Novel inhibitor of brain indoleamine 2,3 dioxygenase, docking and experimental studies

Authors

  • Shazia Dawood Department of Biochemistry United Medical and Dental College Karachi
  • Samina Bano Clinical Biochemistry and Psychopharmacology Research Unit Department of Biochemistry University of Karachi

DOI:

https://doi.org/10.3329/icpj.v6i6.34180

Keywords:

Indoleamine 2, 3-dioxygenase, tryptophan, Molegro Virtual Docker, Hypericum perforatum, cytokines, N-formyl kynurenine

Abstract

Indoleamine 2,3-dioxygenase (IDO) is a haem-containing monomeric enzyme that catalyze the conversion of tryptophan (L-TRP) to N-formyl kynurenine. IDO activity is regulated by cytokines. Pro inflammatory cytokines are potent inducers of IDO, whereas anti-inflammatory cytokines are IDO inhibitors. Prostaglandin E2 induces IDO activity. In inflammation the relationship between immune system and the kynurenine pathway play an important role. IDO is an important therapeutic target for the treatment of inflammation. Present study evaluates the binding of Hypericum perforatum (HP) against IDO enzyme using MVD software acute and chronic effects of HP on IDO enzyme activity. Docking results show that HP fit well in the allosteric site of IDO. Energy scores for HP -158.687 Kcal/mol. Administration of HP (500mg/kg/3ml) shows that serum IDO activity was significantly increased (171%, P<0.01) and (114%, P<0.01) respectively after acute and chronic treatment. Brain IDO activity was decreased by 42%, (P<0.01) after acute and 43% (P<0.01) chronic treatment. It is concluded from the present study that HP is noncompetitive inhibitor of IDO as proofs by docking further its inhibitory effects on brain IDO reveals its anti-inflammatory effect.

Dawood and Bano, International Current Pharmaceutical Journal, May 2017, 6(6): 34-39

http://www.icpjonline.com/documents/Vol6Issue6/01.pdf

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Published

2017-10-03

How to Cite

Dawood, S., & Bano, S. (2017). Novel inhibitor of brain indoleamine 2,3 dioxygenase, docking and experimental studies. International Current Pharmaceutical Journal, 6(6), 34–39. https://doi.org/10.3329/icpj.v6i6.34180

Issue

Vol. 6 No. 6 (2017)

Section

Original Articles

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