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Science 31 May 1985:
Vol. 228. no. 4703, pp. 1049 - 1055
DOI: 10.1126/science.3887571
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Articles

Science, Vol 228, Issue 4703, 1049-1055
Copyright © 1985 by American Association for the Advancement of Science

articles

Qinghaosu (artemisinin): an antimalarial drug from China

DL Klayman

The herb Artemisia annua has been used for many centuries in Chinese traditional medicine as a treatment for fever and malaria. In 1971, Chinese chemists isolated from the leafy portions of the plant the substance responsible for its reputed medicinal action. This compound, called qinghaosu (QHS, artemisinin), is a sesquiterpene lactone that bears a peroxide grouping and, unlike most other antimalarials, lacks a nitrogen-containing heterocyclic ring system. The compound has been used successfully in several thousand malaria patients in China, including those with both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Derivatives of QHS, such as dihydroqinghaosu, artemether, and the water-soluble sodium artesunate, appear to be more potent than QHS itself. Sodium artesunate acts rapidly in restoring to consciousness comatose patients with cerebral malaria. Thus QHS and its derivatives offer promise as a totally new class of antimalarials.


THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
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Synthesis, Antimalarial Activity, and Intracellular Targets of MEFAS, a New Hybrid Compound Derived from Mefloquine and Artesunate.
F. de Pilla Varotti, A. C. C. Botelho, A. A. Andrade, R. C. de Paula, E. M. S. Fagundes, A. Valverde, L. M. U. Mayer, J. S. Mendonca, M. V. N. de Souza, N. Boechat, et al. (2008)
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Acidity enhances the formation of a persistent ozonide at aqueous ascorbate/ozone gas interfaces.
S. Enami, M. R. Hoffmann, and A. J. Colussi (2008)
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In Vitro Activity of Artemisinin in Combination with Clotrimazole or Heat-treated Amphotericin B against Plasmodium falciparum.
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Induction of Nuclear Translocation of Constitutive Androstane Receptor by Peroxisome Proliferator-activated Receptor {alpha} Synthetic Ligands in Mouse Liver.
D. Guo, J. Sarkar, K. Suino-Powell, Y. Xu, K. Matsumoto, Y. Jia, S. Yu, S. Khare, K. Haldar, M. S. Rao, et al. (2007)
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Biological screening of natural products and drug innovation in China.
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Evidence for the Involvement of Carbon-centered Radicals in the Induction of Apoptotic Cell Death by Artemisinin Compounds.
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Artesunate and artemether are effective fasciolicides in the rat model and in vitro.
J. Keiser, X. Shu-Hua, M. Tanner, and J. Utzinger (2006)
J. Antimicrob. Chemother. 57, 1139-1145
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Antimalarial Artemisinin Drugs Induce Cytochrome P450 and MDR1 Expression by Activation of Xenosensors Pregnane X Receptor and Constitutive Androstane Receptor.
O. Burk, K. A. Arnold, A. K. Nussler, E. Schaeffeler, E. Efimova, B. A. Avery, M. A. Avery, M. F. Fromm, and M. Eichelbaum (2005)
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COMPARISON OF THE BIOEQUIVALENCE OF THREE ORAL FORMULATIONS OF DIHYDROARTEMISININ BASED ON EX VIVO BLOOD SCHIZONTOCIDAL ACTIVITIES AGAINST PLASMODIUM FALCIPARUM.
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PHARMACOKINETIC STUDY OF ARTEMISININ AFTER ORAL INTAKE OF A TRADITIONAL PREPARATION OF ARTEMISIA ANNUA L. (ANNUAL WORMWOOD).
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Am J Trop Med Hyg 70, 128-132
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Neurotoxic Mode of Action of Artemisinin.
G. Schmuck, E. Roehrdanz, R. K. Haynes, and R. Kahl (2002)
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Carrier-Mediated Partitioning of Artemisinin into Plasmodium falciparum-Infected Erythrocytes.
N. Vyas, B. A. Avery, M. A. Avery, and C. M. Wyandt (2002)
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Potentiation of Artemisinin Activity against Chloroquine-Resistant Plasmodium falciparum Strains by Using Heme Models.
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Artemisinin, an Endoperoxide Antimalarial, Disrupts the Hemoglobin Catabolism and Heme Detoxification Systems in Malarial Parasite.
A. V. Pandey, B. L. Tekwani, R. L. Singh, and V. S. Chauhan (1999)
J. Biol. Chem. 274, 19383-19388
   Abstract »    Full Text »    PDF »
High In Situ Rat Intestinal Permeability of Artemisinin Unaffected by Multiple Dosing and with No Evidence of P-glycoprotein Involvement.
U. S. H. Svensson, R. Sandström, O. Carlborg, H. Lennernäs, and M. Ashton (1999)
Drug Metab. Dispos. 27, 227-232
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Metabolism of beta -Arteether to Dihydroqinghaosu by Human Liver Microsomes and Recombinant Cytochrome P450.
J. M. Grace, A. J. Aguilar, K. M. Trotman, and T. G. Brewer (1998)
Drug Metab. Dispos. 26, 313-317
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Artemisinin Pharmacokinetics is Time-Dependent during Repeated Oral Administration in Healthy Male Adults.
M. Ashton, T. N. Hai, N. D. Sy, D. X. Huong, N. Van Huong, N. T. Niêu, and L. D. Công (1998)
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