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卤代二萜烯类化合物从柳珊瑚中提取的细胞毒性活性。

Cytotoxic activity of halogenated sesquiterpenes from Laurencia dendroidea.

机构信息

Laboratório de Produtos Bioativos, Universidade Federal do Rio de Janeiro, Campus Macaé Dr. Aloísio Teixeira. Rua Alcides da Conceição, 159, 27933-378, Macaé, Rio de Janeiro, Brazil.

Laboratório de Produtos Naturais e Ensaios Biológicos, Departamento De Produtos Naturais e Alimentos, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, Rio de Janeiro, 21941-902, Brazil.

出版信息

Phytother Res. 2018 Jun;32(6):1119-1125. doi: 10.1002/ptr.6052. Epub 2018 Feb 26.

DOI:10.1002/ptr.6052
PMID:29480520
Abstract

Red algae of the genus Laurencia J. V. Lamouroux are found in tropical and subtropical regions throughout the world and are an extremely rich source of active secondary metabolites with diverse structural features. In the present study, 6 sesquiterpenes (obtusol, (-)-elatol, dendoidiol, debrome-elatol, triquinane, and obtusane) isolated from Laurencia dendroidea were investigated for their cytotoxicity, using 4 cancer cell lines (U937, Jurkat, B16F10, and Colo-205). Among all sesquiterpenes tested, obtusol and (-)-elatol showed a promising activity in the treatment of Colo-205 strain, with IC of 1.2 ± 1.4 and 2.5 ± 1.3 μg/ml, respectively. In addition, fluorescence microscopy results indicated that, at 100 μg/ml, obtusol induced apoptosis at 79% and (-)-elatol at 95%. Activation of Caspases 2, 4, 6, and 8 showed to be involved in (-)-elatol activity and only Caspase 6 in obtusol activity. These data demonstrated the effective apoptosis-inducing activity of the sesquiterpene (-)-elatol and obtusol in the treatment of Colo-205 strain. Therefore, more studies should be done so that the sesquiterpenes (-)-elatol and obtusol might become promising chemotherapy.

摘要

柳珊瑚属的红藻分布于世界各地的热带和亚热带地区,是具有多种结构特征的活性次生代谢产物的极其丰富的来源。在本研究中,从柳珊瑚属中分离得到的 6 种倍半萜类化合物(钝叶醇、(-)-表醇、树状二醇、去溴表醇、三尖杉烷和钝叶烷),用 4 种癌细胞系(U937、Jurkat、B16F10 和 Colo-205)进行了细胞毒性测试。在所测试的所有倍半萜类化合物中,钝叶醇和(-)-表醇在治疗 Colo-205 株方面表现出有希望的活性,IC 分别为 1.2±1.4 和 2.5±1.3μg/ml。此外,荧光显微镜结果表明,在 100μg/ml 时,钝叶醇诱导 79%的细胞凋亡,(-)-表醇诱导 95%的细胞凋亡。Caspase 2、4、6 和 8 的激活被证明与(-)-表醇的活性有关,而仅 Caspase 6 与钝叶醇的活性有关。这些数据表明(-)-表醇和钝叶醇这两种倍半萜类化合物在治疗 Colo-205 株方面具有有效的诱导细胞凋亡活性。因此,应该进行更多的研究,以使(-)-表醇和钝叶醇这两种倍半萜类化合物成为有前途的化疗药物。

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