CN101002808A - Medical use of bidentate achyanthes total sterone - 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 products for treating or preventing osteoporosis. 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 bidentata total sterone can be used to treat and prevent human osteoporosis, 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 field of pharmacy, in particular to the use in the preparation of medicines or health products for treating or preventing osteoporosis.

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; oral administration of ecdysterone 20 mg per day, for 12 consecutive weeks, can significantly inhibit the increase of serum total cholesterol and free cholesterol caused by high-cholesterol feeding. Increases in total fat, total cholesterol and triglyceride levels; oral administration of 5-20 mg per day can improve fat deposition in the liver.

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-mentioned purpose, the technical scheme adopted in the present invention is: the application of Achyranthes bidentata total sterone in the preparation of medicines or health products for treating or preventing osteoporosis. In particular, the application of the total sterone of Achyranthes bidentata with a content of more than 50% in the preparation of medicines or health products for treating or preventing osteoporosis.

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 sterone of Achyranthes bidentata, we found that the total sterone of Achyranthes bidentata can be metabolized into natural estrogen in the human body, and this estrogen has the effect of treating osteoporosis. Explain with animal experiment (Achyranthes knee total sterone on the effect of rat osteoporosis) below:

66 SD rats, non-pregnant females, 15 weeks old, weighing 200±20g. After weighing, the animals were randomly divided into 6 groups, namely blank group, model group, nylestriol group and high, medium and low dose groups of Achyranthes bidentata total sterone, with 11 animals in each group. Firstly, the animals in each group were intraperitoneally injected with 2% pentobarbital (5 mg/kg). After the anesthesia effect was achieved, the skin was cut along the midline of the abdomen, and the muscle, fascia and abdominal viscera were separated to expose the abdominal cavity. Except the blank group underwent sham operation and removed a small piece of adipose tissue near the ovary, each group ligated and cut bilateral ovary tissue, injected gentamicin 0.01ml/kg intraperitoneally, and then sutured the muscle and skin layer by layer. Intragastric administration was started 2 weeks after the operation. During the experiment, the rats were weighed once a week, and the dosage was adjusted according to the body weight. The blank group and the model group were intragastrically administered with distilled water, the nylestriol group was intragastrically administered at a dose of 1.05 mg/kg·w ^-1 , and the large, medium and small dose groups of Achyranthes bidentata total sterone were administered at 100 mg/kg·d ^-1 and 50 mg /kg·d ^-1 , 25mg/kg·d ^-1 doses were intragastrically administered. After 12 weeks, the femoral vein was used to collect live blood to kill the animals. Take the 1/3 part of the left distal femur, fix it in 10% formalin solution at room temperature for 24 hours, soak it in formic acid until it is completely decalcified, cut it along the sagittal plane, stain it with HE, dehydrate it with ethanol, and paraffin wax Embedded, cut along the sagittal plane, section thickness 0.14 μm, measured bone histomorphological indicators. The following three parameters were directly measured on the left distal 1/3 of the femur: total tissue area (T-Ar), trabecular bone area (Tb-Ar) and trabecular bone perimeter (Tb-Pm), using the correction formula Calculate the following two parameters: trabecular area percentage (%Tb-Ar=Tb-Ar÷T-Ar×100%); bone trabecular thickness [Tb-Th=(2÷1.99)×(Tb-Ar÷Tb- Pm)]. Observe and compare the trabecular area percentage and trabecular thickness. SAS9.0 and SPSS11.0 statistical software were used for data processing.

Changes of histomorphological parameters in the 1/3 part of the distal femur (x±s)

group dose n Trabecular area percentage (%) Trabecular bone thickness (μm) Blank group Model group Nylestriol group Achyranthes bidentata total sterone low-dose group Achyranthes bidentata total sterone medium-dose group Achyranthes bidentata total sterone high-dose group --1.05mg/kg.d ^-1 25mg/kg.d ^-1 50mg/kg.d ^-1 100mg/kg.d ^-1 888888 22.64±3.13*19.10±1.68△#23.69±4.45*22.59±2.33*25.74±4.38*27.16±3.80*# 0.63±0.0110.65±0.031#0.69±0.051*0.68±0.043*0.71±0.056*0.77±0.066*#

Note: Compared with blank group, △P<0.05; compared with model group, ^* P<0.05; compared with nylestriol group, #P<0.05; n represents the number of rats in each group.

