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出 处:《华西药学杂志》2016年第4期374-377,共4页West China Journal of Pharmaceutical Sciences
摘 要:目的比较虎杖中白藜芦醇、3,4'-二甲基化白藜芦醇、3,5,4'-三甲基白藜芦醇对高脂饲养小鼠动脉粥样硬化作用的影响。方法小鼠用高脂饲料喂养8周,从第5周开始,给予白藜芦醇组、3,4'-二甲基化白藜芦醇组、3,5,4'-三甲基白藜芦醇组单日单剂量30 mg·kg^(-1),阳性对照组10 mg·kg^(-1)辛伐他丁,通过测定小鼠血清中一系列参数来判断白藜芦醇及其甲基化衍生物在降血脂和抗氧化方面的效果。结果白藜芦醇及其甲基化衍生物均能显著降低小鼠血清中TG、TC、LDL-C、oxLDL、MDA的含量(P<0.05或P<0.01),提高血清中NO、HDL-C的浓度(P<0.01),并增强SOD酶的活力(P<0.01);3,5,4'-三甲基白藜芦醇还可以可显著提高血清中CAT的活性(P<0.01),白藜芦醇两个甲基化产物可降低LDL-C、升高HDLC,增强CAT酶的活力与白藜芦醇比较,显著增强(P<0.01)。结论白藜芦醇及其甲基化衍生物均能有效地降低高脂症小鼠动脉粥样硬化的风险,且白藜芦醇甲基化衍生物可能有更显著的效果,这可能与其增加生物利用度和延长半衰期有关。OBJECTIVE To compare the anti - atherosclerotic effect of resveratrol from Polygonurn cuspidatum and its methylated derivatives on hyperlipidemia mice. METHODS Mice were fed with high - fat diet for 8 weeks and administered a single dose of resveratrol,3,4' - dimethoxy trans - stilbene and 3,5,4' - trimethoxy - trans - stilbene (TMS) ( 30 mg·kg^-1 ) a day from the 5th week,with Simvastatin( 10 mg·kg^-1) as a positive control. Anti -hyperIipidemia and antioxidant effects were determined by a series mice serum indicators. RESULTS Resveratrol and its methylated derivatives could significantly reduce the contents of TG, TC, LDL - C, ox - LDL, MDA ( P 〈 0.05 or P 〈 0.01 ) , increase NO, HDL - C ( P 〈 0.01 ) and enhance SOD ( P 〈 0.01 ) activities in the serum of hypercholesterolemic mice. TMS could also significantly increase the CAT activity( P 〈 0.01 ). Compared with resveratrol, its methylated derivatives could significantly increase the effect on reducing LDL - C, increasing HDL - C and enhancing CAT enzyme activity. CONCLUSION Resveratrol and its methylated derivatives can effectively reduce in atherosclerotic disease risk hypercholesterolemic mice, and methylated derivatives of resveratrol may have more significant effect, which can be related to the possibility that the trimethylated resveratrol acts like a prodrug, prolonging, probably, the half - life of the original compound.
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