Ben Hmidene Asma, Hanaki Mizuho, Murakami Kazuma, Irie Kazuhiro, Isoda Hiroko, Shigemori Hideyuki
Graduate School of Life and Environmental Sciences, University of Tsukuba.
Biol Pharm Bull. 2017;40(2):238-241. doi: 10.1248/bpb.b16-00801.
The prevention of amyloid aggregation is promising for the treatment of age-related diseases such as Alzheimer's (AD) and type 2 diabetes (T2D). Ten antioxidant flavonoids isolated from the medicinal halophyte Tamarix gallica were tested for their amyloid aggregation inhibition potential. Glucuronosylated flavonoids show relatively strong inhibitory activity of Amyloid β (Aβ) and human islet amyloid polypeptide (hIAPP) aggregation compared to their aglycone analogs. Structure-activity relationship of the flavonoids suggests that the catechol moiety is important for amyloid aggregation inhibition, while the methylation of the carboxyl group in the glucuronide moiety and of the hydroxyl group in the aglycone flavonoids decreased it.
预防淀粉样蛋白聚集对于治疗诸如阿尔茨海默病（AD）和2型糖尿病（T2D）等与年龄相关的疾病具有广阔前景。对从药用盐生植物柽柳中分离出的10种抗氧化黄酮类化合物的淀粉样蛋白聚集抑制潜力进行了测试。与它们的苷元类似物相比，糖基化黄酮类化合物对淀粉样β蛋白（Aβ）和人胰岛淀粉样多肽（hIAPP）聚集表现出相对较强的抑制活性。黄酮类化合物的构效关系表明，邻苯二酚部分对于淀粉样蛋白聚集抑制很重要，而糖醛酸部分中的羧基和苷元黄酮类化合物中的羟基甲基化会降低这种抑制作用。
