JP2008143862A - Apolipoprotein b48 concentration rise inhibitor - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a highly safe apoliporpotein B48 concentration rise inhibitor. <P>SOLUTION: The apoliporpotein B48 concentration rise inhibitor comprises a diacylglycerol as an active ingredient, wherein the diacylglycerol is preferably such that its fatty acid composition is of 8-24C and unsaturated fatty acids account for 70 wt.% or greater of the total constitutive fatty acid. <P>COPYRIGHT: (C)2008,JPO&INPIT

Description

  The present invention relates to an apolipoprotein B48 concentration increase inhibitor that can be easily taken.

  Ischemic heart disease is included in heart disease, which is the second leading cause of death among Japanese people, and the number of deaths and mortality rates are increasing year by year. Risk factors for ischemic heart disease include high LDL cholesterolemia, obesity, diabetes, hypertriglycerideemia, low HDL cholesterolemia, hypertension, hyperremnantemia, smoking, and apolipoprotein B48 is one of them. (Non-patent Document 1). Thus, since ischemic heart disease is the most important issue to prevent rather than treating after onset, it is easy to ingest in daily life, and early prevention of risk factors for ischemic heart disease, and What can be improved is desired.

Diacylglycerol is a serum neutral fat lowering agent (Patent Document 1), an LDL cholesterol lowering agent (Patent Document 2), an HDL cholesterol increasing agent (Patent Document 3), a remnant-like lipoprotein increase inhibitor (Non-Patent Document 2), Known as a weight gain inhibitor (Patent Document 4), a fatty liver preventive and therapeutic agent (Patent Document 5), a PAI-1 lowering agent (Patent Document 6), a body fat combustion increasing agent (Patent Document 7), etc. It is said to be effective in the treatment and prevention of sclerosis and hyperlipidemia.
Japanese Unexamined Patent Publication No. 63-104917 JP 2006-62973 A JP 2001-64170 A Japanese Unexamined Patent Publication No. 4-300826 JP-A-4-300828 JP 2001-64169 A JP 2001-64672 A Large-scale clinical research to establish prevention and treatment methods for ischemic heart disease and cerebral infarction associated with hyperremnant lipoproteinemia 2005 General Research Report 2006, 45-47, Ministry of Health, Labor and Welfare Clin Chim Acta 311 (2), 109-117 (2001)

  An object of the present invention is to provide an agent that can be easily taken in daily life and suppresses an increase in blood apolipoprotein B48 concentration, which is one of risk factors for ischemic heart disease.

  The present inventor paid attention to diacylglycerol and examined the influence on the amount of lipoapoprotein in the blood after eating. It was found useful as an agent for preventing bloody heart disease.

  That is, the present invention provides an apolipoprotein B48 concentration increase inhibitor comprising diacylglycerol as an active ingredient.

  The apolipoprotein B48 concentration increase inhibitor of the present invention is useful as a preventive agent for ischemic heart disease because it suppresses an increase in serum apolipoprotein B48 concentration after meals and can be easily taken on a daily basis.

  The constituent fatty acid of diacylglycerol used in the present invention preferably has 8 to 24 carbon atoms, particularly 16 to 22 carbon atoms. It is desirable that the unsaturated fatty acid is preferably 70 to 100% by weight (hereinafter referred to as%), more preferably 80 to 100%, and more preferably 93 to 100% in the total constituent fatty acids of diacylglycerol. In particular, from the viewpoint of further enhancing the effect of suppressing the increase in apolipoprotein B48 concentration, the weight ratio is expressed as (cis-type unsaturated fatty acid amount / trans-type unsaturated fatty acid amount + saturated fatty acid amount) (hereinafter (cis) / (trans + saturated) weight ratio). ) Is preferably 5.5 or more. More preferably, the (cis) / (trans + saturated) weight ratio is 8 to 25, and more preferably 9 to 20. Of the constituent fatty acids of diacylglycerol, the trans unsaturated fatty acid content is particularly preferably 5% or less, and the saturated fatty acid content is particularly preferably 5% or less. Here, examples of the cis-type unsaturated fatty acid include oleic acid, α-linoleic acid, α-linolenic acid, cis-dihomoγ-linolenic acid, cis-arachidonic acid, cis-eicosapentaenoic acid, cis-docosahexaenoic acid, and the like. It is done. Examples of the trans unsaturated fatty acid include the trans unsaturated fatty acid. Examples of saturated fatty acids include palmitic acid, stearic acid, arachidonic acid, and the like.

