Antitumor and Antimicrobial Activity of Some Cyclic Tetrapeptides and Tripeptides Derived from Marine Bacteria |
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| Authors: | Subrata Chakraborty Dar-Fu Tai Yi-Chun Lin Tzyy-Wen Chiou |
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| Institution: | 1.Department of Chemistry, National Dong Hwa University, Hualien 974, Taiwan; E-Mail: ;2.Department of Life Science, National Dong Hwa University, Hualien 974, Taiwan; E-Mails: (Y.C.L.); (T.W.C.) |
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| 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. |
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| Keywords: | antibiotic antitumor cyclic tetrapeptide cyclic tripeptide |
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