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

Ajit Kumar, Brajendra K. Singh, Nawal K. Sharma, Kapil Gyanda, Sapan K. Jain, Yogesh K. Tyagi, Anil S. Baghel, Mukesh Pandey, 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

Research output: Contribution to journalArticle

22 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)447-455
Number of pages9
JournalEuropean Journal of Medicinal Chemistry
Volume42
Issue number4
DOIs
StatePublished - Apr 1 2007

Keywords

  • Glutathione S-transferase (GST)
  • Micronuclei modulation
  • NADPH cytochrome c reductase
  • Polyphenolic acetates
  • Protein transacetylase (TAase)

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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    Kumar, A., Singh, B. K., Sharma, N. K., Gyanda, K., Jain, S. K., Tyagi, Y. K., Baghel, A. S., Pandey, M., Sharma, S. K., Prasad, A. K., Jain, S. C., Rastogi, R. C., Raj, H. G., Watterson, A. C., Van der Eycken, E., & Parmar, V. S. (2007). Specificities of acetoxy derivatives of coumarins, biscoumarins, chromones, flavones, isoflavones and xanthones for acetoxy drug: Protein transacetylase. European Journal of Medicinal Chemistry, 42(4), 447-455. https://doi.org/10.1016/j.ejmech.2006.09.008