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

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-MB23...

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Main Authors: Ivan Montenegro, Giacomo Tomasoni, Claudia Bosio, Natalia Quiñones, Alejandro Madrid, Hector Carrasco, Andres Olea, Rolando Martinez, Mauricio Cuellar, Joan Villena
Format: Article
Language:English
Published: MDPI AG 2014-11-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/19/11/18993
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author Ivan Montenegro
Giacomo Tomasoni
Claudia Bosio
Natalia Quiñones
Alejandro Madrid
Hector Carrasco
Andres Olea
Rolando Martinez
Mauricio Cuellar
Joan Villena
author_facet Ivan Montenegro
Giacomo Tomasoni
Claudia Bosio
Natalia Quiñones
Alejandro Madrid
Hector Carrasco
Andres Olea
Rolando Martinez
Mauricio Cuellar
Joan Villena
author_sort Ivan Montenegro
collection DOAJ
description 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.
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spelling doaj.art-e1b598cd36b14f0790bc4fceb7b65e512022-12-22T01:15:34ZengMDPI AGMolecules1420-30492014-11-011911189931900610.3390/molecules191118993molecules191118993Study on the Cytotoxic Activity of Drimane Sesquiterpenes and Nordrimane Compounds against Cancer Cell LinesIvan Montenegro0Giacomo Tomasoni1Claudia Bosio2Natalia Quiñones3Alejandro Madrid4Hector Carrasco5Andres Olea6Rolando Martinez7Mauricio Cuellar8Joan Villena9Facultad de Farmacia, Escuela de Química y Farmacia, Universidad de Valparaíso, Av. Gran Bretaña N° 1093, Valparaíso 234000, ChileDepartamento de Química, Facultad de Ciencias Exactas, Universidad Andrés Bello, Quillota 910, Viña del Mar 2520000, ChileDepartamento de Química, Facultad de Ciencias Exactas, Universidad Andrés Bello, Quillota 910, Viña del Mar 2520000, ChileFacultad de Farmacia, Escuela de Química y Farmacia, Universidad de Valparaíso, Av. Gran Bretaña N° 1093, Valparaíso 234000, ChileDepartamento de Química, Universidad Técnica Federico Santa María, Av. España N° 1680, Valparaíso 2340000, ChileFacultad de Ciencias de la Salud, Universidad Autónoma de Chile, Carlos Antúnez 1920, Providencia, Santiago 7500000, ChileFacultad de Ciencias de la Salud, Universidad Autónoma de Chile, Carlos Antúnez 1920, Providencia, Santiago 7500000, ChileDepartamento de Química, Facultad de Ciencias Exactas, Universidad Andrés Bello, Quillota 910, Viña del Mar 2520000, ChileFacultad de Farmacia, Escuela de Química y Farmacia, Universidad de Valparaíso, Av. Gran Bretaña N° 1093, Valparaíso 234000, ChileCentro de Investigaciones Biomédicas (CIB), Escuela de Medicina, Universidad de Valparaíso, Av. Hontaneda N° 2664, Valparaíso 234000, ChileTwelve 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.http://www.mdpi.com/1420-3049/19/11/18993cytotoxic activitycancer cell linesapoptosismitochondrial membrane permeabilitycaspasa-3 activitynordrimanesdrimanessesquiterpenes
spellingShingle Ivan Montenegro
Giacomo Tomasoni
Claudia Bosio
Natalia Quiñones
Alejandro Madrid
Hector Carrasco
Andres Olea
Rolando Martinez
Mauricio Cuellar
Joan Villena
Study on the Cytotoxic Activity of Drimane Sesquiterpenes and Nordrimane Compounds against Cancer Cell Lines
Molecules
cytotoxic activity
cancer cell lines
apoptosis
mitochondrial membrane permeability
caspasa-3 activity
nordrimanes
drimanes
sesquiterpenes
title Study on the Cytotoxic Activity of Drimane Sesquiterpenes and Nordrimane Compounds against Cancer Cell Lines
title_full Study on the Cytotoxic Activity of Drimane Sesquiterpenes and Nordrimane Compounds against Cancer Cell Lines
title_fullStr Study on the Cytotoxic Activity of Drimane Sesquiterpenes and Nordrimane Compounds against Cancer Cell Lines
title_full_unstemmed Study on the Cytotoxic Activity of Drimane Sesquiterpenes and Nordrimane Compounds against Cancer Cell Lines
title_short Study on the Cytotoxic Activity of Drimane Sesquiterpenes and Nordrimane Compounds against Cancer Cell Lines
title_sort study on the cytotoxic activity of drimane sesquiterpenes and nordrimane compounds against cancer cell lines
topic cytotoxic activity
cancer cell lines
apoptosis
mitochondrial membrane permeability
caspasa-3 activity
nordrimanes
drimanes
sesquiterpenes
url http://www.mdpi.com/1420-3049/19/11/18993
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