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Antitumor and antimicrobial activity of some cyclic tetrapeptides and tripeptides derived from marine bacteria.

ABSTRACT: Marine derived cyclo(Gly-l-Ser-l-Pro-l-Glu) was selected as a lead to evaluate antitumor-antibiotic activity. Histidine was chosen to replace the serine residue to form cyclo(Gly-l-His-l-Pro-l-Glu). Cyclic tetrapeptides (CtetPs) were then synthesized using a solution phase method, and subjected to antitumor and antibiotic assays. The benzyl group protected CtetPs derivatives, showed better activity against antibiotic-resistant Staphylococcus aureus in the range of 60-120 ?M. Benzyl group protected CtetPs 3 and 4, exhibited antitumor activity against several cell lines at a concentration of 80-108 ?M. However, shortening the size of the ring to the cyclic tripeptide (CtriP) scaffold, cyclo(Gly-l-Ser-l-Pro), cyclo(Ser-l-Pro-l-Glu) and their analogues showed no antibiotic or antitumor activity. This phenomenon can be explained from their backbone structures.

SUBMITTER: Chakraborty S

PROVIDER: S-EPMC4446616 | biostudies-literature | 2015 May

REPOSITORIES: biostudies-literature

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Antitumor and antimicrobial activity of some cyclic tetrapeptides and tripeptides derived from marine bacteria.

Chakraborty Subrata S Tai Dar-Fu DF Lin Yi-Chun YC Chiou Tzyy-Wen TW

Marine drugs 20150515 5

Marine derived cyclo(Gly-l-Ser-l-Pro-l-Glu) was selected as a lead to evaluate antitumor-antibiotic activity. Histidine was chosen to replace the serine residue to form cyclo(Gly-l-His-l-Pro-l-Glu). Cyclic tetrapeptides (CtetPs) were then synthesized using a solution phase method, and subjected to antitumor and antibiotic assays. The benzyl group protected CtetPs derivatives, showed better activity against antibiotic-resistant Staphylococcus aureus in the range of 60-120 μM. Benzyl group protect ...[more]

PMID: 25988520

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