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The Gallic Acid–Phospholipid Complex Improved the Antioxidant Potential of Gallic Acid by Enhancing Its Bioavailability

机译:没食子酸-磷脂复合物通过增强其生物利用度提高了没食子酸的抗氧化能力

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摘要

Gallic acid (GA) is well known for its antioxidant and hepatoprotective activity, though its effectiveness is restricted due to rapid metabolism and elimination. To overcome these problems, gallic acid–phospholipid complex was prepared and the effect of phospholipid complexation was investigated on carbon tetrachloride (CCl4)-induced oxidative damage in rat liver. The complex significantly reduced the hepatic marker enzymes in rat serum and restored the antioxidant enzyme levels with respect to CCl4-induced group (P < 0.05 and P < 0.01). Also, the complex improved the pharmacokinetics of GA by increasing the relative bioavailability and elimination half-life. The study therefore suggests that phospholipid complexation has enhanced the therapeutic efficacy of GA which may be due to its improved absorption and increased bioavailability in rat serum.Electronic supplementary materialThe online version of this article (doi:10.1208/s12249-013-9991-8) contains supplementary material, which is available to authorized users.
机译:没食子酸(GA)以其抗氧化剂和保肝活性而闻名,尽管由于快速的代谢和消除作用,其功效受到限制。为克服这些问题,制备了没食子酸-磷脂复合物,并研究了磷脂复合物对四氯化碳(CCl4)诱导的大鼠肝脏氧化损伤的影响。该复合物显着降低了大鼠血清中的肝标志物酶,并且相对于CCl4诱导的组恢复了抗氧化酶水平(P <0.05和P <0.01)。而且,该复合物通过增加相对生物利用度和消除半衰期而改善了GA的药代动力学。因此,这项研究表明磷脂络合物增强了GA的治疗功效,这可能是由于其在大鼠血清中的吸收改善和生物利用度提高所致。电子补充材料本文的在线版本(doi:10.1208 / s12249-013-9991-8)包含补充材料,授权用户可以使用。

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