A golden phoenix arising from the herbal nest — A review and reflection on the study of antimalarial drug Qinghaosu
Feature Article First Online: 28 October 2010 Received: 15 January 2010 Accepted: 06 May 2010 Abstract
Qinghaosu (QHS) and its derivatives are a new generation of antimalarial drugs characterized by fast action, high efficacy, and good tolerance. This feature article states the discovery of QHS from traditional Chinese medicine qinghao (
Artemisia annua L.) and reviews the progress during the past four decades in the research of phytochemistry of A. annua, chemical reactions and biotransformation of QHS, chemical synthesis and biosynthesis of QHS, synthesis and antimalarial activity of QHS derivatives and analogs, pharmacological studies, clinical application, and the antimalarial mechanism. Undoubtedly, QHS is an example of the value of traditional Chinese medicine in modern medicinal research. Ying LI graduated from the graduate school of Shanghai Institute of Materia Medica, Chinese Academy of Sciences in 1966. Right after her graduation, she was engaged in the exploration of new antimalarials. She and her colleagues conducted structure determination and synthesis of some active principles of traditional Chinese medicines. Since 1976, she has been working in the area of qinghaosu, especially the structure modification and structure-activity relationship of it. She synthesized a number of derivatives and analogs of qinghaosu, including artemether and arteether. Artemether has been approved to be a new antimalarial drug and prevention drug for Schistosomiasis. Her recent research interest is focused on qinghaosu derivatives in the application to anticancer and immunopression. She has published more than 60 papers and book chapters. Yu-Lin WU graduated from the graduate school of Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences. Since his graduation, Mr. Wu has been continuously engaged in chemical researches of natural products and organic synthesis mainly in the same Institute. He was promoted to full professorship in 1989, and was then appointed to several senior positions, including the Director of the State Key Laboratory of Bio-organic and Natural Products Chemistry, SIOC, CAS from 1990 to 1999. He has served in several academic societies, such as the Chairman of the Division of Organic Chemistry, Chinese Chemical Society (1994-2006). His major research interest focuses on the natural products, especially the active principles of Chinese traditional herbs and their structure-activity relationship. His research areas in organic chemistry and medicinal chemistry include antimalarial drug qinghaosu, antitumor natural product annonaceous acetogenins, insect antifeedent tonghaosu, and the syntheses of sialic acid and its analogs. His research group has published over 240 papers, book chapters, and 2 monographs in the area of organic chemistry.