Sample records for vitro schistosomicidal activity

  1. In Vitro Schistosomicidal Activity of Some Brazilian Cerrado Species and Their Isolated Compounds

    PubMed Central

    Cunha, Nayanne Larissa; Uchôa, Camila Jacintho de Mendonça; Cintra, Lucas Silva; de Souza, Herbert Cristian; Peixoto, Juliana Andrade; Silva, Claudia Peres; Magalhăes, Lizandra Guidi; Gimenez, Valéria Maria Meleiro; Groppo, Milton; Rodrigues, Vanderlei; da Silva Filho, Ademar Alves; Andrade e Silva, Márcio Luís; Cunha, Wilson Roberto; Pauletti, Patrícia Mendonça; Januário, Ana Helena

    2012-01-01

    Miconia langsdorffii Cogn. (Melastomataceae), Roupala montana Aubl. (Proteaceae), Struthanthus syringifolius (Mart.) (Loranthaceae), and Schefflera vinosa (Cham. & Schltdl.) Frodin (Araliaceae) are plant species from the Brazilian Cerrado whose schistosomicidal potential has not yet been described. The crude extracts, fractions, the triterpenes betulin, oleanolic acid, ursolic acid and the flavonoids quercetin 3-O-?-D-rhamnoside, quercetin 3-O-?-D-glucoside, quercetin 3-O-?-D-glucopyranosyl-(1-2)-?-L-rhamnopyranoside and isorhamnetin 3-O-?-D-glucopyranosyl-(1-2)-?-L-rhamnopyranoside were evaluated in vitro against Schistosoma mansoni adult worms and the bioactive n-hexane fractions of the mentioned species were also analyzed by GC-MS. Betulin was able to cause worm death percentage values of 25% after 120?h (at 100??M), and 25% and 50% after 24 and 120?h (at 200??M), respectively; besides the flavonoid quercetin 3-O-?-D-rhamnoside promoted 25% of death of the parasites at 100??M. Farther the flavonoids quercetin 3-O-?-D-glucoside and quercetin 3-O-?-D-rhamnoside at 100??M exhibited significantly reduction in motor activity, 75% and 87.5%, respectively. Biological results indicated that crude extracts of R. montana, S. vinosa, and M. langsdorffii and some n-hexane and EtOAc fractions of this species were able to induce worm death to some extent. The results suggest that lupane-type triterpenes and flavonoid monoglycosides should be considered for further antiparasites studies. PMID:22924053

  2. In vitro schistosomicidal effects of aqueous and dichloromethane fractions from leaves and stems of Piper species and the isolation of an active amide from P. amalago L. (Piperaceae).

    PubMed

    Carrara, V S; Vieira, S C H; de Paula, R G; Rodrigues, V; Magalhăes, L G; Cortez, D A G; Da Silva Filho, A A

    2014-09-01

    Dichloromethane and aqueous fractions from leaves and stems of Piper arboreum Aubl., P. aduncum L., P. amalago L., P. crassinervium H.B. & K., P. diospyrifolium Kunth, P. hispidum Sw. and P. xylosteoides (Kunth) Steud. were tested against adult worms of Schistosoma mansoni. The in vitro activity was evaluated in terms of mortality, number of separated worms and number of worms with reduced motor activity. Most dichloromethane fractions from all Piper species showed moderate schistosomicidal activity, but aqueous fractions were not active. The dichloromethane fraction of P. amalago leaves (at 100 ?g/ml) showed the highest activity, resulting in worm mortality, the separation of worm pairs and reduced motor activity. Chromatographic fractionation of the dichloromethane fraction of P. amalago leaves led to the isolation of its major compound, which was also tested against adults of S. mansoni. The isolated piperamide N-[7-(3',4'-methylenedioxyphenyl)-2(Z),4(Z)-heptadienoyl] pyrrolidine, at 100 ? m, resulted in the mortality of all adult worms after 24 h of incubation. The findings suggest that species of Piper are potential sources of schistosomicidal compounds. PMID:23561585

  3. Cytochalasin D abolishes the schistosomicidal activity of praziquantel.

    PubMed

    Pica-Mattoccia, Livia; Valle, Cristiana; Basso, Annalisa; Troiani, Anna Rita; Vigorosi, Fabio; Liberti, Piero; Festucci, Alfredo; Cioli, Donato

    2007-04-01

    To test the hypothesis that calcium channels of schistosomes are the targets for the action of praziquantel, we subjected schistosomes in vitro to pharmacological agents capable of interfering with the functioning of calcium channels. After 1-h exposure to these agents, praziquantel was added and incubation continued overnight. Worms were then washed, resuspended in drug-free medium and observed during the following 7-10 days. About 50% of schistosomes pre-exposed to the calcium channel blockers nicardipine and nifedipine were able to survive a praziquantel concentration (3 microM) that normally killed the majority of adult male worms. Since the organization of the actin cytoskeleton controls the activity of calcium channels in a number of different systems, we also pre-exposed schistosomes to the actin depolymerizing agent cytochalasin D. This treatment rendered the parasites completely refractory to the effects of very high praziquantel levels (up to 36 microM). These results are consistent with the hypothesis that schistosome calcium channels are involved in the mechanism of action of praziquantel. PMID:17083933

  4. In vivo schistosomicidal activity of three novels 8-hydroxyquinoline derivatives against adult and immature worms of Schistosoma mansoni.

    PubMed

    Allam, Gamal; Eweas, Ahmad F; Abuelsaad, Abdelaziz S A

    2013-09-01

    Schistosomiasis control is widely dependent on a single drug, praziquantel (PZQ). The potential for development of resistance to PZQ has justified the search for new alternative chemotherapies. In a previous study, we have been reported that three of 8-hydroxyquinoline derivatives namely: 3-((8-hydroxyquinolin-5-yl) sulfonyl) pentane-2,4-dione (HQSP), 5-((2,4-diphenyl-3H-benzo[b][1,4]diazepin-3-yl) sulfonyl) quinolin-8-ol (HQBD), and 5-((2,4-diphenyl-3H-pyrido[3,4-b][1,4] diazepin-3-yl) sulfonyl) quinolin-8-ol (HQPD) possess a potent anti-schistosomal activity in vitro. The aim of the present study was to evaluate the in vivo schistosomicidal effect of these three compounds on adult and immature worms of Schistosoma mansoni and their induced pathology. Treatment of S. mansoni-infected mice with 1000, 250, 150, and 200 mg/kg body weight of PZQ, HQSP, HQBD, and HQPD, respectively, reduced adult and immature worm burden by 94.63 and 31.32%, 73.63 and 5.45%, 76.5 and 28.11%, and 81.25 and 56.84%, respectively, compared to infected untreated mice. Moreover, numbers of egg per gram liver and intestine were decreased by 84 and 95.51%, 47.84 and 46.28 %, 53.18 and 59.37 %, and 54.22 and 67.26 as a result of PZQ, HQSP, HQBD, and HQPD treatment, respectively. Hepatic granuloma volume was also reduced by 40.10, 42.96, 35.72, and 72.09% due to PZQ, HQSP, HQBD, and HQPD treatment, respectively. In addition, hepatic histopathological alterations and collagen fiber deposition that accompanied with S. mansoni infection were largely retrieved with different treatments, especially HQPD treatment. Furthermore, humoral immune response, especially IgG response against S. mansoni antigens, was augmented with different treatments. This study concluded that among the three tested 8-hydroxyquinoline derivatives, HQPD is the most effective compound against adult and pre-mature worms of S. mansoni and can be used for the development of a new schistosomicidal drug. PMID:23793335

  5. Antimycobacterial activity of lichen metabolites in vitro

    Microsoft Academic Search

    Krist??n Ingólfsdóttir; Gavin A. C. Chung; Vilhjálmur G. Skúlason; Stefán R. Gissurarson; Margrét Vilhelmsdóttir

    1998-01-01

    Several compounds, whose structures represent the most common chemical classes of lichen metabolites, were screened for in vitro activity against Mycobacterium aurum, a non-pathogenic organism with a similar sensitivity profile to M. tuberculosis. Of the compounds tested, usnic acid from Cladonia arbuscula exhibited the highest activity with an MIC value of 32 ?g\\/ml. Atranorin and lobaric acid, both isolated from

  6. In vitro antimycoplasmal activity of oleuropein

    Microsoft Academic Search

    Pio Maria Furneri; Andreana Marino; Antonina Saija; Nicola Uccella; Giuseppe Bisignano

    2002-01-01

    The activity of oleuropein, a phenolic glycoside contained in olive oil, was investigated in vitro against Mycoplasma hominis, Mycoplasma fermentans, Mycoplasma pneumoniae and Mycoplasma pirum. Oleuropein inhibited mycoplasmas at concentrations from 20 to 320 mg\\/l. The MICs of oleuropein to M. pneumoniae, M. pirum, M. hominis and M. fermentans were 160, 320, 20 and 20 mg\\/l, respectively.

  7. In vitro activity of ciprofloxacin against mycobacteria

    Microsoft Academic Search

    H. Gaya; M. V. Chadwick

    1985-01-01

    Sir, Ciprofloxacin, a new quinoline carboxylic acid derivative, has high in vitro activity against a wide range of pathogens including members of the family Enterobacteriaeeae and Pseudomonas aeruginosa (1). The pharmacokinetics after oral administration of the drug are characterized by rapid absorption, good diffusion into the extracellular space, and elimination by biliary excretion, hepatic metabolism, glomerular filtration and tubular secretion

  8. Salbutamol exhibits androgenic activity in vitro

    PubMed Central

    von Bueren, André O; Ma, Risheng; Schlumpf, Margret; Lichtensteiger, Walter

    2007-01-01

    Background Salbutamol has been shown to mediate anabolic effects after intravenous administration. However, the mechanism responsible for the anabolic actions of salbutamol remains unknown. Aim To investigate the potential mechanism by which salbutamol mediates anabolic effects in vitro. Methods The potential androgenic activity of salbutamol was investigated in vitro by the A?Screen assay that measures androgen?dependent inhibition of proliferation of the androgen receptor (AR)?positive human mammary carcinoma cell line, MCF7?AR1. Results The assay was validated with three known androgens; methyltrienolone (R1881), 5??dihydrotestosterone (DHT) and danazol. IC50 values of R1881, DHT and danazol, 4.41×10–11, 4.44×10?11 and 1.08×10?8?M, respectively, were in the ranges known from earlier studies. Our results demonstrate that salbutamol exhibits androgenic activity, with an IC50 value of 8.93×10?6?M. Anti?estrogenic or cytotoxic effects, which might have interfered with the assay, were excluded by additional experiments on wild?type MCF7 and MCF7?AR1 cells, respectively. Conclusion These data indicate that salbutamol exerts anabolic effects through androgen receptor agonistic activity in vitro. PMID:17510230

  9. Antimycobacterial activity of lichen metabolites in vitro.

    PubMed

    Ingólfsdóttir, K; Chung, G A; Skúlason, V G; Gissurarson, S R; Vilhelmsdóttir, M

    1998-04-01

    Several compounds, whose structures represent the most common chemical classes of lichen metabolites, were screened for in vitro activity against Mycobacterium aurum, a non-pathogenic organism with a similar sensitivity profile to M. tuberculosis. Of the compounds tested, usnic acid from Cladonia arbuscula exhibited the highest activity with an MIC value of 32 microg/ml. Atranorin and lobaric acid, both isolated from Stereocaulon alpinum, salazinic acid from Parmelia saxatilis and protolichesterinic acid from Cetraria islandica all showed MIC values >/=125 microg/ml. PMID:9795033

  10. In vitro antibacterial activity of ceftizoxime.

    PubMed

    Andreoni, O; Andreoni, S; Molinari, G L; Farinetti, F

    1985-04-01

    During 1983, the antibacterial activity of ceftizoxime has been tested in vitro against 325 strains of Enterobacteriaceae, Streptococcaceae, Micrococcaceae, Pseudomonaceae and Acinetobacter sp. isolated from material of human origin (blood, urine, faeces, sputum, various exudates). Except for S. faecalis and some strains of P. rettgeri, P. aeruginosa, A. calcoaceticus, Staphylococcus spp. all the strains examined were found to be sensitive to the antibiotic, whose MIC was 0.05-1.5 micrograms/ml in the great majority of cases. For 72 ceftizoxime-sensitive strains the MBC/MIC ratio was nearly always under 4:1, confirming the drug's bactericidal activity. On strains of Enterobacteriaceae (E. coli, K. pneumoniae, S. marcescens, S. typhimurium) MIC of ceftizoxime achieved a minimum bactericidal time (MBT) between 3 and 4 hours of bacteria-antibiotic contact, and bacterial survival percentages were, in any case, very low as early as the 1st hour. PMID:3859380

  11. Antioxidant Activity of Rhizoma Cibotii in vitro

    PubMed Central

    Mai, Wenqiong; Chen, Dongfeng; Li, xican

    2012-01-01

    Purpose: The paper tried to systematically investigate the in vitro antioxidant activity of Rhizoma Cibotii (RC) for the first time. Method: The methanol extract from RC (MERC) was prepared then systematically investigated by various antioxidant assays, including: DPPH• (1, 1-diphenyl-2-picrylhydrazyl radical), ABTS•+ (3-ethylbenzthiazoline-6- sulfonic acid diammonium salt radical), •O2- (superoxide anion radical), •OH (hydroxyl radical) scavenging assays, Fe3+ reducing power, Cu2+ reducing power assays, compared with positive controls Trolox (± -6 -hydroxyl -2,5, 7, 8-tetramethlychromane-2-carboxylic acid) and BHA (butylated hydroxyanisole). Its total phenolics and caffeic acid content were also measured by Folin-Ciocalteu method and HPLC, respectively. Result: MERC exhibited effective antioxidant activity in dose-dependent manners and its IC50 values were calculated as 44.2 ± 0.62, 19.84 ± 0.31, 137.66 ± 2.90, 22.94 ± 0.90, 289.73 ± 46.17, 53.52 ± 1.51 µg /mL?for DPPH•, ABTS•+, •O2-, •OH scavenging assays, Fe3+ reducing power, Cu2+ reducing power assays, respectively. Its total phenolics content was 50.88 ± 1.24 mg CAE /g and the caffeic acid content was 1.82 ± 0.19 mg/g. Conclusion: Rhizoma Cibotii has effective in vitro antioxidant activity which may attribute to its total phenolics, among which caffeic acid can be considered as one of the active components. The pharmacological effects or healthcare functions of whole RC may result from the synergistic effects caused by the combination of its components and its antioxidant effect plays an important role in the synergistic effects. PMID:24312778

  12. Anthelmintic Activity of Crude Extract and Essential Oil of Tanacetum vulgare (Asteraceae) against Adult Worms of Schistosoma mansoni

    PubMed Central

    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

    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

  13. In Vitro Anti-Candida Activity of Zataria multiflora Boiss

    Microsoft Academic Search

    Ali Zarei Mahmoudabadi; Muhammad Ali Dabbagh; Zahra Fouladi

    2007-01-01

    Zataria multiflora Boiss known as Avishan Shirazi (in Iran) is one of the valuable Iranian medicinal plants. The aim of study was to evaluate anti-Candida activity of Z. multiflora against different species of Candida in vitro. Anti-Candida activity of the aqueous, ethanolic and methanolic maceration extract of the aerial parts of Z. multiflora Boiss was studied in vitro. Anti-Candida activity

  14. Neutrophil activation in vitro and in vivo in Wegener's granulomatosis

    Microsoft Academic Search

    Elisabeth Brouwer; Minke G Huitema; A H Leontine Mulder; Peter Heeringa; Harry van Goor; Jan Willem Cohen Tervaert; Jan J Weening; Cees G M Kallenberg

    1994-01-01

    Neutrophil activation in vitro and in vivo in kidneys in Wegener's granulomatosis. The mechanisms underlying glomerular capillary wall injury in Wegener's granulomatosis (WG) are not well understood. Anti-neutrophil cytoplasmic antibodies (ANCA), present in sera from patients with WG, are known to stimulate respiratory burst and degranulation of primed polymorphonuclear neutrophils (PMN) in vitro. Experimental studies have shown that oxygen radical

  15. Original article In vitro cholesterol-lowering activity

    E-print Network

    Paris-Sud XI, Université de

    Original article In vitro cholesterol-lowering activity of Lactobacillus plantarum and Lactobacillus paracasei strains isolated from the Italian Castelmagno PDO cheese Simona BELVISO*, Manuela with probiotic characteristics, mostly isolated from human gut. In this work, eight Lactobacillus plantarum

  16. Effects of dental resin metabolites on estrogenic activity in vitro

    Microsoft Academic Search

    Y. Nomura; H. Ishibashi; M. Miyahara; R. Shinohara; F. Shiraishi; K. Arizono

    2003-01-01

    Three monomers (Bis-GMA, UDMA, and TEGDMA) and five polymerization initiators (CQ, BPO, DMPT, DMAEMA, and ATU) commonly used in dental composite resins were tested for estrogenic activity using a reporter gene assay (yeast two-hybrid system) in vitro, and compared with bisphenol-A (BPA). Estrogenic activity was indicated by agonist and antagonist activity, with (+S9) and without (-S9) metabolic activation using rat

  17. Antioxidant activity of Piper betle L. leaf extract in vitro

    Microsoft Academic Search

    Nabasree Dasgupta; Bratati De

    2004-01-01

    Piper betle leaves are used as masticatory in Asian countries. In the present study, antioxidant activities of aqueous extracts of three local varieties of P. betle leaves were evaluated by several in vitro systems, e.g. DPPH radical scavenging activity, superoxide radical scavenging activity in a riboflavin\\/light\\/NBT system, hydroxyl radical scavenging activity and inhibition of lipid peroxidation induced by FeSO4 in

  18. In vitro estrogenic activity of Achillea millefolium L

    Microsoft Academic Search

    G. Innocenti; E. Vegeto; S. Dall’Acqua; P. Ciana; M. Giorgetti; E. Agradi; A. Sozzi; G. Fico; F. Tomč

    2007-01-01

    Isolation and biological characterization of pure compounds was used to identify and characterize estrogenic activity and estrogen receptors (ER) preference in chemical components of Achillea millefolium. This medicinal plant is used in folk medicine as an emmenagogue. In vitro assay, based on recombinant MCF-7 cells, showed estrogenic activity in a crude extract of the aerial parts of A. millefolium. After

  19. 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...

  20. Evaluation of the Anti-Schistosoma mansoni Activity of Thiosemicarbazones and Thiazoles

    PubMed Central

    de Oliveira, Sheilla Andrade; de Oliveira Filho, Gevânio Bezerra; Moreira, Diogo Rodrigo Magalhaes; Gomes, Paulo André Teixeira; da Silva, Anekécia Lauro; de Barros, Andréia Ferreira; da Silva, Aline Caroline; dos Santos, Thiago André Ramos; Pereira, Valéria Ręgo Alves; Gonçalves, Gabriel Gazzoni Araújo; Brayner, Fábio André; Alves, Luiz Carlos; Wanderley, Almir Gonçalves; Leite, Ana Cristina Lima

    2014-01-01

    Schistosomiasis is a chronic and debilitating disease caused by a trematode of the genus Schistosoma and affects over 207 million people. Chemotherapy is the only immediate recourse for minimizing the prevalence of this disease and involves predominately the administration of a single drug, praziquantel (PZQ). Although PZQ has proven efficacy, there is a recognized need to develop new drugs as schistosomicides since studies have shown that repeated use of this drug in areas of endemicity may cause a temporary reduction in susceptibility in isolates of Schistosoma mansoni. Hydrazones, thiosemicarbazones, phthalimides, and thiazoles are thus regarded as privileged structures used for a broad spectrum of activities and are potential candidates for sources of new drug prototypes. The present study determined the in vitro schistosomicidal activity of 10 molecules containing these structures. During the assays, parameters such motility and mortality, oviposition, morphological changes in the tegument, cytotoxicity, and immunomodulatory activity caused by these compounds were evaluated. The results showed that compounds formed of thiazole and phthalimide led to higher mortality of worms, with a significant decline in motility, inhibition of pairing and oviposition, and a mortality rate of 100% starting from 144 h of exposure. These compounds also stimulated the production of nitric oxide and tumor necrosis factor alpha (TNF-?), thereby demonstrating the presence of immunomodulatory activity. The phthalyl thiazole LpQM-45 caused significant ultrastructural alterations, with destruction of the tegument in both male and female worms. According to the present study, phthalyl thiazole compounds possess antischistosomal activities and should form the basis for future experimental and clinical trials. PMID:24165185

  1. In vitro activities of four novel triazoles against Scedosporium spp.

    PubMed

    Carrillo, A J; Guarro, J

    2001-07-01

    In order to develop new approaches to the treatment of the severe and usually fatal infections caused by Scedosporium spp., the in vitro antifungal activities of four novel triazoles (posaconazole, ravuconazole, voriconazole, and UR-9825) and some current antifungals (amphotericin B, ketoconazole, itraconazole, and nystatin) were determined. The latter group was clearly ineffective against the two species tested. The four new antifungals showed activity against Scedosporium apiospermum, and UR-9825 and voriconazole were active against S. prolificans. PMID:11408242

  2. In Vitro Activities of Four Novel Triazoles against Scedosporium spp.

    PubMed Central

    Carrillo, A. J.; Guarro, J.

    2001-01-01

    In order to develop new approaches to the treatment of the severe and usually fatal infections caused by Scedosporium spp., the in vitro antifungal activities of four novel triazoles (posaconazole, ravuconazole, voriconazole, and UR-9825) and some current antifungals (amphotericin B, ketoconazole, itraconazole, and nystatin) were determined. The latter group was clearly ineffective against the two species tested. The four new antifungals showed activity against Scedosporium apiospermum, and UR-9825 and voriconazole were active against S. prolificans. PMID:11408242

  3. In Vitro Antibacterial and Antifungal Activity of Salicylanilide Benzoates

    PubMed Central

    Krátký, Martin; Vinšová, Jarmila; Buchta, Vladimír

    2012-01-01

    The resistance to antimicrobial agents brings a need of novel antimicrobial agents. We have synthesized and found the in vitro antibacterial activity of salicylanilide esters with benzoic acid (2-(phenylcarbamoyl)phenyl benzoates) in micromolar range. They were evaluated in vitro for the activity against eight fungal and eight bacterial species. All derivatives showed a significant antibacterial activity against Gram-positive strains with minimum inhibitory concentrations ?0.98??mol/L including methicillin-resistant Staphylococcus aureus strain. The most active compounds were 5-chloro-2-(3,4-dichlorophenylcarbamoyl)phenyl benzoate and 4-chloro-2-(4-(trifluoromethyl)phenylcarbamoyl)phenyl benzoate. The antifungal activity is significantly lower. PMID:22666101

  4. In vitro antibacterial and antifungal activity of salicylanilide benzoates.

    PubMed

    Krátký, Martin; Vinšová, Jarmila; Buchta, Vladimír

    2012-01-01

    The resistance to antimicrobial agents brings a need of novel antimicrobial agents. We have synthesized and found the in vitro antibacterial activity of salicylanilide esters with benzoic acid (2-(phenylcarbamoyl)phenyl benzoates) in micromolar range. They were evaluated in vitro for the activity against eight fungal and eight bacterial species. All derivatives showed a significant antibacterial activity against Gram-positive strains with minimum inhibitory concentrations ? 0.98??mol/L including methicillin-resistant Staphylococcus aureus strain. The most active compounds were 5-chloro-2-(3,4-dichlorophenylcarbamoyl)phenyl benzoate and 4-chloro-2-(4-(trifluoromethyl)phenylcarbamoyl)phenyl benzoate. The antifungal activity is significantly lower. PMID:22666101

  5. In Vitro Antibacterial Activity of Argemone mexicana L. (Papaveraceae)

    Microsoft Academic Search

    M. Mashiar Rahman; Jahangir Alam; Shamima Akhtar Sharmin; M. Mizanur Rahman; Atiqur Rahman; M. F. Alam

    2009-01-01

    The aim of this study was to examine the efficacy of various extracts from stems of Argemone mexicana L. as antibacterial potential against a range of food-borne bacteria. The antibacterial activity of various extracts (hexane, chloroform, ethyl acetate and ethanol) of A. mexicana L. stems was determined in vitro, using agar diffusion method and MIC determination test against ten (five

  6. Identification and Characterization of in Vitro Galactosyltransferase Activities Involved in

    E-print Network

    Showalter, Allan M.

    of [AO] repetitive units, specifically, a chemically synthesized [AO]7 acceptor and a transgenically]Gal monosaccharide and Hyp-[14 C]Gal disaccharide were identified in the base hydrolysates of the GalT reaction gradient centrifugation. The in vitro assay reported here to detect GalT activities using AGP peptide

  7. Retinol inhibits aromatase activity and expression in vitro

    Microsoft Academic Search

    Henry P. Ciolino; Zhaoli Dai; Vidhya Nair

    2011-01-01

    Aromatase converts androgens into estrogens and is thought to supply a local source of estrogen that facilitates the growth of hormone-responsive tumor cells. Inhibition of aromatase is therefore an important chemopreventive strategy. We investigated the effect of retinol and selected retinoids on the activity and expression of aromatase in two human carcinoma cell lines in vitro. Retinol (ROH) and all-trans

  8. In Vitro Antimicrobial Activities of Bakuchiol against Oral Microorganisms

    Microsoft Academic Search

    HARUMI KATSURA; RYO-ICHI TSUKIYAMA; AKIKO SUZUKI; MAKIO KOBAYASHI

    2001-01-01

    Bakuchiol was isolated from the seeds of Psoralea corylifolia, a tree native to China with various uses in traditional medicine, followed by extraction with ether and column chromatography combined with silica gel and octyldecyl silane. In this study, the antimicrobial activities of bakuchiol against some oral microorganisms were evaluated in vitro. The cell growth of Streptococcus mutans was inhibited in

  9. Icariin suppresses bone resorption activity of rabbit osteoclasts in vitro

    Microsoft Academic Search

    Jian Huang; JinChao Zhang; TianLan Zhang; Kui Wang

    2007-01-01

    The effect of icariin on the bone resorption activity of rabbit osteoclasts is assessed in vitro. Osteoclasts were isolated from Japanese white rabbits and cultured on plates with a sterilized bone slice in each well.\\u000a After treatment with icariin at various concentrations, the bone resorption activity of osteoclasts was evaluated by examining\\u000a pit areas, superoxide anion (·O\\u000a 2\\u000a ?\\u000a )

  10. In Vitro Phytotoxicity and Antioxidant Activity of Selected Flavonoids

    PubMed Central

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

    2012-01-01

    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

  11. Purification and in vitro activities of rabbit platelet microbicidal proteins.

    PubMed Central

    Yeaman, M R; Tang, Y Q; Shen, A J; Bayer, A S; Selsted, M E

    1997-01-01

    Recent in vitro studies have demonstrated that rabbit platelets release a small, cationic antimicrobial protein in response to thrombin stimulation under physiological conditions (M. R. Yeaman, S. M. Puentes, D. C. Norman, and A. S. Bayer, Infect. Immun. 60:1202-1209, 1992). This observation prompted our present investigation, focused on determining the array of antimicrobial proteins contained within rabbit platelets and their in vitro activity against common bloodstream pathogens. A group of small (6.0- to 9.0-kDa), cationic proteins with in vitro antimicrobial activity was purified from whole and thrombin-stimulated rabbit platelets by gel filtration and reversed-phase high-performance liquid chromatography. Purified proteins in micromolar concentrations (10 to 40 microg/ml) exerted in vitro microbiostatic and/or microbicidal activities against Staphylococcus aureus, Escherichia coli, and Candida albicans in a dose-dependent manner. The antimicrobial activities of proteins purified from rabbit platelet acid extracts were generally inversely related to pH, with maximal activity observed at pH 5.5. In contrast, the predominant protein isolated from thrombin-stimulated rabbit platelets, though biochemically and microbiologically similar to proteins extracted by acid, exhibited antimicrobial activities which were modestly enhanced at pH 7.2 compared with pH 5.5. Amino acid compositional analyses in combination with molecular mass determinations suggest that the majority of these proteins are distinct molecules not derived from a single common precursor. Collectively, these data indicate that rabbit platelets contain proteins which exert potent in vitro antimicrobial activity against bacterial and fungal pathogens which commonly invade the bloodstream. Moreover, several of these proteins were released from platelets stimulated with thrombin under physiological conditions and exerted potent antimicrobial activities in physiological pH ranges. These observations support the hypothesis that platelets serve an important role in host defense against infection, via localized release of antimicrobial proteins in response to stimuli associated with tissue injury or microbial colonization. PMID:9038312

  12. Berry polyphenols inhibit pancreatic lipase activity in vitro

    Microsoft Academic Search

    Gordon J. McDougall; Nimish N. Kulkarni; Derek Stewart

    2009-01-01

    Polyphenol-rich extracts from a range of berries were tested for their ability to inhibit pancreatic lipase activity in vitro. Blackcurrant and rowan extracts had no effect, blueberry caused slight inhibition, whilst lingonberry, Arctic bramble, cloudberry, strawberry and raspberry were considerably more effective. Inhibition by the cloudberry extract showed a saturation effect with an apparent EC50 of around 5?g phenols\\/ml.The inhibitory

  13. Effects of flavonoids on aromatase activity, an in vitro study

    Microsoft Academic Search

    C. Pelissero; M. J. P. Lenczowski; D. Chinzi; B. Davail-Cuisset; J. P. Sumpter; A. Fostier

    1996-01-01

    In the study, the inhibitory effect of flavonoids, including isoflavonic phytoestrogens, on the ovarian aromatase enzyme complex from the rainbow trout, Oncorhynchus mykiss, was assessed in vitro. Some of the compounds tested on fish were also tested on human placental aromatase activity as a comparison between the two sources of enzyme. It was found that flavone, dl-aminoglutethimide, apigenin, quercetin, 7,4?-dihydroxyflavone,

  14. Lack of in vitro antimicrosporidian activity of thalidomide.

    PubMed

    Ridoux, O; Drancourt, M

    1999-09-01

    Thalidomide was evaluated for its in vitro activity against Encephalitozoon species by using the MRC-5 cell system. A cytotoxic effect was observed for concentrations of 10(1) microg/ml (P < 10(5)) and 5 microg/ml (P < 10(5)). Thalidomide did not significantly inhibit the growth of any of the microsporidia under study. These data suggest that thalidomide is not an etiologic treatment in microsporidial enteritis. PMID:10471585

  15. Risperidone and Paliperidone Inhibit P-Glycoprotein Activity In Vitro

    Microsoft Academic Search

    Hao-Jie Zhu; Jun-Sheng Wang; John S Markowitz; Jennifer L Donovan; Bryan B Gibson; C Lindsay DeVane

    2007-01-01

    Risperidone (RSP) and its major active metabolite, 9-hydroxy-risperidone (paliperidone, PALI), are substrates of the drug transporter P-glycoprotein (P-gp). The goal of this study was to examine the in vitro effects of RSP and PALI on P-gp-mediated transport. The intracellular accumulation of rhodamine123 (Rh123) and doxorubicin (DOX) were examined in LLC-PK1\\/MDR1 cells to evaluate P-gp inhibition by RSP and PALI. Both

  16. In vitro activities of novel catecholate siderophores against Plasmodium falciparum.

    PubMed Central

    Pradines, B; Ramiandrasoa, F; Basco, L K; Bricard, L; Kunesch, G; Le Bras, J

    1996-01-01

    The activities of novel iron chelators, alone and in combination with chloroquine, quinine, or artemether, were evaluated in vitro against susceptible and resistant clones of Plasmodium falciparum with a semimicroassay system. N4-nonyl,N1,N8-bis(2,3-dihydroxybenzoyl) spermidine hydrobromide (compound 7) demonstrated the highest level of activity: 170 nM against a chloroquine-susceptible clone and 1 microM against a chloroquine-resistant clone (50% inhibitory concentrations). Compounds 6, 8, and 10 showed antimalarial activity with 50% inhibitory concentrations of about 1 microM. Compound 7 had no effect on the activities of chloroquine, quinine, and artemether against either clone, and compound 8 did not enhance the schizontocidal action of either chloroquine or quinine against the chloroquine-resistant clone. The incubation of compound 7 with FeCI3 suppressed or decreased the in vitro antimalarial activity of compound 7, while no effect was observed with incubation of compound 7 with CuSO4 and ZnSO4. These results suggest that iron deprivation may be the main mechanism of action of compound 7 against the malarial parasites. Chelator compounds 7 and 8 primarily affected trophozoite stages, probably by influencing the activity of ribonucleotide reductase, and thus inhibiting DNA synthesis. PMID:8878587

  17. In vitro activity of the nisin dehydratase NisB

    PubMed Central

    Garg, Neha; Salazar-Ocampo, Luis M. A.; van der Donk, Wilfred A.

    2013-01-01

    The biosynthesis of several classes of ribosomally synthesized and posttranslationally modified peptides involves dehydration of serine and threonine residues. For class I lantibiotics, thiopeptides, and goadsporin, this dehydration is catalyzed by lanthionine biosynthetic enzyme B (LanB) or LanB-like proteins. Although LanB proteins have been studied since 1992, in vitro reconstitution of their dehydration activity has been elusive. We show here the in vitro activity of the dehydratase involved in the biosynthesis of the food preservative nisin (NisB). In vitro, NisB dehydrated its substrate peptide NisA eight times in the presence of glutamate, ATP, Mg2+, and the ribosomal/membrane fraction of bacterial cell extract. Mutation of 23 highly conserved residues of NisB identified a number of amino acids that are essential for dehydration activity. In addition, these mutagenesis studies identified three mutants, R786A, R826A, and H961A, that result in multiple glutamylations of the NisA substrate. Glutamylation was observed during both Escherichia coli coexpression of NisA with these mutants and in vitro assays. Treatment of the glutamylated substrate with WT NisB results in dehydrated NisA, suggesting that the glutamylated peptide is an intermediate in dehydration. Collectively, these studies suggest that dehydration involves glutamylation of the side chains of Ser and Thr followed by elimination. The latter step has precedent in the virginiamycin resistance protein virginiamycin B lyase. These studies will facilitate investigation of other LanB proteins involved in the biosynthesis of lantibiotics, thiopeptides, and goadsporin. PMID:23589847

  18. Synthesis and In Vitro Cytotoxic Activity of Chromenopyridones

    PubMed Central

    Singh, Balwinder; Sharma, Vishal; Singh, Gagandeep; Kumar, Rakesh; Arora, Saroj; Ishar, Mohan Paul Singh

    2013-01-01

    Novel substituted chromenopyridones (3a–j and 6a–d) were synthesized and evaluated in vitro for the cytotoxic activity against various human cancer cell lines such as prostate (PC-3), breast (MCF-7), CNS (IMR-32), cervix (Hela), and liver (Hep-G2). preliminary cytotoxic screening showed that all the compounds possess a good to moderate inhibitory activity against various cancer cell lines. Particularly, compound 6b bearing allyl moiety displayed a significant cytotoxic potential in comparison to standard drugs. PMID:25379292

  19. Hepatoprotective and antihyperliposis activities of in vitro cultured Anoectochilus formosanus.

    PubMed

    Du, Xiao-Ming; Sun, Ning-Yi; Hayashi, Jun; Chen, Yang; Sugiura, Minoru; Shoyama, Yukihiro

    2003-01-01

    The pharmacological effects of an aqueous extract of the whole plants of in vitro cultured Anoectochilus formosanus were investigated experimentally for hepatoprotective and antihyperliposis activities. The extract showed significant antihepatotoxic activity against carbon tetrachloride induced cytotoxicity in primary cultured rat hepatocytes. In an assay for antihyperliposis using aurothioglucose-induced obese mice, the extract suppressed significantly the increase in the weights of body and liver, ameliorated triglyceride levels in the liver and serum, and also significantly reduced the deposition of adipose tissue. PMID:12557243

  20. Carotenoid composition and in vitro pharmacological activity of rose hips.

    PubMed

    Horváth, Györgyi; Molnár, Péter; Radó-Turcsi, Erika; Deli, József; Kawase, Masami; Satoh, Kazue; Tanaka, Toru; Tani, Satoru; Sakagami, Hiroshi; Gyémánt, Nóra; Molnár, József

    2012-01-01

    The aim of the present study was to compare carotenoid extracts of Rose hips (Rosa canina L.) with regard to their phytochemical profiles and their in vitro anti-Helicobacter pylori (H. pylori), cytotoxic, multidrug resistance (MDR) reversal and radical scavenging activity. Carotenoid composition was investigated in the different fractionation of rose hips, using extraction methods. Six main carotenoids - epimers of neochrome, lutein, zeaxanthin, rubixanthin, lycopene, ?,?-carotene - were identified from Rose hips by their chromatographic behavior and UV-visible spectra, which is in accordance with other studies on carotenoids in this plant material. The active principles in the carotenoid extract might differ, depending upon the extraction procedures. PMID:22428123

  1. In vitro antioxidant and antihyperlipidemic activities of Bauhinia variegata Linn

    PubMed Central

    Rajani, G.P.; Ashok, Purnima

    2009-01-01

    Objectives: To evaluate the ethanolic and aqueous extracts of Bauhinia variegata Linn. for in vitro antioxidant and antihyperlipidemic activity. Materials and Methods: Ethanolic and aqueous extracts of the stem bark and root of B. variegata Linn. were prepared and assessed for in vitro antioxidant activity by various methods namely total reducing power, scavenging of various free radicals such as 1,2-diphenyl-2-picrylhydrazyl (DPPH), super oxide, nitric oxide, and hydrogen peroxide. The percentage scavenging of various free radicals were compared with standard antioxidants such as ascorbic acid and butylated hydroxyl anisole (BHA). The extracts were also evaluated for antihyperlipidemic activity in Triton WR-1339 (iso-octyl polyoxyethylene phenol)-induced hyperlipidemic albino rats by estimating serum triglyceride, very low density lipids (VLDL), cholesterol, low-density lipids (LDL), and high-density lipid (HDL) levels. Result: Significant antioxidant activity was observed in all the methods, (P < 0.01) for reducing power and (P < 0.001) for scavenging DPPH, super oxide, nitric oxide, and hydrogen peroxide radicals. The extracts showed significant reduction (P < 0.01) in cholesterol at 6 and 24 h and (P < 0.05) at 48 h. There was significant reduction (P < 0.01) in triglyceride level at 6, 24, and 48 h. The VLDL level was also significantly (P < 0.05) reduced from 24 h and maximum reduction (P < 0.01) was seen at 48 h. There was significant increase (P < 0.01) in HDL at 6, 24, and 48 h. Conclusion: From the results, it is evident that alcoholic and aqueous extracts of B. variegata Linn. can effectively decrease plasma cholesterol, triglyceride, LDL, and VLDL and increase plasma HDL levels. In addition, the alcoholic and aqueous extracts have shown significant antioxidant activity. By the virtue of its antioxidant activity, B. variegata Linn. may show antihyperlipidemic activity. PMID:20177495

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

    PubMed

    Cai, Y; Wang, J; Liang, B

    1999-02-01

    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

  3. In vitro antioxidant activities of Solanum surattense leaf extract

    PubMed Central

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

    2013-01-01

    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

  4. Antioxidant activity of Botryococcus braunii extract elucidated in vitro models.

    PubMed

    Rao, Ambati Ranga; Sarada, Ravi; Baskaran, Vallikannan; Ravishankar, Gokare Aswathanarayana

    2006-06-28

    Botryococcus braunii is a green colonial microalga that is used mainly for the production of hydrocarbons, exopolysaccharides, and carotenoids. In the present study, the antioxidant properties of acetone extracts of B. braunii were evaluated using in vitro model systems such as 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydroxy radical scavenging, and lipid peroxidation in human low-density lipoprotein and rat tissues. Acetone extracts of B. braunii (equivalent to 10 ppm total carotenoid) exhibited 71 and 67% antioxidant activity in DPPH and hydroxyl radical scavenging model systems, respectively. Similarly, the extract also showed 72, 71, and 70% antioxidant activity in the liver, brain, and kidney of rats. Low-density lipoprotein oxidation induced by Cu2+ ions was also protected (22, 38, and 51%) by the algal extract in a dose-dependent manner (4, 6, and 8 ppm levels of total carotenoid). Thiobarbituric acid reactive substances concentration in the blood, liver, and kidney of rats was also significantly decreased in B. braunii treated samples compared with those of control. Carotenoids (violaxanthin, astaxanthin, lutein, zeaxanthin, chlorophylls a and b, and alpha, beta-carotene) identified in the B. braunii acetone extract may be exhibiting antioxidant activity. Among the carotenoids, lutein represents more than 75% of the total carotenoids. B. braunii extract was shown to be effective for protecting biological systems against various oxidative stresses in vitro. This is the first report on the antioxidant properties of B. braunii. PMID:16787003

  5. Geometric complexity is increased in in vitro activated platelets.

    PubMed

    Bianciardi, Giorgio

    2015-06-01

    This article investigates the use of computerized fractal analysis for objective characterization of the complexity of platelets in vitro stimulated by low level thrombin (0.02 U mL(-1) ), collected from healthy individuals and observed by means of transmission electron microscopy. Platelet boundaries were extracted by means of automatically image analysis. Local fractal dimension was evaluated by the box-counting technique (measure of geometric complexity of the platelet outline). The results showed that the platelet boundary is fractal when observed by transmission electron microscopy and that, after an in vitro platelet activation test, the shape of platelets present increased geometric complexity in comparison to the no stimulated platelets (P?activation. The results may play important roles in the evaluation of the platelets status in pathological conditions, like as atherosclerosis and diabetes mellitus, where in in vivo activated platelets have been described. Microsc. Res. Tech. 78:485-488, 2015. © 2015 Wiley Periodicals, Inc. PMID:25808036

  6. Antibacterial activity of cerium colloids against opportunistic microorganisms in vitro.

    PubMed

    Babenko, L P; Zholobak, N M; Shcherbakov, A B; Voychuk, S I; Lazarenko, L M; Spivak, M Ya

    2012-01-01

    The CeO2 sol with the size of nanoparticles 2-4 nm has been synthesized. It has been determined that the synthesized nanocrystalline cerium has antibacterial activity in vitro against different groups of opportunistic microorganisms: clinical strains of Escherichia coli, Staphylococcus aureus and Candida albicans. The rate of viability depression of test-cultures depends on the concentration of cerium dioxide nanoparticles and time of incubation. It is shown that the sol interacts with the bacterial cell surface. It is suggested that the observed differences of antibacterial action of nanocrystalline cerium dioxide can be related to the structural characteristics of the cell surface. PMID:22830198

  7. Anthelmintic activity in vitro and in vivo of Baccharis trimera (Less) DC against immature and adult worms of Schistosoma mansoni.

    PubMed

    de Oliveira, Rosimeire Nunes; Rehder, Vera Lúcia Garcia; Oliveira, Adriana Silva Santos; Jeraldo, Veronica de Lourdes Sierpe; Linhares, Arício Xavier; Allegretti, Silmara Marques

    2014-04-01

    Although its efficiency against all Schistosoma species, praziquantel (PZQ) shows low efficacy against schistosomula and juvenile stages. The potential for development of resistance to PZQ has justified the search for new alternative chemotherapies. In this scenario, studies to new formulations, more comprehensive and without adverse effects, are being conducted. One viable and promising treatment is the study of medicinal plants as a new approach to the experimental treatment for Schistosomiasis. Amongst all the variety of the medicinal species studied, we can highlight Baccharis trimera (Less) DC, known as "Carqueja-amarga". This paper not only describes the effect of crude dichloromethane extract (DE) and aqueous fraction (AF) obtained from B. trimera, in vitro but also is the first one that investigates the in vivo efficacy of B. trimera against schistosomula, juvenile and adult worms of Schistosoma mansoni BH strain. In the experiment, mice were treated with DE, AF and PZQ (40 and 200mg/kg) over the period of larval development (3 and 30 post-infection; pi), and adult worms (60days post-infection; pi). The in vitro results show that the DE and AF effects are dose-dependents, being the 130?g/mL the most effective one in a shorter period of incubation. The exposure of the in vitro samples over adult parasites were able to inhibit 100% of the oviposition in females. Likewise caused the mortality of the parasites with morphological alterations on the tegument, on the suckers, oral and acetabulum, in both males and females after 6-72h of exposure. Additionally, the in vivo treatments against juvenile and adult infection were more effective compared to the control group untreated. Administrations of AF and DE in day 30pi (juvenile worms) show female worm total burden reductions of 75% and 68% respectively. At the same period of infection reductions of respectively 98% and 97% egg/g in the faeces were seen. In relation to the different egg developmental stages (oogram), the results showed significant reductions, due to the reduction in the number of worms, especially the females. In conclusion, B. trimera exhibits major schistosomicidal effects in vivo against immature and adult worms of S. mansoni, opening up perspectives for future researches on substance or compound isolation and the elucidation of its mechanisms of action. PMID:24602876

  8. In vitro activities of sparfloxacin, tosufloxacin, ciprofloxacin, and fleroxacin.

    PubMed Central

    Barry, A L; Fuchs, P C

    1991-01-01

    The in vitro activity of sparfloxacin was compared with those of tosufloxacin, ciprofloxacin, and fleroxacin against 730 bacterial isolates representing 49 different species. Sparfloxacin and ciprofloxacin had similar spectra of activity, but sparfloxacin was less active against Pseudomonas aeruginosa and more active against many gram-positive cocci and anaerobic bacteria. Tosufloxacin MICs were generally 8- to 16-fold lower than those for sparfloxacin or ciprofloxacin. All four fluoroquinolones were active against nalidixic acid-susceptible strains of the family Enterobacteriaceae (MIC for 90% of the isolates [MIC90], less than or equal to 0.25 micrograms/ml) but nalidixic acid-resistant strains were less susceptible (MIC90, greater than or equal to 4.0 micrograms/ml). Against Pseudomonas aeruginosa isolates, MIC90s were 1.0 micrograms/ml for tosufloxacin, 2.0 micrograms/ml for ciprofloxacin, and 4.0 micrograms/ml for sparfloxacin. Against Enterococcus faecalis, sparfloxacin and ciprofloxacin MIC90s were 1.0 and 2.0 micrograms/ml, respectively. MIC90s for ciprofloxacin-susceptible Staphylococcus aureus were 0.016 micrograms/ml for tosufloxacin, 0.06 micrograms/ml for sparfloxacin, and 0.5 micrograms/ml for both ciprofloxacin and fleroxacin. With four species of gram-negative bacilli, mutants resistant to two to four times the sparfloxacin MIC occurred spontaneously at frequencies of 10(-7) to 10(-9): single-step high-level resistance was not observed. In vitro-selected sparfloxacin-resistant mutants displayed cross-resistance to other quinolones, as did clinical isolates of ciprofloxacin-resistant S. aureus. Tosufloxacin MICs with broth microdilution methods were four- to eightfold greater than those obtained with agar dilution methods. The two procedures gave comparable results when sparfloxacin or ciprofloxacin was being tested. PMID:1906696

  9. Strongyloides ratti: In Vitro and In Vivo Activity of Tribendimidine

    PubMed Central

    Keiser, Jennifer; Thiemann, Kai; Endriss, Yvette; Utzinger, Jürg

    2008-01-01

    Background Strongyloidiasis is a truly neglected tropical disease, but its public health significance is far from being negligible. At present, only a few drugs are available for the treatment and control of strongyloidiasis. Methodology/Principal Findings We investigated the activity of tribendimidine against third-stage larvae (L3) of Strongyloides ratti in vitro and against juvenile and adult stages of the parasite in vivo. S. ratti larvae incubated in PBS buffer containing 10–100 µg/ml tribendimidine died within 24 hours. A single 50 mg/kg oral dose of tribendimidine administered to rats infected with 1-day-old S. ratti showed no effect. The same dose administered to rats harboring a 2-day-old infection showed a moderate reduction of the intestinal parasite load. Three days post-exposure a significant reduction of the immature worm burden was found. Administration of tribendimidine at doses of 50 mg/kg and above to rats harboring mature S. ratti resulted in a complete elimination of the larval and adult worm burden. For comparison, we also administered ivermectin at a single 0.5 mg/kg oral dose to rats infected with adult S. ratti and found a 90% reduction of larvae and a 100% reduction of adult worms. Conclusion/Significance Tribendimidine exhibits activity against S. ratti in vitro and in vivo. The effect of tribendimidine in humans infected with S. stercoralis should be assessed. PMID:18235851

  10. The in vitro estrogenic activities of triclosan and triclocarban.

    PubMed

    Huang, Hongyu; Du, Guizhen; Zhang, Wei; Hu, Jialei; Wu, Di; Song, Ling; Xia, Yankai; Wang, Xinru

    2014-09-01

    Triclosan (TCS) and triclocarban (TCC), as broad spectrum antibacterial agents, are distributed widely in the environment and humans. Most studies have focused on their distribution and biodegradation, but the endocrine-disrupting effects of these chemicals, especially their estrogenic effects, are still unclear. In the present study, we investigated the estrogenic effects of TCS and TCC using a series of in vitro assays, including the ER reporter gene assay in the CV-1 cells, E-screen assay and evaluation of estrogen-responsive genes in the MCF-7 cells. The tested concentrations of TCS and TCC were both from 1?×?10(-9) to 1?×?10(-6) ?M. Results showed that TCS and TCC exerted estrogenic activities by inducing luciferase activities in an ER reporter gene assay, promoting the proliferation of the MCF-7 cells, up-regulating the expression of pS2 and down-regulating ER? expression at both the mRNA and protein levels in the MCF-7 cells. We further found that TCS and TCC could alter the expression of multiple microRNAs (mir-22, mir-206 and mir-193b) in the MCF-7 cells, which would help understand the mechanisms of their estrogenic effects on regulating the expression of ER?. In brief, our results demonstrated the potential estrogenic effects and profiled in vitro data for further risk assessment of TCS and TCC. PMID:24740835

  11. Activity-dependent plasticity of mouse hippocampal assemblies in vitro

    PubMed Central

    Keller, Martin K.; Draguhn, Andreas; Both, Martin; Reichinnek, Susanne

    2015-01-01

    Memory formation is associated with the generation of transiently stable neuronal assemblies. In hippocampal networks, such groups of functionally coupled neurons express highly ordered spatiotemporal activity patterns which are coordinated by local network oscillations. One of these patterns, sharp wave-ripple complexes (SPW-R), repetitively activates previously established groups of memory-encoding neurons, thereby supporting memory consolidation. This function implies that repetition of specific SPW-R induces plastic changes which render the underlying neuronal assemblies more stable. We modeled this repetitive activation in an in vitro model of SPW-R in mouse hippocampal slices. Weak electrical stimulation upstream of the CA3-CA1 networks reliably induced SPW-R of stereotypic waveform, thus representing re-activation of similar neuronal activity patterns. Frequent repetition of these patterns (100 times) reduced the variance of both, evoked and spontaneous SPW-R waveforms, indicating stabilization of pre-existing assemblies. These effects were most pronounced in the CA1 subfield and depended on the timing of stimulation relative to spontaneous SPW-R. Additionally, plasticity of SPW-R was blocked by application of a NMDA receptor antagonist, suggesting a role for associative synaptic plasticity in this process. Thus, repetitive activation of specific patterns of SPW-R causes stabilization of memory-related networks. PMID:26041998

  12. In vitro Antioxidant Activities of Trianthema portulacastrum L. Hydrolysates

    PubMed Central

    Yaqoob, Sadaf; Sultana, Bushra; Mushtaq, Muhammad

    2014-01-01

    Hydrolysates of Trianthema portulacastrum in acidified methanol were evaluated for their total phenolic (TP) constituents and respective antioxidant activities using in vitro assays (i.e., 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, percent inhibition of linoleic acid peroxidation, and ferric reducing power). The observed results indicate that root, shoot, and leaf fractions of T. portulacastrum contain 50.75~98.09 mg gallic acid equivalents/g dry weight of TP. In addition, these fractions have substantial reducing potentials (0.10~0.59), abilities to inhibit peroxidation (43.26~89.98%), and DPPH radical scavenging capabilities (6.98~311.61 ?g/mL IC50). The experimental data not only reveal T. portulacastrum as potential source of valuable antioxidants, but also indicate that acidified methanol may be an ideal choice for the enhanced recovery of phenolic compounds with retained biological potential for the food and pharmaceutical industry. PMID:24772406

  13. In vitro antioxidant activity of Rubus ellipticus fruits.

    PubMed

    Sharma, Uma Shankar; Kumar, Arun

    2011-01-01

    Various studies have been done to identify antioxidants from plant sources and efforts have been taken to incorporate it in conventional therapy. In our present study, petroleum ether, ethanolic, and aqueous extracts of Rubus ellipticus fruits have been evaluated for in vitro antioxidant activity using DPPH radical scavenging and reducing power assay. BHA was used as a standard antioxidant for DPPH radical scavenging activity. The reducing power assay of extracts was carried out with ascorbic acid as a standard reducing agent. All the analysis was made with the use of UV-Visible spectrophotometer. The results of the both assay showed that all the extracts of R. ellipticus fruits possess significant free radical scavenging and reducing power properties at concentration-dependent manner. Hence, it can be concluded that the R. ellipticus fruits could be pharmaceutically exploited for antioxidant properties. PMID:22171292

  14. In vitro antioxidant activity of Rubus ellipticus fruits

    PubMed Central

    Sharma, Uma Shankar; Kumar, Arun

    2011-01-01

    Various studies have been done to identify antioxidants from plant sources and efforts have been taken to incorporate it in conventional therapy. In our present study, petroleum ether, ethanolic, and aqueous extracts of Rubus ellipticus fruits have been evaluated for in vitro antioxidant activity using DPPH radical scavenging and reducing power assay. BHA was used as a standard antioxidant for DPPH radical scavenging activity. The reducing power assay of extracts was carried out with ascorbic acid as a standard reducing agent. All the analysis was made with the use of UV-Visible spectrophotometer. The results of the both assay showed that all the extracts of R. ellipticus fruits possess significant free radical scavenging and reducing power properties at concentration-dependent manner. Hence, it can be concluded that the R. ellipticus fruits could be pharmaceutically exploited for antioxidant properties. PMID:22171292

  15. Comparative in-vitro activity of tigemonam, a new monobactam.

    PubMed

    Rylander, M; Gezelius, L; Norrby, S R

    1988-09-01

    The in-vitro activity against Gram-negative aerobic bacterial pathogens of a new oral monobactam, tigemonam, was compared with those of amoxycillin/clavulanic acid, aztreonam, cefaclor, ceftazidime, cefuroxime, ciprofloxacin, co-trimoxazole and gentamicin, by an agar-dilution method. Tigemonam inhibited 90% of strains tested of Escherichia coli, Klebsiella spp., Proteus spp., Salmonella spp., Haemophilus influenzae and Branhamella catarrhalis at concentrations of 0.25 mg/l or below. The MIC90 for Enterobacter spp. was 16 mg/l and for Citrobacter 4 mg/l. Pseudomonas aeruginosa was resistant to tigemonam but susceptible to aztreonam. In comparison with the other oral antibiotics tested, tigemonam was generally more active. Tigemonam showed minimal inoculum dependence, between 10(2) and 10(6) cfu per spot. It is concluded that tigemonam is a candidate for clinical trials in patients with infections caused by Gram-negative aerobes other than pseudomonas and acinetobacter. PMID:3182428

  16. In Vitro Anti-rotaviral Activity of Achillea kellalensis

    PubMed Central

    Taherkhani, Reza; Farshadpour, Fatemeh; Makvandi, Manoochehr

    2013-01-01

    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

  17. In Vitro Antileukemic Activity of Xanthosoma sagittifolium (Taioba) Leaf Extract

    PubMed Central

    Caxito, Marina L. C.; Correia, Rachell R.; Gomes, Anne Caroline C.; Justo, Graça; Coelho, Marsen G. P.; Sakuragui, Cássia M.; Kuster, Ricardo M.; Sabino, Katia C. C.

