How Chinese scientists discovered qinghaosu (artemisinin) and developed its derivatives? What are the future perspectives?

Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
Médecine tropicale: revue du Corps de santé colonial 02/1998; 58(3 Suppl):9-12.
Source: PubMed


Since the middle of this century and especially since the 1960s and 1970s. Chinese scientists have put considerable effort and resources into the search for new antimalarial compounds extracted from Chinese traditional herbs. Archaeological findings indicate that qinghao (Artemisia annua L.) has been used as a traditional remedy in China for over two thousand years. Its antimalarial principle was finally isolated in 1971 and named artemisinin or qinghaosu (meaning the principle of qinghao in Chinese). Its rapid action, low toxicity and powerful effect against falciparum malaria made it a favored subject for research. In 1976, the unique structure of the molecule, characterized by an endoperoxide and an alternative O-C-O-C segment, was identified. The specific lactone reduction discovered during the determination of the structure opened the way for the synthesis of qinghaosu derivatives, and thereafter a series of more active and more oil- or water-soluble derivatives was developed. Subsequent studies of the structure/activity relationship led to the discovery of dihydroartemisinin, artemether and artesunate. Now qinghaosu and these three derivatives are being used around the world as effective new antimalarial drugs in the fight against falciparum malaria, including multi-drug-resistant Plasmodium falciparum. At the present time new qinghaosu analogues or derivatives are being developed and studies of their structure/activity relationships, their antimalarial mechanisms, their interaction with ferrous ions and the DNA damage associated with these processes are being actively pursued. In addition, recent studies also indicate that some qinghaosu derivatives have other bioactivities, including antiparasitic (against Schistosoma japonicum, Toxoplasma gondii and so on) and anticancer activities. Research into qinghaosu and its derivatives has already produced and will no doubt continue to produce results of the utmost importance in the fight against malaria and other diseases.

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    Evidence-based Complementary and Alternative Medicine 04/2014; 2014:525340. DOI:10.1155/2014/525340 · 1.88 Impact Factor
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    • "In recent years, studies have demonstrated that artemisinin and its derivatives had a significant cytotoxic effects toward cancer cells and could reverse multiple drug resistance of tumors [8]–[10]. Artemisinin was first isolated from leaves of Artemisia annua, a Chinese traditional herb, by Chinese pharmacists in 1971 [11]. Artemether, the methyl ether derivative of artemisinin, is widely used in the therapy of malaria [12]. "
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    PLoS ONE 04/2013; 8(4):e60834. DOI:10.1371/journal.pone.0060834 · 3.23 Impact Factor
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    • "Reduction of the lactone in dihydroartemisinin and artemether has led to increased oil solubility, whereas the acidic moiety lends water solubility to artesunate [88, 89]. Consequently, artemisinin derivatives, such as dihydroartemisinin, artemether, and artesunate, are developed and being used around the world as effective antimalarial drugs, including those targeted against multidrug-resistant Plasmodium falciparum [90]. These derivatives appear to be more potent than the parent compound and the most rapidly acting among all other antimalarial agents [91]. "
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