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Artemisinin

The comparative antimalarial properties of weak base and neutral synthetic ozonides

December 22, 2009 - 13:35 -- Patrick Sampao
Author(s): 
Yuanqing Tang, Sergio Wittlin, Susan A. Charman, Jacques Chollet, Francis C.K. Chiu, Julia Morizzi, Lisa M. Johnson, Josefina Santo Tomas, Christian Scheurer, Chistopher Snyder, Lin Zhou, Yuxiang Dong, William N. Charman, Hugues Matile, Heinrich Urwyler, Arnulf Dorn, Jonathan L. Vennerstrom
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 2, 15 January 2010, Pages 563-566

Thirty-three N-acyl 1,2,4-dispiro trioxolanes (secondary ozonides) were synthesized. For these ozonides, weak base functional groups were not required for high antimalarial potency against Plasmodium falciparum in vitro, but were necessary for high antimalarial efficacy in Plasmodium berghei-infected mice. A wide range of Log P/DpH 7.4 values were tolerated, although more lipophilic ozonides tended to be less metabolically stable.

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Continued cytoadherence of Plasmodium falciparum infected red blood cells after antimalarial treatment

December 10, 2009 - 09:22 -- Patrick Sampao
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Author(s): 
Katie R. Hughes, Giancarlo A. Biagini, Alister G. Craig
Reference: 
Molecular and Biochemical Parasitology, Volume 169, Issue 2, February 2010, Pages 71-78

These findings show that cytoadherence, a potential pathogenic property of P. falciparum infected red blood cells, continues long after the parasite has been killed.

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Fabrication of drug nanoparticles by evaporative precipitation of nanosuspension

November 26, 2009 - 07:15 -- Patrick Sampao
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Author(s): 
M. Kakran, N.G. Sahoo, L. Li, Z. Judeh, Y. Wang, K. Chong, L. Loh.
Reference: 
International Journal of Pharmaceutics, Volume 383, Issues 1-2, 4 January 2010, Pages 285-292, doi:10.1016/j.ijpharm.2009.09.030

Evaporative precipitation of nanosuspension (EPN) was used to fabricate nanoparticles of a poorly water-soluble antimalarial drug, artemisinin (ART), with the aim of enhancing its dissolution rate. We investigated the nanoparticle fabrication of ART via a full factorial experimental design considering the effects of drug concentration and solvent to antisolvent ratio on the physical, morphological and dissolution properties of ART.

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Review; Artemisinin-based combination therapies: a vital tool in efforts to eliminate malaria

November 18, 2009 - 12:42 -- Kabogo Ndegwa
Author(s): 
Richard T. Eastman1 & David A. Fidock1
Reference: 
Nature Reviews Microbiology 7, 864-874 (December 2009) doi:10.1038/nrmicro2239

Plasmodium falciparum resistance to chloroquine and sulphadoxine–pyrimethamine has led to the recent adoption of artemisinin-based combination therapies (ACTs) as the first line of treatment against malaria. ACTs comprise semisynthetic artemisinin derivatives paired with distinct chemical classes of longer acting drugs. These artemisinins are exceptionally potent against the pathogenic asexual blood stages of Plasmodium parasites and also act on the transmissible sexual stages.

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ABC - antibiotics-based combinations for the treatment of severe malaria?

November 18, 2009 - 12:31 -- Kabogo Ndegwa
Author(s): 
Harald Noedl.
Reference: 
Trends in Parasitology, Volume 25, Issue 12, December 2009, Pages 540-544, doi:10.1016/j.pt.2009.09.001.

Almost one million people die of severe malaria every year. In recent years, artemisinin-based combination therapies have become the backbone of the treatment of uncomplicated falciparum malaria and have helped to reduce the burden of malaria in large parts of the malaria-endemic world. However, the treatment of severe malaria,the clinical syndrome responsible for most malaria-associated deaths, remains largely unaffected by this development.

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Review: Pharmacokinetic and Toxicological Profile of Artemisinin Compounds: An Update

November 13, 2009 - 11:22 -- Ingeborg van Schayk
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Author(s): 
Bikash Medhi, Sazal Patyar, Ramya S. Rao, Prasad Byrav DS, Ajay Prakash
Reference: 
Pharmacology 2009;84:323-332

Artemisinin has been used effectively in malaria treatment. With the emerging resistance to malaria, the optimum and judicial use of the drug has become important.

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