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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

Encapsulation of metalloporphyrins improves their capacity to block the viability of the human malaria parasite Plasmodium falciparum

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Autor(es):
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Alves, Eduardo [1, 2] ; Iglesias, Bernardo A. [3] ; Deda, Daiana K. [3] ; Budu, Alexandre [1] ; Matias, Tiago A. [3] ; Bueno, Vania B. [3] ; Maluf, Fernando V. [4] ; Guido, Rafael V. C. [4] ; Oliva, Glaucius [4] ; Catalani, Luiz H. [3] ; Araki, Koiti [3] ; Garcia, Celia R. S. [1]
Número total de Autores: 12
Afiliação do(s) autor(es):
[1] Univ Sao Paulo, Dept Fisiol, Inst Biociencias, BR-05508 Sao Paulo - Brazil
[2] Univ Sao Paulo, Dept Parasitol, Inst Ciencias Biomed, BR-05508 Sao Paulo - Brazil
[3] Univ Sao Paulo, Inst Quim, Dept Quim Fundamental, BR-05508 Sao Paulo - Brazil
[4] Univ Sao Paulo, Ctr Biotecnol Mol Estrutural, Inst Fis Sao Carlos, BR-05508 Sao Paulo - Brazil
Número total de Afiliações: 4
Tipo de documento: Artigo Científico
Fonte: Nanomedicine-Nanotechnology Biology and Medicine; v. 11, n. 2, p. 351-358, FEB 2015.
Citações Web of Science: 8
Resumo

Several synthetic metallated protoporphyrins (M-PPIX) were tested for their ability to block the cell cycle of the lethal human malaria parasite Plasmodium falciparum. After encapsulating the porphyrin derivatives in micro-and nanocapsules of marine atelocollagen, their effects on cultures of red blood cells infected (RBC) with P. falciparum were verified. RBCs infected with synchronized P. falciparum incubated for 48 h showed a toxic effect over a micromolar range. Strikingly, the IC50 of encapsulated metalloporphyrins reached nanomolar concentrations, where Zn-PPIX showed the best antimalarial effect, with an IC50 = 330 nM. This value is an 80-fold increase in the antimalarial activity compared to the antimalarial effect of non-encapsulated Zn-PPIX. These findings reveal that the incubation of P. falciparum infected-RBCs with 20 mu M Zn-PPIX reduced the size of hemozoin crystal by 34%, whereas a 28% reduction was noticed with chloroquine, confirming the importance of heme detoxification pathway in drug therapy. From the Clinical Editor: In this study, synthetic metalloporphyrins were tested as therapeutics that target Plasmodium falciparum. The IC50 of encapsulated metalloporphyrins was found to be in the nanomolar concentration range, with encapsulated Zn-PPIX showing an 80-fold increase in its antimalarial activity compared to the non-encapsulated form. (C) 2015 Published by Elsevier Inc. (AU)

Processo FAPESP: 11/51295-5 - Genômica funcional em Plasmodium
Beneficiário:Célia Regina da Silva Garcia
Linha de fomento: Auxílio à Pesquisa - Temático