CN114948981A - Application of harpagoside as effective component in preparation of medicine for treating osteoporosis - Google Patents
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- 208000001132 Osteoporosis Diseases 0.000 title claims abstract description 39
- KVRQGMOSZKPBNS-FMHLWDFHSA-N Harpagoside Chemical compound O([C@@H]1OC=C[C@@]2(O)[C@H](O)C[C@]([C@@H]12)(C)OC(=O)\C=C\C=1C=CC=CC=1)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O KVRQGMOSZKPBNS-FMHLWDFHSA-N 0.000 title claims abstract description 22
- 239000003814 drug Substances 0.000 title claims abstract description 22
- KVRQGMOSZKPBNS-BYYMOQGZSA-N Harpagoside Natural products C[C@@]1(C[C@@H](O)[C@@]2(O)C=CO[C@@H](O[C@@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)[C@H]12)OC(=O)C=Cc4ccccc4 KVRQGMOSZKPBNS-BYYMOQGZSA-N 0.000 title claims abstract description 21
- 238000002360 preparation method Methods 0.000 title claims abstract description 13
- 102000002260 Alkaline Phosphatase Human genes 0.000 claims abstract description 19
- 108020004774 Alkaline Phosphatase Proteins 0.000 claims abstract description 19
- 102000007591 Tartrate-Resistant Acid Phosphatase Human genes 0.000 claims abstract description 14
- 108010032050 Tartrate-Resistant Acid Phosphatase Proteins 0.000 claims abstract description 14
- 239000004480 active ingredient Substances 0.000 claims abstract description 14
- 210000002966 serum Anatomy 0.000 claims abstract description 10
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims abstract description 9
- 239000011575 calcium Substances 0.000 claims abstract description 9
- 229910052791 calcium Inorganic materials 0.000 claims abstract description 9
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims abstract description 8
- 239000011574 phosphorus Substances 0.000 claims abstract description 8
- 229910052698 phosphorus Inorganic materials 0.000 claims abstract description 8
- 238000011552 rat model Methods 0.000 claims abstract description 5
- 239000002775 capsule Substances 0.000 claims abstract description 4
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- RLFWWDJHLFCNIJ-UHFFFAOYSA-N 4-aminoantipyrine Chemical compound CN1C(C)=C(N)C(=O)N1C1=CC=CC=C1 RLFWWDJHLFCNIJ-UHFFFAOYSA-N 0.000 description 2
- 201000005670 Anovulation Diseases 0.000 description 2
- 206010002659 Anovulatory cycle Diseases 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 102000015735 Beta-catenin Human genes 0.000 description 2
- 108060000903 Beta-catenin Proteins 0.000 description 2
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- 102100030053 Secreted frizzled-related protein 3 Human genes 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
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- 231100000552 anovulation Toxicity 0.000 description 2
- 230000003262 anti-osteoporosis Effects 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- RNFNDJAIBTYOQL-UHFFFAOYSA-N chloral hydrate Chemical compound OC(O)C(Cl)(Cl)Cl RNFNDJAIBTYOQL-UHFFFAOYSA-N 0.000 description 2
- 229960002327 chloral hydrate Drugs 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 229940000406 drug candidate Drugs 0.000 description 2
- 230000004821 effect on bone Effects 0.000 description 2
- 239000003777 experimental drug Substances 0.000 description 2
- 229910052500 inorganic mineral Inorganic materials 0.000 description 2
- 238000010603 microCT Methods 0.000 description 2
- 239000011707 mineral Substances 0.000 description 2
- 210000001672 ovary Anatomy 0.000 description 2
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- 235000019698 starch Nutrition 0.000 description 2
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- 206010002091 Anaesthesia Diseases 0.000 description 1
- 102000005701 Calcium-Binding Proteins Human genes 0.000 description 1
- 108010045403 Calcium-Binding Proteins Proteins 0.000 description 1
- 102000006311 Cyclin D1 Human genes 0.000 description 1
- 108010058546 Cyclin D1 Proteins 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 102000003886 Glycoproteins Human genes 0.000 description 1
- 108090000288 Glycoproteins Proteins 0.000 description 1
- 208000030136 Marchiafava-Bignami Disease Diseases 0.000 description 1
- 208000029725 Metabolic bone disease Diseases 0.000 description 1
- 102000005741 Metalloproteases Human genes 0.000 description 1
- 108010006035 Metalloproteases Proteins 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 229930182555 Penicillin Natural products 0.000 description 1
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 description 1
- 206010039984 Senile osteoporosis Diseases 0.000 description 1
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- 239000002253 acid Substances 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 239000012670 alkaline solution Substances 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 230000037005 anaesthesia Effects 0.000 description 1
- 230000002146 bilateral effect Effects 0.000 description 1
- 239000003150 biochemical marker Substances 0.000 description 1
