenesis in vivo. An MTT assay was performed to determine the viability of human umbilical vein endothelial cells (HUVECs) with and without treatment. Cell cycle progression of HUVECs was examined by FACS analysis with propidium iodide staining. HUVEC migration was determined using a scratch wound method. Tube formation of HUVECs was assessed with an ECMatrix gel system, and mRNA and protein expression of VEGF-A in both HUVECs and HepG2 human hepatocellular carcinoma cells were examined by RT-PCR and ELISA, respectively. Our results showed that TARAP inhibited angiogenesis in the CAM model in vivo and inhibited HUVEC proliferation via blocking cell cycle G1 to S progression in a dose- and time-dependent manners in vitro. Moreover, TARAP inhibited HUVEC migration and tube formation and downregulated mRNA and protein expression of VEGF-A in both HepG2 cells and HUVECs. Our findings suggest that the anti-angiogenic activity of TARAP may partly contribute to its antitumor properties and may be valuable for the treatment of diseases involving pathologic angiogenesis such as cancer. PMID:25148840

Zhao, Jinyan; Lin, Wei; Zhuang, Qunchuan; Zhong, Xiaoyong; Cao, Zhiyun; Hong, Zhenfeng; Peng, Jun

2014-11-01

371

Niosomal gel of lornoxicam for topical delivery: in vitro assessment and pharmacodynamic activity.  

PubMed

Lornoxicam is a potent oxicam class of non steroidal anti-inflammatory agent, prescribed for mild to moderate pain and inflammation. Niosomal gel of lornoxicam was developed for topical application. Lornoxicam niosomes (Lor-Nio) were fabricated by thin film hydration technique. Bilayer composition of niosomal vesicles was optimized. Lor-Nio dispersion was characterized by DSC, XRD, and FT-IR. Morphological evaluation was performed by scanning electron microscopy (SEM). Lor-Nio dispersion was incorporated into a gel using 2% w/w Carbopol 980 NF. Rheological and texture properties of Lor-Nio gel formulation showed suitability of the gel for topical application. The developed formulation was evaluated for in vitro skin permeation and skin deposition studies, occlusivity test and skin irritation studies. Pharmacodynamic activity of the Lor-Nio gel was performed by carragenan-induced rat paw model. Optimized Lor-Nio comprised of Span 60 and cholesterol in a molar ratio of 3:1 with 30 ?M dicetyl palmitate as a stabilizer. It had particle size of 1.125 ± 0.212 ?m (d 90), with entrapment efficiency of 52.38 ± 2.1%. DSC, XRD, and IR studies showed inclusion of Lor into niosomal vesicles. SEM studies showed spherical closed vesicular structure with particles in nanometer range. The in vitro skin permeation studies showed significant improvement in skin permeation and skin deposition for Lor-Nio gel (31.41 ± 2.24 ?g/cm(2), 30.079 ± 1.2 ?g/cm(2)) over plain lornoxicam gel (7.37 ± 1.27 ?g/cm(2), 6.6 ± 2.52 ?g/cm(2)). The Lor-Nio gel formulation showed enhanced anti-inflammatory activity by exhibiting mean edema inhibition (87.69 ± 1.43%) which was significantly more than the plain lornoxicam gel (53.84 ± 2.21%). PMID:23818079

Kumbhar, Deepak; Wavikar, Preeti; Vavia, Pradeep

2013-09-01

372

Antioxidant and antiproliferative activities of Abrus precatorius leaf extracts - an in vitro study  

PubMed Central

Background The use of traditional medicine at the primary health care level is widespread and plant-based treatments are being recommended for curing various diseases by traditional medical practitioners all over the world. The phytochemicals present in the fruits, vegetables and medicinal plants are getting attention day-by-day for their active role in the prevention of several human diseases. Abrus precatorius is a widely distributed tropical medicinal plant with several therapeutic properties. Therefore in the present study, A. precatorius leaf extracts were examined for their antioxidant and cytotoxic properties in vitro in order to discover resources for new lead structures or to improve the traditional medicine. Methods In this study, antioxidant and antiproliferative properties of the different leaf extracts (hexane, ethyl acetate, ethanol and water) from A. precatorius were investigated along with the quantification of the polyphenol and flavonoid contents. The ability of deactivating free radicals was extensively investigated with in vitro biochemical methods like DPPH•, •OH, NO, SO2- scavenging assays and inhibition capability of Fe(II)-induced lipid peroxidation. Furthermore, antiproliferative activities using different human cancer cell lines and primary cell line was carried out by MTT method. Results Total phenolic content and total flavonoid content of the extracts were found in the range of 1.65?±?0.22 to 25.48?±?0.62 GAE mg/g dw and 6.20?±?0.41 to 17.16?±?1.04 QE mg/g dw respectively. The experimental results further revealed that A. precatorius extracts showed strong antiradical properties, capable to chelate Fe2+ and possess good inhibition ability of lipid peroxidation. In addition, as a first step towards the identification of phytoconstituents endowed with potent chemopreventive activities, we evaluated the inhibitory effects of A. precatorius extracts on the proliferation of four different human tumour cell lines such as human colon adenocarcinoma cells (Colo-205), human retinoblastoma cancer cells (Y79), human hepatocellular carcinoma cells (HepG2) and Leukemia cells (SupT1). Ethanol extract (APA) and ethyl acetate extract (APE) of A. precatorius had apparent capabilities of inhibiting the survival of tested human cancer cell lines. Moreover, it was observed that the A. precatorius extracts did not inhibit the growth of mice peritoneal macrophages, thus confirming that plants extracts are selective against the cancer cell lines. Conclusion This work provides a scientific support for the high antioxidant and antiproliferative activity of this plant and thus it may find potential applications in the treatment of the diseases caused by ROS. Further studies are needed to confirm in vivo anti-tumorgenicity and subsequent chemical characterization of the active molecule(s). PMID:23452983

2013-01-01

373

In vitro testing of African traditional medicines for cytotoxic, immune modulatory and anti-HIV activities.  

