CN117338799A - Application of geniposide in preparation of medicine for treating hyperplasia of mammary glands - Google Patents
Application of geniposide in preparation of medicine for treating hyperplasia of mammary glands Download PDFInfo
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- CN117338799A CN117338799A CN202311383374.1A CN202311383374A CN117338799A CN 117338799 A CN117338799 A CN 117338799A CN 202311383374 A CN202311383374 A CN 202311383374A CN 117338799 A CN117338799 A CN 117338799A
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- hyperplasia
- geniposide
- mammary glands
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- 206010020718 hyperplasia Diseases 0.000 title claims abstract description 54
- 210000005075 mammary gland Anatomy 0.000 title claims abstract description 45
- IBFYXTRXDNAPMM-BVTMAQQCSA-N Geniposide Chemical compound O([C@@H]1OC=C([C@@H]2[C@H]1C(=CC2)CO)C(=O)OC)[C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O IBFYXTRXDNAPMM-BVTMAQQCSA-N 0.000 title claims abstract description 39
- IBFYXTRXDNAPMM-FZEIBHLUSA-N Geniposide Natural products COC(=O)C1=CO[C@@H](O[C@H]2O[C@@H](CO)[C@H](O)[C@@H](O)[C@@H]2O)[C@H]2[C@@H]1CC=C2CO IBFYXTRXDNAPMM-FZEIBHLUSA-N 0.000 title claims abstract description 38
- VGLLGNISLBPZNL-RBUKDIBWSA-N arborescoside Natural products O=C(OC)C=1[C@@H]2C([C@H](O[C@H]3[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O3)OC=1)=C(CO)CC2 VGLLGNISLBPZNL-RBUKDIBWSA-N 0.000 title claims abstract description 38
- 239000003814 drug Substances 0.000 title claims abstract description 25
- 238000002360 preparation method Methods 0.000 title claims abstract description 7
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 claims abstract description 48
- 239000000186 progesterone Substances 0.000 claims abstract description 24
- 229960003387 progesterone Drugs 0.000 claims abstract description 24
- 210000000481 breast Anatomy 0.000 claims abstract description 23
- 102000003946 Prolactin Human genes 0.000 claims abstract description 19
- 108010057464 Prolactin Proteins 0.000 claims abstract description 19
- 229940097325 prolactin Drugs 0.000 claims abstract description 16
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims abstract description 13
- 210000002445 nipple Anatomy 0.000 claims abstract description 13
- 229960005309 estradiol Drugs 0.000 claims abstract description 8
- 229930182833 estradiol Natural products 0.000 claims abstract description 8
- 239000004480 active ingredient Substances 0.000 claims abstract description 7
- 239000000203 mixture Substances 0.000 claims description 12
- 238000009472 formulation Methods 0.000 claims description 3
- 239000002775 capsule Substances 0.000 claims description 2
- 239000008187 granular material Substances 0.000 claims description 2
- 239000007788 liquid Substances 0.000 claims description 2
- 239000006187 pill Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 8
- 241000700159 Rattus Species 0.000 description 24
- 210000002966 serum Anatomy 0.000 description 9
- 229940079593 drug Drugs 0.000 description 6
- 210000001519 tissue Anatomy 0.000 description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 210000002784 stomach Anatomy 0.000 description 4
- 238000011282 treatment Methods 0.000 description 4
- 201000010099 disease Diseases 0.000 description 3
- 230000002124 endocrine Effects 0.000 description 3
- 239000003163 gonadal steroid hormone Substances 0.000 description 3
- 229940088597 hormone Drugs 0.000 description 3
- 239000005556 hormone Substances 0.000 description 3
- UYIFTLBWAOGQBI-BZDYCCQFSA-N Benzhormovarine Chemical compound C([C@@H]1[C@@H](C2=CC=3)CC[C@]4([C@H]1CC[C@@H]4O)C)CC2=CC=3OC(=O)C1=CC=CC=C1 UYIFTLBWAOGQBI-BZDYCCQFSA-N 0.000 description 2
- 238000008157 ELISA kit Methods 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 230000002159 abnormal effect Effects 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- 238000001514 detection method Methods 0.000 description 2
- 229950002007 estradiol benzoate Drugs 0.000 description 2
- 239000000262 estrogen Substances 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 230000004185 hypothalamic-pituitary-gonadal axis Effects 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- 206010028980 Neoplasm Diseases 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 206010046798 Uterine leiomyoma Diseases 0.000 description 1
- 238000003975 animal breeding Methods 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000001715 carotid artery Anatomy 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 230000001627 detrimental effect Effects 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 210000000981 epithelium Anatomy 0.000 description 1
- 229940011871 estrogen Drugs 0.000 description 1
- 238000000556 factor analysis Methods 0.000 description 1
- 208000031424 hyperprolactinemia Diseases 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 238000011866 long-term treatment Methods 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000000178 monomer Substances 0.000 description 1
- 238000000465 moulding Methods 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 238000010606 normalization Methods 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 230000027758 ovulation cycle Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 230000035755 proliferation Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 238000007619 statistical method Methods 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 229940126680 traditional chinese medicines Drugs 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/14—Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
Abstract
The invention discloses application of geniposide in preparation of a medicament for treating hyperplasia of mammary glands. The invention discovers the application of geniposide in treating hyperplasia of mammary glands for the first time. Studies have shown that geniposide can reduce nipple height and breast diameter of hyperplasia of mammary glands, and reduce prolactin PRL and estradiol E 2 The level of the progesterone PROG is improved, and the medicine has definite curative effect on hyperplasia of mammary glands. Geniposide can be used as a single active ingredient or can be combined with other active ingredients to effectively treat hyperplasia of mammary glands.
