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

Author:

Garcia Catarina12,Silva Catarina Oliveira2,Monteiro Carlos M3,Nicolai Marisa1,Viana Ana4,Andrade Joana M12,Barasoain Isabel5,Stankovic Tijana6,Quintana José7,Hernández Inmaculada7,González Ignacio7,Estévez Francisco7,Díaz-Lanza Ana M2,Reis Catarina P3,Afonso Carlos AM3,Pesic Milica6,Rijo Patrícia13

Affiliation:

1. Research Center for Biosciences & Health Technologies (CBIOS), Universidade Lusófona de Humanidades e Tecnologias, 1749–024 Lisbon, Portugal

2. Department of Biomedical Sciences, Faculty of Pharmacy, University of Alcalá, Ctra. A2, Km 33.600 – Campus Universitario, 28871 Alcalá de Henares, Spain

3. Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, 1649–003 Lisbon, Portugal

4. CQB, Faculdade de Ciências, University of Lisbon, Campo Grande 1749–016, Lisbon, Portugal

5. Centro de Investigaciones Biológicas Consejo Superior de Investigaciones Científicas Ramiro de Maeztu, 9, 28040 Madrid, Spain

6. Institute for Biological Research ‘Siniša Stanković’, University of Belgrade, Despota Stefana 142, 11060 Belgrade, Serbia

7. 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

Abstract

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.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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