Hu Qin, Gao Lina, Peng Bo, Liu Xinmin
College of Life Sciences and Bio-Engineering, Beijing University of Technology, Beijing 100024, P.R. China.
Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences, Beijing 100193, P.R. China.
Exp Ther Med. 2017 Oct;14(4):3074-3080. doi: 10.3892/etm.2017.4888. Epub 2017 Aug 4.
Baicalin and baicalein are flavonoid compounds derived from Georgi. These compounds have been used in the treatment of numerous diseases, including fibrotic diseases. However, research regarding their antifibrotic effects and mechanism of action in renal fibrosis is limited. In the present study, normal rat kidney interstitial fibroblast (NRK-49F) cells were stimulated with transforming growth factor (TGF)-β1, with or without baicalin/baicalein, and assessed for proliferation, apoptosis, extracellular matrix (ECM) accumulation, collagen expression, TGF-β1 expression and mothers against decapentaplegic homolog 3 (SMAD3) protein activation. The results revealed that baicalin and baicalein exhibited antifibrotic effects , whereas baicalein had a stronger inhibitory action compared with baicalin on TGF-β1-induced NRK-49F cell proliferation, deposition of ECM, collagen synthesis, endogenous TGF-β1 expression and phosphorylation of SMAD3. In conclusion, the findings of the present study indicate that baicalin and baicalein, particularly baicalein, exhibit antifibrotic effects by inhibiting the TGF-β1 pathway. Therefore, these compounds have the potential to be developed as novel agents to treat renal fibrosis.
黄芩苷和黄芩素是从黄芩中提取的黄酮类化合物。这些化合物已被用于治疗多种疾病,包括纤维化疾病。然而,关于它们在肾纤维化中的抗纤维化作用及其作用机制的研究有限。在本研究中,用转化生长因子(TGF)-β1刺激正常大鼠肾间质成纤维细胞(NRK-49F),同时添加或不添加黄芩苷/黄芩素,并评估细胞的增殖、凋亡、细胞外基质(ECM)积累、胶原蛋白表达、TGF-β1表达以及母亲对五体不全同源物3(SMAD3)蛋白的激活情况。结果显示,黄芩苷和黄芩素均表现出抗纤维化作用,而与黄芩苷相比,黄芩素对TGF-β1诱导的NRK-49F细胞增殖、ECM沉积、胶原蛋白合成、内源性TGF-β1表达及SMAD3磷酸化具有更强的抑制作用。总之,本研究结果表明,黄芩苷和黄芩素,尤其是黄芩素,通过抑制TGF-β1信号通路发挥抗纤维化作用。因此,这些化合物有潜力被开发为治疗肾纤维化的新型药物。