- 210000002805 bone matrix Anatomy 0.000 description 1
- 230000018678 bone mineralization Effects 0.000 description 1
- 238000005119 centrifugation Methods 0.000 description 1
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- 210000003541 chondroclast Anatomy 0.000 description 1
- 238000004737 colorimetric analysis Methods 0.000 description 1
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- 238000001514 detection method Methods 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 239000012954 diazonium Substances 0.000 description 1
- 150000001989 diazonium salts Chemical class 0.000 description 1
- 230000037213 diet Effects 0.000 description 1
- 235000005911 diet Nutrition 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- XPPKVPWEQAFLFU-UHFFFAOYSA-J diphosphate(4-) Chemical compound [O-]P([O-])(=O)OP([O-])([O-])=O XPPKVPWEQAFLFU-UHFFFAOYSA-J 0.000 description 1
- 235000011180 diphosphates Nutrition 0.000 description 1
- TYJOJLOWRIQYQM-UHFFFAOYSA-L disodium;phenyl phosphate Chemical compound [Na+].[Na+].[O-]P([O-])(=O)OC1=CC=CC=C1 TYJOJLOWRIQYQM-UHFFFAOYSA-L 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 210000003195 fascia Anatomy 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 238000003304 gavage Methods 0.000 description 1
- PCHJSUWPFVWCPO-UHFFFAOYSA-N gold Chemical compound [Au] PCHJSUWPFVWCPO-UHFFFAOYSA-N 0.000 description 1
- 230000013632 homeostatic process Effects 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 201000000916 idiopathic juvenile osteoporosis Diseases 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 208000017169 kidney disease Diseases 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- 210000002540 macrophage Anatomy 0.000 description 1
- 230000003340 mental effect Effects 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 210000000963 osteoblast Anatomy 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 229940049954 penicillin Drugs 0.000 description 1
- 208000001685 postmenopausal osteoporosis Diseases 0.000 description 1
- -1 potassium ferricyanide Chemical compound 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 150000004059 quinone derivatives Chemical class 0.000 description 1
- 238000010526 radical polymerization reaction Methods 0.000 description 1
- 230000003014 reinforcing effect Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
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- 238000005507 spraying Methods 0.000 description 1
- 210000000130 stem cell Anatomy 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 210000001694 thigh bone Anatomy 0.000 description 1
- 210000002303 tibia Anatomy 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 238000009966 trimming Methods 0.000 description 1
- 230000003827 upregulation Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- Health & Medical Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Coloring Foods And Improving Nutritive Qualities (AREA)
Abstract
The invention relates to an application of active ingredients in preparing a medicine for treating osteoporosis, wherein the active ingredients are harpagoside which can also be the only active ingredient, the active ingredients can be added with pharmaceutical excipients to prepare a preparation, the preparation form is one of tablets, capsules, granules and oral liquid, and the preparation can increase the content of inorganic calcium and phosphorus in the serum of a rat model with ovarioosteoporosis and reduce the content of alkaline phosphatase (ALP) and the content of tartrate-resistant acid phosphatase (TRAP) in the serum of the rat model with ovarioosteoporosis.
Description
Technical Field
The invention belongs to the technical field of medicines, and particularly relates to application of an effective component in preparation of a medicine for treating osteoporosis, wherein the effective component is harpagoside.
Background
Osteoporosis (OP) is a systemic metabolic bone disease characterized by a decrease in bone mass and a deterioration in bone microstructure, which increases bone fragility and is prone to fracture. They are generally classified into two groups according to the cause of the disease: the first is primary osteoporosis, about more than 90% of osteoporosis belongs to the same class, and is divided into high-conversion postmenopausal osteoporosis, low-conversion senile osteoporosis and unidentified idiopathic osteoporosis of the same type in teenagers, pregnant women, lactating women and other people; the other is secondary osteoporosis due to drugs or certain diseases affecting bone metabolism, etc. Along with the increase of the elderly population in China year by year, the number of people suffering from osteoporosis due to bone degenerative diseases caused by age is increased, so that the fracture, disability and fatality rate is greatly improved. In order to improve the life quality of patients and relieve the economic and mental stress, researches and applications for finding effective osteoporosis prevention and treatment methods are not slow.
