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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 μM. Benzyl group protected CtetPs 3 and 4, exhibited antitumor activity against several cell lines at a concentration of 80-108 μM. 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.

journal_name

Mar Drugs

journal_title

Marine drugs

authors

Chakraborty S,Tai DF,Lin YC,Chiou TW

doi

10.3390/md13053029

subject

Has Abstract

pub_date

2015-05-15 00:00:00

pages

3029-45

issue

5

issn

1660-3397

pii

md13053029

journal_volume

13

pub_type

杂志文章

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