JP3507116B2 - Cholesterol elevation inhibitor - Google Patents

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to banaba leaves (Lagerstroemia speciosa) from Southeast Asia, including the Philippines.
l.) and a cholesterol elevation inhibitor.

[0002]

2. Description of the Related Art Banaba is a plant of the family Liliaceae that is distributed in tropical Asia, and is also known as Pleurotus cornucopia. In the Philippines, which is the place of origin for a long time, these leaves have been decocted and consumed. On the other hand, however, since Banaba leaves were produced in the tropics, they were heavily contaminated with various bacteria, and required a sufficient sterilization operation for normal drinking.

Conventionally, in order to extract this main component,
First, banaba leaves are crushed, then heat sterilized and packed directly into tea bags or the like, and then brewed for a long time as in the case of traditional Chinese medicine. In the method, it is difficult to perform homogeneous extraction because the extraction conditions are not maintained at all, and the once-decocted extract is easy to rot and does not last as long as it is.
It was necessary to brew the required amount every day, which was very troublesome and troublesome.

Therefore, the inventor of the present invention extracted banaba leaves with hot water, an organic solvent or a mixed solution of an organic solvent and hot water, concentrated the extract solution, and dried it to obtain a dry powder.
A method for extracting a banaba leaf powder extract from banaba leaves is disclosed (JP-A-5-310587).

Regarding the pharmacological effect of the banaba leaf extract thus obtained, the pharmacological effect as an antidiabetic agent was confirmed in the above-mentioned JP-A-5-310587, but other pharmacological effects are still uncertain. I can't find any reports that I confirmed.

[0006]

Therefore, an object of the present invention is to clinically confirm the pharmacological effect of a banaba leaf extract extracted from banaba leaves under certain conditions, while at the same time increasing the cholesterol elevation inhibitor from the banaba leaf extract. Is to get.

[0007]

In the present invention, banaba leaves are extracted with hot water or an organic solvent, or a mixed solution of an organic solvent and water, and a cholesterol elevation inhibitory agent containing this extract as an active ingredient is obtained. Was successful. Furthermore, the extraction solution obtained by extracting banaba leaves with hot water or an organic solvent, or a mixed solution of an organic solvent and water was adsorbed on a synthetic resin adsorbent, and distilled water was flowed to prevent resin adsorption. We succeeded in obtaining a cholesterol elevation inhibitor from the banaba leaf extract thus separated and purified by allowing the components to flow out and separating and purifying an extract having a higher cholesterol elevation inhibiting effect.

The banaba leaf extract according to the present invention is obtained by extracting dried and crushed banaba leaves with hot water at a temperature of about 60 ° C to 100 ° C, preferably close to or above the boiling point, that is, 95 ° C to 100 ° C. Either extraction with a solvent such as methanol or ethanol, extraction with a mixed solution of an organic solvent and water, or extraction of the residue after the above hot water extraction with a mixed solution of an organic solvent or an organic solvent and water is performed. Obtainable. At this time, the amount of hot water, the organic solvent, or the mixed solution of the organic solvent and water is 1:10 to 1: 100, preferably about 1:25 with respect to the weight of the dried banaba leaf. .

As the synthetic resin adsorbent in the present invention,
Styrene-divinylbenzene synthetic resin such as DIAION HP-10,20,30,40,50 manufactured by Mitsubishi Kasei Co., Amberlite XAD-2,4 manufactured by Organo, or Sumitomo Chemical Co., Ltd. ) The duolite s series manufactured by
Dextran-based synthetic resin, such as Sepha manufactured by Pharmacia
adex LH-20 can be used. The dextran-based synthetic resin forms a polysaccharide-like stitch in which the dextran chains constituting the dextran chain are three-dimensionally cross-linked, so that the ratio of the number of carbon atoms to the hydroxyl group is relatively large, particularly LH-2.
Since 0 has a hydroxypropyl group that is ether-bonded to each glucose unit of the dextran chain,
Especially big. Therefore, the dextran-based synthetic resin gel, particularly LH-20, has both hydrophilicity and lipophilicity and can be considered to be similar to the styrene-divinylbenzene-based synthetic resin in terms of adsorptivity. However,
At present, the styrene-divinylbenzene-based synthetic resin is superior from the economical point of view.

