Effects of Apigenin Mannich Base Derivative in Celery Seed on Anti-Hyperurimia Activities
In order to study anti-hyperuricemic effect and mechanism of apigenin mannich base derivative isolated from celery seed.The hyperuricemic mice model were induced by an intraperitoneal injection of uricase inhibitor potassium oxonate.APN083,a apigenin deriva-tive,8-(4-Ethyl-piperazin-l-methyl)-5,7-dihydroxy-2-(4-hydroxy-phenyl)-benzo-4-ketone,was synthesized and anti-hyperuricemic effect of APN083 were determined in hyperuricemic mice.The potential inhibition mechanism of the compound on XO were researched by using the methods of molecular simulation technology.Results:indicuted that compared with the model group,serum uric acid levels and CRE levels in vivo were decreased significantly in groups received APN083 at the doses of 15,7.5 mg/kg(P＜0.05).In vitro inhibition experi-ments showed that APN083 had a moderate inhibitory effect on XO enzyme.The result of molecular docking confirmed that the compound bound to the active cavity of XO,interacting with some amino acid residues,plugging the cavity and finally inhibiting the activity of XO.Apigenin mannich base derivative APN083 could reduce the level of serum uric acid and had a moderate inhibitory effect on XO enzyme.
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