The Wnt/beta-catenin pathway has positive regulation effect on bone mass and strength. The Wnt signal transduction pathway regulates the expression of a plurality of genes such as downstream Cyclin D1, C-myc and the like through beta-catenin, thereby participating in regulating the differentiation and proliferation of stem cells. The activation of the Wnt signaling pathway is regulated by different families of proteins, including Dickkopfs and secreted frizzled related proteins (sFRPs), sFRP is a glycoprotein, which contains a cysteine-like domain that allows FRPs to bind to both soluble Wnt proteins in the extracellular compartment and Fz receptors, thus strongly regulating Wnt signaling and maintaining bone homeostasis.
Disclosure of Invention
The invention aims to: (1) the application of the effective components in preparing medicines for treating osteoporosis is provided. (2) The effective component is harpagoside. (3) The harpagoside as the active ingredient is added with pharmaceutic adjuvants to prepare the preparation.
In order to achieve the purpose, the invention provides the following technical scheme: the application of the effective component in preparing the medicine for treating osteoporosis, wherein the effective component is harpagoside.
The harpagoside is the only effective component in the application of the effective component in preparing the medicine for treating osteoporosis.
The application of the effective components in preparing the medicine for treating osteoporosis is to add pharmaceutic adjuvants into the effective components and prepare the effective components into a dosage form.
The effective component is applied to preparing a medicine for treating osteoporosis, and the dosage form is one of tablets, capsules, granules and oral liquid.
The harpagoside can increase the contents of inorganic calcium and phosphorus in the serum of a rat model with ovarian osteoporosis.
The harpagoside can reduce the content of alkaline phosphatase (ALP) and tartrate-resistant acid phosphatase (TRAP) in serum of a rat model with ovariectomy and osteoporosis.
Harpagoside, CAS: 19210-12-9, molecular formula: c 24 H 30 O 11 Molecular weight 494.488, available from Shanghai-derived leaf Biotech, Inc.
Detailed Description
The technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the embodiments of the present invention, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all of the embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.
Example 1: taking 10g of harpagoside, adding starch, and preparing into tablets.
Example 2: taking 10g of harpagoside, adding dextrin, and preparing into granules.
Example 3: taking 10g of harpagoside, adding starch, and preparing into capsules.
Example 4: effect of harpagoside on bone Density
4.1 experimental drugs and animals: the experimental drug was harpagoside tablet prepared in example 1. Clean SD rats, male, weighing 240-310 g, were provided by Shanghai Seipaibikai laboratory animals Co.
4.2 preparation of model: after 1 week of acclimation, rats were randomly divided into Sham (Sham, 8) and ovariectomized (32). Injecting 10% chloral hydrate (0.3mL/100g · bw) into abdominal cavity to anaesthetize rat, trimming abdominal hair, disinfecting with 75% alcohol, dissecting abdominal cavity, finding and cutting bilateral ovary, spraying small amount of penicillin, and suturing wound. Sham groups sutured the wound after removal of a small amount of fat from the abdominal cavity. The rats recovered for 30 days after surgery, and the ovariectomized groups were randomized into 4 groups by weight: model control group (OVX), positive drug control group (E2, 0.3mg/kg, 1mL/100g BW), inventive low dose group (1000mg/kg BW, 1mL/100g BW) and inventive high dose group (2000mg/kg BW, 1mL/100g BW), 8 of each group. The Sham and OVX groups were gavaged with 1mL/100 g.BW. The gavage is carried out once a day for 90 days. Meanwhile, blood is collected from the orbit once every 30 days, the level of E2 is analyzed, and when the level of E2 in the anovulation non-positive drug group is obviously less than Sham and the level of TRACP is obviously less than OVX, the anovulation modeling is successful. After the last gastric lavage, all rats are fasted for 10-12h, during which water can be freely drunk, blood of the rats is taken from the orbit after 5% chloral hydrate anesthesia, the rats are kept stand at room temperature for 40min, after the blood is coagulated, the rats are placed at 4 ℃ for 1 h, serum is collected by centrifugation at 4 ℃ and 3000rpm for 20min and stored at-80 ℃ for standby. After the rat is sacrificed, the femur and tibia of the rat are taken out rapidly, fascia is stripped, the far end of the left femur of the rat is fixed in 10% neutral formalin solution for histological analysis; the rat right femur distal end is used for Micro-CT analysis; quickly putting the rest part into liquid nitrogen, and storing at-80 deg.C for use.
