Journal
FREE RADICAL BIOLOGY AND MEDICINE
Volume 110, Issue -, Pages 399-407Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.freeradbiomed.2017.06.020
Keywords
Malaxinic acid; Malaxinic acid aglycone; Metabolite; Malaxinic acid glucuronate; Rat; Absorption; Pharmacokinetics; Antioxidative activity; Blood plasma
Funding
- Korea Institute of Planning and Evaluation for Technology in Food, Agriculture, Forestry and Fisheries (IPET) through the High Value-Added Food Technology Development Program - Ministry of Agriculture, Food and Rural Affairs (MAFRA) [315069-3]
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Malaxinic acid (MA) is a phenolic acid compound, found mainly in pear fruits (Pyrus pyrifolia N.), that is isoprenylated on the C-3 position of benzoic acid. Recently, the effects of prenylated phenolics on health have received much interest owing to their reported potent beneficial biological effects. We conducted a comparative study in rats to determine the metabolism, pharmacokinetics, and antioxidative activities of MA and its corresponding aglycone (MAA). MA and MAA were orally administered to rats (Sprague-Dawley, male, 6 weeks old) and their metabolites in plasma were analyzed. In addition, the MA metabolites in plasma were separated and the structures were confirmed via NMR and HR-MS analyses. The antioxidative activities of MA and MAA were evaluated by measuring their inhibitory effects on the 2,2'-azobis(2-amidinopropane) dihydrochloride- or copper ion-induced lipid peroxidation of rat plasma. MA was not absorbed in the intact form (the glucoside); both MA and MAA were absorbed as MAA and its metabolite form (glucuronide or sulfate). Moreover, the observed metabolite was the glucuronate of MAA rather than the glucuronide or sulfate. Concentrations of the free form of aglycone (MA administration, 4.6 +/- 2.2 mu M; MAA administration, 7.2 +/- 2.3 mu M) and total MAA (MA administration, 19.6 +/- 4.4 mu M; MAA administration, 21.7 +/- 3.3 mu M) in plasma reached a maximum at 15 min after the oral administration of MA and MAA, respectively. The relative inhibitory effects on the formation of cholesteryl ester hydroperoxides in plasma collected at 15 min after the oral administration of MA, MAA, and p-hydroxybenzoic acid (p-HBA) were as follows: MAA > MA >= p-HBA > control. Although the majority of MA and MAA is metabolized to conjugates, the compounds may contribute to the antioxidant defenses in the blood circulation owing to the presence of a phenolic hydroxyl group in the free form.
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