In vitro anti-HIV-1 virucidal activity of tyrosine-conjugated tri- and dihydroxy bile salt derivatives

A. A. Al-Jabri, M. D. Wigg, E. Elias, R. Lambkin, C. O. Mills, J. S. Oxford

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

The cellular toxicity and anti-human immunodeficiency virus type 1 (HIV-1) virucidal activity of four synthesized tyrosine-conjugated bile salt derivatives with high surfactant activities, namely di-iodo-deoxycholyltyrosine (DIDCT), di-iodo-chenodeoxycholyltyrosine (DICDCT), di-iodo-cholylglycyltyrosine (DICGT) and deoxycholyltyrosine (DCT), were evaluated and compared with either sodium deoxycholate or nonoxynol-9. DIDCT, DICDCT and DCT but not DICGT showed virucidal activity against three different laboratory-adapted strains of HIV-1 (RF, IIIB and MN). All the bile salt derivatives tested excluding DICGT were virucidal at a concentration as low as 10 ng/mL. DCT had the highest anti-HIV-1 virucidal potency, suggesting that monopeptide 7α,12α dihydroxy bile salt derivatives have the most potent antiviral activity. Complexing of iodine to the bile salt derivative (as in DICGT) decreases virucidal potency.

Original languageEnglish
Pages (from-to)617-621
Number of pages5
JournalJournal of Antimicrobial Chemotherapy
Volume45
Issue number5
Publication statusPublished - 2000

ASJC Scopus subject areas

  • Microbiology
  • Pharmacology

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