In Vitro Anti-HIV Activity of Biflavonoids Isolated from Rhus succedanea and Garcinia multiflora

• Published in: Journal of natural products (Washington, D.C.) D.C.), 1997-09, Vol.60 (9), p.884-888
• Main Authors: Lin, Yuh-Meei, Anderson, Herbert, Flavin, Michael T, Pai, Yeah-Huei S, Mata-Greenwood, Eugenia, Pengsuparp, Thitima, Pezzuto, John M, Schinazi, Raymond F, Hughes, Stephen H, Chen, Fa-Ching
• Format: Article
• Language: English
• Subjects: AGATHISFLAVONE; AMENTOFLAVONE; Anti-HIV Agents - isolation & purification; Anti-HIV Agents - pharmacology; ANTIVIRAL; ANTIVIRAL AGENTS; Biological and medical sciences; BRANCHE; BRANCHES; Cell Survival - drug effects; Cells, Cultured; CHEMICAL COMPOSITION; CHEMICAL STRUCTURE; COMPOSICION QUIMICA; COMPOSITION CHIMIQUE; DRUG PLANTS; ESPECTROMETRIA; ESTRUCTURA QUIMICA; FEUILLE; FLAVONOIDE; FLAVONOIDES; FLAVONOIDS; Flavonoids - isolation & purification; Flavonoids - pharmacology; GARCINIA; GB-1A 7"-O-BETA-GLUCOSIDE; GB-1A HEXAMETHYL ETHER; GB-2A; General pharmacology; GENERO HUMANO; GENRE HUMAIN; GN-1A; HERPETOVIRIDAE; HINOKIFLAVONE; HIV Reverse Transcriptase - antagonists & inhibitors; HIV-1 - drug effects; HOJAS; HUMAN IMMUNODEFICIENCY VIRUS; Humans; LEAVES; Lymphocytes - drug effects; Lymphocytes - metabolism; MANKIND; Medical sciences; MORELLOFLAVONE; MORELLOFLAVONE HEPTAMETHYL ETHER; Pharmacognosy. Homeopathy. Health food; Pharmacology. Drug treatments; PLANTAS MEDICINALES; PLANTE MEDICINALE; Plants, Medicinal - chemistry; Plants, Toxic; RAMAS; Reverse Transcriptase Inhibitors - pharmacology; RHUS; RHUSFLAVANONE; ROBUSTAFLAVONE; SPECTRAL ANALYSIS; SPECTROMETRIE; SPECTROMETRY; STRUCTURE CHIMIQUE; SUCCEDANEAFLAVANONE; TAIWAN; Toxicodendron - chemistry; VIRICIDAS; Virus Replication - drug effects; VOLKENSIFLAVONE; VOLKENSIFLAVONE HEXAMETHYL ETHER
• ISSN: 0163-3864; 1520-6025
• DOI: 10.1021/np9700275

Eleven biflavonoids, including amentoflavone (1), agathisflavone (2), robustaflavone (3), hinokiflavone (4), volkensiflavone (5), morelloflavone (7), rhusflavanone (9), succedaneaflavanone (10), GB-1a (11), GB-1a 7‘‘-O-β-glucoside (13), and GB-2a (14) isolated from Rhus succedanea and Garcinia multiflora, as well as their methyl ethers, volkensiflavone hexamethyl ether (6), morelloflavone heptamethyl ether (8), and GB-1a hexamethyl ether (12), were evaluated for their anti-HIV-1 RT activity. The results indicated that compounds 3 and 4 demonstrated similar activity against HIV-1 reverse transcriptase (RT), with IC50 values of 65 μM. Compounds 1, 2, 7, 11, and 14 were moderately active against HIV-1 RT, with IC50 values of 119 μM, 100 μM, 116 μM, 236 μM, and 170 μM, respectively. Morelloflavone (7) also demonstrated significant antiviral activity against HIV-1 (strain LAV-1) in phytohemagglutinin-stimulated primary human peripheral blood mononuclear cells at an EC50 value of 6.9 μM and a selectivity index value of approximately 10. The other biflavonoids were either weakly active, inactive, or not selective against HIV-1 in human lymphocytes.