JP2602387B2 - Lipase inhibitor - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to lipase inhibitors,
More specifically, it effectively inhibits pancreatic lipase, which is the key to obesity, which does not have lipid digestion and absorption in vivo, and can contribute to the suppression and prevention of obesity, and also causes degradation of foods and odor caused by lipase The present invention relates to a highly safe lipase inhibitor that can be used for preventing lipase.

[0002]

2. Description of the Related Art Lipase (pancreatic lipase) functions as a key enzyme in the digestion and absorption of lipids in humans, and attempts have been made to develop drugs that inhibit pancreatic lipase to suppress or prevent obesity. For example, JP-A-55-981
An antiobesity and triglyceride reducing agent described in No. 14,
Oxetanones described in JP-A-61-252663 and obesity preventive agents described in JP-A-1-102022 can be exemplified.

[0003] For the same purpose, foods and drinks to which an inhibitory substance isolated from cereals and beans are added (Japanese Patent Application Laid-Open No. 64-3426).
No. 4) and a method for extracting inhibitory substances from fat-rich seeds (JP-A-49-41580).

On the other hand, forage (Fodder plan)
t) that tannins inhibit lipase and (Bri)
tissue J. Nutrition, 60, 275
(1988)), and an extract (tannin) of beans (Field bean) is known to inhibit lipase (J. Sci. Food Agric., 30, 4).
58 (1979)). It has also been reported that proteins from soybeans, cereals and radish seeds inhibit this (Agr).
ic. Biol. Chem. , 37,1225,
(1973), Nurt. Rep. Int. , 3
2, 1107 (1985), Journal of the Japan Food Industry Association, 35,
430 (1988)). Further, hemicellulose, wheat bran, and the like (J. Food Sci., 49, 956 (19)
84), Am. J. Clin. Nutr. , 42,6
29 (1985)), phosphatidylcholine in soybean seeds (Research Report of the Faculty of Agriculture, Meiji University, 73, 9 (198)
6)), myo-inositol (J. Food Sc)
i. , 53, 250 (1988)) and the like.

[0005] Regarding crude drugs, extracts of 14 kinds of crude drugs such as peonies, oren, psyllium, buttonbi, genoshoko, tea and the like are disclosed as microorganisms against lipase (Japanese Patent Application Laid-Open No. 64-90131). In addition, the result of examining the inhibitory effect of 25 kinds of crude drugs against microbial lipase has been reported (Meiji University, Faculty of Agriculture, Research Report, 69, 15 (1985)).

More recently, a lipase inhibitor comprising an aqueous extract of peppers, pumpkins, shimeji, maitake, hijiki, green tea, black tea, and oolong tea (Japanese Patent Laid-Open No. 3-219873).
No. 3) and a lipid absorption-suppressed food (JP-A-3-228664) characterized by incorporating epigallocatechin gallate, which is a main component in green tea.

[0007]

It is known that natural crude drugs are highly safe and have various medicinal effects. From the extracts of these many crude drugs, those that inhibit lipase activity were searched, and this time, it was found that several kinds of crude drug extracts had a remarkably high inhibitory effect.

[0008] The present invention has a remarkably high inhibitory effect on pancreatic lipase, which controls the digestion and absorption of lipids in vivo and is a key to obesity, and can inhibit this to contribute to the suppression and prevention of obesity. An object of the present invention is to provide a highly safe lipase inhibitor that can be used for preventing deterioration of foods and the like and odor generation due to lipase.

[0009]

According to the present invention, a polar or non-polar solvent extract of one or more crude drugs selected from the group consisting of Dokkatsu, Ryokyo, Acacia, L., Sempens and Katsumeishi is used as an active ingredient. A lipase inhibitor is provided.

[0010] Dokkatsu (independent) is Angelica
It is the root of pubescens maximowicz (Shishuudo), and is said to be effective in Chinese medicine as a sweating, carminative, and painkiller to remove colds and spread edema. Glabra-lactone, Angelical on roots
(7-Methoxy-6-coumarinalde
hyde) is present.

[0011] Ryokyo (Ryokyo) is a ginger of the family Ginger, Alpina officinarum.
The rhizome of Hance (general name galanga) is called Ryokyo.

[0012] Betel nut (Acacia lutes) is a species of betel palm, Areca Cathu L. And grown in Malaya, Indonesia and the Philippines. Arecoline, Arecadin, Guva
Cine and the like are present therein, and are said to be effective in removing parasites and healing visual impairment. Malayas and Thais have the habit of biting this.

[0013] Youbaihi (Yangmei skin) is, bayberry, My
rica rubra Siebold et Zuc
It is the bark of carini and is found throughout Kyushu. It is known that tannin, Myricetin and the like exist. In Kampo, it is said to be effective for diarrhea, bruises and detoxification.
Myricetin has a diuretic effect.

[0014] Sampens (Yamabushi) is a Japanese name for "Karaoketsumei" , Cassia noname Honda ( Ca
ssia mimosoides L. var. n
Oma Makino) is a dried version of the foliage at the orchard stage, and is produced throughout the country. Tea is used as beach tea and bean tea instead. It is said that Kampo has diuretic and laxative effects. It is said that there is no side effect even with heavy drinking.

