CN106852921A - It is a kind of to treat medicine of breast cancer and its preparation method and application - Google Patents
It is a kind of to treat medicine of breast cancer and its preparation method and application Download PDFInfo
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- CN106852921A CN106852921A CN201611209677.1A CN201611209677A CN106852921A CN 106852921 A CN106852921 A CN 106852921A CN 201611209677 A CN201611209677 A CN 201611209677A CN 106852921 A CN106852921 A CN 106852921A
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- breast cancer
- sesamol
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- 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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
- A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
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- 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
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/047—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
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- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
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- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Medicine of breast cancer and its preparation method and application is treated the invention discloses a kind of, the medicine is made up of the following raw material according to weight portion：37 parts of sesamol, 7 15 parts of C14H10Cl2NNaO2,13 parts of nicotinic acid, 11 19 parts of inositol.Sesamol, C14H10Cl2NNaO2 are mixed with inositol, the deionized water of 3.8 times of three's mass is added, microwave treatment 8min is obtained mixture A；Mixture A is mixed with nicotinic acid, the ultrasonically treated 20min at a temperature of 40 DEG C, then medicine is obtained final product to dry in 45 DEG C of stirrings.Medicine of the present invention has the low advantage of toxic and side effect under the synergy of each raw material while it is obtained notable drug effect when breast cancer is treated, and obtains unexpected technique effect.The present invention have the advantages that raw material simply, be easy to get, dosage is small, curative effect is high, have no toxic side effect.Used as anti-breast cancer medicine, preparation process is simple, low cost is suitable to large-scale promotion to the present invention.
Description
Technical field
It is specifically a kind of to treat medicine of breast cancer and its preparation method and application the present invention relates to pharmaceutical technology field.
Background technology
Cancer is common frdquently encountered disease, and the life of the people and healthy in serious harm, due to pathogenesis of cancer position not
Together, can there are a variety of cancers, such as breast cancer, stomach cancer, breast cancer, osteocarcinoma, cutaneum carcinoma, intestinal cancer, liver cancer.
Breast cancer is that the malignant tumour in mammary gland galandular epithelium tissue occurs.99% occurs in women in breast cancer, and male is only
Account for 1%.The cause of disease of breast cancer is not yet fully apparent from, and research finds that the morbidity of breast cancer has certain regularity, with mammary gland
The women of cancer high risk factor easily suffers from breast cancer.So-called high risk factor refers to the various hazards relevant with pathogenesis of breast carcinoma,
And the hazards that most of patient with breast cancers have are known as the high risk factor of breast cancer.It is aobvious according to China's tumour registration annual report
Show：Reduced levels at 0~24 years old age bracket of women with breast cancer agespecific attack rate, are gradually increasing after 25 years old, and group reaches within 50~54 years old
To peak, it is gradually reduced later within 55 years old.Family history of breast cancer is the hazards of mammary gland carcinogenesis.In recent years find that corpus mamma is caused
The close also hazards as breast cancer.The hazards of breast cancer also have menarche it is early (<12 years old), menopause late (>55 years old)；
It is unmarried, do not educate, late childbirth, non-lactation；Suffer from the not timely diagnosis and treatment of benign breast disease；Confirm to suffer from through hospital's biopsy (biopsy)
Atypical hyperplasia；Chest receives the irradiation of too high dose radioactive ray；Long-term taking exogenous estrogen；Post menopausal is fat；
Long-term excessive consumption of alcohol；And carry the mutator related to breast cancer.
The scheme of current clinical treatment breast cancer is mainly controlled including operation, radiotherapy, chemotherapy, endocrine therapy and traditional Chinese medicine
Treat etc..Nearly 100 are founded from radical mastectomy for many years, operation is always one of main method for the treatment of breast cancer, especially
It is prefered method that focus is limited to part or lymph node patient.But, research shows, patient with breast cancer after initial surgery still
Risk of recurrence higher so is faced with, the peak of its recurrence concentrates on about 2 years or so.Postoperative chemotherapy and endocrine therapy can be with
The year case fatality rate of breast cancer is set to decline 20% or so, but chemotherapy, radiotherapy and endocrine therapy often produce gastrointestinal reaction, in vain
The side effects such as cell reduction, alopecia.How while radiotherapy in breast cancer chemotherapeutic efficacy is increased, its toxic and side effect is reduced as far as possible,
Improve the attention that quality of life gradually causes this area researcher.In sum, evident in efficacy, poison is found in research
The Chinese medicine of the low treatment breast cancer of property is still current medical science urgent problem.