Description
Technical Field
The invention belongs to the technical field of new application of medicines, and particularly relates to application of geniposide in preparation of medicines for treating hyperplasia of mammary glands.
Background
Under the action of endocrine hormones, particularly oestrogens, the mammary glands undergo proliferation and involution changes with changes in menstrual cycle. For some reasons, endocrine hormone metabolism is unbalanced, estrogen level is increased, hyperplasia and subinvolution of mammary tissue can occur, and after a period of time, the hyperplasia of mammary tissue can not completely subside, so that hyperplasia of mammary glands is formed. Hyperplasia of the mammary glands, neither tumor nor inflammation, is observed from a histological point of view: is hyperplasia and degeneration of mammary gland, and is closely related to endocrine dysfunction. The disease is well developed in middle-aged women, teenagers and postmenopausal women, and 50 to 70 percent of present large urban professional women have hyperplasia of mammary glands with different degrees. Hyperplasia of the breast is often manifested as pain in the breast and breast contact with nodules, which are not detrimental to the disease itself, but psychological stress, and fear that they will not develop breast cancer or become cancerous later. There are various pathological types of hyperplasia of mammary glands, such as simple lobular hyperplasia (which accounts for the majority of hyperplasia of mammary glands), and the pressure can be gradually relieved only by adjusting the mind and relieving the pressure. If hyperplasia of lobule of mammary glands is accompanied with hyperplasia of epithelium of the catheter and severe abnormal shape is caused, the hyperplasia is a precancerous lesion (occupying a very small part), and regular examination is required to be actively treated, so that the hyperplasia is prevented.
At present, hormone medicines are adopted by Western medicine to relieve hyperplasia of mammary glands, but a plurality of side effects and serious complications are often accompanied, so that the medicine is not suitable for long-term treatment; surgery is also very difficult to accept by most people and is easily recurrent; the traditional Chinese medicine can effectively treat hyperplasia of mammary glands, and has small toxic and side effects. However, traditional Chinese medicines are often compositions, have more medicinal ingredients and poor patient adaptability, and more effective monomer medicines are required to be continuously searched for treating hyperplasia of mammary glands.
Disclosure of Invention
The invention aims to: in order to solve the defects of the prior art, the invention provides application of geniposide in preparing medicaments for treating hyperplasia of mammary glands.
The technical scheme is as follows: in order to achieve the aim of the invention, the invention adopts the following technical scheme:
in a first aspect, the invention provides the use of geniposide in the manufacture of a medicament for the treatment of hyperplasia of mammary glands.
As a specific embodiment, the geniposide is capable of reducing nipple height and breast diameter in a patient with hyperplasia of mammary glands.
As a specific embodiment, the geniposide can reduce prolactin PRL and estradiol E in patients with hyperplasia of mammary glands 2 Levels, increased progesterone PROG levels.
Preferably, the medicament is an oral formulation.
Further preferably, the oral preparation is one of a tablet, a granule, a capsule, an oral liquid and a dripping pill.
Further preferably, the oral preparation comprises geniposide and pharmaceutically acceptable auxiliary materials and/or carriers.
