Heo M Y, Yu K S, Kim K H, Kim H P, Au W W
College of Pharmacy, Kangweon National University, Chuncheon, South Korea.
Mutat Res. 1992 Dec 16;284(2):243-9. doi: 10.1016/0027-5107(92)90008-p.
14 flavonoids, including flavone and flavonol derivatives, were tested for their anticlastogenic effect against induction of micronuclei by benzo[a]pyrene in polychromatic erythrocytes of mice. When each flavonoid was administered orally, together with intraperitoneally administered benzo[a]pyrene, most flavonol derivatives showed an anticlastogenic effect. The data suggest that the 2,3-double bond and 3,5,7-hydroxyl groups in the flavonoid molecules may be essential to produce anticlastogenic effects against benzo[a]pyrene. Galangin, one of the active compounds, and (-)-epicatechin, a weak one, were administered to mice in order to compare their anticlastogenic effect against 3 different kinds of carcinogens: ethyl methanesulfonate, 7,12-dimethylbenz[a]anthracene, and adriamycin. Galangin showed a stronger anticlastogenic effect than (-)-epicatechin against ethyl methanesulfonate and 7,12-dimethylbenz[a]anthracene. However, there was no significant effect against adriamycin-induced micronuclei by both compounds. Our study indicates that most flavonoids are anticlastogenic agents. Their anticlastogenic effects are apparently independent of their own clastogenic activities. Furthermore, their anticlastogenic activities do not apply universally to all types of genotoxic chemicals.
对14种黄酮类化合物(包括黄酮和黄酮醇衍生物)进行了测试,以研究它们对苯并[a]芘在小鼠多染性红细胞中诱导微核的抗断裂作用。当每种黄酮类化合物与腹腔注射的苯并[a]芘一起口服给药时,大多数黄酮醇衍生物都显示出抗断裂作用。数据表明,黄酮类分子中的2,3-双键和3,5,7-羟基可能是产生抗苯并[a]芘断裂作用的关键。为了比较它们对3种不同致癌物(甲磺酸乙酯、7,12-二甲基苯并[a]蒽和阿霉素)的抗断裂作用,将活性化合物之一高良姜素和较弱的(-)-表儿茶素给小鼠给药。高良姜素对甲磺酸乙酯和7,12-二甲基苯并[a]蒽的抗断裂作用比(-)-表儿茶素更强。然而,两种化合物对阿霉素诱导的微核均无显著作用。我们的研究表明,大多数黄酮类化合物是抗断裂剂。它们的抗断裂作用显然与其自身的断裂活性无关。此外,它们的抗断裂活性并不普遍适用于所有类型的遗传毒性化学物质。