首页|钠-葡萄糖共转运蛋白2抑制剂在心血管疾病中的抗炎作用及机制

钠-葡萄糖共转运蛋白2抑制剂在心血管疾病中的抗炎作用及机制

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钠-葡萄糖共转运蛋白(SGLT)-2抑制剂是一类新型口服降血糖药,主要通过抑制肾脏近端小管葡萄糖的重吸收,促进尿糖排泄,降低血糖。大量临床研究发现SGLT-2抑制剂具有良好的心血管保护作用。同时,众多基础研究发现多种SGLT-2抑制剂在细胞及动物模型中表现出良好的抗炎活性,SGLT-2抑制剂的心血管保护机制可能与抑制炎症反应密切相关。如卡格列净通过提高AMP活化蛋白激酶(AMPK)、内皮型一氧化氮合酶(eNOS)等抗炎信号传导抑制炎症反应;达格列净可显著降低白细胞介素(IL)-1β、IL-6及肿瘤坏死因子(TNF)-α等炎症因子的表达,促进巨噬细胞向抗炎表型的极化;恩格列净可以减少糖尿病心肌病、高血压和心力衰竭模型中的心脏炎症。
Anti-inflammatory effects and mechanisms of sodium-glucose cotransporter 2 inhibitors in cardiovascular diseases
Sodium-glucose cotransporter 2(SGLT-2)inhibitors comprise a new class of oral hypoglycemic agents that promote the excretion of urine sugar and reduce blood sugar mainly by inhibiting the reabsorption of glucose in proximal renal tubules.Numerous clinical studies have found that SGLT-2 inhibitors have good effects on cardiovascular system.At the same time,many basic studies have found that a variety of SGLT-2 inhibitors exhibit anti-inflammatory activity in both cellular and animal models,and the cardiovascular protective mechanism may be closely related to inhibiting inflammatory response.For example,canagliflozin inhibits inflammatory response by enhancing anti-inflammatory signaling pathways such as AMP activated protein kinase(AMPK)and endothelial nitric oxide synthase(eNOS).Dapagliflozin significantly reduces t he expression of inflammatory factors such as interleukin(IL)-1β,IL-6,and tumor necrosis factor(TNF)-α,and promotes the polarization of macrophages towards anti-inflammatory phenotype.Empagliflozin reduces cardiac inflammation in diabetes cardiomyopathy,hypertension,and heart failure models.

sodium-glucose cotransporter 2 inhibitorcardiovascular systeminflammatorymolecular mechanisms of pharmacological action

王悦、李冰清、陈余文、李文倩、万少枝、李册兴、孙培媛、吕建峰

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三峡大学附属仁和医院心血管内科,湖北宜昌 443000

钠-葡萄糖共转运蛋白2抑制剂 心血管系统 炎症 药理作用分子作用机制

湖北省卫生健康委科研项目湖北省卫生健康委中医药科研立项项目

WJ2021F061ZY2021F018

2024

中国新药与临床杂志
中国药学会 上海市食品药品监督管理局科技情报研究所

中国新药与临床杂志

CSTPCD北大核心
影响因子:0.967
ISSN:1007-7669
年,卷(期):2024.43(3)
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