CN101011436A - Medical usage of total phytosterone from achyranthes - Google Patents

Abstract

The present invention relates to the use of total sterone of Achyranthes bidentata in the field of pharmacy, in particular to the use in the preparation of medicines or health care products for treating or preventing fatty liver and lipid-lowering and weight-loss drugs. The total sterone of Achyranthes bidentata refers to the sum of sterones contained in the effective parts of Achyranthes bidentata, mainly including ecdysterone, achyranthes sterone, and amaranthus sterone. Studies have found that taking Achyranthes knuckle total sterone can be used for the treatment and prevention of fatty liver and fat-lowering weight loss, and it is safe and has little toxic and side effects.

Description

Medicinal use of total sterone in Achyranthes bidentata

technical field

The present invention relates to the use of total sterone of Achyranthes bidentata in the pharmaceutical field, in particular to the application in the preparation of fat-lowering and weight-loss drugs or health products, and the application in the preparation of drugs or health products for treating or preventing fatty liver.

Background technique

Achyranthes bidentata BI., also known as Achyranthes bidentata BI., is the root of Amaranthaceae, a perennial herb, cultivated or wild on the side of mountain roads, excavated in winter when the stems and leaves are withered, and the fibrous roots and soil are removed , dried and cut into pieces for medicinal purposes. Mainly produced in Hunan, Hubei, Henan, Sichuan, Guizhou and other places. Achyranthes bidentata is a traditional Chinese medicine. Its taste is sweet and bitter, and its nature is flat. It enters the liver and kidney meridians. It has the functions of invigorating liver and kidney, strengthening muscles and bones, promoting blood circulation and dredging collaterals. Indications: blood stagnation amenorrhea, dysmenorrhea, menstrual bleeding, bruises, soft waist and knees, spasms of limbs, hematemesis, epistaxis, hematuria due to gonorrhea, gingival swelling and pain, sore throat, carbuncle, etc. Sterosterone is one of the active ingredients of Achyranthes bidentata, mainly including ecdysterone, achyranthes sterone, and amaranthus sterone. Xu Xiuying, Zheng Yimin, and Wang Long's "Research Progress of Plant Ecdysteroids" (Journal of Biology, 2005.122 (2): 12-15 pages) discloses the effect of ecdysterone as follows: give rabbits oral ecdysterone per day 5-20 mg, for 10-12 weeks, can significantly inhibit the increase of serum total cholesterol and free cholesterol caused by high-cholesterol feeding.

Contents of the invention

The object of the present invention is to provide a new application of the total sterone of Achyranthes bidentata, that is, a new application in the preparation of medicines.

In order to achieve the above object, the first technical scheme adopted by the present invention is: the application of Achyranthes bidentata total sterone in the preparation of lipid-lowering and weight-loss drugs or health care products. In particular, the application of the total sterone of Achyranthes bidentata with a content of more than 50% in the preparation of lipid-lowering and weight-loss drugs or health care products. The "fat reduction" in the "fat reduction and weight loss" refers to the reduction of blood fat.

In order to achieve the above-mentioned purpose, the second technical scheme adopted by the present invention is: the application of Achyranthes bidentata total sterone in the preparation of medicines or health products for treating or preventing fatty liver. Especially the application of the total sterone of Achyranthes bidentata with a content of more than 50% in the preparation of medicines or health care products for treating or preventing fatty liver.

The total sterone of Achyranthes bidentata refers to the sum of sterones contained in the effective parts of Achyranthes bidentata, mainly including ecdysterone, sterone of achyranthes bidentata, and sterone of red amaranth.

In our research on the total steroids of Achyranthes bidentata, we found that the total steroids of Achyranthes bidentata can be metabolized into natural estrogen in the human body. This estrogen has the effect of reducing fat and weight loss, especially for treating or preventing fatty liver . The animal experiment (Achyranthes knee total sterone has the effect of treating or preventing fatty liver and reducing fat and losing weight in rats) is described below:

