Antimalarials

Publication Title: 
Parasitology Research

The absence of a vaccine and the rampant resistance to almost all antimalarial drugs have accentuated the urgent need for new antimalarial drugs and drug targets for both prophylaxis and chemotherapy. The aim of the study was to discover effective plant extracts against Plasmodium falciparum. In the present study, the hexane, chloroform, ethyl acetate, acetone, and methanol extracts of Citrus sinensis (peel), Leucas aspera, Ocimum sanctum, Phyllanthus acidus (leaf), Terminalia chebula (seed) were tested for their antimalarial activity against chloroquine (CQ)-sensitive (3D7) strain of P.

Author(s): 
Bagavan, Asokan
Rahuman, Abdul Abdul
Kamaraj, Chinnaperumal
Kaushik, Naveen Kumar
Mohanakrishnan, Dinesh
Sahal, Dinkar
Publication Title: 
PLoS pathogens

A new generation of strategies is evolving that aim to block malaria transmission by employing genetically modified vectors or mosquito pathogens or symbionts that express anti-parasite molecules. Whilst transgenic technologies have advanced rapidly, there is still a paucity of effector molecules with potent anti-malaria activity whose expression does not cause detrimental effects on mosquito fitness. Our objective was to examine a wide range of antimicrobial peptides (AMPs) for their toxic effects on Plasmodium and anopheline mosquitoes.

Author(s): 
Carter, Victoria
Underhill, Ann
Baber, Ibrahima
Sylla, Lakamy
Baby, Mounirou
Larget-Thiery, Isabelle
Zettor, AgnËs
Bourgouin, Catherine
Langel, Ulo
Faye, Ingrid
Otvos, Laszlo
Wade, John D.
Coulibaly, Mamadou B.
Traoré, Sekou F.
Tripet, Frederic
Eggleston, Paul
Hurd, Hilary
Publication Title: 
Journal of the Royal Society of Medicine

With the current increase of international travel and increasing drug resistance, United Kingdom residents stand a high risk of contracting malaria when they visit endemic countries. The development of anti-malarial agents from old traditional plant remedies to modern synthetic drugs is briefly reviewed. Resistance to the latter has spread rapidly since the 1950s, culminating in the widespread distribution of multiple drug-resistant strains of Plasmodium falciparum in most endemic areas.

Author(s): 
Peters, W.
Publication Title: 
The American Journal of Clinical Nutrition

Young female mice were fed torula-yeast-based diets deficient in vitamin E or selenium or supplemented with cod-liver oil to determine the effect of host antioxidant status on the therapeutic efficacy of the Chinese traditional antimalarial drug qinghaosu (QHS), a sesquiterpene endoperoxide. Vitamin E deficiency enhanced the antimalarial action of QHS against Plasmodium yoelii, both in terms of decreased parasitemia and improved survival but Se deficiency did not.

Author(s): 
Levander, O. A.
Ager, A. L.
Morris, V. C.
May, R. G.
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

TLC scanning technique was found to have good specificity for studying the absorption and distribution of artemether in rats. Plasma or tissue homogenates 0.2-1.0 ml were placed in glass extraction tubes and water was added to make 1.0 ml. Each sample was extracted 3 times with 4 ml mixed organic solvent (n-pentane: dichloromethane = 1:1, vol:vol). The organic layers of 3 extractions were combined and evaporated. The residue was dissolved in 100-300 microliters of ethylacetate and spotted on TLC plates.

Author(s): 
Jiang, J. R.
Zou, C. D.
Shu, H. L.
Zeng, Y. L.
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

Ultrastructural changes in Plasmodium gallinaceum oocysts and sporozoites were studies after 5 antimalarials (pyrimethamine, primaquine, artemisinine, 5-p-fluorobenzoxyl-primaquine citrate and nitroquine) were administered to Aedes albopictus. Obvious disfigurement, such as abnormal vacuoles of various sizes in the cytoplasma, thickened oocyst capsules and damaged sporozoite pellical membranes were found in many oocysts and sporozoites in the mosquitoes.

Author(s): 
Hu, C. R.
Chen, P. H.
Chen, J. M.
Huang, Q.
Publication Title: 
Antimicrobial Agents and Chemotherapy

The antimalarial compound qinghaosu (artemisinin) was tested in vitro for the ability to inhibit plaque formation by Toxoplasma gondii in fibroblasts. Qinghaosu at 0.4 microgram/ml for 5 days eliminated all plaques and microscopic foci of T. gondii. At 1.3 micrograms/ml for 14 days, qinghaosu completely eliminated T. gondii. Pretreatment of host cells or T. gondii with qinghaosu had no effect on T. gondii growth. There was no apparent toxicity to human fibroblasts in long-term studies.

Author(s): 
Ke, O. Y.
Krug, E. C.
Marr, J. J.
Berens, R. L.
Publication Title: 
Antimicrobial Agents and Chemotherapy

The susceptibility of Pneumocystis carinii to artemisinin (qinghaosu) was determined in short-term primary culture. In untreated cultures, trophozoites increased an average of fivefold over 4 days. Inhibition of parasite growth in cultures treated with artemisinin at concentrations as low as 0.5 microM was seen. In contrast, artemisinin concentrations up to 100 microM had no effect on feeder layer cells.

Author(s): 
Merali, S.
Meshnick, S. R.
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

The effects of alpha-dimethylamino-cyclohexoxyl-dimethyl gallium (DCDG), a new antimalarial drug developed in China, on the ultrastructure of murine malaria parasites in vivo was studied in comparison with those of chloroquine (CQ) and artemisinin (Art). All these 3 antimalarials were administered ig to mice at dosages of 1-3, 40-80, and 200-400 mg.kg-1 for DCDG, CQ, and Art respectively, based on a similar intensity of morphological changes in the parasites. Blood samples were collected for electron microscopy from 15 min to 48 h after medication.

Author(s): 
Yan, G. H.
Wang, G. J.
Li, Y. C.
Publication Title: 
Memórias Do Instituto Oswaldo Cruz

The vast majority of the 1-2 million malaria associated deaths that occur each year are due to anemia and cerebral malaria (the attachment of erythrocytes containing mature forms of Plasmodium falciparum to the endothelial cells that line the vascular beds of the brain). A "model system" for the study of cerebral malaria employs amelanotic melanoma cells as the "target" cells in an in vitro cytoadherence assay.

Author(s): 
Smith, H.
Crandall, I.
Prudhomme, J.
Sherman, I. W.

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