Dahiya Rajiv
Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura, 281 001, UP, India.
Acta Pol Pharm. 2007 Nov-Dec;64(6):509-16.
A natural cyclic heptapeptide segetalin D [VIII] was synthesized by coupling of tripeptide unit Boc-Pro-Gly-Leu-OMe [V] with tetrapeptide unit Boc-Ser-Phe-Ala-Phe-OMe [VI] after proper deprotection at carboxyl and amino ends followed by cyclization of linear peptide segment. Structure of VIII was confirmed by spectral and elemental analyses. The newly synthesized cyclopeptide was tested for its antibacterial, antifungal, anthelmintic and cytotoxic activities. Compound VIII showed high cytotoxicity against Dalton's lymphoma ascites (DLA) and Ehrlich's ascites carcinoma (EAC) cell lines with CTC50 values of 7.54 and 13.56 microM. Moreover, VIII exhibited potent anthelmintic activity against earthworms Eudrilus species, Megascoplex konkanensis and Pontoscotex corethruses at a dose of 2 mg/mL.
通过将三肽单元Boc-Pro-Gly-Leu-OMe [V]与四肽单元Boc-Ser-Phe-Ala-Phe-OMe [VI]在羧基和氨基末端进行适当脱保护后偶联，随后使线性肽段环化，合成了一种天然环状七肽segetalin D [VIII]。通过光谱和元素分析确认了VIII的结构。对新合成的环肽进行了抗菌、抗真菌、驱虫和细胞毒性活性测试。化合物VIII对道尔顿淋巴瘤腹水（DLA）和艾氏腹水癌（EAC）细胞系表现出高细胞毒性，CTC50值分别为7.54和13.56 microM。此外，VIII在2 mg/mL的剂量下对蚯蚓Eudrilus species、Megascoplex konkanensis和Pontoscotex corethruses表现出强效驱虫活性。
