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

Robin Pettit, Gary D. Cage, George Pettit, Jessica A. Liebman

Research output: Contribution to journalArticlepeer-review

23 Scopus citations

Abstract

The in vitro activity of the steroidal amide 3β-acetoxy-17β-(L- prolyl)amino-5α-androstane against 179 Gram-positive clinical isolates was examined. The minimum bactericidal concentration (MBC)/MIC ratios were ≤ 2 for 73% of methicillin-resistant Staphylococcus 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 3β-acetoxy-17β-(L-prolyl)amino- 5α-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. (C) 2000 Elsevier Science B.V. and International Society of Chemotherapy.

Original languageEnglish (US)
Pages (from-to)299-304
Number of pages6
JournalInternational Journal of Antimicrobial Agents
Volume15
Issue number4
DOIs
StatePublished - Aug 1 2000

Keywords

  • Antibacterial susceptibility
  • Steroidal amide

ASJC Scopus subject areas

  • Microbiology (medical)
  • Infectious Diseases
  • Pharmacology (medical)

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