Mechanism of biochemical action of substituted 4-methylbenzopyran-2-ones. Part 10: Identification of inhibitors for the liver microsomal acetoxycoumarin: protein transacetylase

Raj, Hanumantharao G. and Singh, Ishwar and Kohli, Ekta and Kumari, Ranju and Gupta, Garima and Tyagi, Yogesh K. and Kumar, Ajit and Prasad, Ashok K. and Kaushik, Narendra K. and Olsen, Carl E. and Watterson, Arthur C. and Parmar, Virinder S. (2003) Mechanism of biochemical action of substituted 4-methylbenzopyran-2-ones. Part 10: Identification of inhibitors for the liver microsomal acetoxycoumarin: protein transacetylase. Bioorganic and Medicinal Chemistry, 11 (6). pp. 1015-1019. ISSN 0968-0896

Full content URL: http://dx.doi.org/10.1016/S0968-0896(02)00515-1

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Item Type:Article
Item Status:Live Archive

Abstract

The quantitative structure-activity relationship (QSAR) studies conducted by us earlier revealed the cardinal role of the pyran ring carbonyl group in the acetoxy polyphenolic compounds for the acetoxy polyphenol: protein transacetylase (TAase) activity. Hence, an attempt was made to examine whether such substrate analogues of benzopyran acetates which lack in the pyran ring carbonyl group, such as 7-acetoxy-2,3-dihydro-2,2-dimethylbenzopyran (BPA), cetachin pentaacetate (CPA) and hematoxylin pentaacetate (HPA) could inhibit the 7,8-diacetoxy-4-methylcoumarin (DAMC):protein (glutathione-S-transferase) transacetylase activity. These compounds were indeed found to remarkably inhibit the TAase activity in a concentration dependent manner and exerted their inhibitory action very rapidly. Further BPA, CPA and HPA were found to abolish the TAase mediated activation of NADPH cytochrome C reductase as well as the inhibition of liver microsome catalyzed aflatoxin B, (AFB(1))-DNA binding by DAMC very effectively. These results strongly suggest that the acetoxybenzopyrans merit as potent inhibitors of TAase. (C) 2002 Elsevier Science Ltd. All rights reserved.

Keywords:Pharmacy
Subjects:B Subjects allied to Medicine > B200 Pharmacology, Toxicology and Pharmacy
Divisions:College of Science > School of Pharmacy
ID Code:11308
Deposited On:24 Jul 2013 08:58

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