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

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• 作者：Yong Joo Park^a ; Chang-Ik Choi^b ; Kyu Hyuck Chung^a ; ^{khchung@skku.edu" class="auth_mail" title="E-mail the corresponding author} ; Ki Hyun Kim^a ; ^{khkim83@skku.edu" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Pharbilignan C ; Pharbitis nil ; Antiproliferative ; Apoptosis ; Intrinsic pathway
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 October 2016
• 年：2016
• 卷：26
• 期：19
• 页码：4645-4649
• 全文大小：1482 K

文摘

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 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.