| Texto completo | |
| Autor(es): |
Silva, Adriana Farias
[1]
;
Bastos, Erick Leite
[2]
;
Torres, Marcelo Der Torossian
[1]
;
Costa-da-Silva, Andre Luis
[3]
;
Ioshino, Rafaella Sayuri
[3]
;
Capurro, Margareth Lara
[3]
;
Alves, Flavio Lopes
[4]
;
Miranda, Antonio
[4]
;
Fischer Vieira, Renata de Freitas
[4]
;
Oliveira, Jr., Vani Xavier
[1]
Número total de Autores: 10
|
| Afiliação do(s) autor(es): | [1] Univ Fed ABC, Ctr Ciencias Nat & Humanas, BR-09210170 Santo Andre, SP - Brazil
[2] Univ Sao Paulo, Inst Quim, Dept Quim Fundamental, Sao Paulo - Brazil
[3] Univ Sao Paulo, Inst Ciencias Biomed, Dept Parasitol, BR-05508 Sao Paulo - Brazil
[4] Univ Fed Sao Paulo, Dept Biofis, Sao Paulo - Brazil
Número total de Afiliações: 4
|
| Tipo de documento: | Artigo Científico |
| Fonte: | JOURNAL OF PEPTIDE SCIENCE; v. 20, n. 8, p. 640-648, AUG 2014. |
| Citações Web of Science: | 12 |
| Resumo | |
Angiotensin II (AII) as well as analog peptides shows antimalarial activity against Plasmodium gallinaceum and Plasmodium falciparum, but the exact mechanism of action is still unknown. This work presents the solid-phase synthesis and characterization of eight peptides corresponding to the alanine scanning series of AII plus the amide-capped derivative and the evaluation of the antiplasmodial activity of these peptides against mature P. gallinaceum sporozoites. The Ala screening data indicates that the replacement of either the Ile(5) or the His(6) residues causes minor effects on the in vitro antiplasmodial activity compared with AII, i.e. AII (88%), {[}Ala(6)]-AII (79%), and {[}Ala(5)]-AII (75%). Analogs {[}Ala(3)]-AII, {[}Ala(1)]-AII, and AII-NH2 showed antiplasmodial activity around 65%, whereas the activity of the {[}Ala(8)]-AII, {[}Ala(7)]-AII, {[}Ala(4)]-AII, and {[}Ala(2)]-AII analogs is lower than 45%. Circular dichroism data suggest that AII and the most active analogs adopt a beta-fold conformation in different solutions. All AII analogs, except {[}Ala(4)]-AII and {[}Ala(8)]-AII, show contractile responses and interact with the AT(1) receptor, {[}Ala(5)]-AII and {[}Ala(6)]-AII. In conclusion, this approach is helpful to understand the contribution of each amino acid residue to the bioactivity of AII, opening new perspectives toward the design of new sporozoiticidal compounds. Copyright (C) 2014 European Peptide Society and John Wiley \& Sons, Ltd. (AU) | |
| Processo FAPESP: | 11/23036-5 - Pigmentos betalâmicos de flores: fluorescência e capacidade antirradicalar |
| Beneficiário: | Erick Leite Bastos |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |
| Processo FAPESP: | 11/10823-9 - Compostos antimaláricos derivados da angiotensina II |
| Beneficiário: | Vani Xavier de Oliveira Junior |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |
| Processo FAPESP: | 08/51869-9 - Uma nova perspectiva na prevencao e no tratamento quimioterapico da malaria. |
| Beneficiário: | Vani Xavier de Oliveira Junior |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |