Drug – bio-affecting and body treating compositions – Plant material or plant extract of undetermined constitution... – Containing or obtained from roseaceae
Reexamination Certificate
1998-09-22
2003-07-01
Prats, Francisco (Department: 1651)
Drug, bio-affecting and body treating compositions
Plant material or plant extract of undetermined constitution...
Containing or obtained from roseaceae
C424S725000
Reexamination Certificate
active
06586020
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Technical Field of the Invention
The present invention relates to novel bradykinin antagonist compositions comprising at least one extract of at least one plant of the Rosaceae family.
This invention also relates to the administration of at least one plant of the Rosaceae family, as the active species or agent for treating disorders associated with an excessive synthesis and/or release of bradykinin.
2. Description of the Prior Art
Bradykinin is a peptide of plasma origin which is released from a kininogenic precursor by a plasma protease deemed kallikrein (EC 3.4.21.24). This nanopeptide is one of the key mediators of inflammation and exhibits mitogenic properties. The receptors for this kinin can be separated into two principal subtypes B1 and B2. Bradykinin acts especially on the B2 receptor and causes stimulation of numerous systems of production of second messengers, including inositol triphosphates (ip3), known to cause the release of calcium from the intracellular storage sites in the cells including the keratinocyte. Bradykinin also induces the phosphorylation of tyrosine residues through activation of the B2 receptor, depolarization or hyperpolarization of the cell membrane, as well as the activation of the metabolism of arachidonic acid.
Bradykinin is involved in a large number of physiopathological disorders such as, for example, vasodilation and increase in vascular permeability, hypotension, pain or the proliferation of the connective tissue. Vasodilation and increase in vascular permeability may have as consequence, inter alia, acne rosacea, telangiectasia or a rhynophyma. The proliferation of the connective tissue results in the formation of keloids.
Bradykinin is suspected of playing a role in the mechanism leading to hair loss.
Moreover, bradykinin causes an inflammatory response by activation of phospholipase A2 and by formation of prostaglandins and/or the release of various inflammation mediators, cytokines, leukotrienes. It is also involved in the stimulation of nerve endings, the contraction of the smooth muscles of the digestive and respiratory tracts and of the uterus. An excessive production of bradykinin may cause diarrhoeas in gastrointestinal disorders and stimulate the nasopharyngeal secretions in allergic rhinitis.
Bradykinin is moreover known to stimulate ion transport and fluid secretions by various epithelia.
The administration of bradykininergic antagonists is therefore one of the effective alternatives to all cosmetic and/or pathological disorders involving the systems described above, in particular inflammatory processes of neurogenic origin or otherwise.
For a substance to be recognized as a bradykinin antagonist, it should induce a coherent pharmacological response including or otherwise its attachment to the bradykinin receptor.
Thus, within this definition is any compound which may interfere with the effects of bradykinin by its attachment to the receptor for the latter (B1 or B2) and/or any compound which, independently of the attachment to the receptor(s), induces by any mechanism an effect which is the opposite of that known for bradykinin (for example, interfering with the synthesis of bradykinin).
In particular, for a substance to be recognized as a bradykinin receptor antagonist, it should, in particular, exhibit the following characteristics:
(a) have a selective affinity for the receptors specific for this compound: of the B
1
and/or B
2
type. The experimental models used are established on a culture of mesenteric aorta cells (receptor attachment to B
1
receptors according to the technique described by J. P. Galizzi published in
Brit. J. Pharmacol
, 113, 389 (1984)) and/or on the intestine (receptor attachment to B
2
receptors according to the technique described by Burch R. M. published in
Biotech. Update
(
Dupont
-
Nen
), 7, 2 (1992); and/or
(b) have a bradykinin receptor antagonist pharmacological activity, namely, induce a coherent pharmacological response in specific tests. The pharmacological activity is in this event evaluated on isolated organs according to the techniques described by Rhaleb N. E. et al., in
Brit. J. Pharmacol
., 94, 445 (1990) as regards an antagonist activity of the B
1
and/or B
2
type.
