Antitumor and Antimicrobial Activity of Some Cyclic Tetrapeptides and Tripeptides Derived from Marine Bacteria

Marine Drugs

Subrata Chakraborty¹  Dar-Fu Tai¹  Yi-Chun Lin²  Tzyy-Wen Chiou² 

[1] Department of Chemistry, National Dong Hwa University, Hualien 974, Taiwan; E-Mail:;Department of Life Science, National Dong Hwa University, Hualien 974, Taiwan; E-Mails:

关键词: antibiotic;    antitumor;    cyclic tetrapeptide;    cyclic tripeptide;   

DOI  :  10.3390/md13053029

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.