Study on the Cytotoxic Activity of Drimane Sesquiterpenes and Nordrimane Compounds against Cancer Cell Lines

Molecules

Ivan Montenegro⁴  Giacomo Tomasoni⁵  Claudia Bosio⁵  Natalia Quiñones⁴  Alejandro Madrid³  Hector Carrasco⁶  Andres Olea⁶  Rolando Martinez⁵  Mauricio Cuellar⁴  Joan Villena¹  Jean Jacques Vanden Eynde²  Annie Mayence² 

[1] Centro de Investigaciones Biomédicas (CIB), Escuela de Medicina, Universidad de Valparaíso, Av. Hontaneda N° 2664, Valparaíso 234000, ChileFacultad de Farmacia, Escuela de Química y Farmacia, Universidad de Valparaíso, Av. Gran Bretaña N° 1093, Valparaíso 234000, Chile;;Departamento de Química, Universidad Técnica Federico Santa María, Av. España N° 1680, Valparaíso 2340000, Chile; E-Mail:;Facultad de Farmacia, Escuela de Química y Farmacia, Universidad de Valparaíso, Av. Gran Bretaña N° 1093, Valparaíso 234000, Chile; E-Mails:;Departamento de Química, Facultad de Ciencias Exactas, Universidad Andrés Bello, Quillota 910, Viña del Mar 2520000, Chile; E-Mails:;Facultad de Ciencias de la Salud, Universidad Autónoma de Chile, Carlos Antúnez 1920, Providencia, Santiago 7500000, Chile; E-Mails:

关键词: cytotoxic activity;    cancer cell lines;    apoptosis;    mitochondrial membrane permeability;    caspasa-3 activity;    nordrimanes;    drimanes;    sesquiterpenes;   

DOI  :  10.3390/molecules191118993

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.