Montenegro Ivan, Tomasoni Giacomo, Bosio Claudia, Quiñones Natalia, Madrid Alejandro, Carrasco Hector, Olea Andres, Martinez Rolando, Cuellar Mauricio, Villena Joan
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.
Molecules. 2014 Nov 18;19(11):18993-9006. doi: 10.3390/molecules191118993.
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.
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。