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

The cellular toxicity and anti-human immunodeficiency virus type 1 (HIV-1) virucidal activity of four synthesized tyrosine-conjugated bile salt deriva tives with high surfactant activities, namely di-iodo-deoxycholyltyrosine ( DIDCT), di-iodo-chenodeoxycholyltyrosine (DICDCT), di-iodo-cholylglycyltyro sine (DICGT) and deoxycholyltyrosine (DCT), were evaluated and compared wit h 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 ex cluding DICGT were virucidal at a concentration as low as 10 ng/mL. DCT had the highest anti-HIV-1 virucidal potency, suggesting that mono-peptide 7 a lpha,12 alpha dihydroxy bile salt derivatives have the most potent antivira l activity. Complexing of iodine to the bile salt derivative las in DICGT) decreases virucidal potency.