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Identification and structural characterization of a new pro-apoptotic cyclic octapeptide cyclosaplin from somatic seedlings of Santalum album L.
- Source :
-
Peptides [Peptides] 2014 Apr; Vol. 54, pp. 148-58. Date of Electronic Publication: 2014 Feb 03. - Publication Year :
- 2014
-
Abstract
- Small cyclic peptides exhibiting potent biological activity have great potential for anticancer therapy. An antiproliferative cyclic octapeptide, cyclosaplin was purified from somatic seedlings of Santalum album L. (sandalwood) using gel filtration and RP-HPLC separation process. The molecular mass of purified peptide was found to be 858 Da and the sequence was determined by MALDI-ToF-PSD-MS as 'RLGDGCTR' (cyclic). The cytotoxic activity of the peptide was tested against human breast cancer (MDA-MB-231) cell line in a dose and time-dependent manner. The purified peptide exhibited significant antiproliferative activity with an IC50 2.06 μg/mL. In a mechanistic approach, apoptosis was observed in differential microscopic studies for peptide treated MDA-MB-231 cells, which was further confirmed by mitochondrial membrane potential, DNA fragmentation assay, cell cycle analysis and caspase 3 activities. The modeling and docking experiments revealed strong affinity (kcal/mol) of peptide toward EGFR and procaspase 3. The co-localization studies revealed that the peptide sensitizes MDA-MB-231 cells by possibly binding to EGFR and induces apoptosis. This unique cyclic octapeptide revealed to be a favorable candidate for development of anticancer agents.<br /> (Copyright © 2014 Elsevier Inc. All rights reserved.)
- Subjects :
- Antineoplastic Agents, Phytogenic chemistry
Antineoplastic Agents, Phytogenic pharmacology
Breast Neoplasms drug therapy
Breast Neoplasms pathology
Caspase 3 metabolism
Cell Line, Tumor
DNA Fragmentation drug effects
Dose-Response Relationship, Drug
ErbB Receptors metabolism
Female
Humans
Inhibitory Concentration 50
Membrane Potential, Mitochondrial drug effects
Molecular Docking Simulation
Peptides, Cyclic isolation & purification
Seedlings chemistry
Apoptosis drug effects
Peptides, Cyclic chemistry
Peptides, Cyclic pharmacology
Santalum chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1873-5169
- Volume :
- 54
- Database :
- MEDLINE
- Journal :
- Peptides
- Publication Type :
- Academic Journal
- Accession number :
- 24503375
- Full Text :
- https://doi.org/10.1016/j.peptides.2014.01.023