80 male SD rats of SPF grade, weighing 180g-200g, after the rats were bought back and adapted to feeding for 1 week, 10 rats were randomly selected as the basic control group and fed with the basic feed [formula: barley flour 20%, dehydrated vegetables (Cabbage with moisture removed) 10%, soybean flour 20%, yeast 1%, bone meal 5%, corn 16%, bran 16%, fish meal 10%, salt 2%], and the other 70 were fed as high-fat group High-fat feed [i.e. use casein instead of soybean meal in formula as basic feed, high-fat feed is 76.2% basic feed, 12% large oil, 10% sucrose, 1.5% cholesterol, 0.3% pig bile salt]. After 2 months of free drinking and food intake, 40 obese model rats were screened out according to the criterion that the average body weight of the rats fed the high-fat diet was greater than the average body weight of the rats in the basal diet group plus 1.4 standard deviations. These 40 obese rats were randomly divided into obese control group (gastric administration of normal saline) and low, middle and high total sterone groups of Achyranthes bidentata by body weight (doses were respectively 25mg/kg BW, 50mg/kg BW and 100mg /kgBW, given by gavage). All groups continued to be fed high-fat diet and weighed every week. After 4 weeks, blood was collected from the femoral artery to detect various indicators. Triglyceride (TG), total cholesterol (TC), and high-density lipoprotein cholesterol (HDL-C) were determined by enzymatic method with a biochemical analyzer and supporting reagents. Using SPSS12.0 software, the data are described as mean ± standard deviation (x ± s).

Table 1 Effect of Achyranthes bidentata total sterone on blood lipids in obese rats (mmol/L)

group TG TC HDL basic control group 10 2.15±0.44 2.16±0.36 1.25±0.27 obese control group 10 3.19±0.41# 3.95±0.42# 0.85±0.18 Achyranthes knuckle total sterone (25mg/kg) 10 3.18±0.40# 3.53±0.32# 0.91±0.34 Achyranthes knuckle total steroids (50mg/kg) 10 3.02±0.26*# 2.97±0.40* 0.95±0.36* Achyranthes knuckle total sterone (100mg/kg) 10 2.63±0.41* 2.25±0.31* 0.97±0.28*

Note: Compared with the obese control group, *P<0.05; compared with the basic control group, #P<0.05.

Table 2 Effect of Achyranthes bidentata total sterone on liver tissue indexes of rats with hyperlipidemia fatty liver (n=10)

Group TC (mg/g wet tissue) TG (mg/g wet tissue) Liver weight coefficient (g/100g) Obese control group 2.68±0.35 25.17±2.15 2.86±0.23 Achyranthes bidentata total sterone 100mg/kg group 1.70±0.11 ^* 12.57±3.10 ^* 2.28±0.17 ^*

Note: Compared with the obese control group, *P<0.05; n represents the number of rats in each group.

The results in Table 1 show that the total steroids of Achyranthes bidentata at 50 mg/kg and 100 mg/kg can significantly reduce the blood TG and TC levels of obese rats, and increase the HDL-C level. The results in Table 2 show that total steroids from Achyranthes bidentata can significantly reduce the content of TG and TC in the liver tissue of rats with hyperlipidemia fatty liver, and at the same time reduce the coefficient of liver weight. The above results clearly show that total sterone in Achyranthes bidentata has a good therapeutic effect on hyperlipidemia fatty liver.

Table 3 Effect of Achyranthes bidentata total sterone on body weight of obese rats (g)

group Week 0 Week 2 Week 4 basic control group 10 349.1±38.8 369.2±43.2 380.4±26.5 obese control group 10 458.3±38.4 498.6±42.1 526.7±43.7 Achyranthes knuckle total sterone (25mg/kg) 10 465.5±33.9  477.5±20.3*  488.2±33.7* Achyranthes knuckle total steroids (50mg/kg) 10 460.9±38.7  455.1±45.1* 471.1±31.9* Achyranthes knuckle total sterone (100mg/kg) 10 450.4±31.0 452.3±35.6* 448.6±37.7*

Note: Compared with the obese control group, *P<0.05.

Table 3 shows that the total sterone of Achyranthes bidentata can significantly reduce the body weight of obese rats, showing a good fat-lowering and weight-loss effect.

