Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-11-20
1997-09-23
Criares, Theodore J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514457, A61K 3135
Patent
active
056705387
DESCRIPTION:
BRIEF SUMMARY
This application is filed under 35 U.S.C. 371 of PCT/FR93/01312 filed Dec. 28, 1993 which claims priority of application FR 92/15801 filed in France Dec. 28, 1992.
A subject of the present invention is the use of prodelphinidins, and more particularly those obtained from the Ribes species, in particular Ribes nigrum, for obtaining medicaments intended for the treatment of arthrosis.
Under normal conditions, the articular cartilage undergoes slow reshaping via a chondroresorption mechanism perfectly compensated for by a chondrorepair process (or chondroformation) which maintains the articular cartilage in dynamic equilibrium (Franchimont et al., 1991).
The chondroresorption is provided by the chondrocyte itself which produces prostaglandins amongst which are PGE2, proteolytic enzymes (collagenase, stromelysine, serine proteases . . . ) and oxygen free radicals which attack the cartilage matrix, disrupt it and destroy it.
At the same time as this chondroresorption, a homeostatic chondroformation takes place which repairs the altered and/or resorbed material; macromolecules are produced which form the structure of the basic substance: collagens of type II and type IX, proteoglycans, junction proteins, etc . . . The clonal proliferation of chondrocytes can be assisted when chondroformation must be significant. This chondroformation phase is a process dependent on several factors amongst which are the concentration of macromolecules of the areas close to the chondrocyte and the hormonal balance, in particular the secretion of growth hormone, IGF I and II, calcitonin, androgens . . .
Various pathogenic factors can arise which accelerate the degradation of the cartilage by acceleration of the chondroresorption process disturbing the equilibrium between chondroresorption and chondrorepair in favour of the former. These are, amongst others, articular functional and weight overloads, deposits of microcrystals and nutritional disorders of the articular structures. These pathogenic factors act by stimulating the production of cytokines (I L1 beta, TNF alpha, IL6 . . . ) by the chondrocytes themselves, by other cells of neighbouring structures such as the A synoviocytes of the articular synovial membrane. The imbalance will be all the more marked if hormonal disturbances exist (as is the case after 50, the age at which arthrosis can develop) making chondrorepair less effective.
This biochemical imbalance leads to a weakening of the articular cartilage which first of all cracks on the surface then more deeply exposing the sub-chondral bone. Arthrosis is the clinical expression of this loss of cartilage function, which is itself a consequence of the biochemical imbalance between chondroresorption and chondrorepair.
The treatment of arthrosis using medicaments is poor: non-steroid anti-inflammatories combat pain and improve movement; they do not stop the development of the disease, in particular the destruction of cartilage, and they do not enable cartilage to be repaired.
In particular, the use of pyknogenols originating from plant extracts such as Ribes nigrum, for the preparation of medicaments with an anti-inflammatory activity, is the subject of the International Application WO 92/14457 of the 14th Feb. 1992.
Furthermore, the use of proanthocyanidins for the prevention or the treatment of pathologies due to the biological effects of free radicals, in particular inflammations, is the subject of the U.S. Pat. No. 4,698,360 filed on 9th Apr. 1985.
A specific aim of the present invention is to provide medicaments which, by their properties for reducing chondroresorption and stimulating chondrorepair, allow the effective treatment of arthrosis or any other pathology directly or indirectly associated with destruction of cartilage and the absence of repair of the latter by the biological mechanisms of the organism.
A subject of the present invention is the use of prodelphinidins of formula (I): ##STR1## in which: R.sub.1 and R.sub.2 independently represent H or OH, (gallo-catechin/epigallocatechin), and, corresponds to a ga
REFERENCES:
patent: 4268517 (1981-05-01), Niebes et al.
patent: 4698360 (1987-10-01), Masquelier
"Anti-Inflammatory Prodelphinidins from Black Currant (Ribes nigrum) Leaves", Planta Med., vol. 57, Supl. 1991, p. A131, by M. Tits et al.
"Evidence by in vivo and in vitro studies that binding of pycnogenols to elastin affects its rate of degradation by elastases", Biochemical Pharmacology, vol. 33, No. 24, 1984, pp. 3933-3939, by J.M. Tixier et al.
Angenot Luc
Bassleer Corine
Franchimont, deceased Paul
Tits Monique
Criares Theodore J.
Laboratoires Dolisos
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