Affiliation:
1. Department of Integrative Biology, School of Biosciences and Technology, Vellore Institute of Technology, Vellore 632014, Tamil Nadu, India
Abstract
Background:
Thrombosis represents as the prime contributor to the burden of diseases,
worldwide. Conventional anticoagulants for thrombosis therapy have a common bleeding side
effect. Bioactive peptides are studied to be an effective alternative for currently available
therapeutic drugs.
Objective:
In this study, VITPOR AI peptide, a previously reported coagulation FXIIa inhibitor
from Nori (Porphyra yezoensis), was assessed for its inhibitory activity against FXIIa and its in
vivo mode of action.
Methods:
In vivo efficacy as well as the antithrombotic property of the peptide was evaluated in
mice model by ex vivo activated Partial Thromboplastin Time assay, tail transection model and
whole blood clotting time. The enzyme kinetics was studied using chromogenic substrate assay.
Results:
The kinetic behaviour of VITPOR AI showed that the peptide is a competitive inhibitor of
FXIIa. Peptide showed significant inhibition of platelet adhesion and aggregation. VITPOR AI
exhibited significant antithrombotic activity. Furthermore, ex vivo activated Partial Thromboplastin
Time assay revealed that VITPOR AI exhibited potent anticoagulant activity in vivo. Tail bleeding
assay revealed that the peptide did not prolong bleeding time in mice even at a higher dose of
5 mg/kg. Cytotoxicity studies of the peptide against human blood leukocytes indicated the safety of
the peptide.
Conclusion:
VITPOR AI could be prospected as a potent anticoagulant with Factor XIIa inhibition,
antiplatelet aggregation and antithrombotic activity. It was also studied to have no bleeding side
effect.
Funder
Vellore Institute of Technology
Publisher
Bentham Science Publishers Ltd.
Subject
Biochemistry,General Medicine,Structural Biology
Cited by
2 articles.
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