Liu Ming, Yin Hua, Liu Ge, Dong Jianjun, Qian Zhonghua, Miao Jinlai
Key Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China , Qingdao 266003, China.
J Agric Food Chem. 2014 Jun 18;62(24):5548-54. doi: 10.1021/jf500426z. Epub 2014 Jun 4.
Xanthohumol (XN) is a unique prenylated flavonoid in hops (Humulus lupulus L.) and beer. XN alleviates hyperglycemia and has potential usage in the treatment of type 2 diabetes. In the present study, a series of in vitro experiments were performed to investigate whether XN was an effective inhibitor of α-glucosidase. The results showed that XN inhibited α-glucosidase in a reversible and noncompetitive manner, with an IC50 value of 8.8 μM and that XN inhibited the release of glucose from the maltose in the apical side of the Caco-2 cell monolayer. Fluorescence and circular dichroism spectra results indicated that XN directly bound to α-glucosidase and induced minor conformational changes of the enzyme. These results demonstrated that XN is a promising α-glucosidase inhibitor, which therefore could be used as functional food to alleviate postprandial hyperglycemia and as a potential candidate for the development of an antidiabetic agent.
黄腐酚（XN）是啤酒花（Humulus lupulus L.）和啤酒中一种独特的异戊烯基化黄酮类化合物。XN可缓解高血糖，在2型糖尿病治疗中具有潜在用途。在本研究中，进行了一系列体外实验，以研究XN是否为α-葡萄糖苷酶的有效抑制剂。结果表明，XN以可逆和非竞争性方式抑制α-葡萄糖苷酶，IC50值为8.8 μM，且XN抑制了Caco-2细胞单层顶端侧麦芽糖释放葡萄糖。荧光和圆二色光谱结果表明，XN直接与α-葡萄糖苷酶结合，并引起该酶的微小构象变化。这些结果表明，XN是一种有前景的α-葡萄糖苷酶抑制剂，因此可作为功能性食品来缓解餐后高血糖，并作为开发抗糖尿病药物的潜在候选物。
