Acarbose is an oral α-glucosidase inhibitor (IC50 = 11nM), which belongs to the class of oligosaccharide drugs [1]. Acarbose mainly competitively and reversibly inhibits α-glucosidase and pancreatic amylase on the “brush border” of the small intestine, thereby delaying the decomposition of carbohydrates into monosaccharides and slowing down the rapid increase in blood sugar after meals [2-3]. Acarbose is mainly used as an adjuvant treatment for type 2 diabetes [4].
In A7r5 cells, Acarbose (0.5-5μM; 24h, 48h) inhibited the phosphorylation of focal adhesion kinase (FAK) and Akt, activities of the matrix metalloproteinases (MMPs) MMP-2 and MMP-9, and protein expressions of small G proteins (Ras, Cdc42, RhoA, and Rac1) in a dose-dependent manner [5]. In LPS-stimulated THP-1 cells, Acarbose (1μM; 24h) suppressed LPS-induced acetylation of histones H3 (H3) and H4 in the IP-10 and MCP-1 promoter regions [6]. In A7r5 cells, Acarbose (3μM; 24h) reduced diabetes-induced cell migration [7].
In streptozotocin-induced diabetic mice model, Acarbose (50mg/kg; po; 14d) administration by gavage reduced the severity of insulitis and improved insulin levels in the experimental diabetic mice [8]. In aging HET3 mice, Acarbose (1000mg/kg; po; 1200d) improves health and lifespan [9].
References:
[1]. Hanefeld M, Schaper F. Acarbose: oral antidiabetes drug with additional cardiovascular benefits[J]. Expert review of cardiovascular therapy, 2008, 6(2): 153-163.
[2]. Khan F, Khan M V, Kumar A, et al. Recent advances in the development of alpha-glucosidase and alpha-amylase inhibitors in type 2 diabetes management: insights from in silico to in vitro studies[J]. Current Drug Targets, 2024, 25(12): 782-795.
[3]. Bhatnagar A, Mishra A. α-Glucosidase inhibitors for diabetes/blood sugar regulation[M]//Natural products as enzyme inhibitors: An industrial perspective. Singapore: Springer Nature Singapore, 2022: 269-283.
[4]. Chiasson J L, Josse R G, Gomis R, et al. Acarbose for prevention of type 2 diabetes mellitus: the STOP-NIDDM randomised trial[J]. The Lancet, 2002, 359(9323): 2072-2077.
[5]. Yu M H, Lin M C, Huang C N, et al. Acarbose inhibits the proliferation and migration of vascular smooth muscle cells via targeting Ras signaling[J]. Vascular Pharmacology, 2018, 103: 8-15.
[6]. Lin Y C, Chen Y C, Hsiao H P, et al. The effects of acarbose on chemokine and cytokine production in human monocytic THP-1 cells[J]. Hormones, 2019, 18(2): 179-187.
[7]. Chuang W Y, Yu M H, Yang T Y, et al. Acarbose attenuates migration/proliferation via targeting microRNA-143 in vascular smooth muscle cells under diabetic conditions[J]. Journal of Food and Drug Analysis, 2020, 28(3): 461.
[8]. Zhao B, Wu F, Han X, et al. Protective effects of acarbose against insulitis in multiple low-dose streptozotocin-induced diabetic mice[J]. Life Sciences, 2020, 263: 118490.
[9]. Harrison D E, Strong R, Alavez S, et al. Acarbose improves health and lifespan in aging HET3 mice[J]. Aging cell, 2019, 18(2): e12898.
Acarbose是一种口服α-葡萄糖苷酶抑制剂（IC50 = 11nM），属于寡糖类药物 [1]。Acarbose主要竞争性地可逆性地抑制小肠“刷状缘”上的α-葡萄糖苷酶和胰淀粉酶，从而延缓碳水化合物分解为单糖，减缓餐后血糖的快速升高 [2-3]。Acarbose主要用于2型糖尿病的辅助治疗 [4]。
在A7r5细胞中，Acarbose（0.5-5μM；24h，48h）以剂量依赖性方式抑制黏着斑激酶（FAK）和Akt的磷酸化、基质金属蛋白酶（MMPs）MMP-2和MMP-9的活性以及小G蛋白（Ras、Cdc42、RhoA和Rac1）的蛋白表达 [5]。在LPS刺激的THP-1细胞中，Acarbose（1μM；24h）可抑制LPS诱导的IP-10和MCP-1启动子区组蛋白H3（H3）和H4的乙酰化 [6]。在A7r5细胞中，Acarbose（3μM；24h）可降低糖尿病诱导的细胞迁移 [7]。
在链脲佐菌素诱发的糖尿病小鼠模型中，通过管饲法给予Acarbose（50mg/kg；po；14d）可减轻实验性糖尿病小鼠的胰岛炎严重程度，并改善其胰岛素水平 [8]。在衰老的HET3小鼠中，Acarbose（1000mg/kg；po；1200d）可改善其健康和寿命 [9]。