Abstract
Heparin has been widely used as an anticoagulant for more than 80 years. However, there is now considerable evidence that heparin also possesses anti-inflammatory activity, both experimentally and clinically. Importantly in many instances, the anti-inflammatory actions of heparin are independent of anticoagulant activity raising the possibility of developing novel drugs based on heparin that retain the anti-inflammatory activity. Heparin exhibits anti-inflammatory activities via a variety of mechanisms including neutralization of cationic mediators, inhibition of adhesion molecules, and the inhibition of heparanase, all involved in leukocyte recruitment into tissues. It is anticipated that furthering our understanding of the anti-inflammatory actions of heparin will lead to the development of novel anti-inflammatory drugs for a variety of clinical indications.
Highlights
Heparin has been used for over eighty years as an anticoagulant
Heparin belongs to the glycosaminoglycan (GAG) family of polysaccharides which are characterised by alternating hexuronic acid and hexosamine disaccharides as the backbone structure, there are a number of other molecules that fall into the GAG family
Mast cells contain an array of inflammatory mediators packed in to their granules which are released on stimulation, and heparin has been found packed in conjunction with a range of cationic molecules, for example, chymase and tryptase
Summary
Heparin has been used for over eighty years as an anticoagulant. Despite its widespread use, the exact mechanism for the anticoagulant activity of heparin was not elucidated until the 1960s and the specific polysaccharide sequence within the heparin molecule required for this interaction was not defined until nearly twenty years later [1]. In addition to the well described anticoagulant effect of heparin, a range of polysaccharides, some derived from heparin, and some from related structures, have been found to interact with a wide variety of biological pathways and systems, raising the possibility that such drugs may have wider therapeutic uses than inhibiting coagulation. These other activities of heparin and related drugs are less well understood than anticoagulant activity, but such drugs are under investigation for a wide range of clinical indications, for the treatment of inflammatory diseases. Hexosamine—βGlcNAc: β-D-N-acetylglucosamine; GlcNAc: α-D-N-acetylglucosamine; GalNAc: β-D-N-acetylgalactosamine; GalNAc(4S): β-D-Nacetylgalactosamine-4-O-sulfate; GalNAc(6S): β-D-N-acetylgalactosamine-6-O-sulfate; GalNAc(4S,6S): β-D-N-acetylgalactosamine-4-O, 6-O-sulfate; GlcNS: α-D-N-sulfoglucosamine; GlcNS(6S): α-D-N-sulfoglucosamine-6-O-sulfate
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