Synthesis and Pharmacological Studies on a Cyclooligopeptide from Marine Bacteria |
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| Authors: | Dahiya Rajiv Gautam Hemendra |
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| Institution: | 1. Department of Pharmaceutical Chemistry, Globus College of Pharmacy, Bhojpur Road, Bhopal‐462 045, Madhya Pradesh, India;2. Department of Pharmacology, Institute of Pharmacy, Invertis University, Bareilly‐243 123, Uttar Pradesh India |
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| Abstract: | A natural proline‐rich tetrapeptide cyclo‐prolyl‐leucyl‐prolyl‐phenylalanyl was prepared employing solution‐phase method of peptide synthesis through coupling of dipeptide fragments Boc‐l‐Pro‐l‐Leu‐OH and l‐Pro‐l‐Phe‐OMe which utilizes diisopropylcarbodiimide (DIPC) as coupling agent and N‐methylmorpholine (NMM) as the base. Deprotection of linear tetrapeptide unit followed by its cyclization provided a cyclopeptide, identical in all aspects to the natural molecule. Pharmacological evaluation showed cytotoxic, antifungal and antihelmintic potential of synthesized peptide against Dalton's Lymphoma Ascites (DLA) and Ehrlich's Ascites Carcinoma (EAC) cell lines, pathogenic dermatophytes and earthworms. |
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| Keywords: | marine bacteria natural product solution phase synthesis peptides biological activity cytotoxicity |
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