活性天然产物蛋白靶点的快速筛选策略

Rapid Screening Strategy for Target Identification of Bioactive Natural Products

来源于中药等自然资源的活性天然产物是药物的重要来源,筛选确定活性天然产物的蛋白靶点是明确其药理,毒理和成药的重要环节。目前传统的靶点筛选方法是基于分子标记示踪完成的,周期长且改变了天然产物本身的分子结构和药理作用,具有很大的弊端。新型冠状病毒引发的疫情(Coronavirus disease 2019,COVID-19)启示我们,快速的揭示药物的作用靶点对明确药物的药理和推广使用具有重要价值。近年来,结合蛋白质理化性质与蛋白质组学的非标记天然产物药理靶点的快速筛选技术日趋成熟。通过实例对目前主流的活性天然产物蛋白靶点的非标记筛选策略进行整理和总结,以期为该领域工作者提供前瞻性参考。

Bioactive natural products from traditional Chinese medicine and other natural resources are the important origin of medicines.Identification of the protein target in bioactive natural products is the key step to clarify the pharmacology and toxicology of them and prepared medicines.The current traditional target screening method is based on the molecular marker tracing,which has a long cycle and also leads to changes in the structure and pharmacological effect of natural products,and thus it has drawbacks.The novel coronavirus diseases(Coronavirus Disease 2019,COVID-19)enlightens us:It is of great value to reveal the target of drug action for the promotion and application of natural products.In recent years,the rapid screening technology for the pharmacological targets of unlabeled natural products based on the protein physical and chemical properties and omics is maturing.In this article,we sort and summarize the major unlabeled and rapid screening strategies for the protein targets of natural products via the practical cases,and aim to provide a prospective reference for the practioners in this field.