Artemesinin

Publication Title: 
Bulletin of the World Health Organization

Eleven Thai isolates and one West African isolate of Plasmodium falciparum were tested for their susceptibility to the Chinese antimalarial drugs artemisinine (qinghaosu) and artemether. The isolates were cultivated by the Trager-Jensen candle-jar technique and exposed to the action of the drugs for 36-48 hours. Artemisinine inhibited growth of most isolates at 10(-7)-10(-8) mol/litre and artemether at 10(-8) mol/litre (with an initial parasitaemia of 0.5-1.0%).

Author(s): 
Thaithong, S.
Beale, G. H.
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 Journal of Clinical Investigation

Plasmodium falciparum infecting hemoglobin (Hb) H and/or Hb Constant Spring erythrocytes in vitro was relatively more resistant than that infecting normal erythrocytes to artesunate and chloroquine, while the sensitivity to pyrimethamine was unchanged. The 50% inhibitory concentrations (IC50) for artesunate in HbH (alpha-thal 1/alpha-thal 2), HbH (alpha-thal 1/Hb Constant Spring), and homozygous Hb Constant Spring erythrocytes were 4.5 +/- 2.8, 8.5 +/- 3.2, and 2.6 +/- 1.6 nM compared with 0.82 +/- 0.35 nM in normal erythrocytes (P less than 0.002 for all three cases).

Author(s): 
Yuthavong, Y.
Butthep, P.
Bunyaratvej, A.
Fucharoen, S.
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: 
Antimicrobial Agents and Chemotherapy

To determine whether artemether, a derivative of the antimalarial agent qinghaosu, is therapeutically active against Schistosoma mansoni, we determined the in vitro, in vivo, and histopathologic effects of the drug on S. mansoni worms. In vitro, toxic effects of artemether on S. mansoni were not seen at concentrations of less than 100 micrograms/ml. However, in vivo, 30 and 50% reductions in the lengths of male and female worms, respectively, were observed 14 days after treatment. By 56 days worm dimensions had returned to control values.

Author(s): 
Xiao, S. H.
Catto, B. A.
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: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

Sodium artesunate (SA), a synthetic derivative of artemisinin first isolated in China, is a water soluble antimalaria used clinically in China. The jejunum of mouse was mounted in Ussing chambers and bathed in NaCl Ringer. There was a potential difference (PD) across the intestinal wall with the serosa being positive. Addition of SA to the mucosal side of the D-glucose (5.5 mmol/L) NaCl Ringer bathing solution, caused a significant decrease in both PD and short circuit current (I(sc)). However, SA had little effect when added to the glucose free Ringer bathing solution.

Author(s): 
Wang, J. Y.
Yuan, L. Z.
Wang, M. D.
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: 
Memórias Do Instituto Oswaldo Cruz

The action of the ether of artemisinin (artemether) on Schistosoma mansoni in mice and hamsters experimentally infected with the LE strain was studied. In mice, the drug showed high schistosomicidal activity using a single intramuscular dose of 100 mg/kg/day. By the oral route, this dose showed a low activity. Mice treated with a single intramuscular dose of 200 mg/kg/day, and examined 15 days after treatment, presented 100% alteration of the oogram; when examined 45 days after treatment, the oogram was normal.

Author(s): 
Araújo, N.
Kohn, A.
Katz, N.

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