PubMed

African Traditional Medicines (ATMs) serve as a major source of primary healthcare for African people. The reasons for their use range from easy access, affordability, beliefs in traditional systems and long term safety. ATMs have been used to treat individuals infected with HIV and therefore need scientific validation; a view supported by Traditional Health Practitioners (THPs). This study aimed to evaluate the in vitro cytotoxicity, immune modulatory and anti-HIV activities of traditional multiple herbal preparations from local THPs. Ugambu, Ihashi, Product Nene, Product Blue, SPNa and SDKc ATM were supplied by local THPs. Changes in adenosine triphosphate (ATP) & glutathione (GSH) over 24 hours were measured using luminometry. Changes in 12 cytokines were assayed using an ELISA-based absorbance assay. Protective effects against HIV killing of MT-4 cells were tested using the XTT assay and antiviral activity was measured using an HIV-1 viral load assay. Cyclosporine and AZT were used as positive controls. Ugambu, Ihashi, Product Nene and SDKc induced a dose dependent toxicity on treated PBMCs by reducing ATP and GSH at high doses (p< 0.001). These medicinal preparations, along with SPNa, showed immunomodulatory activity by significantly (p< 0.001) changing the secretion of pro-inflammatory cytokines. Product Blue stimulated the levels of ATP and GSH in treated PBMCs at all doses however this product did not show any immunomodulatory activity on cytokine secretion when compared to control cells. Ugambu, Ihashi, Product Nene showed promising anti-HIV activity relative to AZT (p< 0.01). This study has shown that some of these traditional medicinal preparations have at least one or all the properties of immunostimulation, immunomodulation or antiretroviral effects. The mechanism of action of the shown activities should further be investigated. PMID:23983349

Gqaleni, Nceba; Ngcobo, Mlungisi; Parboosing, Raveen; Naidoo, Anneta

2012-01-01

374

In Vitro and In Vivo antifungal activities of selected Cameroonian dietary spices  

PubMed Central

Background Spices and herbs have been used in food since ancient times to give taste and flavor and also as food preservatives and disease remedies. In Cameroon, the use of spices and other aromatic plants as food flavoring is an integral part of dietary behavior, but relatively little is known about their antifungal potential. The present work was designed to assess the antifungal properties of extracts from spices used in Cameroonian dietary. Methods The in vitro antifungal activities of twenty three extracts from twenty one spices were assessed by the broth micro-dilution method against eight fungi. Also, the in vivo activity of Olax subscorpioidea extract (the most active extract) was evaluated in rat model of disseminated candidiasis due to Candida albicans by estimating the fungal burden in blood and kidney. Results Seven extracts (30%) exhibited moderate to significant antifungal activities, inhibiting the growth of the microorganisms at concentrations ranging from 0.048 to 0.39 mg/mL. Olax subscorpioidea extract exhibited the highest antifungal activity particularly against?Candida albicans and Candida tropicalis (MIC of 0.097 mg/mL and 0.048 mg/mL respectively). Sixteen extracts (70%) were weakly active (MICs?>?6.25 mg/mL). Oral administration of O. subscorpioidea extract at the dose 2 g/kg of body weight (bw) to artificially infected rats revealed a drop in the number of colony forming units per milliliter (cfu/mL) of Candida albicans cells in the blood below the detection limit (100 cfu/mL) while a modest decrease was observed in the kidney. Conclusion The present work shows that some of the spices studied possess interesting antifungal properties and could be used to treat candidiasis. Among the plant species tested, Olax subscorpioidea displayed the most promising result. PMID:24533718

2014-01-01

375

Two systems in vitro that show insulin-stimulated serine kinase activity towards the insulin receptor.  

PubMed Central

Two systems in vitro are described that show insulin-stimulated phosphorylation of the insulin receptor on serine residues. In the first system, insulin receptor was purified partially from Fao rat hepatoma cells by direct solubilization of the cells in Triton X-100 and chromatography on wheat-germ-agglutinin-agarose. Phosphorylation of these preparations with [gamma-32P]ATP in the presence or absence of insulin resulted in 32P incorporation exclusively into phosphotyrosine residues. Serine kinase activity towards the insulin receptor was reconstituted by adding extracts of Fao cells. Prior exposure of the cells to insulin stimulated serine kinase activity towards the insulin receptor in extracts 7.2-fold. A receptor serine kinase activity enhanced by treatment of cells with cyclic AMP analogues was also retained in the reconstituted system. In the second system, insulin receptor and insulin-sensitive serine kinase activity towards the insulin receptor were co-purified from human placenta. The protocol involved preparation of membranes, before solubilization and chromatography on wheat-germ-agglutinin-agarose, by using gentle procedures designed not to disrupt a potentially labile association between the insulin receptor and the serine kinase. Serine kinase activity in these preparations towards the insulin receptor was stimulated up to 10-fold by insulin, and the stoicheiometry of serine phosphorylation was estimated to be approx 0.8 mol/mol of insulin receptor for phosphorylations performed in the presence of insulin. Thus a preparation of insulin receptor is described for the first time that is phosphorylated to high stoicheiometry on serine in an insulin-dependent manner. Conditions that facilitate recovery and assay of serine kinase activity are defined and discussed. These systems provide a basis for characterizing the nature of the insulin-sensitive serine kinase that phosphorylates the insulin receptor, and defining its role in insulin action and control of receptor function. Images Fig. 1. Fig. 2. Fig. 3. Fig. 4. Fig. 5. PMID:2965579

Smith, D M; King, M J; Sale, G J

1988-01-01

376

Cannabidiol and other cannabinoids reduce microglial activation in vitro and in vivo: relevance to Alzheimer's disease.  

