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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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

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Author(s):
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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]
Total Authors: 12
Affiliation:
[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
Total Affiliations: 4
Document type: Journal article
Source: Nanomedicine-Nanotechnology Biology and Medicine; v. 11, n. 2, p. 351-358, FEB 2015.
Web of Science Citations: 8
Abstract

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)

FAPESP's process: 11/51295-5 - Functional genomics in Plasmodium
Grantee:Célia Regina da Silva Garcia
Support Opportunities: Research Projects - Thematic Grants