| Title |
A conjugate of the lytic peptide Hecate and gallic acid: structure, activity against cervical cancer, and toxicity
|
|---|---|
| Published in |
Amino Acids, April 2015
|
| DOI | 10.1007/s00726-015-1980-7 |
| Pubmed ID | |
| Authors |
Paulo R. S. Sanches, Bruno M. Carneiro, Mariana N. Batista, Ana Cláudia S. Braga, Esteban N. Lorenzón, Paula Rahal, Eduardo Maffud Cilli |
| Abstract |
Conjugate compounds constitute a new class of molecules of important biological interest mainly for the treatment of diseases such as cancer. The N-terminus region of cationic peptides has been described as important for their biological activity. The aim of this study was to evaluate the lytic peptide Hecate (FALALKALKKALKKLKKALKKAL) and the effect of conjugating this macromolecule with gallic acid (C7H6O5) in terms of structure, anti-cancer activity, and toxicity. An N-terminus GA-Hecate peptide conjugate was synthesized to provide information regarding the relationship between the amino-terminal region and its charge and the secondary structure and biological activity of the peptide; and the effects of gallic acid on these parameters. Peptide secondary structure was confirmed using circular dichroism (CD). The CD measurements showed that the peptide has a high incidence of α-helical structures in the presence of SDS and LPC, while GA-Hecate presented lower incidence of α-helical structures in the same chemical environment. An evaluation of the anti-cancer activity in HeLa cancer cells indicated that both peptides are active, but that coupling gallic acid at the N-terminus decreased the activity of the free peptide. GA-Hecate showed lower activity in non-tumor keratinocyte cells but higher hemolytic activity. Our findings suggest that the N-terminus of Hecate plays an important role in its activity against cervical cancer by affecting it secondary structure, toxicity, and hemolytic activity. This study highlights the importance of the N-terminus in antitumor activity and could provide an important tool for developing new anti-cancer drugs. |
Mendeley readers
The data shown below were compiled from readership statistics for 32 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Brazil | 1 | 3% |
| Unknown | 31 | 97% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 6 | 19% |
| Researcher | 5 | 16% |
| Student > Bachelor | 5 | 16% |
| Professor > Associate Professor | 3 | 9% |
| Student > Master | 3 | 9% |
| Other | 6 | 19% |
| Unknown | 4 | 13% |
| Readers by discipline | Count | As % |
|---|---|---|
| Biochemistry, Genetics and Molecular Biology | 9 | 28% |
| Medicine and Dentistry | 4 | 13% |
| Chemistry | 3 | 9% |
| Pharmacology, Toxicology and Pharmaceutical Science | 2 | 6% |
| Agricultural and Biological Sciences | 2 | 6% |
| Other | 3 | 9% |
| Unknown | 9 | 28% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 21 September 2015.
All research outputs
#20,292,660
of 22,829,083 outputs
Outputs from Amino Acids
#1,285
of 1,520 outputs
Outputs of similar age
#223,390
of 264,276 outputs
Outputs of similar age from Amino Acids
#22
of 26 outputs
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