Means is a 3-O-beta-D-GLYUKURONOPIRANOZIL-beta-D-GLYUKURONOPIRANOZID OLEA-9 (11) 12 (13) -diene-30-oic acid, exhibit anti-HIV-1 activity and a process for its preparation

摘要

FIELD: medicine, pharmaceutics.;SUBSTANCE: presented agent - glycoside (1) is a practically non-toxic substance for cells, 12 times less toxic for MT-4 cells than a comparator drug GC (purity 97%) and ensures high-effective inhibition of RNA-dependent DNA-polymerase activity of HIV-1 reverse transcriptase (RT). Also, the present invention provides a method for preparing 3-O-β-D-glucopyranosyl-β-D-glucopyranoside olean-9(11), 12(13)-diene-30-acid (1) which consists in GC recovery by 4.5-5.5-fold sodium boron hydride excess in a mixture of isopropanol-water (1:1), boiling for 1-2 h; it is followed by processing of a reaction mixture with 5% hydrogen chloride (pH 1-2) at 20-22°C and extraction in butanol to produce mixed glycosides (1) and (4) in the relation of 2:1 to be processed by highly acidic cation exchange resins (CU2-8, Dowex 50, amberlite resin IR-120) in the H⁺- form in 70-75% ethanol and column chromatographic separation on silicagel to prepare the target product.;EFFECT: what is declared is the agent representing 3-O-β-D-glucopyranosyl-β-D-glucopyranoside olean-9(11), 12(13)-diene-30-acid of formula (1) - an analogue of glycyrrhizic acid showing anti-HIV-1 virus activity, inhibiting collection of virus-specific protein p24, and exceeds glycyrrhizic acid by selectivity index (SI) in 4,8 times.;2 cl, 3 ex, 1 tbl