title: HIV-1 integrase inhibitory substances from Coleus parvifolius.
abstract: For the purpose of discovering anti-HIV-1 agents from natural sources, water and EtOH extracts of 50 Thai plants were screened for their inhibitory activity against HIV-1 integrase (IN), an enzyme essential for viral replication. Of these plants, an EtOH extract of Coleus parvifolius Benth. (aerial parts) showed potent activity against HIV-1 IN with an IC50 value of 9.2 microg/mL. From this extract, 11 compounds were isolated and identified as luteolin 5-O-beta-d-glucopyranoside (1), luteolin (2), luteolin 7-methyl ether (3), luteolin 5-O-beta-d-glucuronide (4), 5-O-beta-d-glucopyranosyl-luteolin 7-methyl ether (5), rosmarinic acid (6), rosmarinic acid methyl ester (7), daucosterol (8), a mixture of alpha- and beta-amyrin (9, 10) and phytol (11). Of these compounds, rosmarinic acid methyl ester (7), rosmarinic acid (6), luteolin (2) and luteolin 7-methyl ether (3) exhibited inhibitory activities against HIV-1 IN with IC50 values of 3.1, 5.0, 11.0 and 11.0 microM, respectively. Among rosmarinic acid derivatives, the HIV-1 IN inhibitory activity increased in turn for a dimer (IC50 = 5.0 microM), a trimer (IC50 = 1.4 microM), and a tetramer (IC50 = 1.0 microM).
authors.affiliation: Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, Toyama, Japan.
authors.forename: Supinya
authors.initials: S
authors.lastname: Tewtrakul
authors.forename: Hirotsugu
authors.initials: H
authors.lastname: Miyashiro
authors.forename: Norio
authors.initials: N
authors.lastname: Nakamura
authors.forename: Masao
authors.initials: M
authors.lastname: Hattori
authors.forename: Takuya
authors.initials: T
authors.lastname: Kawahata
authors.forename: Toru
authors.initials: T
authors.lastname: Otake
authors.forename: Tomokazu
authors.initials: T
authors.lastname: Yoshinaga
authors.forename: Tamio
authors.initials: T
authors.lastname: Fujiwara
authors.forename: Tanomjit
authors.initials: T
authors.lastname: Supavita
authors.forename: Supreeya
authors.initials: S
authors.lastname: Yuenyongsawad
authors.forename: Pranee
authors.initials: P
authors.lastname: Rattanasuwon
authors.forename: Sukanya
authors.initials: S
authors.lastname: Dej-Adisai
mesh_terms: D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D031330:Coleus; D035264:Flowers; D005638:Fruit; D019427:HIV Integrase / Q000187:drug effects*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D008519:Medicine, Traditional; D008826:Microbial Sensitivity Tests; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D018515:Plant Leaves; D018517:Plant Roots; D012639:Seeds; D013785:Thailand; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D010936:Plant Extracts; D019427:HIV Integrase