Structure-activity relationship studies of Longicalcynin A analogues, as anticancer cyclopeptides

Publication date: Available online 17 November 2019Source: Chemico-Biological InteractionsAuthor(s): Mohammadreza Gholibeikian, Abdolhamid Bamoniri, Mohammad Hassan HoushdarTehrani, Bi Bi Fatemeh Mirjalili, Hamid Reza BijanzadehAbstractCancer has emerged as the main cause of the highest rate of mortality in the world. Drugs used in cancer, although, show some beneficial effects on cancerous organs, demonstrate side effects on other normal tissues. On the other hand, anticancer peptides, being effective on target tissues, should be safe and less harmful on healthy organs, since peptides have several advantages, i.e., high activity, specificity, affinity, being less immunogenic and not accumulate in the body. In the present work, analogues of Longicalcynin A, a naturally occurring anticancer cyclopeptide, were synthesized and evaluated their cytotoxicity in order to gain information from structure-activity relationships of the such cyclopeptides which may lead to find novel and safer anticancer peptide compound(s) to be used in clinic. Peptides were prepared by the solid-phase peptide synthesis method using trityl-resin. Peptide cyclization was performed in liquid phase. To study anticancer activity of the peptide analogues of Longicalycinin A, several methods including MTT, flow cytometry analysis and Lysosomal membrane integrity assay were employed using two cell lines HepG2 and HT-29. Fibroblast cells were used to control the safety of the synthesized cyclopeptides on normal...
Source: Chemico Biological Interactions - Category: Biochemistry Source Type: research