棘白菌素类抗真菌药物的结构与微生物合成

Structure and Biosynthesis of Antifungal Drug Echinocandins

棘白菌素类抗真菌药物为一种新型脂肽类化合物,通过非竞争性抑制真菌细胞壁中的β-1,3-葡聚糖合酶活性进而抑制真菌细胞壁的合成。已有caspofungin、micafungin和anidulafungin三种药品成功上市。由于来源微生物的多样性,该类化合物的氨基酸组成、脂肪酸链以及侧链修饰均存在差异。本文从化学结构与生物合成的角度出发,总结了该类化合物的研究进展,主要包括棘白菌素类药物的化学多样性、产生菌的生物特性以及它们在发酵生产中所面临的工程问题等。

Echinocandins are a new group of lipopeptide antifungal antibiotics with inhibiting the activity of β-1,3-glucan synthase and biosynthesis of fungal cell wall.Three echinocandins-caspofungin,micafungin and anidulafungin have been launched.The combination of amino acids,fatty chains and the modification of side chains for these lipopeptides are different because of different producing microorganisms.The chemical structure and biosynthesis,including their chemical diversity,biological characteristics of producing strain and problems in fermentation process are mainly reviewed.