Literature DB >> 19278854

Synthesis, anti-inflammatory, and antioxidant activities of 18beta-glycyrrhetinic acid derivatives as chemical mediators and xanthine oxidase inhibitors.

Dravidum Maitraie1, Chi-Feng Hung, Huang-Yao Tu, Ya-Ting Liou, Bai-Luh Wei, Shyh-Chyun Yang, Jih-Pyang Wang, Chun-Nan Lin.   

Abstract

Twenty 18beta-glycyrrhetic acid (18beta-GA) derivatives 2-21 including 13 new 18beta-GA derivatives were synthesized and evaluated as anti-inflammatory and antioxidant agents. Compounds 7 and 20 with a 3,4-seco-structure and compound 6 with a lactone moiety showed potent inhibitory effect on superoxide anion generation in rat neutrophils response to fMLP/CB and PMA, respectively. Compound 6 with a lactone moiety revealed stronger inhibitory effect on XO activity than those of compounds 13 and 14 with a 3,4-seco-structure. Compound 14, a 30-isoproylcarbamoyl seco-compound exhibited potent inhibitory effect on NO accumulation and iNOS protein expression while compounds 3, 10, 13, 15, 17, and 21 revealed potent inhibitory effect on tumor necrosis factor-alpha (TNF-alpha) formation in RAW 264.7 cells in response to lipopolysaccharide (LPS). The cleavage of ring A of 3 attenuated the inhibitory effect on TNF-alpha formation in RAW 264.7 cells in response to LPS except for 17. The present results suggested these compounds were potential to be served as anti-inflammatory and antioxidant agents.

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Year:  2009        PMID: 19278854     DOI: 10.1016/j.bmc.2009.02.025

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  15 in total

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Journal:  J Comput Aided Mol Des       Date:  2009-12-29       Impact factor: 3.686

6.  18ß-glycyrrhetinic acid derivative promotes proliferation, migration and aquaporin-3 expression in human dermal fibroblasts.

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10.  Design and preparation of derivatives of oleanolic and glycyrrhetinic acids with cytotoxic properties.

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Journal:  Drug Des Devel Ther       Date:  2018-05-21       Impact factor: 4.162

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