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Alkoxyamines Designed as Potential Drugs against Plasmodium and Schistosoma Parasites ArchiMer
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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Heme oxygenase 1 overexpression increases iron fluxes in Caco-2 cells Biol. Res.
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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Carbon monoxide: from toxin to endogenous modulator of cardiovascular functions BJMBR
Johnson,R.A.; Kozma,F.; Colombari,E..
Carbon monoxide (CO) is a pollutant commonly recognized for its toxicological attributes, including CNS and cardiovascular effects. But CO is also formed endogenously in mammalian tissues. Endogenously formed CO normally arises from heme degradation in a reaction catalyzed by heme oxygenase. While inhibitors of endogenous CO production can raise arterial pressure, heme loading can enhance CO production and lead to vasodepression. Both central and peripheral tissues possess heme oxygenases and generate CO from heme, but the inability of heme substrate to cross the blood brain barrier suggests the CNS heme-heme oxygenase-CO system may be independent of the periphery. In the CNS, CO apparently acts in the nucleus tractus solitarii (NTS) promoting changes in...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Carbon monoxide; Heme; Heme oxygenase; Blood pressure; Central nervous system; Vascular tone.
Ano: 1999 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-879X1999000100001
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