    2015-01-01

    Xanthosoma sagittifolium Schott is a herb of the Araceae family, popularly known as taioba, which is consumed as food in some regions of Brazil, Africa, and Asia. This species has already been evaluated for the antifungal activities. However, based on its potential antitumor activity, the present study further aimed to examine the antitumor, as well as chelation, activity of X. sagittifolium leaf extract. Results showed that hydroethanolic extract of X. sagittifolium leaves (HEXs-L) exhibits cytotoxic effects against the immortalized line of human T-lymphocytic (Jurkat) and myelogenous (K562) leukemia cells, but not nontumor RAW 264.7 macrophages or NIH/3T3 fibroblasts. HEXs-L inhibited 50.3% of Jurkat cell proliferation, reducing by 20% cells in G2/M phase, but increasing cells in sub-G1 phase, thereby inducing apoptosis by 54%. In addition, HEXs-L inhibited NO production by 59%, as determined by Griess reaction, and chelated 93.8% of free Fe(II), as demonstrated by ferrozine assay. Phytochemical studies were carried out by ESI-MS, identifying apigenin di-C-glycosides as major compounds. Overall, this work revealed that leaf extract of Xanthosoma sagittifolium presented chelating activity and in vitro antitumor activity, arresting cell cycle and inducing apoptosis of leukemia cells, thus providing evidence that taioba leaves may have practical application in cancer therapy. PMID:26180533

  18. In vitro antioxidant activities of antioxidant-enriched toothpastes.

    PubMed

    Battino, M; Ferreiro, M S; Armeni, T; Politi, A; Bompadre, S; Massoli, A; Bullon, P

    2005-03-01

    Several forms of periodontal diseases (PD) are often associated with modified phagocytosing leukocytes and contemporary free radical production. Host antioxidant defenses could benefit from toothpastes used as adjuncts to counteract plaque-associated bacteria. The aim of the present study was to determine possible antioxidant activity (AA) of 12 differently antioxidant-enriched toothpastes, regardless of their efficacy as antimicrobial agents. Toothpastes were enriched alternatively with sodium ascorbyl phosphate, alpha-tocopherol acetate, pycnogenol, allantoin and methyl salycilate or a mixture of these. AA was tested in a cell-free system with a ABTS-decolorization assay improved by means of a flow injection analysis device. Comet assay, using NCTC 2544 keratinocytes, was performed to test if it was possible to identify any protection against in vitro DNA fragmentation provoked by a challenge with H(2)O(2) in cultures pre-incubated with toothpaste extracts. Only toothpastes containing sodium ascorbyl phosphate displayed clear AA with I(50) values ranging between 50 and 80 mg of toothpaste/ml water. COMET analysis of cells challenged with H(2)O(2) in presence of toothpaste extracts revealed a limited protection exerted by sodium ascorbyl phosphate. The results described herein indicate that toothpastes containing sodium ascorbyl phosphate possess AA. All the data were obtained in systems in vitro and the demonstration of in vivo AA is desirable. These findings could be useful in the treatment and maintenance of some forms of PD and should be considered when arranging new toothpaste formulations. PMID:15788239

  19. Screening of compounds for antimicrosporidial activity in vitro.

    PubMed

    Didier, E S; Maddry, J A; Kwong, C D; Green, L C; Snowden, K F; Shadduck, J A

    1998-01-01

    Relatively few effective compounds are available for treating microsporidiosis in humans. In this study, several compounds were assayed for activity against Encephalitozoon intestinalis (Cali, Kotler et Orenstein, 1993) and Vittaforma corneae Shadduck, Meccoli, Davis et Font, 1990 in vitro. Of the benzimidazoles tested, albendazole was most effective and the MIC50 values were 8.0 ng/ml and 55.0 ng/ml for E. intestinalis and V. corneae, respectively. Fumagillin and its analogue, TNP-470 were nearly equally effective against both E. intestinalis and V. corneae. The MIC50 values of fumagillin were 0.52 ng/ml and 0.81 ng/ml, and the MIC50 values of TNP-470 were 0.35 ng/ml and 0.38 ng/ml for E. intestinalis and V. corneae, respectively. In addition, 12 of 44 purines and pteridines with putative tubulin binding activity that were synthesized at Southern Research Institute (SRI), inhibited microsporidial replication by more than 50% at concentrations that were not toxic to the host cells. Several chitin synthesis/assembly inhibitors inhibited growth of the microsporidia in vitro but were toxic for the host cells making it difficult to interpret the results. One exception was lufenuron, which caused no significant toxicity to the host cells and expressed approximate MIC50 values of 2.95 micrograms/ml and 6.3 micrograms/ml against E. intestinalis and V. corneae, respectively. These results warrant further studies on albendazole, fumagillin, TNP-470, lufenuron, and the selected SRI purines and pteridines for developing therapeutic strategies for microsporidiosis. PMID:9684323

  20. Substrate elasticity affects bovine satellite cell activation kinetics in vitro.

    PubMed

    Lapin, M R; Gonzalez, J M; Johnson, S E

    2013-05-01

    Satellite cells support efficient postnatal skeletal muscle hypertrophy through fusion into the adjacent muscle fiber. Nuclear contribution allows for maintenance of the fiber myonuclear domain and proficient transcription of myogenic genes. Niche growth factors affect satellite cell biology; however, the interplay between fiber elasticity and microenvironment proteins remains largely unknown. The objective of the experiment was to examine the effects of hepatocyte growth factor (HGF) and surface elasticity on bovine satellite cell (BSC) activation kinetics in vitro. Young's elastic modulus was calculated for the semimembranosus (SM) and LM muscles of young bulls (5 d; n = 8) and adult cows (27 mo; n = 4) cattle. Results indicate that LM elasticity decreased (P < 0.05) with age; no difference in Young's modulus for the SM was noted. Bovine satellite cells were seeded atop polyacrylamide bioscaffolds with surface elasticities that mimic young bull and adult cow LM or traditional cultureware. Cells were maintained in low-serum media supplemented with 5 ng/mL HGF or vehicle only for 24 or 48 h. Activation was evaluated by proliferating cell nuclear antigen (PCNA) immunocytochemistry. Results indicate that BSC maintained on rigid surfaces were activated at 24 h and refractive to HGF supplementation. By contrast, fewer (P < 0.05) BSC had exited quiescence after 24 h of culture on surfaces reflective of either young bull (8.1 ± 1.7 kPa) or adult cow (14.6 ± 1.6 kPa) LM. Supplementation with HGF promoted activation of BSC cultured on bioscaffolds as measured by an increase (P < 0.05) in PCNA immunopositive cells. Culture on pliant surfaces affected neither activation kinetics nor numbers of Paired box 7 (Pax7) immunopositive muscle stem cells (P > 0.05). However, with increasing surface elasticity, an increase (P < 0.05) in the numbers of muscle progenitors was observed. These results confirm that biophysical and biochemical signals regulate BSC activation. PMID:23463548

  1. In Vitro Antimalarial Activity and Drug Interactions of Fenofibric Acid

    PubMed Central

    Wong, Rina P. M.

    2012-01-01

    Plasmodium falciparum has developed resistance to most available treatments, underscoring the need for novel antimalarial drugs. Fibrates are lipid-modifying agents used to reduce morbidity and mortality associated with cardiovascular disease. They may have antimalarial activity through modulation of P-glycoprotein and ATP-binding cassette subfamily A member (ABC-1)-mediated nutrient transport and/or via a putative peroxisome proliferator-activated receptor alpha-like protein. We therefore examined in vitro antimalarial activities of fibrates and their interactions with chloroquine and dihydroartemisinin in chloroquine-sensitive (3D7) and chloroquine-resistant (W2mef) strains of P. falciparum using the conventional isotopic assay microtechnique. A bioassay was used to assess inhibition activities of human plasma after therapeutic fenofibrate doses. Fenofibric acid, the main metabolite of fenofibrate, was the most potent of the fibrates tested, with mean 50% inhibitory concentrations of 152 nM and 1,120 nM for chloroquine-sensitive and -resistant strains, respectively. No synergistic interaction between fibrates and chloroquine or dihydroartemisinin was observed. Plasma fenofibric acid concentrations, quantified by high-performance liquid chromatography in seven healthy volunteers after treatment (mean, 15.3 mg/liter, or 48 ?M), inhibited P. falciparum. BLAST analysis revealed the likely presence of an ABC-1 transporter homolog in P. falciparum. Our findings demonstrate that fenofibric acid has activity similar to the activities of conventional antimalarial drugs at concentrations well below those achieved after therapeutic doses. It may inhibit P. falciparum growth by inhibiting intracellular lipid transport. PMID:22430967

  2. In vitro antioxidant activity of liquor from fermented shrimp biowaste.

    PubMed

    Sachindra, Nakkarike M; Bhaskar, Narayan

    2008-12-01

    Shrimp waste was fermented using lactic culture and the separated fermented liquor was lyophilized. In vitro antioxidant activities of the lyophilized powder were evaluated with respect scavenging of different radicals and quenching of generated singlet oxygen. The sample showed strong radical scavenging and singlet oxygen quenching in a dose dependent manner (p<0.001). The sample exhibited 40% scavenging of DPPH radical at 1.0mg/ml concentration while the ABTS radical scavenging was 95% even at 0.5mg/ml concentrations. Hydroxyl radical scavenging activity as measured by chemiluminescence technique showed 80% scavenging and peroxyl radical scavenging was 65% at 1.0mg/ml concentration. The singlet oxygen quenching ability of the powder was 68.3% at 1.0mg/ml concentration. The sample was found to contain low molecular weight proteins. The formation of peptides and amino acids during hydrolysis of shrimp waste protein during fermentation is expected to be responsible for the antioxidant activity. In addition as the product also contains carotenoids, it can be used as an ingredient in aquaculture feed formulations for beneficial effects. PMID:18513957

  3. Amino ozonides exhibit in vitro activity against Echinococcus multilocularis metacestodes.

    PubMed

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

    2014-01-01

    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

  4. In Vitro Activities of Iodonium Salts against Oral and Dental Anaerobes

    Microsoft Academic Search

    Ellie J. C. Goldstein; Diane M Citron; Yumi Warren; C. Vreni Merriam; Kerin Tyrrell; Helen Fernandez; Ukkiramapandian Radhakrishnan; Peter J. Stang; Georg Conrads

    2004-01-01

    The comparative in vitro activities of 11 iodonium salt compounds, 0.12% chlorhexidine, and four antimi- crobial agents against 322 anaerobic and fastidious potential dental and periodontal bacterial pathogens were studied. Iodonium salts 3, 4, 5, 9, and 10 had in vitro activities comparable to that of chlorhexidine against most isolates. These compounds may be suitable for incorporation into an oral

  5. In vitro activity and susceptibility to hydrolysis of S-1006.

    PubMed Central

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

    1992-01-01

    The in vitro activity of S-1006, the active component of a new orally absorbed cephalosporin, S-1108, inhibited 90% of Staphylococcus aureus isolates at less than or equal to 2 micrograms/ml, 90% of group A, B, C, F, and G streptococci and Streptococcus pneumoniae isolates at less than or equal to 0.12 microgram/ml, and all Haemophilus influenzae isolates at less than or equal to 0.06 microgram/ml. Although 50% of the members of the family Enterobacteriaceae were inhibited by less than or equal to 2 micrograms of S-1006 per ml, Enterobacter spp. and Citrobacter freundii resistant to ceftriaxone were resistant to S-1006. The MICs of S-1006 for approximately 20% of Providencia, Proteus vulgaris, and Serratia isolates were 4 micrograms/ml. S-1006 was hydrolyzed by the plasmid TEM-3, TEM-5, PSE-1, and PSE-4 beta-lactamases and by the chromosomal beta-lactamase of Enterobacter and Morganella spp. and P. vulgaris. PMID:1416835

  6. In vivo and in vitro antimalarial activity of bergenin

    PubMed Central

    LIANG, JIAO; LI, YINGHUI; LIU, XUEWU; HUANG, YUXIAO; SHEN, YAN; WANG, JUN; LIU, ZHONGXIANG; ZHAO, YA

    2014-01-01

    Malaria is a potentially life-threatening protozoal parasitic disease transmitted by female Anopheles mosquitoes. Drug therapy is currently the most widely used method for the control and treatment of this disease. Several plants were found to contain substances possessing antimalarial properties. In this study, we investigated the antimalarial activity of bergenin, a sesquiterpene lactone compound derived from Rodgersia aesculifolia Batal. The results indicated that bergenin effectively inhibited Plasmodium falciparum growth in vitro (IC50, 14.1 ?g/ml, with ~100% inhibition at 50 ?g/ml), without apparent cytotoxicity to erythrocytes or to mammalian HeLa and HepG2 cells. Bergenin exhibited less cytotoxic activity and the selectivity index (SI) was 887 and 1,355 for HeLa and HepG2 cells, respectively. The administration of bergenin to Plasmodium berghei-infected mice for 6 days significantly inhibited the growth of the parasites. Taken together, these findings provide evidence that bergenin may be a promising novel drug for antimalarial treatment. PMID:24649107

  7. Amphipathic DNA Polymers Exhibit Antiherpetic Activity In Vitro and In Vivo

    Microsoft Academic Search

    David I. Bernstein; Nathalie Goyette; Rhonda Cardin; Earl R. Kern; Guy Boivin; James Ireland; Jean-Marc Juteau; Andrew Vaillant

    2008-01-01

    Phosphorothioated oligonucleotides have a sequence-independent antiviral activity as amphipathic polymers (APs). The activity of these agents against herpesvirus infections in vitro and in vivo was investigated. The previously established sequence-independent, phosphorothioation-dependent antiviral activity of APs was confirmed in vitro by showing that a variety of equivalently sized homo- and heteropolymeric AP sequences were similarly active against herpes simplex virus type

  8. Assessment of antioxidant activity by using different in vitro methods.

    PubMed

    Schlesier, K; Harwat, M; Böhm, V; Bitsch, R

    2002-02-01

    In this study, six common tests for measuring antioxidant activity were evaluated by comparing four antioxidants and applying them to beverages (tea and juices): Trolox equivalent antioxidant capacity assay (TEAC I-III assay), Total radical-trapping antioxidant parameter assay (TRAP assay), 2,2-diphenyl-l-picrylhydrazyl assay (DPPH assay), N,N-dimethyl-p-phenylendiamine assay (DMPD assay), Photochemiluminescence assay (PCL assay) and Ferric reducing ability of plasma assay (FRAP assay). The antioxidants included gallic acid representing the group of polyphenols, uric acid as the main antioxidant in human plasma, ascorbic acid as a vitamin widely spread in fruits and Trolox as water soluble vitamin E analogue. The six methods presented can be divided into two groups depending on the oxidising reagent. Five methods use organic radical producers (TEAC I-III, TRAP, DPPH, DMPD, PCL) and one method works with metal ions for oxidation (FRAP). Another difference between these tests is the reaction procedure. Three assays use the delay in oxidation and determine the lag phase as parameter for the antioxidant activity (TEAC I, TRAP, PCL). They determine the delay of radical generation as well as the ability to scavenge the radical. In contrast, the assays TEAC II and III, DPPH, DMPD and FRAP analyse the ability to reduce the radical cation (TEAC II and III, DPPH, DMPD) or the ferric ion (FRAP). The three tests acting by radical reduction use preformed radicals and determine the decrease in absorbance while the FRAP assay measures the formed ferrous ions by increased absorbance. Gallic acid was the strongest antioxidant in all tests with exception of the DMPD assay. In contrast, uric acid and ascorbic acid showed low activity in some assays. Most of the assays determine the antioxidant activity in the micromolar range needing minutes to hours. Only one assay (PCL) is able to analyse the antioxidant activity in the nanomolar range. Black currant juice showed highest antioxidant activity in all tests compared to tea, apple juice and tomato juice. Despite these differences, results of these in vitro assays give an idea of the protective efficacy of secondary plant products. It is strongly recommended to use at least two methods due to the differences between the test systems investigated. PMID:11999386

  9. In vitro antimicrobial activity of Medilox® super-oxidized water

    PubMed Central

    2014-01-01

    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

  10. In vitro activity of olive oil polyphenols against Helicobacter pylori.

    PubMed

    Romero, Concepción; Medina, Eduardo; Vargas, Julio; Brenes, Manuel; De Castro, Antonio

    2007-02-01

    Helicobacter pylori is linked to a majority of peptic ulcers and to some types of gastric cancer, and resistance of the microorganism to antibiotic treatment is now found worldwide. Virgin olive oil is an unrefined vegetable oil that contains a significant amount of phenolic compounds. Under simulated conditions, we have demonstrated that these substances can diffuse from the oil into the gastric juice and be stable for hours in this acidic environment. In vitro, they exerted a strong bactericidal activity against eight strains of H. pylori, three of them resistant to some antibiotics. Among the phenolic compounds, the dialdehydic form of decarboxymethyl ligstroside aglycon showed the strongest bactericidal effect at a concentration as low as 1.3 microg/mL. Although the experimental conditions are different from other reported works, this bactericidal concentration is much lower than those found for phenolic compounds from tea, wine, and plant extracts. These results open the possibility of considering virgin olive oil a chemopreventive agent for peptic ulcer or gastric cancer, but this bioactivity should be confirmed in vivo in the future. PMID:17263460

  11. In Vitro Antimicrobial Activities of Bakuchiol against Oral Microorganisms

    PubMed Central

    Katsura, Harumi; Tsukiyama, Ryo-Ichi; Suzuki, Akiko; Kobayashi, Makio

    2001-01-01

    Bakuchiol was isolated from the seeds of Psoralea corylifolia, a tree native to China with various uses in traditional medicine, followed by extraction with ether and column chromatography combined with silica gel and octyldecyl silane. In this study, the antimicrobial activities of bakuchiol against some oral microorganisms were evaluated in vitro. The cell growth of Streptococcus mutans was inhibited in a bakuchiol concentration-dependent manner, and growth of S. mutans was completely prevented by 20 ?g of bakuchiol per ml. The bactericidal effect of bakuchiol on S. mutans was dependent on temperature and stable under the following conditions: sucrose, 0 to 10% (wt/vol); pH, 3.0 to 7.0; organic acids (3% [wt/vol] citric and malic acids). Bakuchiol showed bactericidal effects against all bacteria tested, including S. mutans, Streptococcus sanguis, Streptococcus salivarius, Streptococcus sobrinus, Enterococcus faecalis, Enterococcus faecium, Lactobacillus acidophilus, Lactobacillus casei, Lactobacillus plantarum, Actinomyces viscosus, and Porphyromonas gingivalis, with MICs ranging from 1 to 4 ?g/ml and the sterilizing concentration for 15 min ranging from 5 to 20 ?g/ml. Furthermore, bakuchiol was also effective against adherent cells of S. mutans in water-insoluble glucan in the presence of sucrose and inhibited the reduction of pH in the broth. Thus, bakuchiol would be a useful compound for development of antibacterial agents against oral pathogens and has great potential for use in food additives and mouthwash for preventing and treating dental caries. PMID:11600349

  12. In vitro activity of dietary flavonol congeners against human cancer cell lines

    Microsoft Academic Search

    Chrisiida Tsimplouli; Costas Demetzos; Margarita Hadzopoulou-Cladaras; Panayotis Pantazis; Konstantinos Dimas

    Background  Flavonoids have physiological activity and a variety of pharmacological properties, including anticancer activity in vitro, but structure–anticancer activity relationships are unclear.\\u000a \\u000a \\u000a \\u000a \\u000a Aim  The objectives of this work were to investigate the activity of dietary flavonol congeners against cell lines derived from\\u000a human solid tumours and to examine whether the in vitro activity was associated with specific structural feature(s) of the\\u000a molecules.

  13. Spontaneous activity of rat pretectal nuclear complex neurons in vitro

    Microsoft Academic Search

    Nora Prochnow; Matthias Schmidt

    2004-01-01

    BACKGROUND: Neurons in the mammalian pretectum are involved in the control of various visual and oculomotor tasks. Because functionally independent pretectal cell populations show a wide variation of response types to visual stimulation in vivo, they may also differ in their intrinsic properties when recorded in vitro. We therefore performed whole-cell patch clamp recordings from neurons in the caudal third

  14. In vitro antioxidant activity of polysaccharide from Gardenia jasminoides ellis

    USGS Publications Warehouse

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

    2011-01-01

    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.

  15. In vitro Activity of Sparfloxacin Compared with Ciprofloxacin and Ofloxacin against Respiratory Tract Pathogens

    Microsoft Academic Search

    A.-S. Malmborg; S. Ahlén

    1993-01-01

    The in vitro activity of sparfloxacin, a new fluoroquinolone, was compared with ciprofloxacin and ofloxacin against 166 consecutive isolates from the upper respiratory tract of outpatients. The strains were fully susceptible to three quinolones. The antibacterial activity of sparfloxacin was comparable or better than that of ofloxacin and ciprofloxacin against all strains. Sparfloxacin was fourfold more active against Staphylococcus aureus

  16. Tracking transmitter-gated P2X cation channel activation in vitro and in vivo

    E-print Network

    Newman, Eric A.

    Tracking transmitter-gated P2X cation channel activation in vitro and in vivo Esther Richler1 approach to track activation of ATP-gated P2X receptors and potentially other transmitter-gated cation, regional expression variation, mobility and activation of transmitter-gated P2X channels in living neurons

  17. Comparative In Vitro Activities of Gemifloxacin, Other Quinolones, and Nonquinolone Antimicrobials against Obligately Anaerobic Bacteria

    PubMed Central

    Kleinkauf, Niels; Ackermann, Grit; Schaumann, Reiner; Rodloff, Arne C.

    2001-01-01

    The in vitro activity of gemifloxacin was compared to that of other quinolone and nonquinolone antimicrobials against 204 anaerobes by the agar dilution technique. The data indicate that gemifloxacin has a rather selective anaerobic activity. Most Peptostreptococcus, Porphyromonas, and Fusobacterium species are susceptible, while gemifloxacin's activity against other gram-negative anaerobes appears to be variable. PMID:11353648

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

    Microsoft Academic Search

    ANA ESPINEL-INGROFF

    2001-01-01

    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

  19. Phagocytic activity of Limulus polyphemus amebocytes in vitro.

    PubMed

    Coates, Christopher J; Whalley, Tim; Nairn, Jacqueline

    2012-11-01

    Phagocytosis of invading microorganisms is a fundamental component of innate immunity. The Atlantic horseshoe crab, Limulus polyphemus, possesses a single immune cell type, the granular amebocyte. Amebocytes release a repertoire of potent immune effectors in the presence of pathogens, and function in hemostasis. In contrast to other arthropod immunocytes, the properties of amebocyte phagocytosis remain poorly characterised, restricted by the technical challenges associated with handling these labile cells. We have addressed these challenges and observed the internalisation of microbial and synthetic targets by amebocytes in vitro. Confirmation of target internalisation was achieved using a combination of fluorescent quenching and lipophilic membrane probes: R18 and FM 1-43. Viability, morphological integrity and functionality of extracted amebocytes appeared to be retained in vitro. The phagocytic properties of L. polyphemus amebocytes described here, in the absence of endotoxin, are similar to those observed for arthropod immunocytes and mammalian neutrophils. PMID:22910042

  20. In vitro antiviral activity of lactoferrin and ribavirin upon hantavirus

    Microsoft Academic Search

    M. E. Murphy; H. Kariwa; T. Mizutani; K. Yoshimatsu; J. Arikawa; I. Takashima

    2000-01-01

    Summary.  ?Bovine lactoferrin (LF) and ribavirin (Rbv) were tested as antiviral agents against Seoul type hantavirus (SR-11 strain)\\u000a in vitro. Hantaviral foci number in Vero E6 cells infected with SR-11 was reduced with LF treatment by 5 days post infection\\u000a to obtain a 50% effective dose (ED50) of 2500??g\\/ml, while pretreatment with LF was highly efficacious having an ED50 of 39??g\\/ml.

  1. Studies on the activities of rumen microorganisms in vitro 

    E-print Network

    Johnson, Carl Edward

    1957-01-01

    EXTRACTS AND SUCROSE SOLUTIONS TO INHIBIT CELLULOSE DIGESTION BI RUMEN MICROORGANISMS IN VITRO PART III l. SLVFRAL TYPES OF FISTULA PLUGS USED fN RUMEN STUDIES . ~ ~ 47 2. A NEW TYPE OF BJEUFATIC FISTULA PLUG 49 DETAILS OF CONSTRUCTION OF THE PNEUMATIC... FISTULA PLUG . . 50 PART I EFFECTS OF MESQUITE BEAN EXTRACTS ON THE DIGESTION OF CELLULOSE BY RUMEN MICROORGANISMS INTRODUCTION Mesquite beans have been used as feed for oattle sinoe the extensive invasion by the mesquite tree (PORN~, )~i...

  2. In vitro Activity of Celery Essential Oil against Malassezia furfur

    PubMed Central

    Lee, Min Hee

    2009-01-01

    Antifungal activity of celery essential oil against Malassezia furfur was investigated using broth microdilution and vapor contact methods. Potent antifungal activity was evident using both methods. Fungicidal activity was revealed in the vapor contact method. PMID:23983510

  3. Chemical composition and biological activities of essential oil from Salvia sclarea plants regenerated in vitro.

    PubMed

    Ku?ma, Lukasz; Kalemba, Danuta; Rózalski, Marek; Rózalska, Barbara; Wieckowska-Szakiel, Marzena; Krajewska, Urszula; Wysoki?ska, Halina

    2009-01-01

    The essential oils obtained by hydrodistillation of dried aerial parts of Salvia sclarea L. plants, regenerated in vitro and reproduced from seeds, were analyzed by GC and GC-MS. The oils from in vitro and in vivo plants were compared in respect to their chemical composition as well as antimicrobial and cytotoxic activities. The chemical profiles of both oils were very similar, although the yield of essential oil from in vitro plants was lower (0.1%, v/w) than the oil yield isolated from in vivo S. sclarea plants (0.2%, v/w). Both oils showed antimicrobial and cytotoxic activity. The oil from in vitro regenerated plants of S. sclarea exhibited stronger cytotoxic action against NALM-6 cell lines in comparison with the essential oil from in vivo plants. PMID:19384275

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

    PubMed Central

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

    2011-01-01

    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

  5. In vitro and in vivo antileishmanial activities of a Brazilian green propolis extract

    Microsoft Academic Search

    Karina Pontin; Ademar A. Da Silva Filho; Fransérgio Francisco Santos; Márcio Luís Andrade e Silva; Wilson Roberto Cunha; N. P. Dhammika Nanayakkara; Jairo Kenupp Bastos; Sérgio de Albuquerque

    2008-01-01

    The in vitro antileishmanial activity of Brazilian green propolis hydroalcoholic extract (BPE) were carried out on Leishmania (Viannia) braziliensis against both promastigote (doses ranging from 1 to 750 ?g mL?1) and amastigote (10, 100, and 250 ?g mL?1) assays in comparison with the positive (amphotericin B) and negative (dimethyl sulfoxide at 1% in physiologic solution)\\u000a control groups. BPE displayed in vitro antileishmanial

  6. Components of normal serum block the focal segmental glomerulosclerosis factor activity in vitro

    Microsoft Academic Search

    Ram Sharma; Mukut Sharma; Ellen T. Mccarthy; Xiu-Li Ge; Virginia J. Savin

    2000-01-01

    Components of normal serum block the focal segmental glomerulosclerosis factor activity in vitro.BackgroundSera from some patients with focal segmental glomerulosclerosis (FSGS) increase glomerular albumin permeability (Palb) in vitro. The hypothesis that a component of normal serum can protect the glomerular permeability barrier was tested using sera from FSGS patients, normal individuals, and several mammalian and avian species.MethodsIn most experiments, isolated

  7. Gemcitabine aerosol: in vitro antitumor activity and deposition imaging for preclinical safety assessment in baboons

    Microsoft Academic Search

    Frédéric Gagnadoux; Valérie Leblond; Laurent Vecellio; José Hureaux; Alain Le Pape; Michčle Boisdron-Celle; Jérome Montharu; Caroline Majoral; Joseph Fournier; Thierry Urban; Patrice Diot; Jean-Louis Racineux; Etienne Lemarié

    2006-01-01

    Aim: To characterize gemcitabine aerosol, its in vitro activity against lung cancer cells, its deposition, and tolerance in a non-human primate model. Methods: In vitro cytotoxicity of nebulized gemcitabine against NCI-H460 and A549 lung cancer cells was tested using a growth inhibition assay and compared with non-nebulized gemcitabine. The 99mTc-DTPA-radiolabeled gemcitabine aerosol was characterized by cascade impaction and the gemcitabine

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

    PubMed

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

    2014-06-01

    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

  9. The effect of recombinant tissue plasminogen activator on MMP-2 and MMP-9 activities in vitro.

    PubMed

    Golab, Piotr; Kielbus, Michal; Bielewicz, Joanna; Kurzepa, Jacek

    2015-01-01

    One of the most significant side effects during recombinant tissue plasminogen activator (rtPA) for acute stroke treatment is intracranial bleeding. Gelatinases [matrix metalloproteinase (MMP)-2 and MMP-9] are one of the agents involved in the blood-brain barrier destruction resulting in secondary bleeding into the ischemic area during stroke. Previous papers revealed that patients with high baseline MMP-9 serum level have higher risk of intracranial bleeding after thrombolytic therapy. Our objective was to evaluate rtPA influence on serum MMP-2 and MMP-9 activities in vitro. Nine sera obtained from healthy donors were applied for experiment. The commercially available rtPA (Actylise) were diluted with included solvent and additionally with phosphate-buffered saline (PBS) to get concentrations: 2, 4, 8, and 16 ?g/ml. Next, 100 ?l of serum was mixed with equal proportion with different concentrations of rtPA to obtain final rtPA concentrations: 1, 2, 4, and 8 ?g/ml. The sera together with rtPA were incubated for 1 or 2 hours at 37 °C. The activity of gelatinases was estimated with zymography. The activities of MMP-9 (92 kDa) and MMP-2 (72 kDa) were increased by incubation with rtPA in a dose-dependent manner. Simultaneously, the activity of band at 200 kDa (MMP-9/MMP-9 homodimer) was decreased. The activity of gelatinases incubated for 2 hours was elevated in comparison with 1-hour incubation; however, the increase was observed even for sample without rtPA. In conclusion, this study showed that rtPA can increase the biological activity of MMP-2 and MMP-9 on posttranslational level. PMID:24963695

  10. In vitro extracellular recording of spontaneous activity of the intergeniculate leaflet neurons.

    PubMed

    Blasiak, Anna; Lewandowski, Marian H

    2004-07-23

    In the view of importance of intergeniculate leaflet in circadian rhythms processes and lack of information about electrophysiological properties of isolated intergeniculate leaflet (IGL) neurons, we carried out extracellular recordings of the spontaneous activity of rat IGL cells in vitro. Unlike other structures of visual thalamus, IGL neurons have the ability to generate a robust spontaneous neuronal activity when maintained in vitro. We have observed that in a standard incubation fluid IGL neurons display at least three distinct firing patterns: continuously irregular-with a wide variety of firing rates, tonic-with a very stable level of activity, and phasic (slow bursts)-with intermittent silent periods. Our study is the first electrophysiological demonstration of IGL neuronal activity in vitro. PMID:15223369

  11. [In vitro evaluation of antibacterial activity and cytocompatibility of antibacterial stainless steel containing copper].

    PubMed

    Guan, Junlin; Guo, Lei; Fu, Yuping; Chai, Hongwei

    2013-04-01

    To study the in vitro antibacterial activity and biocompatibility of 317L stainless steel containing 4.5% copper alloy (317L-Cu), we produced 317L-Cu stainless steel with epsilon-Cu phase. The cell proliferation of osteoblasts on material surface was detected in vitro. Escherichia coli was cultured with 317L-Cu for evaluating the antibacterial activity. We found that the 317L-Cu could effectively kill the Escherichia coli on material surface. The cell proliferation of osteoblasts on material surface was not different significantly, compared with titanium material. Our study clearly demonstrated that the 317L-Cu alloys had a significant antimicrobial activity and was biocompatible in vitro, so it would be suitable to be used as a new medical material with antibacterial activity. PMID:23858758

  12. EFFECT OF CYTOKININ-ACTIVE PHENYLUREA DERIVATIVES ON SHOOT MULTIPLICATION, PEROXIDASE AND SUPEROXIDE DISMUTASE ACTIVITIES OF in vitro CULTURED CARNATION

    Microsoft Academic Search

    Todor Genkov; Iordanka Ivanova

    Summary. In the present study examined the effects of different types of cyto- kinins on the growth of in vitro cultured carnation. NAA alone produced nei- ther multiplication nor elongation. Combined with BAP, NAA increased multiplication. The biological activity of 4-PU-30 and especially that of thidi- azuron was considerably higher than BAP's activity. In equal concentrations with BAP thidiazuron increased

  13. Potent Inhibitors of Plasmodium Phospholipid Metabolism with a Broad Spectrum of In Vitro Antimalarial Activities

    Microsoft Academic Search

    Marie L. Ancelin; Michele Calas; Valerie Vidal-Sailhan; Serge Herbute; Pascal Ringwald; Henri J. Vial

    2003-01-01

    We characterized the potent in vitro antimalarial activity and biologic assessment of 13 phospholipid polar head analogs on a comparative basis. There was a positive relationship between the abilities of the drugs to inhibit parasite growth in culture and their abilities to specifically inhibit phosphatidylcholine biosynthesis of Plasmodium falciparum-infected erythrocytes. Maximal activity of G25 was observed for the trophozoite stage

  14. Antioxidative activity of persimmon and grape seed extract: in vitro and in vivo

    Microsoft Academic Search

    Hong Seok Ahn; Tae Il Jeon; Joo Yong Lee; Seong Gu Hwang; Yoongho Lim; Dong Ki Park

    2002-01-01

    We determined in vitro radical scavenging activity of persimmon seed extract (PSE) and grape seed extract (GSE), and quantified total tannin concentrations of each extract. It has been found that both PSE and GSE have radical scavenging activities, and total tannin concentration of PSE was significantly higher than GSE (p < 0.05). In order to investigate the protective effect on

  15. Activation of microglia by Borna disease virus infection: in vitro study

    Technology Transfer Automated Retrieval System (TEKTRAN)

    Neonatal Borna disease virus (BDV) infection of the rat brain is associated with microglial activation and damage to the certain neuronal populations. Since persistent BDV infection of neurons in vitro is noncytolytic and noncytopathic, activated microglia have been suggested to be responsible for n...

  16. Evaluation of African medicinal plants for their in vitro trypanocidal activity

    Microsoft Academic Search

    F. Freiburghaus; R. Kaminsky; M. H. H. Nkunya; R. Brun

    1996-01-01

    Petroleum ether, dichloromethane, methanol and water extracts from 24 plants, belonging to 19 families, which are reported in the literature as traditional remedies for sleeping sickness (human African trypanosomiasis) were screened for in vitro activity against Trypanosoma brucei rhodesiense, as well as for cytotoxicity for a human fibroblast cell-line (WI-38). The trypanocidal activity of the natural compounds berberine and harmane,

  17. In Vitro Nitric Oxide Scavenging Activity of Ethanol Leaf Extracts of Four Bangladeshi Medicinal Plants

    Microsoft Academic Search

    Moni Rani Saha; Rumana Jahangir; Israt Jahan Biv

    2008-01-01

    The ethanol leaf extracts of four medicinal plants named Hibiscus mutabilis, Leucas aspera, Ixora coccinea and Polyalthia longifolia 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

  18. In vitro inhibitory effect of SR 27417, a potent platelet-activating factor (PAF) receptor antagonist,

    E-print Network

    Paris-Sud XI, Université de

    Short Note In vitro inhibitory effect of SR 27417, a potent platelet-activating factor (PAF) receptor antagonist, on the PAF-induced bovine platelet aggregation Miriam BASTOS DA SILVAa, Annie of the platelet-activating factor (PAF) receptor, on PAF-induced platelet aggregation was studied in blood

  19. Development of a novel in vitro onychomycosis model for the evaluation of topical antifungal activity.

    PubMed

    Sleven, Reindert; Lanckacker, Ellen; Boulet, Gaëlle; Delputte, Peter; Maes, Louis; Cos, Paul

    2015-05-01

    A novel in vitro onychomycosis model was developed to easily predict the topical activity potential of novel antifungal drugs. The model encompasses drug activity and diffusion through bovine hoof slices in a single experimental set-up. Results correspond well with the antifungal susceptibility assay and Franz cell diffusion test. PMID:25772040

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

    Microsoft Academic Search

    Esteban Toro; Scott F Michael

    2004-01-01

    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

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

    PubMed Central

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

    2011-01-01

    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

  2. In vitro and in vivo evaluation of a new active heat moisture exchanger

    Microsoft Academic Search

    Davide Chiumello; Paolo Pelosi; Gilbert Park; Andrea Candiani; Nicola Bottino; Ezio Storelli; Paolo Severgnini; Dunia D'Onofrio; Luciano Gattinoni; Massimo Chiaranda

    2004-01-01

    INTRODUCTION: In order to improve the efficiency of heat moisture exchangers (HMEs), new hybrid humidifiers (active HMEs) that add water and heat to HMEs have been developed. In this study we evaluated the efficiency, both in vitro and in vivo, of a new active HME (the Performer; StarMed, Mirandola, Italy) as compared with that of existing HMEs (Hygroster and Hygrobac;

  3. Effects of heparin on synaptic activity in the hemorrhagic stroke model in vitro.

    PubMed

    Mokrushin, A A; Pavlinova, L I

    2012-04-01

    We studied the ability of heparin to modify synaptic activity on the original stroke model in vitro. Cultured slices of the brain slices from hypertensive rats were treated with the autoblood clot. Administration of heparin (2 mg/ml) before autoblood treatment had a protective effect on ionotropic glutamatergic and GABAergic receptors, whose activity was inhibited by the blood. PMID:22803164

  4. A Study on the In Vitro Antioxidant Activity of Juniper (Juniperus communis L.) Fruit Extracts

    Microsoft Academic Search

    Mahfuz Elmasta?; ?lhami Gülçin; ?ükrü Beydemir; Ö. ?rfan Küfrevio?lu

    2006-01-01

    This study aimed at evaluating the in vitro antioxidant activity of water and ethanol extracts of juniper (Juniperus communis L., Family Cupressaceae) fruit. The antioxidant properties of both Juniper extracts were studied using different antioxidant assays, including reducing power, free radical scavenging, superoxide anion radical scavenging, hydrogen peroxide scavenging, and metal chelating activities. Both the water and the ethanol extracts

  5. In vitro Activities of Ciprofloxacin, Ofloxacin, Norfloxacin and Rosoxacin Compared with Cinoxacin and Trimethoprim

    Microsoft Academic Search

    Asbjorn Digrams; William L. Dibb; Eva Benonisen

    1985-01-01

    The in vitro activities of ciprofloxacin, ofloxacin, norfloxacin, rosoxacin, cinoxacin and trimethoprim have been compared. An agar dilution method has been employed for the measurement of minimal inhibitory concentrations (MICs). 426 clinical, bacterial urinary isolates mainly from hospitalised patients were included; all common urinary tract pathogens were represented. The newer quinolones were highly active against Enterobacteriaceae species, Pseudomonas aeruginosa and

  6. In vitro antioxidant activity study of novel chromone derivatives.

    PubMed

    Phosrithong, Narumol; Samee, Weerasak; Nunthanavanit, Patcharawee; Ungwitayatorn, Jiraporn

    2012-06-01

    Forty-eight chromone derivatives were evaluated for their antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl free radical scavenging assay, ferrous ions (Fe(2+) ) chelating activity test, total antioxidant activity test (Ferric thiocyanate and Thiobarbituric acid methods), and total reductive capability (potassium ferricyanide reduction). 7,8-Dihydroxy-2-(3'-trifluoromethylphenyl)-3-(3?-trifluoromethylbenzoyl) chromone 32 showed stronger radical scavenging and metal chelating activities than butylated hydroxytoluene, vitamin E, and trolox. Chromone derivatives that exhibited good radical scavenging and metal chelating also displayed strong total antioxidant and reductive power activities. The results obtained from this study indicated that the synthesized chromone derivatives have remarkable antioxidant activity. PMID:22381130

  7. In vitro activity of ponazuril against Theileria equi.

    PubMed

    Wise, L Nicki; Ueti, Massaro W; Kappmeyer, Lowell S; Hines, Melissa T; White, Stephen N; Davis, Wendell; Knowles, Donald P

    2012-04-30

    The equid hemoprotozoan parasite Theileria equi is endemic in most regions worldwide. Infection of horses is a cause of significant economic loss due to costs associated with disease and restriction of trade with non-endemic nations. The ability of certain drugs such as imidocarb dipropionate to eliminate persistent T. equi infection and transmission risk is controversial. The anti-protozoal agent ponazuril has been used successfully to treat equine Sarcosystis neurona and Toxoplasma gondii. The hypothesis that ponazuril inhibits replication of T. equi in vitro was tested. T. equi infected equine erythrocyte cultures were treated with ponazuril at multiple concentrations. Cessation of parasite replication was observed over a 5-day period and the degree of inhibition was variable between drug concentrations. Ponazuril inhibited T. equi in erythrocyte culture at all concentrations tested but parasite elimination required at least 500 ?g/mL. The high dose of ponazuril required for in vitro inhibition likely limits its ability to control or clear T. equi infection in vivo, however additional research to evaluate related drugs is warranted. PMID:22130334

  8. Activity of flumequine against Escherichia coli: in vitro comparison with nalidixic and oxolinic acids.

    PubMed Central

    Greenwood, D

    1978-01-01

    The in vitro activity of the new antibacterial agent, flumequine, against Escherichia coli was compared with those of oxolinic acid and nalidixic acid. As judged by turbidimetric criteria, flumequine was considerably more active than nalidixic acid and slightly less active than oxolinic acid against both nalidixic acid-susceptible and -resistant strains. Resistance to all three drugs could be easily induced in vitro. The comparative efficacy of flumequine, oxolinic acid, and nalidixic acid was also tested in an in vitro model of the treatment of bacterial cystitis. In this system, suppression of bacterial growth was obtained with markedly lower concentrations of flumequine and oxolinic acid than of nalidixic acid, but prevention of the emergence of bacterial populations that exhibited increased resistance to these compounds depended on the maintenance of adequate drug levels. PMID:400825

  9. Antithrombotic activities of pellitorine in vitro and in vivo.

    PubMed

    Ku, Sae-Kwang; Lee, In-Chul; Kim, Jeong Ah; Bae, Jong-Sup

    2013-12-01

    Pellitorine (PLT), an active amide compound, is well known to possess insecticidal, antibacterial and anticancer properties. However, the anti-coagulant functions of PLT are not studied yet. Here, the anticoagulant activities of PLT were examined by monitoring activated partial thromboplastin time (aPTT), prothrombin time (PT), and the activities of cell-based thrombin and activated factor X (FXa). Furthermore, the effects of PLT on the expressions of plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) were tested in tumor necrosis factor (TNF)-? activated human umbilical vein endothelial cells (HUVECs). Treatment with PLT resulted in prolonged aPTT and PT and inhibition of the activities of thrombin and FXa, and PLT inhibited production of thrombin and FXa in HUVECs. And PLT inhibited thrombin-catalyzed fibrin polymerization and platelet aggregation. In accordance with these anticoagulant activities, PLT elicited anticoagulant effects in mouse. In addition, treatment with PLT resulted in the inhibition of TNF-?-induced production of PAI-1 and in the significant reduction of the PAI-1 to t-PA ratio. Collectively, PLT possesses antithrombotic activities and offers bases for development of a novel anticoagulant. PMID:23973654

  10. Anticoagulant activities of piperlonguminine in vitro and in vivo.

    PubMed

    Lee, Wonhwa; Yoo, Hayoung; Ku, Sae-Kwang; Kim, Jeong Ah; Bae, Jong-Sup

    2013-10-01

    Piperlonguminine (PL), an important component of Piper longum fruits, is known to exhibit anti-hyperlipidemic, anti-platelet and anti-melanogenic activities. Here, the anticoagulant activities of PL were examined by monitoring activated-partial-thromboplastin-time (aPTT), prothrombin-time (PT), and the activities of thrombin and activated factor X (FXa). The effects of PL on the expressions of plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) were also tested in tumor necrosis factor-? (TNF-?) activated HUVECs. The results showed that PL prolonged aPTT and PT significantly and inhibited the activities of thrombin and FXa. PL inhibited the generation of thrombin and FXa in HUVECs. In accordance with these anticoagulant activities, PL prolonged in vivo bleeding time and inhibited TNF-? induced PAI-1 production. Furthermore, PAI-1/t-PA ratio was significan- tly decreased by PL. Collectively, our results suggest that PL possesses antithrombotic activities and that the current study could provide bases for the development of new anticoagulant agents. PMID:24148768

  11. Activation of polyunsaturated fatty acids by rat tissues in vitro

    SciTech Connect

    Reddy, T.S.; Bazan, N.G.

    1984-12-01

    The conversion of labeled palmitic, linoleic, arachidonic and docosahexaenoic acids to their respective acyl CoA's was studied in homogenates and microsomes of rat tissues. The highest activity, both in homogenates and microsomes, was seen in liver and heart. There was moderate activity in retina, brain, lung, kidney and testes and the lowest activity was found in spleen. Docosahexaenoic acid was activated much less actively in heart tissue than the other fatty acids. In all tissues examined, the highest activation was observed with arachidonic acid and the lowest with docosahexaenoic acid. Except for liver, those tissues that contained high levels of docosahexaenoic acid also had the highest activation capacity for this fatty acid.

  12. Anticoagulant activities of piperlonguminine in vitro and in vivo

    PubMed Central

    Lee, Wonhwa; Yoo, Hayoung; Ku, Sae-Kwang; Kim, Jeong Ah; Bae, Jong-Sup

    2013-01-01

    Piperlonguminine (PL), an important component of Piper longum fruits, is known to exhibit anti-hyperlipidemic, antiplatelet and anti-melanogenic activities. Here, the anticoagulant activities of PL were examined by monitoring activatedpartial-thromboplastin-time (aPTT), prothrombin-time (PT), and the activities of thrombin and activated factor X (FXa). The effects of PL on the expressions of plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) were also tested in tumor necrosis factor-? (TNF-?) activated HUVECs. The results showed that PL prolonged aPTT and PT significantly and inhibited the activities of thrombin and FXa. PL inhibited the generation of thrombin and FXa in HUVECs. In accordance with these anticoagulant activities, PL prolonged in vivo bleeding time and inhibited TNF-? induced PAI-1 production. Furthermore, PAI-1/t-PA ratio was significantly decreased by PL. Collectively, our results suggest that PL possesses antithrombotic activities and that the current study could provide bases for the development of new anticoagulant agents. [BMB Reports 2013; 46(10): 484-489] PMID:24148768

  13. In vitro evaluation of antioxidant activity of Cordia dichotoma (Forst f.) bark

    PubMed Central

    Nariya, Pankaj B.; Bhalodia, Nayan R.; Shukla, Vinay J.; Acharya, Rabinarayan; Nariya, Mukesh B.

    2013-01-01

    Cordia dichotoma Forst. f. bark, identified as botanical source of Shleshmataka in Ayurvedic pharmacopoeia. Present investigation was undertaken to evaluate possible antioxidant potential of methanolic and butanol extract of C. dichotoma bark. In vitro antioxidant activity of methanolic and butanol extract was determined by 1,1, diphenyl–2, picrylhydrazyl (DPPH) free radical scavenging assay. The extracts were also evaluated for their phenolic contents and antioxidant activity. Phenolic content was measured using Folin–Ciocalteu reagent and was calculated as Gallic acid equivalents. Antiradical activity of methanolic extract was measured by DPPH assay and was compared to ascorbic acid and ferric reducing power of the extract was evaluated by Oyaizu method. In the present study three in vitro models were used to evaluate antioxidant activity. The first two methods were for direct measurement of radical scavenging activity and remaining one method evaluated the reducing power. The present study revealed that the C. dichotoma bark has significant radical scavenging activity. PMID:24049418

  14. Neuraminidase inhibitory activities of flavonols isolated from Rhodiola rosea roots and their in vitro anti-influenza viral activities

    Microsoft Academic Search

    Hyung Jae Jeong; Young Bae Ryu; Su-Jin Park; Jang Hoon Kim; Hyung-Jun Kwon; Jin Hyo Kim; Ki Hun Park; Mun-Chual Rho; Woo Song Lee

    2009-01-01

    Five flavonols (3, 5, and 9–11) were isolated from Rhodiola rosea, and compared with commercially available flavonoids (1, 2, 4, 6–8, and 12–14) to facilitate analysis of their structure–activity relationship (SAR). All compounds (1–14) showed neuraminidase inhibitory activities with IC50 values ranging from 0.8 to 56.9?M. The in vitro anti-influenza virus activities of flavonoids 1–6, 8–12, and 14 were evaluated

  15. Synthesis, antimycobacterial activity and in vitro cytotoxicity of 5-chloro-N-phenylpyrazine-2-carboxamides.

    PubMed

    Zitko, Jan; Servusová, Barbora; Paterová, Pavla; Mandíková, Jana; Kubí?ek, Vladimír; Ku?era, Radim; Hrabcová, Veronika; Kuneš, Ji?í; Soukup, Ond?ej; Doležal, Martin

    2013-01-01

    5-Chloropyrazinamide (5-Cl-PZA) is an inhibitor of mycobacterial fatty acid synthase I with a broad spectrum of antimycobacterial activity in vitro. Some N-phenylpyrazine-2-carboxamides with different substituents on both the pyrazine and phenyl core possess significant in vitro activity against Mycobacterium tuberculosis. To test the activity of structures combining both the 5-Cl-PZA and anilide motifs a series of thirty 5-chloro-N-phenylpyrazine-2-carboxamides with various substituents R on the phenyl ring were synthesized and screened against M. tuberculosis H37Rv, M. kansasii and two strains of M. avium. Most of the compounds exerted activity against M. tuberculosis H37Rv in the range of MIC = 1.56-6.25 µg/mL and only three derivatives were inactive. The phenyl part of the molecule tolerated many different substituents while maintaining the activity. In vitro cytotoxicity was decreased in compounds with hydroxyl substituents, preferably combined with other hydrophilic substituents. 5-Chloro-N-(5-chloro-2-hydroxyphenyl)pyrazine-2-carboxamide (21) inhibited all of the tested strains (MIC = 1.56 µg/mL for M. tuberculosis; 12.5 µg/mL for other strains). 4-(5-Chloropyrazine-2-carboxamido)-2-hydroxybenzoic acid (30) preserved good activity (MIC = 3.13 µg/mL M. tuberculosis) and was rated as non-toxic in two in vitro models (Chinese hamster ovary and renal cell adenocarcinoma cell lines; SI = 47 and 35, respectively). PMID:24317522

  16. Antioxidative Activity of Lichen Thamnolia vermicularis in vitro

    PubMed Central

    Luo, Heng; Ren, Meirong; Lim, Kwang-Mi; Koh, Young Jin; Wang, Li-Song

    2006-01-01

    This study was aimed at evaluating the antioxidant activities of methanol extract of Thamnolia vermicularis. The antioxidant activity, reducing power, superoxide anion radical scavenging and free radical scavenging activities were studied. The antioxidant activity of the extract correlated with its concentration (0.2~2 mg/ml) in the reaction mixtures containing linoleic acid. Upto 67% of lipid peroxidation was inhibited by 2 mg/ml of the lichen extract. The extract showed strong free radical scavenging activity similar to that of BHA (positive control) in a manner of concentration dependent. The lichen extract also showed moderate effects on superoxide anoin scavenging activity and reducing power, which was not so effective as that of Quercetin and BHA used as positive controls. This study suggests that T. vermicularis lichen can be used as a novel source of natural antioxidant. PMID:24039484

  17. Anti-Herpetic Activity of Callissia fragrans and Simmondsia chinensis Leaf Extracts In Vitro

    PubMed Central

    Yarmolinsky, Ludmila; Zaccai, Michele; Ben-Shabat, Shimon; Huleihel, Mahmoud

    2010-01-01

    The antiviral activity of Callissia fragrans and Simnondsia chinensis aquatic and ethanol leaf extracts, as well as purified fractions from these extracts was studied against herpetic viruses in vitro. Ethanol extract of C. fragrans effectively inhibited the infection of Vero cells by HSV-1, HSV-2 in vitro, while its aquatic extract inhibited only VZV. Although S. chinensis leaf extract strongly inhibited all studied viruses, the selectivity index of this extract was very low, due to its high toxicity. However, the majority of its fractions showed low toxicity and higher antiviral activity and therefore very high SI. Strong interactions between virus and extracts were found. PMID:20700398

  18. Comparison of In Vitro Activity of Cephalexin, Cephradine, and Cefaclor

    PubMed Central

    Bill, Nancy J.; Washington, John A.

    1977-01-01

    Inhibitory activity of cephalexin, cephradine, and cefaclor was compared by the WHO-ICS agar dilution technique. Cefaclor was substantially more active against staphylococci, streptococci, gonococci, meningococci, Haemophilus, Escherichia coli, Klebsiella pneumoniae, Citrobacter diversus, Proteus mirabilis, salmonellae, and shigellae than was cephalexin, which in turn was more active than cephradine. Cefaclor appeared to be less resistant to staphylococcal penicillinase than did the other two agents. None of these cephalosporins was active against Enterobacter, Serratia, indole-positive Proteeae, Pseudomonas, or Bacteroides fragilis. PMID:301005

  19. In vitro TRPV1 activity of piperine derived amides.

    PubMed

    Correa, Edwin Andrés; Högestätt, Edward D; Sterner, Olov; Echeverri, Fernando; Zygmunt, Peter M

    2010-05-01

    A series of natural and synthetic piperine amides were evaluated for activity on the human TRPV1 expressed in HEK293 cells. The agonistic effect of piperine amides was mainly dependent on the length of the carbon chain. Structural changes of double bonds and stereochemistry in the aliphatic chain of these compounds did not change their potency or efficacy, indicating that increased rigidity or planarity of the piperine structure does not affect the activity. The opening of the methylenedioxy ring or changes in the heterocyclic ring of the piperine molecule reduced or abolished activity. Furthermore, inactive compounds did not display functional antagonistic activity. PMID:20381363

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

    PubMed Central

    2011-01-01

    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

  1. In vitro augmentation of natural killer cell activity by manganese chloride

    Microsoft Academic Search

    Ralph J. Smialowicz; Ronald R. Rogers; Marie M. Riddle; Denise G. Rowe; Robert W. Luebke

    1986-01-01

    The in vitro cultivation of murine spleen cells with MnCl2 resulted in the enhancement of natural killer (NK) cell activity as measured in a 4?h Cr?release assay. Optimal enhancement of NK activity was observed at concentrations of 70–20 ?g MnCl2\\/culture (72–144 ?M Mn). Enhancement of NK activity by MnCl2 was not associated with any changes in the number or viability

  2. Comparative in vitro activity of levofloxacin and ofloxacin against Gram-positive bacteria

    Microsoft Academic Search

    George M. Eliopoulos; Christine B. Wennersten; Robert C. Moellering

    1996-01-01

    The in vitro activity of levofloxacin against 506 Gram-positive bacteria was compared with those of D(?)-ofloxacin, ofloxacin, ciprofloxacin, and sparfloxacin. Levofloxacin was generally twice as active as ofloxacin against these organisms (range, 0–3 twofold dilutions). Sparfloxacin appeared to have the greatest activity overall, but for several groups of organisms minimum inhibitory concentrations (MIC90s) of this com pound were within one

  3. Synthesis and in vitro antibacterial activity of quaternary ammonium cephalosporin derivatives bearing oxazolidinone moiety

    Microsoft Academic Search

    In Hwa Chung; Choong Sup Kim; Jae Hong Seo; Bong Young Chung

    1999-01-01

    Several oxazolidinones having amine moiety were prepared to form a quaternary ammonium salt with cephalosporin nucleus, and\\u000a antibacterial activity of the quaternary ammonium cephalosporin derivatives bearing oxazolidinone moiety were examined particularly\\u000a with expectation of dual activity. However, the cephalosporin-oxazolidinone compounds revealed rather weaker antibacterial\\u000a activityin vitro than their parent exazolidinone and cephalosporin without showing any characteristic activity as expected.

  4. Grape Seed Extract Activates Th1 Cells In Vitro

    Microsoft Academic Search

    Narayanan Nair; Supriya Mahajan; Ram Chawda; Chithan Kandaswami; Thomas C. Shanahan; Stanley A. Schwartz

    2002-01-01

    Although flavonoids manifest a diverse range of biological activities, including antitumor and antiviral effects, the molecular mechanisms underlying these activities await elucidation. We hypothesize that the flavonoid constituents of a proprietary grape seed extract (GSE) that contains procyandins exert significant antiviral and antitumor effects, by inducing production of the Th1-derived cytokine gamma interferon (IFN-) by peripheral blood mononuclear cells) from

  5. Temporal changes in intestinal Na+ -ATPase activity and in vitro

    E-print Network

    Young, Graham

    , may contribute signifi- cantly to seawater adaptation. In brown trout (Salmo trutta), the activity activity and fluid absorption across this region of the gut in euryhaline rainbow trout (Salmo gairdneri) and Atlantic salmon (Salmo salar; Madsen, 1990; Cornell et al., 1994; Specker et al., 1994). Furthermore

  6. Cortical synchronized activity evoked by thalamocortical stimulation in vitro.

    PubMed

    Gil, Z; Amitai, Y

    1995-01-01

    Epileptiform activity was studied in the thalamocortical (THC) slice preparation. Inhibition was gradually attenuated with increasing doses of bicuculline methiodide (BMI). We compared the ability of thalamic and intracortical (INC) stimulation to evoke epileptiform activity. Synchronized population activity was identified by its all-or-none appearance at a threshold stimulus intensity, by a variable latency and by horizontal propagation to large distances. For most slices (20 out of 24) we could establish a threshold dose of BMI (0.4-0.7 microM) under which THC-evoked population events had epileptiform properties, while INC-evoked ones did not. Increasing the BMI dose by 0.2 microM resulted in the appearance of epileptiform field potentials when stimulating intracortically. It is concluded that the tendency of the neocortex to generate synchronized population activity is higher when it is activated through the THC pathway. PMID:7746472

  7. In vitro cytotoxicity activity of Diosquinone, a naphthoquinone epoxide.

    PubMed

    Adeniyi, B A; Robert, M F; Chai, H; Fong, H H S

    2003-03-01

    Diosquinone [1], a naphthoquinone epoxide previously isolated from the root bark of Diospyros mespiliformis (Hostch) and D. tricolor [Ebenaceae] is been assessed for cytotoxicity activity against ten cancer cell lines by standard NIH method. The ethno-pharmacological claim of this plant and the previously observed good antibacterial activity of this compound among the others isolated from this plant suggest its probable cytotoxicity activity. Diosquinone was observed to be very active against most of the cancer cell lines. It shows very good activity against all the cell lines tested with ED50 value ranging between 0.18 microg/ml. against Human Glioblastoma (U373) to 4.5 microg/ml. against Hormone dependent human prostrate cancer( LNCaP). PMID:12672163

  8. In vitro augmentation of natural killer cell activity by manganese chloride

    SciTech Connect

    Smialowicz, R.J.; Rogers, R.R.; Riddle, M.M.; Rowe, D.G.; Luebke, R.W.

    1986-01-01

    The in vitro cultivation of murine spleen cells with MnCl/sub 2/ resulted in the enhancement of natural killer (NK) cell activity as measured in a 4-h /sup 51/Cr-release assay. Optimal enhancement of NK activity was observed at concentrations of 10-20 ..mu..g MnCl/sub 2//culture (72-144 ..mu..M Mn/sup 2 +/). Enhancement of NK activity by MnCl/sub 2/ was not associated with any changes in the number or viability of cells following culture. The addition of antiasialo GM/sub 1/ antibody and complement to spleen cell cultures completely abrogated the enhancement of NK activity by MnCl/sub 2/. The enhancement of NK activity by MnCl/sub 2/ in vitro was accompanied by interferon induction. The addition of rabbit antimouse interferon to spleen cells cultured with MnCl/sub 2/ reduced NK activity. NK activity in cultures treated with MnCl/sub 2/ was also reduced upon removal of plastic adherent cells. However, restoration of enhanced NK activity by addition of adherent cells to nonadherent cells in the presence of MnCl/sub 2/ was not observed. Similar effects of NK activity were observed with polyinosinic-polycytidylic acid (Poly I x C), a known interferon inducer and NK enhancer. The results demonstrate that murine splenic NK activity is enhanced in vitro by MnCl/sub 2/ and that this enhancement may be mediated by interferon induction. The results also suggest that in vitro enhancement of NK activity by MnCl/sub 2/, as with Poly I x C, may require participation of an adherent cell population for NK augmentation.

