Baicalein Inhibits MMPs Expression via a MAPK-Dependent Mechanism in Chondrocytes
Baicalein Inhibits MMPs Expression via a MAPK-Dependent Mechanism in Chondrocytes
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DOI：
10.1159/000374075
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发表时间：
2015-01-01
影响因子：
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通讯作者：
Wu, Li-Dong
中科院分区：
文献类型：
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作者：
Chen, Wei-Ping;Xiong, Yan;Wu, Li-Dong
背景：黄芩素是从黄芩中分离得到的一种黄酮类化合物。在此，我们研究了黄芩素在体内外的抗骨关节炎作用。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，采用实时荧光定量聚合酶链式反应和酶联免疫吸附试验检测基质金属蛋白酶(MMPs)的表达。Western印迹法检测丝裂原活化蛋白激酶(MAPK)的表达。在实验性骨关节炎(OA)模型上，用黄芩素治疗，通过大体形态和组织学评价软骨损伤情况。结果：黄芩素在体内外均能显著降低MMPs的表达。此外，黄芩素显著降低p38和细胞外信号调节激酶(ERK)的磷酸化，但对c-jun氨基末端激酶(JNK)的磷酸化无明显影响。此外，关节内注射黄芩素可改善兔前交叉韧带切断(ACLT)所致的骨性关节炎模型的软骨损伤。结论：黄芩素可作为治疗骨性关节炎的潜在药物。版权所有(C)2015年S.Karger AG，巴塞尔
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-1 beta)-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. Copyright (C) 2015 S. Karger AG, Basel