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Orally active anti-hypertensive peptides found based on enteroendocrine cell responses to a dipeptide library
- Sasai, Masaki, Sun, XingHui, Okuda, Chinatsu, Nakato, Junya, Kanamoto, Ryuhei, Ohinata, Kousaku
- Biochemical and biophysical research communications 2018 v.503 no.2 pp. 1070-1074
- animal disease models, antihypertensive effect, blood pressure, bovine serum albumin, cholecystokinin, dipeptides, hypertension, oral administration, rats, secretion
- We previously reported that an orally administered dipeptide, Arg-Phe (RF), which causes enteroendocrine cell responses, lowered blood pressure in spontaneously hypertensive rats (SHRs). In this study, we found that Phe-Trp (FW), induced the most potent enteroendocrine cell responses out of total 338 dipeptides. An FW analogue, Phe-Trp-Gly-Lys (FWGK), which was effectively produced by tryptic digestion of bovine serum albumin, decreased blood pressure after oral administration. The minimum effective dose of FWGK (50 μg/kg) was 1/300 of that of RF (15 mg/kg). FWGK stimulated cholecystokinin (CCK) secretion in the enteroendocrine cells and exhibited vasorelaxing and antihypertensive effects via the CCK1 system.