  9. In vitro differentiation of human macrophages with enhanced antimycobacterial activity

    PubMed Central

    Vogt, Guillaume; Nathan, Carl

    2011-01-01

    Mycobacterium tuberculosis causes widespread, persistent infection, often residing in macrophages that neither sterilize the bacilli nor allow them to cause disease. How macrophages restrict growth of pathogens is one of many aspects of human phagocyte biology whose study relies largely on macrophages differentiated from monocytes in vitro. However, such cells fail to recapitulate the phenotype of tissue macrophages in key respects, including that they support early, extensive replication of M. tuberculosis and die in several days. Here we found that human macrophages could survive infection, kill Mycobacterium bovis BCG, and severely limit the replication of M. tuberculosis for several weeks if differentiated in 40% human plasma under 5%–10% (physiologic) oxygen in the presence of GM-CSF and/or TNF-? followed by IFN-?. Control was lost with fetal bovine serum, 20% oxygen, M-CSF, higher concentrations of cytokines, or premature exposure to IFN-?. We believe that the new culture method will enable inquiries into the antimicrobial mechanisms of human macrophages. PMID:21911939

  10. In vitro neuroprotective activities of compounds from Angelica shikokiana Makino.

    PubMed

    Mira, Amira; Yamashita, Shuntaro; Katakura, Yoshinori; Shimizu, Kuniyoshi

    2015-01-01

    Angelica shikokiana is widely marketed in Japan as a dietary food supplement. With a focus on neurodegenerative conditions such as Alzheimer's disease, the aerial part was extracted and through bio-guided fractionation, fifteen compounds [?-glutinol, ?-amyrin, kaempferol, luteolin, quercetin, kaempferol-3-O-glucoside, kaempferol-3-O-rutinoside, methyl chlorogenate, chlorogenic acid, hyuganin E, 5-(hydroxymethyl)-2-furaldehyde, ?-sitosterol-3-O-glucoside, adenosine (isolated for the first time from A. shikokiana), isoepoxypteryxin and isopteryxin] were isolated. Isolated compounds were evaluated for in vitro neuroprotection using acetylcholine esterase inhibitory, protection against hydrogen peroxide and amyloid ? peptide (A?25-35)-induced neurotoxicity in neuro-2A cells, scavenging of hydroxyl radicals and intracellular reactive oxygen species and thioflavin T assays. Quercetin showed the strongest AChE inhibition (IC50 value = 35.5 µM) through binding to His-440 and Tyr-70 residues at the catalytic and anionic sites of acetylcholine esterase, respectively. Chlorogenic acid, its methyl ester, quercetin and luteolin could significantly protect neuro-2A cells against H2O2-induced neurotoxicity and scavenge hydroxyl radical and intracellular reactive oxygen species. Kaempferol-3-O-rutinoiside, hyuganin E and isoepoxypteryxin significantly decreased A?25-35-induced neurotoxicity and Th-T fluorescence. To the best of our knowledge, this is the first report about neuroprotection of hyuganin E and isoepoxypteryxin against A?25-35-induced neurotoxicity. PMID:25786165

  11. Secretory activity of Poecilia latipinna (Teleostei) pituitary in vitro: rostral pars distalis and proximal pars distalis.

    PubMed

    Batten, T F; Young, G; Ball, J N

    1983-07-01

    The ultrastructure of each adenohypophysial secretory cell type was examined in pituitaries of adult female mollies (Poecilia latipinna) after various periods in vitro, and with varied medium osmotic pressure (OP), Na+, and Ca2+ concentrations. Prolactin (PRL) cells were markedly activated by 18 hr, and after 7 or 14 days were almost totally degranulated, with massive arrays of Golgi and RER. Reduction in OP, but not Na+ or Ca2+, caused an additional activation of PRL cells after periods of 18 hr or longer. Corticotroph (ACTH) cells became noticeably activated by 4 hr, and were possibly affected by OP, but not Na+ or Ca2+. Growth hormone (GH) cells were activated by 6 hr, and after 18 hr were quite degranulated with extensive arrays of RER. OP had no effect on GH cells before 3 days, when reduced OP appeared to cause an additional activation, with the appearance of large irregular secretory granule (SG)-like inclusions. Na+ and Ca2+ again had no effect. Gonadotrophic (GtH) cells appeared to be little affected by in vitro incubation; however, the very active cells from vitellogenic fish underwent a reduction in dilated RER after prolonged culture. Thyrotrophic (TSH) cells gradually became activated in vitro, but the response again varied with the sexual condition of the fish. Neither GtH nor TSH cells were affected by OP, Na+, or Ca2+. The findings are discussed in relation to hypothalamic control, via releasing/inhibiting factors, of adenohypophysial cell activity. PMID:6309607

  12. Steady States and Dynamics of Urokinase-Mediated Plasmin Activation In Silico and In Vitro

    PubMed Central

    Venkatraman, Lakshmi; Li, Huipeng; Dewey, C. Forbes; White, Jacob K.; Bhowmick, Sourav S.; Yu, Hanry; Tucker-Kellogg, Lisa

    2011-01-01

    Plasmin (PLS) and urokinase-type plasminogen activator (UPA) are ubiquitous proteases that regulate the extracellular environment. Although they are secreted in inactive forms, they can activate each other through proteolytic cleavage. This mutual interplay creates the potential for complex dynamics, which we investigated using mathematical modeling and in vitro experiments. We constructed ordinary differential equations to model the conversion of precursor plasminogen into active PLS, and precursor urokinase (scUPA) into active urokinase (tcUPA). Although neither PLS nor UPA exhibits allosteric cooperativity, modeling showed that cooperativity occurred at the system level because of substrate competition. Computational simulations and bifurcation analysis predicted that the system would be bistable over a range of parameters for cooperativity and positive feedback. Cell-free experiments with recombinant proteins tested key predictions of the model. PLS activation in response to scUPA stimulus was found to be cooperative in vitro. Finally, bistability was demonstrated in vitro by the presence of two significantly different steady-state levels of PLS activation for the same levels of stimulus. We conclude that ultrasensitive, bistable activation of UPA-PLS is possible in the presence of substrate competition. An ultrasensitive threshold for activation of PLS and UPA would have ramifications for normal and disease processes, including angiogenesis, metastasis, wound healing, and fibrosis. PMID:22004735

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

    PubMed Central

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

    2014-01-01

    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

  14. Botulinum Toxin Suppression of CNS Network Activity In Vitro

    PubMed Central

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

    2014-01-01

    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

  15. In vitro antibacterial activity of some plant essential oils

    PubMed Central

    Prabuseenivasan, Seenivasan; Jayakumar, Manickkam; Ignacimuthu, Savarimuthu

    2006-01-01

    Background: To evaluate the antibacterial activity of 21 plant essential oils against six bacterial species. Methods: The selected essential oils were screened against four gram-negative bacteria (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Proteus vulgaris) and two gram-positive bacteria Bacillus subtilis and Staphylococcus aureus at four different concentrations (1:1, 1:5, 1:10 and 1:20) using disc diffusion method. The MIC of the active essential oils were tested using two fold agar dilution method at concentrations ranging from 0.2 to 25.6 mg/ml. Results: Out of 21 essential oils tested, 19 oils showed antibacterial activity against one or more strains. Cinnamon, clove, geranium, lemon, lime, orange and rosemary oils exhibited significant inhibitory effect. Cinnamon oil showed promising inhibitory activity even at low concentration, whereas aniseed, eucalyptus and camphor oils were least active against the tested bacteria. In general, B. subtilis was the most susceptible. On the other hand, K. pneumoniae exhibited low degree of sensitivity. Conclusion: Majority of the oils showed antibacterial activity against the tested strains. However Cinnamon, clove and lime oils were found to be inhibiting both gram-positive and gram-negative bacteria. Cinnamon oil can be a good source of antibacterial agents. PMID:17134518

  16. In vitro activities of four xyloglucan endotransglycosylases from Arabidopsis

    NASA Technical Reports Server (NTRS)

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

    1999-01-01

    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.

  17. 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...

  18. 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...

  19. In vitro activities of streptomycin and 11 oral antimicrobial agents against clinical isolates of Klebsiella rhinoscleromatis.

    PubMed Central

    Perkins, B A; Hamill, R J; Musher, D M; O'Hara, C

    1992-01-01

    We tested in vitro the activities of streptomycin and tetracycline--antibiotics that have long been used to treat rhinoscleroma--as well as several newer oral agents by using 23 isolates of the causative organism Klebsiella rhinoscleromatis. All isolates were inhibited by clinically achievable concentrations of trimethoprim-sulfamethoxazole, amoxicillin-clavulanate, chloramphenicol, ciprofloxacin, cephalexin, cefuroxime, and cefpodoxime. PMID:1416867

  20. Polyphenols in Chocolate, Which Have Antioxidant Activity, Modulate Immune Functions in Humans in Vitro

    Microsoft Academic Search

    Chiaki Sanbongi; Noboru Suzuki; Tsuyoshi Sakane

    1997-01-01

    We studied the effects of antioxidants from chocolate, cacao liquor polyphenol (CLP), on human immune functionsin vitro.CLP is an enriched polyphenol fraction purified from cacao liquor that is a major component of chocolate. It has been shown that polyphenols have antioxidant activity, and reactive oxygen species (ROS) are involved in immune responses. CLP inhibited both hydrogen peroxide and superoxide anion,

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

    Microsoft Academic Search

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

    2002-01-01

    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

  2. Guarana ( Paullinia cupana): toxic behavioral effects in laboratory animals and antioxidant activity in vitro

    Microsoft Academic Search

    R Mattei; R. F Dias; E. B Esp??nola; E. A Carlini; S. B. M Barros

    1998-01-01

    The effects on toxic and behavioral levels of guarana (Paullinia cupana) were assessed in rats and mice subsequent to acute and chronic administrations and were compared to those produced by Ginseng (Panax ginseng). Experimental parameters included tests for antioxidant capacity in vitro and measured in vivo, toxicological screening, progress in weight, motor activity, death rate, and histopathological examination of the

  3. Estrogenic Activity Assessment of Environmental Chemicals Using in Vitro Assays: Identification of Two New Estrogenic Compounds

    Microsoft Academic Search

    Isabelle Lascombe; Dominique Beffa; Urs Rüegg; Joseph Tarradellas; Walter Wahli

    Environmental chemicals with estrogenic activities have been suggested to be associated with deleterious effects in animals and humans. To characterize estrogenic chemicals and their mecha- nisms of action, we established in vitro and cell culture assays that detect human estrogen recep- tor ? (hER?)-mediated estrogenicity. First, we assayed chemicals to determine their ability to modulate direct interaction between the hER?

  4. In Vitro Activities of Eight Antifungal Drugs against 104 Environmental and Clinical Isolates of Aureobasidium pullulans

    PubMed Central

    Najafzadeh, M. Javad; Sutton, Deanna A.; Keisari, M. Saradeghi; Zarrinfar, H.; de Hoog, G. Sybren; Chowdhary, Anuradha

    2014-01-01

    Aureobasidium pullulans is an unusual agent of phaeohyphomycosis. The in vitro activities of antifungals against 104 isolates of Aureobasidium pullulans var. pullulans and A. pullulans var. melanigenum revealed low MIC90s of amphotericin B, posaconazole, and itraconazole. However, they were resistant to fluconazole (?64 ?g/ml) and had high MICs of voriconazole, isavuconazole, caspofungin, and micafungin. PMID:25001309

  5. In Vitro Antimalarial Activity of Different Inhibitors of the Plasmodial Isoprenoid Synthesis Pathway.

    PubMed

    da Silva, Marcia F; Saito, Alexandre Y; Peres, Valnice J; Oliveira, Antonio C; Katzin, Alejandro M

    2015-08-01

    Previous studies have shown that fosmidomycin, risedronate, and nerolidol exert antimalarial activity in vitro. We included squalestatin, an inhibitor of the isoprenoid metabolism in Erwinia uredovora, and found that combinations of compounds which act on different targets of the plasmodial isoprenoid pathway possess important supra-additivity effects. PMID:26055383

  6. In Vitro Activities of Voriconazole in Combination with Three Other Antifungal Agents against Candida glabrata

    Microsoft Academic Search

    Francesco Barchiesi; Elisabetta Spreghini; Monia Maracci; Annette W. Fothergill; Isabella Baldassarri; Michael G. Rinaldi; Giorgio Scalise

    2004-01-01

    Candida glabrata has recently emerged as a significant pathogen involved in both superficial and deep-seated infections. In the present study, a checkerboard broth microdilution method was performed to investigate the in vitro activities of voriconazole (VOR) in combination with terbinafine (TRB), amphotericin B (AMB), and flucytosine (5FC) against 20 clinical isolates of C. glabrata. Synergy, defined as a fractional inhibitory

  7. Effects of sucrose on photosynthesis and phosphoenolpyruvate carboxylase activity of in vitro cultured strawberry plantlets

    Microsoft Academic Search

    Chafik Hdider; Yves Desjardins

    1994-01-01

    Photosynthesis and phosphoenolpyruvate carboxylase activity were investigated in 5, 10 and 28 day-old micropropagated strawberry plantlets (Fragaria x ananassa Duch. cv Kent) rooted in vitro with different levels of sucrose (0, 1, 3 and 5%) on cellulose plugs (Sorbarods). The photosynthetic capability was influenced by the level of sucrose in the culture medium with the largest rates of photosynthesis corresponding

  8. Comparison of relative antioxidant activities of British medicinal plant species in vitro

    Microsoft Academic Search

    David Mantle; Fadel Eddeb; Anne T. Pickering

    2000-01-01

    We have determined the relative levels of endogenous antioxidant activity in a range of British medicinal plant species (representative of a variety of plant families, selected on the basis of their widespread use in traditional herbal medicine), via competitive scavenging of the ABTS+ or O2? radicals in vitro. A number of plant species with appreciable levels (i.e. greater than or

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

    Microsoft Academic Search

    Cailean Clarkson; Vinesh J. Maharaj; Neil R. Crouch; O GRACE; Pamisha Pillay; Motlalepula G. Matsabisa; Niresh Bhagwandin; Peter J. Smith; Peter I. Folb

    2004-01-01

    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

  10. Immunosuppressive Activity of Bovine Follicular Fluid on Bovine T Lymphocytes In Vitro1

    Microsoft Academic Search

    H. A. Fahmi; A. G. Hunter; R. J. F. Markham; B. E. Seguin

    1985-01-01

    Follicular fluid from bovine follicles at various stages of the estrous cycle and cysts were tested in vitro for immuno- suppressive activity. Mitogen-stimulated lymphocyte assays and the mixed lymphocyte reaction were used as test procedures and thymidine uptake was monitored. Follicular fluid and cyst fluid inhibited the deoxyribonucleic acid syn- thesis response of bovine lymphocytes to mitogenic and antigenic stimulation.

  11. Activity of Porphyridium sp. polysaccharide against herpes simplex viruses in vitro and in vivo

    Microsoft Academic Search

    Mahmoud Huheihel; Vladimir Ishanu; Jacov Tal

    2002-01-01

    The cell wall sulfated polysaccharide of the red microalga Porphyridium sp. exhibited impressive antiviral activity against herpes simplex virus types 1 and 2 (HSV-1 and -2) both in vitro (cell culture) and in vivo (rats and rabbits). Depending on the concentration, this polysaccharide completely inhibited or slowed down the development of the cytopathic effect in HSV-infected cells, but did not

  12. In vivo anti-inflammatory and in vitro antioxidant activities of Mediterranean dietary plants

    Microsoft Academic Search

    Filomena Conforti; Silvio Sosa; Mariangela Marrelli; Federica Menichini; Giancarlo A. Statti; Dimitar Uzunov; Aurelia Tubaro; Francesco Menichini; Roberto Della Loggia

    2008-01-01

    Five hydroalcoholic extracts of edible plants from Calabria region (Italy) used in local traditional medicine for the treatment of inflammatory diseases were evaluated for their in vivo topical anti-inflammatory activity (inhibition of croton oil-induced ear oedema in mice) and in vitro antioxidant and antiradical properties (inhibition of linoleic acid oxidation and bovine brain liposomes peroxidation, DPPH radical scavenging). All the

  13. 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 ...

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

    Microsoft Academic Search

    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

    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

  15. In vitro Activities of Caspofungin, Amphotericin B and Azoles Against Coccidioides posadasii Strains from Northeast, Brazil

    Microsoft Academic Search

    R. A. Cordeiro; R. S. N. Brilhante; M. F. G. Rocha; M. A. B. Fechine; A. K. F. Costa; Z. P. Camargo; J. J. C. Sidrim

    2006-01-01

    Coccidioidomycosis is a systemic infection caused by the soil-dwelling dimorphic fungi Coccidioides spp. The disease is endemic in semiarid Northeast Brazil, where it is caused by C. posadasii. The aim of this study was to perform antifungal susceptibility tests of clinical and environmental strains of C. posadasii from Northeast Brazil. The in vitro activities of caspofungin, amphotericin B and azoles

  16. In Vitro and In Vivo Activities of Nitazoxanide against Clostridium difficile

    Microsoft Academic Search

    CATHERINE S. MCVAY; RIAL D. ROLFE

    2000-01-01

    We have used the hamster model of antibiotic-induced Clostridium difficile intestinal disease to evaluate nitazoxanide (NTZ), a nitrothiazole benzamide antimicrobial agent. The following in vitro and in vivo activities of NTZ in the adult hamster were examined and compared to those of metronidazole and vancomycin: (i) MICs and minimum bactericidal concentrations (MBCs) against C. difficile, (ii) toxicity, (iii) ability to

  17. In vitro activity of amphotericin B, flucytosine and fluconazole against yeasts causing bloodstream infections

    Microsoft Academic Search

    J. Berenguer; V. Fernández-Baca; R. Sánchez; E. Bouza

    1995-01-01

    The in vitro activity of amphotericin B, flucytosine and fluconazole against 95 yeasts causing fungemia in a single institution over the last eight years was determined by a broth macromethod recommended by the National Committee for Clinical Laboratory Standards. All strains were inhibited by amphotericin B concentrations of ? 1 µg\\/ml. With flucytosine in most species the MIC50 was between

  18. In Vitro Activities of 25 Quinolones and Fluoroquinolones against Liver and Blood Stage Plasmodium spp

    Microsoft Academic Search

    Nassira Mahmoudi; Liliane Ciceron; Jean-Francois Franetich; Khemais Farhati; Olivier Silvie; Wijnand Eling; Robert Sauerwein; Martin Danis; Dominique Mazier; Francis Derouin

    2003-01-01

    The in vitro activities of 25 quinolones and fluoroquinolones against erythrocytic stages of Plasmodium falciparum and against liver stages of Plasmodium yoelii yoelii and P. falciparum were studied. All compounds were inhibitory for chloroquine-sensitive and chloroquine-resistant P. falciparum grown in red blood cells. This inhibitory effect increased with prolonged incubation and according to the logarithm of the drug concentration. Grepafloxacin,

  19. In vitro and in vivo Antiplasmodial Activity of Momordica balsamina Alone or in a Traditional Mixture

    Microsoft Academic Search

    F. Benoit-Vical; P. Grellier; A. Abdoulaye; I. Moussa; A. Ousmane; A. Berry; K. Ikhiri; C. Poupat

    2006-01-01

    Background: Because of the dramatic situation of malaria in Africa, there is an urgent need to find new and cheap drugs, such as herbal medicines. Here we report the study of the in vitro and in vivo antimalarial activity of Momordica balsamina alone or in a traditional mixture used in Niger. Methods: Extracts were obtained with different solvents and tested

  20. In vitro Antifungal Activity of Limonene against Trichophyton rubrum

    PubMed Central

    Kim, Hoon; Lee, Min Hee

    2009-01-01

    In this study, the antifungal activities of limonene against Trichophyton rubrum were evaluated via broth microdilution and vapor contact assays. In both assays, limonene was shown to exert a potent antifungal effect against T. rubrum. The volatile vapor of limonene at concentrations above 1 µl/800 ml air space strongly inhibited the growth of T. rubrum. The MIC value was 0.5% v/v in the broth microdilution assay. The antifungal activity of limonene against T. rubrum was characterized as a fungicidal effect. PMID:23983542

  1. In vitro anti-MRSA activity of carvone with gentamicin.

    PubMed

    Mun, Su-Hyun; Kang, Ok-Hwa; Joung, Dae-Ki; Kim, Sung-Bae; Choi, Jang-Gi; Shin, Dong-Won; Kwon, Dong-Yeul

    2014-04-01

    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

  2. In vitro anti-MRSA activity of carvone with gentamicin

    PubMed Central

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

    2014-01-01

    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

  3. In vitro antimicrobial activity of mangrove plant Sonneratia alba

    PubMed Central

    Saad, Shahbudin; Taher, Muhammad; Susanti, Deny; Qaralleh, Haitham; Awang, Anis Fadhlina Izyani Bt

    2012-01-01

    Objective To investigate the antimicrobial property of mangrove plant Sonneratia alba (S. alba). Methods The antimicrobial activity was evaluated using disc diffusion and microdilution methods against six microorganisms. Soxhlet apparatus was used for extraction with a series of solvents, n-hexane, ethyl acetate and methanol in sequence of increasing polarity. Results Methanol extract appeared to be the most effective extract while n-hexane extract showed no activity. The antimicrobial activities were observed against the gram positive bacteria Staphylococcus aureus (S. aureus) and Bacillus cereus (B. cereus), the gram negative Escherichia coli (E. coli) and the yeast Cryptococcus neoformans. Pseudomonas aeruginosa and Candida albicans appeared to be not sensitive to the concentrations tested since no inhibition zone was observed. E. coli (17.5 mm) appeared to be the most sensitive strain followed by S. aureus (12.5 mm) and B. cereus (12.5 mm). Conclusions From this study, it can be concluded that S. alba exhibits antimicrobial activities against certain microorganisms. PMID:23569943

  4. In vitro TRPV1 activity of piperine derived amides

    Microsoft Academic Search

    Edwin Andrés Correa; Edward D. Högestätt; Olov Sterner; Fernando Echeverri; Peter M. Zygmunt

    2010-01-01

    A series of natural and synthetic piperine amides were evaluated for activity on the human TRPV1 expressed in HEK293 cells. The agonistic effect of piperine amides was mainly dependent on the length of the carbon chain. Structural changes of double bonds and stereochemistry in the aliphatic chain of these compounds did not change their potency or efficacy, indicating that increased

  5. Perflubron attenuates neutrophil adhesion to activated endothelial cells in vitro.

    PubMed

    Woods, C M; Neslund, G; Kornbrust, E; Flaim, S F

    2000-05-01

    Infiltration of activated neutrophils into the lung appears to be a key element in the severe lung injury that develops in animal models of acute lung injury. Partial liquid ventilation with perflubron has been shown to ameliorate tissue damage compared with conventional mechanical ventilation in acute lung injury models. Pilot experiments indicated that indirect exposure to perflubron could modulate the degree to which subsequent neutrophil binding to endothelial cell monolayers was upregulated after lipopolysaccharide activation. Endothelial cell monolayers preexposed to perflubron showed >40% reductions in the surface steady-state levels of E-selectin and intercellular adhesion molecule-1 achieved after proinflammatory activation (P < 0.05), which correlated with a reduction in the real-time association constants measured by biosensor techniques. These results indicate that direct contact with the perflubron liquid phase is not necessary to attenuate inflammatory responses. Rather, diffusion of perflubron from the alveolar space into the adjacent pulmonary vascular endothelial layer may modulate neutrophil adhesion and thereby reduce the rate of infiltration of activated neutrophils into the injured lung. PMID:10781432

  6. Inhibition of catalase activity in vitro by diesel exhaust particles

    SciTech Connect

    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

    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.

  7. In Vitro Activity of Netilmicin Compared with Gentamicin, Tobramycin, Amikacin, and Kanamycin

    PubMed Central

    Eickhoff, Theodore C.; Ehret, Josephine M.

    1977-01-01

    The in vitro activity of netilmicin was compared with that of gentamicin, tobramycin, amikacin, and kanamycin against 636 strains of bacteria recently isolated from clinical sources. Gentamicin was the most active antibiotic, but netilmicin and tobramycin closely paralleled it. Netilmicin was generally four-to eightfold less active than gentamicin against Serratia and group A streptococci, and was twofold less active against Pseudomonas aeruginosa. When effects of inoculum size and concentration of divalent cations in the media were evaluated, netilmicin was shown to be similar to gentamicin in vitro. Minimum inhibitory concentrations for P. aeruginosa were increased as much as 18-fold when the Mg2+ and Ca2+ concentrations were increased to physiological levels in Mueller-Hinton broth. PMID:879733

  8. Natural killer cell activity and lymphocyte activation: Investigating the effects of a selection of essential oils and components in vitro

    Microsoft Academic Search

    M. D. Standen; Paul A Connellan; David N Leach

    2006-01-01

    A selection of essential oils and components were tested in vitro for potential immunomodulating effects on natural killer cell activity (NKCA) and lymphocyte activation through CD69 expression.\\u000aMatricaria recutita, Boswellia carteri, Pelargonium graveolens, Lavandula angustifolia, Citrus limon, Melaleuca alternifolia, Melaleuca viridiflora, Santalum spicatum, Cedrus atlantica, and Thymus vulgaris ct. linalool essential oils were solubilised with ethanol and methylated â-cyclodextrin 1:5:25

  9. In Vitro Activity of TR700, the Active Ingredient of the Antibacterial Prodrug TR701, against Linezolid-Resistant Strains

    Microsoft Academic Search

    K. J. Shaw; S. Poppe; R. Schaadt; V. Brown-Driver; J. Finn; C. M. Pillar; D. Shinabarger; G. Zurenko

    2008-01-01

    TR-701 is the orally active prodrug of TR-700, a novel oxazolidinone that demonstrates four- to eightfold- greater activity than linezolid (LZD) against Staphylococcus and Enterococcus spp. In this study evaluating the in vitro sensitivity of LZD-resistant isolates, TR-700 demonstrated 8- to 16-fold-greater potency than LZD against all strains tested, including methicillin-resistant Staphylococcus aureus (MRSA), strains of MRSA carrying the mobile

  10. In Vitro and In Vivo Antibacterial Activities of BO2727, a New Carbapenem

    Microsoft Academic Search

    YOSHINARI ASAHI; SHUICHI MIYAZAKI; ANDKEIZO YAMAGUCHI

    1995-01-01

    BO-2727, a new injectable carbapenem, was evaluated for its in vitro and in vivo antibacterial activities in comparison with those of biapenem, meropenem, imipenem, cefpirome, and ceftazidime. BO-2727 had activity comparable to that of imipenem against methicillin-susceptible staphylococci and streptococci, with MICs at which 90% of strains tested (MIC90s) are inhibited being equal to 0.5 mg\\/ml or less. Against methicillin-

  11. In Vitro Anti-Helicobacter pylori Activities of New Rifamycin Derivatives, KRM-1648 and KRM-1657

    Microsoft Academic Search

    JUNKO K. AKADA; MUTSUNORI SHIRAI; KENJI FUJII; KIWAMU OKITA; TERUKO NAKAZAWA

    1999-01-01

    The new rifamycin derivatives KRM-1657 and KRM-1648 were evaluated for their in vitro antimicrobial activities against 44 strains of Helicobacter pylori. Although the drugs were not very active against other gram-negative bacteria, the MICs at which 90% of isolates are inhibited for these drugs were lower (0.002 and 0.008 mg\\/ml, respectively) than those of amoxicillin and rifampin for H. pylori.

  12. In vitro evaluation of the cytotoxic, hemolytic and clastogenic activities of Rhizostoma pulmo toxin(s).

    PubMed

    Allavena, A; Mariottini, G L; Carli, A M; Contini, S; Martelli, A

    1998-06-01

    Cytotoxic, hemolytic and clastogenic activities of Rhizostoma pulmo toxin(s) contained in the jelly tissue free of nematocysts were investigated in mammalian cells with in vitro procedures. At the concentration of 37.6 microg/ml the tissue protein produced the death of 50% V79 cells; a similar potency was observed in terms of hemolytic activity. The toxin(s) was not clastogenic for human lymphocytes in culture at the concentration of 5 microg/ml. PMID:9663699

  13. Inhibitory effect of oestradiol on activation of rat hepatic stellate cells in vivo and in vitro

    Microsoft Academic Search

    I Shimizu; Y Mizobuchi; M Yasuda; M Shiba; Y-R Ma; T Horie; F Liu; S Ito

    1999-01-01

    BackgroundHepatic stellate cells play a key role in the pathogenesis of hepatic fibrosis.AimsTo examine the inhibitory effect of oestradiol on stellate cell activation.MethodsIn vivo, hepatic fibrosis was induced in rats by dimethylnitrosamine or pig serum. In vitro, rat stellate cells were activated by contact with plastic dishes resulting in their transformation into myofibroblast-like cells.ResultsIn the dimethylnitrosamine and pig serum models,

  14. In Vitro Activity of LY333328, an Investigational Glycopeptide Antibiotic, against Enterococci and Staphylococci

    Microsoft Academic Search

    RICHARD S. SCHWALBE; ANGELA C. MCINTOSH; SADAF QAIYUMI; JUDITH A. JOHNSON; ROBERT J. JOHNSON; KATHLEEN M. FURNESS; WILLIAM J. HOLLOWAY

    1996-01-01

    The in vitro activities of LY333328 were compared with those of vancomycin, teicoplanin, and quinupristin- dalfopristin (Synercid) against 219 strains of enterococci and staphylococci, including vancomycin-resistant enterococci and methicillin-resistantStaphylococcus aureus. MICs and MBCs were determined by a microtiter dilution protocol. LY333328 demonstrated superior activity against vancomycin-resistant enterococci and was the only antibiotic which was bactericidal. Its potency was comparable or

  15. Can pharmaceuticals interfere with the synthesis of active androgens in male fish? An in vitro study

    Microsoft Academic Search

    Denise Fernandes; Sabine Schnell; Cinta Porte

    2011-01-01

    The in vitro interference of fibrate (gemfibrozil, clofibrate, clofibric acid), anti-inflammatory (ibuprofen, diclofenac), and anti-depressive (fluoxetine, fluvoxamine) drugs with key enzymatic activities—C17,20-lyase and CYP11?-involved in the synthesis of active androgens in gonads of male carp have been investigated. Among the tested compounds, fluvoxamine and fluoxetine were the strongest inhibitors of C17,20-lyase and CYP11? enzymes, with IC50s in the range of

  16. Effect of Low Dose Gamma Irradiation together with Lipid A on Human Leukocytes Activities In Vitro

    NASA Astrophysics Data System (ADS)

    Belyakova, E.; Dubnickova, M.; Boreyko, A.

    2010-01-01

    The influence of gamma irradiation and of Lipid A from Escherichia coli on phagocytosis, lyzosyme and peroxidase activities of human leukocytes, in vitro was investigated. Leukocytes samples were irradiated with 1 and 5 Gy, respectively. The number of irradiated leukocytes was decreased in the irradiated samples. Only samples with additive Lipid A were not damaged by irradiation. The Lipid A had positive influence on biological activities of the irradiated leukocytes.

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

    Microsoft Academic Search

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

    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

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

    Microsoft Academic Search

    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

    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

  19. In vitro antimicrobial activity of Achyranthes coynei Sant.

    PubMed Central

    Ankad, Gireesh; Upadhya, Vinayak; Pai, Sandeep R.; Hegde, Harsha V.; Roy, Subarna

    2013-01-01

    Objective To validate the traditional use of Achyranthes coynei (A. coynei) Sant. as an antimicrobial in treatment of various infectious diseases. Methods Leaf extracts of A. coynei obtained through successive solvent extraction using petroleum ether, dichrloromethane, chloroform and methanol were used to screen the antimicrobial activity on five Gram positive, five Gram negative bacteria and two fungi. Minimum inhibitory concentration (MIC) was determined by two fold tube-dilution method. Results Methanolic leaf extract was more effective than other three extracts on the tested bacteria. Methanolic extract was efficient on Staphylococcus epidermis, Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa with MIC values (0.62±0.00) mg/mL. The fungal organisms were less susceptible against extracts tested. Conclusions These results support the traditional use of leaf extracts of A. coynei as they have antimicrobial potential. Further studies are needed for establishing safety, toxicity and pharmacological activity with phytochemical investigation.

  20. In vitro leishmanicidal activity of Tityus discrepans scorpion venom

    Microsoft Academic Search

    Adolfo Borges; Sylvia Silva; Elena Velasco; Marco Alvarez; Marcelo J. M. Alfonzo; Alicia Jorquera; Leonardo De Sousa; Olinda Delgado

    2006-01-01

    Leishmania parasites are sensitive to peptides with antimicrobial and ion-channel inhibitory activity. Because scorpion venoms are rich sources of such peptides, the leishmanicidal effect of Tityus discrepans venom was investigated. A negative correlation between cell growth and venom concentration was observed for venom-treated cultures of Leishmania (L.) mexicana mexicana promastigotes; 50% growth inhibition was obtained at 0.4 ?g\\/ml. Light microscopy showed

  1. Anti-invasive activity of alkaloids and polyphenolics in vitro

    Microsoft Academic Search

    Virinder S. Parmar; Marc E. Bracke; Jan Philippe; Jesper Wengel; Subhash C. Jain; Carl E. Olsen; Kirpal S. Bisht; Nawal K. Sharma; Andy Courtens; Sunil K. Sharma; Krist'l Vennekens; Veerle Van Marck; Sanjay K. Singh; Naresh Kumar; Ajay Kumar; Sanjay Malhotra; Rajesh Kumar; Vivek K. Rajwanshi; Rajni Jain; Marc M. Mareel

    1997-01-01

    Invasiveness, the ability of certain tumour cells to migrate beyond their natural tissue boundaries, often leads to metastasis, and usually determines the fatal outcome of cancer. The need for anti-invasive agents has led us to search for possibly active compounds among alkaloids and polyphenolics. One hundred compounds were screened in an assay based on the confrontation of invasive human MCF-7\\/6

  2. In vitro antibacterial activity of some plant essential oils

    Microsoft Academic Search

    Seenivasan Prabuseenivasan; Manickkam Jayakumar; Savarimuthu Ignacimuthu

    2006-01-01

    BACKGROUND:: To evaluate the antibacterial activity of 21 plant essential oils against six bacterial species. METHODS:: The selected essential oils were screened against four gram-negative bacteria (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Proteus vulgaris) and two gram-positive bacteria Bacillus subtilis and Staphylococcus aureus at four different concentrations (1:1, 1:5, 1:10 and 1:20) using disc diffusion method. The MIC of the

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

    PubMed

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

    2012-01-01

    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

  4. In vitro antioxidant and antiproliferative activities of nine Salvia species.

    PubMed

    Loizzo, Monica Rosa; Abouali, Morteza; Salehi, Peyman; Sonboli, Ali; Kanani, Mohammad; Menichini, Francesco; Tundis, Rosa

    2014-01-01

    Supported by a growing increase of scientific research attesting the health properties of salvia species, we have decided to investigate nine Salvia namely Salvia sclarea, Salvia atropatana, Salvia sahendica, Salvia hydrangea, Salvia xanthocheila, Salvia macrosiphon, Salvia glutinosa, Salvia chloroleuca and Salvia ceratophylla species for their antioxidant and antiproliferative activities. In order to correlate the bioactivity with their phytochemical content, the total phenol and total flavonoid contents were also determined. S. ceratophylla exhibited the strongest activity against C32 cells with an IC50 value of 20.8 ?g mL(- 1), while S. glutinosa exhibited an IC50 value of 29.5 ?g mL(- 1) against ACHN cell line. Interestingly, S. glutinosa displayed also the highest DPPH radical-scavenging activity with an IC50 of 3.2 ?g mL(- 1). These species are characterised by the highest total phenol and flavonoid contents. The obtained results suggest that Salvia species are healthy plant foods. PMID:25039830

  5. Urokinase-type plasminogen activator does not affect in vitro bovine embryo development and quality.

    PubMed

    Krania, Fotini; Dovolou, Eleni; Rekkas, Constantinos A; Heras, Sonia; Pappas, Ioannis; Soom, Ann Van; Amiridis, Georgios S

    2015-06-01

    The effects of modification of the in vitro embryo culture media (IVC) with the addition of urokinase-type plasminogen activator (u-PA) on the yield and/or quality of bovine embryos were examined in two experiments. In Experiment 1, denuded embryos were cultured in semi-defined synthetic oviductal fluid (SOF) for seven days, while in Experiment 2 embryos were co-cultured with cumulus cell monolayer in a serum-containing SOF medium. Plasminogen activator activity (PAA) and plasminogen activator inhibition (PAI) were determined in all spent IVC media. At the activity used (5 IU/ml), u-PA had no effect either on in vitro embryo production rates or on embryo quality as revealed by gene expression analysis of 10 important mRNA transcripts related to apoptosis, oxidation, implantation and metabolism. PAA and PAI analysis indicated the need for wellbalanced plasminogen activators and inhibitors as a culture environment for embryo development. However, more research is needed to unveil the mechanism by which u-PA is involved in in vitro embryo production systems. PMID:26051263

  6. Activation of complement pathways in xenotransplantation: an in vitro study.

    PubMed

    Walpen, Alexander J; Mohacsi, Paul; Frey, Caroline; Roos, Anja; Daha, Mohamed R; Rieben, Robert

    2002-05-01

    Pig-to-human xenotransplantation faces the problem of hyperacute graft rejection due to the presence of human naturally occurring antibodies against the disaccharide Galalpha1-3Gal (anti-Gal antibodies) expressed on pig endothelium. Antibody-mediated complement activation is usually referred to as classical pathway activation. In this study we examined if the alternative complement pathway is also directly activated through anti-Gal antibodies or if the classical pathway is indispensable. We therefore developed a hemolysis test with rabbit erythrocytes (E), which have an activating surface for the alternative complement pathway and express abundant amounts of Galalpha1-3Gal, and used this assay in addition to the standard complement tests CH50 and AP50. In this rabbit E CH50 (RECH50) assay we were able to study activation of both major complement pathways simultaneously. FACS analysis was used to trace complement and antibody deposition on rabbit E. Anti-Gal depletion of human serum by immunoabsorption revealed a 65% reduction of rabbit E hemolysis in the RECH50 test (value before absorption: 28 +/- 5.8, after absorption: 9.9 +/- 2.8, P<0.001), but only a 35% reduction of lysis in the AP50 test (AP50 before 11.3 +/- 2.1, after 7.4 +/- 2.0, P<0.002). Repletion with purified anti-Gal fully restored hemolysis in both assays. Serum depleted of Clq showed a reduced lysis of rabbit E as compared to normal human serum; this effect increased with higher serum dilutions. The reciprocal picture, i.e. less effect on hemolysis with increasing dilution, was seen with factor D depleted serum. Comparison of the RECH50 values with the AP50 values revealed an 8.4-fold increase of lysis in the RECH50 test, in which both complement pathways are running. By FACS analysis, complement deposition on rabbit E was determined and components of the classical pathway were found, especially in sera where the alternative pathway was disrupted. We conclude that in our model anti-Gal induce lysis via both classical and alternative complement pathways, but that the alternative pathway activation is of minor importance. In addition, we saw that with higher serum dilutions, the classical pathway (i.e. anti-Gal-mediated lysis) takes a predominant role in lysing the rabbit E. As anti-Gal-mediated activation of the alternative complement cascade seems of minor importance based on our results, and as there are only few surfaces in transplanted organs that would favor the alternative pathway to be executed, the specific inhibition of early steps of the classical pathway appears as a realistic strategy in pig-to-primate xenotransplantation that-to the benefit of the patient-leaves the mainly anti-bacterial defense by the alternative pathway intact. PMID:12180841

  7. 2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro.

    PubMed

    ?ezní?ková, Eva; Popa, Alexandr; Gucký, Tomáš; Zatloukal, Marek; Havlí?ek, Libor; Bazgier, Václav; Berka, Karel; Jorda, Radek; Popa, Igor; Nasereddin, Abdelmajeed; Jaffe, Charles L; Kryštof, Vladimír; Strnad, Miroslav

    2015-06-01

    Here we describe the leishmanicidal activities of a library of 2,6,9-trisubstituted purines that were screened for interaction with Cdc2-related protein kinase 3 (CRK3) and subsequently for activity against parasitic Leishmania species. The most active compound inhibited recombinant CRK3 with an IC50 value of 162nM and was active against Leishmania major and Leishmania donovani at low micromolar concentrations in vitro. Its mode of binding to CRK3 was investigated by molecular docking using a homology model. PMID:25937014

  8. Impact of Bacterial Biofilm Formation on In Vitro and In Vivo Activities of Antibiotics

    PubMed Central

    Schwank, Silvia; Rajacic, Zarko; Zimmerli, Werner; Blaser, Jürg

    1998-01-01

    The impact of bacterial adherence on antibiotic activity was analyzed with two isogenic strains of Staphylococcus epidermidis that differ in the features of their in vitro biofilm formation. The eradication of bacteria adhering to glass beads by amikacin, levofloxacin, rifampin, or teicoplanin was studied in an animal model and in a pharmacokinetically matched in vitro model. The features of S. epidermidis RP62A that allowed it to grow on surfaces in multiple layers promoted phenotypic resistance to antibiotic treatment, whereas strain M7 failed to accumulate, despite initial adherence on surfaces and growth in suspension similar to those for RP62A. Biofilms of S. epidermidis M7 were better eradicated than those of strain RP62A in vitro (46 versus 31%; P < 0.05) as well as in the animal model (39 versus 9%; P < 0.01). PMID:9559803

  9. Impact of bacterial biofilm formation on in vitro and in vivo activities of antibiotics.

    PubMed

    Schwank, S; Rajacic, Z; Zimmerli, W; Blaser, J

    1998-04-01

    The impact of bacterial adherence on antibiotic activity was analyzed with two isogenic strains of Staphylococcus epidermidis that differ in the features of their in vitro biofilm formation. The eradication of bacteria adhering to glass beads by amikacin, levofloxacin, rifampin, or teicoplanin was studied in an animal model and in a pharmacokinetically matched in vitro model. The features of S. epidermidis RP62A that allowed it to grow on surfaces in multiple layers promoted phenotypic resistance to antibiotic treatment, whereas strain M7 failed to accumulate, despite initial adherence on surfaces and growth in suspension similar to those for RP62A. Biofilms of S. epidermidis M7 were better eradicated than those of strain RP62A in vitro (46 versus 31%; P < 0.05) as well as in the animal model (39 versus 9%; P < 0.01). PMID:9559803

  10. Similar activity of mecamylamine stereoisomers in vitro and in vivo

    PubMed Central

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

    2014-01-01

    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

  11. [In vitro study of the antimutagenic activity of alphahederin].

    PubMed

    Villani, P; Orsičre, T; Sari-Minodier, I; Bouvenot, G; Botta, A

    2001-01-01

    Authors have studied the antimutagenic power of alphahederin (a saponin extracted from Hedera helix) versus a clastogenic agent, doxorubicin and an aneugenic agent, carbendazim. We have applied a protocol of incorporation of alphahederin (pretreatment, simultaneous treatment and post treatment) to determine a mechanism of action. According to this protocol, alphahederin induces a significant diminution of the rate of micronuclei wathever the phases of the protocol. These results demonstrate the antimutagenic activity of alphahederin with a mechanism of action, both desmutagenic and bioantimutagenic. PMID:11397676

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

    PubMed Central

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

    2014-01-01

    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

  13. In vitro antimicrobial activity and biocompatibility of propolis containing nanohydroxyapatite.

    PubMed

    Grenho, L; Barros, J; Ferreira, C; Santos, V R; Monteiro, F J; Ferraz, M P; Cortes, M E

    2015-04-01

    The high number of biomaterial associated infections demands new strategies to prevent this problem. In this study the suitability of nanohydroxyapatite (nanoHA)-based surfaces containing two Brazilian extracts of propolis (green and red ones) to prevent bacterial growth and biofilm formation, as well as its non-cytotoxic nature, was investigated. Optical density, colony forming units and MTT reduction assay were used to assess the materials' antibacterial activity against planktonic and sessile growth of Staphylococcus aureus. NanoHA matrix was able to absorb both types of propolis and the obtained results revealed the antibacterial effectiveness of the novel materials expressed as the reduction of bacterial growth and biofilm formation ability. Additionally, cell culture tests showed the growth of fibroblasts with high metabolic activity and without membrane damage. Therefore, these nanoHA-based surfaces containing natural products deriving from bees may be a promising bioactive biomaterial to be further studied with the aim of application to orthopaedic or dental devices. PMID:25784672

  14. In vitro activity of Bay Y3118 against anaerobic bacteria.

    PubMed Central

    Wexler, H M; Molitoris, E; Finegold, S M

    1993-01-01

    The antimicrobial activity of a new quinolone, Bay Y3118, was determined against 326 strains of anaerobic bacteria and compared with the activities of ampicillin-sulbactam, cefotetan, clindamycin, imipenem, metronidazole, and sparfloxacin. The National Committee for Clinical Laboratory Standards-approved Wadsworth agar dilution technique with Brucella-laked blood agar was used throughout the study. Breakpoints used to determine the percent susceptible were 2 micrograms/ml for Bay Y3118 and sparfloxacin, 4 micrograms/ml for clindamycin, 8 micrograms/ml for imipenem, 16 micrograms/ml for metronidazole and ampicillin-sulbactam, and 32 micrograms/ml for cefotetan. Species tested included Bacteroides fragilis (57 strains), other B. fragilis group species (79 strains), Bacteroides gracilis (10 strains), other Bacteroides spp. (9 strains), Prevotella spp. (30 strains), Porphyromonas spp. (9 strains), Fusobacterium spp. (36 strains), Bilophila wadsworthia (14 strains), Clostridium spp. (36 strains), Peptostreptococcus spp. (20 strains), and gram-positive non-spore-forming rods (26 strains). Bay Y3118 inhibited all but 1 of 326 anaerobic bacteria tested at the breakpoint level or lower. PMID:8285647

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

    SciTech Connect

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

    1995-09-19

    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.

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

    SciTech Connect

    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

    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.

  17. An in vitro and in vivo study of the ?-amylase activity of phaseolamin.

    PubMed

    de Gouveia, Neire Moura; Alves, Fernanda Vieira; Furtado, Fabiana Barcelos; Scherer, Danielli Luana; Mundim, Antonio Vicente; Espindola, Foued Salmen

    2014-08-01

    We evaluated the polypeptide profiles, inhibition of human salivary ?-amylase activity, and hemagglutination properties of a commercial phaseolamin sample. We also performed an in vivo assay to investigate the effects of a commercial phaseolamin treatment (100, 500, or 1500?mg/kg) over 20 days on the glycemia, body weight, and serum biochemical parameters (total cholesterol, triglycerides, alanine aminotransferase, and aspartate aminotransferase) of nondiabetic and streptozotocin-induced diabetic rats. The in vitro evaluation showed defined protein profiles, low hemagglutination activity, and high ?-amylase inhibition. None of the experimental groups treated with phaseolamin or acarbose showed decreases in body weight. Our data demonstrate that phaseolamin inhibits amylase activity in vitro, reduces blood glucose levels, decreases or attenuates some of the renal and hepatic effects of diabetes in streptozotocin-induced rats, and could therefore have therapeutic potential in the treatment or prevention of the complications of diabetes. PMID:24650210

  18. In vitro and in vivo anti-plasmodial activity of essential oils, including hinokitiol.

    PubMed

    Fujisaki, Ryuichi; Kamei, Kiyoko; Yamamura, Mariko; Nishiya, Hajime; Inouye, Shigeharu; Takahashi, Miki; Abe, Shigeru

    2012-03-01

    Abstract. The anti-plasmodial activity of 47 essential oils and 10 of their constituents were screened for in vitro activity against Plasmodium falciparum. Five of these essential oils (sandalwood, caraway, monarda, nutmeg, and Thujopsis dolabrata var. hondai) and 2 constituents (thymoquinone and hinokitiol) were found to be active against P. falciparum in vitro, with 50% inhibitory concentration (IC50) values equal to or less than 1.0 microg/ml. Furthermore, in vivo analysis using a rodent model confirmed the anti-plasmodial potential of subcutaneously administered sandalwood oil, and percutaneously administered hinokitiol and caraway oil against rodent P. berghei. Notably, these oils showed no efficacy when administered orally, intraperitoneally or intravenously. Caraway oil and hinokitiol dissolved in carrier oil, applied to the skin of hairless mice caused high levels in the blood, with concentrations exceeding their IC50 values. PMID:23082579

  19. G17-modified hammerhead ribozymes are active in vitro and in vivo

    PubMed Central

    Kalweit, Anne; Hammann, Christian

    2013-01-01

    Natural hammerhead ribozymes (HHRz) feature tertiary interactions between hairpin loops or bulges in two of three helices that surround the catalytic core of conserved nucleotides. Their conservation was originally established on minimal versions lacking the tertiary interactions. While those sequence requirements in general also apply to natural versions, we show here differences for the HHRz cleavage site N17. A guanosine at this position strongly impairs cleavage activity in minimal versions, whereas we observe for the G17 variants of four tertiary stabilized HHRz significant cleavage and ligation activity in vitro. Kinetic analyses of these variants revealed a reduced rate and extent of cleavage, compared with wild-type sequences, while variants with distorted tertiary interactions cleaved at a reduced rate, but to the same extent. Contrary to this, G17 variants exhibit similar in vitro ligation activity as compared with the respective wild-type motif. To also address the catalytic performance of these motifs in vivo, we have inserted HHRz cassettes in the lacZ gene and tested this ?-galactosidase reporter in Dictyostelium discoideum. In colorimetric assays, we observe differences in the enzymatic activity of ?-galactosidase, which correlate well with the activity of the different HHRz variants in vitro and which can be unambiguously attributed to ribozyme cleavage by primer extension analysis. PMID:24145822

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

    PubMed Central

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

    2014-01-01

    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

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

    PubMed

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

    2014-01-01

    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

  2. Antioxidative and in vitro antiproliferative activity of Arctium lappa root extracts

    PubMed Central

    2011-01-01

    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

  3. Evaluation of potential endocrine activity of 2,4-dichlorophenoxyacetic acid using in vitro assays.

    PubMed

    Coady, Katherine K; Kan, H Lynn; Schisler, Melissa R; Gollapudi, B Bhaskar; Neal, Barbara; Williams, Amy; LeBaron, Matthew J

    2014-08-01

    The herbicide 2,4-dichlorophenoxyacetic acid (2,4-D) was evaluated in five in vitro screening assays to assess the potential for interaction with the androgen, estrogen and steroidogenesis pathways in the endocrine system. The assays were conducted to meet the requirements of the in vitro component of Tier 1 of the United States Environmental Protection Agency's Endocrine Disruptor Screening Program (EDSP), and included assays for estrogen receptor (ER) binding (rat uterine cytosol ER binding assay), ER-mediated transcriptional activation (HeLa-9903-ER? transactivation assay), androgen receptor (AR) binding (rat prostate cytosol AR binding assay), aromatase enzymatic activity inhibition (recombinant human CYP19 aromatase inhibition assay), and interference with steroidogenesis (H295R steroidogenesis assay). Results from these five assays demonstrated that 2,4-D does not have the potential to interact in vitro with the estrogen, androgen, or steroidogenesis pathways. These in vitro data are consistent with a corresponding lack of endocrine effects observed in apical in vivo animal studies, and thus provide important supporting data valuable in a comprehensive weight of evidence evaluation indicating a low potential of 2,4-D to interact with the endocrine system. PMID:24815817

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

    PubMed

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

    2015-08-01

    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 (AOPs) 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

  5. In vitro free radical scavenging activity of platinum nanoparticles

    NASA Astrophysics Data System (ADS)

    Watanabe, Aki; Kajita, Masashi; Kim, Juewon; Kanayama, Atsuhiro; Takahashi, Kyoko; Mashino, Tadahiko; Miyamoto, Yusei

    2009-11-01

    A polyacrylic acid (PAA)-protected platinum nanoparticle species (PAA-Pt) was prepared by alcohol reduction of hexachloroplatinate. The PAA-Pt nanoparticles were well dispersed and homogeneous in size with an average diameter of 2.0 ± 0.4 nm (n = 200). We used electron spin resonance to quantify the residual peroxyl radical (\\mathrm {AOO}^{\\bullet } ) generated from 2,2-azobis (2-aminopropane) dihydrochloride (AAPH) by thermal decomposition in the presence of O2 and a spectrophotometric method to quantify the residual 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical. PAA-Pt scavenged these two radicals in a dose-dependent manner. Platinum was the functional component. PAA-Pt reduced the rate of oxygen consumption required for linoleic acid peroxidation initiated by \\mathrm {AOO}^{\\bullet } generated from AAPH, indicating inhibition of the propagation of linolate peroxidation. A thiobarbituric acid test also revealed dose-dependent inhibition of the linolate peroxidation by PAA-Pt. Fifty micromolar platinum, as PAA-Pt, completely quenched 250 µM DPPH radical for 5 min. Even when twice diluted in half, the PAA-Pt still quenched 100% of the 250 µM DPPH radical. The scavenging activity of PAA-Pt is durable. These observations suggest that PAA-Pt is an efficient scavenger of free radicals.

  6. Titanium nanotubes activate genes related to bone formation in vitro

    PubMed Central

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

    2012-01-01

    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

  7. E.coli Fis protein activates ribosomal RNA transcription in vitro and in vivo.

    PubMed Central

    Ross, W; Thompson, J F; Newlands, J T; Gourse, R L

    1990-01-01

    An upstream activation region (UAR) contributes to the extremely high activity of the Escherichia coli ribosomal RNA promoter, rrnB P1, increasing its activity 20- to 30-fold over that of the same promoter lacking the UAR. We have used DNase footprinting to define three specific sites in the rrnB P1 UAR that bind Fis, a protein identified previously by its role in recombinational enhancer function in other systems. We find that purified Fis activates transcription from promoters containing these sites 10- to 20-fold in vitro at concentrations correlating with the filling of these sites. Three approaches indicate that Fis contributes to the function of the UAR in vivo. First, there is a progressive loss in the activity of rrnB P1-lacZ fusions as Fis binding sites are deleted. Second, an rrnB P1 promoter with a mutation in a Fis binding site has 5-fold reduced transcription activity in vivo, dramatically reduced Fis binding in vitro, and shows no Fis dependent transcription activation in vitro. Third, upstream activation is reduced 5-fold in a Fis- strain. We show that rRNA promoters derepress in response to the loss of Fis in vivo in accord with the predictions of the negative feedback model for rRNA regulation. We find that fis is not essential for the function of two control systems known to regulate rRNA, growth rate dependent control and stringent control. On the basis of these results, we propose roles for Fis and the upstream activation system in rRNA synthesis. Images Fig.1 Fig.4 Fig.5 Fig.6 PMID:2209559

  8. Lactate dehydrogenase activity is inhibited by methylmalonate in vitro.

    PubMed

    Saad, Laura O; Mirandola, Sandra R; Maciel, Evelise N; Castilho, Roger F

    2006-04-01

    Methylmalonic acidemia (MMAemia) is an inherited metabolic disorder of branched amino acid and odd-chain fatty acid metabolism, involving a defect in the conversion of methylmalonyl-coenzyme A to succinyl-coenzyme A. Systemic and neurological manifestations in this disease are thought to be associated with the accumulation of methylmalonate (MMA) in tissues and biological fluids with consequent impairment of energy metabolism and oxidative stress. In the present work we studied the effect of MMA and two other inhibitors of mitochondrial respiratory chain complex II (malonate and 3-nitropropionate) on the activity of lactate dehydrogenase (LDH) in tissue homogenates from adult rats. MMA potently inhibited LDH-catalyzed conversion of lactate to pyruvate in liver and brain homogenates as well as in a purified bovine heart LDH preparation. LDH was about one order of magnitude less sensitive to inhibition by MMA when catalyzing the conversion of pyruvate to lactate. Kinetic studies on the inhibition of brain LDH indicated that MMA inhibits this enzyme competitively with lactate as a substrate (K (i)=3.02+/-0.59 mM). Malonate and 3-nitropropionate also strongly inhibited LDH-catalyzed conversion of lactate to pyruvate in brain homogenates, while no inhibition was observed by succinate or propionate, when present in concentrations of up to 25 mM. We propose that inhibition of the lactate/pyruvate conversion by MMA contributes to lactate accumulation in blood, metabolic acidemia and inhibition of gluconeogenesis observed in patients with MMAemia. Moreover, the inhibition of LDH in the central nervous system may also impair the lactate shuttle between astrocytes and neurons, compromising neuronal energy metabolism. PMID:16758363

  9. Antiviral activity of glycyrrhizin against hepatitis C virus in vitro.

    PubMed

    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

    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

  10. Theileria annulata induces abberrant T cell activation in vitro and in vivo.

    PubMed Central

    Campbell, J D; Howie, S E; Odling, K A; Glass, E J

    1995-01-01

    The protozoan parasite of cattle, Theileria annulata, causes a severe lymphoproliferative disease, developing initially in the draining lymph node, which is often fatal in naive animals. Infection of macrophages with T. annulata leads to an augmentation of their antigen-presenting capability in vitro and infected cells can induce proliferation of autologous resting T cells from naive animals. This inappropriate activation of T cells may play an important role in the failure of the host to mount an effective immune response in vivo. To investigate this hypothesis we characterized further the response of T cells from naive cattle to infected cells in vitro, and also examined the development of the immune response in lymph nodes draining the sites of T. annulata infection. Both CD4+ and CD8+ T cells from naive peripheral blood mononuclear cells (PBMC) were induced to proliferate and express the activation markers IL-2R and MHC class II when cultured with infected cells. This effect was seen in both 'naive' and 'memory' T cells, and was dependent upon contact with infected cells. In vitro, infected cells are therefore capable of activating T cells irrespective of their antigen specificity or memory status. In draining lymph nodes, although large numbers of IL-2R+ cells developed following infection, these activated cells were only associated with areas of parasite-induced proliferating cells, and subsequently disappeared from the node. Cells expressing IL-2R were not present in recognized sites for T cell development. Germinal centres were severely affected, losing T cell-dependent zones followed by a total destruction of morphology. T cell function is therefore severely disrupted within draining nodes. This study has shown that parasitized cells supply sufficient signals in vitro to activate T cells irrespective of specificity. T cells also are not stimulated in a conventional manner in vivo, and this may play an important role in preventing an effective immune response from being generated. Images Fig. 4 Fig. 5 Fig. 5 PMID:7851012

  11. Silylation improves the photodynamic activity of tetraphenylporphyrin derivatives in vitro and in vivo.

    PubMed

    Horiuchi, Hiroaki; Hosaka, Masahiro; Mashio, Hiroyuki; Terata, Motoki; Ishida, Shintaro; Kyushin, Soichiro; Okutsu, Tetsuo; Takeuchi, Toshiyuki; Hiratsuka, Hiroshi

    2014-05-12

    The effects of silyl and hydrophilic groups on the photodynamic properties of tetraphenylporphyrin (TPP) derivatives have been studied in vitro and in vivo. Silylation led to an improvement in the quantum yield of singlet oxygen sensitization for both sulfo and carboxy derivatives, although the silylation did not affect other photophysical properties. Silylation also improved the cellular uptake efficiency for both sulfo and carboxy derivatives, enhancing the in vitro photodynamic activity of the photosensitizer in U251 human glioma cells. The carboxy derivative (SiTPPC4 ) was found to show higher cellular uptake efficiency and in vitro photodynamic activity than the corresponding sulfo derivative (SiTPPS4 ), which indicates that the carboxy group is a more promising hydrophilic group than the sulfo group in the silylated porphyrin. SiTPPC4 was found to show high selective accumulation efficiency in tumors, although almost no tumor selectivity was observed for the nonsilylated porphyrin. The concentration of SiTPPC4 in tumors was 13 times higher than that in muscle 12?h after drug administration. We also studied tumor response after treatment and found that silylation enhanced in vivo photodynamic activity significantly. SiTPPC4 shows higher photodynamic activity than NPe6 with white light irradiation. PMID:24710805

  12. New triazoles and echinocandins: mode of action, in vitro activity and mechanisms of resistance.

    PubMed

    Fera, Maria Teresa; La Camera, Erminia; De Sarro, Angelina

    2009-10-01

    Different types of mycoses, especially invasive mycoses caused by yeasts and molds, are a growing problem in healthcare. The most notable explanation for this increase is a rise in the number of immunocompromised patients owing to advances in transplantation, the emergence of AIDS and a rise in the number of invasive surgical procedures. Despite advances in medical practice, some therapeutic problems remain. In addition, intrinsic or acquired antifungal resistance may pose a serious problem to antifungal therapy. A new generation of triazole agents (voriconazole, posaconazole, isavuconazole, ravuconazole and albaconazole) and the recent class of the echinocandins (caspofungin, micafungin and anidulafungin) have become available, and represent an alternative to conventional antifungals for serious fungal infection management. Currently, only two of the recent triazole generation (voriconazole and posaconazole) and all three echinocandins are available for clinical use. More precisely, voriconazole and posaconazole are indicated for the treatment of invasive fungal infections and the echinocandins for the treatment of specific candidiasis. Voriconazole and posaconazole have a very broad spectrum of antifungal activity that includes Candida species, and filamentous and dimorphic fungi. Their activity extends to both fluconazole- and itraconazole-resistant strains of Candida. A major difference between posaconazole and voriconazole is that posaconazole has activity against Zygomycetes including Mucor spp., Rhizopus spp. and Cunninghamella spp., and voriconazole has no activity against this class of fungi. Ravuconazole, isavuconazole and albaconazole have shown very potent in vitro activity against species of Candida, Cryptococcus and Aspergillus, and they are currently in various stages of development. All three echinocandin agents, caspofungin, micafungin and anidulafungin, are similar in their spectrum of activity. Echinocandins do not possess in vitro activity against important basidiomycetes, including Cryptococcus, Rhodotorula and Trichosporon. This review attempts to deliver the most up-to-date knowledge on the mode of action and mechanisms of resistance to triazoles and echinocandins in fungal pathogens. In addition, the in vitro activity data available on triazoles and echinocandins are reported. PMID:19803707

  13. In vitro-in vivo activity relationship of substituted benzimidazole cell division inhibitors with activity against Mycobacteria tuberculosis

    PubMed Central

    Knudson, Susan E.; Kumar, Kunal; Awasthi, Divya; Ojima, Iwao; Slayden, Richard A.

