Specificities of acetoxy derivatives of coumarins, biscoumarins, chromones, flavones, isoflavones and xanthones for acetoxy drug: Protein transacetylase

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• 作者：Ajit Kumar ; Brajendra K. Singh ; Nawal K. Sharma ; Kapil Gy ; a ; Sapan K. Jain ; Yogesh K. Tyagi ; Anil S. Baghel ; Mukesh P ; ey ; Sunil K. Sharma ; Ashok K. Prasad ; Subhash C. Jain ; Ramesh C. Rastogi ; Hanumantharao G. Raj ; Arthur C. Watterson ; Erik Van der Eycken ; Virinder S. Parmar
• 关键词：Polyphenolic acetates ; Glutathione S-transferase (GST) ; Micronuclei modulation ; NADPH cytochrome c reductase ; Protein transacetylase (TAase)
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2007
• 出版时间：April 2007
• 年：2007
• 卷：42
• 期：4
• 页码：447-455
• 全文大小：629 K

文摘

The earlier work carried out in our laboratory led to the identification of a novel rat liver microsomal enzyme termed as acetoxy drug: protein transacetylase (TAase), catalyzing the transfer of acetyl group from polyphenolic acetates (PA) to functional proteins. In this paper, we have reported the comparison of the specificities of acetoxy derivatives of coumarins, biscoumarins, chromones, flavones, isoflavones and xanthones with special reference to the phenyl moiety/bulky group on the pyran ring of PA. The results clearly indicated that compounds having phenyl moieties, when used as the substrates, resulted in a significant reduction of TAase catalyzed activity. The alteration in TAase catalyzed activation of NADPH cytochrome c reductase and inhibition of benzene-induced micronuclei in bone marrow cells by PA were in tune with their specificities to TAase.