4.5 Article

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

期刊

FUTURE MEDICINAL CHEMISTRY
卷 10, 期 10, 页码 1177-1189

出版社

FUTURE SCI LTD
DOI: 10.4155/fmc-2017-0239

关键词

6,7-dehydroroyleanone; cytotoxicity; extraction; isolation; multidrug resistance; nanotechnology; Plectranthus

资金

  1. PADDIC (ALIES-COFAC) as part of the PhD Program in Health Sciences from Universidad de Alcala de Henares
  2. Universidade Lusofona de Humanidades e Tecnologias
  3. Fundacao para a Ciencia e Tecnologia [UID/DTP/04567/2016 - CBIOS/PRUID/B11/2017]
  4. Ministry of Education, Science and Technological Development of the Republic of Serbia [III41031]
  5. COST Action [CM1407]

向作者/读者索取更多资源

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.

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