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熊果酸对正常的和多种糖尿病模型动物具有降血糖作用。熊果酸是:(1)通过抗氧化和调节免疫功能,保护β-细胞和刺激胰岛素表达和分泌;(2)通过抑制蛋白酪氨酸磷酸酶1B(PTP1B)表达和活性,和Ι型11β-羟基甾体脱氢酶(11β-HSD1)活性以及促进过氧化物酶体增殖子激活型受体-α(PPAR-α)的表达和激活,对抗胰岛素抵抗,促进组织细胞摄取和利用葡萄糖,改善脂、糖代谢紊乱;(3)通过抑制α-葡萄糖苷酶活性,延缓肠道吸收葡萄糖,产生降血糖作用。综述熊果酸降血糖药理作用及其机制的文献,对其研究进展作了分析,为抗代谢综合征新药的研发提供参考。
Ursolic acid has a hypoglycemic effect on normal and various diabetic animal models. Ursolic acid is: (1) protects β-cells and stimulates insulin expression and secretion through anti-oxidant and modulatory immune functions; (2) inhibits expression and activity of protein tyrosine phosphatase 1B (PTP1B) - hydroxysteroid dehydrogenase (11β-HSD1) activity as well as promote the expression and activation of peroxisome proliferator-activated receptor-α (PPAR-α), resist insulin resistance, promote tissue cell uptake and utilization of glucose, Improve lipid, glucose metabolism disorders; (3) by inhibiting α-glucosidase activity, delay intestinal absorption of glucose, hypoglycemic effect. The literature summarizing the hypoglycemic pharmacological effects of ursolic acid and its mechanism, and the progress of its research were analyzed to provide reference for the development of new anti-metabolic syndrome drugs.