JP4613017B2 - Oral composition containing difructose anhydride - Google Patents

Description

  The present invention relates to an oral composition having a β-glucosidase activity enhancing action in intestinal contents. The present invention also relates to an oral composition that promotes absorption of a physiologically active substance body by degrading a glycoside having physiological activity by enhancing β-glucosidase activity in the intestinal contents.

In general, food components taken orally by humans are absorbed by passive transport or active transport from the small intestine after degradation by digestive enzymes of the small intestine. When the components are oligosaccharides or polysaccharides, they are hydrolyzed into monosaccharides and absorbed by hydrolytic enzymes such as intestinal maltase, sucrase, trehalase or lactase.
Many food components useful for living organisms such as flavonoids, isoflavonoids, saponins, anthocyanins, pyridoxine and the like that are orally ingested as glycosides are known. In particular, flavonoid glycosides and isoflavonoid glycosides are said to be absorbed after sugar and aglycone are released after hydrolysis by the small intestine sugar hydrolase. However, its hydrolysis and absorption are not complete, and some of these glycosides reach the large intestine and are absorbed after hydrolysis with enzymes derived from intestinal bacteria. Some of these glycosides are absorbed into the body and discharged as they are without performing their functions.
It is known that beta-glucosidase contributes greatly as an enzyme derived from intestinal bacteria that hydrolyzes flavonoid glycosides and isoflavonoid glycosides in the large intestine. (Non-Patent Document 1: Rowland I et al. British Journal of Nutrition 89, separate volume 1 pages S45-S58 2003)

On the other hand, difructose anhydride III (hereinafter referred to as DFA III) has a bifidobacteria growth action (Patent Document 1: Japanese Patent Publication No. 3-5788) and increases the amount of calcium absorption (Patent Document 2: Japanese Patent Laid-Open No. 11-151). No. -43438) and having a diuretic action (Patent Document 3: Japanese Patent Laid-Open No. 2003-321371) have already been known, but the action of enhancing the beta-glucosidase activity in the intestinal contents has not been known.
Japanese Patent Publication No. 3-5788 Japanese Patent Laid-Open No. 11-43438 JP 2003-321371 A Rowland I et al. British Journal of Nutrition Vol. 89, separate volume 1 pages S45-S58 2003

  As described above, glycosides useful for living organisms are usually excreted without being completely absorbed. Then, this invention makes it a subject to accelerate | stimulate absorption of the glycoside useful for a biological body.

  The inventors of the present invention focused on the beta glucosidase activity in the intestinal contents and, as a result of continuing research, have the effect of enhancing the beta glucosidase activity in the intestinal contents and further promote the absorption of glycosides having physiological activity. It has been found that beta-glucosidase activity in the intestinal contents is increased by administration of difructose anhydride as a component having an action to act. That is, the present invention relates to an oral composition having a beta-glucosidase activity enhancing action in intestinal contents, characterized by containing difructose anhydride as an active ingredient.

(1) An oral composition comprising difructose anhydride and a glycoside having physiological activity (2) The oral composition of (1), wherein the glycoside having physiological activity is a polyphenol glycoside (3) The oral composition of (1), wherein the glycoside having physiological activity is a flavonoid glycoside or an isoflavonoid glycoside.

Oral compositions containing the difructose anhydride of the present invention enhance beta glucosidase activity in the intestinal contents.
By enhancing the beta glucosidase activity, absorption of glycosides having physiological activity can be promoted.
By providing an oral composition containing difructose anhydride and a glycoside having a physiological activity, the glycoside having a physiological activity can be absorbed into the body with a good effect.

  The difructose anhydride (DFA) as used in the present invention is a cyclic disaccharide in which the reducing ends of two fructose are bonded to a hydroxyl group other than one reducing end. Conventionally, it was known to exist in caramel and the like, but industrially, inulin is produced by an inulin-degrading enzyme, for example, inulin fructotransferase (EC 2.4.1.93) produced by Arthrobacter sp. Strain H65-7. Or levan can be fermented with levanfructotransferase (EC 2.4.1.10) produced by Arthrobacter nicotinovorans GS-9. There are five types of derivatives due to the difference in the binding mode of bimolecular fructose, which are referred to as DFAI, DFAII, DFAIII, DFAIV, and DFAV, respectively. The DFA as used in the present invention refers to all of them, but in the present invention, DFAIII (di-D-fructofuranose-1,2 ′) which is excellent in industrial production efficiency, stability after purification, etc. : 2,3'dianhydride) and DFAIV (di-D-fructofuranose-2,6 ': 6,2'dianhydride) are preferably used.

  The oral composition according to the present invention contains DFA as an active ingredient, and can be used as a pharmaceutical type, food and drink type, animal feed type composition, for example, for humans or animals. There are no limitations as long as it is a form that can be finally administered orally, such as pharmaceuticals, foods and drinks, prepared milk powder, enteral nutrients, health foods and drinks, and feed additives. Moreover, the content of the active ingredient is not particularly limited.

  When used as a food-and-drink type composition, DFA or a processed product thereof can be used as it is or in combination with other foods or food ingredients, and can be used according to conventional methods. Moreover, since the heat stability and acid stability are high in processing, a normal food processing method can be applied without any problem. The food type oral composition containing DFA is not subject to any particular limitation such as powder, granule, paste, liquid or suspension. For example, it can also be exemplified by formulating into a health drink using various ingredients commonly used in the production of sweeteners, sour agents, vitamins and other drinks.

