JPET Assistant Professor of Medicine (Clinician-Educator)

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
 QUICK SEARCH:   [advanced]


     


Journal of Pharmacology And Experimental Therapeutics Fast Forward
First published on September 16, 2005; DOI: 10.1124/jpet.105.092684


0022-3565/06/3161-169-175$20.00
JPET 316:169-175, 2006
This Article
Right arrow Full Text
Right arrow Full Text (PDF)
Right arrow All Versions of this Article:
jpet.105.092684v1
316/1/169    most recent
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Right arrow Citation Map
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by Yu, Z.
Right arrow Articles by Cheng, C. H. K.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Yu, Z.
Right arrow Articles by Cheng, C. H. K.
Right arrowPubmed/NCBI databases
*Compound via MeSH
*Substance via MeSH
Medline Plus Health Information
*Antioxidants

ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION

The Dual Actions of Morin (3,5,7,2',4'-Pentahydroxyflavone) as a Hypouricemic Agent: Uricosuric Effect and Xanthine Oxidase Inhibitory Activity

Zhifeng Yu, Wing Ping Fong, and Christopher H. K. Cheng

Department of Biochemistry, The Chinese University of Hong Kong, Shatin, Hong Kong, China

Hyperuricemia is associated with a number of pathological conditions such as gout. Lowering of elevated uric acid level in the blood could be achieved by xanthine oxidase inhibitors and inhibitors of renal urate reabsorption. Some natural compounds isolated from herbs used in traditional Chinese medicine have been previously demonstrated to possess xanthine oxidase inhibitory activities. In the present investigation, morin (3,5,7,2',4'-pentahydroxyflavone), which occurs in the twigs of Morus alba L. documented in traditional Chinese medicinal literature to treat conditions akin to gout, was demonstrated to exert potent inhibitory action on urate uptake in rat renal brush-border membrane vesicles, indicating that this compound acts on the kidney to inhibit urate reabsorption. Lineweaver-Burk transformation of the inhibition kinetics data demonstrated that the inhibition of urate uptake was of a competitive type, with a Ki value of 17.4 µM. In addition, morin was also demonstrated to be an inhibitor of xanthine oxidase. Lineweaver-Burk analysis of the enzyme kinetics indicated that the mode of inhibition was of a mixed type, with Ki and Kies values being 7.9 and 35.1 µM, respectively. Using an oxonate-induced hyperuricemic rat model, morin was indeed shown to exhibit an in vivo uricosuric action, which could explain, in part at least, the observed hypouricemic effect of morin in these rats. The potential application of this compound in the treatment of conditions associated with hyperuricemia was discussed.


Received July 15, 2005; accepted September 14, 2005.

Address correspondence to: Dr. Christopher H. K. Cheng, Department of Biochemistry, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong, China. E-mail: chkcheng{at}cuhk.edu.hk




This article has been cited by other articles:


Home page
Drug Metab. Dispos.Home page
Z. Yu, W. P. Fong, and C. H. K. Cheng
Morin (3,5,7,2',4'-Pentahydroxyflavone) Exhibits Potent Inhibitory Actions on Urate Transport by the Human Urate Anion Transporter (hURAT1) Expressed in Human Embryonic Kidney Cells
Drug Metab. Dispos., June 1, 2007; 35(6): 981 - 986.
[Abstract] [Full Text] [PDF]




Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
 Molecular Interventions Drug Metabolism and Disposition

Copyright © 2006 by the American Society for Pharmacology and Experimental Therapeutics.