Anticancer activity of VmCT1 analogs against MCF-7 cells
| Autor: | Cibele Nicolaski Pedron, Marcelo D. T. Torres, Vani Xavier Oliveira, Giselle Cerchiaro, Roseli Hiromi Sato, Anderson Orzari Ribeiro, Gislaine P. Andrade |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Cell Survival Antimicrobial peptides Peptide Antineoplastic Agents 02 engineering and technology Microscopy Atomic Force Biochemistry Scorpions 03 medical and health sciences Drug Discovery Structure–activity relationship Animals Humans Amino Acid Sequence Peptide sequence Pharmacology chemistry.chemical_classification Chemistry Circular Dichroism Organic Chemistry Wild type 021001 nanoscience & nanotechnology Antimicrobial 030104 developmental biology MCF-7 Cancer cell MCF-7 Cells Molecular Medicine 0210 nano-technology Antimicrobial Cationic Peptides |
| Zdroj: | Chemical biologydrug design. 91(2) |
| ISSN: | 1747-0285 |
| Popis: | Antimicrobial peptides are considered promising drug candidates due to their broad range of activity. VmCT1 (Phe-Leu-Gly-Ala-Leu-Trp-Asn-Val-Ala-Lys-Ser-Val-Phe-NH2 ) is an α-helical antimicrobial peptide that was obtained from the Vaejovis mexicanus smithi scorpion venom. Some of its analogs showed to be as antimicrobial as the wild type, and they were designed for understanding the influence of physiochemical parameters on antimicrobial and hemolytic activity. Some cationic antimicrobial peptides exhibit anticancer activity so VmCT1 analogs were tested to verify the anticancer activity of this family of peptides. The analogs were synthesized, purified, characterized, and the conformational studies were performed. The anticancer activity was assessed against MCF-7 mammary cancer cells. The results indicated that [Glu]7 -VmCT1-NH2 , [Lys]3 -VmCT1-NH2 , and [Lys]7 -VmCT1-NH2 analogs presented moderated helical tendency (0.23-0.61) and tendency of anticancer activity at 25 μmol/L in 24 hr of experiment; and [Trp]9 -VmCT1-NH2 analog that presented low helical tendency and moderated anticancer activity at 50 μmol/L. These results demonstrated that single substitutions on VmCT1 led to different physicochemical features and could assist on the understanding of anticancer activity of this peptide family. |
| Databáze: | OpenAIRE |
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