    2014-01-01

    Structure based drug design was used to develop a compound library of novel 2,5,6- and 2,5,7-trisubstituted benzimidazoles. Three structural analogs, SB-P1G10, SB-P8B2 and SB-P3G2 were selected from this library based on previous studies for advanced study. In vitro studies revealed that SB-P8B2 and SB-P3G2 had sigmoidal kill-curves while in contrast SB-P1G10 showed a narrow zonal susceptibility. The in vitro studies also demonstrated that exposure to SB-P8B2 or SB-P3G2 was bactericidal, while SB-P1G10 treatment never resulted in complete killing. The dose curves for the three compounds against clinical isolates were comparable to their respective dose curves in the laboratory strain of M. tuberculosis. SB-P8B2 and SB-P3G2 exhibited antibacterial activity against non-replicating bacilli under low oxygen conditions. SB-P3G2 and SB-P1G10 were assessed in acute short-term animal models of tuberculosis, which showed that SB-P3G2 treatment demonstrated activity against M. tuberculosis. Together, these studies reveal an in vitro- in vivo relationship of the 2,5,6-trisubstituted benzimidazoles that serves as a criterion for advancing this class of cell division inhibitors into more resource intensive in vivo efficacy models such as the long-term murine model of tuberculosis and Pre-IND PK/PD studies. Specifically, these studies are the first demonstration of efficacy and an in vitro–in vivo activity relationship for 2,5,6-trisubstituted benzimidazoles. The in vivo activity presented in this manuscript substantiates this class of cell division inhibitors as having potency and efficacy against M. tuberculosis. PMID:24746463

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

    PubMed

    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

    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

  15. In vitro activity of DNA gyrase inhibitors, singly and in combination, against Mycobacterium avium complex.

    PubMed

    Babinchak, T J; Fass, R J

    1992-01-01

    The in vitro activities of the DNA gyrase inhibitors ciprofloxacin, coumermycin, and novobiocin against 31 clinical isolates of Mycobacterium avium complex were studied using a microdilution technique. Minimal inhibitory concentrations (MICs) were determined in 4 days using Middlebrook 7H9 broth, and minimal bactericidal concentrations (MBCs) were determined by subculturing to Middlebrook 7H10 agar. MICs were: ciprofloxacin, 0.5-greater than 16 (mean, 4.1) micrograms/ml; novobiocin, 4-greater than 128 (mean, 54.7) micrograms/ml; and coumermycin, 2-greater than 16 (mean, 17.5) micrograms/ml. MBCs were usually more than two dilution steps higher than MICs. Checkerboard studies failed to reveal synergistic or antagonistic inhibitory activity of DNA gyrase-A and DNA gyrase-B inhibitors in vitro. PMID:1319302

  16. Synthesis and “in Vitro” Trypanocidal Activity Evaluation of Some Organo-iron Compounds.

    PubMed Central

    Neto, Alberto F.; Cardoso, Silvia A.; Albuquerque, Sérgio; Miller, Joseph

    2002-01-01

    Eight organo-iron ferrocene derivatives and arenocenium salts were prepared and evaluated by “in vitro” assay against one strain of Trypanosoma cruzi (Y). Six of the eight organo-iron compounds assayed, piperazinium diferrocenoate 1, ?6-(o-xylene)-?5-(cyclopentadienyl) Iron(II) hexafluorophosphate 3, ?6-(mesitylene)-?5-(cyclopentadienyl) iron(II) hexafluorphosphate 5, ?6-(durene)-?5-(cyclopentadienyl) iron(II) hexafluorphosphate 6, ?6-(?-chlorotoluene)-?5-(cyclopentadienyl) Iron(II) hexafluorphosphate 7 and ?6-(chlorobenzene)-?5-(cyclopentadienyl) iron(II) picrate 8 , were poorly active in the “in vitro” assays. Only two compounds 1,1'–(N-pyperidinocarbonyl) ferrocene 2(IC50=2.4 ?g/mL) and ?6-(o-xylene)-?5(cyclopentadienyl) iron(II) picrate 4 (IC50=12.08 ?g/mL), were more active. Thus, some of the compounds are promising to be used against Chagas' disease as a prophylactic agents. PMID:18476014

  17. In vitro and in vivo antimicrobial activities of sporaricin A, a new aminoglycoside.

    PubMed Central

    Kobayashi, F; Saino, Y; Koshi, T; Hattori, Y

    1980-01-01

    The in vitro and in vivo antimicrobial activity of sporaricin A, a new aminoglycoside, was compared with that of amikacin, dibekacin, and gentamicin. Sporaricin A showed a broad spectrum of activity against various gram-positive and -negative bacteria, including amikacin-, dibekacin-, or gentamicin-resistant strains. Sporaricin A inhibited more than 90% of clinical isolates of staphylococci, Klebsiella, Enterobacter, Citrobacter, Serratia, and Proteus, except for P. morganii and P. inconstans, at the concentration of 3.13 microgram/ml. This activity, except for that against Serratia, was similar to that of amikacin. Against P. inconstans and S. marcescens, sporaricin A was more effective than amikacin, dibekacin, and gentamicin. However, its activity against Pseudomonas aeruginosa was relatively weak in comparison with three other aminoglycosides. Sporaricin A was highly effective against bacteria that had various aminoglycoside-inactivating enzymes and that were resistant to the other drugs tested, but it was not active against those with aminoglycoside 3-acetyltransferase-I. The activity of sporaricin A tended to be greater with a reduction in inoculum size of bacteria and an increase in medium pH and decreased slightly in the presence of 10 to 50% horse serum. The in vitro activity was confirmed by in vivo tests in experimental infections with various bacteria. Its protective effect seemed to be equal to or greater than that of amikacin or dibekacin. PMID:7425599

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

    PubMed

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

    2014-11-15

    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

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

    Microsoft Academic Search

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

    2009-01-01

    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

  20. In vitro antioxidant activity and total phenolic content of ethanolic leaf extract of Stevia rebaudiana Bert

    Microsoft Academic Search

    Shruti Shukla; Archana Mehta; Vivek K. Bajpai; Savita Shukla

    2009-01-01

    The aim of this study was to assess the in vitro potential of ethanolic leaf extract of Stevia rebaudiana as a natural antioxidant. The DPPH activity of the extract (20, 40, 50, 100 and 200?g\\/ml) was increased in a dose dependent manner, which was found in the range of 36.93–68.76% as compared to ascorbic acid 64.26–82.58%. The IC50 values of

  1. In vitro activity of tigecycline against resistant micro-organisms isolated from burn patients

    Microsoft Academic Search

    F. Timurkaynak; H. Arslan; Ö. Kurt Azap; S. Serin Senger; Ö. Ba?aran; S. Özbalikci Karaman; M. Haberal

    2008-01-01

    Infections in burn patients are usually caused by multidrug-resistant micro-organisms. Tigecycline, a derivative of glycylcyclines, is an effective antibiotic against the resistant strains. The aim of this study is to determine the in vitro activity of tigecycline against the multidrug-resistant bacteria isolated from burn patients. Fourty-seven bacteria isolated from 118 patients hospitalized in the burn unit during 2003–2006 were included

  2. In vitro effects of antiepileptic drugs on acetylcholinesterase and ectonucleotidase activities in zebrafish ( Danio rerio) brain

    Microsoft Academic Search

    A. M. Siebel; E. P. Rico; K. M. Capiotti; A. L. Piato; C. T. Cusinato; T. M. A. Franco; M. R. Bogo; C. D. Bonan

    2010-01-01

    Carbamazepine (CBZ), phenytoin (PHT), and gabapentine (GBP) are classical antiepileptic drugs (AEDs) that act through a variety of mechanisms. We have tested the in vitro effects of CBZ, PHT, and GBP at different concentrations on ectonucleotidase and acetylcholinesterase activities in zebrafish brain. CBZ inhibited ATP hydrolysis at 1000?M (32%) whereas acetylcholine hydrolysis decreased at 500?M (25.2%) and 1000?M (38.7%). PHT

  3. Potent In Vitro Antimalarial Activity of Metacycloprodigiosin Isolated from Streptomyces spectabilis BCC 4785

    PubMed Central

    Isaka, Masahiko; Jaturapat, Amonlaya; Kramyu, Jarin; Tanticharoen, Morakot; Thebtaranonth, Yodhathai

    2002-01-01

    Bioassay-guided fractionation of the extract from the fermentation broth of Streptomyces spectabilis BCC 4785 led to the isolation of three principle antimalarial agents, metacycloprodigiosin, bafilomycin A1, and spectinabilin. Metacycloprodigiosin exhibited potent in vitro activity against Plasmodium falciparum K1, with a 50% inhibitory concentration of 0.0050 ± 0.0010 ?g/ml, while its cytotoxicity was much weaker. PMID:11897600

  4. In Vitro Activities of Garenoxacin (BMS-284756) against 170 Clinical Isolates of Nine Pasteurella Species

    Microsoft Academic Search

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

    2002-01-01

    Received 12 November 2001\\/Returned for modification 28 March 2002\\/Accepted 21 May 2002 The in vitro susceptibilities of 170 clinical isolates plus 12 American Type Culture Collection strains of Pasteurella species comprising nine species and three Pasteurella multocida subspecies were studied by an agar dilution method. Garenoxacin (BMS-284756), a new des-fluoro(6) quinolone, was active at <0.06 g\\/ml against all isolates, including

  5. A comparison of in vitro and in vivo EDSTAC test battery results for detecting antiandrogenic activity

    Microsoft Academic Search

    Grantley D. Charles; H. Lynn Kan; Melissa R. Schisler; B. Bhaskar Gollapudi; M. Sue Marty

    2005-01-01

    The androgen receptor (AR) transactivation, binding, and Hershberger assays are being developed for large-scale screening of chemicals for endocrine activity. The goal of this study was to evaluate the correlation between in vitro and in vivo antiandrogenicity assays using a variety of compounds (p,p'-DDE, flutamide (FLUT), spironolactone, procymidone, RU486, methoxychlor (MXC), benzo(a)pyrene (BAP), and selected metabolites). For the AR transactivation

  6. In vitro growth inhibition activities of recombinant feline interferon on all lines derived from canine tumours

    Microsoft Academic Search

    K Ogiwara; A. T Suchiya

    1995-01-01

    To evaluate the anti-tumour effect of recombinant feline interferon (rFeIFN) against canine neoplastic cells, the antiproliferation and anti-colony-forming activities of rfeifn were investigated in vitro, using four cell lines derived from canine tumours; oral acanthomatous epulis (mca-b1), mammary benign mixed tumour (mcm-b2), squamous cell carcinoma (cscc), and malignant melanoma (cmc-1). The rfeifn had a dose-dependent inhibitory effect on the cell

  7. Diterpenes Synthesized from the Natural Serrulatane Leubethanol and Their in Vitro Activities against Mycobacterium tuberculosis.

    PubMed

    Escarcena, Ricardo; Perez-Meseguer, Jonathan; Del Olmo, Esther; Alanis-Garza, Blanca; Garza-González, Elvira; Salazar-Aranda, Ricardo; Waksman de Torres, Noemí

    2015-01-01

    Seventeen new derivatives of the natural diterpene leubethanol, including some potential pro-drugs, with changes in the functionality of the aliphatic chain or modifications of aromatic ring and the phenolic group, were synthesized and tested in vitro by the MABA technique for their activity against the H37Rv strain of Mycobacterium tuberculosis. Some compounds showed antimycobacterial selectivity indices higher than leubethanol. PMID:25905603

  8. The in vitro cytotoxic and apoptotic activity of Triphala—an Indian herbal drug

    Microsoft Academic Search

    Swayamjot Kaur; Husheem Michael; Saroj Arora; Pirkko L. Härkönen; Subodh Kumar

    2005-01-01

    A study on cytotoxic effect of acetone extract of “Triphala” whose antimutagenicity has already been tested (Kaur S., Arora S., Kaur K., Kumar S., 2002. The in vitro antimutagenic activity of Triphala—an Indian herbal drug. Food Chemistry and Toxicology 40, 47–54) was extended to test its cytotoxic effects on cancer cell-lines using Shionogi 115 (S115) and MCF-7 breast cancer cells

  9. In vitro antibacterial activity of some Iranian medicinal plant extracts against Helicobacter pylori

    Microsoft Academic Search

    M. Hajimahmoodi; M. Shams-Ardakani; P. Saniee; F. Siavoshi; M. Mehrabani; H. Hosseinzadeh; P. Foroumadi; M. Safavi; M. Khanavi; T. Akbarzadeh; A. Shafiee; A. Foroumadi

    2011-01-01

    Helicobacter pylori infection causes lifelong chronic gastritis, which can lead to peptic ulcer, mucosa-associated lymphoid tissue (MALT) lymphoma and gastric cancer. The growing problem of antibiotic resistance by the organism demands the search for novel candidates from plant-based sources. In the present study, we evaluated the in vitro anti-H. pylori activity of some selected medicinal plants on clinical isolates of H.

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

    Microsoft Academic Search

    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

    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

  11. In Vitro Activities of Cephalosporins and Quinolones against Escherichia coli Strains Isolated from Diarrheic Dairy Calves

    Microsoft Academic Search

    JOSEANTONIO ORDEN; JOSEANTONIO RUIZ-SANTA-QUITERIA; SILVIA GARCIA; DOLORES CID; RICARDO DE LA FUENTE

    1999-01-01

    The in vitro activities of several cephalosporins and quinolones against 195 strains of Escherichia coli isolated from dairy calves affected by neonatal diarrhea were determined. One hundred thirty-seven of these strains produced one or more potential virulence factors (F5, F41, F17, cytotoxic necrotizing factor, verotoxin, and the eae gene), but the remaining 58 strains did not produce any of these

  12. Activity of Imipenem against Klebsiella pneumoniae Biofilms In Vitro and In Vivo

    PubMed Central

    Chen, Ping; Seth, Akhil K.; Abercrombie, Johnathan J.; Mustoe, Thomas A.

    2014-01-01

    Encapsulated Klebsiella pneumoniae has emerged as one of the most clinically relevant and more frequently encountered opportunistic pathogens in combat wounds as the result of nosocomial infection. In this report, we show that imipenem displayed potent activity against established K. pneumoniae biofilms under both static and flow conditions in vitro. Using a rabbit ear model, we also demonstrated that imipenem was highly effective against preformed K. pneumoniae biofilms in wounds. PMID:24247132

  13. Amaranth seed protein hydrolysates have in vivo and in vitro antihypertensive activity

    Microsoft Academic Search

    Mariana Fritz; Bruno Vecchi; Gustavo Rinaldi; María Cristina Ańón

    2011-01-01

    The objective of this work was to study the hydrolytic release of encrypted peptides with antihypertensive activity from storage proteins of Amaranthus mantegazzianus, as determined by in vitro assays, for the first time by in vivo studies in animal models, and by ex vivo assays. Hydrolysates with hydrolysis degree (DH) of 45% and 65% (IC50 0.12mg\\/ml, equivalent to 300–600?M) exhibited

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

    PubMed Central

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

    2014-01-01

    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

  15. Effects of Adherence, Activation and Distinct Serum Proteins on the In Vitro Human Monocyte Maturation Process

    Microsoft Academic Search

    Yukio Akiyama; Richard Griffith; Paul Miller; G. W. Stevenson; Stacy Lund; D. J. Kanapa; Henry C. Stevenson

    Elutriator-punfied human monocytes were cultured in a serum-free (SF) medium, and various serum proteins and functional activating agents were assessed for their effects on the in vitro maturation of human monocytes to macrophages. Following 3 days of suspension culture in Teflon Iabware, 60% of the monocytes were easily recovered. When varying concentrations of human AB serum (HuAB) were employed, human

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

    Microsoft Academic Search

    Ahmed M. Mohamadin; Ashraf B. Abdel-Naim

    2003-01-01

    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

  17. A Quantitative In Vitro Assay for Chemical Mosquito-Deterrent Activity without Human Blood Cells 1

    Microsoft Academic Search

    Jerome A. Klun; Matthew Kramer; Aijun Zhang; Shifa Wang; Mustapha Debboun

    2008-01-01

    5 ABSTRACT. We report that an aqueous solution containing 10 23 M adenosine triphosphate (ATP) and citrate-phosphate-dextrose-adenine (CPDA-1) can effectively replace transfusable human red blood cells in an in vitro Klun and Debboun bioassay system for evaluating chemicals for mosquito feeding-deterrent activity, using either Aedes aegypti or Anopheles stephensi. These species fed with similar avidity through collagen membrane covering aqueous

  18. Synergistic in vitro antiretroviral activity of a humanized monoclonal anti-CD4 antibody (TNX-355) and enfuvirtide (T-20).

    PubMed

    Zhang, Xing-Quan; Sorensen, Meredith; Fung, Michael; Schooley, Robert T

    2006-06-01

    Recently, antiretroviral agents directed at several steps involved in viral entry have been shown to reduce viral replication in vitro and in vivo. We have demonstrated a high level of in vitro synergistic antiretroviral activity for two entry inhibitors that are directed at sequential steps in the entry process. PMID:16723592

  19. Synergistic In Vitro Antiretroviral Activity of a Humanized Monoclonal Anti-CD4 Antibody (TNX-355) and Enfuvirtide (T-20)

    PubMed Central

    Zhang, Xing-Quan; Sorensen, Meredith; Fung, Michael; Schooley, Robert T.

    2006-01-01

    Recently, antiretroviral agents directed at several steps involved in viral entry have been shown to reduce viral replication in vitro and in vivo. We have demonstrated a high level of in vitro synergistic antiretroviral activity for two entry inhibitors that are directed at sequential steps in the entry process. PMID:16723592

  20. IN VITRO AND IN VIVO STUDY OF AN ANTIMICROBIAL ACTIVITY DISPLAYED BY THE REDMOUTH DISEASE AGENT, YERSINIA RUCKERI

    E-print Network

    Paris-Sud XI, Université de

    IN VITRO AND IN VIVO STUDY OF AN ANTIMICROBIAL ACTIVITY DISPLAYED BY THE REDMOUTH DISEASE AGENT in epide- miology of yersiniosis will be discussed. Materials and Methods In vitro studies were performed and the cultural conditions in order to obtain clearer and larger inhibition pictures. So a meat peptone (Ref19521

  1. Global Surveillance of In Vitro Activity of Micafungin against Candida: a Comparison with Caspofungin by CLSI-Recommended Methods

    Microsoft Academic Search

    M. A. Pfaller; L. Boyken; R. J. Hollis; S. A. Messer; S. Tendolkar; D. J. Diekema

    2006-01-01

    Micafungin is an echinocandin antifungal agent that has recently been approved for the prevention of invasive fungal infection and the treatment of esophageal candidiasis. Prospective sentinel surveillance for the emergence of in vitro resistance to micafungin among invasive Candida sp. isolates is indicated. We determined the in vitro activity of micafungin against 2,656 invasive (bloodstream or sterile site) unique patient

  2. Substituted titanocenes induce caspase-dependent apoptosis in human epidermoid carcinoma cells in vitro and exhibit antitumour activity in vivo

    Microsoft Academic Search

    J H Bannon; I Fichtner; A O'Neill; C Pampillón; N J Sweeney; K Strohfeldt; R W Watson; M Tacke; M M Mc Gee; MM Mc Gee

    2007-01-01

    Titanocene compounds are a novel series of agents that exhibit cytotoxic effects in a variety of human cancer cells in vitro and in vivo. In this study, the antiproliferative activity of two titanocenes (Titanocenes X and Y) was evaluated in human epidermoid cancer cells in vitro. Titanocenes X and Y induce apoptotic cell death in epidermoid cancer cells, with IC50

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

    NASA Astrophysics Data System (ADS)

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

    2010-10-01

    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.

  4. Anti-glycated and antiradical activities in vitro of polysaccharides from Ganoderma capense

    PubMed Central

    Yan, Chunyan; Kong, Fansheng; Zhang, Dezhi; Cui, Jiangxia

    2013-01-01

    Background Ganoderma capense is a Ganoderma species and is widely used, especially in Asia, as a well-known medicinal mushroom for health-promoting effect and for treatment of chronic diseases, such as diabetes, aging, etc. G. capense is rich of polysaccharide. Objective: To isolate the polysaccharides from G. capense and evaluate their anti-glycated and antiradical activities in vitro. Materials and Methods The dried powder of submerged fermentation culturing mycelium of G. capense was defatted, extracted with water/alkaline water followed by ethanol precipitation and deproteinated. And four crude polysaccharides, named as GC50, GC70, GC90 and GCB, were obtained. For the first time, the in vitro anti-glycated activities of the four samples were studied by non-enzymatic glycation reaction. Then, the DPPH radical and hydroxyl radical assays were established to estimate the antiradical capacity of the four samples. Meanwhile the contents of polysaccharides were determined by phenol-sulphuric acid colorimetry. Results and Conclusion Preliminary antiradical in vitro studies indicated that the four crude polysaccharides showed concentration-dependent scavenging abilities on DPPH and hydroxyl radicals. The evaluation of anti-glycation activity suggested that GC70 had good potential for inhibiting the formation of advanced glycation end products. Time- and dose-dependent effects were also observed for all GC70 samples. PMID:23661989

  5. Structure-activity relationship of hybrids of Cinchona alkaloids and bile acids with in vitro antiplasmodial and antitrypanosomal activities.

    PubMed

    Leverrier, Aurélie; Bero, Joanne; Cabrera, Julián; Frédérich, Michel; Quetin-Leclercq, Joëlle; Palermo, Jorge A

    2015-07-15

    In this work, a series of hybrid compounds were tested as antiparasitic substances. These hybrids were prepared from bile acids and a series of antiparasitic Cinchona alkaloids by the formation of a covalent C-C bond via a decarboxylative Barton-Zard reaction between the two entities. The bile acids showed only weak antiparasitic properties, but all the hybrids exhibited high in vitro activities (IC50: 0.48-5.39 ?M) against Trypanosoma brucei. These hybrids were more active than their respective parent alkaloids (up to a 135 fold increase in activity), and displayed good selectivity indices. Aditionally, all these compounds inhibited the in vitro growth of a chloroquine-sensitive strain of Plasmodium falciparum (3D7: IC50: 36.1 nM to 8.72 ?M), and the most active hybrids had IC50s comparable to that of artemisinin (IC50: 36 nM). Some structure-activity relationships among the group of 48 hybrids are discussed. The increase in antiparasitic activity may be explained by an improvement in bioavailability, since the more lipophilic derivatives showed the lowest IC50s. PMID:26063305

  6. The capture proteasome assay: A method to measure proteasome activity in vitro.

    PubMed

    Vigneron, Nathalie; Abi Habib, Joanna; Van den Eynde, Benoît J

    2015-08-01

    Because of its crucial role in various cellular processes, the proteasome is the focus of intensive research for the development of proteasome inhibitors to treat cancer and autoimmune diseases. Here, we describe a new and easy assay to measure the different proteasome activities in vitro (chymotrypsin-like, caspase-like, and trypsin-like) based on proteasome capture on antibody-coated plates, namely the capture proteasome assay (CAPA). Applying the CAPA to lysates from cells expressing standard proteasome, immunoproteasome, or intermediate proteasomes ?5i or ?1i-?5i, we can monitor the activity of the four proteasome subtypes. The CAPA provided similar results as the standard whole-cell proteasome-Glo assay without the problem of contaminating proteases requiring inhibitors. However, the profile of trypsin-like activity differed between the two assays. This could be partly explained by the presence of MgSO4 in the proteasome-Glo buffer, which inhibits the trypsin-like activity of the proteasome. The CAPA does not need MgSO4 and, therefore, provides a more precise measurement of the trypsin-like activity. The CAPA provides a quick and accurate method to measure proteasome activity in vitro in a very specific manner and should be useful for the development of proteasome inhibitors. PMID:25912419

  7. Antitumor activity of norditerpenoid dilactones in Podocarpus plants: structure-activity relationship on in vitro cytotoxicity against Yoshida sarcoma.

    PubMed

    Hayashi, Y; Matsumoto, T; Tashiro, T

    1979-06-01

    The in vitro cytotoxicity of norditerpenoid dilactones isolated from Podocarpus plants was determined against cultured Yoshida sarcoma cells. The dilactones involved 15 natural lactones as well as their derivatives, which include appropriate modifications necessary to the estimation of the structure-activity relationship. The unsaturated system on the B/C ring portion, the dienolide or the epoxyenolide moiety, is essential for the activity, but the gamma-lactone group on the A/B ring portion is not. Other oxygenated substituents on the skeletal carbons, such as hydroxyl, acyloxyl, or epoxide group, also show some significant effect. PMID:572795

  8. ATP-Sensitive Potassium Channel Activation Induces Angiogenesis In Vitro and In Vivo.

    PubMed

    Umaru, Bukar; Pyriochou, Anastasia; Kotsikoris, Vasileios; Papapetropoulos, Andreas; Topouzis, Stavros

    2015-07-01

    Intense research is conducted to identify new molecular mechanisms of angiogenesis. Previous studies have shown that the angiogenic effects of hydrogen sulfide (H2S) depend on the activation of ATP-sensitive potassium channels (KATP) and that C-type natriuretic peptide (CNP), which can act through KATP, promotes endothelial cell growth. We therefore investigated whether direct KATP activation induces angiogenic responses and whether it is required for the endothelial responses to CNP or vascular endothelial growth factor (VEGF). Chick chorioallantoic membrane (CAM) angiogenesis was similarly enhanced by the direct KATP channel activator 2-nicotinamidoethyl acetate (SG-209) and by CNP or VEGF. The KATP inhibitors glibenclamide and 5-hydroxydecanoate (5-HD) reduced basal and abolished CNP-induced CAM angiogenesis. In vitro, the direct KATP openers nicorandil and SG-209 and the polypeptides VEGF and CNP increased proliferation and migration in bEnd.3 mouse endothelial cells. In addition, VEGF and CNP induced cord-like formation on Matrigel by human umbilical vein endothelial cells (HUVECs). All these in vitro endothelial responses were effectively abrogated by glibenclamide or 5-HD. In HUVECs, a small-interfering RNA-mediated decrease in the expression of the inwardly rectifying potassium channel (Kir) 6.1 subunit impaired cell migration and network morphogenesis in response to either SG-209 or CNP. We conclude that 1) direct pharmacologic activation of KATP induces angiogenic effects in vitro and in vivo, 2) angiogenic responses to CNP and VEGF depend on KATP activation and require the expression of the Kir6.1 KATP subunit, and 3) KATP activation may underpin angiogenesis to a variety of vasoactive stimuli, including H2S, VEGF, and CNP. PMID:25977483

  9. In vitro activities of azole antifungal agents against Propionibacterium acnes isolated from patients with acne vulgaris.

    PubMed

    Sugita, Takashi; Miyamoto, Mayumi; Tsuboi, Ryoji; Takatori, Kazuhiko; Ikeda, Reiko; Nishikawa, Akemi

    2010-01-01

    The Gram-positive bacterium Propionibacterium acnes is the causative agent of acne vulgaris. Antibiotics such as tetracycline and macrolide derivatives are used to treat this skin disease; however, the isolation frequency of antibiotic-resistant P. acnes has been increasing. The anti-P. acnes activity of imidazole antifungal agents was reported more than 20 years ago, and since then, new azole antifungal agents have been marketed. Thus, this study determined the in vitro activities of azole antifungal agents against P. acnes isolated from patients with acne vulgaris. Of the five agents tested, miconazole, ketoconazole, and itraconazole showed concentration-dependent anti-P. acnes activity, including against antibiotic-resistant isolates. Time-kill assay also showed the time-dependent activity of the drugs. Fluconazole and voriconazole showed no anti-P. acnes activity. PMID:20045949

  10. In vitro antibacterial and antifungal activity of salicylanilide pyrazine-2-carboxylates.

    PubMed

    Krátký, Martin; Vinšová, Jarmila; Buchta, Vladimír

    2012-07-01

    The development of new antimicrobial agents for the treatment of infectious diseases remains challenging due to the increasing impact of antibiotic resistance. Since salicylanilides and esters of pyrazine-2-carboxylic acid have been described as potential antimicrobials, we have designed and synthesized a series of 2-(phenylcarbamoyl)phenyl pyrazine-2-carboxylates. These were evaluated in vitro for the activity against fungi and Gram-positive and Gram-negative bacteria. All derivatives showed significant antibacterial activity against Gram-positive strains (MIC ? 0.98 ?mol/L) including methicillin-resistant Staphylococcus aureus. The most active molecule was 5-chloro-2-(3-chlorophenylcarbamoyl)phenyl pyrazine-2-carboxylate. With one exception these esters were at least partly active against fungi tested strains, in particular against mould strains (MIC ? 1.95 ?mol/L). The most active antifungal agent overall proved to be 2-(4-bromophenylcarbamoyl)-4-chlorophenyl pyrazine-2-carboxylate. PMID:22548336

  11. Anti-Helicobacter pylori activities of Chenopodium ambrosioides L. in vitro and in vivo

    PubMed Central

    Ye, Hui; Liu, Yu; Li, Ning; Yu, Jing; Cheng, Hong; Li, Jiang; Zhang, Xue-Zhi

    2015-01-01

    AIM: To investigate the bactericidal effects of Chenopodium ambrosioides L. (CAL) against Helicobacter pylori (H. pylori) both in vitro and in vivo. METHODS: For in vitro experiments, the inhibitory activity of CAL was tested using an agar dilution method; H. pylori strain NCTC11637 was incubated on Columbia blood agar plates containing serial concentrations of CAL. The minimal inhibitory concentration (MIC) was determined by the absence of H. pylori colonies on the agar plate. Time-kill curves were used to evaluate bactericidal activity; the average number of colonies was calculated at 0, 2, 8 and 24 h after liquid incubation with concentrations of CAL at 0.5, 1, and 2 × MIC. For in vivo experiments, H. pylori-infected mice were randomly divided into CAL, triple therapy (lansoprazole, metronidazole, and clarithromycin), blank control, or H. pylori control groups. The eradication ratios were determined by positive findings from rapid urease tests (RUTs) and by histopathology. RESULTS: In vitro, the MIC of CAL against H. pylori was 16 mg/L. The time-kill curves showed a stable and persistent decreasing tendency with increasing CAL concentration, and the intensity of the bactericidal effect was proportional to dose; the 1 and 2 × MIC completely inhibited the growth of H. pylori at 24 h. In vivo, the eradication ratios in the CAL group were 60% (6/10) by RUT and 50% (5/10) by histopathology. Ratios in the triple therapy group were both 70% (7/10), and there was no difference between the CAL and triple therapy groups. Histopathologic evaluation revealed massive bacterial colonization on the surface of gastric mucosa and slight infiltration of mononuclear cells after inoculation with H. pylori, but no obvious inflammation or other pathologic changes in gastric mucosa of mice from CAL and triple therapy groups. CONCLUSION: CAL demonstrates effective bactericidal activity against H. pylori both in vitro and in vivo. PMID:25892867

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

    PubMed

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

    2014-12-18

    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

  13. Activation of human mononuclear cells by porcine biologic meshes in vitro

    Microsoft Academic Search

    S. B. Orenstein; Y. Qiao; U. Klueh; D. L. Kreutzer; Y. W. Novitsky

    2010-01-01

    Introduction  While porcine-based biologic meshes are increasingly used for hernia repair, little data exist on tissue responses to such\\u000a products. Host foreign body reaction, local inflammation, and wound healing are principally controlled by monocytes\\/macrophages\\u000a (M\\/MŘs). Exaggerated activation of M\\/MŘs may deleteriously influence mesh integration and remodeling. We hypothesized that\\u000a common porcine meshes induce the differential activation of M\\/MŘs in vitro.\\u000a \\u000a \\u000a \\u000a \\u000a Materials

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

    PubMed

    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

    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

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

    SciTech Connect

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

    2008-01-01

    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.

  16. In vitro, but not in vivo, reversibility of peritoneal macrophages activation during experimental acute pancreatitis

    PubMed Central

    Gea-Sorlí, Sabrina; Closa, Daniel

    2009-01-01

    Background Systemic inflammatory response syndrome is one of the major pathobiologic processes underlying severe acute pancreatitis and the degree of macrophage activation could be one of the factors that finally determine the severity of the disease. We evaluated the activation phenotype in peritoneal macrophages during the progression of an experimental model of acute pancreatitis induced in rats by intraductal administration of 5% sodium taurocholate and the effect of IL-4 and IL-13 to modulate this activation. Samples of pancreas, lung and adipose tissue as well as plasma were also obtained. In some animals IL4 and IL13 were injected 1 h after induction in order to modulate macrophage activation. The expressions of TNF? and Mannose Receptor, as indicators of classical and alternative macrophage activation, were evaluated. Levels of myeloperoxidase and plasma lipase were determined to evaluate the severity of the inflammatory process. The stability of IL-4 in ascitic fluid and plasma was evaluated. Results Peritoneal macrophages showed a classical M1 activation clearly induced 3 h after pancreatitis induction and maintained until 18 h. Treatment with IL-4 and IL-13 reversed the activation of macrophages from a classical M1 to alternative M2 in vitro, but failed to modulate the response of peritoneal macrophages in vivo despite a reduction in inflammation was observed in lung and adipose tissue. Finally, IL-4 shows a short half-live in ascitic fluid when compared with plasma. Conclusion Peritoneal macrophages adopt a pro-inflammatory activation early during acute pancreatitis. Treatment with M2 cytokines could revert in vitro the pancreatitis-induced activation of macrophages but fails to modulate its activation in vivo. This treatment has only a moderate effect in reducing the systemic inflammation associated to acute pancreatitis. Hydrolytic enzymes presents in ascitic fluid could be involved in the degradation of cytokines, strongly reducing its utility to modulate peritoneal macrophages in pancreatitis. PMID:19646232

  17. 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 ...

  18. Association of physical activity in the past year and immediately after in vitro fertilization on pregnancy

    PubMed Central

    Evenson, Kelly R.; Calhoun, Kathryn C.; Herring, Amy H.; Pritchard, David; Wen, Fang; Steiner, Anne Z.

    2014-01-01

    Objective To estimate the association of physical activity on in vitro fertilization (IVF). Design Prospective cohort study. Setting Academic infertility clinic. Patient(s) Women (n = 121) undergoing nondonor IVF embryo transfer (fresh or frozen). Intervention(s) The women completed a questionnaire on past year physical activity and wore an accelerometer from embryo transfer to serum pregnancy testing. Main Outcome Measure(s) Implantation, intrauterine gestation, and live birth. Result(s) Based on self-reported past year physical activity, the adjusted odds of intrauterine gestation was higher among those that had higher continuous active living (odds ratio [OR] 1.96, 95% confidence interval [CI] 1.09–3.50), sports/exercise (OR 1.48, CI 1.02–2.15), and total activity (OR 1.52, 95%CI 1.15–2.01) indices. After embryo transfer, women did almost no vigorous activity (median 0 min/d) as measured by the accelerometer. More of their time was spent in light activity (median 3.0 h/d) and sedentary behaviors (median 9.3 h/d). Accelerometer-measured physical activity and sedentary behavior after embryo transfer were not associated with any IVF outcome. Conclusion(s) An active lifestyle in the preceding year favorably impacted the IVF outcome. After embryo transfer, women engaged in mostly light physical activity and sedentary behaviors; therefore, the impact of vigorous physical activity on implantation could not be determined. PMID:24524834

  19. Aqueous extracts of Roselle (Hibiscus sabdariffa Linn.) varieties inhibit ?-amylase and ?-glucosidase activities in vitro.

    PubMed

    Ademiluyi, Adedayo O; Oboh, Ganiyu

    2013-01-01

    This study sought to investigate the inhibitory effect of aqueous extracts of two varieties (red and white) of Hibiscus sabdariffa (Roselle) calyces on carbohydrate hydrolyzing enzymes (?-amylase and ?-glucosidase), with the aim of providing the possible mechanism for their antidiabetes properties. Aqueous extracts were prepared (1:100 w/v) and the supernatant used for the analysis. The extracts caused inhibition of ?-amylase and ?-glucosidase activities in vitro.The IC(50) revealed that the red variety (25.2 ?g/mL) exhibited higher ?-glucosidase inhibitory activity than the white variety (47.4 ?g/mL), while the white variety (90.5 ?g/mL) exhibited higher ?-amylase inhibitory activity than the red variety (187.9 ?g/mL). However, the ?-glucosidase inhibitory activities of both calyces were higher than that of their ?-amylase. In addition, the red variety possessed higher antioxidant capacity as exemplified by the (•)OH scavenging abilities, Fe(2+) chelating ability, and inhibition of Fe(2+)-induced pancreatic lipid peroxidation in vitro. The enzyme inhibitory activities and antioxidant properties of the roselle extracts agreed with their phenolic content. Hence, inhibition of ?-amylase and ?-glucosidase, coupled with strong antioxidant properties could be the possible underlying mechanism for the antidiabetes properties of H. sabdariffa calyces; however, the red variety appeared to be more potent. PMID:23216107

  20. In vitro antiprotozoal activity of extracts of five Turkish Lamiaceae species.

    PubMed

    Kirmizibekmez, Hasan; Atay, Irem; Kaiser, Marcel; Yesilada, Erdem; Tasdemir, Deniz

    2011-11-01

    The in vitro antiprotozoal activities of crude methanolic extracts from the aerial parts of five Lamiaceae plants (Salvia tomentosa, S. sclarea, S. dichroantha, Nepeta nuda subsp. nuda and Marrubium astracanicum subsp. macrodon) were evaluated against four parasitic protozoa, i.e. Trypanosoma brucei rhodesiense, T. cruzi, Leishmania donovani and Plasmodium falciparum. The cytotoxic potentials of the extracts on L6 cells were also evaluated. Melarsoprol, benznidazole, miltefosine, chloroquine and podophyllotoxin were used as reference drugs. All crude MeOH extracts showed antiprotozoal potential against at least three parasites, so they were dispersed in water and partitioned against n-hexane and chloroform to yield three subextracts that were screened in the same test systems. The n-hexane extract of N. nuda was the most active against T. brucei rhodesiense while the CHCl3 extracts of S. tomentosa and S. dichroantha showed significant activity against L. donovani. All organic extracts displayed in vitro antimalarial and moderate trypanocidal activities against T. cruzi with the n-hexane extract of S. sclarea being the most active against the latter. The extracts displayed low or no cytotoxicity towards mammalian L6 cells. PMID:22224291

  1. In vitro antioxidant activity of non-cultivated vegetables of ethnic Albanians in southern Italy.

    PubMed

    Pieroni, A; Janiak, V; Dürr, C M; Lüdeke, S; Trachsel, E; Heinrich, M

    2002-08-01

    A total of 27 extracts from non-cultivated and weedy vegetables traditionally consumed by ethnic Albanians (Arbëreshë) in the Vulture area (southern Italy) were tested for their free radical scavenging activity (FRSA) in the DPPH (1,1-diphenyl-2-picrylhydrazil radical) screening assay, for their in vitro non-enzymatic inhibition of bovine brain lipid peroxidation and for their inhibition of xanthine oxidase (XO). In both antioxidant assays strong activity was shown for Leopoldia comosa (bulbs, syn.: Muscari comosum) and Centaurea calcitrapa (young whorls). In the lipid peroxidation assay, extracts from leaves of Origanum heracleoticum, Urtica dioica and Tordylium apulum showed a remarkable inhibitory activity (> 50%), too. In the case of Leopoldia comosa and Origanum heracleoticum this activity was comparable to quercetin (at a concentration of 50 microM) and Rhodiola rosea extract. Extracts from non-cultivated Cichorium intybus, Chondrilla juncea and Stellaria media showed strong in vitro inhibition of xanthine oxidase, with an activity higher than that of a reference extract from Ledum groenlandicum. These findings suggest that weedy vegetables may be useful antioxidants of interest in the prevention of ageing related diseases, CNS disorders and as potential sources of phytomedicines against hyperuricaemia and gout. PMID:12203269

  2. Characterization and antioxidant activity in vitro and in vivo of polysaccharide purified from Rana chensinensis skin.

    PubMed

    Wang, Zhanyong; Zhao, Yuanyuan; Su, Tingting; Zhang, Jing; Wang, Fei

    2015-08-01

    Preliminary characterization and antioxidant activity in vitro and in vivo investigation of the polysaccharide fraction named as RCSP II, which was extracted from Rana chensinensis skin, were performed. Results indicated that RCSP II comprised glucose, galactose, and mannose in a molar ratio of 87.82:2.77:1.54 with a molecular weight of 12.8kDa. Antioxidant activity assay in vitro showed that RCSP II exhibited 75.2% scavenging activity against 2,2'-azino-bis(3-ethylbenz-thiazoline-6-sulfonic acid) radicals at the concentration of 2500mg/L and 85.1% against chelated ferrous ion at 4000mg/L. Antioxidant activity assay in vivo further showed that RCSP II increased the activities of antioxidant enzymes, decreased the levels of malondialodehyde, and enhanced total antioxidant capabilities in livers and sera of d-galactose induced mice. These results suggested that RCSP II could have potential antioxidant applications as medicine or functional food. PMID:25933517

  3. In vitro ovicidal and larvicidal activity of Agave sisalana Perr. (sisal) on gastrointestinal nematodes of goats.

    PubMed

    Botura, Mariana B; dos Santos, Jener David G; da Silva, Gisele D; de Lima, Hélimar G; de Oliveira, Joăo Victor A; de Almeida, Maria Angela O; Batatinha, Maria José M; Branco, Alexsandro

    2013-02-18

    This study describes the in vitro anthelmintic activity of aqueous extracts (AE), ethyl acetate extracts (EE), flavonoid fractions (FF) and saponin fractions (SF) obtained from sisal waste (Agave sisalana) against gastrointestinal nematodes of goats. The activity of these extracts was evaluated by performing inhibition of egg hatch (EHA) and larval migration (LMI) assays. The EC(50) results of the EHA corresponded to 4.7, 0.1 and 0.05 mg/mL for EE, EA and FF, respectively. The SF fraction showed no ovicidal activity. The percent efficacies that were observed for the LMI were 50.3, 33.2 and 64.1% for the AE, EE and SF, respectively. The FF fraction did not show activity against the larvae. The analysis of the FF fraction indicates the presence of a homoisoflavonoid. This report suggests that the A. sisalana has activity in vitro against gastrointestinal nematodes of goats. This effect is likely related to the presence of homoisoflavonoid and saponin compounds, which have different actions for specific stages of nematode development. PMID:23146415

  4. Neuronal medium that supports basic synaptic functions and activity of human neurons in vitro

    PubMed Central

    Bardy, Cedric; van den Hurk, Mark; Eames, Tameji; Marchand, Cynthia; Hernandez, Ruben V.; Kellogg, Mariko; Gorris, Mark; Galet, Ben; Palomares, Vanessa; Brown, Joshua; Bang, Anne G.; Mertens, Jerome; Böhnke, Lena; Boyer, Leah; Simon, Suzanne; Gage, Fred H.

    2015-01-01

    Human cell reprogramming technologies offer access to live human neurons from patients and provide a new alternative for modeling neurological disorders in vitro. Neural electrical activity is the essence of nervous system function in vivo. Therefore, we examined neuronal activity in media widely used to culture neurons. We found that classic basal media, as well as serum, impair action potential generation and synaptic communication. To overcome this problem, we designed a new neuronal medium (BrainPhys basal + serum-free supplements) in which we adjusted the concentrations of inorganic salts, neuroactive amino acids, and energetic substrates. We then tested that this medium adequately supports neuronal activity and survival of human neurons in culture. Long-term exposure to this physiological medium also improved the proportion of neurons that were synaptically active. The medium was designed to culture human neurons but also proved adequate for rodent neurons. The improvement in BrainPhys basal medium to support neurophysiological activity is an important step toward reducing the gap between brain physiological conditions in vivo and neuronal models in vitro. PMID:25870293

  5. Neuronal medium that supports basic synaptic functions and activity of human neurons in vitro.

    PubMed

    Bardy, Cedric; van den Hurk, Mark; Eames, Tameji; Marchand, Cynthia; Hernandez, Ruben V; Kellogg, Mariko; Gorris, Mark; Galet, Ben; Palomares, Vanessa; Brown, Joshua; Bang, Anne G; Mertens, Jerome; Böhnke, Lena; Boyer, Leah; Simon, Suzanne; Gage, Fred H

    2015-05-19

    Human cell reprogramming technologies offer access to live human neurons from patients and provide a new alternative for modeling neurological disorders in vitro. Neural electrical activity is the essence of nervous system function in vivo. Therefore, we examined neuronal activity in media widely used to culture neurons. We found that classic basal media, as well as serum, impair action potential generation and synaptic communication. To overcome this problem, we designed a new neuronal medium (BrainPhys basal + serum-free supplements) in which we adjusted the concentrations of inorganic salts, neuroactive amino acids, and energetic substrates. We then tested that this medium adequately supports neuronal activity and survival of human neurons in culture. Long-term exposure to this physiological medium also improved the proportion of neurons that were synaptically active. The medium was designed to culture human neurons but also proved adequate for rodent neurons. The improvement in BrainPhys basal medium to support neurophysiological activity is an important step toward reducing the gap between brain physiological conditions in vivo and neuronal models in vitro. PMID:25870293

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

    PubMed Central

    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

    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

  7. In Vitro RNase and Nucleic Acid Binding Activities Implicate Coilin in U snRNA Processing

    PubMed Central

    Broome, Hanna J.; Hebert, Michael D.

    2012-01-01

    Coilin is known as the marker protein for Cajal bodies (CBs), subnuclear domains important for the biogenesis of small nuclear ribonucleoproteins (snRNPs) which function in pre-mRNA splicing. CBs associate non-randomly with U1 and U2 gene loci, which produce the small nuclear RNA (snRNA) component of the respective snRNP. Despite recognition as the CB marker protein, coilin is primarily nucleoplasmic, and the function of this fraction is not fully characterized. Here we show that coilin binds double stranded DNA and has RNase activity in vitro. U1 and U2 snRNAs undergo a processing event of the primary transcript prior to incorporation in the snRNP. We find that coilin displays RNase activity within the CU region of the U2 snRNA primary transcript in vitro, and that coilin knockdown results in accumulation of the 3? pre-processed U1 and U2 snRNA. These findings present new characteristics of coilin in vitro, and suggest additional functions of the protein in vivo. PMID:22558428

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

    PubMed

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

    2014-05-01

    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

  9. Newly Designed and Synthesized Curcumin Analogs with in vitro Cytotoxicity and Tubulin Polymerization Activity.

    PubMed

    Fawzy, Iten M; Youssef, Khairia M; Ismail, Nasser S M; Gullbo, Joachim; Abouzid, Khaled A M

    2015-07-01

    Novel curcumin analogs with 4-piperidone ring were designed, synthesized, and evaluated for their cytotoxic activities against five different cancer cell lines. 3,5-bis(4-Hydroxy-3-methoxybenzylidene)-4-oxo-N-phenylpiperidine-1-carbothioamide (XIIe) exhibited considerable cytotoxic activity with IC50 values in 1-2.5 ?m range. In silico and in vitro, studies were also performed to predict the binding affinity of the target compounds to the ?-chain of tubulin receptor (PDB code 1SA1) and their abilities to affect microtubules polymerization cycle. 3,5-bis(3-Iodo-5-methoxy-4-propoxybenzylidene)-N-acetylpiperidin-4-one (VIIa) was found to exert 93.3% inhibition of tubulin and destabilization of microtubules in vitro compared to vincristine while, 3,5-bis(3,4,5-trimethoxybenzylidene)-N-benzoylpiperidin-4-one (XIIc) showed high potency in a different way where it exerted 94.8% stabilization of microtubules in vitro compared to positive control paclitaxel. PMID:25352318

  10. In Vitro Reconstitution of the Complete Clostridium thermocellum Cellulosome and Synergistic Activity on Crystalline Cellulose

    PubMed Central

    Krauss, Jan; Zverlov, Vladimir V.

    2012-01-01

    Artificial cellulase complexes active on crystalline cellulose were reconstituted in vitro from a native mix of cellulosomal enzymes and CipA scaffoldin. Enzymes containing dockerin modules for binding to the corresponding cohesin modules were prepared from culture supernatants of a C. thermocellum cipA mutant. They were reassociated to cellulosomes via dockerin-cohesin interaction. Recombinantly produced mini-CipA proteins with one to three cohesins either with or without the carbohydrate-binding module (CBM) and the complete CipA protein were used as the cellulosomal backbone. The binding between cohesins and dockerins occurred spontaneously. The hydrolytic activity against soluble and crystalline cellulosic compounds showed that the composition of the complex does not seem to be dependent on which CipA-derived cohesin was used for reconstitution. Binding did not seem to have an obvious local preference (equal binding to Coh1 and Coh6). The synergism on crystalline cellulose increased with an increasing number of cohesins in the scaffoldin. The in vitro-formed complex showed a 12-fold synergism on the crystalline substrate (compared to the uncomplexed components). The activity of reconstituted cellulosomes with full-size CipA reached 80% of that of native cellulosomes. Complexation on the surface of nanoparticles retained the activity of protein complexes and enhanced their stability. Partial supplementation of the native cellulosome components with three selected recombinant cellulases enhanced the activity on crystalline cellulose and reached that of the native cellulosome. This opens possibilities for in vitro complex reconstitution, which is an important step toward the creation of highly efficient engineered cellulases. PMID:22522677

  11. In vitro reconstitution of the complete Clostridium thermocellum cellulosome and synergistic activity on crystalline cellulose.

    PubMed

    Krauss, Jan; Zverlov, Vladimir V; Schwarz, Wolfgang H

    2012-06-01

    Artificial cellulase complexes active on crystalline cellulose were reconstituted in vitro from a native mix of cellulosomal enzymes and CipA scaffoldin. Enzymes containing dockerin modules for binding to the corresponding cohesin modules were prepared from culture supernatants of a C. thermocellum cipA mutant. They were reassociated to cellulosomes via dockerin-cohesin interaction. Recombinantly produced mini-CipA proteins with one to three cohesins either with or without the carbohydrate-binding module (CBM) and the complete CipA protein were used as the cellulosomal backbone. The binding between cohesins and dockerins occurred spontaneously. The hydrolytic activity against soluble and crystalline cellulosic compounds showed that the composition of the complex does not seem to be dependent on which CipA-derived cohesin was used for reconstitution. Binding did not seem to have an obvious local preference (equal binding to Coh1 and Coh6). The synergism on crystalline cellulose increased with an increasing number of cohesins in the scaffoldin. The in vitro-formed complex showed a 12-fold synergism on the crystalline substrate (compared to the uncomplexed components). The activity of reconstituted cellulosomes with full-size CipA reached 80% of that of native cellulosomes. Complexation on the surface of nanoparticles retained the activity of protein complexes and enhanced their stability. Partial supplementation of the native cellulosome components with three selected recombinant cellulases enhanced the activity on crystalline cellulose and reached that of the native cellulosome. This opens possibilities for in vitro complex reconstitution, which is an important step toward the creation of highly efficient engineered cellulases. PMID:22522677

  12. Novel heterocyclic-substituted benzofuran histamine H 3 receptor antagonists: In vitro properties, drug-likeness, and behavioral activity

    Microsoft Academic Search

    Marlon Cowart; Gregory A. Gfesser; Kaitlin E. Browman; Ramin Faghih; Thomas R. Miller; Ivan Milicic; John L. Baranowski; Kathleen M. Krueger; David G. Witte; Angela L. Molesky; Victoria A. Komater; Michael J. Buckley; Gilbert J. Diaz; Gerard D. Gagne; Deliang Zhou; Xiaoqing Deng; Liping Pan; Ellen M. Roberts; Marilyn S. Diehl; Jill M. Wetter; Kennan C. Marsh; Gerard B. Fox; Jorge D. Brioni; Timothy A. Esbenshade; Arthur A. Hancock

    2007-01-01

    Three novel heterocyclic benzofurans A-688057 (1), A-687136 (2), and A-698418 (3) were profiled for their in vitro and in vivo properties as a new series of histamine H3 receptor antagonists. The compounds were all found to have nanomolar potency in vitro at histamine H3 receptors, and when profiled in vivo for CNS activity, all were found active in an animal

  13. In vitro Short-Time Killing Activity of PovidoneIodine (Isodine® Gargle) in the Presence of Oral Organic Matter

    Microsoft Academic Search

    Akiko Yoneyama; Masaki Shimizu; Makiko Tabata; Junko Yashiro; Toshihiko Takata; Muneo Hikida

    2006-01-01

    In order to estimate the clinical efficacy of a povidone-iodine oral antiseptic (PVP-I) on oral bacterial infectious diseases, we studied the effect of oral organic matter on the in vitro killing activity of PVP-I. In addition, we compared the in vitro short-time killing activity of PVP-I with those of other oral antiseptics using mouth-washing and gargling samples collected from healthy

  14. Bio-active nanoemulsions enriched with gold nanoparticle, marigold extracts and lipoic acid: In vitro investigations.

