title: In vitro anti-HIV-1 virucidal activity of tyrosine-conjugated tri- and dihydroxy bile salt derivatives.
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 7alpha,12alpha dihydroxy bile salt derivatives have the most potent antiviral activity. Complexing of iodine to the bile salt derivative (as in DICGT) decreases virucidal potency.
authors.affiliation: Department of Medical Microbiology and Retroscreen Virology, St Bartholomew's and The Royal London School of Medicine and Dentistry, 64 Turner Street, London, UK. aaljabri@squ.edu.om
authors.forename: A A
authors.initials: AA
authors.lastname: Al-Jabri
authors.forename: M D
authors.initials: MD
authors.lastname: Wigg
authors.forename: E
authors.initials: E
authors.lastname: Elias
authors.forename: R
authors.initials: R
authors.lastname: Lambkin
authors.forename: C O
authors.initials: CO
authors.lastname: Mills
authors.forename: J S
authors.initials: JS
authors.lastname: Oxford
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002793:Cholic Acids / Q000737:chemistry* / Q000494:pharmacology*; D003840:Deoxycholic Acid / Q000031:analogs & derivatives / Q000494:pharmacology; D003902:Detergents / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D017137:Nonoxynol / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013501:Surface-Active Agents / Q000494:pharmacology; D014443:Tyrosine / Q000737:chemistry*
chemical_list: D019380:Anti-HIV Agents; D002793:Cholic Acids; D003902:Detergents; D013501:Surface-Active Agents; D003840:Deoxycholic Acid; D017137:Nonoxynol; D014443:Tyrosine