Protective Effects of Quercetin and Quercetin-5',8-Disulfonate against Carbon Tetrachloride-Caused Oxidative Liver Injury in Mice

Molecules

Yanmang Cui¹  Yong Han¹  Xingbin Yang²  Yanfei Sun² 

[1] School of Pharmacy, Fourth Military Medical University, Xi’an 710032, China;College of Food Engineering and Nutritional Science, Shaanxi Normal University, Xi’an 710062, China

关键词: quercetin;    quercetin-5';    8-disulfonate;    hepatoprotective effects;    HPLC;    absorption;   

DOI  :  10.3390/molecules19010291

来源: mdpi

【 摘 要 】

Oxidative stress is one of the major factors in the pathogenesis of liver disease. Quercetin is a plant-based antioxidant traditionally used as a treatment for hepatic injury, but its poor solubility affects its bioavailability. We here report the regulative effects on hepatoprotection and absorption in mice of quercetin sulfation to form quercetin-5',8-disulfonate (QS), a novel synthetic compound. Oral administration of both QS and the parent quercetin at 100, 200 and 500 mg/kg·bw prior to acute CCl₄ oxidative damage in mice, effectively attenuated serum alanine aminotransferase (ALT), aspartate aminotransferase (AST) and lactate dehydrogenase (LDH) activities and hepatic malondialdehyde (MDA) levels (p < 0.05), and suppressed the CCl₄-induced depletion of glutathione peroxidase (GSH-Px) and total superoxide dismutase (T-SOD). Selective 5',8-sulfation of quercetin increased the hepatoprotective effect, and its relative absorption relative to quercetin (p < 0.05) as indicated by an improved 24-hour urinary excretion and a decreased fecal excretion determined by HPLC. These results and histopathological observations collectively demonstrate that quercetin sulfation increases its hepatoprotective effects and absorption in mice, and QS has potential as a chemopreventive and chemotherapeutic agent for liver diseases.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.