耐药时代下新型抗菌天然产物的发现策略

Strategies for discovery of novel antibacterial natural products under the antibiotic crisis

天然产物及其衍生物是抗菌药物发现的主要来源,但现今细菌耐药性的加剧给其研发带来巨大挑战。新抗菌药物的发现速度远低于细菌耐药产生的速度。21世纪以来,基因组学的创新和新抗菌资源的开发、对已知天然产物价值的重新认识以及抗菌辅佐剂的开发、组合生物合成等新研发策略的发展,为临床提供了大量新的抗菌先导化合物。天然产物化学结构具有多样性,在目前细菌耐药日趋严重的情况下,天然产物在抗菌新药研发中占据重要地位。

Natural products and their derivatives are main sources for the discovery of antibiotic drugs, however, nowadays the intensification of bacterial resistance imposes a huge challenge for their research and development. At the same time, the rate for new antibiotics discovery is much slower than that of bacterial drug resistance. Since the 21 st century, the advancement of several new methods, including new technologies such as the innovation of genomics and development of new antibacterial resources, repurposed the known natural products, and combinatorial biosynthesis etc., have brought new life to natural products and also provided new antibacterial lead compounds for clinical practice. The chemical structures of natural products are characterized by diversity and novelty. Under the current antibiotic crisis, natural products will regain its dominance in the development of new drugs.