The Hepatoprotection Study Of Flavonoids And Its Sulfonation On Liver Injury In Mice

Flavonoids are a kind of polyphenols existed in nature, which widely exist in legumes,fruits, vegetables and other food-borne in the form of plants combination (flavonoidglycosides) or flavonoid glycosides. Biochemical and pathological studies have shownthat flavonoids have antioxidation, antitumor, dilate blood vessels, and many otherfunctions. However, flavonoids own poor solubility in water for its special chemicalstructure that seriously influenced their bioavailability. In order to improve the status,people made various attempts, one of the most common used methods is to increase thehydrophilicity of flavonoids by chemical modification.We chose quercetin, baicalein and phloretin for sulfonation modification and got therelevant sulfonation products: sulfonation quercetin, sulfonation baicalein and sulfonationphloretin. The structure of sulfonation derivatives was confirmed using the method ofinfrared spectra, nuclear magnetic resonance hydrogen and carbon spectrum. Quercetin, baicalein, phloretin and their corresponding sulfonation derivatives wereapplied into CCl4/alcohol-induced acute liver injury in mice, with the protection at threedoses of100,200, and500mg/kg in advance. Administration of sulfonation quercetin,sulfonation baicalein and sulfonation phloretin at the dose of500mg/kg, the serum ALTlevels decrease to35.7IU/L,36.8IU/L and39.8IU/L, respectively, without significantdifference compared with the normal index,35.5IU/L. The content of sulfonationquercetin in24-h urine is2.1mg at the dose of500mg/kg,1.0mg more than the quercetin.The content of sulfonation quercetin in24-h feces is2.6mg at the dose of500mg/kg,3.8mg less than the quercetin. Besides, compared with parent drugs group, the state of livercell in the sulfonation derivates groups are better protected, and the number of mutationcell is less. The results indicate that sulfonation derivatives have better hepatoprotectiveeffects and bioavailability than the parent drugs.Sulfonation reaction of quercetin, baicalein and phloretin not only improves itswater-solubility, but also increases the absorbance in the body, providing new approachfor exploitation of medicine.