In a second aspect, the invention provides the use of a composition comprising geniposide in the manufacture of a medicament for the treatment of hyperplasia of mammary glands.
As a specific embodiment, the geniposide is capable of reducing nipple height and breast diameter in a patient with hyperplasia of mammary glands.
As a specific embodiment, the geniposide can reduce prolactin PRL and estradiol E in patients with hyperplasia of mammary glands 2 Levels, increased progesterone PROG levels.
As a specific embodiment, one or more active ingredients are included in the composition, which necessarily include geniposide. That is, geniposide can be used as a single active ingredient to exert the effect of treating hyperplasia of mammary glands in the composition; geniposide can also be combined with other active components for treating hyperplasia of mammary glands to form the composition, so as to play a role in treating hyperplasia of mammary glands together.
The beneficial effects are that: the invention discovers the application of geniposide in treating hyperplasia of mammary glands for the first time. Studies have shown that geniposide can reduce nipple height and breast diameter of hyperplasia of mammary glands, and reduce prolactin PRL and estradiol E 2 The level of the progesterone PROG is improved, and the medicine has definite curative effect on hyperplasia of mammary glands. Geniposide can be used as a single active ingredient or can be combined with other active ingredients to effectively treat hyperplasia of mammary glands.
Detailed Description
The technical solutions in the embodiments of the present invention will be clearly and completely described below. The specific conditions are not noted in the examples and are carried out according to conventional conditions or conditions recommended by the manufacturer. The reagents or apparatus used were conventional products commercially available without the manufacturer's attention.
Examples
1. Experimental materials
1.1 major reagents
Geniposide, CAS number: 24512-63-8, shanghai Hotan Biotechnology Co., ltd; rupixiao tablet (Shenyang Red medicine group Co., ltd.). Estradiol benzoate, progesterone (Shanghai Ala Biochemical technologies Co., ltd.); rat estradiol (E2), progesterone (PROG), prolactin (PRL) enzyme-linked immunosorbent assay kit (wuhanhua bikeside biotechnology limited).
1.2 laboratory animals
Female SD rats were purchased from the nanjing green longshan animal breeding ground. The related operation of each experiment meets the requirements of the guidelines for the management and use of laboratory animals.
2. Experimental method
2.1 grouping and administration
The 60 rats were randomly divided into a blank group, a model group, a positive drug group and a low, medium and high dose group of geniposide, each group having 10 rats. The inner side of the hind legs of each group of rats except the blank group was intramuscularly injected with estradiol benzoate (0.5 mg/kg) 1 time a day for 25 days, followed by intramuscular injection of progesterone (5 nmg/kg) 1 time a day for 5 days to establish a model of hyperplasia of mammary glands. Meanwhile, normal saline (1 mL/100 g) is administrated by the stomach of rats in a blank group and a model group, the nodules of breast of the rats in a positive medicament group are administrated by the stomach of the rats in 960mg/kg respectively, the geniposide is administrated by the stomach of the rats in low, medium and high dose groups in 150mg/kg, 200mg/kg and 250mg/kg respectively, and the geniposide is administrated by the stomach of the rats in a positive medicament group 1 time a day for 42 days continuously.
2.2 index detection
After 24 hours of last dose, the vernier caliper precisely measures the 2 nd pair of nipple height and breast diameter of the rat. Collecting blood from carotid artery of rat, centrifuging at 4deg.C and 3500r/min for 10min to collect serum, preserving at-20deg.C, and determining serum E of rat according to ELISA kit specification 2 PROG, PRL levels.
2.3 statistical analysis
The SPSS13.0 statistical software package was applied for processing. The normalization and variance alignment test is performed on the measured data. Metering data toThe mean-average number of multiple samples is compared in pairs by single-factor analysis of variance.
3 results
3.1 influence of geniposide on rat nipple height and breast diameter
The nipple height and breast diameter of the rats were measured as described above, and the results are shown in table 1 below.
TABLE 1 rat nipple height and breast diametern＝10)
Note that: p <0.05 compared to the blank group; compared to the model group, #p <0.05.
From the results in table 1 above, it can be seen that the nipple height and breast diameter of rats in the model group are significantly improved compared to the blank group, indicating that the molding was successful. Compared with the model group, the positive medicine group and the geniposide low, medium and high dose groups of rats have significantly reduced nipple height and breast diameter. The treatment effect of the geniposide dosage group is equivalent to that of the nodules of breast eliminating tablets.