    PubMed

    Guler, Emine; Barlas, F Baris; Yavuz, Murat; Demir, Bilal; Gumus, Z Pinar; Baspinar, Yucel; Coskunol, Hakan; Timur, Suna

    2014-09-01

    A novel and efficient approach for the preparation of enriched herbal formulations was described and their potential applications including wound healing and antioxidant activity (cell based and cell free) were investigated via in vitro cell culture studies. Nigella sativa oil was enriched with Calendula officinalis extract and lipoic acid capped gold nanoparticles (AuNP-LA) using nanoemulsion systems. The combination of these bio-active compounds was used to design oil in water (O/W) and water in oil (W/O) emulsions. The resulted emulsions were characterized by particle size measurements. The phenolic content of each nanoemulsion was examined by using both colorimetric assay and chromatographic analyses. Two different methods containing cell free chemical assay (1-diphenyl-2-picrylhydrazyl method) and cell based antioxidant activity test were used to evaluate the antioxidant capacities. In order to investigate the bio-activities of the herbal formulations, in vitro cell culture experiments, including cytotoxicity, scratch assay, antioxidant activity and cell proliferation were carried out using Vero cell line as a model cell line. Furthermore, to monitor localization of the nanoemulsions after application of the cell culture, the cell images were monitored via fluorescence microscope after FITC labeling. All data confirmed that the enriched N. sativa formulations exhibited better antioxidant and wound healing activity than N. sativa emulsion without any enrichment. In conclusion, the incorporation of AuNP-LA and C. officinalis extract into the N. sativa emulsions significantly increased the bio-activities. The present work may support further studies about using the other bio-active agents for the enrichment of herbal preparations to strengthen their activities. PMID:25009101

  15. Effects of Guanxinning injection on rat cytochrome P450 isoforms activities in vivo and in vitro.

    PubMed

    Yu, Yue; Liu, Yan; Li, Qian; Sun, Jiahui; Lin, Haiou; Liu, Gaofeng

    2015-06-01

    1. We aimed to investigate the regulatory effects of Guanxinning injection (GXNI) on activities of cytochrome P1A2 (CYP1A2), CYP2C11, CYP2D1 and CYP3A1/2 by probe drugs in rats in vivo and in vitro. 2. GXNI-treated and blank control groups were administered GXNI and physiological saline by caudal vein for 14 days consecutively, then they were given the probe drugs of caffeine (10?mg/kg), tolbutamide (10?mg/kg), metoprolol (20?mg/kg) and dapsone (10?mg/kg) by intraperitoneal injection. The blood samples were collected at different times for ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) analysis. Changes of the pharmacokinetics parameters between the GXNI-treated and the blank control groups were used to evaluate the effects of GXNI on the four CYP450 isoforms in rats in vivo. After blood collection, the livers of rats were taken and made microsomes for in vitro tests. The relevant metabolites of phenacetin, tolbutamide, dextromethorphan and testosterone were analyzed quantitatively by high-performance liquid chromatography (HPLC) after microsome incubation. The statistical differences between the two groups were observed to detect the effects of GXNI on the four CYP450 isoforms in rats in vitro. 3. The in vivo and in vitro results demonstrated that GXNI could induce CYP1A2 activity in rats, but had no significant effects on CYP2C11, CYP2D1 and CYP3A1/2. PMID:25495039

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

    PubMed Central

    Thirugnanasampandan, Ramaraj; David, Delma

    2014-01-01

    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

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

    PubMed Central

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

    2013-01-01

    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

  18. In vitro effect of levan-activated macrophages on Lewis lung carcinoma cells.

    PubMed

    Leibovici, J; Hoenig, S; Pinchassov, A

    1986-01-01

    The polysaccharide levan (polyfructose) has previously been shown to exert an inhibitory effect on the growth of several murine tumors. This activity is mediated by a host reaction, involving mainly macrophages but also other elements of the immune system. It was not clear, however, whether levan-activated macrophages act by a direct cytocidal effect on the tumor cells or via the activation of a specific immune response to the tumor. In the present study, the possibility of a direct cytotoxicity of levan-activated macrophages against Lewis lung carcinoma cells was tested by coculture in vitro. It was found that levan-induced (as well as paraffin oil induced) macrophages actually exert a direct cytotoxic effect on Lewis lung carcinoma cells. The tumor cell killing is mediated by cell to cell contact. A cytoplasmic bridge was often seen between the macrophage and the tumor cell. The remaining tumor cells in the lysed area appear slender, shrunken and non-dividing. PMID:3759297

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

    PubMed

    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

    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

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

    PubMed Central

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

    2013-01-01

    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

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

    PubMed

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

    2013-10-01

    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

  2. In Vitro and In Vivo Activities of the Nitroimidazole TBA-354 against Mycobacterium tuberculosis

    PubMed Central

    Cho, S.; Yang, T. J.; Kim, Y.; Wang, Y.; Lu, Y.; Wang, B.; Xu, J.; Mdluli, K.; Ma, Z.; Franzblau, S. G.

    2014-01-01

    Nitroimidazoles are a promising new class of antitubercular agents. The nitroimidazo-oxazole delamanid (OPC-67683, Deltyba) is in phase III trials for the treatment of multidrug-resistant tuberculosis, while the nitroimidazo-oxazine PA-824 is entering phase III for drug-sensitive and drug-resistant tuberculosis. TBA-354 (SN31354[(S)-2-nitro-6-((6-(4-trifluoromethoxy)phenyl)pyridine-3-yl)methoxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine]) is a pyridine-containing biaryl compound with exceptional efficacy against chronic murine tuberculosis and favorable bioavailability in preliminary rodent studies. It was selected as a potential next-generation antituberculosis nitroimidazole following an extensive medicinal chemistry effort. Here, we further evaluate the pharmacokinetic properties and activity of TBA-354 against Mycobacterium tuberculosis. TBA-354 is narrow spectrum and bactericidal in vitro against replicating and nonreplicating Mycobacterium tuberculosis, with potency similar to that of delamanid and greater than that of PA-824. The addition of serum protein or albumin does not significantly alter this activity. TBA-354 maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates. Spontaneous resistant mutants appear at a frequency of 3 × 10?7. In vitro studies and in vivo studies in mice confirm that TBA-354 has high bioavailability and a long elimination half-life. In vitro studies suggest a low risk of drug-drug interactions. Low-dose aerosol infection models of acute and chronic murine tuberculosis reveal time- and dose-dependent in vivo bactericidal activity that is at least as potent as that of delamanid and more potent than that of PA-824. Its superior potency and pharmacokinetic profile that predicts suitability for once-daily oral dosing suggest that TBA-354 be studied further for its potential as a next-generation nitroimidazole. PMID:25331696

  3. In vitro and in vivo activities of the nitroimidazole TBA-354 against Mycobacterium tuberculosis.

    PubMed

    Upton, A M; Cho, S; Yang, T J; Kim, Y; Wang, Y; Lu, Y; Wang, B; Xu, J; Mdluli, K; Ma, Z; Franzblau, S G

    2015-01-01

    Nitroimidazoles are a promising new class of antitubercular agents. The nitroimidazo-oxazole delamanid (OPC-67683, Deltyba) is in phase III trials for the treatment of multidrug-resistant tuberculosis, while the nitroimidazo-oxazine PA-824 is entering phase III for drug-sensitive and drug-resistant tuberculosis. TBA-354 (SN31354[(S)-2-nitro-6-((6-(4-trifluoromethoxy)phenyl)pyridine-3-yl)methoxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine]) is a pyridine-containing biaryl compound with exceptional efficacy against chronic murine tuberculosis and favorable bioavailability in preliminary rodent studies. It was selected as a potential next-generation antituberculosis nitroimidazole following an extensive medicinal chemistry effort. Here, we further evaluate the pharmacokinetic properties and activity of TBA-354 against Mycobacterium tuberculosis. TBA-354 is narrow spectrum and bactericidal in vitro against replicating and nonreplicating Mycobacterium tuberculosis, with potency similar to that of delamanid and greater than that of PA-824. The addition of serum protein or albumin does not significantly alter this activity. TBA-354 maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates. Spontaneous resistant mutants appear at a frequency of 3 × 10(-7). In vitro studies and in vivo studies in mice confirm that TBA-354 has high bioavailability and a long elimination half-life. In vitro studies suggest a low risk of drug-drug interactions. Low-dose aerosol infection models of acute and chronic murine tuberculosis reveal time- and dose-dependent in vivo bactericidal activity that is at least as potent as that of delamanid and more potent than that of PA-824. Its superior potency and pharmacokinetic profile that predicts suitability for once-daily oral dosing suggest that TBA-354 be studied further for its potential as a next-generation nitroimidazole. PMID:25331696

  4. Inhibitory effect of ebselen on cerebral acetylcholinesterase activity in vitro: kinetics and reversibility of inhibition.

    PubMed

    Martini, Franciele; Bruning, César Augusto; Soares, Suelen Mendonca; Nogueira, Cristina Wayne; Zeni, Gilson

    2015-01-01

    Ebselen is a synthetic organoselenium compound that has been considered a potential pharmacological agent with low toxicity, showing antioxidant, anti-inflammatory and neuroprotective effects. It is bioavailable, blood-brain barrier permeant and safe based on cellular toxicity and Phase I-III clinical trials. There is evidence that ebselen inhibits acetylcholinesterase (AChE) activity, an enzyme that plays a key role in the cholinergic system by hydrolyzing acetylcholine (ACh), in vitro and ex vivo. This system has a well-known relationship with cognitive process, and AChE inhibitors, such as donepezil and galantamine, have been used to treat cognitive deficits, mainly in the Alzheimer's Disease (AD). However, these drugs have poor bioavailability and a number of side effects, including gastrointestinal upsets and hepatotoxicity. In this way, this study aimed to evaluate the effect of ebselen on cerebral AChE activity in vitro and to determine the kinetic profile and the reversibility of inhibition by dialysis. Ebselen inhibited the cerebral AChE activity with an IC50 of 29 µM, similar to IC50 found with pure AChE from electric eel, demonstrating a mixed and reversible inhibition of AChE, since it increased Km and decreased Vmax. The AChE activity was recovered within 60 min of dialysis. Therefore, the use of ebselen as a therapeutic agent for treatment of AD should be considered, although memory behavior tasks are needed to support such hypothesis. PMID:25312723

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

    PubMed

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

    2015-01-01

    Garcinia species are reported to possess antimicrobial, anti-inflammatory, anticancer, anti-HIV and anti-Alzheimer's activities. This study aimed to investigate the in vitro cholinesterase enzyme inhibitory activities of garcihombronane C (1), garcihombronane F (2), garcihombronane I (3), garcihombronane N (4), friedelin (5), clerosterol (6), spinasterol glucoside (7) and 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

  6. In vitro and in vivo antiproliferative activity of laherradurin and cherimolin-2 of Annona diversifolia Saff.

    PubMed

    Schlie-Guzmán, María Adelina; García-Carrancá, Alejandro; González-Esquinca, Alma Rosa

    2009-08-01

    Acetogenins from Annonaceae (ACG) are potent inhibitors of the mitochondrial complex I, they present cytotoxic activity on neoplasic lines, including those with multiresistance to drugs. In vivo antitumor activities of some ACG have been reported; however, no information is available regarding the relationship between their cytotoxic activity in cell cultures and their antiproliferative action in vivo. Laherradurin and cherimolin-2 acetogenins were isolated from Annona diversifolia seeds, and their inhibitory potential was analysed in vitro on HeLa and SW-480 cells. Doses containing 1, 10, 100 and 500 times the IC50 obtained from the proliferation assays and multiplied by the weight of the animal, were injected once daily into athymic mice bearing these cancer cell lines; their effect upon tumor growth was measured over a period of 20 days. Laherradurin was more active than cherimolin-2, and it showed in in vitro proliferation assays a similar IC50 in both neoplasic lines. In athymic mice, laherradurin administered in 10x, 100x and 500x doses, reduced the size of HeLa tumors, and with 100x and 500x doses, affected the SW-480 tumor development. These doses were similar to results found with the control drug doxorubicin (p < or = 0.05). On the other hand, cherimolin-2 had an effect on HeLa tumors cells at 100x and 500x doses (p < or = 0.05). PMID:19170140

  7. Potassium humate inhibits complement activation and the production of inflammatory cytokines in vitro

    SciTech Connect

    van Rensburg, C.E.J.; Naude, P.J. [University of Pretoria, Pretoria (South Africa)

    2009-08-15

    The effects of brown coal derived potassium humate on lymphocyte proliferation, cytokine production and complement activation were investigated in vitro. Potassium humate increased lymphocyte proliferation of phytohaemaglutinin A (PHA) and pokeweed mitogen (PWM) stimulated mononuclear lymphocytes (MNL) in vitro from concentrations of 20 to 80 {mu} g/ml, in a dose dependant manner. On the other hand potassium humate, at 40 {mu} g/ml, significantly inhibited the release of TNF-alpha, IL-1 beta, IL-6 and IL-10 by PHA stimulated MNL. Regarding complement activation it was found that potassium humate inhibits the activation of both the alternative and classical pathways without affecting the stability of the red blood cell membranes. These results indicate that the anti-inflammatory potential of potassium humate could be partially due to the inhibition of pro-inflammatory cytokines responsible for the initiation of these reactions as well as inhibition of complement activation. The increased lymphocyte proliferation observed, might be due to increased IL-2 production as previously been documented.

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

    PubMed Central

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

    2014-01-01

    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

  9. In vitro evaluation of antibacterial, antioxidant, cytotoxic and apoptotic activities of the tubers infusion and extracts of Cyperus rotundus

    Microsoft Academic Search

    Soumaya Kilani; Mohamed Ben Sghaier; Ilef Limem; Ines Bouhlel; Jihed Boubaker; Wissem Bhouri; Ines Skandrani; Aicha Neffatti; Ribai Ben Ammar; Marie Genvičve Dijoux-Franca; Kamel Ghedira; Leila Chekir-Ghedira

    2008-01-01

    The in vitro antibacterial, antioxidant, cytotoxic and apoptotic activities from tubers extracts of Cyperus rotundus (Cyperaceae) were investigated. Antibacterial activity of different extracts was evaluated against five bacterial reference strains. A marked inhibitory effect was observed against Salmonella enteritidis, Staphylococcus aureus and Enterococcus faecalis with total oligomers flavonoids (TOFs) and ethyl acetate extracts. In addition to their antibacterial activity, the

  10. The p53-inhibitor Pifithrin-? inhibits Firefly Luciferase activity in vivo and in vitro

    PubMed Central

    Rocha, Sonia; Campbell, Kirsteen J; Roche, Kevin C; Perkins, Neil D

    2003-01-01

    Background Pifithrin-? is a small molecule inhibitor of p53 transcriptional activity. It has been proposed that the use of pifithrin-? in conjunction with chemotherapeutic and radiation therapies for cancer will reduce the side effects of these treatments in normal tissue that still contains wild type p53. In addition, pifithrin-? provides a useful tool in the laboratory to investigate the function of p53 in model systems. Results While investigating the effects of pifithrin-? on the transcriptional activity of NF-?B, we observed a strong inhibition of reporter plasmids containing the firefly luciferase gene. Firefly luciferase is one of the most commonly used enzymes in reporter gene assays. In contrast, no inhibition of reporter plasmids containing Renilla luciferase or chloramphenicol acetyltransferase was observed. The inhibition of firefly luciferase activity by pifithrin-? was observed both in vivo and in vitro. Pifithrin-? did not inhibit firefly luciferase protein expression, but rather suppressed light production/emission, since addition of exogenous pifithrin-? to active extracts inhibited this activity. Furthermore, pifithrin-? also inhibited recombinant firefly luciferase protein activity. Conclusions Among its other biological activities, pifithrin-? is an inhibitor of firefly luciferase activity. Caution must therefore be taken when using this compound, which has been characterised as an inhibitor of p53 transcriptional activity, to investigate effects on gene expression using transiently transfected reporter plasmids. Furthermore, these results demonstrate that when using novel compounds, the choice of vectors used in the experimental procedures might be of great importance for the correct conclusions to be made. PMID:12967348

  11. Activation of diacylglycerol kinase alpha is required for VEGF-induced angiogenic signaling in vitro.

    PubMed

    Baldanzi, Gianluca; Mitola, Stefania; Cutrupi, Santina; Filigheddu, Nicoletta; van Blitterswijk, Wim J; Sinigaglia, Fabiola; Bussolino, Federico; Graziani, Andrea

    2004-06-17

    Vascular endothelial growth factor-A (VEGF-A) promotes angiogenesis by stimulating migration, proliferation and organization of endothelium, through the activation of signaling pathways involving Src tyrosine kinase. As we had previously shown that Src-mediated activation of diacylglycerol kinase-alpha (Dgk-alpha) is required for hepatocytes growth factor-stimulated cell migration, we asked whether Dgk-alpha is involved in the transduction of angiogenic signaling. In PAE-KDR cells, an endothelial-derived cell line expressing VEGFR-2, VEGF-A165, stimulates the enzymatic activity of Dgk-alpha: activation is inhibited by R59949, an isoform-specific Dgk inhibitor, and is dependent on Src tyrosine kinase, with which Dgk-alpha forms a complex. Conversely in HUVEC, VEGF-A165-induced activation of Dgk is only partially sensitive to R59949, suggesting that also other isoforms may be activated, albeit still dependent on Src tyrosine kinase. Specific inhibition of Dgk-alpha, obtained in both cells by R59949 and in PAE-KDR by expression of Dgk-alpha dominant-negative mutant, impairs VEGF-A165-dependent chemotaxis, proliferation and in vitro angiogenesis. In addition, in HUVEC, specific downregulation of Dgk-alpha by siRNA impairs in vitro angiogenesis on matrigel, further suggesting the requirement for Dgk-alpha in angiogenic signaling in HUVEC. Thus, we propose that activation of Dgk-alpha generates a signal essential for both proliferative and migratory response to VEGF-A165, suggesting that it may constitute a novel pharmacological target for angiogenesis control. PMID:15122338

  12. In vitro activity of RX-P873 against Enterobacteriaceae, Pseudomonas aeruginosa, and Acinetobacter baumannii.

    PubMed

    Flamm, Robert K; Rhomberg, Paul R; Jones, Ronald N; Farrell, David J

    2015-04-01

    RX-P873 is a novel antibiotic from the pyrrolocytosine series which exhibits high binding affinity for the bacterial ribosome and broad-spectrum antibiotic properties. The pyrrolocytosines have shown in vitro activity against multidrug-resistant Gram-negative and Gram-positive strains of bacteria known to cause complicated urinary tract, skin, and lung infections, as well as sepsis. Enterobacteriaceae (657), Pseudomonas aeruginosa (200), and Acinetobacter baumannii (202) isolates from North America and Europe collected in 2012 as part of a worldwide surveillance program were tested in vitro by broth microdilution using Clinical and Laboratory Standards Institute (CLSI) methodology. RX-P873 (MIC90, 0.5 ?g/ml) was >32-fold more active than ceftazidime and inhibited 97.1% and 99.5% of Enterobacteriaceae isolates at MIC values of ?1 and ?4 ?g/ml, respectively. There were only three isolates with an MIC value of >4 ?g/ml (all were indole-positive Protea). RX-P873 (MIC50/90, 2/4 ?g/ml) was highly active against Pseudomonas aeruginosa isolates, including isolates which were nonsusceptible to ceftazidime or meropenem. RX-P873 was 2-fold less active against P. aeruginosa than tobramycin (MIC90, 2 ?g/ml; 91.0% susceptible) and colistin (MIC90, 2 ?g/ml; 99.5% susceptible) and 2-fold more potent than amikacin (MIC90, 8 ?g/ml; 93.5% susceptible) and meropenem (MIC90, 8 ?g/ml; 76.0% susceptible). RX-P873, the most active agent against Acinetobacter baumannii (MIC90, 1 ?g/ml), was 2-fold more active than colistin (MIC90, 2 ?g/ml; 97.0% susceptible) and 4-fold more active than tigecycline (MIC90, 4 ?g/ml). This novel agent merits further exploration of its potential against multidrug-resistant Gram-negative bacteria. PMID:25645834

  13. Determination of in vitro antidiabetic effects, antioxidant activities and phenol contents of some herbal teas.

    PubMed

    Büyükbalci, Aynur; El, Sedef Nehir

    2008-03-01

    In this research, some herbal teas and infusions traditionally used in the treatment of diabetes in Turkey, have been studied for their antidiabetic effects on in vitro glucose diffusion and phenolic contents and antioxidant activities. Ten aqueous herbal tea extracts were examined using an in vitro method to determine their effects on glucose movement across the gastrointestinal tract. Total phenol content of herbal teas was analyzed by Folin-Ciocalteu's procedure. Antioxidant activities of herbal teas were evaluated by the effect of extracts on DPPH radical and hydrogen peroxide scavenging. Antioxidant activity was defined as the amount of the sample to decrease the initial DPPH concentration by 50% as efficient concentration, EC50. Antiradical activity [AE] was calculated as 1/EC50. Values were evaluated statistically. Results support the view that none of the herbal teas showed antidiabetic effect on glucose diffusion using in vitro model glucose absorption. Teas were arranged in the order of green tea > peppermint > thyme > black tea > relax tea > absinthium > shrubby blackberry > sage > roselle > olive leaves according to their total phenol contents. Among ten herbal teas, green tea had the highest hydrogen-donating capacity against to DPPH radical. Ranking of the herbal teas with respect to their DPPH radical scavenging activity were green tea > peppermint > black tea > thyme > relax tea > absinthium > roselle > olive leaves > sage > shrubby blackberry. It was determined that adding flavoring substances such as lemon, bergamot, clove and cinnamon, which are commonly used in preparation of black tea in Turkey resulted to have synergistic effect on total antioxidant activities of black and peppermint teas. The highest hydrogen peroxide inhibition value (65.50%) was obtained for green tea at a 250 microl/ml concentration. The H2O2 scavenging activity of herbal teas decreased in the order green tea > peppermint > relax tea > black tea > thyme > olive leaves > sage > absinthium > shrubby blackberry > roselle. In particular, their phenolic compounds and antioxidant activities may be useful for meal planning in type 2 diabetes. They could contribute to sustain plasma antioxidant level because antioxidants present in plants and herbs prevent the development of vascular diseases seen in type 2 diabetes. PMID:18183488

  14. In vitro antitrypanosomal activity of some phenolic compounds from propolis and lactones from Fijian Kawa (Piper methysticum).

    PubMed

    Otoguro, Kazuhiko; Iwatsuki, Masato; Ishiyama, Aki; Namatame, Miyuki; Nishihara-Tsukashima, Aki; Kiyohara, Hiroaki; Hashimoto, Toshihiro; Asakawa, Yoshinori; Omura, Satoshi; Yamada, Haruki

    2012-07-01

    During our search to discover new antitrypanosomal compounds, eight known plant compounds (three phenolic compounds and five kawa lactones) were evaluated for in vitro activity against Trypanosoma brucei brucei. Among them, we found two phenolic compounds and three kawa lactones possessing an ?-pyrone influenced antitrypanosomal property. In particular, ?-phenethyl caffeate, farnesyl caffeate and dihydrokawain exhibited high or moderate selective and potent antitrypanosomal activity in vitro. We detail here the antitrypanosomal activity and cytotoxicities of the compounds, in comparison with two commonly used antitrypanosomal drugs (eflornithine and suramin). Our findings represent the first report of the promising trypanocidal activity of these compounds. PMID:22116743

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

    PubMed

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

    2014-01-01

    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

  16. In vitro testing of fungicidal activity of biocides against Aspergillus fumigatus.

    PubMed

    Tortorano, Anna Maria; Viviani, Maria Anna; Biraghi, Emanuela; Rigoni, Anna Lisa; Prigitano, Anna; Grillot, Renée

    2005-10-01

    The activity of biocides against Aspergillus fumigatus is unknown. In the European guidelines to evaluate the fungicidal activity of a biocide, the critical step concerning the preparation of conidial suspensions is cumbersome and time-consuming. The aims of this study were to evaluate a simplified procedure to prepare conidial suspensions to test a biocide in comparison with the recommended one and to investigate the in vitro activity of seven biocides by the suspension neutralization method against A. fumigatus clinical isolates. The proposed simplified procedure proved reproducible, gave the same results and was quicker than that described in the European guidelines. Benzalkonium chloride (0.25 %), glutaraldehyde (1.6 %), polyvinylpyrrolidone iodine (1 % available iodine) and polyester glycol iodine (0.18 % available iodine) showed biocidal activity in activity. In addition, a simplified and reproducible procedure may be used for testing the fungicidal activity of new compounds or combined formulations. In conclusion, the biocides tested, which are commonly used in hospital settings, were shown to display biocidal activity against A. fumigatus and a simplified procedure may be adopted for testing the fungicidal activity of new compounds. PMID:16157549

  17. In-vitro Evaluation of Antioxidant Activity and Phenolic Content of Costus speciosus (Koen) J.E. Sm.

    PubMed Central

    Nehete, Jeetendra; Bhatia, Manish; Narkhede, Minal

    2010-01-01

    Costus speciosus (Koen) J.E. Sm. plant and its extracts are used for treatment of fever, snake bites, jaundice, and as a purgative, astringent and antibacterial agent. In the present study, an attempt has been made to evaluate in vitro antioxidant activity of different extracts of this plant by DPPH radical scavenging activity, total antioxidant capacity, nitric oxide scavenging activity, ion chelating activity, hydroxyl radical scavenging activity and its correlation with total phenolic content. PMID:24363737

  18. In Vitro Activity, Synergism, and Testing Parameters of Amikacin, with Comparisons to Other Aminoglycoside Antibiotics

    PubMed Central

    Kelly, Michael T.; Matsen, John M.

    1976-01-01

    The activity of the new aminoglycoside antibiotic, amikacin, was evaluated in vitro against 219 clinical bacterial isolates. One hundred eighty-nine of the 219 strains had agar dilution minimal inhibitory concentration values of 8.0 ?g/ml or less for amikacin. Comparative agar dilution studies were performed for gentamicin, kanamycin, and tobramycin. Gentamicin was the most active overall, but tobramycin and amikacin also had significant activity against most bacterial groups. The effects of divalent cations on the susceptibility of Pseudomonas aeruginosa to amikacin were evaluated, and the minimal inhibitory concentration values varied sixfold over a range of divalent cation concentrations from 0.2 to 8.75 mg%. The effects of media and inoculum size on disk susceptibility testing with amikacin were also evaluated. In addition, a synergistic interaction between carbenicillin and amikacin against P. aeruginosa was demonstrated. Amikacin appears to be a promising new broad spectrum antimicrobial agent. PMID:1259402

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

    PubMed

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

    2015-03-01

    The phytochemical profile of Aloe barbadensis Mill. and Aloe arborescens Mill. was investigated using colorimetric assays, triple quadrupole and time-of-flight mass spectrometry, focusing on phenolic secondary metabolites in the different leaf portions. Hydroxycinnamic acids, several characteristic anthrones and chromones, the phenolic dimer feralolide and flavonoids such as flavones and isoflavones were identified. The stable radical DPPH test and the ORAC assay were then used to determine the in vitro radical scavenging. The outer green rind was the most active, while the inner parenchyma was much less effective. The 5-methylchromones aloesin, aloeresin A and aloesone were the most active among the pure secondary metabolites tested. The results suggest that several compounds are likely to contribute to the overall radical scavenging activity, and indicate that leaf portion must be taken into account when the plant is used for its antioxidant properties. PMID:25306376

  20. In vitro activities of 47 antimicrobial agents against three Campylobacter spp. from pigs.

    PubMed Central

    Gebhart, C J; Ward, G E; Kurtz, H J

    1985-01-01

    The in vitro activities of 47 antimicrobial agents against 30 isolates of Campylobacter species from pigs were determined by the agar dilution technique. The isolates were obtained from pigs with proliferative enteritis and included 10 strains each of Campylobacter coli, Campylobacter sputorum subsp. mucosalis, and "Campylobacter hyointestinalis Gebhart et al." (this name is not on the Approved Lists). Carbadox, furazolidone, nitrofurantoin, gentamicin, and dimetridazole were the most active drugs, inhibiting all three Campylobacter species with a MIC for 50% of the isolates of 2 micrograms/ml or less. Trimethoprim-sulfamethoxazole, cefazolin, sulfachloropyridazine, novobiocin, vancomycin, sulfathiazole, cyclohexamide, bacitracin, p-arsanilic acid, and colistin were the least active, with MICs for 50% of the isolates ranging from 16 to greater than or equal to 128 micrograms/ml. PMID:3985597

  1. Effect of water pollutants and other chemicals upon ribonuclease activity in vitro

    SciTech Connect

    Christensen, G.M.; Olson, D.L.

    1981-12-01

    Ribonuclease was treated in vitro with 73 chemicals, many of which are environmental pollutants, including inorganic, organic, and metal-organic chemicals, pesticides and other biocides, alkyl and aryl industrial pollutants, and certain additional chemicals, to determine their effect upon enzyme activity. Palladium (II and IV) and gold (III) were the strongest inhibitors of RNase activity. Other strong inhibitors, in decreasing order of effect, were: sodium dodecyl sulfate, silver (I), EDTA, mercury (II), copper (II), thiram (fungicide), platinum (IV), malathion (pesticide), lead (II), and beryllium (II). Intermediate effects were found with other inorganic cations, many anions, and some other chemicals. A number of compounds of different chemical types caused no measureable effect. None of the chemicals tested caused a measureable activation of this enzyme.

  2. In vitro inhibition activity of essential oils from some Lamiaceae species against phytopathogenic fungi.

    PubMed

    Kumar, Vinod; Mathela, C S; Tewari, A K; Bisht, K S

    2014-09-01

    Natural products have been in focus as alternative, effective and safe materials against the phytopathogens. Investigations show Nepeta oils as effective in controlling the food crops decay. The inhibitory effects of essential oils derived from Nepeta leucophylla, Nepeta ciliaris, Nepeta clarkei and Calamintha umbrosa against five phytopthogenic fungi have been determined. In vitro antifungal activity varied with their constituents and target species. More active being the oils containing oxygenated terpenoids. Helminthosporium maydis was sensitive to the all oils, IC50 values have 43.6-109.3 ?g mL(-1). The N. leucophylla oil possessing oxygenated iridoids was more effective against H. maydis (IC50 value of 43.6 ?g mL(-1)) while N. ciliaris was more active against Fusarium oxysporum (IC50 value of 219.2 ?g mL(-1)). The oils were effective against the spore germination of all the tested plant pathogens. PMID:25175652

  3. In vitro inhibitory activity of essential oil vapors against Ascosphaera apis.

    PubMed

    Kloucek, Pavel; Smid, Jakub; Flesar, Jaroslav; Havlik, Jaroslav; Titera, Dalibor; Rada, Vojtech; Drabek, Ondrej; Kokoska, Ladislav

    2012-02-01

    This work evaluates the in vitro inhibitory activity of 70 essential oils (EOs) in the vapor phase for the control of Chalkbrood disease caused by Ascosphaera apis Maassen ex Claussen (Olive et Spiltoir). Two wild strains isolated from infected honey bee colonies together with one standard collection strain were tested by the microatmosphere method. From 70 EOs, 39 exhibited an antifungal effect against A. apis standard and wild strains. The greatest antifungal action was observed for EO vapors from Armoracia rusticana, followed by Thymus vulgaris, Cymbopogon flexosus, Origanum vulgare and Allium sativum. An investigation of chemical composition by GC-MS revealed, that the most active EOs contained allyl isothiocyanate, citral, carvacrol and diallyl sulfides as the main constituents. The chemical composition plays a key role, as activities of different EOs from the same botanical species were different according to their composition. PMID:22474973

  4. In Vitro antimycotic activity of xanthorrhizol isolated from Curcuma xanthorrhiza Roxb. against opportunistic filamentous fungi.

    PubMed

    Rukayadi, Yaya; Hwang, Jae-Kwan

    2007-05-01

    Xanthorrhizol was isolated from the rhizome of Curcuma xanthorrhiza (Zingiberaceae) and its in vitro activity against opportunistic filamentous fungi was evaluated using the NCCLS (M38-A) standard method. Xanthorrhizol was found to be active against all the species tested, namely Aspergillus flavus, Aspergillus fumigatus, Aspergillus niger, Fusarium oxysporum, Rhizopus oryzae and Trichophyton mentagrophytes: the MICs being 2.0, 2.0, 2.0, 4.0, 1.0 and 1.0 microg/mL, while the MFCs were 4.0, 4.0, 4.0, 8.0, 2.0 and 2.0 microg/mL, respectively. The susceptibility of six species of filamentous fungi to xanthorrhizol was comparable to that of the commercial antifungal, amphotericin B. Xanthorrhizol also has activity to inhibit the conidial germination of all tested species. The results strongly suggest that xanthorrhizol can be developed as a natural antifungal agent. PMID:17236167

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

    NASA Astrophysics Data System (ADS)

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

    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.

  6. In vitro & in vivo estrogenic activity of glycoside fractions of Solanum nigrum fruit

    PubMed Central

    Jisha, S.; Sreeja, S.; Manjula, S.

    2011-01-01

    Background & objectives: The mature fruits of Solanum nigrum contains steroidal glycosides. These are often used as vegetable and there are evidences on tribal use of these fruits as an oral contraceptive. The present study was carried out to evaluate the estrogenic potential of S. nigrum fruits by in vitro and in vivo assays. Methods: Defatted methanol extract of dried S. nigrum fruits was column fractionated and the glycoside positive fractions pooled. Definite concentrations of the fraction were used for in vitro and in vivo assays. The effect on cell viability was analyzed in MCF-7 cell lines by MTT assay followed by in vitro evaluation of estrogenicity by hydroxy apatite (HAP) binding assay. The results were further evaluated in vivo by performing uterotrophic assay in ovariectomized mouse models. Results: At low concentration (40 ?g/ml), SNGF induced a dose-dependent increase in MCF-7 cell proliferation, while higher extract concentrations (80-320 ?g/ml) caused progressive cell growth inhibition. The competitive binding assay using 3H-E2 suggests that this effect is mediated by estrogen receptor. Mouse uterotrophic assay revealed a classical uterotrophic response in ovariectomized mice in response to S. nigrum glycoside fraction (SNGF). SNGF at a dose of 100 mg/kg of body wt induced the maximum height of luminal epithelial cells which indicated an increase of 30.8 per cent over control (P<0.01) with a correlated increase in uterine wet wt (150% increase over control). Higher doses (250 and 500 mg/kg body wt) of SNGF did not induce any uterotrophic effect. Interpretation & conclusions: Our preliminary data demonstrate the hormone like activity of Solanum glycosides both in vitro and in vivo in mouse, which needs to be further explored to evaluate the possible mechanism and clinical implications. PMID:21985821

  7. In vitro shear stress-induced platelet activation: sensitivity of human and bovine blood.

    PubMed

    Lu, Qijin; Hofferbert, Bryan V; Koo, Grace; Malinauskas, Richard A

    2013-10-01

    As platelet activation plays a critical role in physiological hemostasis and pathological thrombosis, it is important in the overall hemocompatibility evaluation of new medical devices and biomaterials to assess their effects on platelet function. However, there are currently no widely accepted in vitro test methods to perform this assessment. In an effort to develop effective platelet tests for potential use in medical device evaluation, this study compared the sensitivity of platelet responses to shear stress stimulation of human and bovine blood using multiple platelet activation markers. Fresh whole blood samples anticoagulated with heparin or anticoagulant citrate dextrose, solution A (ACDA) were exposed to shear stresses up to 40?Pa for 2?min using a cone-and-plate rheometer model. Platelet activation was characterized by platelet counts, platelet surface P-selectin expression, and serotonin release into blood plasma. The results indicated that exposure to shear stresses above 20?Pa caused significant changes in all three of the platelet markers for human blood and that the changes were usually greater with ACDA anticoagulation than with heparin. In contrast, for bovine blood, the markers did not change with shear stress stimulation except for plasma serotonin in heparin anticoagulated blood. The differences observed between human and bovine platelet responses suggest that the value of using bovine blood for in vitro platelet testing to evaluate devices may be limited. PMID:23738621

  8. Apolipoprotein A-I from striped bass (Morone saxatilis) demonstrates antibacterial activity in vitro.

    PubMed

    Johnston, L Danielle; Brown, Gwynne; Gauthier, David; Reece, Kimberly; Kator, Howard; Van Veld, Peter

    2008-10-01

    HDL and apolipoprotein A-I from teleostean fishes demonstrate in vitro activity against gram-positive and gram-negative bacteria. In this study, we purified ApoA-1 from striped bass (Morone saxatilis) plasma and examined its in vitro antibacterial activity against Streptococcus sp., Escherichia coli, and Mycobacterium marinum. In addition, we obtained sequence for a putative striped bass ApoA-1 gene, which when translated contained the identical sequence generated from N-terminal sequencing of the purified ApoA-1. The predicted secondary and tertiary structures contained the characteristic proline residues and high alpha-helical content conserved between mammals and fishes. Purified ApoA-1 exhibited antibacterial activity against the bacteria assayed. Concentrations of 125 microg/mL for E. coli, 250 microg/mL for Streptococcus sp., and 250 microg/mL for M. marinum, inhibited bacterial growth by 50% compared to control. ApoA-1 plasma concentrations in experimental and wild fish ranged from undetectable levels to greater than 5 mg/mL, indicating that striped bass ApoA-1 is an effective antibacterial agent at concentrations below the range of physiological concentrations in striped bass plasma. We therefore conclude that ApoA-1 could play a role in innate defense against bacterial pathogens in striped bass. PMID:18627791

  9. A fluorescent assay to quantitatively measure in vitro acyl CoA:diacylglycerol acyltransferase activity

    PubMed Central

    McFie, Pamela J.; Stone, Scot J.

    2011-01-01

    Triacylglycerols (TG) are the major storage form of energy in eukaryotic organisms and are synthesized primarily by acyl CoA:1,2-diacylglycerol acyltransferase (DGAT) enzymes. In vitro DGAT activity has previously been quantified by measuring the incorporation of either radiolabeled fatty acyl CoA or diacylglycerol (DG) into TG. We developed a modified acyltransferase assay using a fluorescent fatty acyl CoA substrate to accurately quantify in vitro DGAT activity. In the modified assay, radioactive fatty acyl CoA is replaced with fluorescent NBD-palmitoyl CoA, which is used as a substrate by DGAT with DG to produce NBD-TG. After extraction with organic solvents and separation by thin layer chromatography, NBD-TG formation can be detected and accurately quantified using a fluorescent imaging system. We demonstrate that this method can be adapted to detect other acyltransferase activities. Because NBD-palmitoyl CoA is commercially available at a much lower cost compared with radioactive acyl CoA substrates, it is a more economical alternative to radioactive tracers. In addition, the exposure of laboratory personnel to radioactivity is greatly reduced. PMID:21653930

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

    PubMed Central

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

    2013-01-01

    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

  11. In vitro leishmanicidal activity of 1,3-disubstituted 5-nitroindazoles.

    PubMed

    Marín, Clotilde; Ramírez-Macías, Inmaculada; Rosales, María José; Muro, Beatriz; Reviriego, Felipe; Navarro, Pilar; Arán, Vicente J; Sánchez-Moreno, Manuel

    2015-08-01

    The antiprotozoal activity of some indazole-derived amines (2, 3, 5-8) as well as that of some simple structurally related 3-alkoxy-1-alkyl-5-nitroindazoles (1, 4) against promastigote and amastigote forms of Leishmania infantum and Leishmania braziliensis is reported. In some cases, these compounds showed in vitro activities against the different morphological forms of Leishmania similar to or higher than those of the reference drug glucantime; this fact, along with low unspecific cytotoxicities against macrophages shown by some of them, led to good selectivity indexes (SI). The high efficiency of some 5-nitroindazoles against the mentioned protozoa was confirmed by further in vitro studies on infection rates. Complementary analyses by (1)H NMR of the changes on the metabolites excreted by parasites after treatment with the more active indazole derivatives in many cases showed the decreased excretion of succinate and increased levels of acetate, lactate and alanine, as well as, in some cases, the appearance of glycine and pyruvate as new metabolites. Damage caused by indazoles at the glycosomal or mitochondrial level are consistent with these metabolic changes as well as with the huge ultrastructural alterations observed by transmission electron microscopy (TEM), especially affecting the mitochondria and other cytoplasmic organelles. PMID:25956673

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

    PubMed Central

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

    2013-01-01

    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

  13. Antitumor activity of Portulaca oleracea L. polysaccharides against cervical carcinoma in vitro and in vivo.

    PubMed

    Zhao, Rui; Gao, Xu; Cai, Yaping; Shao, Xingyue; Jia, Guiyan; Huang, Yulan; Qin, Xuegong; Wang, Jingwei; Zheng, Xiaoliang

    2013-07-25

    Portulaca oleracea L. has been used as folk medicine in different countries to treat different ailments in humans. P. oleracea L. polysaccharide (POL-P), extracted from P. oleracea L., is found to have bioactivities such as hypoglycemic and hypolipidemic activities, antioxidant and antitumor activities. In our study, a water-soluble polysaccharide (POL-P3b) was successfully purified from Galium verum L. by DEAE cellulose and Sephadex G-200 column chromatography. To evaluate the anticancer efficacy and associated mechanisms of POL-P3b on cervical cancer in vitro and in vivo, we showed that treatment of HeLa cell with POL-P3b inhibited cell proliferation. In addition, POL-P3b significantly inhibited tumor growth in U14-bearing mice. Further analysis indicated that POL-P3b possesses the activity of inhibiting cervical cancer cell growth in vitro and in vivo at a concentration- and time-dependent manner, and the mechanisms were associated with Sub-G1 phase cell cycle arrest, triggering DNA damage and inducing apoptosis. PMID:23768576

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

    PubMed

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

    2014-07-01

    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

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

    PubMed

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

    2013-01-01

    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

  16. Protein Kinase C Isoform Expression and Activity Alter Paclitaxel Resistance in Vitro

    Microsoft Academic Search

    Lugen Chen; Robert A. Burger; Gretchen M. Zaunbrecher; Huaxu Cheng; A. Jeannine Lincoln; Maria-Claudia Mallarino; Bradley J. Monk; Shafiq A. Khan

    1999-01-01

    Objective.The aim of this study was to assess the relationship of protein kinase C (PKC) isoform expression and functional activity to the development of multidrug resistance in gynecologic malignancies.Methods.Paclitaxel-resistant subclones (T30 and T30-Res) of the Mes-sa human uterine sarcoma cell line were selected through exposure to paclitaxelin vitro.Indices of relative drug resistance were determined by the MTT (3-[4,5-dimethyl-2-thiazolyl]-2,5-diphenyl-2H-tetrazolium bromide) assay.

  17. Growth of ovine granulocyte-macrophage precursors in vitro without exogenous colony-stimulating activity

    SciTech Connect

    Chandra, P.; Joel, D.D.; Chanana, A.D.

    1983-11-01

    Ovine granulocyte-macrophage colony-forming units (CFU-GM) from peripheral blood and bone marrow were cultured in vitro. The colony-stimulating activity (CSA) was provided by various conditioned-media previously reported to contain CSA and by homologous sheep serum (SS). The maximum number of CFU-GM was observed in the cultures containing SS without the addition of exogenous CSA. The CFU-GM appeared earlier in the cultures containing bone marrow cells when compared to the peripheral blood CFU-GM. Replacement of SS by bovine fetal serum resulted in suboptimal growth of ovine CFU-GM.

  18. Antiviral activity of N-benzoylphenylisoserinates of Lactarius sesquiterpenoid alcohols in vitro.

    PubMed

    Krawczyk, Ewa; ?uczak, Miros?aw; Kobus, Miros?aw; Ba?ka, Dariusz; Daniewski, W?odzimierz

    2003-06-01

    Cytotoxic, antiviral, antibacterial and antifungal properties of a new, originally synthesised group of compounds: the N-benzoylphenylisoserinates of sesquiterpenoid alcohols - derivatives of taxol and various sesquiterpenes of Lactarius origin were evaluated in vitro. Among 16 compounds tested, 6 decreased HSV-1 titres. Selectivity indices ranged from 13.9 to 31.7. No activity against RNA viruses (parainfluenza 3, Coxsackie B3, vesicular stomatitis virus, and encephalomyocarditis virus), bacteria: Escherichia coli, Proteus mirabilis, Staphylococcus aureus, Enterococcus faecium and Bacteroides fragilis and fungal strain of Candida albicans was detected. PMID:12865976

  19. Polyoxygenated steroids from the octocoral Leptogorgia punicea and in vitro evaluation of their cytotoxic activity.

    PubMed

    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

    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

  20. In vitro antibacterial activity of minocycline and effect of agar medium utilized in its susceptibility testing.

    PubMed

    Washington, J A; Yu, P K; Martin, W J

    1970-02-01

    The in vitro activity of minocycline against 1,028 bacterial strains was determined in parallel in Mueller Hinton Agar and Trypticase Soy Agar. The broad antibacterial effect of minocycline against gram-positive cocci and gram-negative bacilli is confirmed. Minimal inhibitory concentrations for gram-positive bacteria in Mueller Hinton Agar were at least twofold less than in Trypticase Soy Agar. Minimal inhibitory concentrations for gram-negative bacilli in Mueller Hinton Agar were usually fourfold less than in Trypticase Soy Agar. PMID:4392357

  1. In vitro and in vivo antioxidant activity of a water-soluble polysaccharide from dendrobium denneanum

    USGS Publications Warehouse

    Luo, A.; Ge, Z.; Fan, Y.; Chun, Z.; Jin, He X.

    2011-01-01

    The water-soluble crude polysaccharide (DDP) obtained from the aqueous extracts of the stem of Dendrobium denneanum through hot water extraction followed by ethanol precipitation, was found to have an average molecular weight (Mw) of about 484.7 kDa. Monosaccharide analysis revealed that DDP was composed of arabinose, xylose, mannose, glucose and galactose in a molar ratio of 1.00:2.66:8.92:34.20:10.16. The investigation of antioxidant activity both in vitro and in vivo showed that DDP is a potential antioxidant. ?? 2011.

  2. Antibacterial activity of telithromycin (HMR 3647) in relation to in vitro simulated human plasma kinetics.

    PubMed

    Bonnefoy, A; Le Priol, P

    2001-04-01

    Telithromycin (HMR 3647) is a ketolide suitable for the treatment of respiratory infections. The aim of this study was to demonstrate its antibacterial efficacy against an erythromycin-susceptible Staphylococcus aureus, an erythromycin-resistant Streptococcus pneumoniae and Haemophilus influenzae. The free serum concentrations of telithromycin, produced by repeated oral administration of 800 mg to adults for 10 days, was simulated in an in vitro system. The ketolide displayed bacteriostatic activity against all three strains tested. This study supported the observation that an 800 mg po dose of telithromycin demonstrated antibacterial efficacy against respiratory tract pathogens. PMID:11266424

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

    PubMed Central

    2013-01-01

    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

  4. Comparison of chemical, electrical, and combined activation methods for in vitro matured porcine oocytes.

    PubMed

    Liu, Shuai; Cui, Kuiqing; Li, Hong Li; Sun, Jun Ming; Lu, Xing Rong; Shen, Kai Yuan; Liu, Qing You; Shi, De Shun

    2015-02-01

    Factors influencing porcine oocyte activation were systematically studied. This study included (1) the effect of ionomycin plus various chemical agents on activation, (2) comparison of different electrical activation parameters, (3) optimization of combined activation, and (4) evaluation of the optimized protocols. The results showed that (1) blastocyst rates of ionomycin (Ion) + 6-dimethylaminopurine (6-DMAP) (29.7?±?1.1%), Ion + cytochalasin B (CB) + cycloheximide (CHX) (29.8?±?1.2%), Ion + CB + 6-DMAP (30.4?±?1.6%), and Ion + CB + CHX + 6-DMAP (30.2?±?2.7%) were significantly higher than Ion + CHX (15.8?±?1.5%, p?activation was optimal when oocytes were activated by three direct current (DC) pulses of 1.00 kV cm(-1) for 80 ?s (39.5?±?1.1%); (3) blastocyst rates of DC + CB + CHX (55.4?±?1.2%) and DC + CB + 6-DMAP (50.4?±?2.9%) were significantly higher than DC + 6-DMAP, DC + CB + CHX + 6-DMAP, electrical activation, and chemical activation alone (p?activation blastocysts (40%). Using the optimized electrical and combined activation protocol, high blastocyst rates were generated by intracytoplasmic sperm injection (ICSI) (34.6?±?1.1%), cytoplasmic microinjection (CI) (52.3?±?2.2%), and handmade cloning (HMC) (31.2?±?1.0%), respectively. This study concludes that the optimal activation protocol of in vitro matured porcine oocytes was combined activation with parameter as three DC pulses of 1.00 kV cm(-1) for 80 ?s plus CB and CHX treatment. PMID:25424832

  5. In vitro activities of 36 antimicrobial agents against clinically isolated Bacteroides fragilis.

    PubMed

    Teng, L J; Ho, S W; Chang, S C; Luh, K T; Hsieh, W C

    1991-08-01

    Thirty-six antimicrobial agents were evaluated for in vitro activities against 100 clinical isolates of Bacteroides fragilis. The minimal inhibitory concentration (MIC) of each agent for each isolate was determined by the agar dilution method. Among 25 beta-lactam antibiotics, the most active agent was imipenem with an MIC90 and a geometric mean of 1 and 0.15 micrograms/ml, respectively; followed by ticarcillin-clavulanic acid, and amoxicillin-clavulanic acid. Ampicillin-sulbactam, piperacillin-tazobactam, moxalactam, and flomoxef were the next most active agents. Piperacillin, ticarcillin, ceftizoxime, cefotaxime, cefuzonam, cefoxitin, and cefmetazole were equally active with the MIC50s ranging from 4 to 16 micrograms/ml, and MIC90s ranging from 32 to greater than or equal to 256 micrograms/ml. The remaining 10 beta-lactam antibiotics, ampicillin, amoxicillin, cefazolin, cefuroxime, cefoperazone, cefmenoxime, ceftazidime, cefpirome, aztreonam, and carumonam were less active. All isolates were resistant to cefotiam at a low breakpoint. Among 6 quinolones, ciprofloxacin was the most active agent with an MIC50 and an MIC90 of 4 and 16 micrograms/ml, respectively. All isolates were resistant to nalidixic acid, pipemidic acid, cinoxacin, enoxacin, and norfloxacin. Among 5 frequently used agents, chloramphenicol, ornidazole, and metronidazole were the most effective agents which inhibited 100% of the isolates at 8, 2, and 2 micrograms/ml, respectively; while clindamycin and minocycline had less activity. PMID:1683376

  6. Inhibition of hyaluronidase activity of human and rat spermatozoa in vitro and antispermatogenic activity in rats in vivo by Terminalia chebula, a flavonoid rich plant

    Microsoft Academic Search

    Archana Srivastav; Abhishek Chandra; Madhulika Singh; Farrukh Jamal; Preeti Rastogi; Siron Mani Rajendran; Falgun Wanganuji Bansode; Vijai Lakshmi

    2010-01-01

    Our interest in development of hyaluronidase inhibitors as male antifertility agents led to identification of Terminalia chebula (T. chebula) plant with hyaluronidase (HAase) inhibitory activity of human spermatozoa (?93% inhibition) and rat caudal epididymal spermatozoa (?86% inhibition) in vitro at 30mg\\/ml. We further demonstrated inhibition of hyaluronidase activity of testis and epididymal spermatozoa in vivo coincident with antispermatogenic activity and

  7. A comparison of in vitro and in vivo EDSTAC test battery results for detecting antiandrogenic activity.

    PubMed

    Charles, Grantley D; Kan, H Lynn; Schisler, Melissa R; Bhaskar Gollapudi, B; Sue Marty, M

    2005-01-01

    The androgen receptor (AR) transactivation, binding, and Hershberger assays are being developed for large-scale screening of chemicals for endocrine activity. The goal of this study was to evaluate the correlation between in vitro and in vivo antiandrogenicity assays using a variety of compounds (p,p'-DDE, flutamide (FLUT), spironolactone, procymidone, RU486, methoxychlor (MXC), benzo(a)pyrene (BAP), and selected metabolites). For the AR transactivation assay, AR(+) LNCaP prostate carcinoma cells were transfected with an inducible luciferase reporter construct (pGudLuc7ARE) and exposed for 24 h to test materials (< or = 10 microM) in the presence and absence of 1 nM of the AR agonist R-1881. Each of these materials, including the hydroxlated metabolites of BAP and MXC, produced significant antiandrogenic activity in vitro as evidenced by their inhibition of the response to R-1881. Similarly, in vitro AR binding experiments using the recombinant ligand-binding domain (LBD) of the human AR and fluorescence polarization (FP) methodology yielded IC50s comparable to that of testosterone for RU486 and 9-OH-BAP. Other parent compounds and metabolites exhibited lesser binding affinity. In vivo antiandrogenic activity was evaluated with the Hershberger assay, wherein castrated male CD rats were dosed by gavage for 10 days with (mg/kg per day): MXC (10, 50, 100, and 200), BAP (1, 10, 50, and 100), RU486 (1, 5, 10, and 25), and FLUT (10) in the presence of 0.4 mg/kg per day (sc) of testosterone propionate (TP). Neither BAP nor MXC produced significant decreases in accessory sex tissue (AST) weights relative to TP control. However, 200 MXC resulted in a significant decrease in body weight and 100 BAP significantly increased absolute and relative liver weights. RU486 (25) produced significant decreases in ventral prostate, seminal vesicle, and Cowper's gland weights without affecting body weight. FLUT (10) decreased all AST weights measured. The antiandrogenic activities of the remaining materials (p,p'-DDE, spironolactone, and procymidone) have been demonstrated in previous Hershberger assays. These data indicate the importance of including in vivo results in assessing the endocrine activity of test materials and further stress the importance of a weight of evidence approach in assessing endocrine activity of test materials. PMID:15589981

  8. Antiplatelet, anticoagulant, and fibrinolytic activity in vitro of extracts from selected fruits and vegetables.

    PubMed

    Torres-Urrutia, Constanza; Guzmán, Luis; Schmeda-Hirschmann, Guillermo; Moore-Carrasco, Rodrigo; Alarcón, Marcelo; Astudillo, Luís; Gutierrez, Margarita; Carrasco, Gilda; Yuri, José A; Aranda, Eduardo; Palomo, Iván

    2011-04-01

    A diet rich in fruits and vegetables is known to decrease the risk of cardiovascular disease. However, the information regarding the antithrombotic activity (antiplatelet, anticoagulant, and fibrinolytic) of fruits and vegetables is scarce. The aim of this study was to assess the antithrombotic activity of extracts from fruits and vegetables widely consumed in central Chile. The study included samples of 19 fruits and 26 vegetables, representative of the local diet. The extracts prepared from each sample included an aqueous (juice or pressed solubles) and/or methanol-soluble fraction. The extracts were evaluated for antiplatelet, anticoagulant, and fibrinolytic activity in vitro at a final concentration of 1 mg/ml. The antiplatelet activity was assessed by platelet aggregation inhibition; anticoagulant activity was measured by the prothrombin time (PT), diluted prothrombin time (dPT), activated partial thromboplastin time (APTT), kaolin clotting time (KCT), and thrombin time. The fibrinolytic effect was determined with the euglobin clot lysis time and fibrin plate methods. Extracts of green beans and tomatoes inhibited platelet aggregation induced by ADP and arachidonic acid, in a concentration-dependent manner. The methanolic extracts of grapes prolonged the PT and dPT. Finally, extracts of raspberry prolonged the APTT and also presented fibrinolytic activity. In conclusion, from a screening that included a variety of fruits and vegetables, we found antiplatelet activity in green beans and tomatoes, anticoagulant activities in grapes and raspberries, whereas fibrinolytic activity was observed only in raspberries. Further investigations are necessary to advance in knowledge of the active compounds of these fruits and vegetables and their mechanisms of action. PMID:21311321

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

    PubMed Central

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

    2014-01-01

    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

  10. In Vitro Activity of Rifampicin Combined with Daptomycin or Tigecycline on Staphylococcus haemolyticus Biofilms.

    PubMed

    Szczuka, Ewa; Grabska, Katarzyna; Kaznowski, Adam

    2015-08-01

    Staphylococcus haemolyticus is of increasing concern as a cause of several biofilm-associated infections, and today, it represents the second most common organism among clinical isolates of coagulase-negative staphylococci. However, little is known regarding the treatment of infections caused by these bacteria. In this study, we characterize the biofilm formed by S. haemolyticus strains isolated from bloodstream infections and assess in vitro the activity of rifampicin combined with daptomycin or tigecycline against bacteria growing in a biofilm. The results of our studies indicated that the majority (78 %) of methicillin-resistant Staphylococcus haemolyticus strains have the ability to form a biofilm in vitro. None of these strains carried icaADBC genes indicating that they form biofilm via ica-independent mechanisms. The molecular characterization of the biofilm showed that proteins are the predominant matrix component and play a major role in biofilm structure. Extracellular DNA and polysaccharides, other than polysaccharide intercellular adhesin, are also present in the biofilm matrix, but they play a minor role. The images obtained by confocal laser scanning microscopy showed that most S. haemolyticus strains formed a dense biofilm with a low number of dead cells. In vitro study demonstrated excellent activity of tigecycline in combination with rifampicin against cell growth in the proteinous biofilm. The BIC (biofilm inhibitory concentration) value for tigecycline/rifampicin ranged from 0.062 to 1 µg/ml, whereas for daptomycin/rifampicin from 0.125 to 2 µg/ml. These results indicated that the tigecycline/rifampicin combination was more effective against ica-independent biofilm, formed by S. haemolyticus strains, than the daptomycin/rifampicin combination. PMID:25894996

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

    PubMed

    Taxvig, Camilla; Hadrup, Niels; Boberg, Julie; Axelstad, Marta; Bossi, Rossana; Bonefeld-Jřrgensen, Eva Cecilie; Vinggaard, Anne Marie

    2013-11-01

    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. PMID:23954766

  12. Synthesis and in vitro antioxidant activity evaluation of 3-carboxycoumarin derivatives and QSAR study of their DPPH• radical scavenging activity.