The content of the invention
Medicine of breast cancer and its preparation method and application is treated it is an object of the invention to provide a kind of, it is above-mentioned to solve
The problem proposed in background technology.
To achieve the above object, the present invention provides following technical scheme：
A kind of medicine for treating breast cancer, is made up of the following raw material according to weight portion：Sesamol 3-7 parts, Diclofenac
Sodium 7-15 parts, nicotinic acid 1-3 parts, inositol 11-19 parts.
As further scheme of the invention：The medicine of the treatment breast cancer, by the following raw material group according to weight portion
Into：Sesamol 4-6 parts, C14H10Cl2NNaO2 9-13 parts, nicotinic acid 1.5-2.5 parts, inositol 13-17 parts.
As further scheme of the invention：The medicine of the treatment breast cancer, by the following raw material group according to weight portion
Into：5 parts of sesamol, 11 parts of C14H10Cl2NNaO2,2 parts of nicotinic acid, 15 parts of inositol.
A kind of preparation method of the medicine for treating breast cancer, comprises the steps of：
1) sesamol, C14H10Cl2NNaO2 and inositol are mixed, adds the deionized water of 3.8 times of three's mass, microwave treatment
8min, microwave power is 800W, and mixture A is obtained；
2) mixture A is mixed with nicotinic acid, the ultrasonically treated 20min at a temperature of 40 DEG C, ultrasonic power is 600W, then
45 DEG C of stirrings obtain final product medicine to dry.
Application of the medicine in treatment breast cancer medicines are prepared.
Compared with prior art, the beneficial effects of the invention are as follows：
Medicine of the present invention makes it have while obtaining notable drug effect when breast cancer is treated under the synergy of each raw material
The low advantage of toxic side effect, obtains unexpected technique effect.The present invention has that raw material is simple, is easy to get, dosage is small,
The advantage that curative effect is high, have no toxic side effect.Therefore, medicine of the invention is used as anti-breast cancer medicine, preparation process is simple, low cost,
Patient's interdependence is high, is suitable to large-scale promotion.
Specific embodiment
Below in conjunction with the embodiment of the present invention, the technical scheme in the embodiment of the present invention is clearly and completely described,
Obviously, described embodiment is only a part of embodiment of the invention, rather than whole embodiments.Based in the present invention
Embodiment, the every other embodiment that those of ordinary skill in the art are obtained under the premise of creative work is not made, all
Belong to the scope of protection of the invention.
Embodiment 1
In the embodiment of the present invention, a kind of medicine for treating breast cancer is made up of the following raw material according to weight portion：Sesamol
3 parts, 7 parts of C14H10Cl2NNaO2,1 part of nicotinic acid, 11 parts of inositol.
Sesamol, C14H10Cl2NNaO2 are mixed with inositol, the deionized water of 3.8 times of three's mass, microwave treatment is added
8min, microwave power is 800W, and mixture A is obtained.Mixture A is mixed with nicotinic acid, it is ultrasonically treated at a temperature of 40 DEG C
20min, ultrasonic power is 600W, then obtains final product medicine to dry in 45 DEG C of stirrings.
Embodiment 2
In the embodiment of the present invention, a kind of medicine for treating breast cancer is made up of the following raw material according to weight portion：Sesamol
7 parts, 15 parts of C14H10Cl2NNaO2,3 parts of nicotinic acid, 19 parts of inositol.
