Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – N-c doai
Patent
1996-02-21
1998-05-19
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
N-c doai
514893, A61K 3127
Patent
active
057536970
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/FR94/00793, filed Jun. 29, 1994.
FIELD OF THE INVENTION
The invention relates to antiradical and/or antilipoperoxidative and/or hepatotropic pharmaceutical compositions.
BACKGROUND OF THE INVENTION
In our part of the world, hepatic diseases are dominated by two main aetiological groups:
Their clinical, biological or histological expressions are often similar, if not identical, however, which poses problems of differential diagnosis.
These aetiological distinctions are not found in most of the traditional pharmacopocias concerned with hepatic disorders where the uses of plant extracts are justified in rather vague terms such as "indicated for hepatic diseases", which may cover an extremely wide variety of pathologies.
There is, moreover, a difference in opinion between what is termed traditional medicine and what is termed modern medicine. The former, despite its lack of semeiological rigour, proposes a plethora of remedies. Numerous plant extracts are used empirically in monotherapy or in association by traditional practitioners. Several hundred plants are thus "indicated for hepatic diseases". The latter, despite what is often very precise knowledge of morbid mechanisms and the existence of etiological classifications that are sometimes very subtle, proposes only a modest range of treatments.
The therapeutic indications of Rosmarinus officinalis are numerous and use the various parts of the plant. In particular, diuretic, antiseptic, antirheumatic, healing, astringent, and emmenagogic properties have been found. Above all, Rosmannus officinalis has a privileged place in the field of hepatobiliary diseases. Rosmarinus officinalis is composed of numerous active principles. Its action on the liver (cholagogic and cholesteric) is associated mainly with the presence of rosmarinic acid.
Rosmanol is a compound of the group of diterpene lactones and which has been isolated from Rosmarinus officinalis (Inatani et al., 1982: "Structure of the new antioxydative phenolic diterpene isolated from Rosmary", Agric. Biol. Chem., 46, 1661 et seq.). Rosmanol is known to have an antioxidant activity (in various non-biological tests), which can give rise to applications as antioxidants in foods (oxidation test on "bacon rashers").
Rosmanol has also be isolated from Salvia canariensis and its structure has been determined fully by chemical analysis and by X-ray diffraction (Fraga. et al., 1985: "A revised structure for the diterpene rosmanol", Phytochemistry, Vol. 24, No. 8, 1853-1854).
Rosmanol and 7-ethoxyrosmanol have also been extracted from Rosmarinus officinalis (Studies on Medicinal Plants in Paraguay; Studies on "Romero"; Part 1; T. Hayashi, Planta medica 1987; vol. 53, p 394).
This article points out that rosmanol has an inhibiting effect on urease, but no correlation was established in a certain and unambiguous manner with the use of a therapeutic method of treatment.
Moreover, to this day, no link has been made between the pharmacological properties, particularly the hepatoprotective properties of Rosmarinus officinalis and the active substance responsible for said properties.
SUMMARY OF THE INVENTION
The invention has made it possible to reveal the chemical compound found to be responsible for the antiradical, antilipoperoxidative and hepatotropic activity of Rosmarinus officinalis.
The invention provides novel pharmaceutical compositions, of which the active substance likely to originate from plants, and in particular from Rosmarinus officinalis, has been fully identified and may therefore be correctly proportioned.
The object of the invention is a pharmaceutical composition characterised in that it contains, as active substance, at least one of the compounds corresponding to formula I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, which may be identical or different, represent H, CH.sub.3 or C.sub.2 H.sub.5, possibly in conjunction with a pharmaceutically acceptable salt.
The invention also covers molecules corresponding to formula (I) wherein at least one of the positions
REFERENCES:
M. Pukl et al., "Inhibitory Effect of Carnosolic Acid on HIV-1 Protease", Planta Med., vol. 58, No. 7, 1992, p. A632.
N. Nakatani et al., "Two Antioxidative Diterpenes from Rosemary (Rosmarinus officinalis L.) and a Revised Structure for Rosmanol", Agricultural and Biological Chemistry, vol. 49, No. 8, 1984, pp. 2081-2085.
R. Inatani et al., "Antioxidative Effect of the Constituents of Rosem (Rosmarinus officinalis L.) and Their Derivatives"Agricultural and Biological Chemistry, vol. 47, No. 3, 1983, pp. 521-528.
K. Schwarz et al., "Antioxidative constituents of Rosmarinus officinalis and Salvia officinalis", pp.95-98.
Joyeux Michel
Mortier Francois
Jordan Kimberly
Laboratoires Dolisos
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