Habtemariam Solomon
Pharmacognosy Research Laboratories, Medway School of Science, University of Greenwich, Chatham Maritime, Kent, ME4 4TB, United Kingdom.
Nat Prod Commun. 2011 Feb;6(2):201-3.
Quercetin, kaempferol and to a lesser extent rutin have been reported to have antidiabetic activities when assessed by various assay models including in vitro alpha-glucosidase inhibition studies. A related structural analogue, kaempferol-3-O-rutinoside (KR) however has not yet been studied for such biological effects. It was found that KR is a potent inhibitor of alpha-glucosidase in vitro with over 8-times more activity than the reference antidiabetic drug, acarbose. Furthermore, KR displayed a synergistic effect with a less potent flavonoid aglycones, kaempferol and quercetin. The structure-activity profile of these drugs and implications of drug combinations are discussed.
据报道,槲皮素、山奈酚以及程度稍低的芦丁,在通过包括体外α-葡萄糖苷酶抑制研究在内的各种检测模型进行评估时,具有抗糖尿病活性。然而,一种相关的结构类似物山奈酚-3-O-芸香糖苷(KR)尚未针对此类生物学效应进行研究。研究发现,KR在体外是一种有效的α-葡萄糖苷酶抑制剂,其活性比参考抗糖尿病药物阿卡波糖高8倍以上。此外,KR与活性稍低的黄酮苷元山奈酚和槲皮素表现出协同效应。本文讨论了这些药物的构效关系以及药物组合的意义。