Sesamol, C14H10Cl2NNaO2 are mixed with inositol, the deionized water of 3.8 times of three's mass, microwave treatment is added
8min, microwave power is 800W, and mixture A is obtained.Mixture A is mixed with nicotinic acid, it is ultrasonically treated at a temperature of 40 DEG C
20min, ultrasonic power is 600W, then obtains final product medicine to dry in 45 DEG C of stirrings.
Embodiment 3
In the embodiment of the present invention, a kind of medicine for treating breast cancer is made up of the following raw material according to weight portion：Sesamol
4 parts, 9 parts of C14H10Cl2NNaO2,1.5 parts of nicotinic acid, 13 parts of inositol.
Sesamol, C14H10Cl2NNaO2 are mixed with inositol, the deionized water of 3.8 times of three's mass, microwave treatment is added
8min, microwave power is 800W, and mixture A is obtained.Mixture A is mixed with nicotinic acid, it is ultrasonically treated at a temperature of 40 DEG C
20min, ultrasonic power is 600W, then obtains final product medicine to dry in 45 DEG C of stirrings.
Embodiment 4
In the embodiment of the present invention, a kind of medicine for treating breast cancer is made up of the following raw material according to weight portion：Sesamol
6 parts, 13 parts of C14H10Cl2NNaO2,2.5 parts of nicotinic acid, 17 parts of inositol.
Sesamol, C14H10Cl2NNaO2 are mixed with inositol, the deionized water of 3.8 times of three's mass, microwave treatment is added
8min, microwave power is 800W, and mixture A is obtained.Mixture A is mixed with nicotinic acid, it is ultrasonically treated at a temperature of 40 DEG C
20min, ultrasonic power is 600W, then obtains final product medicine to dry in 45 DEG C of stirrings.
Embodiment 5
In the embodiment of the present invention, a kind of medicine for treating breast cancer is made up of the following raw material according to weight portion：Sesamol
5 parts, 11 parts of C14H10Cl2NNaO2,2 parts of nicotinic acid, 15 parts of inositol.
Sesamol, C14H10Cl2NNaO2 are mixed with inositol, the deionized water of 3.8 times of three's mass, microwave treatment is added
8min, microwave power is 800W, and mixture A is obtained.Mixture A is mixed with nicotinic acid, it is ultrasonically treated at a temperature of 40 DEG C
20min, ultrasonic power is 600W, then obtains final product medicine to dry in 45 DEG C of stirrings.
Comparative example 1
In addition to sesamol is not contained, its formula and preparation process are consistent with embodiment 5.
Comparative example 2
Only contain sesamol, its preparation process is consistent with embodiment 5.
The toxicity test of embodiment 6
1) acute toxicity testing：
Using NIH mouse 60, SPF grades, male and female half and half, 18~22g of body weight carries out acute toxicity test.Mouse is random
It is divided into two groups, every group 30, i.e. control group and administration group, fasting 12 hours before experiment；Medicine prepared by embodiments of the invention 5
Thing is dissolved in water, (concentration is 6.58g crude drugs/ml, maximum concentration) gavage, and gavage volume is 5ml/kg (i.e. single-dose agent
It is 32.9 crude drugs/kg to measure), control group gives normal saline, is administered 2 times within one day, delivery time 6 hours, after administration
Continuous Observation 14 days, and record the toxic reaction and death toll of mouse.Test result indicate that：Compare with control group, after administration
Mouse has no notable difference, tests Continuous Observation 14 days, and mouse systemic situation, diet, drinking-water, body weight increase are normal.Mouse
32.9 crude drugs of oral administration gavage medicine LD50 ＞ of the invention/kg, daily maximum dosage-feeding is 65.8 crude drugs/kg/ days.It is of the invention
Clinical drug dosage is 1.5g crude drugs/day/people, and in terms of 60kg, average dosage is 0.025g crude drugs/kg/ to adult's body weight
Day.By batheroom scale：The dosis tolerata of mouse (average weight is counted with 20g) oral administration gavage medicine of the invention as quantity 1316
Times.Therefore Acute toxicity of the invention is low, clinical application safety.
