title: In vitro anti-HIV activity of biflavonoids isolated from Rhus succedanea and Garcinia multiflora.
abstract: 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-beta-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 microM. Compounds 1, 2, 7, 11, and 14 were moderately active against HIV-1 RT, with IC50 values of 119 microM, 100 microM, 116 microM, 236 microM, and 170 microM, 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 microM 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.
authors.affiliation: MediChem Research, Inc., Lemont, Illinois 60439, USA.
authors.forename: Y M
authors.initials: YM
authors.lastname: Lin
authors.forename: H
authors.initials: H
authors.lastname: Anderson
authors.forename: M T
authors.initials: MT
authors.lastname: Flavin
authors.forename: Y H
authors.initials: YH
authors.lastname: Pai
authors.forename: E
authors.initials: E
authors.lastname: Mata-Greenwood
authors.forename: T
authors.initials: T
authors.lastname: Pengsuparp
authors.forename: J M
authors.initials: JM
authors.lastname: Pezzuto
authors.forename: R F
authors.initials: RF
authors.lastname: Schinazi
authors.forename: S H
authors.initials: SH
authors.lastname: Hughes
authors.forename: F C
authors.initials: FC
authors.lastname: Chen
mesh_terms: D019380:Anti-HIV Agents / Q000302:isolation & purification / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008214:Lymphocytes / Q000187:drug effects / Q000378:metabolism; D010946:Plants, Medicinal / Q000737:chemistry*; D010947:Plants, Toxic; D018894:Reverse Transcriptase Inhibitors / Q000494:pharmacology; D012251:Toxicodendron / Q000737:chemistry*; D014779:Virus Replication / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D005419:Flavonoids; D018894:Reverse Transcriptase Inhibitors; D054303:HIV Reverse Transcriptase