JPH0358330B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention provides aqueous or aqueous organic solvent extracts of one or more crude drugs selected from Saiko, Chimpi, and Scholasticus, or one or more crude drugs selected from Saiko, Chimpi, and Scholoma The lipolysis promoting effect of cancer toxin (toxohormone L) which has lipolytic action is made by adding water or aqueous organic solvent extract of seven kinds of herbal medicines, such as soybean citrus, carrot, licorice, horsetail, and turmeric, as an active ingredient. It is a cancer symptom-improving agent characterized by inhibiting and improving lipid metabolism and anorexia in cancer-bearing patients. Toxohormone L is an acidic protein with a molecular weight of around 70,000 isolated from human liver cancer ascites, and is a factor that acts on adipose tissue and promotes fat decomposition.
Intracerebroventricular injection of rats causes decreased appetite, etc.
Possible cause of body fat loss in cancer cachexia (CANER RESEARCH41, 284-288,
January 1981). The present inventors have provided water or aqueous organic solvent extracts of one or more crude drugs selected from Saiko, Chimpi, and Shyouma, or one or more crude drugs selected from Saiko, Chimpi, and Shyouma. A new drug that contains water or an aqueous organic solvent extract of seven types of herbal medicines, including Astragalus japonica, Astragalus japonica, Carrot, Licorice, Angelica, and Sargassum, inhibits the lipolysis promoting effect of toxohormone L and suppresses a decrease in appetite. The present invention was completed by paying attention to this knowledge. The crude drug extract in the present invention is one or more crude drugs selected from Saiko, Chimpi, and Shyouma, or one or two or more crude drugs selected from Saiko, Chinpi, and Shyouma, and
A crude drug containing seven kinds of herbal medicines, such as Astragalus japonica, Astragalus japonica, Carrot, Licorice, Angelica, and Astragalus, is extracted with water or an aqueous organic solvent [e.g., aqueous alcohol (such as aqueous methanol, aqueous ethanol)],
The obtained extract is filtered and dried by a conventional drying method such as spray drying, freeze drying, or concentration drying. To obtain the desired extract, one or more of the above herbal medicines may be mixed and extracted, or each crude drug may be extracted and then mixed. Extraction conditions can be carried out at room temperature or under heating, but it is preferable to carry out under heating. This extract can be used as it is, but it can be used in powders, granules, tablets, etc. by adding excipients, adjuvants, lubricants, etc. that are used in ordinary formulations and according to the usual method of manufacturing formulations. It can also be used in preparations such as capsules. If desired, this extract may be further purified and used by conventional methods such as dialysis and various chromatography methods. A specific example of the production of the crude drug extract is as follows. Specific example 1. 4.0g each of Astragalus, Sojuyutsu, and Carrot, 3.0g of Astragalus, 2.0g each of Saiko, Asparagus, and Chinpi, 1.5g of Licorice, 1.0g of Asparagus, and 0.5g of Asparagus
Add 10 times the amount of water, that is, 240 ml, to the mixed herbal medicine, heat and extract at 100°C for 1 hour, filter the resulting extract, and spray dry to obtain 2.2 g of dry extract powder. Specific Example 2 Add 10 times the amount of water, that is, 1 part of water, to 100 g of Saiko, heat and extract at 100°C for 1 hour, filter the resulting extract, and concentrate to dryness to obtain 9.5 g of dry extract powder. Specific Example 3 Add 10 times the amount of water, that is, 1 part of water, to 100 g of Chimpi and extract by heating at 100° C. for 1 hour. The obtained extract is filtered and concentrated to dryness to obtain 10.2 g of dry extract powder. Specific Example 4 Add 10 times the amount of water, that is, 1 part of water, to 100 g of Japanese cabbage, heat and extract at 100°C for 1 hour, filter the resulting extract, and freeze-dry to obtain 8.9 g of dry extract powder. Next, experiments and results regarding the inhibition of the lipolysis-promoting effect of toxohormone L by the drug of the present invention will be explained. 100 mg of epididymal adipose tissue sections from male Wistar rats (weight 150-180 g) were suspended in Krebs-Ringer bicarbonate buffer (PH7.4), and 0.1 ml of ascites from a liver cancer patient was used as toxohormone L solution.Specific Example 1 After centrifuging the drug aqueous solution (20 mg/ml) of Specific Example 4 from
Add 0.1 ml of the dialyzed supernatant, 0.5 ml of 5% bovine serum albumin solution, and 0.1 mMCaCl ₂ aqueous solution to make a final volume of 1.0 ml, and after culturing at 37°C for 2 hours,
Free fatty acids were measured by Dole's method. The results are shown in Table 1. That is, Table 1 shows the results of the drug-free group and the drug-administered groups of Specific Examples 1 to 4 regarding the lipolysis promoting effect of toxohormone L. From the results shown in Table 1, it was confirmed that the drug of the present invention inhibits the lipolysis promoting effect of toxohormone L.

