自从有人类历史以来,天然药物一直是人类防病治病的主要来源。天然产物是自然界的生物历经千百万年的进化过程通过自然选择保留下来的二次代谢产物,具有化学多样性、生物多样性和类药性。临床上应用的许多药物都直接或间接来源于天然产物,如天然产物可作为药物半合成的前体物、药物化学合成的模板以及为药物设计提供了新的思路。但是在20世纪80~90年代,由于受高通量筛选和组合化学的影响,天然药物的研究一度进入低谷。近10年来天然药物化学在新药研发中的作用又重新受到科学家的重视,天然产物已成为发现治疗重大疾病的药物或重要先导化合物的主要源泉之一。现就天然药物化学在新药开发中的作用进行了回顾与总结,并对其前景进行了展望。

From prehistoric time,humankind has used plants to alleviate and treat diseases.Natural products are secondary metabolites evolutionary selected and prevalidated by nature after millions of years,displaying a unique chemical diversity and corresponding diversity of the biological activities as well as drug-like properties.Around half of the drugs currently in clinical use are of natural product origin,including directly and indirectly,such as semisynthesis,mimic synthesis or inspired drug design.Despite these successes,large pharmaceutical companies have embraced the era of combinatorial chemistry in favor of high-throughput synthesis and screening during 1980-1990′s.Now the drug discovery industry is facing the considerable challenges,so more and more attention was re-focused on the role of natural product chemistry for the new drug research and development(R D) in the past 10 years.Natural products have become one of the most important resources of novel lead compounds especially for the critical diseases.This paper reviewed the roles of natural product chemistry in the new drug R D,and discussed the prospect of natural product chemistry.

国家自然科学基金项目(81072551);河北省自然科学基金项目(08B032,C2010000489);河北省引进留学人员基金项目(2008-2010);河北省卫生厅基金项目(05089);河北省中医药管理局基金项目(2006053);河北医科大学教育科学研究重点课题(09zd-17)