Clinical weight loss example: In the weight loss specialist clinic, 37 patients with simple obesity were selected as volunteers for weight loss experiments to observe the curative effect. The diagnostic criteria are based on the most widely used body mass index (BMI) in the world, that is, the square of weight (kg) divided by height (m), and the recommendation of Asian adult weight classification, that is, BMI 18.5-22.9 is normal, ≥23.0 is overweight, Among them, 23.0-24.9 means increased risk, 25.0-29.9 means I degree obesity (moderate), and ≥30.0 means II degree obesity (severe). The youngest of the patients was 34 years old, the oldest was 66 years old, and the average age was 47 years old; 11 cases were male and 26 cases were female; 24 cases were of degree I obesity and 13 cases of degree II obesity. Secondary obesity caused by hypothalamus, adrenal, pituitary, thyroid and other diseases was excluded. Treatment method: Oral homemade Achyranthes bidentata total sterone capsules (content 200-300mg/capsule) 2-3 capsules each time, 3 times a day, 1 month as a course of treatment, and observe the curative effect within 2 months. Treatment results: refer to the third revision of China Obesity Research Group of Integrative Traditional Chinese and Western Medicine to formulate standards: markedly effective: weight loss of more than 5kg at the end of treatment; effective: weight loss of 3-5kg at the end of treatment; ineffective: weight loss at the end of treatment has not reached the above standards. Among the 37 patients with simple obesity, 11 cases were markedly effective: the average weight loss was more than 3-6 kg per month, and blood lipids (mainly triglycerides) decreased significantly; 3 cases of ineffectiveness: the weight loss was not obvious, and even the weight gain was below 2kg per month, and the change of blood lipid was not obvious. The effective rate is 91.9%.

In conclusion, the research results show that: as a drug, oral administration of total sterone in Achyranthes can be used for the treatment and prevention of fatty liver as well as lipid-lowering and weight-loss. The dosage is 15-35 mg/kg·d ^-1 , if the adult body weight is calculated as 70 kg, the dosage is 1.0-2.5 g/d ^-1 . When used as a health product, the dosage for adults is 0.2-0.3g/d ^-1 .

Achyranthes bidentata total sterone is mainly made into oral dosage forms when preparing treatment and prevention of fatty liver and lipid-lowering and weight-loss drugs or health products, such as tablets, oral liquids, capsules, powders, pills, granules, etc., and its pharmaceutical process is It is a mature technology, and its dosage form does not affect the curative effect.

The invention has the advantages that: the active parts mainly contain the total sterone of Achyranthes bidentata, which has good effects of treating and preventing fatty liver, lowering fat and reducing weight, is safe, and has little toxic and side effects.

Detailed ways

The present invention will be further described below in conjunction with embodiment:

Embodiment one:

1. Preparation of total sterone in Achyranthes bidentata

Take an appropriate amount of Achyranthes knuckles decoction pieces, boil 3 times at 90-100°C for 2.5 hours each time according to the ratio of 1kg of medicinal materials to 20L of water. After filtering, the extract of Achyranthes bidentata was collected. Put on a D-type macroporous adsorption resin column, and the adsorption flow rate is 1BV/min until the resin is saturated. Rinse the resin with water until the effluent is clear and transparent, elute with 10BV (C ₂ H ₅ OH) = 85% ethanol at an elution flow rate of 0.5 BV/min, and dry the eluent to constant weight. It is the effective part of Achyranthes bidentata, and the yield is not less than 0.15% (the total sterone content of Achyranthes bidentata is more than 60%).

2. The total sterone of Achyranthes bidentata is used to prepare a medicament, and it is administered to the human body orally, and the dosage is controlled at 15-35 mg/kg·d ^-1 . If the adult body weight is calculated as 70 kg, the dosage is 1.0-2.5 g/kg/day. d ^-1 has good effects of treating and preventing fatty liver, lowering fat and losing weight, and is safe with less toxic and side effects. Medicines are mainly made into oral dosage forms, such as tablets, oral liquids, capsules, powders, pills, granules, etc. The pharmaceutical technology is mature technology, and the dosage forms do not affect the curative effect.

Embodiment 2: The total sterone of Achyranthes bidentata prepared in the above embodiment 1 is made into a health product, and it is taken orally to the human body, and the dosage is 0.2-0.3 g/d ^-1 , which has a good effect of preventing fatty liver and reducing Fat weight loss, and safe, with little side effects.

The above-mentioned embodiments are only to illustrate the technical concept and characteristics of the present invention, and the purpose is to enable those skilled in the art to understand the content of the present invention and implement it accordingly, and not to limit the protection scope of the present invention. All equivalent changes or modifications made according to the spirit of the present invention shall fall within the protection scope of the present invention.

Claims (4)

1. Application of Achyranthes bidentata total sterone in the preparation of lipid-lowering and weight-loss medicine or health care product. 2. The application according to claim 1, characterized in that: the application of Achyranthes bidentata total sterone with a content of more than 50% in the preparation of lipid-lowering and weight-loss drugs or health care products. 3. The application of the total sterone of Achyranthes bidentata in the preparation of medicines or health care products for the treatment and prevention of fatty liver. 4. The application according to claim 3, characterized in that: the application of the total sterone of Achyranthes bidentata with a content of more than 50% in the preparation of drugs or health products for the treatment and prevention of fatty liver.