以胆酸为载体的肝靶向疗法

Liver targeted therapy with bile acid as the carrier

通过肝靶向给药技术将化学治疗药物选择性地投放于肝脏,能够减轻或避免其全身的毒副作用。胆酸是唯一的口服有效的小分子肝靶向载体,以胆酸为载体的肝靶向疗法为肝病及肝脏代谢性疾病提供了新的疗法。如胆酸-一氧化氮供体靶向偶合物能够选择性地将一氧化氮投放于肝脏,产生治疗肝硬化的作用;胆酸-脂肪酸靶向偶合物能够选择性地调节肝脏的脂代谢,具有治疗胆结石、脂肪肝和动脉粥样硬化的作用;胆酸-米非司酮偶合物能够选择性地作用于肝脏,产生特异性的降糖作用,而没有全身副作用。

Liver targeted therapy can deliver chemotherapeutic drugs selectively to the liver to avoid side effects or toxicity, Bile acids are the only small molecules with high oral availability and are takenup specifically by the liver, Conjugating nitric oxide releasing components with cholic acid or ursodeoxycholic acid can deliver NO selectively to the liver for the treatment of liver fibrosis, cirrhosis and portal hypertension without significant reduction of arterial pressure; bile acid-mife- pristone conjugate, a liver-selective glucocorticoid receptor （GR） antagonist, can decrease hepatic glucose output and restore glycemic control without systemic side effects; fatty acid-bile acid conjugates can improve cholesterol solubilization, prevent cholesterol crystallization in supersaturated model solutions and human bile, inhibit atherosclerosis, prevent the diet-induced fatty liver.