Tuchinda Patoomratana, Saiai Aroonchai, Pohmakotr Manat, Yoosook Chalobon, Kasisit Jittra, Napaswat Chanita, Santisuk Thawatchai, Reutrakul Vichai
Department of Chemistry, Faculty of Science, Mahidol University, Bangkok, Thailand.
Planta Med. 2004 Apr;70(4):366-70. doi: 10.1055/s-2004-818951.
Thailandiol ( 1), gardenolic acid A ( 2), quadrangularic acid E ( 3) and 3beta-hydroxy-5alpha-cycloart-24(31)-en-28-oic acid ( 4) have been isolated from the leaves and twigs of Gardenia thailandica Tirveng (order: Rubiales; family: Rubiaceae). In addition, 5-hydroxy-7,2',3',4',5',6'-hexamethoxyflavone ( 5), 5,7-dihydroxy-2',3', 4',5',6'-pentamethoxyflavone ( 6), 5-hydroxy-7,2',3',4',5'-pentamethoxyflavone ( 7) and 5,7-dihydroxy-2',3',4',5'-tetramethoxyflavone ( 8) were also isolated from the same source. The structures were elucidated by spectroscopic methods. Crude extracts and compounds 1 - 4 displayed anti-HIV-1 activities as determined by using the (Delta)(Tat/Rev)MC99 virus and 1A2 cell line system. The EC (50) values determined by the syncytium assay ranged from < 7.8 to 110 microg/mL. They also exhibited moderate to high activities in reverse transcriptase (RT) assay; the IC (50) values of compounds 1 - 4, ranged from < 22.5 to 156.8 microg/mL.
从泰国栀子(茜草目;茜草科)的叶和嫩枝中分离出了泰国栀子醇(1)、栀子酸A(2)、四方酸E(3)和3β-羟基-5α-环阿尔廷-24(31)-烯-28-酸(4)。此外,还从同一来源分离出了5-羟基-7,2',3',4',5',6'-六甲氧基黄酮(5)、5,7-二羟基-2',3',4',5',6'-五甲氧基黄酮(6)、5-羟基-7,2',3',4',5'-五甲氧基黄酮(7)和5,7-二羟基-2',3',4',5'-四甲氧基黄酮(8)。通过光谱方法阐明了这些化合物的结构。使用(Delta)(Tat/Rev)MC99病毒和1A2细胞系系统测定,粗提物和化合物1 - 4显示出抗HIV-1活性。通过合胞体测定法确定的EC(50)值范围为< 7.8至110微克/毫升。它们在逆转录酶(RT)测定中也表现出中度至高活性;化合物1 - 4的IC(50)值范围为< 22.5至156.8微克/毫升。