肝素药理作用和药物制剂的研究新进展

Promising Novel Applications of Heparin

肝素作为一线抗凝剂在临床上已经有着80年的应用。肝素抗凝特性主要是通过与抗凝血酶Ⅲ(antithrombin Ⅲ,ATⅢ)的相互作用来发挥。现已发现与肝素存在相互作用的功能蛋白有百余种,表明肝素有众多非抗凝活性具有研发为新药的潜能,如抗肿瘤、抗炎、抗病毒、抗疟疾、抗贫血。此外,肝素还有望用于载药工具以及功能化植入材料;肝素寡糖还有望通过生物工程、化学/酶法合成途径获取。笔者综述肝素的这些新应用和新进展。

Heparin has been used as first-line anticoagulant clinically for 80 years.Heparin mainly exerts its anticoagulant activity through interaction with ATⅢ.It has been found there are more than one hundred heparin-dependent functional proteins which demonstrates promising novel application beyond anticoagulant,such as anti-tumor,anti-malaria anti-inflammation,anti-viral,anti-malaria anti-anemia,etc.Heparin is also hopeful to be used as tool for drug delivery vehicle and functionalized implants material.In addition,heparin oligosaccharides are expected to be produced by chemical/enzymatic and bioengineering synthesis.Above mentioned new developments of heparin are covered in this review.