| Full text | |
| Author(s): |
Der Torossian, Torres Marcelo
[1]
;
Silva, Adriana F.
[1]
;
Alves, Flavio L.
[2]
;
Capurro, Margareth L.
[3]
;
Miranda, Antonio
[2]
;
Xavier, Jr., Oliveira Vani
[1]
Total Authors: 6
|
| Affiliation: | [1] Univ Fed ABC, Ctr Ciencias Nat & Humanas, Santo Andre - Brazil
[2] Univ Fed Sao Paulo, Dept Biofis, Sao Paulo - Brazil
[3] Univ Sao Paulo, Inst Ciencias Biomed 2, Sao Paulo - Brazil
Total Affiliations: 3
|
| Document type: | Journal article |
| Source: | CHEMICAL BIOLOGY & DRUG DESIGN; v. 85, n. 2, p. 163-171, FEB 2015. |
| Web of Science Citations: | 4 |
| Abstract | |
Malaria is an infectious disease responsible for approximately one million deaths annually. The antimalarial effects of angiotensin II and its analogs against Plasmodium gallinaceum and P.falciparum have recently been reported. To evaluate antiplasmodial activity, we synthesized five angiotensin II-restricted analogs containing disulfide bridges. To accomplish this, peptides containing two inserted amino acid residues (cysteine) were synthesized by the Fmoc solid-phase method, purified by liquid chromatography, and characterized by mass spectrometry. Conformational studies were performed by circular dichroism. The results indicated that two of the analogs had higher antiplasmodium activity (92% and 98% activity) than angiotensin II (88% activity), measured by fluorescence microscopy. Results showed that the insertion position must be selected, to preserve the hydrophobic interactions between the non-polar residues, as this affects antiplasmodial activity. The circular dichroism studies suggested that the active analogs as well as the native angiotensin II adopt a -turn conformation in different solutions. This approach provided insight for understanding the effects of restricting the ring size and position on the bioactivity of angiotensin II and provides a new direction for the design of potential chemotherapeutic agents. (AU) | |
| FAPESP's process: | 11/15083-3 - Cyclic Antimalariais Derivates of Angiotensin II |
| Grantee: | Marcelo Der Torossian Torres |
| Support Opportunities: | Scholarships in Brazil - Master |
| FAPESP's process: | 11/10823-9 - Antimalarial compounds derivative from angiotensin II |
| Grantee: | Vani Xavier de Oliveira Junior |
| Support Opportunities: | Regular Research Grants |