Development of bioanalytical assays for variegin, a peptide-based bivalent direct thrombin inhibitor-Reference-Cited by-同舟云学术

Development of bioanalytical assays for variegin, a peptide-based bivalent direct thrombin inhibitor

Published:2017-05 Issue:9 Volume:9 Page:693-705
ISSN:1757-6180
Container-title:Bioanalysis
language:en
Short-container-title:Bioanalysis

Author:

Shih Norrapat¹,de Carvalho Leonardo Pinto²,Lee Yie Hou³,Rocha Mauricio Macario⁴,Pereira Barbosa Adriano Henrique⁴,A de Sousa José Marconi⁴,de C Carvalho Antonio Carlos⁴,Kini R Manjunatha¹,Chan Mark Y²

Affiliation:

1. Department of Biological Sciences, National University of Singapore, 14 Science Drive 4, Block S2 Level 2, Singapore 117543, Singapore

2. Cardiac Department, National University Hospital, Cardiovascular Research Institute (CVRI), National University Heart Centre (NUHCS), National University Health System, 14 Medical Drive, MD6 #08–01, Singapore 117599, Singapore

3. KK Research Centre, KK Women’s & Children’s Hospital, 100 Bukit Timah Road, Singapore 229899, Singapore

4. Cardiac Department, Federal University of Sao Paulo State (UNIFESP), 715 Napoleao de Barros, Sao Paulo 04024–002, Brazil

Abstract

Aim: Variegin is an anticoagulant peptide that will be tested in porcine models of percutaneous coronary intervention. We developed three bioanalytical assays for variegin quantitation and utilized these methods to evaluate pharmacokinetics of variegin in pigs. Results & methodology: The LC–MS/MS, thrombin amidolytic and modified thrombin time assays had a quantitation range of 21.6–5541.7, 10.8–5541.7 and 5.4–5541.7 nM in human plasma, respectively. The elimination half-lives obtained using the LC–MS/MS, modified thrombin time and thrombin amidolytic assays were 52.3 ± 4.4, 50.4 ± 5.9 and 67.7 ± 6.3 min, respectively. Conclusion: We developed three bioanalytical assays for a novel direct thrombin inhibitor, variegin. The thrombin time assay is optimized for variegin quantitation during future porcine studies and clinical trials.

Publisher

Future Science Ltd

Subject

Medical Laboratory Technology,Clinical Biochemistry,General Pharmacology, Toxicology and Pharmaceutics,General Medicine,Analytical Chemistry

Link

http://www.future-science.com/doi/pdf/10.4155/bio-2017-0006

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