Department of Physiology, School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang, 110016, China.
Department of Medicinal Chemistry and Natural Medicine Chemistry, School of Pharmacy, Harbin Medical University, Harbin, 150081, China.
Acta Pharmacol Sin. 2018 Dec;39(12):1855-1864. doi: 10.1038/s41401-018-0026-6. Epub 2018 May 23.
Salvianolic acid A (SAA) is a minor phenolic carboxylic acid extracted from Salviae miltiorrhizae Bunge (Danshen). SAA exhibits a variety of pharmacological activities, such as antioxidative, anti-thrombotic, neuroprotective, and anti-fibrotic effects, as well as protection from myocardial ischemia and prevention of diabetes and other diseases. Furthermore, SAA has shown renal-protective effects in doxorubicin-induced nephropathy. However, there has been limited research regarding the effects of SAA and underlying mechanisms in chronic kidney disease (CKD). Here, we examined the effects and molecular mechanisms of SAA in an established animal model of 5/6 nephrectomized (5/6Nx) rats. The rats were injected with SAA (2.5, 5, and 10 mg/kg per day, intraperitoneally (ip)) for 28 days. SAA dose-dependently lowered the levels of urine protein, blood urea nitrogen, serum creatinine, plasma total cholesterol, and plasma triglycerides in 5/6Nx rats. Histological examination revealed that SAA dose-dependently attenuated renal pathological lesions, evidenced by reduced renal tubulointerstitial fibrosis by decreasing the expression levels of tumor growth factor-β1 and α-smooth muscle actin in 5/6Nx rats. Moreover, SAA dose-dependently inhibited the activation of nuclear factor-κB (NF-κB) and p38 mitogen-activated protein kinase (MAPK) signaling pathways, subsequently attenuating the secretion of tumor necrosis factor-α and interleukin-1β and inhibiting the expression of monocyte chemotactic protein-1, intercellular adhesion molecule-1, and vascular cell adhesion molecule-1 in kidneys of 5/6Nx rats. The above results were consistent with those obtained in lipopolysaccharide-induced HK-2 cells in vitro (a recognized in vitro inflammatory model). In conclusion, our results demonstrated that SAA effectively attenuates kidney injury in 5/6Nx rats. The therapeutic effects of SAA on kidney injury can be attributed to its anti-inflammatory activities through inhibition of the activation of the NF-κB and p38 MAPK signaling pathways.
丹酚酸 A(SAA)是从丹参中提取的一种次要的酚羧酸。SAA 表现出多种药理活性,如抗氧化、抗血栓、神经保护和抗纤维化作用,以及心肌缺血保护和预防糖尿病等疾病。此外,SAA 在阿霉素诱导的肾病中表现出肾脏保护作用。然而,关于 SAA 在慢性肾脏病(CKD)中的作用及其潜在机制的研究有限。在这里,我们在建立的 5/6 肾切除(5/6Nx)大鼠动物模型中研究了 SAA 的作用和分子机制。大鼠每天腹膜内(ip)注射 SAA(2.5、5 和 10mg/kg)28 天。SAA 剂量依赖性地降低了 5/6Nx 大鼠的尿蛋白、血尿素氮、血清肌酐、血浆总胆固醇和血浆甘油三酯水平。组织学检查显示,SAA 剂量依赖性地减轻了肾脏病理损伤,通过降低肿瘤生长因子-β1 和α-平滑肌肌动蛋白的表达水平减轻了肾小管间质纤维化。此外,SAA 剂量依赖性地抑制了核因子-κB(NF-κB)和 p38 丝裂原活化蛋白激酶(MAPK)信号通路的激活,随后减弱了肿瘤坏死因子-α和白细胞介素-1β的分泌,并抑制了单核细胞趋化蛋白-1、细胞间黏附分子-1 和血管细胞黏附分子-1在 5/6Nx 大鼠肾脏中的表达。上述结果与体外脂多糖诱导的 HK-2 细胞(公认的体外炎症模型)的结果一致。总之,我们的结果表明 SAA 可有效减轻 5/6Nx 大鼠的肾脏损伤。SAA 对肾脏损伤的治疗作用可归因于其通过抑制 NF-κB 和 p38 MAPK 信号通路的激活来发挥抗炎作用。