PubMed

Microglial activation is an invariant feature of Alzheimer's disease (AD). It is noteworthy that cannabinoids are neuroprotective by preventing ?-amyloid (A?)-induced microglial activation both in vitro and in vivo. On the other hand, the phytocannabinoid cannabidiol (CBD) has shown anti-inflammatory properties in different paradigms. In the present study, we compared the effects of CBD with those of other cannabinoids on microglial cell functions in vitro and on learning behavior and cytokine expression after A? intraventricular administration to mice. CBD, (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl) pyrrolo-[1,2,3-d,e]-1,4-benzoxazin-6-yl]-1-naphthalenyl-methanone [WIN 55,212-2 (WIN)], a mixed CB(1)/CB(2) agonist, and 1,1-dimethylbutyl-1-deoxy-?(9)-tetrahydrocannabinol [JWH-133 (JWH)], a CB(2)-selective agonist, concentration-dependently decreased ATP-induced (400 ?M) increase in intracellular calcium ([Ca(2+)](i)) in cultured N13 microglial cells and in rat primary microglia. In contrast, 4-[4-(1,1-dimethylheptyl)-2,6-dimethoxyphenyl]-6,6-dimethyl-bicyclo[3.1.1]hept-2-ene-2-methanol [HU-308 (HU)], another CB(2) agonist, was without effect. Cannabinoid and adenosine A(2A) receptors may be involved in the CBD action. CBD- and WIN-promoted primary microglia migration was blocked by CB(1) and/or CB(2) antagonists. JWH and HU-induced migration was blocked by a CB(2) antagonist only. All of the cannabinoids decreased lipopolysaccharide-induced nitrite generation, which was insensitive to cannabinoid antagonism. Finally, both CBD and WIN, after subchronic administration for 3 weeks, were able to prevent learning of a spatial navigation task and cytokine gene expression in ?-amyloid-injected mice. In summary, CBD is able to modulate microglial cell function in vitro and induce beneficial effects in an in vivo model of AD. Given that CBD lacks psychoactivity, it may represent a novel therapeutic approach for this neurological disease. PMID:21350020

Martín-Moreno, Ana María; Reigada, David; Ramírez, Belén G; Mechoulam, R; Innamorato, Nadia; Cuadrado, Antonio; de Ceballos, María L

2011-06-01

377

Anti-Inflammatory and Antiosteoclastogenic Activities of Parthenolide on Human Periodontal Ligament Cells In Vitro  

PubMed Central

Periodontitis is an inflammatory disease that causes osteolysis and tooth loss. It is known that the nuclear factor kappa B (NF-?B) signalling pathway plays a key role in the progression of inflammation and osteoclastogenesis in periodontitis. Parthenolide (PTL), a sesquiterpene lactone extracted from the shoots of Tanacetum parthenium, has been shown to possess anti-inflammatory properties in various diseases. In the study reported herein, we investigated the effects of PTL on the inflammatory and osteoclastogenic response of human periodontal ligament-derived cells (hPDLCs) and revealed the signalling pathways in this process. Our results showed that PTL decreased NF-?B activation, I-?B degradation, and ERK activation in hPDLCs. PTL significantly reduced the expression of inflammatory (IL-1?, IL-6, and TNF-?) and osteoclastogenic (RANKL, OPG, and M-CSF) genes in LPS-stimulated hPDLCs. In addition, PTL attenuated hPDLC-induced osteoclastogenic differentiation of macrophages (RAW264.7 cells), as well as reducing gene expression of osteoclast-related markers in RAW264.7 cells in an hPDLC-macrophage coculture model. Taken together, these results demonstrate the anti-inflammatory and antiosteoclastogenic activities of PTL in hPDLCs in vitro. These data offer fundamental evidence supporting the potential use of PTL in periodontitis treatment. PMID:25610476

Zhang, Xufang; Mao, Xueli

2014-01-01

378

In vitro antiviral activity of penciclovir, a novel purine nucleoside, against duck hepatitis B virus.  

PubMed Central

The in vitro antihepadnavirus activities of the purine nucleoside analogs ganciclovir (9-[2-hydroxy-1-(hydroxymethyl)ethoxymethyl]guanine) and penciclovir [9-(4-hydroxy-3-hydroxymethylbut-1-yl)guanine; BRL 39123] were compared in primary duck hepatocyte cultures congenitally infected with the duck hepatitis B virus (DHBV). Both compounds inhibited DHBV DNA replication to a comparable extent during continuous short-term treatment of the cultures. However penciclovir was more active both during longer-term continuous treatment (50% inhibitory concentrations: penciclovir, 0.7 +/- 0.1 microM; ganciclovir, 4.0 +/- 0.2 microM) and in washout experiments (50% inhibitory concentrations: penciclovir, 3.0 +/- 0.4 microM; ganciclovir, 46 +/- 1.5 microM) designed to compare the persistence of inhibitory activity after removal of the extracellular compound. The effects on viral protein synthesis were similar to the effects on viral DNA replication. These data suggest that penciclovir or its oral form, famciclovir, may have clinical utility in the treatment of chronic hepatitis B virus infection. Images PMID:8031035

Shaw, T; Amor, P; Civitico, G; Boyd, M; Locarnini, S

1994-01-01

379

Chemical composition and in vitro antifungal activity screening of the Allium ursinum L. (Liliaceae).  