The results clearly show that total steroids of Achyranthes bidentata have obvious preventive and therapeutic effects on osteoporosis caused by ovariectomized rats, and the effect is better than that of nilestriol, which is a good treatment and prevention of osteoporosis in Achyranthes bidentata effective part.

Clinical cases: 48 patients with osteoporosis were clinically diagnosed. X-ray findings: generalized osteoporosis, evident in the spine, pelvis, and upper end of the femur, and the average bone density was lower than 2.0 standards for young adults of the same sex Poor or above (T value ≤ -2.0). Then 48 patients with osteoporosis were randomly divided into Achyranthes bidentata total sterone group and calcium gluconate control group. There were 24 patients in each of the two groups. There were 9 males in the treatment group, aged 58-75 years; 15 females, aged 58-75. 60-73 years old; control group 8 males, aged 60-74 years old, 16 females, aged 59-72 years old. Graded according to the degree of osteoporosis: in the treatment group, 8 cases were measured, 11 cases were moderate, and 5 cases were mild; in the control group, 7 cases were severe, 12 cases were moderate, and 5 cases were mild. There was no significant difference between the two groups in terms of gender, age, and degree of disease (p>0.05). Oral homemade Achyranthes bidentata total sterone capsules (content 200-300mg/capsule) 1-2 capsules each time, 3 times a day, for 3-5 consecutive months. The control group used calcium gluconate oral liquid 1-2 sticks each time, 3 times a day, for 3-5 consecutive months. Comparison of the total effective rate between the two groups: 8 cases were cured in the Achyranthes bidentata total sterone treatment group, 9 cases were markedly effective, 6 cases were effective, and 1 case was ineffective, with a total effective rate of 95.8%; 4 cases were cured in the calcium gluconate control group, 7 cases were markedly effective, 7 cases were effective, 6 cases were ineffective, the total effective rate was 75% analysis, and the difference of the total effective rate was significant (p<0.05).

Mechanism of action: Previous studies have shown that estrogen in hormone replacement therapy can effectively prevent postmenopausal rapid bone loss, maintain bone mass, increase bone density, and reduce fracture rate. However, long-term use of estrogen can lead to risks of breast lumps, venous thrombosis, high blood pressure, water retention, endometrial cancer, and breast cancer. For this reason, searching for phytoestrogens without the above-mentioned side effects has become a current domestic and foreign medical research hotspot. The total sterone of Achyranthes bidentata of the present invention can be metabolized into natural phytoestrogens in human body, and phytoestrogens are compounds with weak estrogenic effect in plants. Animal experiments and clinical practice show that total steroids of Achyranthes bidentata have the effect of treating osteoporosis. And degrees combined to exert weak estrogen-like effects. Therefore, the medicine with total sterone of Achyranthes bidentata as the main component can be applied to treat or prevent osteoporosis in human body.

In a word, the results of the study show that: as a medicine, total sterone of Achyranthes bidentata can be used to treat and prevent human osteoporosis if taken orally. The dosage is about 7mg/kg·d ^-1 , if the adult body weight is calculated as 70 kg, the dosage is about 0.5g/d ^-1 . When used as a health product, the dosage for adults is about 0.2-0.3g/d ^-1 .

Achyranthes bidentata total sterone is mainly made into oral dosage forms when preparing medicines or health care products for treating or preventing osteoporosis, such as tablets, oral liquids, capsules, powders, pills, granules, etc., and its pharmaceutical technology is mature The technology, its dosage form does not affect the curative effect.

The invention has the advantages that: the active part mainly contains the total sterone of Achyranthes bidentata, has good effects of treating and preventing osteoporosis, 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 7mg/kg·d ^-1 ± 30%. If the adult body weight is calculated as 70 kg, the dosage is 0.5g/d ^-1 or so, it has a better effect of treating and preventing osteoporosis, and is safe, with little 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 care product, and it is taken orally to the human body, and the dosage is 0.2～0.3g/d ^-1 ±30%, which has good therapeutic and therapeutic effect. It has the function of preventing osteoporosis, and is safe, with little toxic and 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 (2)

1, the Radix Achyranthis Bidentatae total sterone is in preparation treatment or the medicine of prevention of osteoporosis or the application in the health product.

2, application according to claim 1 is characterized in that: content is treated or the medicine of prevention of osteoporosis or the application in the health product in preparation at the Radix Achyranthis Bidentatae total sterone more than 50%.