Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
Synthesis, Cytotoxic and Antimicrobial Screening of a Proline-Rich Cyclopolypeptide
Rajiv DahiyaAkhilesh KumarRajul Gupta
Author information

2009 Volume 57 Issue 2 Pages 214-217


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 IC50 (inhibitory concentration, 50%) values of 10.6 and 14.6 μM. 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 μg/ml.

Content from these authors
© 2009 The Pharmaceutical Society of Japan
Previous article Next article