    PubMed

    Martínez-Martínez, Francisco J; Razo-Hernández, Rodrigo Said; Peraza-Campos, Ana Lilia; Villanueva-García, Manuel; Sumaya-Martínez, Maria Teresa; Cano, Daniel Jaramillo; Gómez-Sandoval, Zeferino

    2012-01-01

    The in vitro antioxidant activities of eight 3-carboxycoumarin derivatives were assayed by the quantitative 1,1-diphenyl-2-picrylhydrazil (DPPH•) radical scavenging activity method. 3-Acetyl-6-hydroxy-2H-1-benzopyran-2-one (C1) and ethyl 6-hydroxy-2-oxo-2H-1-benzopyran-3-carboxylate (C2) presented the best radical-scavenging activity. A quantitative structure-activity relationship (QSAR) study was performed and correlated with the experimental DPPH• scavenging data. We used structural, geometrical, topological and quantum-chemical descriptors selected with Genetic Algorithms in order to determine which of these parameters are responsible of the observed DPPH• radical scavenging activity. We constructed a back propagation neural network with the hydrophilic factor (Hy) descriptor to generate an adequate architecture of neurons for the system description. The mathematical model showed a multiple determination coefficient of 0.9196 and a root mean squared error of 0.0851. Our results shows that the presence of hydroxyl groups on the ring structure of 3-carboxy-coumarins are correlated with the observed DPPH• radical scavenging activity effects. PMID:23519260

  13. Antagonistic Activity against Helicobacter Infection In Vitro and In Vivo by the Human Lactobacillus acidophilus Strain LB

    Microsoft Academic Search

    MARIE-HELENE COCONNIER; VANESSA LIEVIN; ELISABETH HEMERY; ALAIN L. SERVIN

    1998-01-01

    The purpose of the present study was to examine the activity of the human Lactobacillus acidophilus strain LB, which secretes an antibacterial substance(s) against Helicobacter pylori in vitro and in vivo. The spent culture supernatant (SCS) of the strain LB (LB-SCS) dramatically decreased the viability of H. pylori in vitro independent of pH and lactic acid levels. Adhesion of H.

  14. In Vitro Antioxidant Activity of Selected 4-Hydroxy-chromene-2-one Derivatives—SAR, QSAR and DFT Studies

    PubMed Central

    Mladenovi?, Milan; Mihailovi?, Mirjana; Bogojevi?, Desanka; Mati?, Sanja; Ni?iforovi?, Neda; Mihailovi?, Vladimir; Vukovi?, Nenad; Sukdolak, Slobodan; Soluji?, Slavica

    2011-01-01

    The series of fifteen synthesized 4-hydroxycoumarin derivatives was subjected to antioxidant activity evaluation in vitro, through total antioxidant capacity, 1,1-diphenyl-2-picryl-hydrazyl (DPPH), hydroxyl radical, lipid peroxide scavenging and chelating activity. The highest activity was detected during the radicals scavenging, with 2b, 6b, 2c, and 4c noticed as the most active. The antioxidant activity was further quantified by the quantitative structure-activity relationships (QSAR) studies. For this purpose, the structures were optimized using Paramethric Method 6 (PM6) semi-empirical and Density Functional Theory (DFT) B3LYP methods. Bond dissociation enthalpies of coumarin 4-OH, Natural Bond Orbital (NBO) gained hybridization of the oxygen, acidity of the hydrogen atom and various molecular descriptors obtained, were correlated with biological activity, after which we designed 20 new antioxidant structures, using the most favorable structural motifs, with much improved predicted activity in vitro. PMID:21686153

  15. In Vitro Activation of Peroxisome Proliferator Activated Receptor ? by Some Extracts from Food Materials

    Microsoft Academic Search

    CHE-YI CHAO; CHING-jANG HUANG

    Peroxisome proliferator activated receptor ? (PPAR?) is a ligand-dependent transcription factor that regulates the expression of genes involved in lipid metabolism and transport. Activators of PPAR? may be potential hypolipidemic agents, like the fibrate-type drugs. This study was therefore aimed at identifying potential hypolipidemic functional foods by screening activators of PPAR? from food materials. CHO-K1 cells were stably transfected with

  16. Preliminary phytochemical screening and in vitro antioxidant activities of Parkinsonia aculeata Linn.

    PubMed

    Sharma, Sonia; Vig, Adarsh Pal

    2014-01-01

    Butanol and hexane leaves extracts of Parkinsonia aculeata L. (Fabaceae) were assessed for its antioxidant potential by in vitro methods. Phytochemical analysis and antioxidant activity of plant extracts were studied using different in vitro assays. UPLC analysis of extracts was carried out for the identification of chemical constituents. The total phenolic contents of the butanol and hexane leaf extract were 42 mgGAE/g and 34 mgGAE/g whereas flavonoid contents of these extracts were found to be 0.044 mgRE/g and 0.005 mgRE/g, respectively. Among both extracts, butanol extract shows maximum inhibition (%) of 93.88%, 80.02%, 52.06%, 94.68%, and 69.37% in DPPH, non-site-specific and site-specific, FTC, and TBA assays and absorbance of 0.852 and 0.522 in reducing power and CUPRAC assay at the highest concentration tested. The FRAP and TAC values of butanol extract were found to be 678 ?M Fe(II)/g and 36 mgAAE/100 mg. UPLC analysis of extracts revealed the presence of various polyphenols. The tested plant extracts were found to possess potent antioxidant and free radical scavenging activity which may be due to the presence of flavonoids and polyphenols. PMID:24822217

  17. Preliminary Phytochemical Screening and In Vitro Antioxidant Activities of Parkinsonia aculeata Linn.

    PubMed Central

    Sharma, Sonia; Vig, Adarsh Pal

    2014-01-01

    Butanol and hexane leaves extracts of Parkinsonia aculeata L. (Fabaceae) were assessed for its antioxidant potential by in vitro methods. Phytochemical analysis and antioxidant activity of plant extracts were studied using different in vitro assays. UPLC analysis of extracts was carried out for the identification of chemical constituents. The total phenolic contents of the butanol and hexane leaf extract were 42?mgGAE/g and 34?mgGAE/g whereas flavonoid contents of these extracts were found to be 0.044?mgRE/g and 0.005?mgRE/g, respectively. Among both extracts, butanol extract shows maximum inhibition (%) of 93.88%, 80.02%, 52.06%, 94.68%, and 69.37% in DPPH, non-site-specific and site-specific, FTC, and TBA assays and absorbance of 0.852 and 0.522 in reducing power and CUPRAC assay at the highest concentration tested. The FRAP and TAC values of butanol extract were found to be 678??M Fe(II)/g and 36?mgAAE/100?mg. UPLC analysis of extracts revealed the presence of various polyphenols. The tested plant extracts were found to possess potent antioxidant and free radical scavenging activity which may be due to the presence of flavonoids and polyphenols. PMID:24822217

  18. Evaluation of meisoindigo, an indirubin derivative: in vitro antileukemic activity and in vivo pharmacokinetics.

    PubMed

    Huang, Meng; Lin, Hai-Shu; Lee, Ying Shiuan; Ho, Paul C

    2014-10-01

    Meisoindigo has been a routine therapeutic agent in the clinical treatment of chronic myelogenous leukemia (CML) in China since the 1980s. In the present study, the in vitro antileukemic activity of meisoindigo was investigated in acute promyelocytic leukemia (APL) cells, acute myeloid leukemia (AML) cells, and myelomonocytic leukemia cells (NB4, NB4.007/6, HL-60 and U937) comprising both retinoic acid-sensitive and retinoic acid-resistant cells. We found that meisoindigo effectively inhibited the growth and/or proliferation of these four cell types at µM levels. The effects of meisoindigo in these cells are related to its proliferation inhibition and apoptosis induction, and are independent of cell cycle arrest, indicating that meisoindigo could be possible in the treatment of APL, AML and retinoic acid resistant APL. The in vivo pharmacokinetics of meisoindigo and its major circulatory metabolites in rat plasma were then investigated by a newly developed and validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. The profiles of plasma concentration versus time were plotted and the relevant pharmacokinetic parameters were calculated for meisoindigo and its reductive metabolites. The plasma concentrations of meisoindigo after oral administration were much lower than the in vitro IC50s determined in the leukemic cells. The contradicting poor pharmacokinetic characteristics and the established clinical efficacy of meisoindigo could indicate the presence of active metabolites in vivo. PMID:25050545

  19. In vitro synergistic activity of antibiotic combinations against Brucella melitensis using E-test methodology

    PubMed Central

    Kilic, Selcuk; Dizbay, Murat; Hizel, Kenan; Arman, Dilek

    2008-01-01

    The treatment of brucellosis is still problematic, because of high rates of treatment failure or relapses. As the microorganism is an intracellular pathogen, treatment requires combined regimens. However, limited existing data on in vitro combinations are avaliable for Brucellae. The aim of this study was to investigate the in vitro efficacy of various traditional and new antibiotic combinations against 16 Brucella melitensis strains. The combination effect of antimicrobial agents was evaluated by E-test synergy method to obtain a fractional inhibitory concentration (FIC) index. Co-Trimoxazole (SXT) and moxifloxocin (MXF) exhibited the lowest MIC, while Rifampin (RIF) had the highest MIC in the study. Combinations with RIF showed the best synergistic activity (100% of RIF-tetracycline (TET), and 87.5% of RIF-SXT). Synergistic activity was also detected at seven (43.7%) of ciprofloxocin (CIP)-SXT, four (25%) of TET-MXF, and two (12.5%) of TET-SXT combinations. The combinations that demonstrated additivity were TET-SXT, CIP-SXT and TET-MXF. Antagonism was observed only with the TET-Streptomycin (STR) combination in three strains (18.8%). Further work including randomized controlled clinical trials is required to fully evaluate the usefulness of these data. PMID:24031207

  20. In vitro and in vivo antitumor activity of crude extracts obtained from Brazilian Chromobacterium sp isolates

    PubMed Central

    Menezes, C.B.A.; Silva, B.P.; Sousa, I.M.O.; Ruiz, A.L.T.G.; Spindola, H.M.; Cabral, E.; Eberlin, M.N.; Tinti, S.V.; Carvalho, J.E.; Foglio, M.A.; Fantinatti-Garboggini, F.

    2012-01-01

    Natural products produced by microorganisms have been an important source of new substances and lead compounds for the pharmaceutical industry. Chromobacterium violaceum is a Gram-negative ?-proteobacterium, abundant in water and soil in tropical and subtropical regions and it produces violacein, a pigment that has shown great pharmaceutical potential. Crude extracts of five Brazilian isolates of Chromobacterium sp (0.25, 2.5, 25, and 250?µg/mL) were evaluated in an in vitro antitumor activity assay with nine human tumor cells. Secondary metabolic profiles were analyzed by liquid chromatography and electrospray ionization mass spectrometry resulting in the identification of violacein in all extracts, whereas FK228 was detected only in EtCE 308 and EtCE 592 extracts. AcCE and EtCE 310 extracts showed selectivity for NCI/ADR-RES cells in the in vitro assay and were evaluated in vivo in the solid Ehrlich tumor model, resulting in 50.3 and 54.6% growth inhibition, respectively. The crude extracts of Chromobacterium sp isolates showed potential and selective antitumor activities for certain human tumor cells, making them a potential source of lead compounds. Furthermore, the results suggest that other compounds, in addition to violacein, deoxyviolacein and FK228, may be involved in the antitumor effect observed. PMID:23090123

  1. Synthesis and "in Vitro" Trypanocidal Activity Evaluation of Some Organo-iron Compounds.

    PubMed

    E Silva, Máfircio L A; Neto, Alberto F; Cardoso, Silvia A; Albuquerque, Sérgio; Miller, Joseph

    2002-01-01

    Eight organo-iron ferrocene derivatives and arenocenium salts were prepared and evaluated by "in vitro" assay against one strain of Trypanosoma cruzi (Y). Six of the eight organo-iron compounds assayed, piperazinium diferrocenoate 1, eta(6)-(o-xylene)-eta(5)-(cyclopentadienyl) Iron(II) hexafluorophosphate 3, eta(6)-(mesitylene)-eta(5)-(cyclopentadienyl) iron(II) hexafluorphosphate 5, eta(6)-(durene)-eta(5)-(cyclopentadienyl) iron(II) hexafluorphosphate 6, eta(6)-(rho-chlorotoluene)-eta(5)-(cyclopentadienyl) Iron(II) hexafluorphosphate 7 and eta(6)-(chlorobenzene)-eta(5)-(cyclopentadienyl) iron(II) picrate 8 , were poorly active in the "in vitro" assays. Only two compounds 1,1'-(N-pyperidinocarbonyl) ferrocene 2(IC(50)=2.4 mug/mL) and eta(6)-(o-xylene)-eta(5)(cyclopentadienyl) iron(II) picrate 4 (IC(50)=12.08 mug/mL), were more active. Thus, some of the compounds are promising to be used against Chagas' disease as a prophylactic agents. PMID:18476014

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

    PubMed Central

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

    2014-01-01

    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

  3. In vitro fasciolicide activity of some plant extracts against newly excysted flukes.

    PubMed

    Vera-Montenegro, Yolanda; Ibarra-Velarde, Froylán; Ramírez-Avila, Guillermo; Munguía-Xochihua, Javier

    2008-12-01

    The aim of the present study was to evaluate, under in vitro conditions, the activity of 20 plant extracts against newly excysted Fasciola hepatica metacercariae. The plants were selected on the basis of anthelmintic activity, traditional use, availability, solubility, and permanence in the liver. For the in vitro evaluation, 24-well Nunc-immunoplates containing RPMI-1640 culture medium bovine sera plus antibiotics were used. Extract concentrations of 500 and 50 mg/mL were placed in triplicate. Approximately 10 newly excysted flukes were placed in each well, and the plates were incubated in a CO(2) incubator at 5% atmosphere for 3 days. In each plate four control wells containing nontreated flukes were included. All procedures were undertaken under an air-flow cabinet. Efficacy was measured on days 1 and 3 by considering the motility of the live or dead trematodes evaluated with the aid of an inverted microscope. Results indicated that, from all extracts evaluated, Tilia mexicana showed an average efficacy for concentrations of 500 and 50 mg/mL, respectively, of 100 and 100%; Eriobotrya japonica, 100 and 95%; Coffea arabica, 100 and 100%; Crataegus mexicana, 95 and 90%; and Ternstroemia pringlei 100 and 100%. From this preliminary evaluation, we conclude that further and more detailed evaluations at lower concentrations should be undertaken to understand the real efficacy of these plant extracts. PMID:19120205

  4. A quantitative in vitro assay for chemical mosquito-deterrent activity without human blood cells.

    PubMed

    Klun, Jerome A; Kramer, Matthew; Zhang, Aijun; Wang, Shifa; Debboun, Mustapha

    2008-12-01

    We report that an aqueous solution containing 10(-3) M adenosine triphosphate (ATP) and citrate-phosphate-dextrose-adenine (CPDA-1) can effectively replace transfusable human red blood cells in an in vitro Klun and Debboun bioassay system for evaluating chemicals for mosquito feeding-deterrent activity, using either Aedes aegypti or Anopheles stephensi. These species fed with similar avidity through collagen membrane covering aqueous 10(-3) M ATP plus CPDA-1 or red blood cells in CPDA-1 supplemented with ATP. In a 2nd experiment, we evaluated the feeding-deterrent activity of N,N-diethyl-3-methylbenzamide and a newly discovered natural product chemical, (-)-isolongifolenone, against these 2 mosquito species. We found that the feeding-deterrent efficacy of the 2 chemicals was similar whether the feeding stimulant was red blood cells supplemented with ATP or ATP alone with CPDA-1. Since the use of human red blood cells in bioassays raises important health and logistic issues, aqueous ATP with CPDA-1 is a reasonable alternative to human blood cells for routine in vitro chemical screening. PMID:19181057

  5. Bufalin inhibits CYP3A4 activity in vitro and in vivo

    PubMed Central

    Li, Hai-yun; Xu, Wen; Zhang, Xi; Zhang, Wei-dong; Hu, Li-wei

    2009-01-01

    Aim: To investigate the inhibitory interactions of bufalin and CYP3A4. Methods: Recombinant human CYP3A4 was incubated with bufalin in vitro. Bufalin was administered ig and iv to Wistar rats to further estimate its impact on CYP3A4, and midazolam was given to index the activity of CYP3A4. Results: The IC50 of bufalin was 14.52 ?mol/L. Bufalin affected CYP3A4 activity with increases in AUC0–t and t1/2, and decreases in CL and the formation of 1-hydroxy-midazolam after ig or iv administration of midazolam (P<0.05). An increase in Cmax after ig bufalin administration (P<0.05) was observed. Conclusion: Bufalin showed a modest but significant inhibition of CYP3A4 both in vitro and in vivo. The likelihood of an interaction between bufalin and the CYP3A4-metabolized drugs in human might not be negated. PMID:19417737

  6. 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

    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

    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

  7. In vitro anti-inflammatory activity of Ligustrum vulgare extracts and their analytical characterization.

    PubMed

    Macková, Anna; Mucaji, Pavel; Widowitz, Ute; Bauer, Rudolf

    2013-11-01

    Interest in the anti-inflammatory effects of Ligustrum vulgare L., which has been used traditionally in China and Japan prompted us to determine antiinflammatory effects of the plant's compounds in leukocytes. The leaves of L. vulgare were used to prepare a decoction which was successively extracted with organic solvents (dichloromethane (DCM), n-butanol, ethyl acetate) using liquid-liquid partition. Extracts were tested for inhibition of LTB4, resp. PGE2 biosynthesis. Each extract was evaluated for its in vitro cyclooxygenase-1/2 (COX-1/2) inhibitory activity using assays with purified COX-1 and COX-2 enzymes, as well as for their LTB4 formation inhibitory activity using an assay with activated human neutrophil granulocytes. All extracts reported inhibitory actions against COXs in comparison with the synthetic inhibitors NS-398 (IC50 = 2.6 microM) and indomethacin (IC50 = 0.9 microM). The dichloromethane extract of privet leaves showed a considerable inhibitory effect against COX-1 and COX-2 enzyme activity. The DCM extract revealed 2.7 times higher inhibitory activity against LTB4 formation in comparison with the known specific LT inhibitor zileuton (IC50 = 5.0 microM). Additionally, oleuropein and echinacoside were detected by HPLC-DAD and LC-MS in the Ligustrum vulgare leaves. Both compounds exhibited weak inhibitory activity on cyclooxygenases and leukotriene formation. PMID:24427928

  8. Development of a method to quantify in vitro the synergistic activity of "natural" antimicrobials.

    PubMed

    Dufour, M; Simmonds, R S; Bremer, P J

    2003-08-25

    Despite numerous papers being published on the use of hurdle technology to control food-borne pathogens or spoilage organisms, there is no commonly accepted methodology to quantify the level of synergistic activity. This paper describes a method to quantify in vitro the synergistic activity of antibacterial agents against bacteria. Initially, a microtiter plate growth assay was used to determine the inhibitory concentrations of four "natural" antimicrobials (nisin, lauricidin, totarol, and the lactoperoxidase system (LPS)) against a panel of eight bacteria. Using the same microtiter system, the impact of various combinations of antimicrobials was assessed. The degree of synergy was based on the analysis of three criteria: (1) increase in lag phase, (2) reduction in culture density after 24 h, (3) and residual viability at 24 h. Only the lactoperoxidase system was active against all the Gram-positive and Gram-negative bacteria tested. Nisin, lauricidin, and totarol were only effective against the Gram-positive bacteria. The method successfully identified three combinations (nisin-lauricidin, LPS-nisin, and LPS-lauricidin) previously reported to have synergistic activity and highlighted the synergistic activity of two novel combinations (nisin-totarol and LPS-totarol). The development of a quick and reliable method to identify and quantify synergistic activity is a useful screening tool to establish preservative techniques that could have potential antimicrobial synergy in food-based systems. PMID:12878383

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

    PubMed Central

    Tsuchiya, Kanji; Kondo, Masahiro; Nagatomo, Hiroshi

    1978-01-01

    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

  10. Novel daidzein analogs and their in vitro anti-influenza activities.

    PubMed

    Chung, Shu-Ting; Huang, Yi-Ting; Hsiung, Hsin-Yi; Huang, Wen-Hsin; Yao, Chen-Wen; Lee, An-Rong

    2015-04-01

    A series of novel isoflavonoids were synthesized based on structural modifications of daidzein, an active ingredient of traditional Chinese medicine (TCM) and evaluated for their anti-influenza activity, in vitro, against H1N1 Tamiflu-resistant (H1N1 TR) virus in the MDCK cell line. Among them, 4-oxo-4H-1-benzopyran-8-carbaldehydes 11a-11g were most promising, and they demonstrated better activities and selectivities comparable to those the reference ribarivin, a nucleoside antiviral agent. 3-(4-Bromophenyl)-7-hydroxy-4-oxo-4H-1-benzopyran-8-carboxaldehyde (11c) displayed the best inhibitory activity (EC50 , 29.0??M) and selectivity index (SI>10.3). Analysis of the structure?activity relationships (SAR) indicated that both the non-naturally-occurring Br-substituted B-ring and appropriate CHO and OH groups on the A-ring might be critical for the activity and selectivity against H1N1 TR influenza viruses. PMID:25879510

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

    PubMed

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

    2013-09-01

    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

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

    SciTech Connect

    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

    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.

  13. Extraction of polysaccharides from Phellinus nigricans mycelia and their antioxidant activities in vitro.

    PubMed

    Wang, Zhanyong; Wang, Chenyu; Quan, Yue

    2014-01-01

    In this study, response surface methodology was employed to optimize the extraction of polysaccharides from Phellinus nigricans mycelia. A central composite design was adopted to determine optimum parameters (extraction time, extraction temperature, extraction frequency, and ratio of water to raw material) that could yield a maximum polysaccharide. Results revealed the following optimum extraction conditions: extraction time, 2.8h; ratio of water to raw material, 28; extraction frequency, 5; and extraction temperature, 95 °C. Under optimized conditions, the experimental yield of P. nigricans mycelia polysaccharides was 15.33 ± 0.21%, which is consistent with the predicted yield. The antioxidant activity assay in vitro showed that the polysaccharides exhibited a high scavenging activity against superoxide anion, hydroxyl, and 1,1-diphenyl-2-picrylhydrazyl radicals. These polysaccharides also exhibited a strong reducing power. Thus, these polysaccharides can be used as natural antioxidants in functional foods or medicine. PMID:24274486

  14. Rapid and convenient assays to assess potential inhibitory activity on in vitro hepatitis A replication.

    PubMed

    Debing, Yannick; Kaplan, Gerardo G; Neyts, Johan; Jochmans, Dirk

    2013-05-01

    Three different antiviral assays were developed for the in vitro screening of inhibitors of the hepatitis A virus (HAV) of which (i) a cytopathic effect reduction assay suitable for medium-to-high-throughput screening and (ii) two virus yield reduction assays (based on quantification of viral RNA) for genotypes IB and IIIA. The assays were validated for antiviral studies with interferon-alpha (IFN?) and amantadine HCl, two known inhibitors of HAV replication. IFN? effectively inhibited HAV replication, whereas the activity of amantadine HCl appeared to be strain-dependent. Employing these assays, we assessed the effect of the known enterovirus inhibitors pleconaril, rupintrivir and enviroxime on HAV replication. Pleconaril exhibited some very moderate activity, the effect of rupintrivir proved to be strain-dependent. Enviroxime did not inhibit HAV replication, suggesting that phosphatidylinositol-4-kinase III? is not crucial in the HAV life cycle. PMID:23528258

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

    PubMed

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

    2014-11-01

    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

  16. In vitro comparison of the photothermal anticancer activity of graphene nanoparticles and carbon nanotubes.

    PubMed

    Markovic, Zoran M; Harhaji-Trajkovic, Ljubica M; Todorovic-Markovic, Biljana M; Kepi?, Dejan P; Arsikin, Katarina M; Jovanovi?, Svetlana P; Pantovic, Aleksandar C; Drami?anin, Miroslav D; Trajkovic, Vladimir S

    2011-02-01

    The present study compared the photothermal anticancer activity of near-infrared (NIR)-excited graphene nanoparticles and carbon nanotubes (CNT). Despite lower NIR-absorbing capacity, suspension of polyvinylpyrrolidone-coated graphene sheets exposed to NIR radiation (808 nm, 2 W/cm(2)) generated more heat than DNA or sodium dodecylbenzenesulfonate-solubilized single-wall CNT under the same conditions. Accordingly, graphene nanoparticles performed significantly better than CNT in inducing photothermal death of U251 human glioma cells in vitro. The superior photothermal sensitivity of graphene sheets could be largely explained by their better dispersivity, which has been supported by a simple calculation taking into account thermodynamic, optical and geometrical properties of the two type of carbon nanoparticles. The mechanisms of graphene-mediated photothermal killing of cancer cells apparently involved oxidative stress and mitochondrial membrane depolarization resulting in mixed apoptotic and necrotic cell death characterized by caspase activation/DNA fragmentation and cell membrane damage, respectively. PMID:21071083

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

    PubMed

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

    2011-01-01

    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

  18. Evaluation of in Vitro and in Vivo Depigmenting Activity of Raspberry Ketone from Rheum officinale

    PubMed Central

    Lin, Chia-Hsiang Victor; Ding, Hsiou-Yu; Kuo, Shiou-Yi; Chin, Ling-Wei; Wu, Jiumn-Yih; Chang, Te-Sheng

    2011-01-01

    Melanogenesis inhibition by raspberry ketone (RK) from Rheum officinale was investigated both in vitro in cultivated murine B16 melanoma cells and in vivo in zebrafish and mice. In B16 cells, RK inhibited melanogenesis through a post-transcriptional regulation of tyrosinase gene expression, which resulted in down regulation of both cellular tyrosinase activity and the amount of tyrosinase protein, while the level of tyrosinase mRNA transcription was not affected. In zebrafish, RK also inhibited melanogenesis by reduction of tyrosinase activity. In mice, application of a 0.2% or 2% gel preparation of RK applied to mouse skin significantly increased the degree of skin whitening within one week of treatment. In contrast to the widely used flavoring properties of RK in perfumery and cosmetics, the skin-whitening potency of RK has been demonstrated in the present study. Based on our findings reported here, RK would appear to have high potential for use in the cosmetics industry. PMID:21954327

  19. Design, synthesis and in vitro trypanocidal and leishmanicidal activities of novel semicarbazone derivatives.

    PubMed

    Alves, Marina A; de Queiroz, Aline C; Alexandre-Moreira, Magna Suzana; Varela, Javier; Cerecetto, Hugo; González, Mercedes; Doriguetto, Antonio C; Landre, Iara M; Barreiro, Eliezer J; Lima, Lídia M

    2015-07-15

    Trypanosomatids are protozoan parasites that cause various diseases in human, such as leishmaniasis, Chagas disease and sleeping sickness. The highly syntenic genomes of the trypanosomatid species lead the assumption that they can encode similar proteins, indicating the possibility to design new antitrypanosomatid drugs with dual trypanosomicidal and leishmanicidal activities. In this work a series of compounds (6a-h and 7a-h), containing a semicarbazone scaffold as a peptide mimetic framework, was designed and synthesized. From this series compound 7g (LASSBio-1483) highlighted, showing dual in vitro trypanosomicidal and leishmanicidal activities, with potency similar to the standard drugs nifurtimox and pentamidine. This data, taken together with its good in silico druglikeness profile and its great chemical and plasma stability, make LASSBio-1483 (7g) a new antitrypanosomatid lead-candidate. PMID:26069927

  20. N-acetylphenylisoserinates of Lactarius sesquiterpenoid alcohols--cytotoxic, antiviral, antiproliferative and immunotropic activities in vitro.

    PubMed

    Krawczyk, Ewa; Kniotek, Monika; Nowaczyk, Maria; Dzieciatkowski, Tomasz; Przybylski, Maciej; Majewska, Anna; Luczak, Miroslaw

    2006-06-01

    In the present study a new group of derivatives of both paclitaxel and Lactarius sesquiterpenes, the N-acetylphenylisoserinates of Lactarius sesquiterpenoid alcohols, was tested for antiviral, cytotoxic, antiproliferative and immunotropic activities in vitro. Among the 13 compounds tested two, isolactarorufin 8-[ N-acetyl-(2' R,3' S)-3'-phenylisoserinate] and 3-O-ethylfurandiol 8-[ N-acetyl-(2' R,3' S)-3'-phenylisoserinate] inhibited Herpes simplex virus type 1 (HSV-1) replication at low cytotoxic concentrations. Selectivity indices were: > 12.2 and > 106.4, respectively. Both compounds decreased also the number of cell divisions. Mitotic indices of the cells submitted to these compounds were: 96/2000 and 48/1000, respectively, in comparison with control (169/2000). It seems that the antimitotic action of the compounds may be associated with their antiviral activity. Moreover, isolactarorufin 8-[ N-acetyl-(2' R,3' S)-3'-phenylisoserinate] inhibited PHA-induced T lymphocyte proliferation. PMID:16636965

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

    PubMed

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

    2010-02-01

    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

  2. In vitro antimicrobial activity of a new antiseptic central venous catheter.

    PubMed

    Li, C; Zhang, X; Whitbourne, R

    1999-01-01

    A central venous catheter coated with a new antiseptic combination, silver chloride (AgCl) and benzalkonium chloride (BKC) in a polymer matrix, was developed. The antimicrobial efficacy and the ability to prevent surface colonization, after elution in both serum and saline, were evaluated and compared to catheters coated with silver sulfadiazine/chlorhexidine. The results of in vitro assays demonstrated that the AgCl-BKC coated catheters had a broad spectrum of activity against bacteria and C. albicans and prolonged antimicrobial activity for extraction periods of up to 30 days. These data suggest that AgCl-BKC coated catheters may provide another solution for reduction of catheter-related infections. PMID:9934626

  3. Triazole derivatives with improved in vitro antifungal activity over azole drugs

    PubMed Central

    Yu, Shichong; Chai, Xiaoyun; Wang, Yanwei; Cao, Yongbing; Zhang, Jun; Wu, Qiuye; Zhang, Dazhi; Jiang, Yuanying; Yan, Tianhua; Sun, Qingyan

    2014-01-01

    A series of triazole antifungal agents with piperidine side chains was designed and synthesized. The results of antifungal tests against eight human pathogenic fungi in vitro showed that all the compounds exhibited moderate-to-excellent activities. Molecular docking between 8d and the active site of Candida albicans CYP51 was provided based on the computational docking results. The triazole interacts with the iron of the heme group. The difluorophenyl group is located in the S3 subsite and its fluorine atom (2-F) can form H-bonds with Gly307. The side chain is oriented into the S4 subsite and formed hydrophobic and van der Waals interactions with the amino residues. Moreover, the phenyl group in the side chain interacts with the phenol group of Phe380 through the formation of ?–? face-to-edge interactions. PMID:24748772

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

    PubMed

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

    2000-07-01

    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

  5. In vivo anti-inflammatory and in vitro antioxidant activities of Mediterranean dietary plants.

    PubMed

    Conforti, Filomena; Sosa, Silvio; Marrelli, Mariangela; Menichini, Federica; Statti, Giancarlo A; Uzunov, Dimitar; Tubaro, Aurelia; Menichini, Francesco; Loggia, Roberto Della

    2008-02-28

    Five hydroalcoholic extracts of edible plants from Calabria region (Italy) used in local traditional medicine for the treatment of inflammatory diseases were evaluated for their in vivo topical anti-inflammatory activity (inhibition of croton oil-induced ear oedema in mice) and in vitro antioxidant and antiradical properties (inhibition of linoleic acid oxidation and bovine brain liposomes peroxidation, DPPH radical scavenging). All the extracts showed an anti-inflammatory effect: 300 microg/cm(2) provoked oedema reductions ranging from 21 to 27%. All the extracts exerted also radical scavenging and/or antioxidant properties, the most active plant being Mentha aquatica L. (Lamiaceae) which contained the highest amount of phenolics (337 mg/g) and of flavonoids (15.75 mg/g). Moreover, the content and the composition of sterols were assessed by GC-MS in the examined plants Borago officinalis L. (Boraginaceae) contained the highest number of sterols. PMID:18164564

  6. Antioxidant and antitumor activities in vitro of polysaccharides from E. sipunculoides.

    PubMed

    He, Rongjun; Zhao, Yuejun; Zhao, Ruina; Sun, Peilong

    2015-07-01

    Three polysaccharides (SAP30, SAP60 and SAP80) were separated from the body of Edwardsia sipunculoides by tissue homogenate and papain hydrolysis. Total soluble sugar contents, monosaccharide compositions, antioxidant and antitumor activities in vitro of those polysaccharides were investigated, respectively. Results showed that the total soluble sugar contents of SAP composed of Man, GlcN, Rha, GalN, GlcUA, Glc, Gal, Xyl and Fuc were more than 85% estimated by the phenol-sulfuric acid assay. In addition, SAP had potential antioxidant and antitumor activities. SAP30 has the most significant antitumor effect. This study suggested that SAP could be a potential natural antioxidants and antitumor agents. PMID:25834926

  7. Inhibition of iron induced lipid peroxidation and antioxidant activity of Indian spices and Acacia in vitro.

    PubMed

    Yadav, Amit Singh; Bhatnagar, Deepak

    2010-03-01

    The spices used in the Indian foods such as Star anise (Illicium verum), Bay leaves (Cinnamomum zeylanicum) and Cobra's saffron (Mesua ferrea), and Acacia (Acacia catechu), which have medicinal value, were used as test samples, to find their effect on in vitro lipid peroxidation (LPO). Rat liver post mitochondrial supernatant (PMS) in Tris HCl buffer, pH 7.4 was incubated for 0 and 1 h, with various test extracts in three different oxidant systems. The results show that addition of test samples to FeCl(3) medium at 0 h significantly stop the initiation of the LPO. However, the propagation phase of LPO was inhibited by Cobra's saffron and Acacia and not by Star anise and Bay leaves. The test samples also showed strong reducing power and superoxide radical scavenging activity. Cobra's saffron and Acacia showed the highest antioxidant activity, probably due to the higher polyphenol content as compared to other test samples. PMID:20033297

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

    PubMed Central

    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

    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

  9. Optimization of ultrasonic-assisted extraction and in vitro antioxidant activities of polysaccharides from Trametes orientalis.

    PubMed

    Zheng, Yi; Li, Yong; Wang, Wei-dong

    2014-10-13

    A Box-Behnken design was employed to optimize ultrasonic-assisted extraction of Trametes orientalis polysaccharides (TOP). The crude polysaccharides were purified by DEAE cellulose-52 chromatography, giving a main fraction named as PTOP. The antioxidant properties of PTOP were evaluated by different in vitro antioxidant assays, such as 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities, reducing power, superoxide radical scavenging activities, and chelating ability of ferrous ions. The results showed that optimal extraction parameters were as follows: ratio of water to raw material 30.6 mL/g, ultrasonic power 109.8 W, extraction temperature 40.2 °C, and extraction time 42.2 min. Under these conditions, the experimental yield of polysaccharides was 7.49 ± 0.14%, which agreed closely with the predicted value (7.47%). Furthermore, PTOP exhibited antioxidant capacity in a concentration-dependent manner in all assays. PMID:25037357

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

    PubMed

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

    2014-07-01

    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

  11. Impact of fibroblast activation protein on osteosarcoma cell lines in vitro

    PubMed Central

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

    2014-01-01

    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

  12. The Effect of Bioactive Compounds on In Vitro and In Vivo Antioxidant Activity of Different Berry Juices

    PubMed Central

    Slatnar, Ana; Jakopic, Jerneja; Stampar, Franci; Veberic, Robert; Jamnik, Polona

    2012-01-01

    Background Berry fruit is known for its high contents of various bioactive compounds. The latter constitute of anthocyanins, flavonols and flavanols and posses high antioxidative activity. The highly dynamic antioxidant system can be evaluated in vitro and in vivo in several model organisms. These measurements represent a good approximation of the real potential of bioactive compounds in the cells of higher eucarions. The aim of the study was thus to determine in vitro and in vivo antioxidant activity of different berry juices, which reportedly contain high amounts of phenolics. Methodology/Principal Findings Five different berry species were collected from several locations in central Slovenia and juice was extracted from each species separately. Juice was assessed for their in vitro and in vivo antioxidant activity. Phenolic profiles of berries were determined with the use of a HPLC/MS system, in vitro antioxidant activity with the DPPH radical scavenging method and in vivo antioxidative activity using Saccharomyces cerevisiae. The highest diversity of individual phenols was detected for bilberry juice. The highest in vitro antioxidant capacity was determined for blackcurrant juice. A decrease in intracellular oxidation compared to control was observed in the following order: blackcurrant < chokeberry?=?blueberry < bilberry. The results indicate important differences in antioxidant activity of berry juices between in vitro and in vivo studies. Conclusion/Significance In addition to the total content of phenolic compounds entering the cells, a key factor determining antioxidative activity of berry juices is also the ratio between the compounds. Where high content levels of anthocyanins and very low content levels of flavonols and hydroxycinnamic acids were measured a lower intracellular oxidation has been detected. Specifically, intracellular oxidation increased with higher consumption of hydroxycinnamic acids and lower consumption of anthocyanins in the cells. Antioxidative activity also increased when the consumption of analyzed phenols was rather low. PMID:23110118

  13. Evaluation of antimicrobial activity of extracts of in vivo and in vitro grown Vinca rosea L. (Catharanthus roseus) against pathogens.

    PubMed

    Naz, Shagufta; Haq, Rukhama; Aslam, Farah; Ilyas, Saiqa

    2015-05-01

    The antimicrobial activity of Vinca rosea was evaluated against pathogenic bacterial strains (Bacillus subtilis, B. licheniformis and Azotobacter sp.) and fungal strains (Asprgillus niger, Alternaria solani and Rhizopus oryzae) using agar well diffusion method. Methanolic extracts of in vivo leaf, in vitro leaf, in vitro calluses of leaf, nodal and fruit explants were used and exhibited antimicrobial activity as indicated by minimum inhibitory concentration (MIC). In vitro extracts showed better results as compared to the in vivo extracts for both the antibacterial as well as the antifungal activity. Among all the extracts, maximum zone of inhibition (30.3 mm ± 0.58(a)) was formed by in vitro leaf callus extract concentration of 2.0mg/ml against B. licheniformis. Similarly in case of antifungal activity, maximum zone of inhibition (34.6mm ± 0.57(a)) was formed by in vitro leaf callus extract and MIC value is 6.0mg/ml against A. niger. Hence these results clearly depicts that V. rosea possess a great strength to fight against the microbial activity and can be used against various infections. PMID:26004716

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

    PubMed

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

    2013-01-01

    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

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

    PubMed Central

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

    2013-01-01

    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

  16. Comparison of In Vitro Activities of 17 Antifungal Drugs against a Panel of 20 Dermatophytes by Using a Microdilution Assay

    PubMed Central

    Favre, Bertrand; Hofbauer, Bettina; Hildering, Kwang-Soo; Ryder, Neil S.

    2003-01-01

    The in vitro activities of 17 antifungal drugs against a panel of 20 dermatophytes comprising 6 different species were determined using a microdilution assay according to the NCCLS M38-P method with some modifications. Terbinafine was the most potent systemic drug while tolnaftate and amorolfine were the most active topical agents. PMID:14532230

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

    Microsoft Academic Search

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

    2009-01-01

    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

  18. Characterization of the Sensitizing Potential of Chemicals by In Vitro Analysis of Dendritic Cell Activation and Skin Penetration

    Microsoft Academic Search

    Pierre Aeby; Christoph Wyss; Heinz Beck; Peter Griem; Heike Scheffler; Carsten Goebelw

    2004-01-01

    Development of in vitro models to identify sensitizing chemicals receives public interest since animal testing should be avoided whenever possible. In this article we analyze two essential properties of sensitizing chemicals: skin penetration and dendritic cell (DC) activation. Activation of immature DC derived from peripheral blood monocytes was evaluated by flow cytometric analysis of CD86 positive cells and quantitative measurement

  19. In vitro antimicrobial activity of GSQ1530, a new heteroaromatic polycyclic compound.

    PubMed

    Ge, Yigong; Difuntorum, Stacey; Touami, Sofia; Critchley, Ian; Bürli, Roland; Jiang, Vernon; Drazan, Ken; Moser, Heinz

    2002-10-01

    GSQ1530 is a compound derived from a newly identified class of antibiotics referred to as heteroaromatic polycyclic (HARP) antibiotics. The aim of this study was to assess the in vitro antimicrobial activity of GSQ1530. By using an NCCLS broth microdilution assay, the activities of GSQ1530 and other antibiotics were coevaluated against 215 clinical isolates. The MICs at which 90% of isolates are inhibited (MIC(90)s) of GSQ1530 for methicillin-susceptible Staphylococcus aureus and methicillin-resistant S. aureus (MRSA) were 2 and 4 micro g/ml, respectively. The MIC(90)s of GSQ1530 for the streptococci tested were 2 micro g/ml or less, regardless of their susceptibilities to other antibiotics. The MIC(90) of GSQ1530 for the enterococci tested (including vancomycin-resistant enterococci) was 4 micro g/ml. No cross-resistance was found between GSQ1530 and other known antibiotics. In a separate assay, GSQ1530 demonstrated excellent activity against vancomycin-intermediate-susceptible staphylococci (MIC(90), 1 micro g/ml). The minimal bactericidal concentration test was conducted with 73 clinical isolates; GSQ1530 was cidal against streptococci and staphylococci but static against enterococci. An in vitro killing kinetic study revealed a time-dependent profile, with at least a 3-log reduction of bacterial growth within 6 h after exposure to four times the MICs of GSQ1530 for both S. aureus and Streptococcus pneumoniae. The checkerboard study showed that GSQ1530 had a synergistic interaction with rifampin against MRSA. The test medium was found to have little effect on in vitro antimicrobial potency. The MICs of GSQ1530 for gram-positive cocci were 4- to 32-fold higher in the presence of serum proteins. GSQ1530 has high levels of plasma protein binding (91 and 89% for rat and human plasma, respectively). These preliminary results demonstrate that GSQ1530, a representative compound of our novel HARP antibiotics, has broad-spectrum activity against gram-positive bacteria. This novel class of antibacterial compounds is profiled in vivo to assess the therapeutic potential in humans. Ongoing in vivo studies will assess whether this class of molecules has promising in vivo efficacy and safety profiles. PMID:12234840

  20. Evaluation of in vitro antioxidant, antimicrobial, genotoxic and anticancer activities of lichen Cetraria islandica.

    PubMed

    Gruji?i?, Darko; Stoši?, Ivana; Kosani?, Marijana; Stanojkovi?, Tatjana; Rankovi?, Branislav; Miloševi?-Djordjevi?, Olivera

    2014-10-01

    In this study, the antioxidant, antimicrobial, genotoxic and anticancer activities of Cetraria islandica methanol extract were determined by using free radical and superoxide anion scavenging activity, reducing power, determination of total phenolic compounds and flavonoid contents, broth microdilution minimal inhibitory concentration against five bacterial and five fungal species, cytokinesis block micronucleus (MN) assay on peripheral blood lymphocytes (PBLs) and the microculture tetrazolium test on FemX (human melanoma) and LS174 (human colon carcinoma) cell lines. As a result of the study, we found that C. islandica methanol extract exhibited moderate free-radical-scavenging activity with IC50 values 678.38 ?g/ml. Moreover, the tested extract had effective reducing power and superoxide anion radical scavenging. The minimal inhibitory concentration values against the tested microorganisms ranged from 0.312 to 5 mg/ml. The extract increased MN frequency in a dose dependent manner, but it was significant in higher tested concentrations (50, 100 and 200 ?g/ml). No significant differences were observed between NDI values in all treatments and untreated PBLs. In addition, the tested extract had strong anticancer activity towards both cell lines with IC50 values of 22.68 and 33.74 ?g/ml. It can be concluded that the tested extract exhibited a certain level of in vitro antioxidant, antimicrobial, genotoxic and anticancer activities. PMID:24590925

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

    PubMed

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

    2014-06-01

    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

  2. In Vitro and In Vivo Activities of Three Oxazolidinones against Nonreplicating Mycobacterium tuberculosis

    PubMed Central

    Zhang, Ming; Sala, Claudia; Dhar, Neeraj; Vocat, Anthony; Sambandamurthy, Vasan K; Sharma, Sreevalli; Marriner, Gwendolyn; Balasubramanian, V.

    2014-01-01

    Oxazolidinones represent a new class of antituberculosis drugs that exert their function by inhibiting protein synthesis. Here, we compared the activities of three oxazolidinones, linezolid, PNU-100480, and AZD5847, against latent tuberculosis using a simple model employing the streptomycin-starved Mycobacterium tuberculosis strain 18b. The in vitro drug susceptibility results showed that the three oxazolidinones had a bacteriostatic effect against actively growing bacilli but potent bactericidal activity against nonreplicating cells. In the murine model of latent infection with M. tuberculosis 18b, the efficacy of the three compounds varied greatly. Indeed, AZD5847 or its prodrug exhibited no activity or only modest activity, respectively, after 2 months of treatment, whereas both linezolid and PNU-100480 were effective against latent bacilli in mice and showed promising outcomes in combination therapy with rifampin. Moreover, the potency of PNU-100480 was significantly greater than that of linezolid, making it an attractive drug candidate in the development of new combination therapies for latent tuberculosis. PMID:24663022

  3. In Vitro Activities of the Multifunctional RNA Silencing Polymerase QDE-1 of Neurospora crassa*

    PubMed Central

    Aalto, Antti P.; Poranen, Minna M.; Grimes, Jonathan M.; Stuart, David I.; Bamford, Dennis H.

    2010-01-01

    QDE-1 is an RNA- and DNA-dependent RNA polymerase that has functions in the RNA silencing and DNA repair pathways of the filamentous fungus Neurospora crassa. The crystal structure of the dimeric enzyme has been solved, and the fold of its catalytic core is related closely to that of eukaryotic DNA-dependent RNA polymerases. However, the specific activities of this multifunctional enzyme are still largely unknown. In this study, we characterized the in vitro activities of the N-terminally truncated QDE-1?N utilizing structure-based mutagenesis. Our results indicate that QDE-1 displays five distinct catalytic activities, which can be dissected by mutating critical amino acids or by altering reaction conditions. Our data also suggest that the RNA- and DNA-dependent activities have different modes for the initiation of RNA synthesis, which may reflect the mechanism that enables the polymerase to discriminate between template nucleic acids. Moreover, we show that QDE-1 is a highly potent terminal nucleotidyltransferase. Our results suggest that QDE-1 is able to regulate its activity mode depending on the template nucleic acid. This work extends our understanding of the biochemical properties of the QDE-1 enzyme and related RNA polymerases. PMID:20647305

  4. Fast oscillatory activity induced by kainate receptor activation in the rat basolateral amygdala in vitro.

    PubMed

    Randall, Fiona E; Whittington, Miles A; Cunningham, Mark O

    2011-03-01

    The basolateral amygdala (BLA) has a fundamental role in affective processing. In vivo studies have revealed rhythmic population activity of a similar type to that seen in the hippocampus and cortical areas during learning tasks. The amygdala contains densely interconnected networks of inhibitory interneurons similar to those responsible for fast network activity generation in the hippocampus and other cortical structures. Here we report that neuronal networks of the BLA in isolation generate persistent, gamma frequency (30-80 Hz) oscillations upon kainate receptor activation with kainic acid. We show that, like other cortical structures, BLA oscillations are completely dependent upon ?-aminobutyric acid (GABA)ergic inhibition. GABA(A) receptor blockade abolished all oscillations, and the activity was also sensitive to the barbiturate, pentobarbital. Blockade of ?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors or N-methyl-D-aspartate (NMDA) receptors had no significant effect on gamma activity. However, the GluR5-containing kainate receptor-specific antagonist (S)-1-(2-amino-2-carboxyethyl)-3-(2-carboxybenzyl) pyrimidine-2,4-dione (UBP302) abolished oscillations-evidence that glutamatergic receptor involvement is predominantly kainate receptor mediated. The mixed AMPA/kainate receptor antagonist 6-nitro-7-sulphamoylbenzo[f]quinoxalone-2,3-dione disodium (NBQX) abolished all oscillatory activity in 8/14 of slices tested. In the remaining slices, gamma frequency activity was abolished to reveal a low-amplitude, NMDA receptor-dependent, beta frequency (10-20 Hz) oscillation. Gamma oscillations are abolished by gap junction blockade. While these data show the BLA capable of generating gamma rhythms in common with other cortical areas studied to date, the network mechanisms appear to be different, suggesting a unique network structure underlies amygdala rhythmogenesis. Understanding how BLA networks produce synchronous activity is paramount to understanding how the BLA executes influence on important cognitive processes such as emotional learning. PMID:21255131

  5. In Vitro and In Vivo Activities of Chios Mastic Gum Extracts and Constituents against Helicobacter pylori?

    PubMed Central

    Paraschos, Sotirios; Magiatis, Prokopios; Mitakou, Sofia; Petraki, Kalliopi; Kalliaropoulos, Antonios; Maragkoudakis, Petros; Mentis, Andreas; Sgouras, Dionyssios; Skaltsounis, Alexios-Leandros

    2007-01-01

    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

  6. An in Vitro Antimicrobial Activity of Ten Iranian-Made Toothpastes

    PubMed Central

    Sadeghi, Mostafa; Assar, Shokrollah

    2009-01-01

    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

  7. In vitro and in vivo antiplasmodial activity of three Rwandan medicinal plants and identification of their active compounds.

    PubMed

    Muganga, Raymond; Angenot, Luc; Tits, Monique; Frédérich, Michel

    2014-04-01

    In our previous study, we reported the interesting in vitro antiplasmodial activity of some Rwandan plant extracts. This gave rise to the need for these extracts to also be evaluated in vivo and to identify the compounds responsible for their antiplasmodial activity. The aim of our study was, on the one hand, to evaluate the antiplasmodial activity in vivo and the safety of the selected Rwandan medicinal plants used in the treatment of malaria, with the objective of promoting the development of improved traditional medicines and, on the other hand, to identify the active ingredients in the plants. Plant extracts were selected according to their selectivity index. The in vivo antiplasmodial activity of aqueous, methanolic, and dichloromethane extracts was then evaluated using the classical 4-day suppressive test on Plasmodium berghei infected mice. The activity of the plant extracts was estimated by measuring the percentage of parasitemia reduction, and the survival of the experimental animals was recorded. A bioguided fractionation was performed for the most promising plants, in terms of antiplasmodial activity, in order to isolate active compounds identified by means of spectroscopic and spectrometric methods. The highest level of antiplasmodial activity was observed with the methanolic extract of Fuerstia africana (>?70?%) on days 4 and 7 post-treatment after intraperitoneal injection and on day 7 using oral administration. After oral administration, the level of parasitemia reduction observed on day 4 post-infection was 44?% and 37?% with the aqueous extract of Terminalia mollis and Zanthoxylum chalybeum, respectively. However, the Z. chalybeum extract presented a high level of toxicity after intraperitoneal injection, with no animals surviving on day 1 post-treatment. F. africana, on the other hand, was safer with 40?% mouse survival on day 20 post-treatment. Ferruginol is already known as the active ingredient in F. Africana, and ellagic acid (IC50?=?175?ng/mL) and nitidine (IC50?=?77.5?ng/mL) were identified as the main active constituents of T. mollis and Z. chalybeum, respectively. F. africana presented very promising antiplasmodial activity in vivo. Although most of the plants tested showed some level of antiplasmodial activity, some of these plants may be toxic. This study revealed for the first time the role of ellagic acid and nitidine as the main antimalarial compounds in T. mollis and Z. chalybeum, respectively. PMID:24710900

  8. Virtual Screening Analysis and In-vitro Xanthine Oxidase Inhibitory Activity of Some Commercially Available Flavonoids

    PubMed Central

    Umamaheswari, Muthuswamy; Madeswaran, Arumugam; Asokkumar, Kuppusamy

    2013-01-01

    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

  9. In vitro activities of voriconazole in combination with three other antifungal agents against Candida glabrata.

    PubMed

    Barchiesi, Francesco; Spreghini, Elisabetta; Maracci, Monia; Fothergill, Annette W; Baldassarri, Isabella; Rinaldi, Michael G; Scalise, Giorgio

    2004-09-01

    Candida glabrata has recently emerged as a significant pathogen involved in both superficial and deep-seated infections. In the present study, a checkerboard broth microdilution method was performed to investigate the in vitro activities of voriconazole (VOR) in combination with terbinafine (TRB), amphotericin B (AMB), and flucytosine (5FC) against 20 clinical isolates of C. glabrata. Synergy, defined as a fractional inhibitory concentration (FIC) index of < or = 0.50, was observed in 75% of VOR-TRB, 10% of VOR-AMB, and 5% of VOR-5FC interactions. None of these combinations yielded antagonistic interactions (FIC index > 4). When synergy was not achieved, there was still a decrease in the MIC of one or both drugs used in the combination. In particular, the MICs were reduced to < or = 1.0 microg/ml as a result of the combination for all isolates for which the AMB MIC at the baseline was > or = 2.0 microg/ml. By a disk diffusion assay, the halo diameters produced by antifungal agents in combination were greater that those produced by each drug alone. Finally, killing curves showed that VOR-AMB exhibited synergistic interactions, while VOR-5FC sustained fungicidal activities against C. glabrata. These studies demonstrate that the in vitro activity of VOR against this important yeast pathogen can be enhanced upon combination with other drugs that have different modes of action or that target a different step in the ergosterol pathway. Further studies are warranted to elucidate the potential beneficial effects of such combination regimens in vivo. PMID:15328091

  10. In vitro antibacterial activity of some Iranian medicinal plant extracts against Helicobacter pylori.

    PubMed

    Hajimahmoodi, M; Shams-Ardakani, M; Saniee, P; Siavoshi, F; Mehrabani, M; Hosseinzadeh, H; Foroumadi, P; Safavi, M; Khanavi, M; Akbarzadeh, T; Shafiee, A; Foroumadi, A

    2011-07-01

    Helicobacter pylori infection causes lifelong chronic gastritis, which can lead to peptic ulcer, mucosa-associated lymphoid tissue (MALT) lymphoma and gastric cancer. The growing problem of antibiotic resistance by the organism demands the search for novel candidates from plant-based sources. In the present study, we evaluated the in vitro anti-H. pylori activity of some selected medicinal plants on clinical isolates of H. pylori. Gastric biopsy samples were obtained from patients presenting with gastroduodenal complications. Helicobacter pylori was isolated from the specimens following standard microbiology procedures. The disc-diffusion method was used to determine the susceptibility of three H. pylori isolates to methanol extracts of 23 Iranian plants. All tests were performed in triplicate. Among them, the extracts of Punica granatum and Juglans regia had remarkable anti-H. pylori activity with mean of inhibition zone diameter of 39 and 16?mm at 100?µg?disc?ą, respectively. In view of the results obtained with P. granatum (pomegranate), the peel extracts of nine cultivars of pomegranate (Shirin-e-Pust Sefid, Agha Mohammad Ali-e-Shirin, Sefid-e-Shomal, Sefid-e-Torsh, Shirin-e-Malase, Tabestani-e-Torsh, Shirin-e-Saveh Malase, Alak-e-Shirin, Pust Siyah) were further assayed against the clinical isolates of H. pylori. The results revealed that all Iranian pomegranate cultivars, except for Alak-e-Shirin, showed significant in vitro anti-H. pylori activity against the clinical isolates of H. pylori (mean of inhibition zone diameter ranging from 16 to 40 mm at 50 µg disc?ą). PMID:21726128

  11. Shc depletion stimulates brown fat activity in vivo and in vitro

    PubMed Central

    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

    2014-01-01

    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

  12. Virtual Screening Analysis and In-vitro Xanthine Oxidase Inhibitory Activity of Some Commercially Available Flavonoids.

    PubMed

    Umamaheswari, Muthuswamy; Madeswaran, Arumugam; Asokkumar, Kuppusamy

    2013-01-01

    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

  13. A new in vitro invasion model for oral cancer using an acellular allogenic dermal matrix (Alloderm): the relationship among in vitro invasion activity, in vivo invasion and metastasis.

    PubMed

    Takahashi, Hidenori; Shigeta, Takashi; Umeda, Masahiro; Komori, Takahide

    2011-01-01

    The purpose of this study was to develop a new in vitro model of cancer invasion using a human dermal equivalent, AlloDerm®. A squamous cell carcinoma line (HSC-2, HSC-3 and OSC20) and a malignant melanoma line (G361) were cultured on AlloDerm® and evaluated histologically to examine destruction of the basement membrane and invasion into the dermis of AlloDerm®. HSC-3 and G361 cells invaded through the basement membrane of AlloDerm® at 21-28 days after seeding, while HSC-2 and OSC20 cells did not. Next, these cells were transplanted into the tongues of nude mice, and the degree of local invasiveness was examined histologically. HSC-3 and G361 cells invaded diffusely to the surrounding tongue tissue, although HSC-2 and OSC20 showed only expansive growth. Further, these cells were transplanted subcutaneously in nude mice to study metastatic activity. Regional and distant metastases were rarely observed after transplantation of HSC-2 and OSC20 cells. On the other hand, HSC-3 and G361 cells frequently metastasized. These findings show a close relationship among in vitro invasiveness on AlloDerm®, in vivo invasiveness, and metastatic activity. This experimental model using AlloDerm® is a potentially new in vitro model of cancer invasion. PMID:22971983

  14. Inhibition of rabbit platelet activation in vitro by antagonists of platelet-activating factor (PAF)

    SciTech Connect

    Cox, C.P.; Wood, K.L.

    1986-03-05

    The authors used washed, (/sup 3/H)serotonin-labeled rabbit platelets to study the in vitro aggregation and secretion responses induced by graded doses of PAF in the presence or absence of specific antagonists of PAF. These antagonists included CV-3988, L-652,731, triazolam and alprazolam. Platelets were pretreated with either an antagonist or the appropriate diluent for 60 sec prior to the addition of PAF (2 x 10/sup -10/ to 2 x 10/sup -7/ M). Aggregation was monitored continuously and recorded as the height of the aggregation tracing at 60 sec post-PAF. Secretion of (/sup 3/H)-serotonin was measured in a sample of the platelets removed at 60 sec post-PAF. When 2 x 10/sup -10/ M PAF was used as the stimulus, the concentration of antagonist needed for 50% inhibition (IC/sub 50/) of secretion was obtained at 0.05 ..mu..M, 0.15 ..mu..M, 0.6 ..mu..M and 2.5 ..mu..M, respectively, for L-652,731, CV-3988, triazolam and alprazolam. The corresponding IC/sub 50/ for aggregation was obtained at 0.2 ..mu..M, 0.1 ..mu..M, 1.5 ..mu..M and 6.5 ..mu..M, respectively. The inhibitory effects of these antagonists could be overcome by increasing the dose of PAF used. Although all of the antagonists were capable of completely inhibiting platelet aggregation and secretion, L-652,731 was the most potent PAF antagonist on a molar basis.