[Table] Next, experiments and results will be explained regarding the ability of the drug of the present invention to alleviate loss of appetite caused by cancer. After transplanting AH130 ascites hepatoma into 4-week-old Donriyu male rats, they were given normal feed (Claire powdered feed) or feed mixed with the drug obtained in Specific Example 1 (Specific Example 1 equivalent to 100 mg/Kg in Claire powdered feed).
Feed for a group given free access to the drug-mixed feed (drug-mixed feed) obtained in Example 1 and given normal feed, and a group given the feed mixed with the drug obtained in Example 1 (drug-mixed feed). Intake was measured. The results are as shown in the drawing. That is, the figure shows the results of the normal feed group and the drug-mixed feed group on appetite loss in AH130 ascites liver cancer-transplanted rats. From the results shown in the drawings, it was confirmed that the drug of the present invention suppresses appetite loss caused by ascites liver cancer. Acute toxicity test for oral administration of the drug of the present invention
When tested using ddY male mice and Wistar male rats, the drugs obtained in Examples 1 to 4 did not cause death even when administered orally at a dose of 15 g/Kg. Therefore, the drug of the present invention has extremely low toxicity and high safety. Considering the experimental data and acute toxicity test results of the present invention, the effective dosage of the drug of the present invention varies depending on the age, weight, and severity of the disease of the patient, but is usually 2 to 3 times a day for adults. It is considered appropriate to take 10g up to three times a day depending on the symptoms. EXAMPLES Next, the present invention will be specifically explained with reference to Examples, but the present invention is not limited thereto. Example 1 Drugs produced according to Specific Examples 1 to 4 above
200g was mixed with 89g of lactose and 5g of magnesium stearate, and this mixture was compressed using a single-shot tablet machine to make slug tablets with a diameter of 20mm and a weight of approximately 23g, which were crushed using an oscillator and sized. The mixture was sieved to obtain good granules of 20 to 50 mesh particles. A single dose of this granule is 3 to 15 g depending on the symptoms.
(equivalent to 2.04 to 10.20 g as the drug of the present invention) 1
Take 3 times a day. Example 2 Drugs manufactured according to Specific Examples 1 to 4 above
200 g was mixed with 20 g of microcrystalline cellulose and 5 g of magnesium stearate, and this mixture was compressed using a single-shot tablet machine to produce tablets with a diameter of 7 mm and a weight of approximately 225 mg. Each tablet contains about the amount of the present invention.
Contains 200mg. This tablet is given in 1 dose according to the symptoms.
Take 10 to 50 tablets three times a day. Example 3 Drugs manufactured according to Specific Examples 1 to 4 above
500mg was filled into hard capsules. This capsule is
Take 4 to 20 capsules a day depending on your symptoms.

[Brief explanation of drawings]

The figure shows the results of the normal diet intake group and the drug-mixed diet intake group on appetite loss in AH130 ascites liver cancer-transplanted rats.

Claims (1)

[Claims] 1. Lipolysis of a cancer toxin (toxohormone L) that has a lipolytic effect and contains water or an aqueous organic solvent extract of one or more crude drugs selected from Saiko, Chimpi, and Shiono as an active ingredient. A cancer symptom improving agent characterized by inhibiting the promoting effect and improving lipid metabolism and anorexia in cancer-bearing patients. 2. One or more herbal medicines selected from Saiko, Chimpi, and Shyouma, including Astragalus, Astragalus, Soujiyutsu, Carrot, Licorice, Angelica,
The active ingredient is Seiraku water or an aqueous organic solvent extract containing seven types of herbal medicines from Taisou, which inhibits the lipolysis-promoting effect of a cancer poisonous drug (toxohormone L) that has lipolytic action, and reduces lipids in cancer-bearing patients. A cancer symptom improving agent characterized by improving metabolism and anorexia.