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艳山姜倍半萜和黄酮类化合物的α-葡萄糖苷酶、醛糖还原酶及糖基化抑制特性研究

Studies on α-glucosidase, aldose reductase and glycation inhibitory properties of sesquiterpenes and flavonoids of Zingiber zerumbet Smith.

作者信息

Ajish K R, Antu K A, Riya M P, Preetharani M R, Raghu K G, Dhanya B P, Radhakrishnan K V

机构信息

a Chemical Sciences & Technology Division, CSIR - National institute for Inderdisciplinary Science and Technology , Thiruvananthapuram 695 019 , Kerala , India.

出版信息

Nat Prod Res. 2015;29(10):947-52. doi: 10.1080/14786419.2014.956741. Epub 2014 Sep 9.

Abstract

Eight known phytochemicals, four sesquiterpenes and four flavonoids of Zingiber zerumbet were screened against α-glucosidase enzyme, aldose reductase enzyme and antiglycation property under in vitro conditions. The results established kaempferol-3-O-methylether as a potent inhibitor of α-glucosidase enzyme with an IC50 value of 7.88 μM. In aldose reductase enzyme inhibition assay, all the compounds except zerumbone epoxide showed good to excellent inhibition properties. Among these, the flavonoid compounds were found to be potent aldose reductase inhibitors compared with the four sesquiterpenes. In addition, compounds such as α-humulene, kaempferol, kaempferol-3-O-methylether and 3″,4″-O-diacetylafzelin displayed potent antiglycation properties. From overall results, we found that kaempferol and kaempferol-3-O-methylether are potent inhibitors of α-glucosidase enzyme, aldose reductase enzyme and glycation reaction, the three main targets of drugs for the treatment of diabetes and its complications.

摘要

在体外条件下,对姜黄的8种已知植物化学物质、4种倍半萜和4种黄酮类化合物进行了α-葡萄糖苷酶、醛糖还原酶和抗糖化特性的筛选。结果表明,山奈酚-3-O-甲基醚是一种有效的α-葡萄糖苷酶抑制剂,IC50值为7.88 μM。在醛糖还原酶抑制试验中,除环氧姜黄酮外,所有化合物均表现出良好至优异的抑制特性。其中,与4种倍半萜相比,黄酮类化合物被发现是有效的醛糖还原酶抑制剂。此外,α-葎草烯、山奈酚、山奈酚-3-O-甲基醚和3″,4″-O-二乙酰阿夫泽林等化合物表现出较强的抗糖化特性。从总体结果来看,我们发现山奈酚和山奈酚-3-O-甲基醚是α-葡萄糖苷酶、醛糖还原酶和糖化反应的有效抑制剂,而这三者是治疗糖尿病及其并发症药物的三个主要靶点。

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