Anticancer properties of the abietane diterpene 6,7-dehydroroyleanone obtained by optimized extraction.

Autor:	Garcia C; Research Center for Biosciences & Health Technologies (CBIOS), Universidade Lusófona de Humanidades e Tecnologias, 1749-024 Lisbon, Portugal.; Department of Biomedical Sciences, Faculty of Pharmacy, University of Alcalá, Ctra. A2, Km 33.600 - Campus Universitario, 28871 Alcalá de Henares, Spain., Silva CO; Department of Biomedical Sciences, Faculty of Pharmacy, University of Alcalá, Ctra. A2, Km 33.600 - Campus Universitario, 28871 Alcalá de Henares, Spain., Monteiro CM; Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, 1649-003 Lisbon, Portugal., Nicolai M; Research Center for Biosciences & Health Technologies (CBIOS), Universidade Lusófona de Humanidades e Tecnologias, 1749-024 Lisbon, Portugal., Viana A; CQB, Faculdade de Ciências, University of Lisbon, Campo Grande 1749-016, Lisbon, Portugal., Andrade JM; Research Center for Biosciences & Health Technologies (CBIOS), Universidade Lusófona de Humanidades e Tecnologias, 1749-024 Lisbon, Portugal.; Department of Biomedical Sciences, Faculty of Pharmacy, University of Alcalá, Ctra. A2, Km 33.600 - Campus Universitario, 28871 Alcalá de Henares, Spain., Barasoain I; Centro de Investigaciones Biológicas Consejo Superior de Investigaciones Científicas Ramiro de Maeztu, 9, 28040 Madrid, Spain., Stankovic T; Institute for Biological Research 'Siniša Stanković', University of Belgrade, Despota Stefana 142, 11060 Belgrade, Serbia., Quintana J; Department of Biochemistry & Molecular Biology, Instituto Universitario de Investigaciones Biomédicas y Sanitarias, University of Las Palmas de Gran Canaria, Paseo Blas Cabrera Felipe s/n, 35016 Las Palmas de Gran Canaria, Spain., Hernández I; Department of Biochemistry & Molecular Biology, Instituto Universitario de Investigaciones Biomédicas y Sanitarias, University of Las Palmas de Gran Canaria, Paseo Blas Cabrera Felipe s/n, 35016 Las Palmas de Gran Canaria, Spain., González I; Department of Biochemistry & Molecular Biology, Instituto Universitario de Investigaciones Biomédicas y Sanitarias, University of Las Palmas de Gran Canaria, Paseo Blas Cabrera Felipe s/n, 35016 Las Palmas de Gran Canaria, Spain., Estévez F; Department of Biochemistry & Molecular Biology, Instituto Universitario de Investigaciones Biomédicas y Sanitarias, University of Las Palmas de Gran Canaria, Paseo Blas Cabrera Felipe s/n, 35016 Las Palmas de Gran Canaria, Spain., Díaz-Lanza AM; Department of Biomedical Sciences, Faculty of Pharmacy, University of Alcalá, Ctra. A2, Km 33.600 - Campus Universitario, 28871 Alcalá de Henares, Spain., Reis CP; Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, 1649-003 Lisbon, Portugal., Afonso CA; Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, 1649-003 Lisbon, Portugal., Pesic M; Institute for Biological Research 'Siniša Stanković', University of Belgrade, Despota Stefana 142, 11060 Belgrade, Serbia., Rijo P; Research Center for Biosciences & Health Technologies (CBIOS), Universidade Lusófona de Humanidades e Tecnologias, 1749-024 Lisbon, Portugal.; Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, 1649-003 Lisbon, Portugal.
Jazyk:	angličtina
Zdroj:	Future medicinal chemistry [Future Med Chem] 2018 May 01; Vol. 10 (10), pp. 1177-1189. Date of Electronic Publication: 2018 May 11.
DOI:	10.4155/fmc-2017-0239
Abstrakt:	Aim: 6,7-dehydroroyleanone (DHR) is a cytotoxic abietane present in the essential oil of Plectranthus madagascariensis. Methods/results: Different extraction parameters were tested, and its extraction optimization was accomplished with a Clevenger apparatus-based hydrodistillation. After isolation, its effect on microtubules, P-glycoprotein and caspases was assessed on several cell lines and the compound was coupled with hybrid nanoparticles. The results show that DHR does not interfere with microtubule formation, but evades the resistance mechanisms of P-glycoprotein. Strong activation of caspases-3 and -9 indicates that DHR is able to induce apoptosis by triggering the intrinsic cell death pathway. Moreover, the assembly of DHR with hybrid nanoparticles was able to potentiate the effect of DHR in cancer cells. Conclusion: DHR seems to be a promising starting material with anticancer properties to further be explored.
Databáze:	MEDLINE
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