阿维菌素(avermectins)是由微生物发酵生产的高效低毒生物杀虫剂,在粮食安全、农产品安全、畜牧业和医药健康等领域具有重大意义。其衍生物伊维菌素(ivermectins)可有效治疗河盲症,帮助超过2亿非洲人幸免于失明。我国的阿维菌素产业利用遗传学改造手段深入挖掘微生物的潜能,大幅度提高了底物利用率、目标产物得率和反应器产率,打破了美国默克公司的产品垄断,从无到有,从弱到强,直至独占全球市场。阿维菌素的生物“智”造不但成为实验室技术向产业成功转化的典范,为其他微生物天然产物药物的研发提供了可借鉴的策略和方法,而且得到广泛的国际认可。本文介绍了阿维菌素的发现、基础及应用研究的发展历程,尤其是中国“智”造的历史沿革,旨在为我国微生物药物的产业化发展提供参考和借鉴。

Avermectins, are pesticides of fermentation products with high efficacy and low toxicity and play important roles in food and agricultural product safety, animal and human health. Ivermectins, the derivatives of avermectins, are used to treat Onchocerciasis, also known as River Blindness. Thanks to these discoveries, more than 200 million Africans are lucky to be exempted from blindness. Great efforts have been made on better understanding of the microbial production system of avermectins through genetic engineering in China. Starting from scratch, Chinese avermectin industry has experienced a comprehensive technological innovation with significantly improved yield, titer and productivity of avermectins, and became the exclusive supplier for the global market. The success of avermectin industry innovation in China not only shed lights on the intelligent yield improvement of other microbial natural product drugs, but also gained wide international recognition. We provide here an overview of the discovery and development of basic and applied research of avermectins, especially historical evolution of avermectins made in China, which will benefit industrial development of microbial drugs in China.