Lee Su-Kyung, Chun Hyo Kon, Yang Jae Young, Han Dong Cho, Son Kwang-Hee, Kwon Byoung-Mog
Korea Research Institute of Bioscience and Biotechnology, 52 Uendong, Yusung, Taejon 305-600, Republic of Korea.
Bioorg Med Chem. 2007 Jun 15;15(12):4085-90. doi: 10.1016/j.bmc.2007.03.081. Epub 2007 Mar 30.
Because the activation of matrix metalloproteinases (MMP) is a key factor in the metastatic process, compounds with the ability to inhibit MMP activity have a potential in the treatment of tumor. From the examination of 2000 plant extracts, obovatal isolated from the extract of the leaves of Magnolia obovata THUNB was a potent inhibitor of MMP-2 enzyme in vitro. In human fibrosarcoma cells (HT1080) activated with MMP-2, obovatal inhibited MMP-2 enzyme activity and expression. In addition, the compound blocked migration and invasion of the cells. This study demonstrates that obovatal exerts its anticancer effects through blocking migration and invasion by inhibition of MMP-2 expression and activity, and also will be a good lead molecule for the development of anti-tumor drug.
由于基质金属蛋白酶（MMP）的激活是转移过程中的关键因素，具有抑制MMP活性能力的化合物在肿瘤治疗方面具有潜力。通过对2000种植物提取物的检测，从日本厚朴（Magnolia obovata THUNB）叶片提取物中分离出的倒卵叶木兰脂素（obovatal）在体外是MMP-2酶的有效抑制剂。在用MMP-2激活的人纤维肉瘤细胞（HT1080）中，倒卵叶木兰脂素抑制MMP-2酶的活性和表达。此外，该化合物还能阻止细胞的迁移和侵袭。本研究表明，倒卵叶木兰脂素通过抑制MMP-2的表达和活性来阻止迁移和侵袭，从而发挥其抗癌作用，并且它将成为开发抗肿瘤药物的良好先导分子。
