Department of Orthopedics, Central Laboratory, Renmin Hospital, Wuhan University, Wuhan, 430060, People's Republic of China.
Apoptosis. 2015 Sep;20(9):1187-99. doi: 10.1007/s10495-015-1152-y.
Chondrocyte apoptosis is an important mechanism involved in osteoarthritis (OA). Berberine (BBR), a plant alkaloid derived from Chinese medicine, is characterized by multiple pharmacological effects, such as anti-inflammatory and anti-apoptotic activities. This study aimed to evaluate the chondroprotective effect and underlying mechanisms of BBR on sodium nitroprusside (SNP)-stimulated chondrocyte apoptosis and surgically-induced rat OA model. The in vitro results revealed that BBR suppressed SNP-stimulated chondrocyte apoptosis as well as cytoskeletal remodeling, down-regulated expressions of inducible nitric oxide synthase (iNOS) and caspase-3, and up-regulated Bcl-2/Bax ratio and Type II collagen (Col II) at protein levels, which were accompanied by increased adenosine monophosphate-activated protein kinase (AMPK) phosphorylation and decreased phosphorylation of p38 mitogen-activated protein kinase (MAPK). Furthermore, the anti-apoptotic effect of BBR was blocked by AMPK inhibitor Compound C (CC) and adenosine-9-β-D-arabino-furanoside (Ara A), and enhanced by p38 MAPK inhibitor SB203580. In vivo experiment suggested that BBR ameliorated cartilage degeneration and exhibited an anti-apoptotic effect on articular cartilage in a rat OA model, as demonstrated by histological analyses, TUNEL assay and immunohistochemical analyses of caspase-3, Bcl-2 and Bax expressions. These findings suggest that BBR suppresses SNP-stimulated chondrocyte apoptosis and ameliorates cartilage degeneration via activating AMPK signaling and suppressing p38 MAPK activity.
软骨细胞凋亡是骨关节炎(OA)的一个重要机制。小檗碱(BBR)是一种从中药中提取的植物生物碱,具有多种药理作用,如抗炎和抗凋亡作用。本研究旨在评估 BBR 对硝普钠(SNP)刺激的软骨细胞凋亡和手术诱导的大鼠 OA 模型的软骨保护作用及其潜在机制。体外结果表明,BBR 抑制 SNP 刺激的软骨细胞凋亡和细胞骨架重塑,下调诱导型一氧化氮合酶(iNOS)和半胱天冬酶-3 的表达,并上调 Bcl-2/Bax 比值和 II 型胶原(Col II)的蛋白水平,同时伴随着 AMPK 磷酸化增加和 p38 丝裂原活化蛋白激酶(MAPK)磷酸化减少。此外,BBR 的抗凋亡作用被 AMPK 抑制剂 Compound C(CC)和腺苷-9-β-D-呋喃糖苷(Ara A)阻断,被 p38 MAPK 抑制剂 SB203580 增强。体内实验表明,BBR 改善了软骨退变,并在大鼠 OA 模型中表现出抗软骨细胞凋亡作用,这通过组织学分析、TUNEL 检测和 caspase-3、Bcl-2 和 Bax 表达的免疫组化分析得到证实。这些发现表明,BBR 通过激活 AMPK 信号通路和抑制 p38 MAPK 活性抑制 SNP 刺激的软骨细胞凋亡并改善软骨退变。