中文摘要：

组合生物合成是公认的产生大量“非天然”的天然产物的一种有效方法，也是近年来药物创新与应用的研究热点和重要手段之一。目前，组合生物合成在聚酮类抗生素等生物活性物质的开发应用研究中已经取得了显著的成果。结合文献中的例子，回顾了运用组合生物合成在天然产物的基础上产生更多结构及功能多样性的聚酮类抗生素的方法和思路，并对某些方法所存在的问题与不足进行了讨论。

英文摘要：

Combinatorial biosynthesis has been accepted as a useful method to produce a larger number of ＂unnatural＂ natural products. And it also has received a great attention in innovation and application of new drugs in recent years. It is now feasible to generate biologically active compounds by combinatorial biosynthesis, and some progress has been made with polyketides. Depending on examples of the literature, this paper reviews the opportunities for increasing structural diversity among natural products by combinatorial biosynthesis. Some of the problems and limitations encountered with the approaches are also discussed.