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

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초록

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 (IC50 of MDA-MB 231 cells: 7.0 +/- 2.0 mu M). 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. (C) 2016 Elsevier Ltd. All rights reserved.

키워드

Pharbilignan CPharbitis nilAntiproliferativeApoptosisIntrinsic pathwaySEEDSCONSTITUENTSMDA-MB-231RELEASEEXTRACTLIGNANSAGENTSMCF-7
제목
Pharbilignan C induces apoptosis through a mitochondria-mediated intrinsic pathway in human breast cancer cells
저자
Park, Yong JooChoi, Chang-IkChung, Kyu HyuckKim, Ki Hyun
DOI
10.1016/j.bmcl.2016.08.054
발행일
2016-10-01
유형
Article
저널명
Bioorganic and Medicinal Chemistry Letters
26
19
페이지
4645 ~ 4649