Biochemical and pharmacological aspects of two bradykinin-potentiating peptides obtained from tryptic hydrolysis of casein.
Peptides that display bradykinin-potentiating activity have been obtained from a number of distinct sources, such as snake venoms, fibrinogen, and casein. This paper describes the characterization of two new peptides generated by tryptic hydrolysis of casein. No homology was found with other known vasoactive or vasopotentiating peptides, especially by the lack of Ile-Pro-Pro motif. The peptides EMPFPK and YPVEPFTE, corresponding to the gamma casein sequence (108-113 and 114-121, respectively), displayed a selective potentiating activity on isolated guinea pig ileum for bradykinin. Besides, the octapeptide YPVEPFTE showed an in vitro competitive inhibitor effect on angiotensin-converting enzyme and thimet oligopeptidase and presented an opiate-like activity, increasing two times the latence time in the hot-plate assay. The results suggest that the isolated bioactive peptides act on conversion and/or inactivation of endogenous peptides by enzymes such as angiotensin-converting enzyme and thimet oligopeptidase by modifying several systemic responses such as blood-pressure regulation and in pain response.
Perpetuo
Elen A
EA
Laboratory of Biochemistry and Biophysics, Butantan Institute, Av Vital Brazil 1500, São Paulo, SP, 05503-900, Brazil.
Juliano
Luis
L
Lebrun
Ivo
I
D000595:Amino Acid Sequence; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000494:pharmacology; D000818:Animals; D001794:Blood Pressure / Q000502:physiology; D001920:Bradykinin / Q000378:metabolism / Q000502:physiology*; D002364:Caseins / Q000737:chemistry / Q000378:metabolism*; D005260:Female; D006168:Guinea Pigs; D006868:Hydrolysis; D007082:Ileum / Q000187:drug effects / Q000378:metabolism; D066298:In Vitro Techniques; D008666:Metalloendopeptidases / Q000037:antagonists & inhibitors / Q000378:metabolism; D009842:Oligopeptides / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D010146:Pain / Q000503:physiopathology; D051381:Rats; D014357:Trypsin / Q000378:metabolism*; D014599:Uterus / Q000187:drug effects / Q000378:metabolism
D000806:Angiotensin-Converting Enzyme Inhibitors; D002364:Caseins; D009842:Oligopeptides; D014357:Trypsin; D008666:Metalloendopeptidases; C022510:thimet oligopeptidase; D001920:Bradykinin