Sulfated polysaccharides activities

CS derivatives/salts have found limited use as detergents (25), antistatic coatings for photographic film (26), oil drilling fluids (25), thickeners in food, cosmetics, and pharmaceuticals (27). They have been recommended for use as cation exchangers (28,29). Also, sulfated polysaccharides have recendy shown interesting antiviral activity (30). 

De Clercq E. Anti-HIV activity of sulfated polysaccharides. In Yalpani M, ed. Carbohydrates and Carbohydrate Polymers, Analysis, Biotechnology,... 

Emphasis in the initial phase of our work was placed on sulfated polysaccharides that are antiviral. Not only were the desired rheological properties and long-term stability achieved in DCE formulations, the activity of the dextran sulfate or N9 were not compromised. DCE formulations containing DS display strong anti-HIV activity in vitro in comparison with negative (not shown) and positive controls (Figure 2). This is an important first step in the screening process towards clinical effectiveness. 

The addition of sulfated polysaccharides to DCE gels have yielded effective microbicides in vitro, including activity against human immunodeficiency virus (HIV). 

As a result of heparin s multiplicity of biological activities and its importance as a major pharmaceutical, other polysaccharides and modified polysaccharides have been examined as potential heparin analogues in drug development (1). These heparin analogues include other GAGs, other non-GAGs, sulfated polysaccharides from plant and animal origins such as lam-... 

Melo, F. R., Pereira, M. S., Foguel, D., and Mourao, P. A. (2004). Antithrombin-mediated anticoagulant activity of sulfated polysaccharides Different mechanisms for heparin and sulfated galactans. J. Biol. Chem. 279, 20824—20835. 

A number of mannose-specific agglutinines (lectins) from Galanthus nivalis, Hippeastrum hybrid, Narcissus pseudonarcissus, Listera ovata, Cymbidium hybrid, Epipactis helleborine, and the N-acetylglucosamine-specific lectin from Urtica dioica have been found to inhibit HIV-1 and HIV-2 infection at similar concentrations as dextran sulfate (IC50 0.2 to 0.6 fig/ml), or even lower (IC50 0.04 to 0.08 pg/ml. Akin to sulfated polysaccharides, the plant lectins also exhibit activity against various enveloped viruses other than HIV, i.e., HSV-1, HSV-2, CMV, RSV, and influenza virus. Plant lectins would primarily interfere with the virus-cell fusion process. Their precise mode of action remains to be resolved. 

Abstract The inhibitory action of polyanionic substances on virus replication was reported more than 50 years ago. Seaweeds, marine invertebrates, and higher plants represent abundant sources of novel compounds of proved antiviral activity. Natural sulfated polysaccharides (SPs) are potent in vitro inhibitors of a wide variety of enveloped viruses, such as herpes simplex virus (HSV) types 1 and 2, human immunodeficiency virus (HIV), human cytomegalovirus (HCMV), dengue virus (DENV), respiratory syncytial virus (RSV), and influenza A virus. Several polysulfate compounds have the potential to inhibit virus replication by blocking the virion binding to the host cell. In contrast, their in vivo efficacy in animal and human systemic infections has undesirable draw-... 

Keywords Antiviral activity Chemical structure Natural sulfated polysaccharides Polyanions Seaweeds... 

Pujol et al. in chapter eight, reviews the chemistry, origin and antiviral activities of naturally occurring sulfated polysaccharides for the prevention and control of viral infections such as HIV-1 and -2, human cytomegalovirus (HCMV), dengue virus (DENV), respiratory syncytial virus (RSV), and influenza A virus. 

In addition to valuable physicochemical properties, sulfated polysaccharides of the red algae are promising biologically active polymers, and many structural works already cited aimed at isolation and characterization of new compounds having potential medical application. The most important types of biological activity of sulfated galactans are listed briefly in this section. 

M. Shanmugam and K. H. Mody, Heparinoid-active sulfated polysaccharides from marine algae as potential blood anticoagulant agents, Curr. Sci., 79 (2000) 1672-1683. 

N. Griinewald, I. Groth, and S. Alban, Evaluation of seasonal variations of the structure and antiinflammatory activity of sulfated polysaccharides extracted from the red alga Delesseria sanguinea (Hudson) Lamouroux (Ceramiales, Delesseriaceae), Biomacromolecules, 10 (2009) 1155-1162. 

N. Bourgougnon, M. Lahaye, J.-C. Chermann, and J.-M. Komprobst, Composition and antiviral activities of sulfated polysaccharide from Schizymenia dubyi (Rhodophyta, Gigartinales), Bioorg. Med. Chem. Lett., 3 (1993) 1141-1146. 

The variety of methods that have been used for assaying anticoagulant activity makes difficult a comparison of the results of different workers."-It is claimed that the most satisfactory, although not the most convenient, method involves animal tests. By the use of three groups of animals, for control and for injection of standard heparin and of synthetic products, the effect of the latter group is thought to be most accurately assessed. Subsequent references to the activity of sulfated polysaccharides will be limited to comparisons with that of the heparin preparations used by individual authors and not with that of a common standard. 

The preceding data suggest that the activity of heparin is not simply a function of the degree of sulfation, since heparin preparations of high activity contain fewer sulfate groups than the more weakly acting, synthetic products. Karrer and associates" also point out that the relatively rapid disappearance of heparin activity in vivo, compared to the slow disappearance of activity of synthetic, sulfated polysaccharides, may be due to a different mode of action. 

Summarizing, it may be stated that the combination of size, shape, degree of sulfation, and distribution of sulfate groups endows heparin with a specific, anticoagulant activity of a type which may be different from that shown by synthetic, sulfated polysaccharides," and that inactivation appears to take place with relatively little chemical change in the molecule. The sulfation of heparin may well result in its conversion to the class of synthetic, sulfated mucopolysaccharides. 

Heparin is a mixture of sulfated polysaccharides with molecular weights of 15-20,000 daltons. Low-molecular-weight (LMW) heparins (e.g., enoxaparin) have potential advantage of longer half-life, less thrombocytopenia, and possibly enhanced activity against factor Xa. 

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