2) long term toxicity test：
The medicine of the embodiment of the present invention 5 presses 10.78,20.35 and 33.48g crude drugs/kg continuous uses 15 weeks to mouse
After (1.0ml/100g body weight, daily 2 times) and drug withdrawal 3 weeks, as a result show：Hair, behavior, size of the medicine of the present invention to rat
Just, the index such as body weight, organ weights, blood picture, hepatic and renal function, blood sugar, blood fat has no significant effect, and internal organs naked eyes do not find different
Sample change and histological indications show, medication 15 weeks and be discontinued 3 weeks after, each internal organs of rat without substantially changes.Illustrate this
Invention medicine does not have abnormal reaction, using safety to small toxicity after rat long-term prescription yet after drug withdrawal.
Embodiment 7
Inhibitory action of the pharmaceutical composition of the present invention to transplanted breast carcinoma
(1) preparation of transplanted breast carcinoma mouse model
SPF grades of female sex-health TA2 mouse 60,6 week old, weight 16g-18g.Take the exponential phase of in vitro culture
MA-891 mouse mastopathy cells, it is 1 × 10 to adjust MA-891 cell concentrations with aseptic PBS7/mL.Aseptically, will
It is subcutaneous that MA-891 mouse mastopathy cells are inoculated in the right armpit of TA2 mouse, and inoculum concentration is that only (cell number is 2 × 10 to 0.2ml/6/
Only).Whole seeded process must be carried out in aseptic cover with sterile working, and inoculation is completed in 1h.Treat that subcutaneous transplantation knurl volume reaches
60mm3During left and right (about 10d), model manufacturing success.
(2) packet and administration
It is divided into following 5 groups, every group 12 by knurl volume and mice with tumor body weight homeostatic principle：
Model control group：1 times/day of the physiological saline of gavage equivalent, is administered 60 altogether；
Medicine group of the present invention：Gavage gives the medicine of the preparation of embodiment 5, and dosage is 25mg crude drugs/kg, 1 times/day, is given altogether
Medicine 40 days；
1 group of comparative example：Gavage gives the medicine of the preparation of comparative example 1, and dosage is 25mg crude drugs/kg, 1 times/day, 40 is administered altogether
Day；
2 groups of comparative example：Gavage gives the medicine of the preparation of comparative example 2, and dosage is 25mg crude drugs/kg, 1 times/day, 40 is administered altogether
Day；
5-FU groups：Intraperitoneal injection 10mg/kg oxaliplatins, the next day be administered once, 10 times altogether.
Dislocated after last dose 48h and put to death mouse, cut off transplantable tumor, weigh knurl weight.Tumor-like hyperplasia (%) IR=(1- realities
Test a group knurl weight average/model control group knurl weight average) × 100%.Medicine is relatively embodied to mouse breast cancer by knurl weight
The influence of MA-891 Carbazole alkaloids knurl growth.Data are represented with mean ± standard deviation (x ± s), carried out using SPSS15.0 softwares
Variance analysis.
(3) result and analysis
Result of the test shows (referring to table 1)：Compared with model control group, each treatment group is to MA-891 mouse breast cancer models
The inhibitory action of growth be respectively provided with pole significant difference (P ＜ 0.01), collaboration work of this explanation medicine of the present invention in each raw material
There is highly significant curative effect under in terms of breast cancer is treated.In addition, medicine group of the present invention is better than chemotherapy in terms of tumour inhibiting rate
5-FU groups, administration terminates the dead mouse 2 of rear 5-FU groups, and the curative effect of this explanation medicine of the present invention is better than existing chemotherapeutics,
And there is the low advantage of toxic and side effect while notable drug effect is obtained, unexpected technique effect is obtained.
Inhibitory action of the pharmaceutical composition of the present invention of table 1 to transplanted breast carcinoma
| Sample size (starts/terminates) | Knurl weight/g | Average tumour inhibiting rate/% | |
| Model control group | 12/12 | 1.45±0.21 | - |
| 1 group of comparative example | 12/12 | 0.78±0.28** | 46.2 |
| 2 groups of comparative example | 12/11 | 1.32±0.32** | 9.0 |
| 5-FU groups | 12/10 | 0.58±0.23** | 60 |
| Medicine group of the present invention | 12/12 | 0.41±0.15** | 71.7 |
Compare with model control group, * * P ＜ 0.01.