3.2 geniposide against rat serum E 2 Effects of PROG, PRL levels
Detection of E in rat serum according to the method described above 2 PROG, PRL levels, results are shown in table 2 below:
TABLE 2E in rat serum 2 PROG and PRL leveln＝10)
Note that: p <0.05 compared to the blank group; compared to the model group, #p <0.05.
As can be seen from the results of Table 2 above, the serum E of the rats in the model group was compared with the blank group 2 And PRL levels are significantly elevated and PROG levels are significantly reduced. Serum E of rats in low, medium and high dose groups of geniposide, as compared to model group, positive drug group 2 And PRL levels were significantly reduced and PROG levels were significantly increased. The treatment effect of the geniposide dosage group is equivalent to that of the nodules of breast eliminating tablets.
Hypothalamic-pituitary-gonadal axis is a component of neural architectureOne of the parts plays an important role in maintaining the stable internal environment and normal physiological functions of the body, and abnormal secretion of sex hormone can lead to the occurrence of many diseases such as hyperprolactinemia, hyperplasia of mammary glands, hysteromyoma and the like. Various sex hormone levels co-regulate breast tissue, with elevated Prolactin (PRL) levels being considered an important factor in causing hyperplasia of the breast, progesterone (PROG) levels promoting acinar tissue and lobules of the breast, estradiol (E 2 ) The increased levels act to inhibit the growth of fibrous tissue surrounding the ducts and breast ducts. Sex hormone disorders often occur in models of hyperplasia of mammary glands, E can be regulated by modulating hypothalamic-pituitary-gonadal axis balance 2 PROG and PRL levels, restore ovary function, and eliminate lobular hyperplasia and acinar hyperplasia. Thus, serum E is reduced 2 And PRL level, raise PROG level, can effectively relieve hyperplasia of mammary glands.
In conclusion, geniposide can effectively reduce nipple height and breast diameter of mammary gland hyperplasia rats, and obviously reduce serum E 2 And PRL level, raise PROG level, show that it has obvious therapeutic effect for hyperplasia of mammary glands.
The above examples illustrate only a few embodiments of the invention, which are described in detail and are not to be construed as limiting the scope of the invention. It should be noted that it will be apparent to those skilled in the art that several variations and modifications can be made without departing from the spirit of the invention, which are all within the scope of the invention. Accordingly, the scope of protection of the present invention is to be determined by the appended claims.
Claims (10)
1. Application of geniposide in preparing medicine for treating hyperplasia of mammary glands is provided.
2. The use according to claim 1, wherein the geniposide is capable of lowering nipple height and breast diameter in a patient suffering from hyperplasia of mammary glands.
3. Use according to claim 1, characterized in that the geniposide is capable ofReducing prolactin PRL and estradiol E in patients with hyperplasia of mammary glands 2 Levels, increased progesterone PROG levels.
4. The use according to claim 1, wherein the medicament is an oral formulation.
5. The use according to claim 4, wherein the oral preparation is one of a tablet, a granule, a capsule, an oral liquid, and a dripping pill.
6. The use according to claim 4, wherein the oral formulation comprises geniposide and pharmaceutically acceptable excipients and/or carriers.
7. Application of a composition containing geniposide in preparing medicine for treating hyperplasia of mammary glands is provided.
8. The use according to claim 6, wherein the composition is capable of reducing nipple height and breast diameter in a patient with hyperplasia of mammary glands.
9. The use according to claim 6, wherein the composition is capable of reducing prolactin PRL and estradiol E in a patient suffering from hyperplasia of mammary glands 2 Levels, increased progesterone PROG levels.
10. The use according to claim 6, wherein one or more active ingredients are included in the composition, which necessarily include geniposide.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202311383374.1A CN117338799A (en) | 2023-10-24 | 2023-10-24 | Application of geniposide in preparation of medicine for treating hyperplasia of mammary glands |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202311383374.1A CN117338799A (en) | 2023-10-24 | 2023-10-24 | Application of geniposide in preparation of medicine for treating hyperplasia of mammary glands |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN117338799A true CN117338799A (en) | 2024-01-05 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202311383374.1A Pending CN117338799A (en) | 2023-10-24 | 2023-10-24 | Application of geniposide in preparation of medicine for treating hyperplasia of mammary glands |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN117338799A (en) |
-
2023
- 2023-10-24 CN CN202311383374.1A patent/CN117338799A/en active Pending
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