槲皮素在化学预防多种致癌物和诱变物中的作用

S. Shivakumar, Yasodha Lakshmi Tadakaluru, Raja Ratna Reddy Yakkanti, S. Suresh, P. C. Sekhar
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引用次数: 1

摘要

槲皮素是一种普遍存在的植物类黄酮,具有重要的药理和临床活性。在这项研究中,我们决定通过不同的机制在体外和体内研究中证明槲皮素对一系列诱变剂和致癌物质的保护作用。槲皮素对叠氮化钠、苯并(a)芘、一水环磷酰胺、甲烷磺酸甲酯和叶黄醇具有显著的抗诱变作用。槲皮素在体外和体内试验条件下都有效,在存在和不存在代谢激活系统的情况下也有效(大鼠肝脏S9)。槲皮素的自氧化、抗氧化特性、通过CYP1A活性抑制促诱变剂代谢以及多种抗诱变和适应性反应等机制可能解释了槲皮素在癌症预防中的保护作用。综上所述,槲皮素对直接结合DNA(形成DNA加合物)的诱变剂、促诱变剂和产生自由基的烷基化剂具有显著的抑制作用;这可能是其对特定癌症类型有效的抗癌活性的基本原理。
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Role of Quercetin in chemoprevention against wide range of carcinogens and mutagens
Quercetin is a ubiquitous plant flavoniod with significant pharmacological and clinical activity. In this study we determined to demonstrate the protective role of quercetin against range of mutagens and carcinogens in a combination of in vitro and in vivo studies via different mechanisms. Quercetin demonstrated significant protective role against sodium azide, benzo(a)pyrene, cyclophosphamide monohydrate, methyl methane sulphonate and etoposide compared to other mutagens. Quercetin is effective in both in vitro and in vivo test conditions and also in the presence as well as in the absence of metabolic activation system (Rat liver S9).  Auto oxidation, antioxidant properties, inhibition of pro-mutagens metabolism by CYP1A activity and multiple antimutagenic and adaptive response, mechanisms of quercetin may account for its protective role in cancer prevention. In conclusion, the results clearly indicate that quercetin plays a significant role against mutagens that act by direct DNA binding (form DNA adducts), pro-mutagens and alkylating agents with free radical generation; which could be the rationale for its potent anticancer activity against particular cancer types.
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