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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.)

Leishmanicidal activity of Cecropia pachystachya flavonoids: Arginase inhibition and altered mitochondrial DNA arrangement

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Author(s):
Cruz, Ebenezer de Mello [1] ; da Silva, Edson Roberto [2] ; Maquiaveli, Claudia do Carmo [3] ; Sobral Alves, Eliomara Sousa [1] ; Lucon, Jr., Joao Francisco [4] ; Goncalves dos Reis, Matheus Balduino [2] ; Mendes de Toledo, Cleyton Eduardo [5] ; Cruz, Frederico Guare [6] ; Vannier-Santos, Marcos Andre [1]
Total Authors: 9
Affiliation:
[1] CPqGM FIOCRUZ, Ctr Pesquisa Goncalo Moniz, Fundacao Oswaldo Cruz, Lab Biol Parasitaria, BR-40296710 Salvador, BA - Brazil
[2] Univ Sao Paulo, Fac Zootecnia & Engn Alimentos, Dept Vet Med, BR-13635900 Pirassununga, SP - Brazil
[3] Univ Sao Paulo, Fac Med Ribeirao Preto, Dept Fisiol, Programa Posgrad Fisiol, BR-14049900 Ribeirao Preto, SP - Brazil
[4] Univ Sao Paulo, Fac Zootecnia & Engn Alimentos, Programa Posgrad Zootecnia, BR-13635900 Pirassununga, SP - Brazil
[5] Curso Farm, Unidade Ensino Super Inga, BR-87070000 Maringa, Parana - Brazil
[6] Univ Fed Bahia, Inst Quim, Dept Quim Organ, UFBA, BR-40170290 Salvador, BA - Brazil
Total Affiliations: 6
Document type: Journal article
Source: Phytochemistry; v. 89, p. 71-77, MAY 2013.
Web of Science Citations: 26
Abstract

The plant Cecropia pachystachya Trecul is widely used in Brazilian ethnomedicine to treat hypertension, asthma, and diabetes. Arginase is an enzyme with levels that are elevated in these disorders, and it is central to Leishmania polyamine biosynthesis. The aims of this study were to evaluate antileishmanial activity and inhibition of the arginase enzyme by C. pachystachya extracts, and to study changes in cellular organization using electron microscopy. The ethanol extract of C. pachystachya was tested on Leishmania (Leishmania) amazonensis promastigote survival/proliferation and arginase activity in vitro. Qualitative ultrastructural analysis was also used to observe changes in cell organization. The major bioactive molecules of the ethanol extract were characterized using liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS). The ethyl acetate fraction of the ethanol extract diminished promastigote axenic growth/survival, inhibited arginase activity, and altered a mitochondrial kinetoplast DNA (K-DNA) array. The bioactive compounds of C pachystachya were characterized as glucoside flavonoids. Orientin (9) (luteolin-8-C-glucoside) was the main component of the methanol-soluble ethyl acetate fraction obtained from the ethanol extract and is an arginase inhibitor (IC50 15.9 mu M). The ethyl acetate fraction was not cytotoxic to splenocytes at a concentration of 200 mu g/mL. In conclusion, C. pachystachya contains bioactive compounds that reduce the growth of L. (L.) amazonensis promastigotes, altering mitochondrial K-DNA arrangement and inhibiting arginase. (C) 2013 Elsevier Ltd. All rights reserved. (AU)

FAPESP's process: 09/08715-3 - New therapeutic targets: the use of recombinant enzymes for screening of drugs for human and veterinary medical interest.
Grantee:Edson Roberto da Silva
Support Opportunities: Regular Research Grants