College of Pharmacy, Duksung Women's University, Seoul, Republic of Korea.
Oncol Rep. 2012 Feb;27(2):567-72. doi: 10.3892/or.2011.1508. Epub 2011 Oct 20.
Genipin, a constituent of Gardenia jasminoides Ellis, is used in the treatment of hepatic disorders and inflammatory diseases in traditional medicine. Although mounting evidence suggests an anti-tumor activity of genipin in several cancer cell systems, the inhibitory effect of genipin on the growth of breast cancer cells has not been reported yet. The present study aimed to investigate the anti-proliferative activity of genipin in MDA-MB-231 human breast cancer cells. Herein, we showed that genipin efficiently induced apoptosis in MDA-MB-231 cells by the down-regulation of Bcl-2, up-regulation of Bax and proteolytic activation of caspase-3. Activation of JNK and p38 MAPK also increased by genipin. Importantly, genipin significantly inhibited invasive and migratory phenotypes of MDA-MB-231 cells. Taken together, this study demonstrates that genipin induces apoptosis and inhibits invasive/migratory abilities of highly invasive MDA-MB-231 human breast cancer cells, suggesting a potential application of genipin as a chemopreventive agent that may prevent or alleviate metastatic breast cancer.
京尼平是栀子（Gardenia jasminoides Ellis）的一种成分，在传统医学中用于治疗肝脏疾病和炎症性疾病。尽管越来越多的证据表明京尼平在几种癌细胞系统中具有抗肿瘤活性，但京尼平对乳腺癌细胞生长的抑制作用尚未见报道。本研究旨在探讨京尼平对 MDA-MB-231 人乳腺癌细胞的增殖抑制作用。本文表明，京尼平通过下调 Bcl-2、上调 Bax 和半胱天冬酶-3 的蛋白水解激活，有效地诱导 MDA-MB-231 细胞凋亡。JNK 和 p38 MAPK 的激活也被京尼平增加。重要的是，京尼平显著抑制 MDA-MB-231 细胞的侵袭和迁移表型。综上所述，本研究表明，京尼平诱导高度侵袭性的 MDA-MB-231 人乳腺癌细胞凋亡，并抑制其侵袭/迁移能力，提示京尼平作为一种化学预防剂具有潜在的应用价值，可能预防或减轻转移性乳腺癌。