PubMed

The objective of the study was to summarize the methods for isolating and identifying natural sulfur compounds from Allium ursinum (ramson) and to discuss the active constituents with regard to antifungal action. Using chromatographic techniques, the active constituents were isolated and subsequently identified. Analyses by high-performance liquid chromatography (HPLC) suggested that these compounds were sulfur constituents, with a characteristic absorbance at 250 nm. Gas chromatography-mass spectrometry (GC-MS) analyses allowed the chemical structures of the isolated constituents to be postulated. We adopted the same methods to identify the health-giving profiling of ramsons and the effects are thought to be primarily derived from the presence and breakdown of the alk(en)ylcysteine sulphoxide, alliin and its subsequent breakdown to allicin (sulfur-compounds of ramson) in connection with antifungal action. The aim of the study was the characterization of the chemical composition of ramsons and the testing of the action of the in vitro extracts, on different strains of Candida albicans. The main goal was to highlight the most efficient extracts of Allium ursinum that can provide long-term antifungal activity without remissions. The extracts from Allium ursinum plants, inhibited growth of Candida spp. cells at concentrations ranging from 0.5 to 4.0 mg/mL, while that of adherent cells at concentrations ranging from 1.0 to > 4.0 mg/mL, depending on the yeast and plant species. PMID:22408399

Bagiu, Radu Vasile; Vlaicu, Brigitha; Butnariu, Monica

2012-01-01

380

Human tumor cells cultured "in vitro" activate platelet function by producing ADP or thrombin.  

PubMed

We studied the effects on platelet function of different human tumour cells cultured "in vitro": Mo T lymphocyte cell line, NCI-N592 small cell lung carcinoma cell line, and 5637 bladder carcinoma cell line. Mo and NCI-N592 cells possessed a slight, dose-dependent platelet aggregating activity, which was completely abolished by apyrase and unaffected by hirudin. The cell-free supernatant also induced an aggregation response, which was very similar to that obtained with tumour cell suspensions. The presence of ADP in the cell-free supernatants of cell suspensions was confirmed by HPLC analysis. On the contrary, aggregation induced by 5637 cells was preceded by a significant lag phase; it was not affected by apyrase but it was abolished by hirudin, and the cell-free supernatant had no effect. These data suggest that Mo and NCI-N592 cells activate platelets by producing ADP, while 5637 cells stimulate platelet function by generating thrombin. The amount of ADP produced by the first two tumour cell lines was measured by bioassay: the extent of such production was similar for both cell lines and the maximum was reached after 60 minutes and maintained for up to 3 hours. These results suggest that neoplastic cells can activate platelets by different mechanisms: such investigations should be performed in homologous systems and in well-defined experimental conditions. PMID:2628235

Zucchella, M; Dezza, L; Pacchiarini, L; Meloni, F; Tacconi, F; Bonomi, E; Grignani, G; Notario, A

1989-01-01

381

Chemical Composition and in Vitro Antifungal Activity Screening of the Allium ursinum L. (Liliaceae)  

PubMed Central

The objective of the study was to summarize the methods for isolating and identifying natural sulfur compounds from Allium ursinum (ramson) and to discuss the active constituents with regard to antifungal action. Using chromatographic techniques, the active constituents were isolated and subsequently identified. Analyses by high-performance liquid chromatography (HPLC) suggested that these compounds were sulfur constituents, with a characteristic absorbance at 250 nm. Gas chromatography-mass spectrometry (GC-MS) analyses allowed the chemical structures of the isolated constituents to be postulated. We adopted the same methods to identify the health-giving profiling of ramsons and the effects are thought to be primarily derived from the presence and breakdown of the alk(en)ylcysteine sulphoxide, alliin and its subsequent breakdown to allicin (sulfur-compounds of ramson) in connection with antifungal action. The aim of the study was the characterization of the chemical composition of ramsons and the testing of the action of the in vitro extracts, on different strains of Candida albicans. The main goal was to highlight the most efficient extracts of Allium ursinum that can provide long-term antifungal activity without remissions. The extracts from Allium ursinum plants, inhibited growth of Candida spp. cells at concentrations ranging from 0.5 to 4.0 mg/mL, while that of adherent cells at concentrations ranging from 1.0 to > 4.0 mg/mL, depending on the yeast and plant species. PMID:22408399

Bagiu, Radu Vasile; Vlaicu, Brigitha; Butnariu, Monica

2012-01-01

382

Evaluation of nitric oxide scavenging activity of certain spices in vitro: a preliminary study.  

PubMed

The plant extracts of some commonly used spices were examined for their possible regulatory effect on nitric oxide (NO) levels using sodium nitroprusside as a NO donor in vitro. Most of the extracts tested demonstrated direct scavenging of NO and exhibited significant activity and the potency of scavenging activity was in the following order: Foeniculum vulgare (aqueous) > Citrus limettiodes > Murraya koenigii (seed, aqueous) > Murraya koenigii (leaf, aqueous) > Curcuma aromatica (aqueous) > Murraya koenigii (leaf, dichloromethane:methanol) > Mentha arvensis (chloroform) > Mentha arvensis (aqueous) > Curcuma longa > Gingko biloba > Foeniculum vulgare (dichloromethane:methanol) > Zingiber officinale (aqueous) > Curcuma aromatica (ethanolic) > Murraya koenigii (seed, dichloromethane:methanol). All the evaluated extracts exhibited a dose-dependent NO scavenging activity. The aqueous extract of Foeniculum vulgare showed a greatest NO scavenging effect of 79.75% at 62.5 microg/mL as compared to the positive control, Gingko biloba where 36.22% scavenging was observed at similar concentration. The present results suggest that these spices might be potent and novel therapeutic agents for scavenging of NO and the regulation of pathological conditions caused by excessive generation of NO and its oxidation product, peroxynitrite. PMID:13678266

Baliga, Manjeshwar Shrinath; Jagetia, Ganesh Chandra; Rao, Shaival Kamalaksha; Babu, Kiran

2003-08-01

383

In vitro activity of tylvalosin against Spanish field strains of Mycoplasma hyopneumoniae.  