  When used as a pharmaceutical type composition, the active ingredient is administered in various forms. Examples of the dosage form include oral administration using tablets, capsules, granules, powders, syrups and the like. These various preparations are usually used in the pharmaceutical formulation technical field such as excipients, binders, disintegrants, lubricants, flavoring agents, solubilizers, suspension agents, coating agents, etc. Can be formulated using known adjuvants. The amount used varies depending on symptoms, age, body weight, and dosage form, but is usually in the range of 0.5 to 2000 mg, preferably 1 to 1000 mg per kg of body weight per day for oral administration to adults. It is better to administer.

Examples of the glycoside having a physiological activity in the present invention include polyphenol glycosides and flavonoid glycosides.
Polyphenol refers to a compound having a plurality of hydroxyl groups in the benzene ring. Tannins (gallotannins and ellagitannins as hydrolyzed tannins, catechins and epicatechins as condensed tannins), catechins (catechins and epicatechins), flavonoids (flavones, Flavonol, flavanone, flavanonol, isoflavone, chalcone, aurone, leucoanthocyanin, catechin), lignan (sesaminol, pinoresinol), lignin, coumarin, simple phenol (protocatechuic acid, gallic acid, syringic acid), etc. It is known to have By ingesting the difructose anhydride of the present invention, digestion and absorption of these polyphenols can be promoted.

  Flavonoids are also included in the above polyphenols, but in a narrow sense, flavones (such as luteolin and apigenin), flavonols (such as quercetin and kaempferol), flavanones (such as naringenin and hesperetin), flavonols, isoflavones (such as daidzein, genistein, and glycitein) ) In a broad sense, and includes anthocyanidins, leucocyanidines, catechins, chalcones (phloretin, isoliquiritigenin, etc.), aurones, cumestanes (eg, cumesterol), etc.

  Flavonoids are expected to have antioxidant effects, but other flavonoids with estrogenic activity include chalcones isoliqueritigenin, isoflavones genistein, daidzein, glycitein, flavonol kaempferol, and flavanones naringenin. And flavones apigenin and kumestane cumesterol. In addition, flavonoids are expected to be effective in preventing cancer, preventing aging, and improving effects such as dementia / diabetes / arteriosclerosis / gastric ulcer / hepatitis.

  The oral composition of the present invention can be formulated with DFA together with the above-mentioned polyphenols or flavonoid glycosides having physiological activity, which is preferable for promoting the absorption of these glycosides.

〔Example〕
The present invention will be described in more detail with reference to the following examples, which are merely illustrative and the present invention is not limited thereto.

The intestinal beta-glucosidase activity enhancing action of DFA was examined.
After 24 Wistar male rats (3 weeks old) were preliminarily raised on solid feed for 3 days, they were given 7 g of basic food for 3 days and divided into 4 groups. Each was fed a diet consisting of 7 g basic food plus 0.5 g DFA III or 0.5 g sucrose. After 3 weeks of this breeding, the animals were sacrificed, the contents of the cecum were collected, and beta-glucosidase was measured by the following method.
After collecting the contents of the cecum, the contents were stirred in place to make it uniform. The total weight of the contents was measured and stored at −20 ° C. until analysis. About 0.5 g of a sample was collected, 0.1 M phosphate buffer (pH 6.4) was added to a concentration of 1:20 (w / w), homogenization was performed under ice cooling, and then ultrasonic waves ( 20s) The supernatant was crushed and centrifuged (500 G × 15 min) for measurement. 200 μL of a measurement sample was added to 100 μL of p-nitrophenol glucoside (1.5 mg / mL) and incubated at 37 ° C. for 30 minutes. Thereafter, 1.6 mL of a 0.25 mol / L sodium carbonate solution was added, and the absorbance at 400 nm was measured. From the measured absorbance, the absorbance of the sample blank was subtracted, and the amount of product per 30 minutes was calculated using the calibration curve of the p-nitrophenol solution.

The results are shown in Figure 1.
In FIG. 1, S is an abbreviation for sucrose, and D is an abbreviation for DFAIII. Moreover, 0.5 shows that the feed which added 0.5g to the basic meal of 7g was given.
As is clear from this result, the ingestion of DFA showed an enhancement of the beta glucosidase activity of the intestinal contents.

The formulation example of the tablet containing DFAIII (Difructose Anhydride) and Rutin (flavonoid glycoside) is shown.
Formulation Example 1 Tablet (Amount: Mass%)
DFAIII 77
Quercetin 4 glucoside * 2
Cornstarch 20
Guar gum 1
* Quercetin 4 glucoside is a glucose glycoside of quercetin, a kind of flavonoid.

The formulation example of the juice containing DFAIII (difructose anhydride) and daidzin (flavonoid glycoside) is shown.
Formulation Example 2 Juice (Amount:% by mass)
DFAIII 10
Daijin * 2
Frozen and concentrated Wenzhou mandarin orange juice 5
Citric acid 0.2
L-ascorbic acid 0.02
Fragrance 0.2
Dye 0.1
Water 82.48
* Daidine is a glucose glycoside of daidzein, a type of flavonoid.

Graph showing enhancement of beta-glucosidase activity by DFAIII

Claims (3)

  An oral composition comprising difructose anhydride and a glycoside having physiological activity   The oral composition according to claim 1, wherein the glycoside having physiological activity is a polyphenol glycoside.   The oral composition according to claim 1, wherein the glycoside having physiological activity is a flavonoid glycoside or an isoflavonoid glycoside.