论文部分内容阅读
目的:研究12种天然黄酮类化合物清除羟自由基(OH)的构效关系.方法:使用产生并能灵敏检测OH的抗坏血酸-CuSO_(4-)酵母-H_2O_2 的化学发光体系.结果:槲皮素、泽漆新苷、金丝桃苷、山奈素、黄芩苷、补骨脂甲素、石吊兰素、映山红素、补骨脂乙素和染料术素能有效地清除OH,抑制体系化学发光,它们的半数抑制浓度(IC_(50))值(95％可信限)分别是:12.1(9.9-14.5)g/L,15.8(14.0-19.2)g/L,19.5(16.8-27.4)g/L,20.1(13.6-29.0)g/L,34.6(28.4-43.4)g/L,66.8(63.2-74.4)g/L,187(14-235)g/L,211(165-284)g/L,262 (190-346)g/L和708(498-994)g/L,而川陈和补甲-Ac则无效.结论:(1)黄酮类酚羟基是清除OH的主要活性基团;(2)B环上羟基和A环上羟基都是清除OH的重要活性基团;(3)位于A环和/或B环上的邻二羟基能大大提高相应环的清除OH活性;(4)对槲皮素、泽漆新苷、金丝桃苷、黄芩苷、石 吊兰素和映山红素的IC_(50)值进行比较,发现它们的B环3’,4’位上的羟基具有高清除OH活性;它们的B环上羟基清除活性高于A环上羟基;它们的C环3位上的羟基或糖苷与清除OH的能力也有相关性;(5)黄酮类化合物的种类也影响其清除OH活性.
Objective: To study the structure-activity relationship of 12 natural flavonoids scavenging hydroxyl radical (OH) .Methods: The chemiluminescence system of ascorbic acid-CuSO_ (4-) Yeast-H_2O_2 was established and sensitive detection of OH.Results: Hypericin, zeaxanthin, hyperoside, kaempferol, baicalin, psoralen, trapididin, rehmannia, psoralen and dyestuff effectively remove OH and inhibit the chemiluminescence of the system , And their IC50 values (95% confidence limits) were 12.1 (9.9-14.5) g / L, 15.8 (14.0-19.2) g / L and 19.5 (16.8-27.4) g /L.20.1(13.6-29.0)g/L,34.6(28.4-43.4)g/L,66.8(63.2-74.4)g/L,187(14-235)g/L,211(165-284)g / L, 262 (190-346) g / L and 708 (498-994) g / L respectively, while Chuan Chen and Bu Jia-Ac were not effective.Conclusion: (1) Flavonoid phenolic hydroxyl is the main active group (2) the hydroxyl groups on ring B and the hydroxyl groups on ring A are all the important active groups for scavenging OH; (3) the ortho-dihydroxy groups on ring A and / or ring B can greatly enhance the scavenging OH activity of the corresponding ring; (4) IC_ (50) values of quercetin, zeaxanthin, hyperin, baicalin, spain and azin were compared and found that their B ring 3 , The hydroxyl groups on the 4 ’position have high OH scavenging activity; the hydroxyl scavenging activity on the B ring is higher than the hydroxyl group on the A ring; the hydroxyl group or glycoside at the 3 position of C ring is also related to the ability to scavenge OH; ) The type of flavonoids also affects their ability to scavenge OH.