Peptides derived from RWQWRWQWR (1R5R9R) sequence containing D-aminoacids. Characterization by RP-HPLC and ESI-QTOF MS, and cytotoxic effect against breast cancer cells and non-cancerous fibroblast primary cell culture
Code | Sequence | RP-HPLC | ESI-MS (Ma) | IC50, µg/mL (µM) | |||
---|---|---|---|---|---|---|---|
tR (min) | Purity (%) | Theoretical | Exp. | MCF-7 | Fibroblasts | ||
1R5R9R | RWQWRWQWR | 6.3 | 92 | 1,485.75 | 1,485.88 | 120 (81) | > 200 (135)* |
1 | dRWQWRWQWR | 5.9 | 99 | 1,485.76 | 1,485.77 | > 200 (135)* | > 200 (135)* |
2 | RdWQWRWQWR | 6.7 | 94 | 1,485.76 | 1,485.77 | > 200 (135)* | > 200 (135)* |
3 | RWdQWRWQWR | 5.9 | 99 | 1,485.76 | 1,485.76 | > 200 (135)* | > 200 (135)* |
4 | RWQdWRWQWR | 6.5 | 95 | 1,485.76 | 1,485.77 | > 200 (135)* | > 200 (135)* |
5 | RWQWdRWQWR | 5.9 | 95 | 1,485.76 | 1,485.77 | > 200 (135)* | > 200 (135)* |
6 | RWQWRdWQWR | 6.1 | 89 | 1,485.76 | 1,485.77 | > 200 (135)* | > 200 (135)* |
7 | RWQWRWdQWR | 6.1 | 100 | 1,485.76 | 1,485.77 | > 200 (135)* | > 200 (135)* |
8 | RWQWRWQdWR | 6.3 | 98 | 1,485.76 | 1,485.77 | > 200 (135)* | > 200 (135)* |
9 | RWQWRWQWdR | 6.3 | 99 | 1,485.76 | 1,485.77 | > 200 (135)* | > 200 (135)* |
10 | dRWQWdRWQWdR | 5.4 | 94 | 1,485.76 | 1,485.77 | > 200 (135)* | > 200 (135)* |
11 | RdWQdWRdWQdWR | 6.5 | 99 | 1,485.76 | 1,485.77 | > 200 (135)* | > 200 (135)* |
12 | RWdQWRWdQWR | 5.6 | 99 | 1,485.76 | 1,485.77 | > 200 (135)* | > 200 (135)* |
13 | dRdWdQdWdRdWdQdWdR | 6.4 | 90 | 1,485.76 | 1,485.77 | > 200 (135)* | > 200 (135)* |
dR, dW, dQ indicate the position of D-Arg, D-Trp and D-Gln, respectively. *: IC50 could not be reached at the evaluated concentrations; ESI-MS: electrospray ionization mass spectrometry; IC50: half maximal inhibitory concentration; Ma: corresponds to monoisotopic mass; RP-HPLC: reversed-phase high-performance liquid chromatography; tR: retention time