Numerous compounds have already been recognized as bradykinin antagonists. Representative are the optionally modified synthetic or natural peptides such as D-Arg-[Hyp3, D-Phe7]-bradykinin (NPC567), [Thi 5, 8, D-Phe7]-bradykinin, D-Arg, [Hyp3, Thi5,8, D-Phe7]-bradykinin, N-&agr;-adamantaneacetyl-D-Arg-[Hyp3, Thi5,8, D-Phe7]-bradykinin, des-Arg9, [Leu8]-bradykinin (all marketed by Sigma) or, alternatively, compounds described in WO-95/08566, WO-95/07294, EP-0623350, EP-0622361, WO-94/11021, EP-0596406, WO-94/06453, WO-94/09001, EP-0578521, EP-0564972, EP-0552106, WO-93/11789, U.S. Pat. No. 5,216,165, U.S. Pat. No. 5,212,182, WO-92/17201, EP-0496369, EP-0472220, EP-0455133, WO-91/09055, WO-91/02746, EP-0413277, EP-0370453, EP-0359310, WO-90/03980, WO-89/09231, WO-89/09230, WO-89/01780, EP-0334244, EP-0596406, WO-86/07263 or P-guanido-benzoyl-[Hyp3,Thi5,D-Tic7,Oic8]-bradykinin (S 16118) (Feletou M & al.,
Pharmacol. Exp. Ther
., June 1995, 273, 1078-84), D-Arg-[Hyp3, Thi5, D-Tic7,Oic8]-bradykinin (HOE 140) (Feletou M & al.,
Eur. J. Pharmacol
, 1995, 274, 57-64), D-Arg-[Hyp3, D-Hype (trans-propyl)7 Oic8]-bradykinin (NPC 17731) (Herzig M. C. S. and Leeb-Lundberg L. M. F.,
J. Biol. Chem
., 1995, 270, 20591-20598) or those indicated in
Bradykinin Antagonists: development and applications
(Stewart J. M.,
Biopolymers
, 1995, 37, 143-155), or, alternatively, synthetic or natural chemical molecules such as, for example, those described in Salvino et al.,
J. Med. Chem
., 3, 2583-2584 (1993).
As a general rule, these bradykinin antagonists which, moreover, provide excellent results, are chemical molecules which may have harmful side effects.
Serious need continues to exist for novel active agents or species which meet the criteria for a bradykinin antagonist, especially if they are of natural origin and are devoid of side effects.
Heretofore, it has never been demonstrated or suggested in the prior art that an extract of at least one plant of the Rosaceae family exhibits the criteria for a bradykinin antagonist.
Indeed, plants of the Rosaceae family are principally used for their aromatic and ornamental properties.
In the prior art, plants of the Rosaceae family have been included in compositions for the treatment of urogenital diseases (FR-76/36295), in lightening cosmetic compositions (JP-08208451) or in compositions for protecting against ultraviolet radiation (EP-A-781544), for the preparation of antioxidant compounds (EP-A-94/401669), or, alternatively, for the preparation of antimicrobial and/or insecticidal compounds for the protection of plants (DE-4327792).
SUMMARY OF THE INVENTION
It has now unexpectedly and surprisingly been determined that extracts of at least one plant of the Rosaceae family elicit bradykinin-antagonizing activity.
Thus, it has now been determined that an extract of at least one plant of the Rosaceae family presents the characteristics defined as characterizing a bradykinin antagonist and can therefore be administered as a bradykinin antagonist.
Accordingly, the present invention features cosmetic/pharmaceutical compositions comprising an effective active agent amount of at least one Rosaceae extract which serves as a bradykinin antagonist.
DETAILED DESCRIPTION OF BEST MODE AND SPECIFIC/PREFERRED EMBODIMENTS OF THE INVENTION
More particularly according to the present invention, by “active ingredient” is intended any molecule or extract capable of modifying or of modulating the functioning of at least one given biological system.
The extract of at least one plant of the Rosaceae family may be any extract prepared from any plant material derived from at least one plant of the Rosaceae family.
Thus, the extract of at least one plant of the Rosaceae family according to the invention
Breton Lionel
Pineau Nathalie
Burns Doane Swecker & Mathis L.L.P.
Prats Francisco
Societe L'Oreal S.A.
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