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四环素类药物是抑制细菌蛋白合成的一大类广谱抗生素,广泛用于多种细菌及立克次氏体、衣原体、支原体等所致之感染。四环素类药物由Ⅱ型聚酮体途径(polyketide synthase,PKSⅡ)合成,通过一套可重复使用的结构域在重复的反应步骤中多次催化酚聚酮结构的生成。该类化合物的结构多样性主要来源于聚酮合成后的修饰。本文对四环素类药物的生物合成途径及关键酶调控机制的研究进展展开综述。
Tetracyclines are a broad spectrum of antibiotics that inhibit the synthesis of bacterial proteins and are widely used in infections caused by a variety of bacteria and rickettsia, chlamydia, mycoplasma and the like. Tetracyclines are synthesized by the polyketide synthase (PKSII) type II and catalyze the production of phenolic polyketides several times over a set of reusable domains in repeated reaction steps. The structural diversity of these compounds comes mainly from the modification of polyketides. This article reviews the biosynthetic pathway of tetracycline drugs and the regulatory mechanisms of key enzymes.