[0010]

【Example】

[Production method] Fresh leaves of Philippine Banaba are dried naturally or forcibly and adequately and then crushed with a crusher. 1 kg of well-mixed Banaba leaves is squeezed in about 50 liters of distilled water for about 30 minutes. Extracted at 100 ° C. The obtained extract was filtered, centrifuged, and then concentrated by an evaporator and dried by a method such as freeze-drying or spray-drying to obtain a crude extract (banaba leaf extract). At this time, the yield of the crude extract was about 10% (W / W) based on the dried banaba leaf (raw material).

Next, a glass column having a diameter of 10 cm and a length of 100 cm was filled with 2.5 liters of a styrene-divinylbenzene synthetic resin (product name: DIAION HP-20 manufactured by Mitsubishi Kasei Kogyo Co., Ltd.), and this filling was performed. After the agent was washed with methanol and further washed with distilled water, the crude extract (total amount) was dissolved in 1 liter of distilled water, and this was poured into a glass column. Then, about 6 times as much distilled water as the column volume was flowed to flow out the fraction not adsorbed on the styrene-divinylbenzene-based synthetic resin (hereinafter referred to as non-adsorbed fraction), while 10 times the equivalent of about 5 times
A fraction adsorbed on the styrene-divinylbenzene-based synthetic resin (hereinafter referred to as an adsorption fraction) was eluted by flowing 0% methanol. The non-adsorbed fraction and the adsorbed fraction thus obtained were concentrated and dried by a method such as freeze-drying or spray-drying to obtain a dry powder. The yields at this time were about 4.3% for the non-adsorbed fraction and about 2.7% for the adsorbed fraction based on the dried banaba leaf (raw material).

[Cholesterol elevation inhibitory effect test] Using a type II hereditary diabetic mouse, a cholesterol elevation inhibitory effect test of banaba leaf extract was tested as follows.

[0013] Using the adsorption fraction and unadsorbed fraction obtained by the above production method as a test sample, KKA ^y T ^a as experimental animals
^Jc1 mice (type II inherited diabetic mice) were used.

(1) Experiment 1 Type II hereditary diabetic mice (4 weeks old) were fed a basic diet (gasein 25.0% (W / W) (hereinafter% (W / W) omitted), salt mixture 3.
5, vitamin mixture 1.0, vitamin C and vitamin K
0.2, choline chloride 0.2, corn oil 5.0, sugar 5
After breeding for 1 week with 1.0, starch (α) 14.1), it was divided into two groups of 7 animals each, and one group contained 5.0% (W / W) of cellulose equivalent to the above basic diet. Was added to the target group, and the other group had 5
% (W / W) A diet supplemented with an equivalent amount of crude extract (banaba leaf extract) was administered (hereinafter, referred to as “crude extraction group”), and each was bred for 6 weeks. The diet was administered orally. Finally, blood was collected from the tail vein of the mouse to quantify the total cholesterol in the blood, and the results are shown in Table 2.

[0015]

[Table 1]

From Table 1, it was confirmed that the blood total cholesterol of the crude extraction group was significantly suppressed as compared with that of the control group.

(2) Experiment 2 In the same manner as in Experiment 1 above, after breeding with a basic diet for 1 week,
One group was treated with a diet containing 5.0% (W / W) of the above-mentioned basic food and cellulose as a target group, and the other group was administered with 2.0% (W / W) of the basic food. / W) A diet to which a considerable amount of the adsorbed fraction was added was administered (hereinafter referred to as "adsorption fraction group"), and to another group, 3.0% (W /
W) A diet to which a considerable amount of the non-adsorbed fraction was added was administered (hereinafter, referred to as "non-adsorbed fraction group"), and each was bred for 5 weeks. Body weight, feed intake and water intake before and after breeding were measured, and finally blood was collected from the tail vein to quantify blood total cholesterol and blood triglyceride, and the results are shown in Table 2. The diet was administered orally.

[0018]

[Table 2]

From Table 2, the total blood cholesterol in the adsorbed fraction group was significantly suppressed as compared with that in the control group. Furthermore, rather than blood total cholesterol of this adsorption fraction group,
That of the non-adsorbed fraction group was significantly suppressed. In this case, from the fact that the effect of suppressing the cholesterol elevation of cellulose, which is one of the dietary fibers, has already been confirmed,
It is clear that the non-adsorbed fraction and the adsorbed fraction, that is, the banaba leaf extract of the present invention exerts an effect comparable to that of cellulose in terms of cholesterol suppressing action. Also,
Regarding blood triglyceride (triglyceride), the value of blood triglyceride in the non-adsorption group tended to be closer to the value of the control group than the value of the adsorption fraction group. The effect of suppressing the increase in blood triglyceride (triglyceride) of cellulose has already been confirmed.

