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Selective Activity (selective + activity)
Selected AbstractsSafety and efficacy of oral entecavir given for 28 days in patients with chronic hepatitis B virus infectionHEPATOLOGY, Issue 3 2001Ph.D., Robert A. de Man M.D. Entecavir is an oral antiviral drug with selective activity against hepatitis B virus (HBV). We conducted a randomized, placebo-controlled, dose-escalating study in patients with chronic hepatitis B infection in which we evaluated the efficacy and safety of entecavir given for 28 days. Follow-up was 24 weeks. All doses of entecavir (0.05 mg, 0.1 mg, 0.5 mg, and 1.0 mg) showed a pronounced suppression of replication of the HBV with a 2.21, 2.29, 2.81, and 2.55 mean log10 reduction of viral load, respectively. Approximately 25% of patients on entecavir showed a decline of HBV DNA below the limit of detection of the Chiron HBV-DNA assay (<0.7 MEq/mL). In the postdosing follow-up period patients who were treated with 0.5 and 1.0 mg of entecavir showed a considerably slower return in their HBV DNA levels to baseline compared with those patients treated with lower dosages (P < .05). All doses of entecavir were well tolerated with no significant difference between treated patients and those receiving placebo. No significant changes in alanine transaminase (ALT) levels within the dose groups and the placebo group between baseline and the end of treatment were observed. Three patients (9%) (1 each in the 0.05-, 0.1-, and 0.5-mg groups) experienced asymptomatic hepatitis flares 16 weeks (2 patients) and 24 weeks (1 patient) after withdrawal of entecavir. In conclusion, in this 28-day study of entecavir a pronounced decrease of HBV DNA was observed and there were no significant side effects in entecavir patients in comparison with placebo-treated patients. (HEPATOLOGY 2001;34:578-582.) [source] The 4-acetylantroquinonol B isolated from mycelium of Antrodia cinnamomea inhibits proliferation of hepatoma cellsJOURNAL OF THE SCIENCE OF FOOD AND AGRICULTURE, Issue 10 2010Yu-Wei Lin Abstract BACKGROUND:Antrodia cinnamomea is known for its antihepatoma activity, yet the identity of its active compound was unclear. In this study, a 5-ton fermenter was used to prepare sufficient mycelium of A. cinnamomea for active compound isolation and identification. RESULTS: Using antiproliferative activity toward HepG2 cells as guidance in the isolation process, 4-acetylantroquinonol B was purified and identified to be the major bioactive compound of A. cinnamomea cultivated by submerged fermentation. The median effective doses (EC50) of 4-acetylantroquinonol B for HepG2 cells were 0.10 ± 0.00 and 0.08 ± 0.00 µg mL,1 for 72 and 96 h treatments, respectively. The selective indices of 4-acetylantroquinonol B were 100 and 125 for 72 and 96 h treatments, respectively, indicating that this compound had high selective activity for hepatoma cells. CONCLUSION: 4-Acetylantroquinonol B is the major antihepatoma constituent of Antrodia cinnamomea mycelium produced by submerged fermentation. Copyright © 2010 Society of Chemical Industry [source] Plants as a source of anti-cancer and anti-HIV agentsANNALS OF APPLIED BIOLOGY, Issue 2 2003G M CRAGG Summary Plant-derived compounds have played an important role in the development of several clinically useful anti-cancer agents. These include vinblastine, vincristine, the camptothecin derivatives, topotecan and irinotecan, etoposide, and paclitaxel (Taxol®). Several promising new agents are in clinical development based on selective activity against cancer-related molecular targets, including flavopiridol and Combretastatin A4 phosphate. Recently, plants have yielded several agents showing anti-AIDS activity, and one of these, (+)-calanolide A, is in clinical development. [source] Fungicide Activity of 5-(4-Chlorobenzylidene)-(Z)-2-dimethylamino-1,3-thiazol-4-one against Cryptococcus NeoformansARCHIV DER PHARMAZIE, Issue 1 2010Braulio Insuasty Abstract The present work describes the synthesis and antifungal evaluation of new 5-arylidene-(Z)-2-dimethylamino-1,3-thiazol-4-ones 4a,f, obtained by the reaction of aromatic aldehydes 1 and rhodanine 2 followed by treatment with DMF. All compounds were tested against a panel of yeasts, hialohyphomycetes, and dermatophytes using the microbroth dilution method. Compounds 4a and 4c showed antifungal activity, with compound 4a being the most active one. Compound 4a demonstrated to be fungicidal rather than fungistatic and selective activity against Cryptococcus neoformans and dermatophytes. MIC100, MIC80, and MIC50 of 4a were determined against a panel of clinical isolates of C. neoformans showing ranges of MICs between 2 and 16 ,g/mL. [source] | ||||||||||