Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1993-02-01
1997-03-04
Weddington, Kevin E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514560, A61K 3122, A61K 3120
Patent
active
056079702
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This application is a 371 of PCT/JP92/00857 filed Jul. 06, 1992.
The present invention relates to a novel inhibitory agent for an ACAT enzyme, and more specifically, it relates to a lipid absorption inhibitory edible composition, etc., containing an inhibitory agent for an ACAT enzyme derived from a food component.
BACKGROUND ART
The absorption of a lipid, particularly cholesterol, is believed to be rate determined by a process wherein free cholesterol is converted to ester cholesterol by an ACAT (AcylCoA-Cholesterolacyltransferase) in small intestine epithelial cells. An ACAT inhibitory agent has been found to be useful as an anti-cholesterol agent in this respect. At present, several of these agents are being developed as pharmaceuticals.
DISCLOSURE OF THE INVENTION
As a result of earnest efforts pertaining to the above, the inventors of the present invention found that monoacylglycerol (monoglyceride), a certain kind of fatty acid-like substance derived from microorganism lipids, such as that from lactic acid bacteria and decomposition products of rice bran and wheat bran lipid, demonstrates remarkable inhibitory activity against said enzyme, as those suitable for common use as a so-called functional food component and so forth, and, as a result, the present invention has completed.
Accordingly, in consideration of the present state of the above-mentioned prior art, an object of the present invention is to provide a compound having a remarkable ACAT inhibitory activity, despite being derived from edible natural substances and being essentially non-toxic, as well as an edible composition containing said compound as the active ingredient.
In accordance with the present invention, there are provided an ACAT inhibitory agent containing monoacylglycerol (monoglyceride) as an active ingredient, and a lipid absorption inhibitory edible composition containing the ACAT inhibitory agent and an edible carrier. Although there is no particular limitation to the content of monoacylglycerol (monoglyceride) in the composition, a content of 0.5 to 3% by weight is preferable. Specific examples of the edible carrier include hydroxypropylmethyl cellulose phthalate and casein.
BEST MODE FOR CARRYING OUT THE INVENTION
The present invention will now be explained in detail.
Those present in microorganism lipids such as those of lactic acid bacteria, and hydrolyzed (enzyme) decomposition products of vegetable lipids such as rice bran and wheat bran lipids, which is purified and isolated in a conventional manner, or commercially available monoacylglycerols (monoglycerides) having 22 carbon atoms or less, preferably 16 carbon atoms or less, such as 2-oleylglycerol, 1-oleylglycerol, 1-linoleylglycerol, 1-linolenoylglycerol, 1-stearoylglycerol, 1-palmitoylglycerol or 1-palmitooleylglycerol, exhibit fatty acid-like properties.
The above-mentioned substances can usually be orally administered in a dosage of about 0.1-10 mg/kg (body weight) per day in ordinary form such as tablet or capsule. Since these substances are food components, they are essentially non-toxic when taken orally. On the other hand, in the case of providing same in the form of an edible composition, these substances need not be particularly isolated for utilization, and may be utilized as food auxiliary components such as a microorganism lipid, or the lipid decomposition products of rice bran or wheat bran.
An ACAT activity was assayed according to the method of Heider et al (J. Lipid. Res. 24, 1127-1134 (1983)). That is, a rabbit is fed a 1% cholesterol diet for 3 weeks followed by dissection and extraction of the small intestine. After peeling off the small intestine epithelium and crushing with a homogenizer, incompletely crushed solids are removed by centrifugal separation. The microsome fraction of the 107,000.times. g sediment was suspended in a 0.154M phosphate buffer (pH 7.4), which is then used for ACAT enzyme preparation. The reaction is carried out by adding 18 nmol of bovine serum albumin and 18 nmol of [1- .sup.14 C]oleylCoA (
REFERENCES:
patent: 4272528 (1981-06-01), Von Esch et al.
Journal of Biological Chemistry, vol. 254, No. 5 (1979), pp. 1534-1536, Susanne Bennett Clark, "Mucosal Coenzyme A-dependent Cholesterol Esterification after Intestinal Perfusion of Lipids in Rats".
Proceedings of the Society for Experimental Biology and Medicine, vol. 177, No. 1 (1984), pp. 188-196, L. L. Gallo et al., "Rat Intestinal Acyl Coenzyme A: Cholesterol Acyl Transferase Properties and Localisation".
Journal of Biological Chemistry, vol. 265, No. 14 (1990), pp. 8042-8051, I. Tabas et al., "Rabitt and Human Liver Contain a Novel Pentacyclic . . . ".
Journal of Lipid Research, vol. 24, (1983), pp. 1127-1134, J. Heider et al., "Role of Acyl CoA:cholesterol Acyltransferase in cholesterol . . . ".
Ishihara Kazuoki
Shin Ryouiti
Kabushiki Kaisya Advance
Weddington Kevin E.
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