Pharmacological properties of pentosan polysulfate sodium

The understanding of the multifaceted biological effects of pentosan polysulfate sodium is made possible by considering the interactions with heparan sulphate chains attached to the protein core of proteoglycans receptors on the cell surfaces and in the extracellular matrix (2).

Heparan sulphate is a glycosaminoglycan and is known to be ubiquitous at human cell surfaces, it is generally more abundant than most receptors (1).

The heparan-binding model is the common denominator, which links the varied activities of pentosan polysulfate sodium. For example it is known that heparan sulphate acts as a viral receptor, and that prions enter the cells in part due to their affinity to heparan receptors (3). It is also known that heparin binds to heparin sulphate glycosaminoglycans on the cell surface to block cell signalling induced by these factors, thus reducing the ultimate biological reactions.

It is because pentosan polysulfate sodium has similar capacity to block the binding of important biological molecules, that it possesses an impressive array of actions, for example affecting angiogenesis, coagulation/ fibrinolysis, growth factors/ morphogens, inflammation, or lipid metabolism.

References

1) Bernfield, M., et al., Functions of cell surface heparan sulfate proteoglycans. Annu Rev Biochem, 1999. 68: p. 729-77.
2) Vlodavsky, I. and Y. Friedmann, Molecular properties and involvement of heparanase in cancer metastasis and angiogenesis. J Clin Invest, 2001. 108(3): p. 341-7.
3) Warner RG, Hundt C, Weiss S, Turnbull JE.Identification of the heparan sulfate binding sites in the cellular prion protein. J Biol Chem. 2002 May 24;277(21):18421-30. Epub 2002 Mar 6.