Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-11-02 , DOI: 10.1016/j.bmcl.2020.127665 Yin-Sheng Quan 1 , Xiao-Yong Zhang 2 , Xiu-Mei Yin 1 , Si-Hong Wang 2 , Li-Li Jin 1
In light of the adequate sources for Hylotelephium erythrostictum, its active components have aroused research interest. 2-(3′,4′-dihydroxyphenyl)-2,3-dihydro-4,6-dihydroxy-2-(methoxy)- 3-benzofuranone(1), apigenin(2), diosmetin(3), kaempferol(4), kaempferide(5), rhamnocitrin(6), quercetin(7), and gallic acid(8) were isolated from H. erythrostictum. Rarely occurring naturally, 1 is 2-methoxybenzofuranone type compound against α-glucosidase and exhibits a potential inhibitory effect on α-glucosidase(IC50 = 1.8 μM), with a Ki value of 709 nM. In silico molecular docking was performed for the investigation of the inhibition mechanism. H. erythrostictum is a potential source of antidiabetic agent. This information is useful in finding more potent antidiabetic candidates from medicinal plants for the clinical development of therapeutics.
中文翻译:
潜在的红球菌的α-葡萄糖苷酶抑制剂
在光线的来源充足八宝属erythrostictum,其活性成分已引起研究兴趣。2-(3',4'-二羟基苯基)-2,3-二氢-4,6-二羟基-2-(甲氧基)-3-苯并呋喃酮(1),芹菜素(2),薯os(3),山奈酚(4)),山奈(5),鼠李柠檬素(6),槲皮素(7),和没食子酸(8)从分离H. erythrostictum。很少天然存在的,1是针对α葡糖苷酶2- methoxybenzofuranone型化合物并表现出对α葡萄糖苷酶的电位的抑制作用(IC 50 = 1.8μM),具有K i值为709 nM。在计算机上进行了分子对接以研究抑制机理。红血球菌是抗糖尿病药的潜在来源。该信息可用于从药用植物中找到更有效的抗糖尿病药物,用于治疗药物的临床开发。