title: [Effective components against HIV-1 replicative enzymes isolated from plants].
abstract: Plant active components characterized of many different structures and activities on multiple targets, have made them to be the important sources of inhibitors on HIV-1. For finding leading compounds with new structure against HIV-1, three key HIV-1 replicative enzymes (reverse transcriptase, protease and integrase) were used as screening models. The in vitro activities of 45 plant derived components isolated from Schisandraceae, Rutaceae and Ranunculaceae were reported. Within twelve triterpene components isolated, eight compounds were found to inhibit HIV-1 protease, in these eight active compounds, kadsuranic acid A (7) and nigranoic acid (8), inhibited both HIV-1 protease and integrase; Among fifteen lignans, meso-dihydroguaiaretic acid (15) and kadsurarin (16) were active on HIV-1 reverse transcriptase, and 4, 4-di(4-hydroxy-3-methoxyphenly)-2, 3-dimethylbutanol (13) active on HIV-1 integrase. All of the six alkaloids, seven flavones, and five others compounds were not active or only with low activities against HIV-1 replicative enzymes. Further studies of the triterpene components showing strong inhibitory activities on HIV-1 were warranted.
authors.affiliation: Institute of Medicinal and Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
authors.forename: Zong-gen
authors.initials: ZG
authors.lastname: Peng
authors.forename: Li-jia
authors.initials: LJ
authors.lastname: Xu
authors.forename: Wen-cai
authors.initials: WC
authors.lastname: Ye
authors.forename: Pei-gen
authors.initials: PG
authors.lastname: Xiao
authors.forename: Hong-shan
authors.initials: HS
authors.lastname: Chen
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D019380:Anti-HIV Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D047309:Flavones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D006139:Guaiacol / Q000031:analogs & derivatives / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D019427:HIV Integrase / Q000187:drug effects*; D016333:HIV Protease / Q000187:drug effects*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors*; D017705:Lignans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D010946:Plants, Medicinal / Q000737:chemistry; D029626:Ranunculaceae / Q000737:chemistry; D027821:Rutaceae / Q000737:chemistry; D029633:Schisandraceae / Q000737:chemistry; D014315:Triterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology
chemical_list: D000470:Alkaloids; D019380:Anti-HIV Agents; D004365:Drugs, Chinese Herbal; D047309:Flavones; D017705:Lignans; D014315:Triterpenes; C100860:nigranoic acid; C015816:dihydroguaiaretic acid; D006139:Guaiacol; D019427:HIV Integrase; D054303:HIV Reverse Transcriptase; D016333:HIV Protease