化学
四肽
抗菌剂
三肽
白色念珠菌
脯氨酸
最小抑制浓度
立体化学
肺炎克雷伯菌
细胞毒性
细菌
肽
环肽
氨基酸
生物化学
微生物学
体外
大肠杆菌
有机化学
生物
基因
遗传学
作者
Rajiv Dahiya,Akhilesh Kumar,Rajul Gupta
出处
期刊:Chemical & Pharmaceutical Bulletin
[Pharmaceutical Society of Japan]
日期:2009-01-01
卷期号:57 (2): 214-217
被引量:20
摘要
Present study describes the first total synthesis of a cyclic heptapeptide, stylisin 1 (8) via coupling of tetrapeptide Boc-L-tyrosinyl-L-prolyl-L-leucyl-L-proline-OH and tripeptide L-phenylalanyl-L-isoleucyl-L-proline-OMe followed by cyclization of linear heptapeptide segment. Structure elucidation of synthesized cyclopeptide was done on basis of detailed spectral as well as elemental analysis. From the results of pharmacological screening, it was concluded that cyclopeptide 8 possessed moderate cytotoxicity against Dalton's lymphoma ascites (DLA) and Ehrlich's ascites carcinoma (EAC) cell lines with IC(50) (inhibitory concentration, 50%) values of 10.6 and 14.6 microM. Furthermore, cyclopeptide 8 exhibited moderate to good antimicrobial activity against Gram -ve (negative) bacteria Klebsiella pneumoniae and Pseudomonas aeruginosa, dermatophytes and Candida albicans with minimum inhibitory concentration (MIC) of 6 microg/ml.
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