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Design, synthesis and biological activity of cell‐penetrating peptide‐modified octreotide analogs
Author(s) -
Xie Wenlin,
Liu Jian,
Qiu Minghua,
Yuan Jiancheng,
Xu Anlong
Publication year - 2010
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/psc.1205
Subject(s) - octreotide , chemistry , peptide , in vitro , cell culture , cancer cell , cell , mtt assay , biochemistry , pharmacology , cancer , biology , medicine , somatostatin , genetics
Abstract Four novel octreotide analogs with cell‐penetrating peptides (CPPs) at the N ‐terminus or C ‐terminus were synthesized by a stepwise Fmoc solid‐phase synthesis strategy. The synthesized peptides were analyzed and characterized using reverse phase HPLC and MALDI‐TOF mass spectrometry. The antiproliferative activity of the analogs was tested in vitro on human gastric (SGC‐7901) and hepatocellular cancer (BEL7402) cell lines using the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) assay. Interestingly, these analogs showed a higher anticancer activities than the parent octreotide except CMTPT03 analog. The results demonstrate that the designed octreotide analogs enhance their anticancer activity after linking together the CPPs to octreotide at the N ‐terminus, and are potential molecules for future use in cancer therapy and drug targeting. Copyright © 2009 European Peptide Society and John Wiley & Sons, Ltd.