Abstract:
:Glutathione-S-transferase (GST) a Phase-II drug detoxification enzyme, was detected in Setaria cervi, a bovine filarial parasite. In vitro effect of diethylcarbamazine, butylated hydroxyanisole and phenobarbitone on the GST of adult female S. cervi was assayed by the addition of these compounds in the maintenance medium. The specific activity of GST towards 1-chloro-2,4-dinitrobenzene was increased progressively 1.2-1.97, 1.3-2.4 and 1.2-2.7 times at 10-100 microM of diethylcarbamazine, butylated hydroxyanisole and phenobarbitone, respectively, after 5 h at 37 degrees C. Substrate specificity studies showed a higher increase in specific activity with ethacrynic acid and no change with cumene hydroperoxide. Although the intensity of GST activity band was more in extract from diethylcarbamazine or butylated hydroxyanisole treated worms extract, an extra band of activity appeared in those worm extracts compared to control worm extract. SDS/PAGE showed increased thickness of the band corresponding to purified GST in extracts from diethylcarbamazine/butylated hydroxyanisole/phenobarbitone treated worms. Purification and quantification of GST from diethylcarbamazine and butylated hydroxyanisole treated worms indicated an increase in enzyme specific activity. The increase in GST protein by these agents was blocked by prior treatment with actinomycin D, indicative of a transcription dependent response. The role of this enzyme in motility and viability of microfilariae and adult female was tested in vitro using a range of known GST inhibitors. Of those tested, ethacrynic acid, ellagic acid, 1-chloro-2,4-dinitrobenzene, cibacron blue and butylated hydroxyanisole reduced the viability and motility of microfilariae and adult female worms at micromolar concentrations. These results suggest that S. cervi GST is inducible in response to the antifilarial drug diethylcarbamazine and may play an important role in parasite's survival, thus could be a potential drug target.
journal_name
Acta Biochim Poljournal_title
Acta biochimica Polonicaauthors
Gupta S,Rathaur Ssubject
Has Abstractpub_date
2005-01-01 00:00:00pages
493-500issue
2eissn
0001-527Xissn
1734-154Xpii
20051017journal_volume
52pub_type
杂志文章abstract::A number of antiviral lectins, small proteins that bind carbohydrates found on viral envelopes, are currently in pre-clinical trials as potential drugs for prevention of transmission of human immunodeficiency virus (HIV) and other enveloped viruses, such as the Ebola virus and the coronavirus responsible for severe ac...
journal_title:Acta biochimica Polonica
pub_type: 杂志文章,评审
doi:
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pub_type: 杂志文章,评审
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journal_title:Acta biochimica Polonica
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journal_title:Acta biochimica Polonica
pub_type: 杂志文章,评审
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更新日期:2005-01-01 00:00:00
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journal_title:Acta biochimica Polonica
pub_type: 杂志文章
doi:
更新日期:2006-01-01 00:00:00
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journal_title:Acta biochimica Polonica
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更新日期:2012-01-01 00:00:00
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journal_title:Acta biochimica Polonica
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更新日期:2014-01-01 00:00:00
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journal_title:Acta biochimica Polonica
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更新日期:1999-01-01 00:00:00
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journal_title:Acta biochimica Polonica
pub_type: 杂志文章
doi:024904829
更新日期:2002-01-01 00:00:00
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journal_title:Acta biochimica Polonica
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更新日期:2013-01-01 00:00:00
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journal_title:Acta biochimica Polonica
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doi:
更新日期:2001-01-01 00:00:00
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journal_title:Acta biochimica Polonica
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journal_title:Acta biochimica Polonica
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更新日期:2006-01-01 00:00:00
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journal_title:Acta biochimica Polonica
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更新日期:1996-01-01 00:00:00
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journal_title:Acta biochimica Polonica
pub_type: 杂志文章,评审
doi:024903597
更新日期:2002-01-01 00:00:00
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journal_title:Acta biochimica Polonica
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更新日期:1992-01-01 00:00:00
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更新日期:1990-01-01 00:00:00
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journal_title:Acta biochimica Polonica
pub_type: 杂志文章
doi:10.18388/abp.2015_1111
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journal_title:Acta biochimica Polonica
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更新日期:2000-01-01 00:00:00
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