Department of Chemistry and Center for Innovation in Chemistry (PERCH-CIC), Faculty of Science, Mahidol University, Bangkok, Thailand.
Fitoterapia. 2012 Mar;83(2):368-72. doi: 10.1016/j.fitote.2011.11.015. Epub 2011 Dec 3.
Four new flavones, 5,2'-dihydroxy-7,3',4',5'-tetramethoxyflavone (1), 5,2',5'-trihydroxy-7,3',4'-trimethoxyflavone (2), 5,7,2',5'-tetrahydroxy-6,3',4'-trimethoxyflavone (3) and 5,2',5'-trihydroxy-6,7,3',4'-tetramethoxyflavone (4), along with the known 5,3'-dihydroxy-6,7,4',5'-tetramethoxyflavone (5), 5,7,3',5'-tetrahydroxy-6,4'-dimethoxyflavone (6), syringaldehyde, vanillic acid and scopoletin were isolated from the leaves and twigs of Gardenia carinata (Rubiaceae). Their structures were determined by spectroscopic methods. Flavone 2 exhibited cytotoxic activity against P-388 and MCF-7 cell lines, while 3, 5 and 6 were active only in P-388 cell line. All active compounds were found to inhibit DNA topoisomerase IIα activity, which may be responsible for the observed cytotoxicity. Flavones 1-3, 5 and 6 also exhibited anti-HIV-1 activity in the anti-syncytium assay using (∆Tat/rev)MC99 virus and 1A2 cell line system; 2 was most potent. Only flavones 1 and 6 showed considerably activity against HIV-1 reverse transcriptase.
从山栀（Rubiaceae）的叶和小枝中分离得到了四个新的类黄酮化合物：5,2'-二羟基-7,3',4',5'-四甲氧基黄酮（1）、5,2',5'-三羟基-7,3',4'-三甲氧基黄酮（2）、5,7,2',5'-四羟基-6,3',4'-三甲氧基黄酮（3）和 5,2',5'-三羟基-6,7,3',4'-四甲氧基黄酮（4），以及已知的 5,3'-二羟基-6,7,4',5'-四甲氧基黄酮（5）、5,7,3',5'-四羟基-6,4'-二甲氧基黄酮（6）、丁香醛、香草酸和伞形花内酯。通过光谱方法确定了它们的结构。黄酮 2 对 P-388 和 MCF-7 细胞系表现出细胞毒性活性，而 3、5 和 6 仅在 P-388 细胞系中表现出活性。所有具有活性的化合物均被发现抑制 DNA 拓扑异构酶 IIα 的活性，这可能是观察到的细胞毒性的原因。黄酮 1-3、5 和 6 在用（∆Tat/rev）MC99 病毒和 1A2 细胞系系统进行的抗合胞体测定中也表现出抗 HIV-1 活性；2 最为有效。只有黄酮 1 和 6 对 HIV-1 逆转录酶表现出相当的活性。