  Diacylglycerol is produced, for example, by subjecting an oil and fat having the above-mentioned constituent fatty acid and glycerin to a transesterification reaction, or by causing a lipase to act on a target constituent fatty acid or a mixture of the ester and glycerin to carry out an esterification reaction. Is done. In order to prevent isomerization during the reaction, an esterification reaction using lipase is more preferable. Further, even in the esterification reaction using lipase, in order to prevent isomerization in the purification means after completion of the reaction, the purification means is preferably performed under mild conditions so that isomerization of fatty acid to trans acid does not occur.

  The composition obtained by the above method is usually an oil or fat composition containing diacylglycerol. In the present invention, it is preferable to use an oil or fat composition containing such a diacylglycerol. As such an oil-and-fat composition, the thing containing 20-99% of diacylglycerol, Preferably it is 40-95%, More preferably, it is 60-95% from the point of the increase inhibitory effect of apolipoprotein B48.

The oil and fat composition used in the present invention can contain about 0 to 0.05%, preferably 0 to 0.3% of plant sterols. Here, as plant sterols, α-sitosterol, β-sitosterol, stigmasterol, campesterol, α-sitostanol, stigmasteranol, campestanol, cycloartenol and the like, and their fatty acid esters, ferla Examples include acid esters and cinnamic acid esters.
As the plant sterol, a plant sterol derived from a vegetable oil / fat raw material may be used as it is, and the concentration may be adjusted by blending the plant sterol.

  The oil and fat composition may contain triacylglycerol and monoacylglycerol. The monoacylglycerol content is preferably 0 to 10%, preferably 0.1 to 5%, more preferably 0.1 to 3%. The triacylglycerol content is preferably 0 to 70%, preferably 4 to 55%, more preferably 4 to 35%.

  Since diacylglycerol and an oil-and-fat composition containing the same have an excellent inhibitory effect on serum apolipoprotein B48 concentration increase and are easy to take daily, health-oriented for the purpose of suppressing increase in serum apolipoprotein B48 concentration It is useful as a food and as a pharmaceutical.

  The serum apolipoprotein B48 concentration increase inhibitor of the present invention includes components contained in ordinary oil and fat compositions such as tocopherol, ascorbyl palmitate, ascorbate stearate, BHT, BHA, phospholipids, Emulsifiers such as sugar fatty acid esters, polyglycerin fatty acid esters, and organic fatty acid monoacylglycerols may be blended.

  The apolipoprotein B48 concentration increase inhibitor of the present invention becomes liquid at room temperature and can be widely used as edible oil. Therefore, the apolipoprotein B48 concentration increase inhibitor of the present invention can be suitably used as cooking oil and various processed oil and fat foods.

  Examples of processed foods include oil-in-water processed foods such as drinks, desserts, ice creams, dressings, toppings, mayonnaise; water-in-oil processed foods such as margarine and spreads; peanut butter, flying, baking shortenings, etc. Processed fats and oils; processed foods such as potato chips, snacks, cakes, cookies, pies, breads, chocolates; bakery mixes; processed meat products, frozen entrées; frozen foods. It can also be used in the form of capsules, tablets and the like.

  The intake of the apolipoprotein B48 concentration increase inhibitor of the present invention is preferably 0.03 to 80 g, more preferably 5 to 50 g, particularly 6 to 20 g as diacylglycerol per day for an adult.

  Serum apolipoprotein B48 concentration after ingesting a diet containing 30 g of diacylglycerol or triacylglycerol with uniform fatty acid composition in 10 men with BMI 27 or higher and HOMA-IR (Homeostasis model assessment for insulin resistance) 2 or higher The influence over time was measured by the ELISA method. The composition of the test oil is shown in Table 1. Table 2 shows the amount of increase in serum apolipoprotein B48 concentration obtained by subtracting the measured values 0.5, 4, 6, and 8 hours after ingestion from the initial value.

  From Table 2, if diacylglycerol is ingested, the increase in the maximum (4-6 hours) serum concentration of serum apolipoprotein B48 can be suppressed as compared to the case of ingesting triacylglycerol (general oil). it can.

Claims (2)

  An apolipoprotein B48 concentration increase inhibitor comprising diacylglycerol as an active ingredient.   2. The apolipoprotein B48 concentration increase inhibitor according to claim 1, wherein diacylglycerol has a fatty acid composition of 8 to 24 carbon atoms and 70% by weight or more of unsaturated fatty acids in all the constituent fatty acids.