以槲皮素为先导化合物的抗癌剂研究进展

Research progress on anticancer drugs with quercetin as lead compound

槲皮素具有抗氧化、预防心脑血管疾病、化学预防与抗癌作用,但因其生物利用度低、水溶性差、代谢迅速及酶降解等问题,使其作为药物应用于临床受到了限制。对槲皮素的结构进行修饰、改性以获得溶解性好、生物利用度高、代谢稳定和毒副作用小的槲皮素衍生物是目前研究的热点。近10年来,研究者已经合成了大量槲皮素醚类、酯类、金属配合物、C-4羰基氧取代衍生物及A、B环修饰化合物,并进行了体外抗癌活性检测。因此,对近10年合成的具有抗癌活性的槲皮素衍生物进行综述。

Quercetin has the effects of anti-oxidation, prevention of cardiovascular and cerebrovascular diseases, chemical prevention, and anticancer. Because of the low bioavailability, poor water solubility, rapid metabolism, and enzyme degradation, its clinical application is limited. Due to the good solubility, high bioavailability, stable metabolism, and little the poisonous side effects, quercetin derivatives are the hot spots of the study on the modification of quercetin structure. In the last 10 years, researchers have synthesized a large number of quercetin ethers, esters, metal complexes, C-4 carbonyl oxygen substituted derivatives, and A, B ring modified compounds, and the detection of anticancer activity was conducted in vitro. In this paper, the anticancer activity of quercetin derivatives in recent 10 years is reviewed.