Anti-inflammatory and Antioxidant Peptide-Conjugates: Modulation of Activity by Charged and Hydrophobic Residues

  • K. P. Rakesh
  • R. Suhas
  • D. Channe GowdaEmail author


In the present study, antioxidant and anti-inflammatory activities of a series of quinazolinone-conjugated-peptides were investigated. Substitution of second position of the peptide template ‘GXGVP’ by different amino acids of varying hydrophobicity, charge and polarity has been studied. Quinazolinone-peptides with Trp residue emerged out as the highly potential antioxidant whereas the conjugate with Asp moiety turned to be a good anti-inflammatory agent. These data indicate that more hydrophobicity favours antioxidant property and contrarily, presence of charged species in the molecule assists the reduction of inflammation. Further, conjugates having butyl group in the heterocyclic part and free C-terminus in the peptide part exhibited good inflammation reducing property. Thus, variation of hydrophobic groups, charges and polarity of certain amino acids in the peptide segment of the conjugate could be used to develop “dual war-head” potential therapeutics for treating inflammation and allied diseases.


Peptide-conjugates Antioxidant Anti-inflammatory Charge and hydrophobicity 



3-(4-Oxo-3,4-dihydroquinazolin-2-yl)propanoic acid


4-(4-Oxo-3,4-dihydroquinazolin-2-yl)butanoic acid




N-Hydroxy benzotriazole


N-Methyl morpholine




Trifluoroacetic acid



We gratefully acknowledge University Grant Commission-Basic Science Research (UGC-BSR) for the award of BSR fellowship, Center with Potential for Excellence in a Particular Area (CPEPA), University of Potential Excellence (UPE) and Department of Science and Technology-Promotion of University Research and Scientific Excellence (DST-PURSE), UGC, New Delhi for the financial assistance.

Compliance with Ethical Standards

Conflict of interest

The authors declare that they have no conflicts to interest.

Ethical Approval

This article does not contain any studies with human participants or animals performed by any of the authors.

Supplementary material

10989_2017_9668_MOESM1_ESM.doc (1.5 mb)
Supplementary material 1 (DOC 1521 KB)


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Authors and Affiliations

  1. 1.Department of Studies in ChemistryUniversity of MysoreMysuruIndia
  2. 2.Postgraduate Department of ChemistryJSS College of Arts, Commerce and ScienceMysuruIndia

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