Department of Endocrinology, Hebei Geriatric Hospital, Shijiazhuang, Hebei, China.
Department of Cardiovascular Medicine, Hebei Geriatric Hospital, Shijiazhuang, Hebei, China.
Kaohsiung J Med Sci. 2021 Feb;37(2):136-144. doi: 10.1002/kjm2.12305. Epub 2020 Oct 31.
Skimmin, a natural coumarin derivate, has been showed to be protective against experimental diabetic nephropathy; however, its protective effect on diabetic cardiomyopathy (DCM) is not clarified. By using in vitro and in vivo models, we investigated skimmin's protective effect on impaired heart tissues in DCM. DCM was induced by streptozotocin (STZ, 60 mg/kg) using Sprague Dawley rats, and diabetic rats were treated with either skimmin (15 or 30 mg/kg) or the vehicle for 16 weeks, and normal rats were used as a control. Hematoxylin and eosin and Masson's trichrome staining were performed to evaluate the cardiac histopathology, and the oxidative stress and proinflammation cytokines in heart tissues were measured. The protein levels of key mediators in fibrosis, pyroptosis, and autophagy in heart tissues were investigated using western blotting. In vitro, primary neonatal cardiomyocytes were treated with skimmin (2 and 10 μM) under stimulation by high glucose (30 mM) and low glucose (5 mM) respectively, and the molecular mechanisms on pyroptosis and autophagy were studied. Compared to the vehicle-treated DCM group, skimmin treatment significantly improved the ejection fraction and fractional shortening of the left ventricle and reduced the oxidative stress by increasing the glutathione level and activity of superoxide dismutase and catalase. Skimmin also reduced cardiac fibrosis, and decreased proinflammation cytokines in cardiac tissues. Mechanism studies showed skimmin may enhance the autophagy and ameliorate NLRP3 inflammasome activation to play a protective role in DCM. This study, for the first time, indicates that skimmin might be a promising lead compound for DCM.
skimmin 是一种天然香豆素衍生物,已被证明可预防实验性糖尿病肾病;然而,其对糖尿病心肌病 (DCM) 的保护作用尚不清楚。本研究通过体外和体内模型,研究了 skimmin 对 DCM 受损心脏组织的保护作用。使用链脲佐菌素 (STZ,60mg/kg) 诱导 DCM ,将糖尿病大鼠用 skimmin(15 或 30mg/kg)或载体处理 16 周,正常大鼠作为对照。使用苏木精和伊红以及 Masson 三色染色评估心脏组织病理学,测量心脏组织中的氧化应激和促炎细胞因子。使用 Western blot 检测心脏组织中纤维化、细胞焦亡和自噬的关键介质的蛋白水平。体外,原代乳鼠心肌细胞分别用 skimmin(2 和 10μM)处理,分别在高葡萄糖(30mM)和低葡萄糖(5mM)刺激下,研究细胞焦亡和自噬的分子机制。与载体处理的 DCM 组相比,skimmin 治疗可显著改善左心室射血分数和缩短分数,并通过增加谷胱甘肽水平以及超氧化物歧化酶和过氧化氢酶的活性来减轻氧化应激。skimmin 还可减轻心脏纤维化,并降低心脏组织中的促炎细胞因子。机制研究表明 skimmin 可能通过增强自噬并改善 NLRP3 炎性小体激活来发挥 DCM 的保护作用。本研究首次表明 skimmin 可能是治疗 DCM 的有前途的先导化合物。