Molecules 2014, 19(1), 291-305; doi:10.3390/molecules19010291
Article

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

1, 1, 2, 2 and 1,* email
Received: 22 November 2013; in revised form: 5 December 2013 / Accepted: 12 December 2013 / Published: 27 December 2013
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract: 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.
Keywords: quercetin; quercetin-5',8-disulfonate; hepatoprotective effects; HPLC; absorption
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MDPI and ACS Style

Cui, Y.; Han, Y.; Yang, X.; Sun, Y.; Zhao, Y. Protective Effects of Quercetin and Quercetin-5',8-Disulfonate against Carbon Tetrachloride-Caused Oxidative Liver Injury in Mice. Molecules 2014, 19, 291-305.

AMA Style

Cui Y, Han Y, Yang X, Sun Y, Zhao Y. Protective Effects of Quercetin and Quercetin-5',8-Disulfonate against Carbon Tetrachloride-Caused Oxidative Liver Injury in Mice. Molecules. 2014; 19(1):291-305.

Chicago/Turabian Style

Cui, Yanmang; Han, Yong; Yang, Xingbin; Sun, Yanfei; Zhao, Yan. 2014. "Protective Effects of Quercetin and Quercetin-5',8-Disulfonate against Carbon Tetrachloride-Caused Oxidative Liver Injury in Mice." Molecules 19, no. 1: 291-305.

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