Kuppusamy U R, Khoo H E, Das N P
Department of Biochemistry, Faculty of Medicine, National University of Singapore.
Biochem Pharmacol. 1990 Jul 15;40(2):397-401. doi: 10.1016/0006-2952(90)90709-t.
The order of decreasing potency for five most potent flavonoids as inhibitors of hyaluronidase was found to be: condensed tannin less than luteolin less than apigenin less than kaempferol less than silybin. Kinetic studies of these inhibitors showed that their mode of inhibition was competitive. Aglycones were stronger inhibitors than their corresponding glycosides. The following flavonoid structure conferred potent inhibitory effect: a double bond between carbons 2 and 3; unsubstituted hydroxyl groups at positions 5, 7 and 4' and a ketone group at position 4.
研究发现，五种最具活性的黄酮类化合物作为透明质酸酶抑制剂，其活性递减顺序为：缩合单宁＜木犀草素＜芹菜素＜山奈酚＜水飞蓟宾。对这些抑制剂的动力学研究表明，它们的抑制模式为竞争性抑制。苷元比其相应的糖苷是更强的抑制剂。以下黄酮类结构具有强大的抑制作用：碳2和碳3之间有一个双键；5、7和4'位有未取代的羟基，4位有一个酮基。