It is obvious to a person skilled in the art that the invention is not restricted to the details of above-mentioned one exemplary embodiment, Er Qie
In the case of without departing substantially from spirit or essential attributes of the invention, the present invention can be in other specific forms realized.Therefore, no matter
From the point of view of which point, embodiment all should be regarded as exemplary, and be nonrestrictive, the scope of the present invention is by appended power
Profit requires to be limited rather than described above, it is intended that all in the implication and scope of the equivalency of claim by falling
Change is included in the present invention.
Moreover, it will be appreciated that although the present specification is described in terms of embodiments, not each implementation method is only wrapped
Containing an independent technical scheme, this narrating mode of specification is only that for clarity, those skilled in the art should
Specification an as entirety, the technical scheme in each embodiment can also be formed into those skilled in the art through appropriately combined
May be appreciated other embodiment.
Claims (5)
1. a kind of medicine for treating breast cancer, it is characterised in that be made up of the following raw material according to weight portion：Sesamol 3-7 parts,
C14H10Cl2NNaO2 7-15 parts, nicotinic acid 1-3 parts, inositol 11-19 parts.
2. it is according to claim 1 treatment breast cancer medicine, it is characterised in that by the following raw material group according to weight portion
Into：Sesamol 4-6 parts, C14H10Cl2NNaO2 9-13 parts, nicotinic acid 1.5-2.5 parts, inositol 13-17 parts.
3. it is according to claim 1 treatment breast cancer medicine, it is characterised in that by the following raw material group according to weight portion
Into：5 parts of sesamol, 11 parts of C14H10Cl2NNaO2,2 parts of nicotinic acid, 15 parts of inositol.
4. the preparation method of the medicine of a kind for the treatment of breast cancer as described in claim 1-3 is any, it is characterised in that by following
Step is constituted：
1) sesamol, C14H10Cl2NNaO2 and inositol are mixed, the deionized water of 3.8 times of addition three mass, microwave treatment 8min,
Microwave power is 800W, and mixture A is obtained；
2) mixture A is mixed with nicotinic acid, the ultrasonically treated 20min at a temperature of 40 DEG C, ultrasonic power is 600W, then at 45 DEG C
Stirring obtains final product medicine to dry.
5. application of the medicine as described in claim 1-3 is any in treatment breast cancer medicines are prepared.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611209677.1A CN106852921A (en) | 2016-12-23 | 2016-12-23 | It is a kind of to treat medicine of breast cancer and its preparation method and application |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201611209677.1A CN106852921A (en) | 2016-12-23 | 2016-12-23 | It is a kind of to treat medicine of breast cancer and its preparation method and application |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106852921A true CN106852921A (en) | 2017-06-16 |
Family
ID=59126580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201611209677.1A Pending CN106852921A (en) | 2016-12-23 | 2016-12-23 | It is a kind of to treat medicine of breast cancer and its preparation method and application |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106852921A (en) |
-
2016
- 2016-12-23 CN CN201611209677.1A patent/CN106852921A/en active Pending
Non-Patent Citations (4)
| Title |
|---|
| ALIX JACKLIN等: "The sesame seed oil constituent, sesamol, induces growth arrest and apoptosis of cancer and cardiovascular cells", 《ANNALS OF THE NEW YORK ACADEMY OF SCIENCES》 * |
| MARIA FRANCESCA SANTOLLA等: "Niacin activates the G protein estrogen receptor (GPER)-mediated signaling", 《CELLULAR SIGNALLING》 * |
| 于正洪主编: "《乳腺癌防治导读（第2版）》", 30 November 2015, 东南大学出版社 * |
| 姚静: "《药用辅料应用指南》", 31 August 2011, 中国医药科技出版社 * |
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Application publication date: 20170616 |