SYNTHESIS AND ANTI-HIV-1 ACTIVITY OF OLEAN-9(11),12(13)-DIEN-30-OIC ACID 3Β-(2-O-Β-D-GLUCURONOPYRANOSYL-Β-D-GLUCURONOPYRANOSIDE)

Publication date: 2014

Abstract:

The glycyrrhizic acid (GA) analog olean-9(11),12(13)-dien-30-oic acid 3β-(2-O-β-D-glucuronopyranosyl-β-D-glucuronopyranoside) (II) was synthesized via reduction of GA by NaBH4 in refluxing 2-PrOH:H2O with subsequent work up with HCl (5%). The cytotoxicity and antiviral activity of this glycoside against HIV-1 was studied in MT-4 cell culture. It was found that II was practically non-toxic for MT-4 cells while inhibiting accumulation of virus-specific protein p24 and RNA-dependent DNA-polymerase activity of HIV-1 reverse transcriptase (RT) (IC50 3.1 ±1.0 μg/mL).

Тип: Article

DOI 10.1007/s11094-014-1127-2