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来自泰国栀子叶和嫩枝的抗HIV-1环阿尔廷烷类化合物。

Anti-HIV-1 cycloartanes from leaves and twigs of Gardenia thailandica.

作者信息

Tuchinda Patoomratana, Saiai Aroonchai, Pohmakotr Manat, Yoosook Chalobon, Kasisit Jittra, Napaswat Chanita, Santisuk Thawatchai, Reutrakul Vichai

机构信息

Department of Chemistry, Faculty of Science, Mahidol University, Bangkok, Thailand.

出版信息

Planta Med. 2004 Apr;70(4):366-70. doi: 10.1055/s-2004-818951.

DOI:10.1055/s-2004-818951
PMID:15095155
Abstract

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.

摘要

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。

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