Pharbilignan C induces apoptosis through a mitochondria-mediated intrinsic pathway in human breast cancer cells

Yong Joo Park, Chang Ik Choi, Kyu Hyuck Chung, Ki Hyun Kim

Research output: Contribution to journalArticlepeer-review

14 Scopus citations

Abstract

Pharbitidis Semen, the seed of Morning glory (Pharbitis nil), is a medicinal agent that has traditionally been used as a purgative in Korea. Pharbilignan C (PLC) is a dihydro[b]-benzofuran-type neolignan from Pharbitidis Semen, which reportedly exhibited the most potent cytotoxicity against human tumor cells. To further study the antiproliferative activity of PLC, its molecular mechanisms of action in two breast adenocarcinoma cells, MCF-7 and MDA-MB 231 cells were investigated. PLC inhibited the proliferation of MDA-MB 231 and MCF-7 cells, in order of sensitivity (IC50of MDA-MB 231 cells: 7.0 ± 2.0 μM). PLC induced apoptosis in MDA-MB 231 cells with down regulation of Bcl-2 and up-regulation of Bax expression. It also decreased mitochondrial membrane potential accompanied with increasing initiator caspase, caspase-9 activation and executioner caspase, caspase-3 activation. This study demonstrates that PLC inhibited proliferation of MDA-MB 231 cells by inducing apoptosis via the mitochondria-mediated intrinsic pathway.

Original languageEnglish
Pages (from-to)4645-4649
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number19
DOIs
StatePublished - 2016

Keywords

  • Antiproliferative
  • Apoptosis
  • Intrinsic pathway
  • Pharbilignan C
  • Pharbitis nil

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