A natural proline-rich tetrapeptide cyclo-prolyl-leucyl-prolyl-phenylalanyl was prepared employing solu- tion-phase method of peptide synthesis through coupling of dipeptide fragments Boc-l-Pro-l-Leu-OH and 1-Pro-l-Ph...A natural proline-rich tetrapeptide cyclo-prolyl-leucyl-prolyl-phenylalanyl was prepared employing solu- tion-phase method of peptide synthesis through coupling of dipeptide fragments Boc-l-Pro-l-Leu-OH and 1-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 po- tential of synthesized peptide against Dalton＇s Lymphoma Ascites （DLA） and Ehrlich＇s Ascites Carcinoma （EAC） cell lines, pathogenic dermatophytes and earthworms.展开更多
文摘A natural proline-rich tetrapeptide cyclo-prolyl-leucyl-prolyl-phenylalanyl was prepared employing solu- tion-phase method of peptide synthesis through coupling of dipeptide fragments Boc-l-Pro-l-Leu-OH and 1-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 po- tential of synthesized peptide against Dalton＇s Lymphoma Ascites （DLA） and Ehrlich＇s Ascites Carcinoma （EAC） cell lines, pathogenic dermatophytes and earthworms.
