竞争型MMP-2抑制剂黄芩素对口腔鳞状癌细胞生长和转移作用的影响

Studies of MMP-2 competitive inhibitors of baicalein on oral squamous cell carcinoma

目的：探讨明胶酶（MMP-2）抑制剂黄芩素对口腔鳞状细胞癌细胞的生长和转移抑制机制。方法：采用酶抑制动力学方法,研究了黄芩素（0～150μmol/L）对MMP-2的抑制作用,并进一步的分析了黄芩素（0～200μmol/L）对口腔鳞状细胞癌Tca-8113的生长的抑制作用,Tca-8113细胞转移的抑制作用和Tca-8113细胞中TIMP-2、MMP-2和TGF-β1表达水平的影响。结果：黄芩素能够竞争性的抑制MMP-2的活性和诱导Tca-8113的凋亡（黄芩素半抑制浓度IC50分别为17.26±1.23μmol/L和24.39±0.97μmol/L）;随着黄芩素作用浓度（5、10、50、100μmol/L）的增加,MMP-2和TGF-β1表达均呈现降低趋势,TIMP-2的表达呈增加趋势,且肿瘤细胞穿过人工基底膜的能力下降。结论：黄芩素能够通过抑制MMP-2的活性和增强TIMP-2的表达,诱导了MMP-2和TGF-β1表达的降低,最终对口腔鳞状细胞癌Tca-8113的转移和凋亡起到重要作用。

Purpose： Study the effect of gelatinase（ MMP-2） inhibitor baicalein on oral squamous cell carcinoma growth and metastasis suppressormechanisms. Method： Using the method of enzyme inhibition kinetics method to study the effect of baicalein（ 0 ～ 150μmol / L） on the inhibition of MMP-2,and further analysis of the inhibitory effect of baicalein（ 0 ～ 200μmol / L） on the growth of oral squamous cell carcinomal line Tca-8113,Tca-8113 metastasis of tumor cells and inhibition of TIMP-2,MMP-2 and TGF-β1 expression levels of influence. Results： Baicalein could induce apoptosis in oral squamous cell carcinomal line Tca-811 and inhibitory of MMP-2（ half inhibition Concentration IC50was17. 26 ± 1. 23 μmol / L and 24. 39 ± 0. 97 μmol / L respectively）; With the increasing concentration of baicalein（ 5,10,50,100μmol / L）,MMP-2 and TGF-β1 expression showed a decrease,and TIMP-2 expression showed a inecreasd,the ability of tumor cells through artificial basement membrane is degraded. Conclusion： Baicalein as a inhibitor of MMP-2,which reduced induced MMP-2 and TGF-β1 expression,eventually play an important role on apoptosis of oral squamous cell carcinomal line Tca-8113.