Enzymatic Generation of Highly Anticoagulant Bovine Intestinal Heparin

Li Fu, Kevin Li, Daisuke Mori, Makoto Hirakane, Lei Lin, Navdeep Grover, Payel Datta, Yanlei Yu, Jing Zhao, Fuming Zhang, Murat Yalcin, Shaker A. Mousa, Jonathan S. Dordick, Robert J. Linhardt

Research output: Contribution to journalArticlepeer-review

21 Scopus citations

Abstract

Unlike USP porcine heparin, bovine intestinal heparin (BIH) has a low anticoagulant activity. Treatment with 6-OST-1, -3, and/or 3-OST-1 afforded two remodeled heparins that met USP heparin activity and Mw specifications. We explored the pharmacodynamics and pharmacokinetics in a rabbit model. We conclude that a modest increase in the content of 3-O-sulfo groups in BIH increases the number of antithrombin III binding sites, making remodeled BIH behave similarly to pharmaceutical heparin.

Original languageEnglish
Pages (from-to)8673-8679
Number of pages7
JournalJournal of Medicinal Chemistry
Volume60
Issue number20
DOIs
StatePublished - 26 Oct 2017
Externally publishedYes

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