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黄芩素通过丝裂原活化蛋白激酶(MAPK)依赖机制抑制软骨细胞中基质金属蛋白酶(MMPs)的表达。

Baicalein Inhibits MMPs Expression via a MAPK-Dependent Mechanism in Chondrocytes.

作者信息

Chen Wei-Ping, Xiong Yan, Hu Peng-Fei, Bao Jia-Peng, Wu Li-Dong

机构信息

Department of Orthopedic Surgery, the Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, China.

出版信息

Cell Physiol Biochem. 2015;36(1):325-33. doi: 10.1159/000374075. Epub 2015 May 5.

Abstract

BACKGROUND

Baicalein is a flavonoid isolated from Scutellaria baicalensis Georgi. Here, we investigated the anti-osteoarthritic effect of baicalein in vitro and in vivo.

METHODS

Interleukin-1 beta (IL-1β)-induced chondrocytes were treated with different concentrations of baicalein, real-time PCR and ELISA were performed to detect the matrix metalloproteinases (MMPs) expression. Western blot was used to evaluate the mitogen-activated protein kinase (MAPK) expression. In experimental osteoarthritis (OA), rabbits were treated with baicalein, gross morphological and histological assessment was performed to evaluate the cartilage damage.

RESULTS

Baicalein significantly reduced the expression of MMPs in vitro and in vivo. Moreover, baicalein significantly reduced the phosphorylation of p38 and extracellular signal regulated kinase (ERK), but not of c-Jun N-terminal kinase (JNK). In addition, intra-articular injection of baicalein ameliorated the cartilage damage in a rabbit model of OA induced by anterior cruciate ligament transection (ACLT).

CONCLUSIONS

The results indicate that baicalein may be considered as a potential agent for OA treatment.

摘要

背景

黄芩素是从黄芩中分离出的一种黄酮类化合物。在此,我们研究了黄芩素在体外和体内的抗骨关节炎作用。

方法

用不同浓度的黄芩素处理白细胞介素-1β(IL-1β)诱导的软骨细胞,进行实时聚合酶链反应(PCR)和酶联免疫吸附测定(ELISA)以检测基质金属蛋白酶(MMPs)的表达。采用蛋白质免疫印迹法评估丝裂原活化蛋白激酶(MAPK)的表达。在实验性骨关节炎(OA)中,用黄芩素处理兔子,进行大体形态学和组织学评估以评价软骨损伤情况。

结果

黄芩素在体外和体内均显著降低了MMPs的表达。此外,黄芩素显著降低了p38和细胞外信号调节激酶(ERK)的磷酸化水平,但对c-Jun氨基末端激酶(JNK)的磷酸化水平无影响。另外,关节内注射黄芩素改善了前交叉韧带横断(ACLT)诱导的兔OA模型中的软骨损伤。

结论

结果表明黄芩素可能被视为一种治疗OA的潜在药物。

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