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杜松烷倍半萜和降杜松烷化合物对癌细胞系的细胞毒性活性研究。

Study on the cytotoxic activity of drimane sesquiterpenes and nordrimane compounds against cancer cell lines.

作者信息

Montenegro Ivan, Tomasoni Giacomo, Bosio Claudia, Quiñones Natalia, Madrid Alejandro, Carrasco Hector, Olea Andres, Martinez Rolando, Cuellar Mauricio, Villena Joan

机构信息

Facultad de Farmacia, Escuela de Química y Farmacia, Universidad de Valparaíso, Av. Gran Bretaña N° 1093, Valparaíso 234000, Chile.

Departamento de Química, Facultad de Ciencias Exactas, Universidad Andrés Bello, Quillota 910, Viña del Mar 2520000, Chile.

出版信息

Molecules. 2014 Nov 18;19(11):18993-9006. doi: 10.3390/molecules191118993.

Abstract

Twelve drimanes, including polygodial (1), isopolygodial (2), drimenol (3), confertifolin (4), and isodrimenin (5), were obtained from natural sources. Semi-synthetic derivatives 6-12 were obtained from 1 and 2, and cytotoxic activity was evaluated in vitro against cancer cell lines (HT-29, MDA-MB231, DHF, MCF-7, PC-3, DU-145, and CoN). IC50 values were determined at concentrations of 12.5-100 µM of each compound for 72 h. In addition, it was found that polygodial (1), 8, and 12 induced changes in mitochondrial membrane permeability in CoN, MCF-7, and PC-3 cells.

摘要

从天然来源获得了12种环戊二烯类化合物,包括多香树醛(1)、异多香树醛(2)、环戊二烯醇(3)、 confertifolin(4)和异环戊二烯宁(5)。半合成衍生物6 - 12由1和2制得,并在体外对癌细胞系(HT - 29、MDA - MB231、DHF、MCF - 7、PC - 3、DU - 145和CoN)进行了细胞毒性活性评估。在每种化合物浓度为12.5 - 100 µM的情况下测定72小时的IC50值。此外,发现多香树醛(1)、8和12在CoN、MCF - 7和PC - 3细胞中诱导线粒体膜通透性发生变化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/943d/6270921/9d81322e2b64/molecules-19-18993-g001.jpg

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