PubMed

Mycoplasma hyopneumoniae is involved in the porcine enzootic pneumonia and respiratory disease complex; therefore, the search for new treatment options that contribute to the control of this organism is relevant. The minimal inhibitory concentrations (MICs) and minimal bactericidal concentrations of tylvalosin and 19 other antimicrobial agents against 20 Spanish field isolates of M. hyopneumoniae were determined using the broth microdilution method, with the type strain (J) as a control strain. Tylvalosin had MIC50 and MIC90 values of 0.016 and 0.06?µg/ml, respectively, and was the second-most effective of the assayed antibiotics, after valnemulin. Tiamulin, tylosin and lincomycin were also among the antibiotics with the lowest MIC50 and MIC90 values against the 20 field isolates (0.06-0.25?µg/ml). However, resistance to tylosin and spiramycin, which like tylvalosin, are 16-membered macrolides, was observed. The MIC50 and MIC90 values for ciprofloxacin and enrofloxacin ranged from 0.125 to 1?µg/ml; the corresponding values ranged from 2 to 4?µg/ml for oxytetracyline, which was the most active tetracycline. Furthermore, tylvalosin and valnemulin exhibited the highest bactericidal activities. In conclusion, the macrolide tylvalosin and the pleuromutilin valnemulin exhibited the highest in vitro antimicrobial activities against M. hyopneumoniae field isolates in comparison with the other tested antibiotics. PMID:25185108

Tavío, M M; Poveda, C; Assunçăo, P; Ramírez, A S; Poveda, J B

2014-11-29

384

Extraction, characterization and in vitro antioxidant activity of polysaccharides from black soybean.  

PubMed

Optimization of extraction conditions, preliminary characterization and in vitro antioxidant activity of polysaccharides from black soybean (BSPS) were investigated. The results of Box-Behnken design showed that the optimal extraction conditions for BSPS were as follows: ratio of water to material of 20 ml/g, extraction time of 6.4h and extraction temperature of 92 °C, with a corresponding yield of 2.56%. The crude BSPS were further fractionated on DEAE-52 and Sepharose CL-4B chromatography to afford three purified fractions (BSPS-1, BSPS-2 and BSPS-3). Chemical analysis showed that the three purified fractions were mainly composed of carbohydrate and uronic acid. In addition, BSPS-1 was composed of arabinose, rhamnose, galactose, glucose and mannose in the molar ratio of 1.79:1.00:2.59:26.54:1.01. BSPS-2 was composed of arabinose, rhamnose, xylose, galactose and mannose in the molar ratio of 8.10:4.80:9.15:13.38:1.00. BSPS-3 was composed of arabinose, rhamnose, galactose and mannose in the molar ratio of 16.80:3.60:33.66:1.00. The results of Fourier transform-infrared spectroscopy further confirmed the characteristic polysaccharide structures of the three purified fractions. Moreover, antioxidant assays showed crude BSPS and its purified fractions had potential superoxide anion and DPPH radical scavenging activities, and their antioxidant activity decreased in the order of crude BSPS > BSPS-3 > BSPS-2 > BSPS-1. PMID:25256548

Liu, Jun; Wen, Xiao-yuan; Zhang, Xue-qing; Pu, Hui-min; Kan, Juan; Jin, Chang-hai

2015-01-01

385

Phenolics, aroma profile, and in vitro antioxidant activity of Italian dessert passito wine from Saracena (Italy).  

PubMed

A traditional sweet dessert wine from Saracena (Italy), made with nonmacerated local white grapes (Guarnaccia, Malvasia and Moscato), was analyzed for phenolics and aroma profile and antioxidant activities. The most abundant classes of phenols identified by high-performance liquid chromatography were hydroxybenzoic acids and flavan-3-ols, where gallic acid showed the highest content (376.5 mg/L). The analysis by solid phase microextraction-gas chromatography-mass spectrometry revealed the presence of superior alcohols (from iso-butanol and iso-amyl alcohol up to 2-phenylethanol) and their ethyl esters, terpenes (such as linalool), furfuryl compounds, and free fatty acids (up to palmitic acid) as the key odorants of this wine. The antioxidant activity, evaluated by different in vitro assays 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS), and ?-carotene bleaching test), showed that passito wine had a radical scavenging activity (IC50 value of 0.03 v/v against DPPH·) and inhibited linoleic acid oxidation with an IC50 value of 0.4 v/v after 30 min of incubation. PMID:23574495

Loizzo, Monica R; Bonesi, Marco; Di Lecce, Giuseppe; Boselli, Emanuele; Tundis, Rosa; Pugliese, Alessandro; Menichini, Francesco; Frega, Natale Giuseppe

2013-05-01

386

Growth and Metabolic Activity of Lemon Juice Vesicle Explants in Vitro1  

PubMed Central

Actively growing juice-vesicle explants, established from small lemon (Citrus limon L. Burm. f. var. `Eureka') fruits, were cultured in vitro on defined media. The juice vesicles continued to enlarge in culture for several months, without callus proliferation, and their initial growth was promoted by indoleacetic acid, gibberellic acid, and N6-benzyladenine. The metabolic competence of the explants, and its relevance to whole fruit development, was further investigated. Juice vesicles continued to accumulate protein on all media, for at least 16 days, but sugars did not change much during culture. Acid invertase increased dramatically during the first days of culture, and its specific activity was markedly promoted by indoleacetic acid, and to a lesser degree by gibberellic acid. Total peroxidase of juice vesicles increased progressively up to the 11th day of culture, and its specific activity was promoted by all three hormones, especially by N6-benzyladenine. Explant growth was accompanied by appearance of several cathodic and anodic isoperoxidases. The results suggest that the study of this unique juice vesicle system may contribute to a better understanding of fruit development. Images PMID:16662136

Altman, Arie; Gülsen, Yücel; Goren, Raphael

1982-01-01

387

In vitro and in vivo antitumor activity of tiliacorinine in human cholangiocarcinoma.  