  15. In Vitro Activity of S-3578, a New Broad-Spectrum Cephalosporin Active against Methicillin-Resistant Staphylococci

    PubMed Central

    Fujimura, Takaji; Yamano, Yoshinori; Yoshida, Isamu; Shimada, Jingoro; Kuwahara, Shogo

    2003-01-01

    The in vitro antibacterial activity of S-3578, a new parenteral cephalosporin, against clinical isolates was evaluated. The MICs of the drug at which 90% of the isolates were inhibited were 4 ?g/ml for methicillin-resistant Staphylococcus aureus (MRSA) and 2 ?g/ml for methicillin-resistant Staphylococcus epidermidis, which were fourfold higher than and equal to those of vancomycin, respectively. The anti-MRSA activity of S-3578 was considered to be due to its high affinity for penicillin-binding protein 2a (50% inhibitory concentration, 4.5 ?g/ml). In time-kill studies with 10 strains each of MRSA and methicillin-susceptible S. aureus, S-3578 caused more than a 4-log10 decrease of viable cells on the average at twice the MIC after 24 h of exposure, indicating that it had potent bactericidal activity. Furthermore, in population analysis of MRSA strains with heterogeneous or homogeneous resistance to imipenem, no colonies emerged from about 109 cells on agar plates containing twice the MIC of S-3578, suggesting the low frequency of emergence of S-3578-resistant strains from MRSA. S-3578 was also highly active against penicillin-resistant Streptococcus pneumoniae (PRSP), with a MIC90 of 1 ?g/ml, which was comparable to that of ceftriaxone. S-3578 also had antibacterial activity against a variety of gram-negative bacteria including Pseudomonas aeruginosa, though its activity was not superior to that of cefepime. In conclusion, S-3578 exhibited a broad antibacterial spectrum and, particularly, had excellent activity against gram-positive bacteria including methicillin-resistant staphylococci and PRSP. Thus, S-3578 was considered to be worthy of further evaluation. PMID:12604523

  16. Litomosoides carinii: mode of action in vitro of benzothiazole and amoscanate derivatives with antifilarial activity.

    PubMed

    Davies, K P; Zahner, H; Köhler, P

    1989-05-01

    It is suggested that the recently developed benzothiazole and amoscanate derivatives with antifilarial activity exert their action in vitro by an inhibition of mitochondrial-derived respiration. It was confirmed that the drugs CGP 20376, 21835, 20308, 21306, and 6140 cause a rapid immobilization in vitro of the adult filarial worm, Litomosoides carinii, the time required being similar to rotenone at the same concentration. The other drugs investigated, CGPs 20309, 21833, 24589, 23518, and 13231, were also effective; however, they required much longer incubation times. Submitochondrial particles (SMP) were prepared from Ascaris muscle and rat liver. The concentration of drug causing 50% inhibition of respiration (IC50) was calculated. It was found that the drugs most rapidly inhibiting respiration have IC50s for NADH oxidase of less than 25 microM in both Ascaris and rat liver SMP. This effect on SMP respiration could be overcome by using succinate as a substrate, indicating the site of inhibition to be within complex I of the mitochondrial respiratory chain. Further experiments showed that whereas the respiratory chain's NADH:ferricyanide reductase was unaffected by these drugs, there were pronounced effects on both Ascaris and rat liver NADH:quinone reductase activity. This suggests that the inhibition within complex I occurs after the flavoprotein dehydrogenase, but before the site of the quinone reduction. The other compounds examined, which had a slower effect on motility, also showed inhibition of the NADH oxidase, but not to as great an extent as the aforementioned compounds. The compounds most active against motility were also most effective at inhibiting respiration in intact adult L. carinii. Analysis of the aerobic end products produced by L. carinii showed that acetate production was greatly reduced even in the presence of low concentrations of the drugs. There was also a slight decrease in lactate production. However, a direct effect on the glycolytic pathway was ruled out by two observations. One, that the production of lactate from cell-free extracts of L. carinii is unaffected by the presence of the drugs, and secondly, that a protozoan, Giardia lamblia, reliant on glycolysis for energy production, can survive for long periods of time in the presence of high concentrations of the drugs. A correlation can be observed between the time for immobilization of the filarial worm and the strength of inhibition of mitochondrial respiration. Therefore, it is suggested that, at least in vitro, the mechanism of toxicity of these antifilarials in L. carinii is due to the blocking of the respiratory chain at a site similar to that of rotenone. PMID:2721632

  17. Allosteric regulation of the primase (DnaG) activity by the clamp-loader (?) in vitro

    PubMed Central

    Chintakayala, Kiran; Machón, Cristina; Haroniti, Anna; Larson, Marilyn A.; Hinrichs, Steven H.; Griep, Mark A.; Soultanas, Panos

    2011-01-01

    Summary During DNA replication the helicase (DnaB) recruits the primase (DnaG) in the replisome to initiate the polymerization of new DNA strands. DnaB is attached to the ? subunit of the clamp-loader that loads the ? clamp and interconnects the core polymerases on the leading and lagging strands. The ?–DnaB–DnaG ternary complex is at the heart of the replisome and its function is likely to be modulated by a complex network of allosteric interactions. Using a stable ternary complex comprising the primase and helicase from Geobacillus stearothermophilus and the ? subunit of the clamp-loader from Bacillus subtilis we show that changes in the DnaB–? interaction can stimulate allosterically primer synthesis by DnaG in vitro. The A550V ? mutant stimulates the primase activity more efficiently than the native protein. Truncation of the last 18 C-terminal residues of ? elicits a DnaG-stimulatory effect in vitro that appears to be suppressed in the native ? protein. Thus changes in the ?–DnaB interaction allosterically affect primer synthesis. Although these C-terminal residues of ? are not involved directly in the interaction with DnaB, they may act as a functional gateway for regulation of primer synthesis by ?-interacting components of the replisome through the ?–DnaB–DnaG pathway. PMID:19415803

  18. In vitro and in vivo anthelmintic activity of Euphorbia helioscopia L.

    PubMed

    Lone, Bashir A; Chishti, M Z; Bhat, Fayaz Ahmad; Tak, Hidayatullah; Bandh, Suhaib A

    2012-10-26

    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

  19. Synthesis and Antifungal Activity In Vitro of Isoniazid Derivatives against Histoplasma capsulatum var. capsulatum

    PubMed Central

    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

    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

  20. In vitro antiviral activity of Ficus carica latex against caprine herpesvirus-1.

    PubMed

    Camero, Michele; Marinaro, Mariarosaria; Lovero, Angela; Elia, Gabriella; Losurdo, Michele; Buonavoglia, Canio; Tempesta, Maria

    2014-01-01

    The latex of Ficus carica Linn. (Moraceae) has been shown to possess antiviral properties against some human viruses. To determine the ability of F. carica latex (F-latex) to interfere with the infection of caprine herpesvirus-1 (CpHV-1) in vitro, F-latex was resuspended in culture media containing 1% ethanol and was tested for potential antiviral effects against CpHV-1. Titration of CpHV-1 in the presence or in the absence of F-latex was performed on monolayers of Madin Darby Bovine Kidney (MDBK) cells. Simultaneous addition of F-latex and CpHV-1 to monolayers of MDBK cells resulted in a significant reduction of CpHV-1 titres 3 days post-infection and this effect was comparable to that induced by acyclovir. The study suggests that the F-latex is able to interfere with the replication of CpHV-1 in vitro on MDBK cells and future studies will determine the mechanisms responsible for the observed antiviral activity. PMID:24853920

  1. Synthesis and antifungal activity in vitro of isoniazid derivatives against histoplasma capsulatum var. capsulatum.

    PubMed

    de Aguiar Cordeiro, Rossana; 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

    2014-05-01

    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

  2. Hemodynamic flow improves rat hepatocyte morphology, function, and metabolic activity in vitro.

    PubMed

    Dash, A; 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

    2013-06-01

    In vitro primary hepatocyte systems typically elicit drug induction and toxicity responses at concentrations much higher than corresponding in vivo or clinical plasma C(max) 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

  3. Ultrastructural localization of adenosine triphosphatase activity in lymphocytes activated in vitro by phytohaemagglutinin

    Microsoft Academic Search

    A. Cuschieri; S. Mughal; B. A. Kharbat

    1982-01-01

    Summary  The ultrastructural localization of Ca2+, Mg2+-activated ATPase was studied in phytohaemagglutinin activated lymphocytes and in normal unstimulated lymphocytes. Cells, fixed in paraformaldehyde-glutaraldehyde, were incubated in a medium containing 3mm ATP, 5mm CaCl2 and 2.4mm Pb(NO3)2 in 0.1m tris buffer at pH 8.5, the optimum pH for histochemical demonstration of this enzyme. Reaction product was localized i the endoplasmic reticulum, nuclear

  4. Acetylcholinesterase inhibition and in vitro and in vivo antioxidant activities of Ganoderma lucidum grown on germinated brown rice.

    PubMed

    Hasnat, Abul; Pervin, Mehnaz; Lim, Beong Ou

    2013-01-01

    In this study, the acetylcholinesterase inhibition and in vitro and in vivo antioxidant activities of Ganoderma lucidum grown on germinated brown rice (GLBR) were evaluated. In antioxidant assays in vitro, GLBR was found to have strong metal chelating activity, DPPH, ABTS, hydroxyl and superoxide radical scavenging activity. Cell-based antioxidant methods were used, including lipid peroxidation on brain homogenate and AAPH-induced erythrocyte haemolysis. In antioxidant assays in vivo, mice were administered with GLBR and this significantly enhanced the activities of antioxidant enzymes in the mice sera, livers and brains. The amount of total phenolic and flavonoid compounds were 43.14 mg GAE/g and 13.36 mg CE/g dry mass, respectively. GLBR also exhibited acetylcholinesterase inhibitory activity. In addition, HPLC analyses of GLBR extract revealed the presence of different phenolic compounds. These findings demonstrate the remarkable potential of GLBR extract as valuable source of antioxidants which exhibit interesting acetylcholinesterase inhibitory activity. PMID:23749158

  5. Different Astrocytic Activation between Adult Gekko japonicus and Rats during Wound Healing In Vitro

    PubMed Central

    Chen, Haijiao; Li, Jing; Xu, Man; Hua, Juan; Yao, Jian; Wang, Yongjun; Liu, Yan; Liu, Mei

    2015-01-01

    Glial scar formation is a major obstacle to regeneration after spinal cord injury. Moreover, it has been shown that the astrocytic response to injury differs between species. Gekko japonicas is a type of reptile and it shows differential glial activation compared to that of rats. The purpose of the present study was to compare the proliferation and migration of astrocytes in the spinal cords of geckos and rats after injury in vitro. Spinal cord homogenate stimulation and scratch wound models were used to induce astrocytic activation in adult and embryonic rats, as well as in adult geckos. Our results indicated that astrocytes from the adult rat were likely activated by mechanical stimulation, even though they showed lower proliferation abilities than the astrocytes from the gecko under normal conditions. Furthermore, a transcriptome analysis revealed that the differentially expressed genes in astrocytes from adult rats and those from geckos were enriched in pathways involved in proliferation and the response to stimuli. This implies that intrinsic discrepancies in gene expression patterns might contribute to the differential activation of astrocytes between species. PMID:26020931

  6. Influence of laser irradiation on superoxide dismutase activity of human lymphocytes in vitro

    NASA Astrophysics Data System (ADS)

    Volotovskaya, Anna V.; Kozlova, Nataly M.; Antonovich, Anna N.; Slobozhanina, Ekaterina I.

    2007-06-01

    The treatment of blood with low intensity laser irradiation has become popular in a variety of clinical applications due to its anti-inflammatory, biostimulative and immune-stimulatory effects etc. Laser blood irradiation with infrared and red laser sources have the potential for stimulating antioxidant enzymes activities. At present study the influence of red and infra-red laser irradiation at different doses on superoxide dismutase (SOD) activity of peripheral blood lymphocytes was investigated in vitro. Suspensions of human lymphocytes (concentration of cells 1x10 6 cells/ml) were irradiated with red (670 nm) and infrared (980 nm) therapy lasers at different light doses (0-600 J/sample) and light power (4,5 and 15 mW for red; 50 and 500 mW for infrared) at 20°C. It is revealed doze-depended effect of red and infra-red laser irradiation on superoxide dismutaze activity of peripheral blood lymphocytes. The SOD activity, first of all, depends on irradiation time, but not on intensity or wavelength of irradiation. These data can explain the positive medical effects of a laser blood irradiation. The obtained results confirm a hypothesis that laser irradiation with the different wavelength characteristic (red and infra-red light ranges) reveals a stimulating effect on SOD - antioxidant defence system enzyme in peripheral blood lymphocytes.

  7. Different Astrocytic Activation between Adult Gekko japonicus and Rats during Wound Healing In Vitro.

    PubMed

    Gu, Yun; Yang, Jian; Chen, Haijiao; Li, Jing; Xu, Man; Hua, Juan; Yao, Jian; Wang, Yongjun; Liu, Yan; Liu, Mei

    2015-01-01

    Glial scar formation is a major obstacle to regeneration after spinal cord injury. Moreover, it has been shown that the astrocytic response to injury differs between species. Gekko japonicas is a type of reptile and it shows differential glial activation compared to that of rats. The purpose of the present study was to compare the proliferation and migration of astrocytes in the spinal cords of geckos and rats after injury in vitro. Spinal cord homogenate stimulation and scratch wound models were used to induce astrocytic activation in adult and embryonic rats, as well as in adult geckos. Our results indicated that astrocytes from the adult rat were likely activated by mechanical stimulation, even though they showed lower proliferation abilities than the astrocytes from the gecko under normal conditions. Furthermore, a transcriptome analysis revealed that the differentially expressed genes in astrocytes from adult rats and those from geckos were enriched in pathways involved in proliferation and the response to stimuli. This implies that intrinsic discrepancies in gene expression patterns might contribute to the differential activation of astrocytes between species. PMID:26020931

  8. In vitro antioxidant activity and in vivo antidepressant-like effect of ?-(phenylselanyl) acetophenone in mice.

    PubMed

    Gerzson, Mariana Freire Barbieri; Victoria, Francine N; Radatz, Cátia S; de Gomes, Marcelo G; Boeira, Silvana P; Jacob, Raquel G; Alves, Diego; Jesse, Cristiano Ricardo; Savegnago, Lucielli

    2012-07-01

    In this study, the antioxidant and antidepressant-like effects of ?-(phenylselanyl) acetophenone (PSAP), an organoselenium compound, were investigated. To assess the in vitro antioxidant properties, PSAP was evaluated in four test systems (DPPH, ABTS, FRAP and inhibition of lipid peroxidation). PSAP (100-500 ?M) showed potent antioxidant activity and protected against lipid peroxidation. Additionally, we investigated whether PSAP, when administered in mice (100, 200 and 400mg/kg, per oral, p.o.), could cause acute toxicity. Our results demonstrated that PSAP did not cause the death of any animal, significantly reduce body weight or cause any oxidative tissue stress following treatment. This study also evaluated the effect of PSAP (0.1-10 mg/kg, p.o) on mice in a forced swim test (FST) and tail suspension test (TST), assays that are predictive of depressant activity and motor activity in the open-field. PSAP (5-10 mg/kg) significantly reduced immobility time in the FST and TST without affecting motor activity. In addition, the antidepressant-like effect caused by PSAP (5m/kg, p.o) in mice during the TST was dependent on an interaction with the serotonergic system (5-HT(1A) receptors), but not with the noradrenergic, dopaminergic or adenosinergic system. Together, these results suggest that PSAP possesses antioxidant and antidepressant-like properties and may be of interest as a therapeutic agent for the treatment of depressive disorders. PMID:22484161

  9. A topological study of repetitive co-activation networks in in vitro cortical assemblies

    NASA Astrophysics Data System (ADS)

    Pirino, Virginia; Riccomagno, Eva; Martinoia, Sergio; Massobrio, Paolo

    2015-02-01

    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.

  10. In vitro antimicrobial activity of 20 selected climber species from the Bignoniaceae family.

    PubMed

    Torres, Carola Analía; Zampini, Iris Catiana; Nuńez, María Beatriz; Isla, María Inés; Castro, Marcela Paola; Gonzalez, Ana María

    2013-01-01

    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

  11. In vitro Cytotoxic Activity of Four Plants Used in Persian Traditional Medicine

    PubMed Central

    Zare Shahneh, Fateme; Baradaran, Behzad; Orangi, Mona; Zamani, Fatemeh

    2013-01-01

    Purpose: The aim of this study was to investigate in vitro cytotoxic activity of four methanolic crude plant extracts against panel cell lines. Methods: Methanolic extracts were tested for their possible antitumor activity and cytotoxicity using the 3-(4,5-dimetylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay on six cancer cell lines; non-Hodgkin’s B-cell lymphoma (Raji), human leukemic monocyte lymphoma (U937), human acute myelocytic leukemia (KG-1A), human breast carcinoma (MCF-7 cells), human Prostate Cancer (PC3) and mouse fibrosarcoma (WEHI-164) cell lines and one normal cell line; Human Umbilical Vein Endothelial Cells (HUVEC). Results: All species showed dose dependent inhibition of cell proliferation. IC50 values ranging from 25.66±1.2 to 205.11±1.3 ?g/ml. The highest cytotoxic activity Chelidonium majus L> Ferulago Angulata DC> Echinophora platyloba DC> Salvia officinalis L, respectively. Conclusion: all extracts demonstrate promising cytotoxicity activity as a natural resource for future bio-guided fractionation and isolation of potential antitumor agents. PMID:24312877

  12. Icaritin and its glycosides enhance osteoblastic, but suppress osteoclastic, differentiation and activity in vitro.

    PubMed

    Huang, Jian; Yuan, Lan; Wang, Xi; Zhang, Tian-Lan; Wang, Kui

    2007-08-16

    Icariin, a principal flavonoid glycoside in Herba Epimedii, is hypothesized to possess beneficial effects on bone mass. Icariin is metabolized to icariside II and then to icaritin in vivo. In the present study, we investigated the in vitro effects of icariin, icariside II and icaritin on both osteoblasts and osteoclasts. After treatment with these compounds at concentrations 10(-5)-10(-8) mol/l, osteoblasts were examined for proliferation, alkaline phosphatase activity, osteocalcin secretion and matrix mineralization, as well as expression levels of bone-related proteins. The formation of osteoclasts was assessed by counting the number of multinucleated TRAP-positive cells. The activity of isolated rat osteoclasts was evaluated by measuring pit area, actin rings and superoxide generation. Icariside II and icaritin increased the mRNA expression of ALP, OC, COL-1 and OPG, but suppressed that of RANKL. In addition, these compounds reduced the number of multinucleated TRAP-positive cells and the osteoclastic resorption area. Also decreases were observed in superoxide generation and actin ring formation that are required for osteoclast survival and bone resorption activity. These findings suggest that icaritin, which was more potent than icariin and icariside II, enhanced the differentiation and proliferation of osteoblasts, and facilitated matrix calcification; meanwhile it inhibited osteoclastic differentiation in both osteoblast-preosteoclast coculture and osteoclast progenitor cell culture, and reduced the motility and bone resorption activity of isolated osteoclasts. PMID:17764702

  13. In vitro evaluation of Portuguese propolis and floral sources for antiprotozoal, antibacterial and antifungal activity.

    PubMed

    Falcăo, Soraia I; Vale, Nuno; Cos, Paul; Gomes, Paula; Freire, Cristina; Maes, Louis; Vilas-Boas, Miguel

    2014-03-01

    Propolis is a beehive product with a very complex chemical composition, used since ancient times in several therapeutic treatments. As a contribution to the improvement of drugs against several tropical diseases caused by protozoa, we screened Portuguese propolis and its potential floral sources Populus x Canadensis and Cistus ladanifer against Plasmodium falciparum, Leishmania infantum, Trypanosoma brucei and Trypanosoma cruzi. The toxicity against MRC-5 fibroblast cells was evaluated to assess selectivity. The in vitro assays were performed following the recommendations of WHO Special Programme for Research and Training in Tropical Diseases (TDR) and revealed moderate activity, with the propolis extracts presenting the relatively highest inhibitory effect against T. brucei. Additionally, the antimicrobial activity against Staphylococcus aureus, Candida albicans, Trichophyton rubrum and Aspergillus fumigatus was also verified with the better results observed against T. rubrum. The quality of the extracts was controlled by evaluating the phenolic content and antioxidant activity. The observed biological activity variations are associated with the variable chemical composition of the propolis and the potential floral sources under study. PMID:23722631

  14. In vitro antiproliferative and antioxidant activities of the extracts of Muntingia calabura leaves.

    PubMed

    Zakaria, Z A; Mohamed, A M; Jamil, N S Mohd; Rofiee, M S; Hussain, M K; Sulaiman, M R; Teh, L K; Salleh, M Z

    2011-01-01

    The in vitro antiproliferative and antioxidant activities of the aqueous, chloroform and methanol extracts of Muntingia calabura leaves were determined in the present study. Assessed using the 3,(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) assay, the aqueous and methanol extracts of M. calabura inhibited the proliferation of MCF-7, HeLa, HT-29, HL-60 and K-562 cancer cells while the chloroform extract only inhibited the proliferation of MCF-7, HeLa, HL-60 and K-562 cancer cells. Interestingly, all extracts of M. calabura, which failed to inhibit the MDA-MB-231 cells proliferation, did not inhibit the proliferation of 3T3 (normal) cells, indicating its safety. All extracts (20, 100 and 500 ?g/ml) were found to possess antioxidant activity when tested using the DPPH radical scavenging and superoxide scavenging assays with the methanol, followed by the aqueous and chloroform, extract exhibiting the highest antioxidant activity in both assays. The total phenolic content for the aqueous, methanol and chloroform extracts were 2970.4 ± 6.6, 1279.9 ± 6.1 and 2978.1 ± 4.3 mg/100 g gallic acid, respectively. In conclusion, the M. calabura leaves possess potential antiproliferative and antioxidant activities that could be attributed to its high content of phenolic compounds, and thus, needs to be further explored. PMID:21213408

  15. Stimulatory action of itopride hydrochloride on colonic motor activity in vitro and in vivo.

    PubMed

    Tsubouchi, Tadashi; Saito, Takaharu; Mizutani, Fujie; Yamauchi, Toshie; Iwanaga, Yuji

    2003-08-01

    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

  16. In vitro ?-glucosidase inhibitory activity of phenolic constituents from aerial parts of Polygonum hyrcanicum

    PubMed Central

    2012-01-01

    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

  17. Ligand Binding and Activation of PPAR? by Firemaster® 550: Effects on Adipogenesis and Osteogenesis in Vitro

    PubMed Central

    Pillai, Hari K.; Fang, Mingliang; Beglov, Dmitri; Kozakov, Dima; Vajda, Sandor; Stapleton, Heather M.; Webster, Thomas F.

    2014-01-01

    Background: The use of alternative flame retardants has increased since the phase out of pentabromodiphenyl ethers (pentaBDEs). One alternative, Firemaster® 550 (FM550), induces obesity in rats. Triphenyl phosphate (TPP), a component of FM550, has a structure similar to that of organotins, which are obesogenic in rodents. Objectives: We tested the hypothesis that components of FM550 are biologically active peroxisome proliferator-activated receptor ? (PPAR?) ligands and estimated indoor exposure to TPP. Methods: FM550 and its components were assessed for ligand binding to and activation of human PPAR?. Solvent mapping was used to model TPP in the PPAR? binding site. Adipocyte and osteoblast differentiation were assessed in bone marrow multipotent mesenchymal stromal cell models. We estimated exposure of children to TPP using a screening-level indoor exposure model and house dust concentrations determined previously. Results: FM550 bound human PPAR?, and binding appeared to be driven primarily by TPP. Solvent mapping revealed that TPP interacted with binding hot spots within the PPAR? ligand binding domain. FM550 and its organophosphate components increased human PPAR?1 transcriptional activity in a Cos7 reporter assay and induced lipid accumulation and perilipin protein expression in BMS2 cells. FM550 and TPP diverted osteogenic differentiation toward adipogenesis in primary mouse bone marrow cultures. Our estimates suggest that dust ingestion is the major route of exposure of children to TPP. Conclusions: Our findings suggest that FM550 components bind and activate PPAR?. In addition, in vitro exposure initiated adipocyte differentiation and antagonized osteogenesis. TPP likely is a major contributor to these biological actions. Given that TPP is ubiquitous in house dust, further studies are warranted to investigate the health effects of FM550. Citation: Pillai HK, Fang M, Beglov D, Kozakov D, Vajda S, Stapleton HM, Webster TF, Schlezinger JJ. 2014. Ligand binding and activation of PPAR? by Firemaster® 550: effects on adipogenesis and osteogenesis in vitro. Environ Health Perspect 122:1225–1232;?http://dx.doi.org/10.1289/ehp.1408111 PMID:25062436

  18. Glatiramer acetate increases phagocytic activity of human monocytes in vitro and in multiple sclerosis patients.

    PubMed

    Pul, Refik; Morbiducci, Franco; Škuljec, Jelena; Skripuletz, Thomas; Singh, Vikramjeet; Diederichs, Ute; Garde, Niklas; Voss, Elke Verena; Trebst, Corinna; Stangel, Martin

    2012-01-01

    Beside its effects on T cells, a direct influence on cells of the myelo-monocytic lineage by GA becomes evident. Recently, we demonstrated that GA drives microglia to adopt properties of type II antigen presenting cells (APC) and increases their phagocytic activity. In the present work, we focused on human blood monocytes in order to examine whether GA may increase phagocytic activity in vivo and to evaluate the molecular mechanisms explaining this new discovered mode of action. Peripheral blood mononuclear cells (PBMC) were obtained using a Biocoll-Isopaque gradient and monocytes were subsequently isolated by using CD14 MicroBeads. Phagocytic activity was determined by flow cytometric measurement of the ingestion of fluorescent beads. Flow cytometry was also used to assess monocytic differentiation and expression of phagocytic receptors. Monocytes of GA treated MS patients exhibited a significantly higher phagocytic activity than those of healthy controls or non-treated MS patients. In vitro, a significant phagocytic response was already detectable after 1 h of GA treatment at the concentrations of 62.5 and 125 µg/ml. A significant increase at all concentrations of GA was observed after 3 h and 24 h, respectively. Only monocytes co-expressing CD16, particularly CD14(++)CD16(+) cells, were observed to phagocytose. Treatment of monocytes with IL-10 and supernatants from GA-treated monocytes did not alter phagocytosis. We observed a decrease in CD11c expression by GA while no changes were found in the expression of CD11b, CD36, CD51/61, CD91, TIM-3, and CD206. In our blocking assays, treatment with anti-CD14, anti-CD16, anti-TIM3, anti-CD210, and particularly anti-CD36 antibodies led to a decrease in phagocytosis. Our results demonstrate a new mechanism of action of GA treatment that augments phagocytic activity of human monocytes in vivo and in vitro. This activity seems to arise from the CD14(++)CD16(+) monocyte subset. PMID:23284793

  19. In Vitro Activity of CEM-102 (Fusidic Acid) against Prevalent Clones and Resistant Phenotypes of Staphylococcus aureus

    PubMed Central

    Sahm, D. F.; Pillar, C. M.; Fernandes, P.

    2013-01-01

    Clinical development of CEM-102 (fusidic acid) has recently begun in the United States for chronic oral treatment of prosthetic joint infections. To support this development, the in vitro activity of fusidic acid against important Staphylococcus aureus clones and resistance phenotypes was determined. Against 51 such isolates, the modal fusidic acid MIC was 0.12 ?g/ml (range, 0.06 to 0.25 ?g/ml for 49 isolates). This level of in vitro fusidic acid activity underscores the potential clinical utility of this compound in the United States. PMID:23774441

  20. Correlations between Chondroitin Sulfate Physicochemical Properties and its in-vitro Absorption and Anti-inflammatory Activity

    E-print Network

    Surapaneni, Lahari; Bodine, Ashby B; Brooks, James; Podila, Ramakrishna; Haley-Zitlin, Vivian

    2014-01-01

    Here, we investigated the influence of physicochemical characteristics of chondroitin sulfate (CS) on its in vitro absorption and anti-inflammatory activity. We used eight different synthetic and natural CS samples with a range of molecular weights (7-35 kDa) and sulfation patterns. Our studies indicate that the absorption of CS is moderately correlated to percentage of chondroitin-6-sulfate while the anti-inflammatory activity may be weakly related to the molecular weight and the amount of total sulfation in the samples. Our in vitro studies could provide helpful screening tools for quick and effective evaluation of CS samples as a preliminary step towards in vivo studies.

  1. The novel arylamidine T-2307 maintains in vitro and in vivo activity against echinocandin-resistant Candida albicans.

    PubMed

    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

    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

  2. Eggshell membrane hydrolyzates activate NF-?B in vitro: possible implications for in vivo efficacy

    PubMed Central

    Ruff, Kevin J; Durham, Paul L; O’Reilly, Austin; Long, F Daniel

    2015-01-01

    Purpose Eggshell membrane (ESM) has been shown to contain naturally occurring bioactive components, and biological activities such as reducing proinflammatory cytokines, liver fibrosis, and joint pain in osteoarthritis sufferers have also been reported for ESM matrix as a whole. Nuclear factor kappa-light-chain-enhancer of activated B-cells (NF-?B) is a signaling protein found in the cytoplasm of nearly all human and animal cell types and is a primary regulator of immune function. The studies reported herein were designed to investigate the possible role that NF-?B activity might play in the reported biological activities of ESM. Methods Three ESM hydrolyzates produced via fermentation, enzymatic, or chemical hydrolysis were evaluated in vitro in either human peripheral blood mononuclear cell or THP-1 (human leukemic monocyte) cell cultures for NF-?B activity following 4-hour exposure. The hydrolyzates were compared with untreated control cells or cells incubated with lipopolysaccharide or ascorbic acid. The source of ESM activity was also evaluated. Results NF-?B levels were increased above levels found in untreated cells at all three dilutions (1:100, 1:1,000, and 1:10,000) for the fermentation hydrolyzate of ESM (ESM-FH) (P=0.021, P=0.020, P=0.009, respectively) in peripheral blood mononuclear cells. The enzymatic hydrolyzate of ESM (ESM-EH) also produced statistically significant levels of activated NF-?B at the 1:100 and 1:1,000 dilutions (P=0.004, P=0.006, respectively) but fell just shy of significance at the 1:10,000 dilution (P=0.073). Similarly, ESM-FH (P=0.021, P=0.002) and ESM-EH (P=0.007, P=0.007) activated NF-?B in THP-1 cells at 1:1,000 and 1:10,000 dilutions, respectively. The chemical hydrolyzate of ESM (ESM-CH) showed statistically significant levels of activation at the 1:1,000 dilution (P=0.005) but failed to differ from untreated cells at the 1:10,000 dilution (P=0.193) in THP-1 cells. Conclusion Results from our studies provide evidence that ESM hydrolyzates significantly activate NF-?B, and the source of this activity was investigated to confirm that it is inherent to ESM and not derived from bacterial contamination. Based on our findings, we propose a plausible hypothesis as to how increased NF-?B activity might translate into the in vivo efficacy that has been observed with ESM via an “oral tolerance” mechanism. PMID:25709492

  3. Temporal changes in intestinal Na +, K +ATPase activity and in vitro responsiveness to cortisol in juvenile chinook salmon

    Microsoft Academic Search

    Philip A. Veillette; Graham Young

    2004-01-01

    Seasonal changes in endogenous Na+, K+-ATPase activity were measured in pyloric ceca and posterior intestine of juvenile chinook salmon (Oncorhynchus tshawytscha) maintained in fresh water over 18 months. In tissues from these same fish, the in vitro responsiveness of Na+, K+-ATPase activity to 10 ?g cortisol\\/ml was assessed. There were pronounced increases in endogenous Na+, K+-ATPase activity in summer for

  4. Comparative In-Vitro Activity of Aztreonam and other Antimicrobials against Gram-Negative Hospital Isolates including Pseudomonas aeruginosa

    Microsoft Academic Search

    AB STRACT

    The in-vitro activity of Aztreonam against 251 recent gram-negative bacterial isolates was determined by the Kirby-Bauer disc diffusion method. The activity was compared with ampicillin, amoxycillin\\/clavulanate, cefamandole, ceftazidime, ofloxacin and ciprofloxacln against 197 members of the enterobacteriaceae. Ceftazidime, ofloxacin, ciprofloxacin and amikacin were the drugs compared against 54 Pseudomonas spp. Mean activity of Aztreonam against enterobacteriaceae was 96.44% (190\\/197) with

  5. Comparative in vitro activity of norfloxacin (MK-0366) and ten other oral antimicrobial agents against urinary bacterial isolates.

    PubMed Central

    Khan, M Y; Gruninger, R P; Nelson, S M; Klicker, R E

    1982-01-01

    The in vitro activity of a new oral antimicrobial agent, norfloxacin (MK-0366), was compared with those of nalidixic acid, nitrofurantoin, co-trimoxazole, trimethoprim, sulfamethoxazole, cinoxacin, tetracycline, ampicillin, carbenicillin, and cephalexin against 628 urinary bacterial isolates. Norfloxacin was the most active antimicrobial agent tested against the gram-negative bacilli. It was less active than a few of the other antimicrobial agents against enterococci and Staphylococcus aureus. PMID:6213200

  6. In Vitro Activity of Ozenoxacin against Quinolone-Susceptible and Quinolone-Resistant Gram-Positive Bacteria

    PubMed Central

    López, Y.; Tato, M.; Espinal, P.; Garcia-Alonso, F.; Gargallo-Viola, D.; Cantón, R.

    2013-01-01

    In vitro activity of ozenoxacin, a novel nonfluorinated topical (L. D. Saravolatz and J. Leggett, Clin. Infect. Dis. 37:1210–1215, 2003) quinolone, was compared with the activities of other quinolones against well-characterized quinolone-susceptible and quinolone-resistant Gram-positive bacteria. Ozenoxacin was 3-fold to 321-fold more active than other quinolones. Ozenoxacin could represent a first-in-class nonfluorinated quinolone for the topical treatment of a broad range of dermatological infections. PMID:24080666

  7. Phenolic contents and antioxidant activities of bitter gourd ( Momordica charantia L.) leaf, stem and fruit fraction extracts in vitro

    Microsoft Academic Search

    Jittawan Kubola; Sirithon Siriamornpun

    2008-01-01

    Bitter gourd (Momordica charantia L.) has long been regarded as a food and medicinal plant. We investigated the antioxidant activity of the water extract of leaf, stem and fruit fractions by several in vitro systems of assay, namely DPPH radical-scavenging activity, hydroxyl radical-scavenging activity, ?-carotene–linoleate bleaching assay, ferric reducing\\/antioxidant power (FRAP) assay and total antioxidant capacity. Total phenolic content was

  8. In vitro and in vivo anti-angiogenic activity of girinimbine isolated from Murraya koenigii.

    PubMed

    Iman, Venoos; Karimian, Hamed; Mohan, Syam; Hobani, Yahya Hasan; Noordin, Mohamed Ibrahim; Mustafa, Mohd Rais; Noor, Suzita Mohd

    2015-01-01

    Girinimbine is a carbazole alkaloid isolated from the stem bark and root of Murraya koenigii. Here we report that girinimbine is an inhibitor of angiogenic activity both in vitro and in vivo. MTT results showed that girinimbine inhibited proliferation of human umbilical vein endothelial cells, while results from endothelial cell invasion, migration, tube formation, and wound healing assays demonstrated significant time- and dose-dependent inhibition by girinimbine. A proteome profiler array done on girinimbine-treated human umbilical vein endothelial cells showed that girinimbine had mediated regulation of pro-angiogenic and anti-angiogenic proteins. The anti-angiogenic potential of girinimbine was also evidenced in vivo in the zebrafish embryo model wherein girinimbine inhibited neo vessel formation in zebrafish embryos following 24 hours of exposure. Together, these results showed that girinimbine could effectively suppress angiogenesis, suggestive of its therapeutic potential as a novel angiogenesis inhibitor. PMID:25767375

  9. In vitro activity of carvacrol and thymol combined with antifungals or antibacterials against Pythium insidiosum.

    PubMed

    Jesus, F P K; Ferreiro, L; Bizzi, K S; Loreto, É S; Pilotto, M B; Ludwig, A; Alves, S H; Zanette, R A; Santurio, J M

    2015-06-01

    We describe the in vitro activities of the combinations of carvacrol and thymol with antibiotics (azithromycin, clarithromycin, minocycline and tigecycline) and antifungal agents (amphotericin B, caspofungin, itraconazole and terbinafine) against 23 isolates of the oomycete Pythium insidiosum. The assays were based on the M38-A2 technique and checkerboard microdilution. Based on the mean FICI values, the main synergies observed were combinations of carvacrol+itraconazole and thymol+itraconazole (96%), thymol+clarithromycin (92%), carvacrol+clarithromycin (88%), thymol+minocycline (84%), carvacrol+minocycline (80%), carvacrol+azithromycin (76%), thymol+azithromycin (68%), carvacrol+tigecycline (64%) and thymol+tigecycline (60%). In conclusion, we found that combinations of carvacrol or thymol with these antimicrobial agents might provide effective alternative treatments for cutaneous pythiosis due to their synergistic interactions. Future in vivo experiments are needed to elucidate the safety and therapeutic potential of these combinations. PMID:25639921

  10. Treatment failure after substitution of generic pancrelipase capsules. Correlation with in vitro lipase activity.

    PubMed

    Hendeles, L; Dorf, A; Stecenko, A; Weinberger, M

    1990-05-01

    Pancreatic enzyme products are formulated, manufactured, and sold without submitting efficacy or bioavailability data to the Food and Drug Administration because of a quirk in the law. We documented therapeutic failures in three patients with cystic fibrosis after pharmacists substituted generic pancrelipase capsules for the Pancrease brand. Gastrointestinal symptoms and fat malabsorption rapidly resolved after therapy was reinstituted with brand name products. In vitro analysis indicated that after 1 hour of exposure to simulated gastric fluid, lipase activity was less than 200 U per capsule from all three generic capsules dispensed to the patients compared with 6820 U per capsule from Pancrease. These data indicate that the enteric coating of the generic product was defective and that the substituted product was not bioequivalent to the prescribed brand. We conclude that the Food and Drug Administration should institute regulations over this group of products. PMID:2329633

  11. In vitro and in vivo anti-angiogenic activity of girinimbine isolated from Murraya koenigii

    PubMed Central

    Iman, Venoos; Karimian, Hamed; Mohan, Syam; Hobani, Yahya Hasan; Noordin, Mohamed Ibrahim; Mustafa, Mohd Rais; Noor, Suzita Mohd

    2015-01-01

    Girinimbine is a carbazole alkaloid isolated from the stem bark and root of Murraya koenigii. Here we report that girinimbine is an inhibitor of angiogenic activity both in vitro and in vivo. MTT results showed that girinimbine inhibited proliferation of human umbilical vein endothelial cells, while results from endothelial cell invasion, migration, tube formation, and wound healing assays demonstrated significant time- and dose-dependent inhibition by girinimbine. A proteome profiler array done on girinimbine-treated human umbilical vein endothelial cells showed that girinimbine had mediated regulation of pro-angiogenic and anti-angiogenic proteins. The anti-angiogenic potential of girinimbine was also evidenced in vivo in the zebrafish embryo model wherein girinimbine inhibited neo vessel formation in zebrafish embryos following 24 hours of exposure. Together, these results showed that girinimbine could effectively suppress angiogenesis, suggestive of its therapeutic potential as a novel angiogenesis inhibitor. PMID:25767375

  12. Water soluble polysaccharides from Spirulina platensis: extraction and in vitro anti-cancer activity.

    PubMed

    Kurd, Forouzan; Samavati, Vahid

    2015-03-01

    Polysaccharides from Spirulina platensis algae (SP) were extracted by ultrasound-assisted extraction procedure. The optimal conditions for ultrasonic extraction of SP were determined by response surface methodology. The four parameters were, extraction time (X1), extraction temperature (X2), ultrasonic power (X3) and the ratio of water to raw material (X4), respectively. The experimental data obtained were fitted to a second-order polynomial equation. The optimum conditions were extraction time of 25 min, extraction temperature 85°C, ultrasonic power 90 W and ratio of water to raw material 20 mL/g. Under these optimal conditions, the experimental yield was 13.583±0.51%, well matched with the predicted models with the coefficients of determination (R2) of 0.9971. Then, we demonstrated that SP polysaccharides had strong scavenging activities in vitro on DPPH and hydroxyl radicals. Overall, SP may have potential applications in the medical and food industries. PMID:25583023

  13. In vitro combined bactericidal activity of cefpirome and glycopeptides against glycopeptides and oxacillin-resistant staphylococci.

    PubMed

    Bergeret, M; Boutros, N; Raymond, J

    2004-03-01

    Infections caused by coagulase-negative staphylococci are becoming increasingly important, particularly those of nosocomial origin, as the organisms are frequently multi-resistant. New antimicrobial strategies are needed. The bactericidal activity of a combination of cefpirome with either vancomycin or teicoplanin against 12 strains of methicillin-resistant staphylococci with a decreased susceptibility to teicoplanin was determined in vitro by a time killing method. Strains Mu3 and Mu50 of Staphylococcus aureus were also studied. Cefpirome (0.125-0.5 x MIC) combined with vancomycin (0.25-1 x MIC) or teicoplanin (0.125-1 x MIC) acted synergically against 12 isolates over 18 h in most cases. A synergistic killing effect was also observed with the Mu3 and Mu50 strains of glycopeptide-intermediate S. aureus but over a longer period. PMID:15164965

  14. In vitro antimicrobial activity of Romanian medicinal plants hydroalcoholic extracts on planktonic and adhered cells.

    PubMed

    Stanciuc, A M; Gaspar, A; Moldovan, L; Saviuc, C; Popa, M; M?ru?escu, L

    2011-01-01

    The aim of this study was to assess the antibacterial and antifungal potential of some Romanian medicinal plants, arnica--Arnica montana, wormwood--Artemisia absinthium and nettle--Urtica dioica. In order to perform this antimicrobial screening, we obtained the vegetal extracts and we tested them on a series of Gram-positive and Gram-negative bacteria, and also against two fungal strains. The vegetal extracts showed antimicrobial activity preferentially directed against the planktonic fungal and bacterial growth, while the effect against biofilm formation and development was demonstrated only against S. aureus and C. albicans. Our in vitro assays indicate that the studied plant extracts are a significant source of natural alternatives to antimicrobial therapy, thus avoiding antibiotic therapy, the use of which has become excessive in recent years. PMID:21717806

  15. In Vitro Activities of 25 Quinolones and Fluoroquinolones against Liver and Blood Stage Plasmodium spp.

    PubMed Central

    Mahmoudi, Nassira; Ciceron, Liliane; Franetich, Jean-François; Farhati, Khemais; Silvie, Olivier; Eling, Wijnand; Sauerwein, Robert; Danis, Martin; Mazier, Dominique; Derouin, Francis

    2003-01-01

    The in vitro activities of 25 quinolones and fluoroquinolones against erythrocytic stages of Plasmodium falciparum and against liver stages of Plasmodium yoelii yoelii and P. falciparum were studied. All compounds were inhibitory for chloroquine-sensitive and chloroquine-resistant P. falciparum grown in red blood cells. This inhibitory effect increased with prolonged incubation and according to the logarithm of the drug concentration. Grepafloxacin, trovafloxacin, and ciprofloxacin were the most effective drugs, with 50% inhibitory concentrations of <10 ?g/ml against both strains. Only grepafloxacin, piromidic acid, and trovafloxacin had an inhibitory effect against hepatic stages of P. falciparum and P. yoelii yoelii; this effect combined reductions of the numbers and the sizes of schizonts in treated cultures. Thus, quinolones have a potential for treatment or prevention of malaria through their unique antiparasitic effect against erythrocytic and hepatic stages of Plasmodium. PMID:12878530

  16. In vitro compartmentalization by double emulsions: sorting and gene enrichment by fluorescence activated cell sorting

    E-print Network

    Tawfik, Dan S.

    applied in con- junction with completely in vitro systems such as in vitro compartmentalization (IVC, with a linker and caged biotin [7]. Despite the above limitations, fluorescence is one of the most sensitive isothiocyanate; HTS, high-throughput screening; IVC, in vitro compartmentalization; PBS, phosphate

  17. The acylation of lysophosphatidylglycerol in rat heart: evidence for both in vitro and in vivo activities.

    PubMed

    Cheng, P; Dolinsky, V; Hatch, G M

    1996-07-12

    The reacylation of lysophospholipids back to their parent molecules is important for attaining the appropriate fatty acyl composition in many phospholipids and for preventing the accumulation of arrhythmia generating lysophospholipids in the heart. In this study, we report the presence of an active acyltransferase activity for lysophosphatidylglycerol reacylation to phosphatidylglycerol in rat heart membrane preparations. The activity of acyl-Coenzyme A:1-acylglycerophosphorylglycerol acyltransferase in rat heart subcellular fractions was in the order of microsomal > mitochondrial > cytosol. The activity in the membrane fractions were characterized and found to have a pH optimum in the alkaline range. However, significant enzyme activity was observed at physiological pH. With oleoyl-Coenzyme A as substrate, the microsomal activity had a preference for lysophosphatidylglycerol substrates in the order of myristoyl > palmitoyl > oleoyl > stearoyl. The apparent K(m) values for 1-palmitoylglycerophosphorylglycerol and oleoyl-Coenzyme A were 9.4 and 7.1 microM, respectively. In contrast, the mitochondrial activity had a preference for lysophosphatidylglycerol substrates in the order of oleoyl > myristoyl = stearoyl = palmitoyl. The apparent K(m) values for 1-oleoylglycerophosphorylglycerol and oleoyl-Coenzyme A were 17.8 and 18.0 microM, respectively. Both membrane activities were heat labile as pre-incubation at 55 degrees C for 1 min completely abolished the activity. However, pre-incubation at 50 degrees C resulted in different profiles of inactivation in both microsomal and mitochondrial fractions. Both membrane activities were inhibited by high concentrations of lysophosphatidylglycerol and affected to a similar extent by various detergents. To demonstrate whether reacylation of lysophosphatidylglycerol to phosphatidylglycerol occurred in vivo, isolated rat hearts were perfused for 60 min in the Langendorff mode with 0.1 microM 1-palmitoylglycerophosphoryl[14C]glycerol bound to albumin. 1-Palmitoylglycerophosphoryl[14C]glycerol was readily taken up by the isolated perfused rat heart and significant synthesis of phosphatidyl[14C]glycerol was observed. The findings indicate the presence of an acyl-Coenzyme A:1-acylglycerophosphorylglycerol acyltransferase activity in the rat heart subcellular membranes which is capable of catalyzing lysophosphatidylglycerol acylation to phosphatidylglycerol in vitro and in vivo. PMID:8695656

  18. In vitro assay for osteoinductive activity of different demineralized freeze-dried bone allograft

    PubMed Central

    Vaziri, Shahram; Vahabi, Surena; Torshabi, Maryam

    2012-01-01

    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

  19. In vitro antibacterial activity of Camellia sinensis extract against cariogenic microorganisms

    PubMed Central

    Anita, P.; Sivasamy, Shyam; Madan Kumar, P. D.; Balan, I. Nanda; Ethiraj, Sumathi

    2014-01-01

    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

  20. Niosomal gel of lornoxicam for topical delivery: in vitro assessment and pharmacodynamic activity.

    PubMed

    Kumbhar, Deepak; Wavikar, Preeti; Vavia, Pradeep

    2013-09-01

    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

  1. Ultrastructural localization of adenosine triphosphatase activity in lymphocytes activated in vitro by phytohaemagglutinin.

    PubMed

    Cuschieri, A; Mughal, S; Kharbat, B A

    1982-07-01

    The ultrastructural localization of Ca2+, Mg2+-activated ATPase was studied in phytohaemagglutinin activated lymphocytes and in normal unstimulated lymphocytes. Cells, fixed in paraformaldehyde--glutaraldehyde, were incubated in a medium containing 3 mM ATP, 5 mM CaCl2 and 2.4 mM Pb(NO3)2 in 0.1 M tris buffer at pH 8.5, the optimum pH for histochemical demonstration of this enzyme. Reaction product was localized in the endoplasmic reticulum, nuclear membrane, Golgi apparatus and mitochondria and on the membrane surrounding large electron-dense bodies. Cytoplasmic vesicles and the plasma membrane were negative. Activity in unstimulated lymphocytes showed a similar localization but the amount of endoplasmic reticulum was much less than in activated lymphocytes. The pH of the medium was critical for the localization of the enzyme. At pH 7.5, the cytoplasmic reaction was almost completely inhibited but a dense precipitate was present on the outer surface of the plasma membrane. The reaction was stimulated by either Ca2+ or Mg2+ and was greatly decreased in the absence of these cations or in the presence of p-chloromercuribenzoate or N-ethylmaleimide. Oligomycin inhibited selectively the reaction in mitochondria but not the reaction at other sites. While the reaction in mitochondria showed complete substrate specificity, a mild reaction was obtained at the other sites with uridine diphosphate or sodium beta-glycophosphate as substrate. ATP was, however, the preferential substrate. PMID:6181020

  2. Inhibition of in vitro T cell activation by corneal endothelial cells.

    PubMed

    Obritsch, W F; Kawashima, H; Evangelista, A; Ketcham, J M; Holland, E J; Gregerson, D S

    1992-10-01

    Cells and tissues of the anterior uvea and aqueous humor express activities which inhibit immune responses. These activities include soluble factors such as TGF-beta and uncharacterized cell surface interactions. Relatively little is known regarding the immunologic activities of corneal endothelium, despite its potentially important role in contributing to the immune privilege of the anterior chamber and the high success rate of corneal transplantation. In this report, in vitro studies of cultured rat corneal endothelial (CE) cells were done using S-antigen-specific LEW rat T cell lines, or S-antigen-specific T cell hybridomas, to examine the immunologic capabilities of CE cells. Monolayers of LEW rat CE cells were unable to present antigen or a mitogen, Con A, to T cell lines or hybridomas as assessed by the lack of a proliferative response or IL-2 secretion. Furthermore, the CE cells exerted a potent inhibitory effect when added to in vitro proliferation assays of T cell lines stimulated with antigen or Con A. When T cells were preactivated on conventional antigen presenting cells and then transferred to wells containing CE cells, their proliferation was not inhibited. Although CE cells inhibited activation of T cell lines and hybridomas, they did not inhibit the growth of T cell hybridomas or CTLL cells, nor did the CE cells adversely affect the viability of resting T cells cultured on CE monolayers. The inhibitory effect was reversible as preincubation of T cells on CE cells for up to 6 days followed by washes restored T cell responsiveness when assayed on splenocytes. The inability to stimulate proliferative responses was not affected by preincubation of the CE cells with lymphokines which increase MHC antigen expression. The inhibition observed in these assays was not MHC-restricted as CE cells from both LEW and BN rats were equally inhibitory. CE cells from rabbits and cats were also potent inhibitors of T cell activation, suggesting that the mechanism is evolutionarily conserved. The mechanism of inhibition of CE cells is unknown at this time. PMID:1394442

  3. Antioxidant and antiproliferative activities of Abrus precatorius leaf extracts - an in vitro study

    PubMed Central

    2013-01-01

    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

  4. Cannabidiol and other cannabinoids reduce microglial activation in vitro and in vivo: relevance to Alzheimer's disease.

    PubMed

    Martín-Moreno, Ana María; Reigada, David; Ramírez, Belén G; Mechoulam, R; Innamorato, Nadia; Cuadrado, Antonio; de Ceballos, María L

    2011-06-01

    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

  5. In vitro biological screening of the anticholinesterase and antiproliferative activities of medicinal plants belonging to Annonaceae.

    PubMed

    Formagio, A S N; Vieira, M C; Volobuff, C R F; Silva, M S; Matos, A I; Cardoso, C A L; Foglio, M A; Carvalho, J E

    2015-04-01

    The aim of this research was to investigate the antiproliferative and anticholinesterase activities of 11 extracts from 5 Annonaceae species in vitro. Antiproliferative activity was assessed using 10 human cancer cell lines. Thin-layer chromatography and a microplate assay were used to screen the extracts for acetylcholinesterase (AchE) inhibitors using Ellman's reagent. The chemical compositions of the active extracts were investigated using high performance liquid chromatography. Eleven extracts obtained from five Annonaceae plant species were active and were particularly effective against the UA251, NCI-470 lung, HT-29, NCI/ADR, and K-562 cell lines with growth inhibition (GI50) values of 0.04-0.06, 0.02-0.50, 0.01-0.12, 0.10-0.27, and 0.02-0.04 µg/mL, respectively. In addition, the Annona crassiflora and A. coriacea seed extracts were the most active among the tested extracts and the most effective against the tumor cell lines, with GI50 values below 8.90 µg/mL. The A. cacans extract displayed the lowest activity. Based on the microplate assay, the percent AchE inhibition of the extracts ranged from 12 to 52%, and the A. coriacea seed extract resulted in the greatest inhibition (52%). Caffeic acid, sinapic acid, and rutin were present at higher concentrations in the A. crassiflora seed samples. The A. coriacea seeds contained ferulic and sinapic acid. Overall, the results indicated that A. crassiflora and A. coriacea extracts have antiproliferative and anticholinesterase properties, which opens up new possibilities for alternative pharmacotherapy drugs. PMID:25714885

  6. In vitro biological screening of the anticholinesterase and antiproliferative activities of medicinal plants belonging to Annonaceae

    PubMed Central

    Formagio, A.S.N.; Vieira, M.C.; Volobuff, C.R.F.; Silva, M.S.; Matos, A.I.; Cardoso, C.A.L.; Foglio, M.A.; Carvalho, J.E.

    2015-01-01

    The aim of this research was to investigate the antiproliferative and anticholinesterase activities of 11 extracts from 5 Annonaceae species in vitro. Antiproliferative activity was assessed using 10 human cancer cell lines. Thin-layer chromatography and a microplate assay were used to screen the extracts for acetylcholinesterase (AchE) inhibitors using Ellman's reagent. The chemical compositions of the active extracts were investigated using high performance liquid chromatography. Eleven extracts obtained from five Annonaceae plant species were active and were particularly effective against the UA251, NCI-470 lung, HT-29, NCI/ADR, and K-562 cell lines with growth inhibition (GI50) values of 0.04-0.06, 0.02-0.50, 0.01-0.12, 0.10-0.27, and 0.02-0.04 µg/mL, respectively. In addition, the Annona crassiflora and A. coriacea seed extracts were the most active among the tested extracts and the most effective against the tumor cell lines, with GI50 values below 8.90 µg/mL. The A. cacans extract displayed the lowest activity. Based on the microplate assay, the percent AchE inhibition of the extracts ranged from 12 to 52%, and the A. coriacea seed extract resulted in the greatest inhibition (52%). Caffeic acid, sinapic acid, and rutin were present at higher concentrations in the A. crassiflora seed samples. The A. coriacea seeds contained ferulic and sinapic acid. Overall, the results indicated that A. crassiflora and A. coriacea extracts have antiproliferative and anticholinesterase properties, which opens up new possibilities for alternative pharmacotherapy drugs. PMID:25714885

  7. Metabolic responses differentiate between interictal, ictal and persistent epileptiform activity in intact, immature hippocampus in vitro.

    PubMed

    Ivanov, Anton I; Bernard, Christophe; Turner, Dennis A

    2015-03-01

    Interictal spikes, ictal responses, and status epilepticus are characteristic of abnormal neuronal activity in epilepsy. Since these events may involve different energy requirements, we evaluated metabolic function (assessed by simultaneous NADH and FAD+ imaging and tissue O2 recordings) in the immature, intact mouse hippocampus (P5-P7, in vitro) during spontaneous interictal spikes and ictal-like events (ILEs), induced by increased neuronal network excitability with either low Mg2+ media or decreased inhibition with bicuculline. In low Mg2+ medium NADH fluorescence showed a small decrease both during the interictal build-up leading to an ictal event and before ILE occurrences, but a large positive response during and after ILEs (up to 10% net change). Tissue O2 recordings (pO2) showed an oxygen dip (indicating oxygen consumption) coincident with each ILE at P5 and P7, closely matching an NADH fluorescence increase, indicating a large surge in oxidative metabolism. The ILE O2 dip was significantly larger at P7 as compared to P5 suggesting a higher metabolic response at P7. After several ILEs at P7, continuous, low voltage activity (late recurrent discharges: LRDs) occurred. During LRDs, whilst the epileptiform activity was relatively small (low voltage synchronous activity) oxygen levels remained low and NADH fluorescence elevated, indicating persistent oxygen utilization and maintained high metabolic demand. In bicuculline, NADH fluorescence levels decreased prior to the onset of epileptiform activity, followed by a slow positive phase, which persisted during interictal responses. Metabolic responses can thus differentiate between interictal, ictal-like and persistent epileptiform activity resembling status epilepticus, and confirm that spreading depression did not occur. These results demonstrate clear translational value to the understanding of metabolic requirements during epileptic conditions. PMID:25533681

  8. Enone- and chalcone-chloroquinoline hybrid analogues: in silico guided design, synthesis, antiplasmodial activity, in vitro metabolism, and mechanistic studies.

