生物活性

• 描述α-glucosidases are enzymes responsible for the metabolism of complex carbohydrates into absorbable monosaccharide units. However, hyperglycemia causes a number of abnormalities which contribute to the development of long-term complications of diabetes. Acarbose, an anti-diabetic drug, is an intestinal α-glucosidase inhibitor^[3]. In TNF-α pre-treated A7r5 cells, acarbose (1, 2, and 3 μM) dose-dependently decreased β-galactosidase, Ras expression and increased p-AMPK expression. In HCD (high cholesterol diet)-fed rabbits, the numbers of atherosclerotic plaques in the aortic arch were significantly decreased by acarbose treatment (2.5 and 5.0 mg/kg per day). Further, acarbose (2.5 and 5.0 mg/kg) significantly and dose-dependently decreased the intensity of neointimal IL-6, TNF-α, and iNOS staining, and significantly increased the intensity of neointimal p-AMPK staining. Moreover, acarbose (2.5 and 5.0 mg/kg) significantly and dose-dependently decreased neointimal Ras and β-galactosidase expression in HCD-fed rabbits^[4].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02476760	-	-	Completed	-	Canada, Quebec ... more >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 Collapse <<
  NCT02475499	-	-	Completed	-	Canada, Quebec ... more >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 Collapse <<
  NCT00000620	Atherosclerosis ... more >> Cardiovascular Diseases Hypercholesterolemia Hypertension Diabetes Mellitus, Type 2 Diabetes Mellitus Coronary Disease Collapse <<	Phase 3	Completed	-	United States, Minnesota ... more >> Minneapolis Medical Research Foundation Minneapolis, Minnesota, United States, 55404 United States, New York Columbia University New York, New York, United States, 10027 United States, North Carolina Wake Forest University Winston-Salem, North Carolina, United States, 27106 United States, Ohio Case Western Reserve University Cleveland, Ohio, United States, 44106 United States, Tennessee Veterans Affairs Memphis, Tennessee, United States, 38104 United States, Washington University of Washington Seattle, Washington, United States, 98195 Canada, Ontario McMaster University Hamilton, Ontario, Canada Collapse <<

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• 参考文献

• [1] Okada K, Yanagawa T, et al. The alpha-glucosidase inhibitor acarbose prevents obesity and simple steatosis in sequestosome 1/A170/p62 deficient mice. Hepatol Res. 2009 May;39(5):490-500.

  [2] Wang PY, Kaneko T, et al. Acarbose alone or in combination with ethanol potentiates the hepatotoxicity of carbon tetrachloride and acetaminophen in rats. Hepatology. 1999 Jan;29(1):161-5.

  [3] Martin AE, Montgomery PA. Acarbose: an alpha-glucosidase inhibitor. Am J Health Syst Pharm. 1996 Oct 1;53(19):2277-90

  [4] Chan KC, Yu MH, Lin MC, Huang CN, Chung DJ, Lee YJ, Wu CH, Wang CJ. Pleiotropic effects of acarbose on atherosclerosis development in rabbits are mediated via upregulating AMPK signals. Sci Rep. 2016 Dec 7;6:38642