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Reyser, Thibaud; To, Tung H.; Egwu, Chinedu; Paloque, Lucie; Nguyen, Michel; Hamouy, Alexandre; Stigliani, Jean-luc; Bijani, Christian; Augereau, Jean-michel; Joly, Jean-patrick; Portela, Julien; Havot, Jeffrey; Marque, Sylvain R. A.; Boissier, Jérôme; Robert, Anne; Benoit-vical, Françoise; Audran, Gérard. |
Malaria and schistosomiasis are major infectious causes of morbidity and mortality in the tropical and sub-tropical areas. Due to the widespread drug resistance of the parasites, the availability of new efficient and affordable drugs for these endemic pathologies is now a critical public health issue. In this study, we report the design, the synthesis and the preliminary biological evaluation of a series of alkoxyamine derivatives as potential drugs against Plasmodium and Schistosoma parasites. The compounds (RS/SR)-2F, (RR/SS)-2F, and 8F, having IC50 values in nanomolar range against drug-resistant P. falciparum strains, but also five other alkoxyamines, inducing the death of all adult worms of S. mansoni in only 1 h, can be considered as interesting... |
Tipo: Text |
Palavras-chave: Alkoxyamine; Alkylation; Heme; Malaria; Radical chemistry; Schistosomiasis. |
Ano: 2020 |
URL: https://archimer.ifremer.fr/doc/00648/76024/76920.pdf |
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MENDIBURO,MARÍA JOSE; FLORES,SEBASTIÁN; PIZARRO,FERNANDO; ARREDONDO,MIGUEL. |
Heme oxygenase-1 is a microsomal enzyme that, when induced by stress, protects the cells from oxidative injury. Heme oxygenase-1 participates in the cleavage of the heme ring producing biliverdin, CO and ferrous Fe. The released Fe becomes part of intracellular Fe pool and can be stored in ferritin or released by an iron exporter. The mechanism by which heme enters cells is not completely understood, although it had been suggested that it might be internalized by an endocytosis process. In this study, we expressed a full-length Heme oxygenase-1 cDNA in Caco-2 cells and measured intracellular iron content, heme-iron uptake and transport and immunolocalization of heme oxygenase-1 in these cells. We found that heme oxygenase-1 expressing cells showed... |
Tipo: Journal article |
Palavras-chave: Iron; Heme; Heme oxygenase; Caco-2 cells. |
Ano: 2006 |
URL: http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0716-97602006000100023 |
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