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3,5,2',4'-Tetrahydroxychalcone, a new non-purine xanthine oxidase inhibitor.
Chem Biol Interact. 2011 Feb 01; 189(3):161-6.CB

Abstract

Xanthine oxidase is a key enzyme that catalyses hypoxanthine and xanthine to uric acid and the overproduction of uric acid will lead to hyperuricemia which is an important cause of gout. In the present study, three chalcone derivatives were synthesized and evaluated for inhibitory activity against xanthine oxidase in vitro. Of the compounds, only Compound 1, 3,5,2',4'-tetrahydroxychalcone, exhibited a significant inhibitory activity on xanthine oxidase with an IC(50) value of 22.5 μM. Lineweaver-Burk transformation of the inhibition kinetics data demonstrated that it was a competitive inhibitor of xanthine oxidase and Ki value was 17.4 μM. In vivo, intragastric administration of Compound 1 was able to significantly reduce serum uric acid levels and inhibited hepatic xanthine oxidase activities of hyperuricemic mice in a dose-dependent manner. Acute toxicity study in mice showed that Compound 1 was very safe at a dose of up to 5 g/kg. These results suggest that Compound 1 is a novel competitive xanthine oxidase inhibitor and is worthy of further development.

Authors+Show Affiliations

Kunming Medical University, PR China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

21167141

Citation

Niu, Yanfen, et al. "3,5,2',4'-Tetrahydroxychalcone, a New Non-purine Xanthine Oxidase Inhibitor." Chemico-biological Interactions, vol. 189, no. 3, 2011, pp. 161-6.
Niu Y, Zhu H, Liu J, et al. 3,5,2',4'-Tetrahydroxychalcone, a new non-purine xanthine oxidase inhibitor. Chem Biol Interact. 2011;189(3):161-6.
Niu, Y., Zhu, H., Liu, J., Fan, H., Sun, L., Lu, W., Liu, X., & Li, L. (2011). 3,5,2',4'-Tetrahydroxychalcone, a new non-purine xanthine oxidase inhibitor. Chemico-biological Interactions, 189(3), 161-6. https://doi.org/10.1016/j.cbi.2010.12.004
Niu Y, et al. 3,5,2',4'-Tetrahydroxychalcone, a New Non-purine Xanthine Oxidase Inhibitor. Chem Biol Interact. 2011 Feb 1;189(3):161-6. PubMed PMID: 21167141.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 3,5,2',4'-Tetrahydroxychalcone, a new non-purine xanthine oxidase inhibitor. AU - Niu,Yanfen, AU - Zhu,Huajie, AU - Liu,Jia, AU - Fan,Huafang, AU - Sun,Ling, AU - Lu,Wei, AU - Liu,Xu, AU - Li,Ling, Y1 - 2010/12/15/ PY - 2010/08/30/received PY - 2010/12/02/revised PY - 2010/12/07/accepted PY - 2010/12/21/entrez PY - 2010/12/21/pubmed PY - 2011/3/15/medline SP - 161 EP - 6 JF - Chemico-biological interactions JO - Chem. Biol. Interact. VL - 189 IS - 3 N2 - Xanthine oxidase is a key enzyme that catalyses hypoxanthine and xanthine to uric acid and the overproduction of uric acid will lead to hyperuricemia which is an important cause of gout. In the present study, three chalcone derivatives were synthesized and evaluated for inhibitory activity against xanthine oxidase in vitro. Of the compounds, only Compound 1, 3,5,2',4'-tetrahydroxychalcone, exhibited a significant inhibitory activity on xanthine oxidase with an IC(50) value of 22.5 μM. Lineweaver-Burk transformation of the inhibition kinetics data demonstrated that it was a competitive inhibitor of xanthine oxidase and Ki value was 17.4 μM. In vivo, intragastric administration of Compound 1 was able to significantly reduce serum uric acid levels and inhibited hepatic xanthine oxidase activities of hyperuricemic mice in a dose-dependent manner. Acute toxicity study in mice showed that Compound 1 was very safe at a dose of up to 5 g/kg. These results suggest that Compound 1 is a novel competitive xanthine oxidase inhibitor and is worthy of further development. SN - 1872-7786 UR - https://www.unboundmedicine.com/medline/citation/21167141/352'4'_Tetrahydroxychalcone_a_new_non_purine_xanthine_oxidase_inhibitor_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0009-2797(10)00641-1 DB - PRIME DP - Unbound Medicine ER -