[0015] Ketsumeishi (cassia seed) is, sicklepod (C
assia obtusifolia L. ) Is a mature seed and is native to tropical Asia. It is said that Chinese medicine has a laxative effect, tonicity, and visual acuity improving effect. The component is E
modin, Obtusifolin and the like are known. It is called hub tea and tea is consumed instead.

In extracting the active ingredient from these crude drugs, the extraction solvent is water (or buffer) or an organic solvent (eg, hexane, ether, chloroform, benzene, toluene, ethyl acetate, tetrahydrofuran, butanol, propanol, acetone, ethanol). , Methanol, etc.), one or more of which can be selected, but it is desirable to use water or a buffer for Dokkatsu, Ryokyo, Acacia, and Ilex. Examples of the buffer include docker, areca and oleax which can be suitably used in the pH range of 3.0 to 10.0. On the other hand, it is preferable to use an organic solvent such as THF for Sampens and Katsumeishi.

The crude drug extract can be diluted with an appropriate solvent or concentrated. Further, it can be used in the form of paste or powder by operations such as suction and freeze-drying. These can be mixed in advance with foods or the like, or can be formulated as appropriate and used as a lipase inhibitor.

[0018]

The present invention relates to a lipase inhibitor comprising, as an active ingredient, a polar or non-polar solvent extract of one or more crude drugs selected from the group consisting of six crude drugs of Dokkatsu, Ryokyo, Amberjack, Ilex, Sampens and Ketmeishi. Agent.

These extracts are more effective than tea extracts, which are conventionally considered to have a high lipase inhibitory action. These extracts are not synthetic substances but derived from natural plants, so that their safety is high. High inhibitors can be provided.

These extracts can be used to prevent obesity by inhibiting digestion and absorption of fats and oils, to prevent diseases caused by lipase,
Can be used for prevention. Further, these extracts can be used to prevent deterioration of foods and the like and odor caused by lipase.

[0021]

Industrial Applicability According to the present invention, the present invention has a remarkably high inhibitory effect on pancreatic lipase, which controls the digestion and absorption of lipids in vivo and is a key to obesity, and inhibits this to contribute to the suppression and prevention of obesity. The present invention provides a highly safe lipase inhibitor which can be used for preventing deterioration of foods and the like and malodor caused by lipase.

The lipase inhibitor of the present invention strongly and effectively suppresses the activity of lipase, and is safer because it is derived from natural products unlike synthetic substances.

The product of the present invention can be used for prevention of obesity by lipase inhibition, prevention and prevention of various diseases caused by lipase, and prevention of malodor accompanying degradation of oils and fats caused by lipase. It can be applied to the prevention of deterioration of foods and the like.

[0024]

The present invention will be described in more detail with reference to the following examples, but the present invention is not limited to the following examples.

Example 1-1 (Measuring method of lipase activity ) The lipase activity was measured by using oleic acid ester of 4-methylumbelliferone (4-MUO) as a substrate and producing 4-methylumbelliferone by reaction. This was done by measuring the fluorescence of methylumbelliferone.

The small examiner asked the substrate 4-MUO suspension 1
00 μl, porcine pancreatic lipase (manufactured by Sigma) solution 50
μl and 50 μl of buffer solution, and finally 4-MUO.
05 mM, porcine pancreatic lipase 2.2 μg, Mcllvai
The reaction was carried out at 37 ° C. for 20 minutes under the conditions of a ne buffer (pH 7.4). The reaction was stopped by adding 1 ml of 0.1N hydrochloric acid, and the pH of the solution was adjusted to around 4.3 by adding 2 ml of 0.1 M sodium citrate.
-Fluorescence of methyl umbelliferone (excitation wavelength 320 n
m, fluorescence wavelength 450 nm) was measured with a fluorometer.

Example 1-2 (Preparation of Extract Extract) Dried crude drug was pulverized, and a 50-fold amount of Mc with respect to the pulverized product was used.
After adding an llvaine buffer, homogenizing with a homogenizer and immersing for 1 day for extraction. This was filtered, and the filtrate was used as an extract. Some crude drugs were extracted by the following method. The crushed product is extracted and defatted for one day with 5 times the amount of hexane, and the extraction residue is suction-dried. After adding 5 times the amount of tetrahydrofuran and extracting for 1 day,
After filtration, the filtrate was used as an extract.

Example 1-3 (Measurement of Effect of Extract Extract ) The measurement of the inhibitory effect of the extract on lipase activity was carried out as follows.
Extraction extract was added to the lipase activity measurement system shown in the above Examples and reacted to examine the effect on the activity.

To the extract extracted with Mcllvaine buffer, 50 μl of the extract was added instead of 50 μl of the reaction system buffer, and 5 μl of the extract extracted with THF was added. In addition, the thing which added the same solvent and the same solvent as an extract was set as control, and the activity at the time of adding an extract was shown as relative activity with respect to a control.

Examples 1-4 (Comparison of Various Extracts) The effects of various crude drugs on the lipase activity were examined in accordance with the above Examples. Table 1 shows the results.

[0031]

[Table 1]

It is known that tea extract has a high lipase inhibitory activity, but as is clear from Table 1, these crude drug extracts have a clearly higher lipase inhibitory activity than tea extract. I found out.

Claims (1)

(57) [Claims] 1. Dokatsu, Ryokyo, Areca,
A lipase inhibitor comprising, as an active ingredient, a polar or non-polar solvent extract of one or more crude drugs selected from the group consisting of Spruce, Sampen's and Katsumeishi.