PubMed

Cholangiocarcinoma (CCA) is a fatal cancer with poor prognosis and less than 10% of CCA patients can be offered surgical cure. Conventional chemotherapy results in unfavorable outcomes. At present, plant-derived compounds are gaining interest as potential cancer therapeutics, particularly for treatment-refractory cancers. In this study, antitumor activity of tiliacorinine, the major alkaloid isolated from a tropical plant, on CCA was first demonstrated. Antiproliferative effects of tiliacorinine on human CCA cell lines were investigated using SRB assays. Acridine orange/ethidium bromide staining, flow cytometric analysis and DNA laddering assays were used for apoptotic determination. Apoptosis-related proteins were verified by Western blotting and antitumor activity of tiliacorinine in vivo was demonstrated in CCA xenografted mice. Tiliacorinine significantly inhibited proliferation of human CCA cell lines with IC50 4.5-7 ?M by inducing apoptosis through caspase activation, up- regulation of BAX, and down-regulation of BclxL and XIAP. Tiliacorinine considerably reduced tumor growth in CCA xenografted mice. These results demonstrated antitumor effects of tiliacorinine on human CCA in vitro and in vivo. Tiliacorinine may be an effective agent for CCA treatment. PMID:25227861

Janeklang, Somkid; Nakaew, Archawin; Vaeteewoottacharn, Kulthida; Seubwai, Wunchana; Boonsiri, Patcharee; Kismali, Gorkem; Suksamrarn, Apichart; Okada, Seiji; Wongkham, Sopit

2014-01-01

388

Chitosan-cinnamon beads enhance suppressive activity against Rhizoctonia solani and Meloidogyne incognita in vitro.  

PubMed

A novel chitosan-cinnamon bead carrier was prepared in this study. Chitosan was mixed with cinnamon powder (CP) and cinnamon extract (CE) to obtain chitosan-cinnamon powder (CCP) beads and chitosan-cinnamon extracted (CCE) beads, respectively. The potential antifungal and nematicidal activities of CCP and CCE were investigated against Rhizoctonia solani and Meloidogyne incognita in vitro. Relative antifungal activity of the CCP (5% CP) bead-treated R. solani was 30.9 and 23.9% after 1 and 2 day incubations, respectively. Relative antifungal activity of the CCE (0.5% CE) bead-treated R. solani was 4.3, 3.0 and 4.2% after 1, 2 and 3 days of incubation. Inhibition of hatch by CCP beads with CP of 5% was 78.8%. Inhibition of hatch by CCE beads with CE of 0.5% was 82.0%. J2 mortality following the CCP (5% CP) and CCE (0.5% CE) bead treatments was 85.0 and 95.8%, respectively against M. incognita after 48 h incubations. PMID:24417978

Seo, Dong-Jun; Nguyen, Dang-Minh-Chanh; Park, Ro-Dong; Jung, Woo-Jin

2014-01-01

389

Activity and interactions of antibiotic and phytochemical combinations against Pseudomonas aeruginosa in vitro.  

PubMed

In this study the in vitro activities of seven antibiotics (ciprofloxacin, ceftazidime, tetracycline, trimethoprim, sulfamethoxazole, polymyxin B and piperacillin) and six phytochemicals (protocatechuic acid, gallic acid, ellagic acid, rutin, berberine and myricetin) against five P. aeruginosa isolates, alone and in combination are evaluated. All the phytochemicals under investigation demonstrate potential inhibitory activity against P. aeruginosa. The combinations of sulfamethoxazole plus protocatechuic acid, sulfamethoxazole plus ellagic acid, sulfamethoxazole plus gallic acid and tetracycline plus gallic acid show synergistic mode of interaction. However, the combinations of sulfamethoxazole plus myricetin shows synergism for three strains (PA01, DB5218 and DR3062). The synergistic combinations are further evaluated for their bactericidal activity against P. aeruginosa ATCC strain using time-kill method. Sub-inhibitory dose responses of antibiotics and phytochemicals individually and in combination are presented along with their interaction network to suggest on the mechanism of action and potential targets for the phytochemicals under investigation. The identified synergistic combinations can be of potent therapeutic value against P. aeruginosa infections. These findings have potential implications in delaying the development of resistance as the antibacterial effect is achieved with lower concentrations of both drugs (antibiotics and phytochemicals). PMID:20941374

Jayaraman, Premkumar; Sakharkar, Meena K; Lim, Chu Sing; Tang, Thean Hock; Sakharkar, Kishore R

2010-01-01

390

In Vitro Antileishmanial Activity of Essential Oil of Vanillosmopsis arborea (Asteraceae) Baker  

PubMed Central

The search for new immunopharmacological chemical agents to treat various diseases caused by bacteria, fungi, and protozoa, such as leishmaniasis, for example, has led to the exploration of potential products from plant species and their main active ingredients. Antimonial drugs are the current treatment for leishmaniasis. These drugs cause major side effects and frequent discontinuation of treatment. In this study, we evaluated the in vitro leishmanicidal activity of essential oil of Vanillosmopsis arborea (VAEO) and its major compound ?-bisabolol against Leishmania amazonensis. The essential oil and ?-bisabolol showed activity against promastigotes (IC50 7.35 and 4.95??g/mL resp.) and intracellular amastigotes (IC50 12.58 and 10.70??g/mL, resp.). Neither product showed any cytotoxicity on treated macrophages. The ultrastructural analysis of promastigotes incubated with VAEO or ?-bisabolol at 30??g/mL, showed morphological changes with the accumulation of vesicles electrodense lipid inclusions. The results give evidence that both VAEO and ?-bisabolol have potential as new therapeutic agents against leishmaniasis. PMID:23935675

Colares, Aracélio Viana; Almeida-Souza, Fernando; Taniwaki, Noemi Nosomi; Souza, Celeste da Silva Freitas; da Costa, José Galberto Martins; Calabrese, Kátia da Silva; Abreu-Silva, Ana Lúcia

2013-01-01

391

Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones.  

