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Scientific Articles

Hyperparasitaemia and low dosing are an important source of anti-malarial drug resistance

November 25, 2009 - 16:38 -- Ingeborg van Schayk
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Author(s): 
Nicholas J White, Wirichada Pongtavornpinyo, Richard J Maude, Sompob Saralamba, Ricardo Aguas, Kasia Stepniewska, Sue J Lee, Arjen M Dondorp, Lisa J White, Nicholas PJ Day
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Malaria Journal 2009, 8:253 (11 November 2009)

The probability of de-novo resistant malaria parasites surviving and transmitting depends on the relationship between their degree of resistance and the blood concentration profiles of the anti-malarial drug to which they are exposed. The conditions required for the in-vivo selection of de-novo emergent resistant malaria parasites were examined and relative probabilities assessed.

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Spatial risk profiling of Plasmodium falciparum parasitaemia in a high endemicity area in Cote d'Ivoire

November 25, 2009 - 15:54 -- Ingeborg van Schayk
Author(s): 
Giovanna Raso, Kigbafori D Silue, Penelope Vounatsou, Burton H Singer, Ahoua Yapi, Marcel Tanner, Juerg Utzinger, Eliezer K N'Goran
Reference: 
Malaria Journal 2009, 8:252 (11 November 2009)

The objective of this study was to identify demographic, environmental and socioeconomic risk factors and spatial patterns of Plasmodium falciparum parasitaemia in a high endemicity area of Africa, and to specify how this information can facilitate improved malaria control at the district level.

Synthesis of 9-anilinoacridine triazines as new class of hybrid antimalarial agents.

November 18, 2009 - 13:00 -- Patrick Sampao
Author(s): 
Ashok Kumar, Kumkum Srivastava, S. Raja Kumar, S.K. Puri, Prem M.S. Chauhan
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 19, Issue 24, 15 December 2009, Pages 6996-6999, doi:10.1016/j.bmcl.2009.10.010

There is challenge and urgency to synthesize cost-effective chemotherapeutic agents for treatment of malarianext term after the widespread development of resistance to CQ. In the present study, we synthesized a new series of hybrid 9-anilinoacridine triazines using the cheap chemicals 6,9-dichloro-2-methoxy acridine and cyanuric chloride.

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Cell-based optimization of novel benzamides as potential antimalarial leads.

November 18, 2009 - 12:57 -- Patrick Sampao
Author(s): 
Tao Wu, Advait Nagle, Tomoyo Sakata, Kerstin Henson, Rachel Borboa, Zhong Chen, Kelli Kuhen, David Plouffe, Elizabeth Winzeler, Francisco Adrian, Tove Tuntland, Jonathan Chang, Susan Simerson, Steven Howard, Jared Ek, John Isbell, Xianming Deng, Nathanael S. Gray, David C. Tully, Arnab K. Chatterjee
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 19, Issue 24, 15 December 2009, Pages 6970-6974, doi:10.1016/j.bmcl.2009.10.050

Screening our in-house compound collection using a cell based Plasmodium falciparum proliferation assay we discovered a known pan-kinase inhibitor scaffold as a hit. Further optimization of this series led us to a novel benzamide scaffold which was devoid of human kinase activity while retaining its antiplasmodial activity. The evolution of this compound series leading to optimized candidates with good cellular potency against multiple strains as well as decent in vivo profile is described in this Letter.

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Anti-cancer effects of artesunate in a panel of chemoresistant neuroblastoma cell lines.

November 18, 2009 - 12:56 -- Kabogo Ndegwa
Author(s): 
Martin Michaelis, Malte C. Kleinschmidt, Susanne Barth, Florian Rothweiler, Janina Geiler, Rainer Breitling, Bernd Mayer, Hedwig Deubzer, Olaf Witt, Jörg Kreuter, Hans Wilhelm Doerr, Jaroslav Cinatl, Jindrich Cinatl Jr.
Reference: 
Biochemical Pharmacology, Volume 79, Issue 2, 15 January 2010, Pages 130-136, doi:10.1016/j.bcp.2009.08.013

Artemisinin derivatives are well-tolerated anti-malaria drugs that also exert anti-cancer activity. Here, we investigated artemisinin and its derivatives dihydroartemisinin and artesunate in a panel of chemosensitive and chemoresistant human neuroblastoma cells as well as in primary neuroblastoma cultures.

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Synthesis and structure–activity relationships of cassiarin A as potential antimalarials with vasorelaxant activity.

