Dahiya Rajiv, Kaur Komalpreet
Pharmaceutical Chemistry Department, Rajiv Academy for Pharmacy, Mathura, Uttar Pradesh, India.
Arzneimittelforschung. 2008;58(1):29-34. doi: 10.1055/s-0031-1296463.
In present study, a natural phenylalanine-rich cycloheptapeptide segetalin C (compound VIII) was synthesized by coupling and cyclization of peptide units Boc-gly-L-leu-L-his-OH and L-Phe-L-alaL-phe-L-pro-OMe and examined for different bioactivities. The structure of compound VIII was elucidated by IR, 1H NMR, 13C NMR, mass spectral data and elemental analysis. It was demonstrated that the newly synthesized cyclopeptide has good activity against pathogenic fungi Candida albicans and dermatophytes, in addition to high cytotoxicityagainst Dalton's lymphoma ascites (DLA) and Ehrlich's ascites carcinoma (EAC) cell lines with CTC50 values of 3.35 and 5.72 micromol/L.
在本研究中，通过肽单元Boc-甘氨酸-L-亮氨酸-L-组氨酸-OH和L-苯丙氨酸-L-丙氨酸-L-苯丙氨酸-L-脯氨酸甲酯的偶联和环化反应，合成了一种天然富含苯丙氨酸的环庚肽——水棘针肽C（化合物VIII），并对其不同的生物活性进行了研究。通过红外光谱（IR）、核磁共振氢谱（1H NMR）、核磁共振碳谱（13C NMR）、质谱数据和元素分析确定了化合物VIII的结构。结果表明，新合成的环肽除了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（CTC50值分别为3.35和5.72微摩尔/升）外，对致病性真菌白色念珠菌和皮肤癣菌也具有良好的活性。
