College of Pharmacy, Yanbian University, Yanji 133002, PR China.
Analysis and Inspection Center, Yanbian University, Yanji 133002, PR China.
Bioorg Med Chem Lett. 2020 Dec 15;30(24):127665. doi: 10.1016/j.bmcl.2020.127665. Epub 2020 Nov 2.
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(IC = 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.
鉴于红景天有充足的来源,其活性成分引起了研究兴趣。从红景天中分离得到了 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)、香叶木素(3)、山柰酚(4)、山柰酚-3-O-葡萄糖苷(5)、鼠李柠檬素(6)、槲皮素(7)和没食子酸(8)。1 是一种罕见的天然存在的 2-甲氧基苯并呋喃酮类化合物,对α-葡萄糖苷酶具有潜在的抑制作用,对α-葡萄糖苷酶的抑制活性(IC=1.8μM),Ki 值为 709nM。通过计算机分子对接研究了抑制机制。红景天是一种有潜力的抗糖尿病药物来源。这一信息有助于从药用植物中寻找更有效的抗糖尿病候选药物,为治疗学的临床发展提供帮助。