TY - JOUR
T1 - In vitro anti-HIV-1 virucidal activity of tyrosine-conjugated tri- and dihydroxy bile salt derivatives
AU - Al-Jabri, A. A.
AU - Wigg, M. D.
AU - Elias, E.
AU - Lambkin, R.
AU - Mills, C. O.
AU - Oxford, J. S.
PY - 2000
Y1 - 2000
N2 - 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.
AB - 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.
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U2 - 10.1093/jac/45.5.617
DO - 10.1093/jac/45.5.617
M3 - Article
C2 - 10797083
AN - SCOPUS:0034099949
SN - 0305-7453
VL - 45
SP - 617
EP - 621
JO - Journal of Antimicrobial Chemotherapy
JF - Journal of Antimicrobial Chemotherapy
IS - 5
ER -
