Cyclic Antimalariais Derivates of Angiotensin II

• Grant number: 11/15083-3
• Support Opportunities: Scholarships in Brazil - Master
• Start date: March 01, 2012
• End date: August 31, 2013
• Field of knowledge: Biological Sciences - Biochemistry - Chemistry of Macromolecules
• Principal Investigator: Vani Xavier de Oliveira Junior
• Grantee: Marcelo Der Torossian Torres
• Host Institution: Centro de Ciências Naturais e Humanas (CCNH). Universidade Federal do ABC (UFABC). Ministério da Educação (Brasil). Santo André , SP, Brazil

Abstract

According to the World Health Organization 250 to 500 million people get malaria each year and of those, about 1-2 million cases result in death. Malaria is a disease caused by protozoa of the genus Plasmodium and transmitted by female Anopheles mosquitoes.Among chemotherapy drugs used to treat the disease, peptide class is highlighted by minimizing side effects and acquired resistance to drugs by protozoa of continuous use. Previous studies of our research group showed antisporozoite activity of angiotensin II (AII). This substance, despite of having a 88% of antiplasmodical action cannot be used as a drug for having pressor activity in the renin-angiotensin system. Thus, some studies have been performed with its analogs, which showed antisporozoite activity between 67% and 87%, and no pressor activity was observed.This project proposes the synthesis of cyclic analogs of AII, aiming to increase the antisporozoite activity of these substances, showing no pressor activity. The analogs will be synthesized by solid phase method, purified by High Performance Liquid Chromatography (HPLC) and characterized by mass spectrometry (LC / ESI-MS). The biological assays to verify the antimalarial activity of these compounds will be performed in P. gallinaceum and P. falciparum. And the conformational studies will be carried out by Circular Dichroism (CD), and probably by nuclear magnetic resonance.

Scientific publications

(5)

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

SILVA, ADRIANA F.; ALVES, FALVIO L.; PEDRON, CIBELE N.; TORRES, MARCELO D. T.; SILVA, LEANDRO S.; PINHEIRO, ANA A. S.; MIRANDA, ANTONIO; OLIVEIRA, JR., VANI X.. Anti-plasmodial activity of bradykinin and analogs. Bioorganic & Medicinal Chemistry Letters, v. 25, n. 16, p. 3311-3313, AUG 15 2015. (11/15083-3, 11/10823-9)

TORRES, MARCELO DER TOROSSIAN; SILVA, ADRIANA FARIAS; ALVES, FLAVIO LOPES; CAPURRO, MARGARETH LARA; MIRANDA, ANTONIO; OLIVEIRA JUNIOR, VANI XAVIER. The Importance of Ring Size and Position for the Antiplasmodial Activity of Angiotensin II Restricted Analogs. INTERNATIONAL JOURNAL OF PEPTIDE RESEARCH AND THERAPEUTICS, v. 20, n. 3, p. 277-287, SEP 2014. (11/15083-3, 11/10823-9)

TOROSSIAN TORRES, MARCELO DER; SILVA, ADRIANA FARIAS; SILVA, LEANDRO DE SOUZA; DE SA PINHEIRO, ANA ACACIA; JR OLIVEIRA, VANI XAVIER. Angiotensin II restricted analogs with biological activity in the erythrocytic cycle of Plasmodium falciparum. JOURNAL OF PEPTIDE SCIENCE, v. 21, n. 1, p. 24-28, JAN 2015. (11/15083-3, 11/10823-9)

DER TOROSSIAN, TORRES MARCELO; SILVA, ADRIANA F.; ALVES, FLAVIO L.; CAPURRO, MARGARETH L.; MIRANDA, ANTONIO; XAVIER, JR., OLIVEIRA VANI. Highly Potential Antiplasmodial Restricted Peptides. CHEMICAL BIOLOGY & DRUG DESIGN, v. 85, n. 2, p. 163-171, FEB 2015. (11/15083-3, 11/10823-9)

RODRIGUES FERREIRA, LUIZ HENRIQUE; SILVA, ADRIANA FARIAS; TOROSSIAN TORRES, MARCELO DER; PEDRON, CIBELE NICOLASKI; CAPURRO, MARGARETH LARA; ALVES, FLAVIO LOPES; MIRANDA, ANTONIO; OLIVEIRA, JR., VANI XAVIER. Effects of Amino Acid Deletion on the Antiplasmodial Activity of Angiotensin II. INTERNATIONAL JOURNAL OF PEPTIDE RESEARCH AND THERAPEUTICS, v. 20, n. 4, p. 553-564, DEC 2014. (11/15083-3, 11/10823-9)