当前位置： SCI文献检索 > INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS期刊下所有文献 > Antimicrobial and cancer cell growth inhibitory activities of 3beta-acetoxy-17beta-(L-prolyl)amino-5alpha-androstane in vitro.

Antimicrobial and cancer cell growth inhibitory activities of 3beta-acetoxy-17beta-(L-prolyl)amino-5alpha-androstane in vitro.

Abstract：

:The in vitro activity of the steroidal amide 3beta-acetoxy-17beta-(L-prolyl)amino-5alpha-androstane against 179 gram-positive clinical isolates was examined. The minimum bactericidal concentration (MBC)/MIC ratios were < or = 2 for 73% of methicillin-resistant Staphyllococcus aureus, 59% of vancomycin-resistant Enterococcus spp. and 88% of penicillin-resistant Streptococcus pneumoniae. The androstane derivative was bactericidal for a variety of other gram-positive genera, including Nocardia, Corynebacterium and Listeria. Variation in MICs is pH 6-8 media was slight. The frequency of occurrence of bacterial spontaneous mutations to resistance ranged from 10(-6) to 10(-9). Kill curve analysis confirmed the bactericidal nature of the steroidal amide, and demonstrated that killing was time dependent but not concentration dependent for all organisms. The ability of 3beta-acetoxy-17beta-(L-prolyl)amino-5alpha-androstane to inhibit human cancer cell growth was also evaluated. The concentration required to inhibit 50% of cell growth (GI50) was < 2.5 mg/l for all cell lines examined. In single-dose murine toxicity evaluations, the androstane derivative was non-toxic at doses up to 400 mg/kg.

journal_name

Int J Antimicrob Agents

journal_title

International journal of antimicrobial agents

authors

Pettit RK,Cage GD,Pettit GR,Liebman JA

doi

10.1016/s0924-8579(00)00156-4

subject

Has Abstract

pub_date

2000-08-01 00:00:00

pages

299-304

issue

4

eissn

0924-8579

issn

1872-7913

pii

S0924857900001564

journal_volume

15

pub_type

杂志文章

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