Renierol from marine sponge Haliclona.SP.: a natural inhibitor of xanthine oxidase with hypouricemic effects.
The purpose of this study was to evaluate the inhibitory effect of renierol, extracted from marine sponge Halicdona.SP., on xanthine oxidase (XO) and its hypouricemic effect in vivo. Renierol and a positive control, allopurinol, were tested for their effects on XO activity by measuring the formation of uric acid and superoxide radical from xanthine. Renierol inhibited XO in a concentration-dependent and competitive manner. IC(50) value was 1.85 microg.ml(-1) through the measuring of uric acid and was 1.36 microg.ml(- 1) through the measuring of superoxide radical. Renierol was found to have an in vivo hypouricemic activity against potassium oxonate-induced hyperuricaemia in mice. After oral administration of renierol at doses of 10, 20 and 30 mg.kg(- 1), there was a significant decrease in the serum urate level (4.08 +/- 0.09 mg.dl(- 1), P < 0.01), (3.47 +/- 0.11 mg.dl(- 1), P < 0.01) and (3.12 +/- 0.08 mg.dl(- 1), P < 0.01), when compared to the hyperuricaemic control (6.74 +/- 0.23 mg.dl(- 1)). Renierol was a potent XO inhibitor with hypouricemic activity in mice.
Department of Biochemistry and Molecular Biology, College of Basic Medical Science, Second Military Medical University, Shanghai, P. R. China.
Guo-Fei
GF
Wang
Yan-Jun
YJ
Shang
Bin-Hua
BH
Jiao
Cai-Guo
CG
Huang
D000818:Animals; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000494:pharmacology; D007546:Isoquinolines / Q000008:administration & dosage / Q000494:pharmacology*; D051379:Mice; D010936:Plant Extracts; D011161:Porifera; D011809:Quinones / Q000008:administration & dosage / Q000494:pharmacology*; D013481:Superoxides / Q000032:analysis; D014527:Uric Acid / Q000032:analysis* / Q000652:urine; D019820:Xanthine / Q000378:metabolism; D014969:Xanthine Oxidase / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D007546:Isoquinolines; D010936:Plant Extracts; D011809:Quinones; C531171:renierol; D013481:Superoxides; D019820:Xanthine; D014527:Uric Acid; D014969:Xanthine Oxidase