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Journal of Antimicrobial Chemotherapy (2000) 45, 617-621
© 2000 The British Society for Antimicrobial Chemotherapy

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

A. A. Al-Jabria,*, M. D. Wiggb, E. Eliasc, R. Lambkina, C. O. Millsc and J. S. Oxforda

a Department of Medical Microbiology and Retroscreen Virology, St Bartholomew's and The Royal London School of Medicine and Dentistry, 64 Turner Street, London, UK; b Departmento de Virologia, Universidade Federal do Rio de Janeiro, 21 941-590 Rio de Janeiro, Brasil; c The Queen Elizabeth Hospital, Department of Medicine, Liver Research Laboratories, Edgbaston, Birmingham, UK

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 7{alpha},12{alpha} dihydroxy bile salt derivatives have the most potent antiviral activity. Complexing of iodine to the bile salt derivative (as in DICGT) decreases virucidal potency.

* Correspondence address. Department of Microbiology and Immunology, College of Medicine, SQU, Muscat, Sultanate of Oman. Tel: +968-515186; Fax: +968-513419; E-mail: aaljabri{at}squ.edu.om


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