4.3 serum bone metabolism index detection: the contents of inorganic calcium, phosphorus and alkaline phosphatase (ALP) in blood were measured according to the procedures of the kit instructions. Alkaline phosphatase (ALP) kit principle: the disodium phenylphosphate is decomposed by alkaline phosphatase to generate phosphoric acid and free phenol, the free phenol reacts with 4-aminoantipyrine under the condition of alkaline solution, and then is oxidized by potassium ferricyanide to generate red quinone derivatives, and the shade of red indicates the activity of the enzyme. Tartrate-resistant acid phosphatase (TRAP) kit: TRAP catalyzes the hydrolysis of a substrate to produce free phenol, which reacts with diazonium salts to produce colored azo compounds, and the activity of the enzyme is determined by colorimetry.
TABLE 1 Effect of the invention on the Biochemical indicators of serum from ovariectomized osteoporosis rats
| Group of | Calcium (mmol. L) -1 ) | Phosphorus (mmol. L) -1 ) | ALP/(King units 100 ml) -1 ) | TRAP(U/L) |
| Artificial operation group | 1.898±0.453 | 1.986±0.341 | 5.576±1.564 | 11.314±2.325 |
| Model set | 1.723±0.364 | 1.664±0.325 | 12.124±2.425 | 16.763±2.566 |
| Positive drug group | 2.033±0.442 | 2.124±0.552 | 7.946±1.657* | 11.086±2.463* |
| High dose group | 2.447±0.345* | 2.326±0.542* | 6.852±1.536* | 8.425±1.478* |
| Low dose group | 1.978±0.442 | 1.929±0.402 | 8.809±1.879* | 9.841±1.566* |
Note comparison with model group <0.05, P < 0.01.
The renewal of bone is a dynamic balancing process, and the bone continuously intakes free calcium in blood for the formation of bone and releases calcium generated by bone absorption into blood. The influence of the anti-osteoporosis particles on calcium and phosphorus can be examined by measuring two general biochemical markers of serum calcium and phosphorus in bone metabolism, so as to study whether the anti-osteoporosis particles can promote bone matrix synthesis and bone mineral deposition. During bone mineralization, bone specific alkaline phosphatase (bALP) secreted by osteoblasts can hydrolyze mono acid ester to generate inorganic , increase local inorganic phosphorus concentration, facilitate bone formation, hydrolyze pyrophosphate inhibiting mineralized crystal, and exert effects similar to calcium binding protein or Ga2+ -ATP enzyme. Bone alkaline phosphatase is an important part of total alkaline phosphatase, and since total alkaline phosphatase changes when bone alkaline phosphatase changes, it can be used as one of bone formation markers to partially reflect the bone formation state. Tartrate-resistant acid phosphatase (TRAP) is a glycosylated metallo-protease, is expressed in large quantities in osteoclasts and chondroclasts, has activated macrophages and neurons, is released into the blood by osteoclasts mostly, is positively correlated with bone resorption, is not influenced by factors such as day-night change, diet, liver and kidney diseases and the like, has high specificity, becomes a biochemical marker of second-generation bone resorption, and can reflect the bone resorption state and the osteoclast activity. Remove among the ovary osteoporosis model group and false operation group comparison, model group ALP and TRAP content all show and increase, and thighbone bone density reduces again, explains that model rat bone mass seriously loses and bone formation and bone absorption all show the reinforcing, and bone metabolism becomes active, and the suggestion high conversion type osteoporosis takes place. The femur bone density is obviously increased, and the ALP and TRAP contents are obviously reduced, which shows that the invention can inhibit the activity of osteoclasts, obviously improve the bone mass of osteoporosis rats, inhibit the high transition state of bones and has the function of treating osteoporosis.
