Diglyceride and sterol based organometallic complexes and pharma

Details Diglyceride and sterol based organometallic complexes and pharma Diglyceride and sterol based organometallic complexes and pharma

1998-07-13

2000-10-10

Kishore, Gollamudi S.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

4241951, 424617, 424618, 424630, 424639, 424641, 424646, 424649, 424650, 424651, 424682, 514169, 514866, A61K 3128, A61K 3129, A61K 31295, A61K 31315

Patent

active

061299243

DESCRIPTION:

BRIEF SUMMARY
BACKGROUND OF THE INVENTION

The present invention relates to organometallic complexes based on sterols and diglycerides as novel industrial products.
The invention also relates to pharmaceutical compositions and dietary products containing these complexes.
Acylglycerols, more particularly acylglycerols of fatty acids, are present in the majority of plants and are the main constituents of plant and animal fats.
The only variations from one acylglycerol to another is the number of fatty acids, their position on the glycerol, their chain length and the number and the position of the unsaturated bonds they may contain. In particular, these are mono-, di-, or triacylglycerols.
For both sitosterol and sitostanol, there exists two active isomers, the .beta.-and the .gamma.-isomer. These are also constituents of all plants. In the text, the term sitosterol comprises the beta or the gamma sitosterol (or a mixture of these two isomers), and the term sitostanol comprises beta or gamma sitostanol (or a mixture of these two isomers).
Certain total extracts of plants which, like the majority of plants, contain amongst their very many constituents flavonoids, tannins, saponins, coumarins, alkaloids, triterpenes, sterols, carbohydrates and/or glycosides have been described for their hypoglycaemic activity, such as, for example, acacia extract (Egypt. J. Pharm. Sci., 1992, 33 (1-2), 327-340), or Teucrium oliveranium extract (Fitoterapia, 1984, 55(4), 227-230). No link between the activity and the fraction containing the sterols is established. In these publications, this activity is generally attributed to carbohydrates or polyols of cyclohexane such as condutirol, An inositol derivative isolated from a Gymnema sylvestra extract which does not reduce glycaemia directly, but prevents the sugars from passing through the wall of the intestine.
Some sapogenins have been described for the treatment of diabetes, (sarsasapogenin and similagenin for example, in EP 0 204 661). These are derivatives whose lateral chain is constituted of two cyclic spiro ethers.
Other hypoglycaemic derivatives of plant origin have been described, such as, for example: 26-29; which is a summary of the Japanese patent JP 04054194; summary of the Japanese patent JP 61024597. This product tested on the rat acts as an antidiabetic, the dose via the intraperitoneal route being 10 mg/per rat. This dose reduces the glycaemia by 20%.
The leaves and flowering extremities of the nettle (Urtica dioica) are known traditionally for their antidiabetic properties (first description in the scientific literature was 1926). This activity is reproducible and quantifiable, but nobody has hitherto isolated the active principle(s).
Plant sterols, particularly those from the root of the nettle (Urtica dioica) have for many years been the subject of many studies, especially for the treatment of certain tumors such as adenoma of the prostate.
A Pygeum africanum plant extract, marketed in France for many years by Laboratoires DEBAT under the trademark of TADENAN.RTM. for the treatment of adenoma of the prostate, has been the subject of recent studies which tend to prove that the activity would be due to the sterol-lipid fraction which contain, according to R. Longo and S. Tyra, Farmaco, Ed. Pract. 1983, 38(7), pages 287-292, beta-sitosterol, beta-sitosteryl glucoside and 3 beta-sitostenone as well as n-docosanol and n-docosyl trans-ferulate, according to Chemical Abstracts CA 104(22): 193255j.
In Journal of Natural Products, 1987, 50(5), pages 881-885, N. Chaurasia and M. Wichtl describe the isolation, the separation, and the identification of certain sterols from the root of the nettle.
In 1979, a team of Brazilian researchers described, in Rev. Med. Univ. Fed. Ceara, 19(1-2), 49-53, a green arabica coffee bean extract of which sitosterol would be hypoglycaemic. Since then, it has not been possible for this activity to be reproduced and no work has been published which confirms it.
U.S. Pat. No. 4,588,717 describes, as vitamin supplement, weight reducer and diet supplement w

REFERENCES:
Chemical Abstracts #187365 vol. 116, No. 19, May 1992.
Chemical abstract #580. vol. 121 #1, Jul. 1994.
Chemical Abstract #34320. vol. 116 #5, Feb. 1992.
Chemical Abstracts #442. vol. 103 #1, Jul. 1985.
Chemical Abstract #069237 vol. 110 #9, Feb. 1989.

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