Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1997-02-07
1999-01-05
Davenport, Avis M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
530324, A61K 3800, C07K 500, C07K 700
Patent
active
058563032
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP96/01543 filed Jun. 6, 1996.
FIELD OF THE INVENTION
The present invention relates to a novel peptide, a bronchus-expanding agent and a blood-flow-improving agent.
BACKGROUND OF THE INVENTION
VIP (vasoactive intestinal peptide) is one kind of physiologically active peptide called brain-gut peptide, the action of which is to promote blood flow and depress blood pressure. VIP was extracted from the intestine of a pig in 1970 and it consists of 28 amino acid residues (S. I. Said, V. Mutt Science, 169, 1217 (1970)).
PACAP (pituitary adenylate cyclase activating polypeptide) was isolated from the hypothalamus of a sheep in 1989 in a bioassay system using as an indicator the activation of adenylate cyclase from cultured pituitary cells, and it is a structurally determined peptide consisting of 38 amino acid residues (A. Miyata, A. Arimura et al., Biochem. Biophys. Res. Commun.,164, 567 (1989)). 27 amino acid residues from the N-terminal side of PACAP has the PACAP activity and the amino acid sequence of said 27 amino acids has a considerably similar structure to that of VIP.
VIP and PACAP are similar in amino acid sequence to secretin, glucagon etc. and are thus classified as peptides belonging to the glucagon family. By virtue of their strong action on vessel expansion and blood-flow promotion, VIP and PACAP are expected for use in the treatment of an ulcer, frostbite, bedsore, impotence etc. and in the restoration and growth of hair. In addition, VIP and PACAP have considerably strong relaxation action on the bronchial smooth muscle in the respiratory system, thus alleviating the smooth muscle contraction induced by stimulators such as acetylcholine, histamine, serotonin etc. Such relaxation action of VIP and PACAP differ from the relaxation action caused via adrenalin .beta..sub.2 receptor by general bronchial expansion, so VIP and PACAP are expected to have an treatment effect on asthmatic spasm difficult to cure on which a stimulator of .beta..sub.2 receptor does not effectively act.
Besides VIP and PACAP, a peptide consisting of 28 to 31 amino acid residues with bronchus expanding action, blood-pressure reducing action and hair restoring action is known (see Japanese Patent Application Laid-Open Publication Nos. 246,595/87, 83,012/89 and 297,498/92).
It is however desired to develop a bronchus-expanding agent and a blood-flow-improving agent superior to VIP, PACAP and other peptides in the durability of bronchus-expanding action and blood-flow increasing action.
DISCLOSURE OF THE INVENTION
The object of the present invention is to provide a novel peptide excellent in the durability of bronchus-expanding action and further excellent in blood-flow increasing action, a bronchus-expanding agent and a blood-flow-improving agent comprising said peptide as an active ingredient.
The present invention provides a peptide represented by the general formula (1): ##STR2## wherein A is Ala or Gly; B is Ile or Val; C is Asn or Ser; D is Thr or Ser; E is Leu or Tyr; each of F, I and J is Lys or Arg, and at least one of F, I and J is Arg; G is Met, Leu or nLeu; K is Asn or Ala; L is Ser or Ala; M is Ile or Val; and N is --NH.sub.2 or Asn--NH.sub.2, excluding the combination where A is Ala, B is Val, C is Asn, D is Thr, E is Leu, K is Asn, L is Ser, M is Ile, and N is Asn--NH.sub.2, or the general formula (2): ##STR3## wherein A, B, C, D, E, F, G, I, J, K, L and M possess the same meanings defined as above; at least one of F, I and J is Arg; P is Asn or a chemical bond; Q is Lys, Arg, Lys-Arg, Arg--Arg or a chemical bond; and R is --OH or --NH.sub.2, or pharmaceutically acceptable salts thereof.
Further, the present invention provides a bronchus-expanding agent comprising said peptide or a pharmaceutically acceptable salt thereof as an active ingredient.
Further, the present invention provides a blood-flow-improving agent comprising said peptide or a pharmaceutically acceptable salt thereof as an active ingredient.
Further, the present invention provides a pharmaceutical compositio
REFERENCES:
patent: 4605641 (1986-08-01), Bolin et al.
patent: 4734400 (1988-03-01), Bolin et al.
A. Miyata et al., Biochemical & Biophysical Research Communications, vol. 164, No. 1, pp. 567-574 (1989).
"Polypeptide with Broad Biological Activity: Isolation from Small Intestine", Science, vol. 169, pp. 1217-1218 (1970).
R.B. Merrifield, Synthesis of a Tetrapeptide, vol. 85, pp. 2149-2154 (1963).
Chemical Abstracts, vol. 122, p. 1111, No. 291534r, 1995.
Kashimoto Kazuhisa
Nagano Yumiko
Davenport Avis M.
Itoham Foods Inc.
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