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Am. J. Trop. Med. Hyg., 80(5), 2009, pp. 764-768
Copyright © 2009 by The American Society of Tropical Medicine and Hygiene

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SHORT REPORT


Antifilarial Activity of 1,3-Diarylpropen-1-One: Effect on Glutathione-S-Transferase, a Phase II Detoxification Enzyme

Satish K. Awasthi*, Nidhi Mishra, Sandeep Kumar Dixit, Alka Singh, Marshleen Yadav, Sudhanshu S. Yadav, AND Sushma Rathaur
Chemical Biology Laboratory, Department of Chemistry, University of Delhi, Delhi, India; Department of Biochemistry, Faculty of Science, Banaras Hindu University, Varanasi, India

 

ABSTRACT

Chalcone derivatives were evaluated for their antifilarial activity on Setaria cervi using glutathione-S-transferase (GST) as a drug target. The compounds 1-(4-benzotriazol-1-yl-phenyl)-3-(4-methoxyphenyl)prop-2-en-1-one (5), and 3-(4-methoxyphenyl)-1-(4-pyrrolidin-1-yl-phenyl) prop-2-en-1-one (7) showed a significant suppression (P < 0.01) in GST activity of adult female parasite extract at 3 µM concentration in vitro. However, GST activity was detected along with depletion in GSH level. Except Compounds 1 and 2, all exhibited a significant effect on the motility and viability of adult parasites. Compounds 3-(4-chlorophenyl)-1-(4-piperidin-1-yl-phenyl)prop-2-en-1-one (3), 1-(4-benzotriazol-1-yl-phenyl)-3-(4-methoxyphenyl)prop-2-en-1-one (5), and 3-(4-methoxyphenyl)-1-(4-pyrrolidin-1-yl-phenyl) prop-2-en-1-one (7) exhibited major irreversible effects on viability and resulted in parasite death and also inhibited the GST activity by 84–100% in vitro. We report for the first time the antifilarial activity of chalcones on GST of adult parasites. This study also strengthens our previous findings where GST is reported as a potential drug target for antifilarials.

Received July 29, 2008. Accepted for publication January 18, 2009.

Acknowledgments: S.K.A. thanks Prof. Liam Good, Department of Pathology and Infectious Diseases, Royal Veterinary College, University of London, UK, for reviewing the manuscript.

Financial support: S.K.A. and S.R. are grateful to the Department of Science and Technology (DST; Scheme SR/S0/BB-65//2003), University of Delhi, Delhi, and University Grant Commission (UGC; Scheme F.30-214/2004), New Delhi, India, respectively, for financial assistance. The University of Delhi assisted with publication expenses.

* Address correspondence to Satish K. Awasthi, Chemical Biology Laboratory, Department of Chemistry, Delhi 110007, India. E-mails: skawasthi{at}chemistry.du.ac.in or awasthisatish{at}yahoo.com

Authors’ addresses: Satish K. Awasthi, Nidhi Mishra, and Sandeep Kumar Dixit, Chemical Biology Laboratory, Department Of Chemistry, University of Delhi, Delhi 110007, India. Alka Singh, Marshleen Yadav, Sudhanshu S. Yadav, and Sushma Rathaur, Department of Biochemistry, Faculty of Science, Banaras Hindu University, Varanasi 221005, India.






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