ABSTRACT
Chondroitin sulfate (CS) is a heterogeneous and negatively charged polysaccharide composed of repeating disaccharideunits, and has many pharmacological activities. CS has been recommended as symptomatic slow acting drugs for osteoarthritis (SYSADOA) in clinical practice. CS is shown to have promising prospect as a potential candidate for anti-metastasis of cancers and as a neurite outgrowth agent for neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease characterized by progressive loss of neurons. Moreover, CS is also involved in interaction with virus during its cell entry, wound healing and osteogenesis, and may be a promising drug candidate in these areas. Based on original publications, the research advances of CS in these areas and its applications were reviewed. The possibility of chemoenzymatic synthesis of specific CS chains as potential drugs was also discussed here, which may be used in the treatment of osteoarthritis, anti-metastasis of cancers, and so on.
ABSTRACT
Heparan sulfate (HS) and heparin (HP) are highly sulfated and heterogeneous polysaccharides composed of repeating disaccharide units. HS takes part in regulation of many related biological functions through its interaction with proteins and plays an important role in them. HS is also shown to have promising perspectives as a potential antivirus agent. As a special structure type of HS,HP is also widely used as the clinical anticoagulant drug and demonstrated to be a promising candidate for anticancer and anti-inflammatory drugs. Progress of the research in the areas of anticoagulant， anticancer， anti-inflammatory and antivirus activity of HS/HP and their chemoenzymatic synthesis is summarized in this review.
ABSTRACT
Heparan sulfate (HS) takes part in regulation of many related animal biological functions by its interaction with proteins and plays an important role. As a special structure type of HS, heparin (HP) is also widely used as clinical anticoagulant drug and demonstrated to be a promising candidate for anticancer and anti-inflammatory drugs. Natural HS and HP are highly heterogeneous mixtures differing in their polysaccharide chain lengths, sulfation patterns and so on, which restricts elucidation of the relationship between their structures and functions and further application of their drug potential. There has recently been a breakthrough in chemoenzymatic method developed for an alternative approach different from chemical synthesis, which shortens the synthesis and improves the product yields significantly. Application of chemoenzymatic synthesis accelerates elucidation of structure-function relationships in HS/HP and low-molecular-weight heparins (LMWH) with reversible anticoagulative activity have been obtained. Along with improvement and optimization of chemoenzymatic method and further understanding of structure-function relationship, it will gradually become possible to synthesize structure-specific HS/HP drugs with better and more stable effects and less adverse effects in the future. Recent progress of HS/HP chemoenzymatic synthesis is summarized in this review.