PubMed

A series of novel 5-alkyl/aryl thiadiazole substituted thiazolidin-4-ones were synthesized by a two-step process. In the first step, 5-alkyl/aryl substituted 2-aminothiadiazoles were synthesized, which on reaction with substituted aromatic aldehydes and thioglycolic acid in the presence of dicyclohexylcarbodiimide afforded thiazolidin- 4-ones. All the compounds were synthesized in fairly good yields and their structures were confirmed by spectral and physical data. The title compounds were screened for in vitro anti-proliferative activity on human breast adenocarcinoma cells (MCF-7) by MTT assay. Most of the derivatives showed an IC?? less than 150 ?mol L?ą. Among the compounds tested, 2-(2-nitrophenyl)- 3-(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3f), 2-(3-fluorophenyl)-3-(5-methyl-1,3,4-thiadiazol-2- -yl)-thiazolidin-4-one (3b), and 2-(4-chlorophenyl)-3- -(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3c) were found to be the most active derivatives with IC50 values of 46.34, 66.84, and 60.71 ?mol L?ą, respectively. Antioxidant studies of all the synthesized compounds were carried out by diphenylpicrylhydrazyl (DPPH) assay. Among the compounds tested, 2-phenyl-3-(5-styryl- -1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3s) elicited superior antioxidant activity with IC?? of 161.93 ?mol L?ą. PMID:24152899

Joseph, Alex; Shah, Chaitanyakumar S; Kumar, Suthar Sharad; Alex, Angel Treasa; Maliyakkal, Naseer; Moorkoth, Sudheer; Mathew, Jessy Elizabeth

2013-09-01

392

In Vitro Antifungal Activity of Ankaferd Blood Stopper Against Candida albicans  

PubMed Central

Background Candida albicans is a memeber of the oral flora that can lead to various complications in immunosupresive patients after oral surgery processes. Ankaferd Blood Stopper® (ABS) is a medical plant extract that is safe to use in patients with dental surgery bleedings in Turkey. Objective The study evaluated the antifungal activity of ABS medicinal plant extract against C albicans using the agar diffusion and broth microdilution methods. Methods The plant extract antifungal activity was assessed in vitro either by applying the ABS extract directly and by applying different concentrations of ABS onto Candida culture. For these experiments, an agar diffusion method was used. To determine the minimum inhibitory concentration (MIC), a broth microdilution method was used. Results Different volumes of the active substance (10, 20, 30, and 40 ?L) were applied onto Candida (0.5 McFarland solution) cultivated plate; Candida growth was inhibited in accordance with the volumes of ABS. However, when various dilutions of ABS (1:2, 1:20, 1:40, and 1:80) were added as drops containing 20 ?L, no antifungal effects were found. No MIC values were identified using broth microdilution. When different dilutions of ABS containing 100 ?L of 0.5 McFarland solution of C albicans were cultured depending on the time (10, 20, 30, and 40 minutes), the effect of the duration was not significant. Conclusion The various tests were carried out to investigate antifungal effects of ABS on Candida, but none were found. PMID:24648581

Ciftci, Sevgi; Keskin, Fahriye; Keceli Ozcan, Sema; Erdem, Mehmet Ali; Cankaya, Burak; Bingol, Recep; Kasapoglu, Cetin

2011-01-01

393

Synthesis, in vitro antimicrobial and cytotoxic activities of new carbazole derivatives of ursolic acid.  

PubMed

A series of new carbazole derivatives of ursolic acid were designed and synthesized in an attempt to develop potent antimicrobial or antitumor agents. Their structures were confirmed by using IR, HRMS and (1)H NMR analysis. All the synthesized compounds were evaluated for their antimicrobial activity against four bacterial and three fungal strains using serial dilution method. Compounds 3a, 3b, 4a, 4b and 5a-f exhibited significant antibacterial activity against at least one tested bacteria with MIC values of 3.9-15.6?g/ml. In addition, the in vitro cytotoxicity of these compounds were also assayed against two human tumor cell lines (SMMC-7721 and HepG2) using MTT colorimetric method. From the results, compounds 5a-e and 5h displayed pronounced cytotoxic activity with IC50 values below 10?M. Specially, compound 5e was found to be the most potent compound with IC50 values of 1.08±0.22 and 1.26±0.17?M against SMMC-7721 and HepG2 cells, respectively, comparable to those of doxorubicin. In addition, compound 5e showed reduced cytotoxicity against noncancerous LO2 cells with IC50 value of 5.75±0.48?M. PMID:25537271

Gu, Wen; Hao, Yun; Zhang, Guang; Wang, Shi-Fa; Miao, Ting-Ting; Zhang, Kang-Ping

2015-02-01

394

Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.  

PubMed

Proviral insertion of Moloney virus (PIM) 1, 2, and 3 kinases are serine/threonine kinases that normally function in survival and proliferation of hematopoietic cells. As high expression of PIM1, 2, and 3 is frequently observed in many human malignancies, including multiple myeloma, non-Hodgkins lymphoma, and myeloid leukemias, there is interest in determining whether selective PIM inhibition can improve outcomes of these human cancers. Herein, we describe our efforts toward this goal. The structure guided optimization of a singleton high throughput screening hit in which the potency against all three PIM isoforms was increased >10,000-fold to yield compounds with pan PIM K is < 10 pM, nanomolar cellular potency, and in vivo activity in an acute myeloid leukemia Pim-dependent tumor model is described. PMID:24900629

Burger, Matthew T; Han, Wooseok; Lan, Jiong; Nishiguchi, Gisele; Bellamacina, Cornelia; Lindval, Mika; Atallah, Gordana; Ding, Yu; Mathur, Michelle; McBride, Chris; Beans, Elizabeth L; Muller, Kristine; Tamez, Victoriano; Zhang, Yanchen; Huh, Kay; Feucht, Paul; Zavorotinskaya, Tatiana; Dai, Yumin; Holash, Jocelyn; Castillo, Joseph; Langowski, John; Wang, Yingyun; Chen, Min Y; Garcia, Pablo D

2013-12-12

395

In-vitro activity of levofloxacin, a new fluoroquinolone: evaluation against Haemophilus influenzae and Moraxella catarrhalis.  

