Dahiya Rajiv
Department of Pharmaceutical Chemistry, Rajiv Academy for Pharmacy, Mathura-281 001 (UP), India.
Pak J Pharm Sci. 2007 Oct;20(4):317-23.
Present investigation describes the synthesis of a natural phenylalanine-rich cyclopolypeptide longicalycinin A (10) by coupling of dipeptide unit Boc-L-phe-L-tyr-OH with tripeptide unit L-pro-L-phe-gly-OMe followed by cyclization of linear segment. Synthesized cyclic pentapeptide was characterized by spectral techniques including FTIR, 1H/13C NMR, FAB MS and elemental analysis and screened for different pharmacological activities. It was found that it has good anthelmintic activity against Megascoplex konkanensis, Pontoscotex corethruses and Eudrilus sp. at 2 mg/ml concentration, in addition to high cytotoxicity against Dalton's lymphoma ascites (DLA) and Ehrlich's ascites carcinoma (EAC) cell lines with CTC50 values of 2.62 and 6.37 microM. Dermatophytes were found to be moderately sensitive towards newly synthesized peptide.
目前的研究描述了通过将二肽单元Boc-L-苯丙氨酸-L-酪氨酸-OH与三肽单元L-脯氨酸-L-苯丙氨酸-甘氨酸-OMe偶联，随后使线性片段环化，合成富含天然苯丙氨酸的环多肽长萼豆蔻素A（10）。通过包括傅里叶变换红外光谱（FTIR）、1H/13C核磁共振（NMR）、快原子轰击质谱（FAB MS）和元素分析在内的光谱技术对合成的环五肽进行了表征，并对其不同的药理活性进行了筛选。结果发现，它在2 mg/ml浓度下对康卡纳巨蚓、海滨巨蚓和真蚓具有良好的驱虫活性，此外，对道尔顿淋巴瘤腹水（DLA）和艾氏腹水癌（EAC）细胞系具有高细胞毒性，其半数细胞毒性浓度（CTC50）值分别为2.62和6.37 microM。发现皮肤癣菌对新合成的肽中度敏感。
