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Artemisinins

NOT Open Access | Interactions between Artemisinins and other Antimalarial Drugs in Relation to the Cofactor Model—A Unifying Proposal for Drug Action

December 6, 2012 - 09:19 -- NOT Open Access
Author(s): 
Richard K. Haynes, Kwan-Wing Cheu, Diego Monti, et al.
Reference: 
ChemMedChem, Volume 7, Issue 12, pages 2204–2226, December 2012
MalariaWorld

Artemisinins are proposed to act in the malaria parasite cytosol by oxidizing dihydroflavin cofactors of redox-active flavoenzymes, and under aerobic conditions by inducing their autoxidation.

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Lack of Association of the S769N Mutation in Plasmodium falciparum SERCA (PfATP6) with Resistance to Artemisinins

April 13, 2012 - 13:50 -- Patrick Sampao
Author(s): 
Long Cui, Zenglei Wang, Hongying Jiang, Daniel Parker, Haiyan Wang, Xin-Zhuan Su and Liwang Cui
Reference: 
Antimicrob. Agents Chemother. May 2012 vol. 56 no. 5 2546-2552

MalariaWorldIn this study, we used an allelic exchange strategy to engineer parasite lines carrying the S769N mutations in P. falciparum strain 3D7 and evaluated whether introduction of this mutation modulated parasite sensitivity to ART derivatives.

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A Partial Convergence in Action of Methylene Blue and Artemisinins: Antagonism with Chloroquine, a Reversal with Verapamil, and an Insight into the Antimalarial Activity of Chloroquine

October 6, 2011 - 09:39 -- Kabogo Ndegwa
Author(s): 
Richard K. Haynes, Kwan-Wing Cheu, Ka-Yan Li, Maggie Mei-Ki Tang, Ho-Ning Wong, Min-Jiao Chen, Zu-Feng Guo, Zhi-Hong Guo, Paolo Coghi, Diego Monti
Reference: 
ChemMedChem, Volume 6, Issue 9, pages 1603–1615, September 5, 2011

MalariaWorldArtemisinins rapidly oxidize leucomethylene blue (LMB) to methylene blue (MB); they also oxidize dihydroflavins such as the reduced conjugates RFH2 of riboflavin (RF), and FADH2 of the cofactor flavin adenine dinucleotide (FAD), to the corresponding flavins.

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In vitro activity of new artemisinin derivatives against Plasmodium falciparum clinical isolates from Gabon

April 12, 2011 - 07:46 -- Kabogo Ndegwa
Author(s): 
Jana Held, Shahid A. Soomro, Peter G. Kremsner, F. Herwig Jansen, Benjamin Mordmüller
Reference: 
International Journal of Antimicrobial Agents Volume 37, Issue 5, May 2011, Pages 485-488

Nowadays, artemisinins are the mainstay of malaria treatment, but initial indications of resistance against clinically used derivatives are present.

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Reactions of Antimalarial Peroxides with Each of Leucomethylene Blue and Dihydroflavins: Flavin Reductase and the Cofactor Model Exemplified

March 9, 2011 - 08:30 -- Kabogo Ndegwa
Author(s): 
Haynes, R. K., Cheu, K.-W., Tang, M. M.-K., Chen, M.-J., Guo, Z.-F., Guo, Z.-H., Coghi, P. and Monti, D
Reference: 
ChemMedChem, Special Issue: Rare & Neglected Diseases, Volume 6, Issue 2, pages 279–291, February 7, 2011

Flavin adenine dinucleotide (FAD) is reduced by NADPH–E. coli flavin reductase (Fre) to FADH2 in aqueous buffer at pH 7.4 under argon.

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Review: Plasmodium sensitivity to artemisinins: magic bullets hit elusive targets

February 2, 2011 - 13:53 -- Patrick Sampao
Author(s): 
Xavier C. Ding, Hans-Peter Beck, Giovanna Raso
Reference: 
Trends in Parasitology, Volume 27, Issue 2, February 2011, Pages 73-81

In this review different models of artemisinins’ molecular action are briefly presented, focusing on recent advances, and the evidence of potential association between various gene polymorphisms and artemisinin resistance is comprehensively reviewed.

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Review: Toxicokinetic and toxicodynamic (TK/TD) evaluation to determine and predict the neurotoxicity of artemisinins

December 16, 2010 - 08:30 -- Patrick Sampao
Author(s): 
Qigui Li, Mark Hickman
Reference: 
Toxicology, Volume 279, Issues 1-3, 11 January 2011, Pages 1-9

These findings support a recently published WHO guide for malaria treatment with artemisinin regimens, such as artemisinin-based combination therapies and injectable artesunate, to avoid neurotoxicity.

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Facile Oxidation of Leucomethylene Blue and Dihydroflavins by Artemisinins: Relationship with Flavoenzyme Function and Antimalarial Mechanism of Action

September 16, 2010 - 18:23 -- Ingeborg van Schayk
Author(s): 
Richard K. Haynes Prof. Dr., Wing-Chi Chan, Ho-Ning Wong Dr., Ka-Yan Li, Wai-Keung Wu, Kit-Man Fan, Herman H. Y. Sung Dr., Ian D. Williams Prof. Dr., Davide Prosperi Dr., Sergio Melato Dr., Paolo Coghi Dr., Diego Monti Prof. Dr.
Reference: 
ChemMedChem Volume 5, Issue 8, pages 1282–1299, August 2, 2010

The antimalarial drug methylene blue (MB) affects the redox behaviour of parasite flavin-dependent disulfide reductases such as glutathione reductase (GR) that control oxidative stress in the malaria parasite.

Selective toxicity of dihydroartemisinin on human CD34+ erythroid cell differentiation

September 14, 2010 - 13:03 -- Patrick Sampao
Author(s): 
Sara Finaurini, Luisa Ronzoni, Alessandra Colancecco, Alessandra Cattaneo, Maria Domenica Cappellini, Stephen A. Ward, Donatella Taramelli
Reference: 
Toxicology, Volume 276, Issue 2, 9 October 2010, Pages 128-134

This is the first demonstration that DHA affects human erythropoiesis in vitro, in a dose- and time-dependent manner; the target population seems to be the pro-erythroblast and basophilic erythroblast stage, suggesting that DHA toxicity is limited to primitive human erythropoiesis.

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