Department of Orthopaedic Surgery, Second Affiliated Hospital, School of Medicine, Zhejiang University, PR China.
Phytother Res. 2011 Jun;25(6):878-85. doi: 10.1002/ptr.3359. Epub 2010 Nov 24.
Berberine shows anticancer, antibacterial, antiinflammatory and antioxidant effects and may be useful in many clinical applications. The effects of berberine on articular cartilage metabolism remain unknown, so this study was performed to evaluate these effects in vitro and in vivo. For the in vitro work, rat articular chondrocytes were cultured in a monolayer and matrix metalloproteinase-1 (MMP-1), -3, -13 and tissue inhibitor of metalloproteinase (TIMP-1) expression was evaluated by real-time quantitative PCR. Nitric oxide (NO) levels were determined using the Griess reaction, and glycosaminoglycan (GAG) release was measured using the dimethylmethylene blue method. For the in vivo work, berberine was administered by intraarticular injection, and the effects on MMPs and TIMP-1 were examined at the gene and protein levels. Berberine was found to inhibit the expression of MMP-1, -3 and -13, and increased the level of TIMP-1 at the mRNA level in a dose-dependent manner. In IL-1β-induced rat articular chondrocytes, berberine decreased IL-1β-induced GAG release and NO production. Meanwhile, high-dose berberine exhibited an anticatabolic effect in an IL-1β-induced rat osteoarthritis (OA) model. These findings suggest that berberine may play a protective role in the development of OA and may be useful in the treatment of OA.
小檗碱具有抗癌、抗菌、抗炎和抗氧化作用，可能在许多临床应用中有用。小檗碱对关节软骨代谢的影响尚不清楚，因此进行了这项研究以评估其在体外和体内的作用。在体外工作中，将大鼠关节软骨细胞在单层中培养，并通过实时定量 PCR 评估基质金属蛋白酶-1 (MMP-1)、-3、-13 和金属蛋白酶组织抑制剂 (TIMP-1) 的表达。通过格里斯反应测定一氧化氮 (NO) 水平，通过二甲亚甲基蓝法测定糖胺聚糖 (GAG) 释放。在体内工作中，通过关节内注射给予小檗碱，并在基因和蛋白质水平上检查其对 MMPs 和 TIMP-1 的影响。小檗碱以剂量依赖性方式抑制 MMP-1、-3 和 -13 的表达，并增加 TIMP-1 的 mRNA 水平。在 IL-1β诱导的大鼠关节软骨细胞中，小檗碱降低了 IL-1β诱导的 GAG 释放和 NO 产生。同时，高剂量小檗碱在 IL-1β诱导的大鼠骨关节炎 (OA) 模型中表现出抗分解代谢作用。这些发现表明小檗碱可能在 OA 的发展中发挥保护作用，并可能对 OA 的治疗有用。