4.4 bone Density analysis: bone density is closely related to osteoporosis and is one of the criteria for diagnosing osteoporosis. Rat femoral head bone density was analyzed by micro-CT.
Table 2 effect on bone density (x ± s, n ═ 10)
| Group of | Bone mineral density (g/kg) |
| Artificial operation group | 875.872±40.237 |
| Model set | 492.526±52.683 |
| Positive drug group | 897.451±44.431* |
| High dose group | 902.730±46.514* |
| Low dose group | 887.525±47.452* |
Note comparison with model group <0.05, P < 0.01.
The bone density is the gold standard for determining osteoporosis, and the dual-energy X-ray bone densitometer has the advantages of high full automation degree, convenient use, advanced performance, quick scanning and accurate and reliable result, so the experiment is used for determining the femoral density E2 of the rat with osteoporosis, and the invention obviously improves the bone density of the rat with osteoporosis and can treat the osteoporosis.
Although embodiments of the present invention have been shown and described, it will be appreciated by those skilled in the art that changes, modifications, substitutions and alterations can be made in these embodiments without departing from the principles and spirit of the invention, the scope of which is defined in the appended claims and their equivalents.
Claims (7)
1. The application of the active ingredients in preparing the medicine for treating osteoporosis is characterized in that the active ingredients are harpagoside.
2. The use of the active ingredient of claim 1 in the preparation of a medicament for the treatment of osteoporosis, wherein harpagoside is the sole active ingredient.
3. The use of the active principle of claim 1 for the preparation of a medicament for the treatment of osteoporosis, wherein the active principle is added with pharmaceutical excipients and prepared into a dosage form.
4. The use of the active ingredient of claim 3 in the manufacture of a medicament for the treatment of osteoporosis in the form of one of a tablet, capsule, granule, or oral liquid.
5. The use of the active ingredient of claim 1 in the preparation of a medicament for the treatment of osteoporosis, wherein the active ingredient harpagoside increases the levels of inorganic calcium and phosphorus in serum of rats with ovariectomy.
6. The use of the active principle of claim 1 for the preparation of a medicament for the treatment of osteoporosis, wherein the active principle harpagoside decreases the levels of alkaline phosphatase (ALP) and tartrate-resistant acid phosphatase (TRAP) in serum of a rat model of ovariectomized osteoporosis.
7. The use of the active ingredient of claim 1 in the preparation of a medicament for the treatment of osteoporosis, wherein the active ingredient harpagoside increases bone density.
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020183264A1 (en) * | 2000-11-29 | 2002-12-05 | Shin Joon Shik | Use of harpagid-related compounds for prevention and treatment of osteoporosis, arthritis and ruptured disc and pharmaceutical composition containing the same |
| KR20170011403A (en) * | 2015-07-22 | 2017-02-02 | 원광대학교산학협력단 | Medical compound comprising Harpagoside by inhibit Osteoclast Differentiation |
| WO2021222298A1 (en) * | 2020-04-29 | 2021-11-04 | The Board Of Trustees Of The Leland Stanford Junior University | Mechanical and biochemical activation and control of skeletal stem cells for cartilage regeneration |
-
2022
- 2022-07-13 CN CN202210822579.4A patent/CN114948981A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020183264A1 (en) * | 2000-11-29 | 2002-12-05 | Shin Joon Shik | Use of harpagid-related compounds for prevention and treatment of osteoporosis, arthritis and ruptured disc and pharmaceutical composition containing the same |
| KR20170011403A (en) * | 2015-07-22 | 2017-02-02 | 원광대학교산학협력단 | Medical compound comprising Harpagoside by inhibit Osteoclast Differentiation |
| WO2021222298A1 (en) * | 2020-04-29 | 2021-11-04 | The Board Of Trustees Of The Leland Stanford Junior University | Mechanical and biochemical activation and control of skeletal stem cells for cartilage regeneration |
Non-Patent Citations (1)
| Title |
|---|
| HWA-JIN CHUNG ET AL.: "Anti-Osteoporotic Activity of Harpagoside by Upregulation of theBMP2 and Wnt Signaling Pathways in Osteoblasts and Suppressionof Differentiation in Osteoclasts", J. NAT. PROD., vol. 80, pages 434 - 442 * |
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