Department of Orthopedics, Hainan Hospital of Chinese PLA General Hospital, 80 Jianglin Road, Sanya, Hainan, People's Republic of China.
Department of Gerontology, Hainan Hospital of Chinese PLA General Hospital, Sanya, People's Republic of China.
J Orthop Surg Res. 2023 Mar 13;18(1):198. doi: 10.1186/s13018-023-03571-5.
Osteoarthritis (OA) is the most common degenerative disease in joints among elderly patients. Senescence is deeply involved in the pathogenesis of osteoarthritis. Metformin is widely used as the first-line drug for Type 2 diabetes mellitus (T2DM), and has great potential for the treatment of other aging-related disorders, including OA. However, the role of metformin in OA is not fully elucidated. Therefore, our aim here was to investigate the effects of metformin on human chondrocytes.
After metformin treatment, expression level of microRNA-34a and SIRT1 in chondrocyte were detected with quantitative real-time PCR and immunofluorescence staining. Then, microRNA-34a mimic and small interfering RNA (siRNA) against SIRT1 (siRNA-SIRT1) were transfected into chondrocyte. Senescence-associated β-galactosidase (SA-β-gal) staining was performed to assess chondrocyte senescence. Chondrocyte viability was illustrated with MTT and colony formation assays. Western blot was conducted to detect the expression of P16, IL-6, matrix metalloproteinase-13 (MMP-13), Collagen type II (COL2A1) and Aggrecan (ACAN).
We found that metformin treatment (1 mM) inhibited microRNA-34a while promoted SIRT1 expression in OA chondrocytes. Both miR-34a mimics and siRNA against SIRT1 inhibited SIRT1 expression in chondrocytes. SA-β-gal staining assay confirmed that metformin reduced SA-β-gal-positive rate of chondrocytes, while transfection with miR-34a mimics or siRNA-SIRT1 reversed it. MTT assay and colony formation assay showed that metformin accelerated chondrocyte proliferation, while miR-34a mimics or siRNA-SIRT1 weakened this effect. Furthermore, results from western blot demonstrated that metformin suppressed expression of senescence-associated protein P16, proinflammatory cytokine IL-6 and catabolic gene MMP-13 while elevated expression of anabolic proteins such as Collagen type II and Aggrecan, which could be attenuated by transfection with miR-34a mimics.
Overall, our data suggest that metformin regulates chondrocyte senescence and proliferation through microRNA-34a/SIRT1 pathway, indicating it could be a novel strategy for OA treatment.
骨关节炎(OA)是老年患者中最常见的关节退行性疾病。衰老与骨关节炎的发病机制密切相关。二甲双胍被广泛用作 2 型糖尿病(T2DM)的一线药物,并且在治疗其他与衰老相关的疾病方面具有很大的潜力,包括 OA。然而,二甲双胍在 OA 中的作用尚未完全阐明。因此,我们的目的是研究二甲双胍对人软骨细胞的影响。
用二甲双胍处理后,用实时定量 PCR 和免疫荧光染色检测软骨细胞中 microRNA-34a 和 SIRT1 的表达水平。然后,将 microRNA-34a 模拟物和针对 SIRT1 的小干扰 RNA(siRNA-SIRT1)转染入软骨细胞。用衰老相关β-半乳糖苷酶(SA-β-gal)染色评估软骨细胞衰老。用 MTT 和集落形成实验检测软骨细胞活力。用 Western blot 检测 P16、IL-6、基质金属蛋白酶-13(MMP-13)、Collagen type II(COL2A1)和 Aggrecan(ACAN)的表达。
我们发现,二甲双胍处理(1mM)抑制 OA 软骨细胞中的 microRNA-34a,同时促进 SIRT1 表达。miR-34a 模拟物和 SIRT1 的 siRNA 均可抑制软骨细胞中的 SIRT1 表达。SA-β-gal 染色实验证实,二甲双胍降低了软骨细胞中 SA-β-gal 阳性率,而转染 miR-34a 模拟物或 siRNA-SIRT1 则逆转了这一结果。MTT 检测和集落形成实验表明,二甲双胍加速了软骨细胞的增殖,而 miR-34a 模拟物或 siRNA-SIRT1 则削弱了这一作用。此外,Western blot 结果表明,二甲双胍抑制衰老相关蛋白 P16、促炎细胞因子 IL-6 和分解代谢基因 MMP-13 的表达,同时上调合成代谢蛋白如 Collagen type II 和 Aggrecan 的表达,而转染 miR-34a 模拟物可减弱这一作用。
总的来说,我们的数据表明,二甲双胍通过 microRNA-34a/SIRT1 通路调节软骨细胞衰老和增殖,提示其可能成为 OA 治疗的新策略。