Department of Chemistry and Center of Excellence for Innovation in Chemistry, Faculty of Science, Chiang Mai University, Chiang Mai, 50200, Thailand.
Phytother Res. 2010 Jul;24(7):1009-13. doi: 10.1002/ptr.3057.
Seven labdane-type diterpenes, coronarin E, coronarin A, yunnancoronarin A, yunnancoronarin B, hedyforrestin B, villosin, and hedyforrestin C were isolated from the rhizome of Hedychium gardnerianum and evaluated for cytotoxic activity against human small cell lung cancer (NCI-H187) and non-cancerous Vero cells. The results showed that villosin exhibited potent cytotoxic activity with IC(50) of 0.40 microM, which was higher than that of the drug ellipticine (IC(50) 1.79 microM). Moreover, ellipticine was very toxic to Vero cells (IC(50) 7.47 microM) whereas the toxicity of villosin was undetectable at concentration lower than 166.42 microM. The results have indicated that the lactone ring is essential for high cytotoxic activity and that the presence of a hydroxyl group at the 6 or 7 position causes decrease in activity. The very high cytotoxicity against the NCI-H187 cells and the exceptionally high selectivity index (>416) of villosin suggested that this compound may be used as a potential lead molecule for antitumor therapeutic development.
从姜黄属植物的根茎中分离得到了 7 种喇叭烷二萜，分别为 Coronarin E、Coronarin A、Yunnancoronarin A、Yunnancoronarin B、Hedyforrestin B、Villosin 和 Hedyforrestin C，并对其进行了抗人类小细胞肺癌（NCI-H187）和非癌细胞 Vero 的细胞毒性活性评价。结果表明，Villosin 表现出较强的细胞毒性活性，IC50 为 0.40 μM，高于药物椭圆体（IC50 为 1.79 μM）。此外，椭圆体对 Vero 细胞的毒性非常大（IC50 为 7.47 μM），而 Villosin 的毒性在低于 166.42 μM 的浓度下无法检测到。结果表明，内酯环对于高细胞毒性活性是必需的，而在 6 或 7 位存在羟基会导致活性降低。Villosin 对 NCI-H187 细胞的高细胞毒性和极高的选择指数（>416）表明，该化合物可能被用作抗肿瘤治疗开发的潜在先导分子。
