从 Brachyglottis monroi 中分离得到的 13(E)-labd-13-ene-8alpha,15-diol 的抗病毒和抗癌活性。

Antiviral and anticancer activities of 13(E)-labd-13-ene-8alpha,15-diol isolated from Brachyglottis monroi.

机构信息

Natural Medicines Research Centre, Korea Research Institute of Bioscience and Biotechnology, Daejeon, Republic of Korea.

出版信息

Phytother Res. 2010 Feb;24(2):169-74. doi: 10.1002/ptr.2875.

DOI:10.1002/ptr.2875

PMID:19504469

Abstract

The antiviral activity of 13(E)-labd-13-ene-8alpha,15-diol (1), isolated from Brachyglottis monroi, was examined against human rhinovirus 2 (HRV2) and 3 (HRV3), and the anticancer activity on human cancer cells (A549 and Hep2). Compound (1) showed strong anti-HRV2 and HRV3 activity with a 50% inhibitory concentration (IC(50)) of 2.68 and 0.87 microg/mL, respectively, and a 50% cytotoxicity concentration (CC(50)) of 59.45 microg/mL. Ribavirin only showed anti-HRV3 activity with an IC(50) of 30.48 microg/mL and a CC(50) > 100 microg/mL. The addition of compound (1) to HRV-infected HeLa cells directly reduced the formation of visible cytopathic effect (CPE) and it directly interacted with HRV particles. Furthermore, A549 and Hep2 cells incubated with 32 microg/mL of compound (1) for 48 h exhibited antilung and antilaryngeal cancer activities, with a viability of less than 50%. These results suggest that compound (1) may be used as a potential antiviral and anticancer agent.

摘要

从 Brachyglottis monroi 中分离得到的 13(E)-labd-13-ene-8alpha,15-diol（1）具有抗病毒活性，针对人鼻病毒 2（HRV2）和 3（HRV3）进行了检测，同时对人癌细胞（A549 和 Hep2）也进行了抗癌活性检测。化合物 1 对 HRV2 和 HRV3 表现出很强的抑制活性，半数抑制浓度（IC50）分别为 2.68 和 0.87 μg/mL，细胞毒性浓度（CC50）为 59.45 μg/mL。利巴韦林仅对 HRV3 表现出抗病毒活性，IC50 为 30.48 μg/mL，CC50 ＞100 μg/mL。将化合物 1 添加到 HRV 感染的 HeLa 细胞中可直接减少可见细胞病变效应（CPE）的形成，并且它可以直接与 HRV 颗粒相互作用。此外，用 32 μg/mL 的化合物 1 孵育 A549 和 Hep2 细胞 48 h 后，表现出抗肺癌和抗喉癌活性，细胞活力低于 50%。这些结果表明，化合物 1 可能被用作潜在的抗病毒和抗癌剂。