PubMed

The in-vitro activity of levofloxacin was studied against 10 beta-lactamase-negative and 93 beta-lactamase-positive Moraxella catarrhalis isolates, and 65 beta-lactamase-negative and 35 beta-lactamase-positive Haemophilus influenzae isolates. The MICs of levofloxacin were determined by agar dilution on Mueller-Hinton agar (with the addition of 5% horse blood for M. catarrhalis) or on Haemophilus Test Medium for H. influenzae, and were compared with those of ofloxacin, ciprofloxacin and sparfloxacin, as well as pefloxacin and D-ofloxacin for M. catarrhalis. The fluoroquinolones showed similar activity against isolates of H. influenzae and M. catarrhalis, irrespective of beta-lactamase production. Levofloxacin (MIC50/90 0.06 mg/L) was 64 times more active against M. catarrhalis than D-ofloxacin (MIC50/90 4/8 mg/L) and twice as active as ofloxacin (MIC50/90 0.125 mg/L). Ciprofloxacin had an MIC50/90 of 0.03/0.06 mg/L and sparfloxacin showed an MIC50/90 of 0.015 mg/L against M. catarrhalis irrespective of the resistance phenotype of the isolates. Against H. influenzae, levofloxacin was twice as active as ofloxacin (MIC90 values 0.03 mg/L versus 0.06 mg/L), while the MIC90s of ciprofloxacin and sparfloxacin were both 0.015 mg/L. Our results therefore suggest that levofloxacin has potential for treating respiratory tract infections caused by H. influenzae and M. catarrhalis. PMID:10404333

Kitzis, M D; Goldstein, F W; Miegi, M; Acar, J F

1999-06-01

396

In vitro activities of metronidazole and its hydroxy metabolite against Bacteroides spp.  

PubMed Central

Metronidazole is metabolized to two major oxidative products: an acid metabolite and a hydroxy metabolite. While the activity of the acid metabolite is negligible, the activity of the hydroxy metabolite is approximately 65% of the activity of the parent drug. Pharmacokinetic studies of metronidazole and its hydroxy metabolite have shown that the MICs of both compounds remain above the MICs for most anaerobic organisms over an 8-h dosing interval. By a checkerboard assay, the combined activities of metronidazole and the hydroxy metabolite were examined against 4 quality control strains of Bacteroides species. Macrobroth tube dilutions were set up with Wilkins-Chalgren broth. Serial twofold dilutions of each agent were performed to achieve final concentrations ranging from 0.06 to 4.0 micrograms/ml. The MICs for Bacteroides fragilis and B. distasonis were 1.0 microgram/ml for both parent drug and metabolite. For B. thetaiotamicron and B. ovatus, the MICs of metronidazole and the hydroxy metabolite were 1.0 and 2.0 micrograms/ml, respectively. Synergy was determined by calculating the fractional inhibitory concentration (FIC) index. The interpretative criteria for the FIC index were as follows: synergy, FIC < or = 0.5; partial synergy, 0.51 to 0.75; indifference, FIC 0.76 to 4.0; and antagonism, FIC > 4.0. Partial synergy was observed for the four anaerobes tested, with FIC indices ranging from 0.63 to 0.75. On the basis of this data, in vitro susceptibilities to agents such as metronidazole may ultimately require reevaluation to account for active metabolites. PMID:7811027

Pendland, S L; Piscitelli, S C; Schreckenberger, P C; Danziger, L H

1994-01-01

397

In vitro antimycoplasmal activity of Citrus bergamia essential oil and its major components.  

PubMed

Forty-two strains of Mycoplasma hominis (including PG21), 2 strain of Mycoplasma fermentans (Pg18 and K7), 1 strain of Mycoplasma pneumoniae (strain m129) were investigated for their susceptibilities to Citrus bergamia essential oil and to its major components (limonene, linalyl acetate and linalool). C. bergamia essential oil inhibited mycoplasmas at concentrations from 0.5 to 1% (MIC value as % v/v). M. hominis showed MIC(50) values of 0.5% and MIC(90) values of 1%; M. pneumoniae showed a MIC value of 0.5% while M. fermentans strains were inhibited by MIC values of 1%. M. pneumoniae and M. hominis shared the same susceptibility to linalyl acetate, with MIC values of 0.015% (corresponding to MIC(50) and MIC(90) for M. hominis); M. fermentans strains were less susceptible with MIC values of 0.12%. Among the major components tested, linalool showed higher activity against M. pneumoniae and M. fermentans (MIC values of 0.015 and 0.06%, respectively) but was less active against M. hominis (MIC(50) and MIC(90) values of both 1%); limonene was active against M. pneumoniae (MIC value of 0.03%) but was less active against M. fermentans (MIC values of 1%) and M. hominis (both MIC(50) and MIC(90) values of ?4%). The results indicated that C. bergamia essential oil and its major components had shown an interesting in vitro antimycoplasmal activity. PMID:22465092

Furneri, Pio Maria; Mondello, Luigi; Mandalari, Giuseppina; Paolino, Donatella; Dugo, Paola; Garozzo, Adriana; Bisignano, Giuseppe

2012-06-01

398

Shikonin Exerts Antitumor Activity via Proteasome Inhibition and Cell Death Induction in vitro and in vivo  

PubMed Central

Dysregulation of the ubiquitin-proteasome pathway plays an essential role in tumor growth and development. Shikonin, a natural naphthoquinone isolated from the traditional Chinese medicine Zi Cao (gromwell), has been reported to possess tumor cell-killing activity, and results from a clinical study using a shikonin-containing mixture demonstrated its safety and efficacy for the treatment of late-stage lung cancer. In the present study, we reported that shikonin is an inhibitor of tumor proteasome activity in vitro and in vivo. Our computational modeling predicts that the carbonyl carbons C1 and C4 of shikonin potentially interact with the