November 18, 2009 - 12:54 -- Kabogo Ndegwa
Author(s): 
Hiroshi Morita, Yuichiro Tomizawa, Jun Deguchi, Tokio Ishikawa, Hiroko Arai, Kazumasa Zaima, Takahiro Hosoya, Yusuke Hirasawa, Takayuki Matsumoto, Katsuo Kamata, Wiwied Ekasari, Aty Widyawaruyanti, Tutik Sri Wahyuni, Noor Cholies Zaini, Toshio Honda.
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Bioorganic & Medicinal Chemistry, Volume 17, Issue 24, 15 December 2009, Pages 8234-8240, doi:10.1016/j.bmc.2009.10.013

Cassiarin A 1, a tricyclic alkaloid, isolated from the leaves of Cassia siamea (Leguminosae), shows powerful antimalarial activity against Plasmodium falciparum in vitro as well as P. berghei in vivo, which may be valuable leads for novel antimalarials.

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Anti-tumoral activity of imidazoquines, a new class of antimalarials derived from primaquine.

November 18, 2009 - 12:53 -- Patrick Sampao
Author(s): 
Iva Fernandes, Nuno Vale, Victor de Freitas, Rui Moreira, Nuno Mateus, Paula Gomes.
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 19, Issue 24, 15 December 2009, Pages 6914-6917, doi:10.1016/j.bmcl.2009.10.081

The growth inhibitory activity of imidazoquines, antimalarial imidazolidin-4-ones derived from primaquine, on human cancer cell lines HT-29, Caco-2, and MCF-7 has been evaluated.

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Transport of purines and purine salvage pathway inhibitors by the Plasmodium falciparum equilibrative nucleoside transporter PfENT1.

November 18, 2009 - 12:51 -- Kabogo Ndegwa
Author(s): 
Paul M. Riegelhaupt, María B. Cassera, Richard F.G. Fröhlich, Keith Z. Hazleton, Jonathan J. Hefter, Vern L. Schramm, Myles H. Akabas
Reference: 
Molecular and Biochemical Parasitology, Volume 169, Issue 1, January 2010, Pages 40-49, doi:10.1016/j.molbiopara.2009.10.001

Plasmodium falciparum is a purine auxotroph. The transport of purine nucleosides and nucleobases from the host erythrocyte to the parasite cytoplasm is essential to support parasite growth. P. falciparum equilibrative nucleoside transporter 1 (PfENT1) is a major route for purine transport across the parasite plasma membrane. Malarial parasites are sensitive to inhibitors of purine salvage pathway enzymes. The immucillin class of purine nucleoside phosphorylase inhibitors and the adenosine analog, tubercidin, block growth of P. falciparum under in vitro culture conditions. We sought to determine whether these inhibitors utilize PfENT1 to gain access to the parasite cytosol.

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In Vitro Activities of Piperaquine, Lumefantrine, and Dihydroartemisinin in Kenyan Plasmodium falciparum Isolates and Polymorphisms in pfcrt and pfmdr1.

November 18, 2009 - 12:47 -- Patrick Sampao
Author(s): 
Leah Mwai, Steven M. Kiara, Abdi Abdirahman, Lewa Pole, Anja Rippert, Abdi Diriye, Pete Bull, Kevin Marsh, Steffen Borrmann, and Alexis Nzila
Reference: 
Antimicrobial Agents and Chemotherapy, December 2009, p. 5069-5073, Vol. 53, No. 12, doi:10.1128/AAC.00638-09

We have analyzed the in vitro chemosensitivity profiles of 115 Kenyan isolates for chloroquine (CQ), piperaquine, lumefantrine (LM), and dihydroartemisinin in association with polymorphisms in pfcrt at codon 76 and pfmdr1 at codon 86, as well as with variations of the copy number of pfmdr1.

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Transcriptomic Profiling of the Saccharomyces cerevisiae Response to Quinine Reveals a Glucose Limitation Response Attributable to Drug-Induced Inhibition of Glucose Uptake

November 18, 2009 - 12:43 -- Patrick Sampao
Author(s): 
Sandra C. dos Santos, Sandra Tenreiro, Margarida Palma,Jorg Becker, and Isabel Sá-Correia.
Reference: 
Antimicrobial Agents and Chemotherapy, December 2009, p. 5213-5223, Vol. 53, No. 12, doi:10.1128/AAC.00794-09

Quinine has been employed in the treatment of malaria for centuries and is still used against severe Plasmodium falciparum malaria. However, its interactions with the parasite remain poorly understood and subject to debate. In this study, we used the Saccharomyces cerevisiae eukaryotic model to better understand quinine's mode of action and the mechanisms underlying the cell response to the drug.

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