From the above, it was found that the banaba leaf extract component, especially the non-adsorbed fraction, has a cholesterol elevation inhibitory action. Further, it can be presumed that such a blood cholesterol elevation suppressing action is due to a dietary fiber-like action.

[Effective amount] Assuming that the amount of food consumed by one mouse per day is 0.6 g, the results of Experiments 2 and 3 above and the average body weight of the mice are about 22 g. Approximately 1.4 per kg of mouse body weight
g / day, the non-adsorbed fraction was about 0.
It was found that the intake of only 82 g / day exerts a sufficient inhibitory effect on cholesterol elevation.

[Toxicity test] To a type II hereditary diabetic mouse, a diet prepared by adding the crude extract obtained by the same method as the above-mentioned production method to the above-mentioned basic diet in an amount equivalent to 5% (W / W) thereof for 6 consecutive weeks As a result of administration and observation, no side effects were observed in the mice during and after administration.

[0023]

EFFECTS OF THE INVENTION According to the present invention, it has been revealed that the component containing the banaba leaf extract has an excellent effect of suppressing cholesterol elevation. Furthermore, by adsorbing to a styrene-divinylbenzene-based synthetic resin or a dextran-based synthetic resin and extracting the banaba leaf extract component that has not been adsorbed by the resin, it is possible to separate and purify a component having a higher cholesterol elevation inhibitory effect. Was also found.

Regarding the effective amount of the cholesterol elevation inhibitor of the present invention, the mouse body weight is 1 kg / day, about 1.4 g / day, and the purified one is mouse body weight 1 kg / day.
If only 0.82 g / day is ingested, a sufficient effect of suppressing cholesterol elevation can be obtained, but human sensitivity is higher than that of mice. 1 to 1/100 of
It is estimated that the amount depending on the weight ratio of is sufficient.

Further, the safety of the cholesterol elevation inhibitor according to the present invention is clear from the fact that teas brewed from banaba leaves have always been drunk in the Philippines, etc. You can check its safety.

The agent for suppressing cholesterol elevation of the present invention can be sterilized by autoclave, frozen, for example, freeze-dried to obtain a powder extract, which can be molded into tablets, capsules or granules to be used as a medicine. Further, the powdered extract can be diluted to a suitable concentration for drinking so that it can be made into a can drink or a bottle drink for easy drinking. It can also be mixed with other crude drugs or juices.

   ─────────────────────────────────────────────────── ─── Continued front page    (72) Inventor Toshio Kawasaki               21 Goddess, Sagara-cho, Haibara-gun, Shizuoka Prefecture               Fujizono Central Research Institute (72) Inventor Hisao Nao               2787-34 Otani, Shizuoka City, Shizuoka Prefecture                (56) Reference JP-A-5-279264 (JP, A)                 JP-A-1-299224 (JP, A)                 JP-A-5-336939 (JP, A)                 Mitsuo Takahashi, Ingredients of crape myrtle               (7th Report) Tohoku Pharmaceutical University               Academic Research Annual Report, 1981, vol. 28, p               p. 85-87                 Takashoi Tanaka e               t al, Tannins and R               elevated Compounds C               XVII. Isolation and                 Characterization               of Three New Ellag               itannins, Chem. Phar               m. Bull. , 1992, Vol.               40, No. 11, pp. 2975-2980

Claims (3)

(57) [Claims] 1. An extraction solution obtained by extracting banaba leaves with hot water at about 60 ° C. to 100 ° C. is further added to styrene-dibi.
Nylbenzene synthetic resin or dextran synthetic resin
Adsorbed Banaba leaf extract that was not adsorbed by resin is effective
Cholesterol elevation inhibitory agent as a component . 2. An extraction solution obtained by extracting banaba leaves with an organic solvent or a mixed solution of an organic solvent and water is further extracted.
Tylene-divinylbenzene synthetic resin or dextran
Banaba leaves that have been adsorbed on a synthetic resin and not adsorbed on the resin
An agent for suppressing cholesterol elevation, which comprises an extract as an active ingredient . 3. An extract solution obtained by extracting banaba leaves with hot water at about 60 ° C. to 100 ° C. and extracting the residue with an organic solvent or a mixed solution of an organic solvent and water,
-Divinylbenzene synthetic resin or dextran compound
Banaba leaf extraction that was adsorbed on synthetic resin and was not adsorbed on resin
Cholesterol elevation inhibitory agent containing a substance as an active ingredient .