Synthesis and Pharmacological Evaluation of Site Specific Cationic Anticancer Peptides

Abstract

In spite of current progress in therapy methods, cancer is the main source of death rate and morbidity in all over the world. However, by surgery, localized tumours can usually be treated successfully. For metastatic disease, chemotherapy and radiation therapy are the only choices of treatment. Chemotherapy acts by selecting fast-dividing cells, therefore unable to make a difference between cancer cells and rapidly dividing normal cells which results in many disadvantages. Chemotherapy is unable to selectively target fast dividing cancer cells and dormant cancer. newlineTo rein over this problem, invaluable attempts have been made to evolve novel cytotoxic remedy having the capability to specifically destroy tumour cells without affecting normal cells regardless of the rate of their growth. In the exploration of novel anticancer drugs, host defense cationic peptides are the decisive substitute of chemotherapeutic drugs. Because of the selective and exclusive nature of cationic peptides newlinefor malignant cell, there is a very slight possibility to harm healthy cells. newlineTumour cell membranes usually bring a net negative charge owing to a larger impression of negatively charged molecules like O-glycosylated mucins and phosphatidylserine (PS) than normal. Moreover, It is the negative membrane potential of tumour cells which makes the ACPs selective to cancer cells. Electrostatic interactions among untransformed cells and ACPs are not advised due to the general neutral charge on normal cells by the zwitterionic character of membrane molecules such as phosphatidylcholine (PC), phosphatidylethanolamine (PE), or sphingomyelin. newlineNumerous synthetic or natural cationic peptides have been revealed to exhibit antitumour activity with characteristic comprising the capacity to destroy target cells quickly, the broad-spectrum activity, and the specificity for tumour cells. As compared to chemotherapy or radioactive treatment, peptides possessing higher specificity against tumour cells may be a suitable candidate for destroying tumour cells