Raj, Hanumantharao G., Singh, Ishwar, Kohli, Ekta , Kumari, Ranju, Gupta, Garima, Tyagi, Yogesh K., Kumar, Ajit, Prasad, Ashok K., Kaushik, Narendra K., Olsen, Carl E., 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
Full text not available from this repository.
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 |
Repository Staff Only: item control page