2. Academic Validation
  3. In vitro anticancer activity of methyl caffeate isolated from Solanum torvum Swartz. fruit

In vitro anticancer activity of methyl caffeate isolated from Solanum torvum Swartz. fruit

  • Chem Biol Interact. 2015 Dec 5:242:81-90. doi: 10.1016/j.cbi.2015.09.023.
C Balachandran 1,  N Emi 2,  Y Arun 3,  Y Yamamoto 2,  B Ahilan 4,  B Sangeetha 5,  V Duraipandiyan 6,  Yoko Inaguma 2,  Akinao Okamoto 2,  S Ignacimuthu 4,  N A Al-Dhabi 6,  P T Perumal 3
Affiliations

Affiliations

  • 1 Department of Hematology, Fujita Health University, 1-98, Dengakugakubo, Kutsukake-cho, Toyoake, Aichi 470-1192, Japan; Division of Cancer Biology, Entomology Research Institute, Loyola College, Chennai 600 034, India. Electronic address: [email protected].
  • 2 Department of Hematology, Fujita Health University, 1-98, Dengakugakubo, Kutsukake-cho, Toyoake, Aichi 470-1192, Japan.
  • 3 Organic & Bio-organic Chemistry Laboratory, CSIR-Central Leather Research Institute, Chennai 600 020, India.
  • 4 Division of Cancer Biology, Entomology Research Institute, Loyola College, Chennai 600 034, India.
  • 5 Department of Toxicology, Advinus Therapeutics Ltd, Bangalore 560058, India.
  • 6 Department of Botany and Microbiology, Addiriya Chair for Environmental Studies, College of Science, King Saud University, P.O.Box.2455, Riyadh 11451, Saudi Arabia.
PMID: 26415618 DOI: 10.1016/j.cbi.2015.09.023
Abstract

The present study was undertaken to investigate the Anticancer activity of methyl caffeate isolated from Solanum torvum Swartz. fruit and to explore the molecular mechanisms of action in MCF-7 cells. Cytotoxic properties of hexane, ethyl acetate and methanol extracts were carried out against MCF-7 cells using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay. Ethyl acetate extract showed good cytototoxic activities compared to hexane and methanol extracts. Methyl caffeate was isolated from the ethyl acetate extract using column chromatography. Cytotoxic properties of methyl caffeate was investigated against MCF-7, A549, COLO320, HepG-2 and Vero cells. The compound showed potent cytotoxic properties against MCF-7 cells compared to A549, COLO320 and HepG-2 cells. Methyl caffeate significantly reduced cell proliferation and increased formation of fragmented DNA and apoptotic body in MCF-7 cells. Bcl-2, Bax, Bid, p53, Caspase-3, PARP and cytochrome c release were detected by western blot analysis. The activities of caspases-3 and PARP gradually increased after the addition of isolated compound. Bcl-2 protein was down regulated; Bid and Bax were up regulated after the treatment with methyl caffeate. Molecular docking studies showed that the compound bound stably to the active sites of poly (ADP-ribose) polymerase-1 (PARP1), B cell CLL/lymphoma-2 (Bcl-2), E3 ubiquitin-protein Ligase (MDM2) and tubulin. The results strongly suggested that methyl caffeate induced Apoptosis in MCF-7 cells via Caspase activation through cytochrome c release from mitochondria.

Keywords

Caspases; Cytochrome c; Molecular docking; Solanum torvum; p53.

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