Peptides derived from RWQWRWQWR (1R5R9R) sequence containing RGD or DGR motifs. 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 (M) | IC50, µg/mL (µM) | |||
|---|---|---|---|---|---|---|---|
| tR (min) | Purity (%) | a | b | MCF-7 | Fibroblasts | ||
| 1R5R9R | RWQWRWQWR | 6.3 | 92 | 1,485.75 | 1,485.88 | 120 (81) | > 200 (135)* |
| 14 | RGD-X-RWQWRWQWR | 6.3 | 92 | 1,928.21 | 1,928.48 | 27 (14) | 108 (56) |
| 15 | RWQWRWQWR-Ahx-RGD | 6.3 | 96 | 1,928.21 | 1,928.46 | > 200 (104)* | > 200 (104)* |
| 16 | RGD-X-RWQWRWQWR-X-RGD | 6.1 | 84 | 2,369.69 | 2,368.99 | > 200 (84)* | > 200 (84)* |
| 17 | DGR-X-RWQWRWQWR-X-RGD | 6.0 | 99 | 2,369.69 | 2,369.67 | > 200 (84)* | > 200 (84)* |
| 18 | DGR-X-RWQWRWQWR-X-DGR | 6.1 | 95 | 2,369.69 | 2,369.80 | > 200 (84)* | > 200 (84)* |
| R1R5R9R | RRWQWRWQWR | 6.2 | 93 | 1,631.87 | 1,641.88 | 112 (68) | > 200 (121)* |
| 19 | RGD-X-RRWQWRWQWR | 6.2 | 95 | 2,084.39 | 2,084.62 | 82 (39) | 195 (94) |
| 20 | RRWQWRWQWR-Ahx-RGD | 6.2 | 98 | 2,084.39 | 2,084.62 | > 200 (96)* | > 200 (96)* |
| 21 | RGD-X-RRWQWRWQWR-X-RGD | 6.6 | 97 | 2,525.88 | 2,525.42 | > 200 (79)* | > 200 (79)* |
| 22 | DGR-X-RRWQWRWQWR-X-RGD | 6.2 | 95 | 2,525.88 | 2,525.95 | > 200 (79)* | > 200 (79)* |
| 23 | DGR-X-RRWQWRWQWR-X-DGR | 6.2 | 98 | 2,525.88 | 2,426.321 | > 200 (79)* | > 200 (79)* |
*: IC50 could not be reached at the evaluated concentrations; a: theoretical; b: experimental monoisotopic mass in uma; ESI-MS: electrospray ionization mass spectrometry; IC50: half maximal inhibitory concentration; RP-HPLC: reversed-phase high-performance liquid chromatography; tR: retention time