    PubMed

    Guantai, Eric M; Ncokazi, Kanyile; Egan, Timothy J; Gut, Jiri; Rosenthal, Philip J; Bhampidipati, Ravi; Kopinathan, Anitha; Smith, Peter J; Chibale, Kelly

    2011-05-26

    Analogues of the previously reported antimalarial hybrid compounds 8b and 12 were proposed with the aim of identifying compounds with improved solubility and retained antimalarial potency. In silico characterization predicted improved solubilities of the analogues, particularly at low pH; they retained acceptable predicted permeability properties but were predicted to be susceptible to hepatic metabolism. These analogues were synthesized and found to exhibit notable in vitro antimalarial activity. Compounds 25 and 27 were the most active of the analogues. In vitro metabolism studies indicated susceptibility of the analogues to hepatic metabolism. There was also evidence of primary glucuronidation for analogues 24-27. Presumed cis-trans isomerism of 12, 22, and 23 under in vitro metabolism assay conditions was also observed, with differences in the nature and rates of metabolism observed between isomers. Biochemical studies strongly suggested that inhibition of hemozoin formation is the primary mechanism of action of these analogues. PMID:21500839

  9. Cloning, Expression, and in vitro Functional Activity Assay of phiC31 Integrase cDNA in Escherichia coli

    PubMed Central

    Sekhavati, Mohammad Hadi; Tahmoorespur, Mojtaba; Ghaedi, Kamran; Dormiani, Kianoush; Nassiri, Mohammad Reza; Khazaie, Yahya; Foruzanfar, Mahboubeh; Hosseini, Morteza; Nasr Esfahani, Mohammad Hossein

    2013-01-01

    Objective: The aim of present study was cloning and expression of phiC31 integrase cDNA in a bacterial expression vector. Thus, an intra molecular assay vector was applied to show in vitro activity of recombinant protein. Materials and Methods: In this experimental study, phiC31 cDNA was subcloned into a prokaryotic expression vector and transformed into E.coli Bl21 (DE3). Recombinant phiC31 integrase was purified form the bacterial cell lysates and its activity was verified by an in vitro functional assessment. Results: Sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) of the puri?ed phiC31 integrase confirmed the size of protein (70 kDa). Finally, the functionality of purified phiC31 integrase was verified. Conclusion: The results of this study indicated that the purified integrase has a great potential application for in vitro site-specific integration. PMID:23577305

  10. Trans-cleaving hammerhead ribozymes with tertiary stabilizing motifs: in vitro and in vivo activity against a structured viroid RNA

    PubMed Central

    Carbonell, Alberto; Flores, Ricardo; Gago, Selma

    2011-01-01

    Trans-cleaving hammerheads with discontinuous or extended stem I and with tertiary stabilizing motifs (TSMs) have been tested previously against short RNA substrates in vitro at low Mg2+ concentration. However, the potential of these ribozymes for targeting longer and structured RNAs in vitro and in vivo has not been examined. Here, we report the in vitro cleavage of short RNAs and of a 464-nt highly structured RNA from potato spindle tuber viroid (PSTVd) by hammerheads with discontinuous and extended formats at submillimolar Mg2+. Under these conditions, hammerheads derived from eggplant latent viroid and peach latent mosaic viroid (PLMVd) with discontinuous and extended formats, respectively, where the most active. Furthermore, a PLMVd-derived hammerhead with natural TSMs showed activity in vivo against the same long substrate and interfered with systemic PSTVd infection, thus reinforcing the idea that this class of ribozymes has potential to control pathogenic RNA replicons. PMID:21097888

  11. Artificial oocyte activation and human failed-matured oocyte vitrification followed by in vitro maturation.

    PubMed

    Liu, Y; Cao, Y X; Zhang, Z G; Xing, Q

    2013-02-01

    The investigation presented in this paper was conducted on the effect of oocytes activation on frozen-thawed human immature oocytes followed by in vitro maturation (IVM). A total of 386 failed-matured oocytes (germinal vesicle (GV) and metaphase I (MI) stages) was randomly divided into two groups: fresh group and vitrification group, GV group and MI group, respectively). The matured oocytes were subject to intracytoplasmic sperm injection (ICSI) after IVM had been carried out. The vitrification group was randomly divided into two groups: controlled and artificial oocyte activation (AOA). The injected oocytes in the controlled group were cultured in cleavage medium. The AOA group oocytes were activated by exposing them to 7% anhydrous alcohol for 6 min then cultured in cleavage medium as well. The rates of fertilization and early embryonic development were compared between the controlled and AOA groups. In MI vitrification group, the high-quality embryo formation rate and blastocyst formation rate were significantly higher in the AOA group than in the controlled group (P < 0.01). In the GV vitrification group, the high-quality embryo formation rate was significantly higher in the AOA group than in the controlled group (P < 0.05). These results indicate that AOA may be good for early embryonic development of vitrified immature human oocytes. PMID:21867595

  12. Growth and Metabolic Activity of Lemon Juice Vesicle Explants in Vitro1

    PubMed Central

    Altman, Arie; Gülsen, Yücel; Goren, Raphael

    1982-01-01

    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

  13. Mutagenicity studies in a tyre plant: in vitro activity of workers' urinary concentrates and raw materials.

    PubMed Central

    Crebelli, R; Paoletti, A; Falcone, E; Aquilina, G; Fabri, G; Carere, A

    1985-01-01

    The possible contribution to urinary mutagenicity of occupational exposures in the rubber industry was studied by assaying the urine concentrates of 72 workmen (44 smokers) employed in a tyre plant. Twenty three clerks (16 smokers) engaged in the administrative department of the same factory served as presumptive unexposed controls. XAD-2 resin concentrates of urine samples were assayed in the plate incorporation test and in the microtitre fluctuation assay with Salmonella typhimurium strains TA1535, TA98, and TA100. Furthermore, the in vitro mutagenicity of the major raw materials in use at the plant was determined in the plate incorporation assay with S typhimurium strains TA1535, TA1537, TA98, and TA100. The results obtained from the urinary mutagenicity study show that smoking habits, but not occupation, were statistically significantly related to the appearance of a urinary mutagenicity that was detectable with strain TA98. A possible synergistic effect of occupation with smoking was observed among tyre builders who were also smokers. The study of the raw materials showed that three technical grade materials were weakly active as mutagens in strain TA98 in the absence (poly-p-dinitrosobenzene) or in the presence of metabolic activation (mixed diaryl-p-phenylendiamines and tetramethyltiuram disulphide). The latter chemical was also weakly active in strain TA100. PMID:4015996

  14. Monitoring Hippocampus Electrical Activity In Vitro on an Elastically Deformable Microelectrode Array

    PubMed Central

    Yu, Zhe; Graudejus, Oliver; Tsay, Candice; Lacour, Stéphanie P.; Wagner, Sigurd

    2009-01-01

    Abstract Interfacing electronics and recording electrophysiological activity in mechanically active biological tissues is challenging. This challenge extends to recording neural function of brain tissue in the setting of traumatic brain injury (TBI), which is caused by rapid (within hundreds of milliseconds) and large (greater than 5% strain) brain deformation. Interfacing electrodes must be biocompatible on multiple levels and should deform with the tissue to prevent additional mechanical damage. We describe an elastically stretchable microelectrode array (SMEA) that is capable of undergoing large, biaxial, 2-D stretch while remaining functional. The new SMEA consists of elastically stretchable thin metal films on a silicone membrane. It can stimulate and detect electrical activity from cultured brain tissue (hippocampal slices), before, during, and after large biaxial deformation. We have incorporated the SMEA into a well-characterized in vitro TBI research platform, which reproduces the biomechanics of TBI by stretching the SMEA and the adherent brain slice culture. Mechanical injury parameters, such as strain and strain rate, can be precisely controlled to generate specific levels of damage. The SMEA allowed for quantification of neuronal function both before and after injury, without breaking culture sterility or repositioning the electrodes for the injury event, thus enabling serial and long-term measurements. We report tests of the SMEA and an initial application to study the effect of mechanical stimuli on neuron function, which could be employed as a high-content, drug-screening platform for TBI. PMID:19594385

  15. Hypocholesterolemic Effect and In Vitro Pancreatic Lipase Inhibitory Activity of an Opuntia ficus-indica Extract

    PubMed Central

    Flores-Fernandez, Jose Miguel; Fernandez-Flores, Ofelia; Gutierrez-Mercado, Yanet; Carmona-de la Luz, Joel; Sandoval-Salas, Fabiola; Mendez-Carreto, Carlos

    2015-01-01

    Cholesterol control is fundamental for prevention of cardiovascular disorders. In this work, the hypocholesterolemic activity of an aqueous Opuntia ficus-indica extract (AOE) was tested in triton-induced mice. The inhibitory activity on pancreatic lipase enzyme was evaluated in vitro by the same extract. Furthermore, polyphenol content of the extract was evaluated. Hypercholesterolemia was induced in three groups of mice by intraperitoneal administration of Triton WR-1339. After induction of hypercholesterolemia, the groups were treated with an AOE (500?mg/kg) and saline solution and the positive control group with orlistat, respectively. Cholesterol levels were measured 24?h later in peripheral blood. The levels of blood cholesterol after administration of AOE significantly decreased compared to negative control. The inhibitory activity of AOE on pancreatic lipase enzyme was evaluated at concentrations from 60 to 1000??g/mL. The AOE inhibited the pancreatic lipase with an IC50 = 588.5??g/mL. The AOE had a high content of polyphenolic compounds. These results show that AOE is able to prevent hypercholesterolemia by pancreatic lipase inhibition, in part due to its polyphenolic compounds.

  16. Anti-Inflammatory and Antiosteoclastogenic Activities of Parthenolide on Human Periodontal Ligament Cells In Vitro

    PubMed Central

    Zhang, Xufang; Mao, Xueli

    2014-01-01

    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

  17. Anti-inflammatory and antiosteoclastogenic activities of parthenolide on human periodontal ligament cells in vitro.

    PubMed

    Zhang, Xufang; Fan, Chen; Xiao, Yin; Mao, Xueli

    2014-01-01

    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

  18. In Vitro Antimicrobial Activity of Ethanolic Extract of Polish Propolis against Biofilm Forming Staphylococcus epidermidis Strains

    PubMed Central

    Wojtyczka, Robert D.; K?pa, Ma?gorzata; Idzik, Danuta; Kaba?a-Dzik, Agata; W?sik, Tomasz J.

    2013-01-01

    The aim of the presented study was to examine the antimicrobial activity of ethanol extract of Polish propolis (EEPP) against biofilm-forming CoNS strains in vitro. Our results revealed that EEPP displayed varying degrees of activity against CoNS with MIC values ranging from 1.56 to 0.78?mg/mL. The average MIC was 1.13 ± 0.39?mg/mL while calculated MIC50 and MIC90 values were 0.78?mg/mL and 1.56?mg/mL, respectively. The biofilm formation ability by all tested S. epidermidis strains was inhibited at EEPP concentrations ranging from 0.39 to 1.56?mg/mL. The degree of reduction of AlamarBlue was directly associated with the proliferation of S. epidermidis strains. The increased proliferation of S. epidermidis strains was observed after 12 and 24 hours of incubation in the presence of EEPP concentrations ranging from 0.025 to 0.39?mg/mL. These results suggest that antimicrobial activities of EEPP against S. epidermidis expressed as the reduction of bacterial growth, reduction of biofilm formation ability, and the intensity of proliferation were significantly affected by incubation time and EEPP concentration used as well as the interactions between these factors. PMID:23662143

  19. Chemical Composition and in Vitro Antifungal Activity Screening of the Allium ursinum L. (Liliaceae)

    PubMed Central

    Bagiu, Radu Vasile; Vlaicu, Brigitha; Butnariu, Monica

    2012-01-01

    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

  20. In vitro antibacterial activity of Libanotis montana essential oil in combination with conventional antibiotics.

    PubMed

    Miladinovi?, Dragoljub L; Ili?, Budimir S; Mihajilov-Krstev, Tatjana M; Jovi?, Jovana L; Markovi?, Marija S

    2014-02-01

    The chemical composition and antibacterial activity were examined of Libanotis montana Crantz subsp. leiocarpa (Heuff.) Soó. (Apiaceae) essential oil. Gas chromatography and gas chromatography/mass spectrometry were used to analyze the chemical composition of the oil. The antibacterial activity was investigated by the broth microdilution method against thirteen bacterial strains. The interactions of the essential oil and three standard antibiotics: tetracycline, streptomycin and chloramphenicol toward five selected strains were evaluated using the microdilution checkerboard assay in combination with chemometric methods: principal components analysis and hierarchical cluster analysis. Sesquiterpene hydrocarbons were the most abundant compound class in the oil (67.2%), with beta-elemene (40.4%) as the major compound. The essential oil exhibited slight antibacterial activity against the tested bacterial strains in vitro, but the combinations L. montana oil-chloramphenicol and L. montana oil-tetracycline exhibited mostly either synergistic or additive interactions. These combinations reduced the minimum effective dose of the antibiotics and, consequently, minimized their adverse side effects. In contrast, the association of L. montana essential oil and streptomycin was characterized by strong antagonistic interactions against Escherichia coli ATCC 25922. In the PCA and HCA analyses, streptomycin stood out and formed a separate group. PMID:24689311

  1. In vitro and in vivo studies of trypanocidal activity of dietary isothiocyanates.

    PubMed

    Steverding, Dietmar; Michaels, Sarah; Read, Kevin D

    2014-02-01

    Six dietary isothiocyanates, allyl-isothiocyanate, benzyl-isothiocyanate, phenylethyl-isothiocyanate, sulforaphane, erucin, and iberin, were tested for their trypanocidal activities in vitro using culture-adapted bloodstream forms of Trypanosoma brucei. All isothiocyanates showed a dose-dependent effect on the growth of trypanosomes. Five compounds displayed MIC values of 10?µM and GI50 values of around 1.5?µM, while allyl-isothiocyanate exhibited values of 100 and 11?µM, respectively. The compounds showed similar cytotoxic activities against human HL-60 cells with GI50 values of 1-4?µM and MIC values of 10-100?µM. Short-term experiments revealed that, with the exception of allyl-isothiocyanate, isothiocyanates at a concentration of 10?µM kill trypanosomes within 1-4?h of incubation. In contrast, HL-60 cells were not affected by any of the compounds in short-term incubation experiments. Sulforaphane, the most intensively studied isothiocyanate, was also investigated for its in vivo trypanocidal activity. However, administration of 50?mg/kg sulforaphane orally or intraperitoneally for four days had no effect on the parasitaemia in mice infected with T. brucei compared to control animals treated with vehicle alone. PMID:24452460

  2. In vitro antiviral activity of penciclovir, a novel purine nucleoside, against duck hepatitis B virus.

    PubMed Central

    Shaw, T; Amor, P; Civitico, G; Boyd, M; Locarnini, S

    1994-01-01

    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

  3. The in vivo estrogenic and in vitro anti-estrogenic activity of permethrin and bifenthrin

    PubMed Central

    Brander, Susanne M.; He, Guochun; Smalling, Kelly L.; Denison, Michael S.; Cherr, Gary N.

    2012-01-01

    Pyrethroids are highly toxic to fish at parts per billion or parts per trillion concentrations. Their intended mechanism is prolonged sodium channel opening, but recent studies reveal that pyrethroids such as permethrin and bifenthrin also have endocrine activity. Additionally, metabolites may have greater endocrine activity than parent compounds. We evaluated the in vivo concentration-dependent ability of bifenthrin and permethrin to induce choriogenin (an estrogen-responsive protein) in Menidia beryllina, a fish species known to reside in pyrethroid contaminated aquatic habitats. We then compared the in vivo response to an in vitro assay: CALUX (Chemical Activated Luciferase Gene Expression). Juvenile Menidia beryllina exposed to bifenthrin (1, 10, 100 ng/L), permethrin (0.1, 1, 10 µg/L), and ethinylestradiol (1, 10, 50 ng/L) had significantly higher ng/mL choriogenin (Chg) measured in whole body homogenate than controls. While Chg expression in fish exposed to ethinylestradiol (EE2) exhibited a traditional sigmoidal concentration-response, curves fit to Chg expressed in fish exposed to pyrethroids suggest a unimodal response, decreasing slightly as concentration increases. While the in vivo response indicated that bifenthrin and permethrin or their metabolites act as estrogen agonists, the CALUX assay demonstrated estrogen antagonism by the pyrethroids. Our results, supported by evidence from previous studies, suggest that bifenthrin and permethrin, and/or their metabolites, appear to act as estrogen receptor (ER) agonists in vivo, and that the unmetabolized pyrethroids, particularly bifenthrin, act as an ER antagonists in cultured mammalian cells. PMID:23007834

  4. Antiangiogenic Activity of Acer tegmentosum Maxim Water Extract in Vitro and in Vivo.

    PubMed

    Kim, Eok-Cheon; Kim, So Hun; Piao, Shan-Ji; Kim, Tack-Joong; Bae, Kiho; Kim, Han Sung; Hong, Soon-Sun; Lee, Byoung Ick; Nam, Moonsuk

    2015-07-01

    Angiogenesis, the formation of new blood vessels, is critical for tumor growth and metastasis. Notably, tumors themselves can lead to angiogenesis by inducing vascular endothelial growth factor (VEGF), which is one of the most potent angiogenic factors. Inhibition of angiogenesis is currently perceived as one of the most promising strategies for the blockage of tumor growth. In this study, we investigated the effects of Acer tegmentosum maxim water extract (ATME) on angiogenesis and its underlying signal mechanism. We studied the antiangiogenic activity of ATME by using human umbilical vein endothelial cells (HUVECs). ATME strongly inhibited VEGF-induced endothelial cell proliferation, migration, invasion, and tube formation, as well as vessel sprouting in a rat aortic ring sprouting assay. Moreover, we found that the p44/42 mitogen activated protein (MAP) kinase signaling pathway is involved in the inhibition of angiogenesis by ATME. Moreover, when we performed the in vivo matrigel plug assay, VEGF-induced angiogenesis was potently reduced when compared to that for the control group. Taken together, these results suggest that ATME exhibits potent antiangiogenic activity in vivo and in vitro and that these effects are regulated by the extracellular regulated kinase (ERK) pathway. PMID:26130964

  5. Synthesis and in vitro antiproliferative activity of amido and amino analogues of the marine alkaloid isogranulatimide.

    PubMed

    Lavrard, Hubert; Salvetti, Béatrice; Mathieu, Véronique; Rodriguez, Frédéric; Kiss, Robert; Delfourne, Evelyne

    2015-04-01

    Marine organisms have proven to be a promising source of new compounds with activity against tumor cell lines. Granulatimide and isogranulatimide are marine alkaloids that have been shown to inhibit checkpoint kinase 1 (Chk1), a key protein in the DNA damage response and an emerging target for anticancer therapeutics. Here, we describe the synthesis and preliminary evaluation of amido and amino analogues of isogranulatimide. The new derivatives were prepared in three steps from 2-imidazol-1-yl-1H-indol-5-ylamine. Two of the compounds synthesized exhibited more potent in vitro antiproliferative activity (single-digit micromolar concentration range), by at least one log of magnitude, than the natural product isogranulatimide when evaluated in six human tumor cell lines: non-small-cell lung cancer (A549), colon cancer (LoVo), breast cancer (MCF7), oligodendroglioma (Hs683), glioblastoma (U373), and melanoma (SKMEL28). The mechanism of action of these derivatives remains to be elucidated, given that they did not significantly inhibit Chk1, however these compounds are easily synthesized and exhibit potent anticancer activity and are thus worthy of further study. PMID:25735892

  6. In vitro evaluation of antimicrobial activity of sealers and pastes used in endodontics.

    PubMed

    Leonardo, M R; da Silva, L A; Tanomaru Filho, M; Bonifácio, K C; Ito, I Y

    2000-07-01

    The antimicrobial activity of four root canal sealers (AH Plus, Sealapex, Ketac Endo, and Fill Canal), two calcium hydroxide pastes (Calen and Calasept), and a zinc oxide paste was evaluated. Seven bacterial strains were used, six of them standard; Micrococcus luteus ATCC 9341, Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Staphylococcus epidermidis ATCC 12228, Escherichia coli ATCC 25922, and Enterococcus faecalis ATCC 10541. There was a wild strain of Streptococcus mutans isolated from saliva obtained in an adult dental clinic. Activity was evaluated using the agar diffusion method with Brain Heart Infusion agar and Müller Hinton medium seeded by pour plate. Calcium hydroxide-based sealers and pastes were either placed directly into 4.0 x 4.0 mm wells or by using absorbent paper points. The plates were kept at room temperature for 2 hr for diffusion. After incubation at 37 degrees C for 24 hr, the medium was optimized with 0.05 g% TTC gel and inhibition haloes were measured. All bacterial strains were inhibited by all materials using the well method. However, when the materials were applied with absorbent paper points, Enterococcus faecalis was not inhibited by zinc oxide, and Pseudomonas aeruginosa was not inhibited by AH Plus, Fill Canal, and the zinc oxide-based paste. We conclude that sealers and pastes presented antimicrobial activity in vitro and culture medium optimization with 0.05 g% TTC gel facilitated observation of the inhibition haloes. PMID:11199762

  7. Environmental gestagens activate fathead minnow (Pimephales promelas) nuclear progesterone and androgen receptors in vitro.

    PubMed

    Ellestad, Laura E; Cardon, Mary; Chambers, Ian G; Farmer, Jennifer L; Hartig, Phillip; Stevens, Kyle; Villeneuve, Daniel L; Wilson, Vickie; Orlando, Edward F

    2014-07-15

    Gestagen is a collective term for endogenous and synthetic progesterone receptor (PR) ligands. In teleost fishes, 17?,20?-dihydroxy-4-pregnen-3-one (DHP) and 17?,20?,21-trihydroxy-4-pregnen-3-one (20?-S) are the predominant progestogens, whereas in other vertebrates the major progestogen is progesterone (P4). Progestins are components of human contraceptives and hormone replacement pharmaceuticals and, with P4, can enter the environment and alter fish and amphibian reproductive health. In this study, our primary objectives were to clone the fathead minnow (FHM) nuclear PR (nPR), to develop an in vitro assay for FHM nPR transactivation, and to screen eight gestagens for their ability to transactivate FHM nPR. We also investigated the ability of these gestagens to transactivate FHM androgen receptor (AR). Fish progestogens activated FHM nPR, with DHP being more potent than 20?-S. The progestin drospirenone and P4 transactivated the FHM nPR, whereas five progestins and P4 transactivated FHM AR, all at environmentally relevant concentrations. Progestins are designed to activate human PR, but older generation progestins have unwanted androgenic side effects in humans. In FHMs, several progestins proved to be strong agonists of AR. Here, we present the first mechanistic evidence that environmental gestagens can activate FHM nPR and AR, suggesting that gestagens may affect phenotype through nPR- and AR-mediated pathways. PMID:24911891

  8. Phospholipase A2 activation by hydrogen peroxide during in vitro capacitation of buffalo spermatozoa.

    PubMed

    Shit, Sanjoy; Atreja, S K

    2004-05-01

    Progressively motile, washed buffalo spermatozoa (50 x 10(6) cells in 0.5 ml) were in vitro capacitated in HEPES containing Bovine Gamete Medium 3 (BGM3) in presence of heparin (10 microg/ml), and different concentrations of hydrogen peroxide (10 to 100 microM). Spermatozoa (60%) were capacitated in presence of heparin compared to 56% in presence of 25 microM H2O2 (optimally found suitable for capacitation). The extent of capacitation was measured in terms of acrosome reaction (AR) induced by lysophosphatidyl choline (100 microg/ml). The acrosome reacted cells were counted after triple staining. Catalase (100 microg/ml) significantly reduced the sperm capacitation to 16-18% when added with H2O2, or alone in the capacitation medium. Phospholipase A2 activity of spermatozoa increased linearly up to 50 microM H2O2 concentration included in the assay system. Moreover, significant increase in phospholipase A2 activity was observed after capacitation by both, the heparin and 25 microM H2O2. The activity was always higher in acrosome reacted cells. PMID:15233473

  9. In vitro anti-influenza virus activity of a cardiotonic glycoside from Adenium obesum (Forssk.).

    PubMed

    Kiyohara, Hiroaki; Ichino, Chikara; Kawamura, Yuka; Nagai, Takayuki; Sato, Noriko; Yamada, Haruki; Salama, Maha M; Abdel-Sattar, Essam

    2012-01-15

    Methanolic extracts of six Saudi plants were screened for their in vitro antiviral activity using influenza virus A/PR/8/34 (H1N1) and MDCK cells in an MTT assay. The results indicated that the extracts of Adeniumobesum and Tephorosianubica possessed antiviral activity (99.3 and 93.3% inhibition at the concentration of 10 ?g/ml, respectively). Based on these results A. obesum was selected for further study by applying bioactivity-guided fractionation to isolate its antiviral principle. The antiviral principle was isolated from the chloroform fraction through solvent fractionation, combined open liquid chromatography and HPLC. The isolated active compound A was identified as oleandrigenin-?-D-glucosyl (1?4)-?-D-digitalose, on the basis of its spectral analysis (MS, 1D and 2D NMR). The isolated glycoside showed reduction of virus titre by 69.3% inhibition at concentration of 1 ?g/ml (IC(50)=0.86 ?g/ml). PMID:21899996

  10. In vitro bioassays to screen for endocrine active pharmaceuticals in surface and waste waters.

    PubMed

    Kunz, Petra Y; Kienle, Cornelia; Carere, Mario; Homazava, Nadzeya; Kase, Robert

    2015-03-15

    In the context of the European Water Framework Directive (WFD) it is fully recognized that pharmaceuticals can represent a relevant issue for the achievement of the good chemical and ecological status of European surface water bodies. The recent European Directive on the review of priority substances in surface water bodies has included three pharmaceuticals of widespread use (diclofenac, 17?-ethinylestradiol (EE2), 17?-estradiol (E2)) in the European monitoring list, the so-called watch list. Endocrine active pharmaceuticals such as EE2 and E2 (also occurring as natural hormone) can cause adverse effects on aquatic ecosystems at very low levels. However, monitoring of these pharmaceuticals within the watch list mechanism of the WFD and national monitoring programs can be difficult because of detection problems of most routine analytical methods. With proposed annual average Environmental Quality Standards (AA-EQS) of 0.035 ng/L and 0.4 ng/L, respectively, the estrogenic pharmaceutical EE2 and the natural hormone E2 are among those substances. Sensitive in vitro bioassays could reduce the current detection problems by measuring the estrogenic activity of environmental samples. In a short review article the application of this approach to screen and assess the risks of endocrine active pharmaceuticals with a focus on estrogenic pharmaceuticals in environmental waters is discussed. PMID:25555519

  11. In vitro antimicrobial activity of ethanol and water extracts of Cassia alata.

    PubMed

    Somchit, M N; Reezal, I; Nur, I Elysha; Mutalib, A R

    2003-01-01

    Crude ethanol and water extract of leaves and barks from Cassia alata were tested in vitro against fungi, (Aspergillus fumigatus and Microsporum canis), yeast (Candida albicans) and bacteria (Staphylococcus aereus and Escherichia coli). C. albicans showed concentration-dependent susceptibility towards both the ethanol and water extracts from the barks, but resistant towards the extracts of leaves. The degree of susceptibility varied, the water extract from barks showed bigger inhibition zone than the ethanol extracts (12-16 and 10-14 mm, diameter respectively). The growth of Aspergillus fumigatus and Microsporum canis were not affected by all types of the plant extracts. Results were comparable to standard antifungal drug Tioconazole (18 mm diameter) at equivalent concentration. The anti-bacterial activity of C. alata extracts on S. aureus was detected with only the leaves extracts using water and ethanol. The water extract exhibited higher antibacterial activity than the ethanol extract from leaves (inhibition zones of 11-14 and 9-11 mm, respectively). E. coli showed resistance to all types of extracts. Based on the current findings, it can be concluded that this plant has antimicrobial activity, which is as potent as standard antimicrobial drugs against certain microorganisms. PMID:12499068

  12. Activity and interactions of antibiotic and phytochemical combinations against Pseudomonas aeruginosa in vitro

    PubMed Central

    Jayaraman, Premkumar; Sakharkar, Meena K; Lim, Chu Sing; Tang, Thean Hock; Sakharkar, Kishore R.

    2010-01-01

    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

  13. Activity and interactions of antibiotic and phytochemical combinations against Pseudomonas aeruginosa in vitro.

    PubMed

    Jayaraman, Premkumar; Sakharkar, Meena K; Lim, Chu Sing; Tang, Thean Hock; Sakharkar, Kishore R

    2010-01-01

    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

  14. In Vitro Antileishmanial Activity of Essential Oil of Vanillosmopsis arborea (Asteraceae) Baker

    PubMed Central

    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

    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

  15. In Vitro Nail Penetration and Antifungal Activity of Tavaborole, a Boron-Based Pharmaceutical.

    PubMed

    Coronado, Dina; Merchant, Tejal; Chanda, Sanjay; Zane, Lee T

    2015-06-01

    An effective topical antifungal medication must penetrate through the nail plate at sufficient concentrations to eradicate the fungal infection. Tavaborole topical solution, 5% is a novel boron-based pharmaceutical approved for the treatment of toenail onychomycosis due to Trichophyton rubrum or T mentagrophytes. Four in vitro studies assessed the antifungal activity and nail penetration of tavaborole. In Study 1, tavaborole demonstrated minimum inhibitory concentration (MIC) values ranging from 0.25-2 ?g/mL against all fungi tested; addition of 5% keratin powder did not affect the MIC against T rubrum. The minimum fungicidal concentration (MFC) values for tavaborole against T rubrum and T mentagrophytes were 8 and 16 ?g/mL, respectively. In Study 2, tavaborole effectively penetrated through the nail plate; mean concentrations in the ventral/intermediate nail layer were significantly higher than ciclopirox at day 15. In Study 3, mean cumulative tavaborole penetration through ex vivo human nails was significantly higher than ciclopirox at day 15. In Study 4, tavaborole demonstrated superior nail penetration and fungicidal activity, as measured by zones of inhibition. These studies demonstrated the superior penetration of tavaborole through the nail plate vs ciclopirox. Tavaborole demonstrated robust antifungal activity, with low MIC and MFC values, even in the presence of keratin.

    J Drugs Dermatol. 2015;14(6):609-614.. PMID:26091387

  16. Acaricidal activity of extracts from Ligularia virgaurea against the Sarcoptes scabiei mite in vitro

    PubMed Central

    LUO, BIAO; LIAO, FEI; HU, YANCHUN; LIU, XI; HE, YAJUN; WU, LEI; TAN, HUI; LUO, LIJUAN; ZHOU, YANCHENG; MO, QUAN; DENG, JUNLIANG; WEI, YAHUI

    2015-01-01

    The aim of the present study was to investigate the acaricidal activity of Ligularia virgaurea. An extract was prepared by refluxing with ethanol and steam distillation, and its toxic effect was tested in vitro against Sarcoptes scabiei. The data from the toxicity tests were analyzed using a complementary log-log (CLL) model. The ethanol extract exhibited strong acaricidal activity against these mites; at a concentration of 2 g/ml it killed all S. scabiei within 2 h and at 1 g/ml it killed all S. scabiei within 6 h. Similarly, 2, 1, 0.5 and 0.25 g/ml concentrations of the extract had strong toxicity against S. scabiei, with median lethal time (LT50) values of 0.716, 1.741, 2.968 and 4.838 h, respectively. The median lethal concentration (LC50) values were 1.388, 0.624, 0.310 and 0.213 g/ml for Scabies mite in 1, 2, 4 and 6 h, respectively. The results indicate that the L. virgaurea extract has strong acaricidal activity and may be exploited as a novel treatment for the effective control of acariasis in animals. PMID:26170943

  17. Mutagenicity studies in a tyre plant: in vitro activity of workers' urinary concentrates and raw materials.

    PubMed

    Crebelli, R; Paoletti, A; Falcone, E; Aquilina, G; Fabri, G; Carere, A

    1985-07-01

    The possible contribution to urinary mutagenicity of occupational exposures in the rubber industry was studied by assaying the urine concentrates of 72 workmen (44 smokers) employed in a tyre plant. Twenty three clerks (16 smokers) engaged in the administrative department of the same factory served as presumptive unexposed controls. XAD-2 resin concentrates of urine samples were assayed in the plate incorporation test and in the microtitre fluctuation assay with Salmonella typhimurium strains TA1535, TA98, and TA100. Furthermore, the in vitro mutagenicity of the major raw materials in use at the plant was determined in the plate incorporation assay with S typhimurium strains TA1535, TA1537, TA98, and TA100. The results obtained from the urinary mutagenicity study show that smoking habits, but not occupation, were statistically significantly related to the appearance of a urinary mutagenicity that was detectable with strain TA98. A possible synergistic effect of occupation with smoking was observed among tyre builders who were also smokers. The study of the raw materials showed that three technical grade materials were weakly active as mutagens in strain TA98 in the absence (poly-p-dinitrosobenzene) or in the presence of metabolic activation (mixed diaryl-p-phenylendiamines and tetramethyltiuram disulphide). The latter chemical was also weakly active in strain TA100. PMID:4015996

  18. Zinc ascorbate has superoxide dismutase-like activity and in vitro antimicrobial activity against Staphylococcus aureus and Escherichia coli

    PubMed Central

    Iinuma, Katsuhiro; Tsuboi, Isami

    2012-01-01

    Background: Acne vulgaris is a common dermatological disease, and its pathogenesis is multifactorial. Objective: We examined whether the ascorbic acid derivative zinc ascorbate has superoxide dismutase (SOD)-like activity. SOD is an enzyme that controls reactive oxygen species production. In addition, the in vitro antimicrobial activity of zinc ascorbate against the Gram-positive bacterium Staphylococcus aureus and the Gram-negative bacterium Escherichia coli was tested either alone or in combination with a variety of antimicrobial agents; their fractional inhibitory concentration index was determined using checkerboard tests. Methods: The SOD-like activity was measured in comparison with other ascorbic acid derivatives (ascorbic acid, magnesium ascorbyl phosphate, and sodium ascorbyl phosphate) and zinc. The antimicrobial susceptibility of twelve strains each of S. aureus and E. coli isolated from patients with dermatological infections was tested, in comparison to a type strain of S. aureus and E. coli. Results: Zinc ascorbate had significant (P < 0.001) SOD-like activity compared with other ascorbic acid derivatives and zinc. Moreover, it showed antimicrobial activity against a type strain of S. aureus and E. coli, and its concentration (0.064% and 0.128% for S. aureus and E. coli, respectively) was sufficiently lower than the normal dose (5%) of other ascorbic acid derivatives. Furthermore, combinations of zinc ascorbate with clindamycin, erythromycin, and imipenem against S. aureus (average fractional inhibitory concentration, 0.59–0.90), and with imipenem against E. coli (average fractional inhibitory concentration, 0.64) isolated from patients with dermatological infections showed an additive effect. Conclusions: Our results provide novel evidence that zinc ascorbate may be effective for acne treatment. PMID:23055762

  19. Noradrenergic modulation of activity in a vocal control nucleus in vitro

    PubMed Central

    Solis, Michele M.; Perkel, David J.

    2006-01-01

    Norepinephrine (NE) can profoundly modulate sensory processing, but its effect on motor function is less well understood. Birdsong is a learned behavior involving sensory and motor processes that are influenced by NE. A potential site of NE action is the robust nucleus of the arcopallium (RA): RA receives noradrenergic inputs and has adrenergic receptors, and it is a sensorimotor area instrumental to song production. We hypothesized that NE modulates RA neurons, and as a first test, we examined the effect of NE on RA activity in vitro. We recorded spontaneous activity extracellularly from isolated RA neurons in brain slices made from adult male zebra finches. These neurons exhibited regular tonic activity with firing rates averaging 5.5 Hz. Bath application of NE rapidly and reversibly decreased firing for the majority of neurons, to the extent that spontaneous activity was often abolished. This was likely a direct effect on the cell recorded, since it occurred with blockade of fast excitatory and inhibitory synaptic transmission, or of all synaptic transmission. The NE-induced suppression involved the ?2-adrenergic receptor: yohimbine, an antagonist, completely reversed the suppression, and clonidine, an agonist, partially mimicked it. Perforated patch recordings revealed that NE induced a conductance increase in RA neurons; however, this did not prevent cells from firing when stimulated by afferents in HVC. For some neurons, NE application resulted in an increase in signal-to-noise ratio for spikes evoked by HVC stimulation. Thus, NE could strongly modulate the spontaneous activity of RA cells, potentially enhancing signals relayed through RA. PMID:16371453

  20. Cannabinoid effects on ? amyloid fibril and aggregate formation, neuronal and microglial-activated neurotoxicity in vitro.

    PubMed

    Janefjord, Emelie; Mĺĺg, Jesper L V; Harvey, Benjamin S; Smid, Scott D

    2014-01-01

    Cannabinoid (CB) ligands have demonstrated neuroprotective properties. In this study we compared the effects of a diverse set of CB ligands against ? amyloid-mediated neuronal toxicity and activated microglial-conditioned media-based neurotoxicity in vitro, and compared this with a capacity to directly alter ? amyloid (A?) fibril or aggregate formation. Neuroblastoma (SH-SY5Y) cells were exposed to A?1-42 directly or microglial (BV-2 cells) conditioned media activated with lipopolysaccharide (LPS) in the presence of the CB1 receptor-selective agonist ACEA, CB2 receptor-selective agonist JWH-015, phytocannabinoids ?(9)-THC and cannabidiol (CBD), the endocannabinoids 2-arachidonoyl glycerol (2-AG) and anandamide or putative GPR18/GPR55 ligands O-1602 and abnormal-cannabidiol (Abn-CBD). TNF-? and nitrite production was measured in BV-2 cells to compare activation via LPS or albumin with A?1-42. A?1-42 evoked a concentration-dependent loss of cell viability in SH-SY5Y cells but negligible TNF-? and nitrite production in BV-2 cells compared to albumin or LPS. Both albumin and LPS-activated BV-2 conditioned media significantly reduced neuronal cell viability but were directly innocuous to SH-SY5Y cells. Of those CB ligands tested, only 2-AG and CBD were directly protective against A?-evoked SH-SY5Y cell viability, whereas JWH-015, THC, CBD, Abn-CBD and O-1602 all protected SH-SY5Y cells from BV-2 conditioned media activated via LPS. While CB ligands variably altered the morphology of A? fibrils and aggregates, there was no clear correlation between effects on A? morphology and neuroprotective actions. These findings indicate a neuroprotective action of CB ligands via actions at microglial and neuronal cells. PMID:24030360

  1. In vitro studies on antilithiatic activity of seeds of Dolichos biflorus Linn. and rhizomes of Bergenia ligulata Wall.

    PubMed

    Garimella, T S; Jolly, C I; Narayanan, S

    2001-06-01

    Soxhlet extracts of seeds of Dolichos biflorus and rhizomes of Bergenia ligulata were tested for their in vitro antilithiatic/anticalcification activity by the homogeneous precipitation method. The extracts were compared with an aqueous extract of cystone (a marketed preparation) for their activities. Also a combination of the extracts of the two plants was tested. Extracts of Dolichus biflorus showed activity almost equivalent to cystone while Bergenia ligulata showed less activity and the combination was not as active as the individual extracts. PMID:11406861

  2. [In vitro study of the antifungal activity of two chlorine derivatives to be used in antisepsis].

    PubMed

    Bianchi, P; Repetto, A; Bulletti, S; Mattiacci, P; Rossi, J; Pagiotti, R; Ribaldi, M; Schiaffella, F

    1989-01-01

    The activity of two chlorine derivates, sodium hypochlorite in water solution with NaCl (product A) and electrolytic chloroxidant (product B) has been tested in vitro against potentially human pathogenic fungi (Aspergillus niger, Aspergillus fumigatus, Microsporum gypseum, Candida albicans, Cryptococcus neoformans, Trichophyton mentagrophytes, Microsporum canis, Epidermophyton floccosum, Trichophyton rubrum, Sporotrix schenkii). For A. niger, the relation of the two compounds has also been considered between mycelial and sporidial forms. Dilutions used ranged from 0.15 to 10% (corresponding to 17.2-1150 ppm of active principle for product A, and to 18.3-1220 ppm of active principle for product B). These were applied for different times in order to assess the minimal inhibitory concentration (M.I.C.) and to evaluate the survival time of the microorganisms tested, which were strains from the collection of the Institute of Mycology, (Faculty of Agrarian Science, Perugia) and recently isolated ones from animal and vegetable tissues, cultivated on Sabouraud medium. The cell suspension to be tested was obtained on nutrient broth in shaken flasks (120 rpm) at 28 degrees C for 48 h, and was separated by centrifugation and 10000 rpm at 5 degrees C for 20 min, repeatedly washed with sterile physiologic saline and resuspended in sterile water where it was submitted to delicate pressure in order to fragment the mycelium. Activity tests were carried out on Sabouraud broth and Sabouraud agar with controls for every case without the active principle. Aliquots of the suspensions (microrganism++ + disinfectant) were transferred at regular intervals (1, 3, 5 and 10 minutes) to the two substrates in liquid and solid state, and the growth of microorganisms was followed at 28 degrees C for 48-72 h in the case of yeasts, and for up to 21 days in the case of sower growing fungi. The cell content of the different suspensions was found to range from 10(4) to 10(9) UFC/ml. The active chlorine contents of the two compounds was evaluated by iodometry simultaneously with the pH of the different solutions. Useful data were obtained from the comparison of the two systems of activity assessment of the fluid and agarized substrate. It was thus found that the two compounds were equally active against the species tested. Some of these (A. fumigatus, M. gypseum, A. niger, C. albicans, C. neoformans) were less sensitive to the compounds examined (doses for cell inactivation 0.62-2.5% for product A, and O.15-1.25% for product B) where at any rate product B was more active.(ABSTRACT TRUNCATED AT 400 WORDS) PMID:2483652

  3. Differential activation of NF-?B and nitric oxide in lymphocytes regulates in vitro and in vivo radiosensitivity

    PubMed Central

    Sharma, Deepak; Sandur, Santosh K.; Rashmi, R.; Maurya, D.K.; Suryavanshi, Shweta; Checker, Rahul; Krishnan, Sunil; Sainis, K.B.

    2011-01-01

    Lymphocytes are more sensitive to radiation in vivo than in vitro. However, the mechanism of this differential response is poorly understood. In the present study, it was found that the lipid peroxidation and cell death were significantly higher in lymphocytes following whole body irradiation (WBI) as compared to lymphocytes exposed to radiation in vitro. EL-4 cells transplanted in mice were also more sensitive to radiation than EL-4 cells irradiated in vitro. DNA repair, as assessed by comet assay, was significantly faster in lymphocytes exposed to 4 Gy radiation in vitro as compared to that in lymphocytes obtained from whole body irradiated mice exposed to the same dose of radiation. This was associated with increased NF-?B activation in response to genotoxic stress and lesser activation of caspase in lymphocytes in vitro compared to in vivo. To explain the differential radiosensitivity, we postulated a role of nitric oxide, an extrinsic diffusible mediator of radiosensitivity that has also been implicated in DNA repair inhibition. Nitric oxide levels were significantly elevated in the plasma of whole body irradiated mice but not in the supernatant of cells irradiated in vitro. Addition of sodium nitroprusside (SNP), a nitric oxide donor to cells irradiated in vitro inhibited the repair of DNA damage and enhanced apoptosis (increased Bax to Bcl-2 ratio). Administration of L-NAME, a nitric oxide synthase inhibitor, to mice significantly protected lymphocytes against WBI-induced DNA damage and inhibited in vivo radiation-induced production of nitric oxide. These results confirm that the observed differential radiosensitivity of lymphocytes was due to slow repair of DNA due to nitric oxide production in vivo. PMID:20732448

  4. In vitro metabolism and bioavailability tests for endocrine active substances: What is needed next for regulatory purposes?

    EPA Science Inventory

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

  5. Effect of plant extracts on in vitro methanogenesis, enzyme activities and fermentation of feed in rumen liquor of buffalo

    Microsoft Academic Search

    A. K. Patra; D. N. Kamra; Neeta Agarwal

    2006-01-01

    The extracts of pods of Acacia concinna (Shikakai), seed pulp of Terminalia chebula (harad), Terminalia belerica (bahera), Emblica officinalis (amla) and seed kernel of Azadirachta indica (neem seed) in different solvents (ethanol, methanol and water) were evaluated for their effect on methane production, enzymes activities and rumen fermentation in in vitro gas production test. Gas production per gram dry matter

  6. Antifungal Activity of the Essential Oil of Melaleuca alternifolia (Tea Tree Oil) against Pathogenic Fungi in vitro

    Microsoft Academic Search

    P. Nenoff; U.-F. Haustein; W. Brandt

    1996-01-01

    The in vitro antifungal activity of tea oil, the essential oil of Melaleuca alternifolia, has been evaluated against 26 strains of various dermatophyte species, 54 yeasts, among them 32 strains of Candida albicans and other Candida sp. as well as 22 different Malassezia furfur strains. Minimum inhibitory concentrations (MIC) of tea tree oil were measured by agar dilution technique. Tea

  7. Transforming Growth Factor (TGF ) Mediates Schwann Cell Death In Vitro and In Vivo: Examination of c-Jun Activation,

    E-print Network

    Jessen, Kristjan R

    cell death, seen for example in normal and, especially, injured neonatal nerves, is caused by a limitedTransforming Growth Factor (TGF ) Mediates Schwann Cell Death In Vitro and In Vivo: Examination of c-Jun Activation, Interactions with Survival Signals, and the Relationship of TGF -Mediated Death

  8. In Vitro Activities of Retigeric Acid B Alone and in Combination with Azole Antifungal Agents against Candida albicans

    Microsoft Academic Search

    Lingmei Sun; Shujuan Sun; Aixia Cheng; Xiuzhen Wu; Yu Zhang; Hongxiang Lou

    2009-01-01

    The vitro antifungal activity of retigeric acid B (RAB), a pentacyclic triterpenoid from the lichen species Lobaria kurokawae, was evaluated alone and in combination with fluconazole, ketoconazole, and itraconazole against Candida albicans using checkerboard microdilution and time-killing tests. The MICs for RAB against 10 different C. albicans isolates ranged from 8 to 16 g\\/ml. A synergistic action of RAB and

  9. Development of an In Vitro Activity Assay as an Alternative to the Mouse Bioassay for Clostridium botulinum Neurotoxin Type A

    Microsoft Academic Search

    Reuven Rasooly; Paula M. Do

    2008-01-01

    Currently, the only accepted assay with which to detect active Clostridium botulinum neurotoxin is an in vivo mouse bioassay. The mouse bioassay is sensitive and robust and does not require specialized equipment. However, the mouse bioassay is slow and not practical in many settings, and it results in the death of animals. Here, we describe an in vitro cleavage assay

  10. Toxicity of Australian essential oil Backhousia citriodora (Lemon myrtle). Part 1. Antimicrobial activity and in vitro cytotoxicity

    Microsoft Academic Search

    A. J. Hayes; B. Markovic

    2002-01-01

    The antimicrobial and toxicological properties of the Australian essential oil, lemon myrtle, (Backhousia citriodora) were investigated. Lemon myrtle oil was shown to possess significant antimicrobial activity against the organisms Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, methicillin-resistant S. aureus (MRSA), Aspergillus niger, Klebsiella pneumoniae and Propionibacterium acnes comparable to its major component-citral. An in vitro toxicological study based on

  11. In vitro evaluation of antioxidant activities of aqueous extracts from natural and cultured mycelia of Cordyceps sinensis

    Microsoft Academic Search

    C.-H. Dong; Y.-J. Yao

    2008-01-01

    Cordyceps sinensis, one of the best known traditional Chinese medicines and health foods, has been highly valued for the treatment of a wide range of diseases and reported to have antioxidant properties. In the present study, the antioxidant activities of hot-water extracts from natural and cultured mycelia of C. sinensis were investigated and evaluated using six in vitro assays, including

  12. In Vitro Assays for Assessment of Androgenic and Estrogenic Activity of Defined Mixtures and Complex Environmental Samples

    EPA Science Inventory

    Point sources of 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 assays des...

  13. Studies on the effect of bile and lipolysis products on pancreatic lipase and colipase activity in vitro

    E-print Network

    Paris-Sud XI, Université de

    Studies on the effect of bile and lipolysis products on pancreatic lipase and colipase activity triolein by pancreatic lipase in vitro. The addition of colipase in excess to lipase failed to restore, monoacylglycerol and free fatty acid was hydrolysed by lipase and colipase in the presence of bile. The results

  14. In Vitro Activity of Daptomycin against Vancomycin-Resistant Enterococci of Various Van Types and Comparison of Susceptibility Testing Methods

    Microsoft Academic Search

    James H. Jorgensen; Sharon A. Crawford; Cynthia C. Kelly; Jan E. Patterson

    2003-01-01

    The increasing prevalence of vancomycin-resistant enterococcal (VRE) infections and the limited number of antimicrobial agents for their treatment emphasize a need for new, more effective agents. In this study, the in vitro activity of daptomycin was determined against a collection of 156 VRE from seven different institutions. Van types were characterized by PCR, and pulsed-field gel electrophoresis was performed to

  15. IN VIVO AND IN VITRO STRUCTURE-DOSIMETRY-ACTIVITY RELATIONSHIPS OF SUBSTITUTED PHENOLS IN DEVELOPMENTAL TOXICITY ASSAYS

    EPA Science Inventory

    Structure-dosimetry-activity relationships (SDARs) of a series of substituted phenols were evaluated following exposure of gestation day 11 rats in vivo and in comparable stage embryos in vitro. n the in vivo study, 27 congeners were assayed and log p (a term used synonymously wi...

  16. Pomegranate ellagitannins inhibit ?-glucosidase activity in vitro and reduce starch digestibility under simulated gastro-intestinal conditions.

    PubMed

    Bellesia, Andrea; Verzelloni, Elena; Tagliazucchi, Davide

    2015-02-01

    Pomegranate extract was tested for its ability to inhibit ?-amylase and ?-glucosidase activity. Pomegranate extract strongly inhibited rat intestinal ?-glucosidase in vitro whereas it was a weak inhibitor of porcine ?-amylase. The inhibitory activity was recovered in an ellagitannins-enriched fraction and punicalagin, punicalin, and ellagic acid were identified as ?-glucosidase inhibitors (IC(50) of 140.2, 191.4, and 380.9??mol/L, respectively). Kinetic analysis suggested that the pomegranate extract and ellagitannins inhibited ?-glucosidase activity in a mixed mode. The inhibitory activity was demonstrated using an in vitro digestion system, mimicking the physiological gastro-intestinal condition, and potatoes as food rich in starch. Pre-incubation between ellagitannins and ?-glucosidase increased the inhibitory activity, suggesting that they acted by binding to ?-glucosidase. During digestion punicalin and punicalagin concentration decreased. Despite this loss, the pomegranate extract retained high inhibitory activity. This study suggests that pomegranate ellagitannins may inhibit ?-glucosidase activity in vitro possibly affecting in vivo starch digestion. PMID:25519249

  17. Inhibition of ongoing myeloma IgE synthesis in vitro by activated human T cells.

    PubMed

    Hassner, A; Saxon, A

    1983-04-01

    The ability of activated T cells to suppress ongoing IgE synthesis in vitro was assessed using U266--a human myeloma cell line spontaneously producing IgE. T cells were able to inhibit U266 IgE synthesis in the presence of 10 micrograms/ml of Con A by 41.8% (p less than 0.01). T cells preincubated with 10 or 50 micrograms/ml of Con A and washed extensively were still able to inhibit U266 IgE synthesis in the absence of Con A by 41 and 46% (p less than 0.05 and p less than 0.02, respectively). The decrease in IgE measured was due to inhibition of newly formed IgE by U266, as shown by control experiments with cycloheximide. The inhibition was not due to the simple depletion of nutrient growth factors by the activated T cells, as it did not occur with MOLT-4, T cells that are very active metabolically; nor could it be reversed with medium containing IL 2 and B cell growth factors. Culture supernatants of Con A-activated T cells were also able to suppress IgE synthesis by U266 (21%; p less than 0.01), which suggests that upon appropriate activation, T cells secrete material(s) with inhibitory properties for IgE synthesis. Activation of T cells by mixed lymphocyte culture using puromycin-treated lymphoblastoid cell lines as stimulators also generated T cells that had suppressive activity for IgE synthesis. T cells activated with Con A and subsequently incubated with IgE demonstrated a diminished ability to suppress IgE synthesis. This observation is in agreement with the finding that patients with high levels of IgE may lack isotype-specific suppressor T cells for spontaneous IgE secretion. However, T cells from such patients have so far shown variable loss of IgE suppressive function. These results suggest that human IgE synthesis is susceptible to inhibition at a very differentiated stage, and this may be important in expression of allergic diseases. PMID:6220058

  18. Activated rat hepatic stellate cells influence Th1/Th2 profile in vitro

    PubMed Central

    Xing, Zhi-Zhi; Huang, Liu-Ye; Wu, Cheng-Rong; You, Hong; Ma, Hong; Jia, Ji-Dong

    2015-01-01

    AIM: To investigate the effects of activated rat hepatic stellate cells (HSCs) on rat Th1/Th2 profile in vitro. METHODS: Growth and survival of activated HSCs and CD4+ T lymphocytes cultured alone or together was assessed after 24 or 48 h. CD4+ T lymphocytes were then cultured with or without activated HSCs for 24 or 48 h and the proportion of Th1 [interferon (IFN)-?+] and Th2 [interleukin (IL)-4+] cells was assessed by flow cytometry. Th1 and Th2 cell apoptosis was assessed after 24 h of co-culture using a caspase-3 staining procedure. Differentiation rates of Th1 and Th2 cells from CD4+ T lymphocytes that were positive for CD25 but did not express IFN-? or IL-4 were also assessed after 48 h of co-culture with activated HSCs. Galectin-9 expression in HSCs was determined by immunofluorescence and Western blotting. ELISA was performed to assess galectin-9 secretion from activated HSCs. RESULTS: Co-culture of CD4+ T lymphocytes with activated rat HSCs for 48 h significantly reduced the proportion of Th1 cells compared to culture-alone conditions (-1.73% ± 0.71%; P < 0.05), whereas the proportion of Th2 cells was not altered; the Th1/Th2 ratio was significantly decreased (-0.44 ± 0.13; P < 0.05). In addition, the level of IFN-? in Th1 cells was decreased (-65.71 ± 9.67; P < 0.01), whereas the level of IL-4 in Th2 cells was increased (82.79 ± 25.12; P < 0.05) by co-culturing, as measured by mean fluorescence intensity by flow cytometry. Apoptosis rates in Th1 (12.27% ± 0.99%; P < 0.01) and Th2 (1.71% ± 0.185%; P < 0.01) cells were increased 24 h after co-culturing with activated HSCs; the Th1 cell apoptosis rate was significantly higher than in Th2 cells (P < 0.01). Galectin-9 protein expression was significantly decreased in HSCs only 24 h after co-culturing (P < 0.05) but not after 48 h. Co-culture for 48 h significantly increased the differentiation of Th1 and Th2 cells; however, the increase in the proportion of Th2 cells was significantly higher than that of Th1 cells (1.85% ± 0.48%; P < 0.05). CONCLUSION: Activated rat HSCs lower the Th1/Th2 profile, inhibiting the Th1 response and enhancing the Th2 response, and this may be a novel pathway for liver fibrogenesis.

  19. Establishment of the block against sperm penetration in parthenogenetically activated bovine oocytes matured in vitro.

    PubMed

    Soloy, E; Srsen, V; Pavlok, A; Hyttel, P; Thomsen, P D; Smith, S D; Procházka, R; Kubelka, M; Hřier, R; Booth, P; Motlík, J; Greve, T

    1997-09-01

    The ability of a single electric pulse to mimic a block against sperm penetration in bovine oocytes matured in vitro was investigated. Confocal laser scanning microscopy detected a global loss of spots, presumed to be cortical granules, stained with Lens culinaris agglutinin, in pulsed oocytes. Transmission electron microscopy revealed that cortical granule exocytosis occurred within 1 min of stimulation and the number of remaining cortical granules was significantly reduced in all pulsed oocytes. The ability of pulsed oocytes to undergo fertilization in vitro was also affected, as only 31% of the pulsed oocytes were penetrated compared with 87% in the control group. Since incidences of penetration in pulsed oocytes (31%), and of polyspermy in control oocytes (18%) did not differ and were highly correlated (P = 0.009) among trials (n = 15), the induced block is considered to be comparable with the natural block triggered by a spermatozoon. The increased resistance of the zona pellucida to pronase E observed in pulsed oocytes suggests that the induced block depends, at least partly, on modifications of zona pellucida glycoproteins. Finally, the majority (66%) of pulsed, penetrated oocytes did not form male pronuclei, probably as a consequence of asynchrony between the formation of female pronucleus and sperm penetration. The reduced ability of the cytoplasm to induce the formation of a male pronucleus was accompanied by a fall in histone H1 kinase activity to basal values by 3 h after stimulation. These results demonstrate that a single electric pulse can induce a block against sperm penetration similar to that of the spermatozoon itself. PMID:9370979

  20. In vitro studies on the lymphoma growth-inhibitory activity of sulfasalazine.

    PubMed

    Gout, Peter W; Simms, Chris R; Robertson, May C

    2003-01-01

    Sulfasalazine (SASP) is a novel, potent inhibitor of cellular cystine uptake mediated by the x(c)- cystine/glutamate antiporter. Lymphoid cells cannot synthesize cyst(e)ine and depend for growth on its uptake from their micro-environment. We previously showed that SASP (0.2 mM) can abrogate lymphoma cell proliferation in vitro by specifically inhibiting x(c)- -mediated cystine uptake. Intraperitoneal administration of SASP to Noble rats markedly suppressed Nb2-U17 rat lymphoma transplant growth, notably without major toxicity to the hosts. Since Nb2-U17 cells are x(c)- -deficient, the growth arrest was apparently not due to SASP-tumor cell interaction, but possibly to interference with x(c)- -mediated cysteine secretion by somatic cells. In this study we found that replication of x(c)- -deficient Nb2-11 lymphoma cells can be sustained in vitro, in the absence of cystine uptake enhancers, by co-culturing with IMR-90 fibroblasts known to secrete cysteine. SASP, at 0.15 and 0.2 mM, arrested replication of fibroblast-driven Nb2-11 cells by 93 and 100%, respectively, without impeding fibroblast proliferation. Addition of 2-mercapto-ethanol (60 microM), a cystine uptake enhancer, almost completely prevented this growth arrest, indicating that SASP specifically inhibited cysteine secretion by the fibroblasts, a process based on x(c)- -mediated cystine uptake. It is proposed that the lymphoma growth-inhibitory activity of SASP in vivo involves inhibition of cysteine secretion by tumor-associated somatic cells (macrophages, dendritic cells), leading to cysteine starvation of the tumor cells and apoptosis. The difference between the lymphoma cells and fibroblasts in sensitivity to SASP treatment is consistent with the marked antitumor effect of SASP lacking significant side effects. PMID:12544255