CN107865855A - Apigenin is preparing the application in treating breast cancer medicines - Google Patents
Apigenin is preparing the application in treating breast cancer medicines Download PDFInfo
- Publication number
- CN107865855A CN107865855A CN201610849064.8A CN201610849064A CN107865855A CN 107865855 A CN107865855 A CN 107865855A CN 201610849064 A CN201610849064 A CN 201610849064A CN 107865855 A CN107865855 A CN 107865855A
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- CN
- China
- Prior art keywords
- apigenin
- breast cancer
- mcf
- cancer medicines
- medicines
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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
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses Apigenin to prepare the application in treating breast cancer medicines, belongs to technical field of new application of medicine.The present invention is evaluated by external MTT antineoplastic activity and found, growths of the Apigenin to Breast cancer lines 4T1, MCF 7, MDA MB 231 and MCF 7B also has significant inhibitory action.Therefore, Apigenin can be used to prepare anti-breast cancer medicines, have good development prospect.For Apigenin of the present invention, the purposes in treatment breast cancer medicines are prepared belongs to first public, and it is unexpectedly strong for the inhibitory activity of breast cancer cell.
Description
Technical field
The present invention relates to compound Apigenin new application, more particularly to Apigenin to prepare treatment breast cancer medicines
In application.
Background technology
Cancer is one of disease maximum to human life and health harm, has substantial amounts of people to die from cancer every year.Anticancer
The research and development of medicine are always the focus of study of pharmacy.It is natural products or derivatives thereof to have 74% in antineoplastic, such as Japanese yew
Alcohol and its derivative are exactly the current clinically relatively good antineoplastic of application effect.Therefore, found from natural products anti-
Chemical compound for treating cancer or lead compound have great importance.
Compound Apigenin of the present invention is one and delivers within 2013 (Ebenezer de Mello Cruz, et
al.,Leishmanicidal activity of Cecropia pachystachya flavonoids:Arginase
inhibition and altered mitochondrial DNA arrangement.Phytochemistry,89(2013)
71-77.) noval chemical compound, the compound possess brand-new framework types (Ebenezer de Mello Cruz, et al.,
Leishmanicidal activity of Cecropia pachystachya flavonoids:Arginase
inhibition and altered mitochondrial DNA arrangement.Phytochemistry,89(2013)
71-77.), belong to first public for purposes of the Apigenin of the present invention in treatment breast cancer medicines are prepared, due to
Belong to brand-new structure type, and it is unexpectedly strong for the inhibitory activity of breast cancer cell, in the absence of by other changes
Compound provides the possibility of any enlightenment, possesses prominent substantive distinguishing features, while obviously have significantly for the preventing and treating of breast cancer
Progress.
The content of the invention
It is an object of the invention to do not find that it has the report of anti-breast cancer activity in being studied according to existing Apigenin
Present situation, there is provided applications of the Apigenin in anti-breast cancer medicines are prepared.
Shown in the compound Apigenin structures such as formula (I)：
Applications of the Apigenin in breast cancer medicines are treated, breast cancer cell be Breast cancer lines 4T1,
MCF-7, MDA-MB-231 and MCF-7B.
One kind treats breast cancer medicines, is that active component addition auxiliary material is prepared by Apigenin, preparation method is to take 5
G of compound Apigenin, 195 grams of dextrin is added, mixed, Conventional compression is made 1000.
One kind treats breast cancer medicines, is that active component addition auxiliary material is prepared by Apigenin, preparation method is to take 5
G of compound Apigenin, 195 grams of starch is added, mixed, it is encapsulated to be made 1000.
The present invention is evaluated by external MTT antineoplastic activity and found, Apigenin is to Breast cancer lines 4T1, MCF-
7th, MDA-MB-231 and MCF-7B growth also has significant inhibitory action, suppresses the IC50 values difference of this 4 plants of cell growths
For 0.49 ± 0.31 μM, 0.83 ± 0.52 μM, 0.49 ± 0.23 μM and 0.81 ± 0.57 μM.Therefore, Apigenin can be used to make
Standby anti-breast cancer medicines, have good development prospect.
Belong to first public for purposes of the Apigenin of the present invention in treatment breast cancer medicines are prepared, due to
Framework types belong to brand-new framework types, and it is unexpectedly strong for the inhibitory activity of breast cancer cell, is not present
The possibility of any enlightenment is provided by other compounds, possesses prominent substantive distinguishing features, at the same it is obvious for the preventing and treating of breast cancer
With significant progressive.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by specific reality
Any restrictions of example are applied, but are defined in the claims.
Embodiment
Compound Apigenin involved in the present invention preparation method referring to document (Ebenezer de Mello Cruz,
et al.,Leishmanicidal activity of Cecropia pachystachya flavonoids:Arginase
inhibition and altered mitochondrial DNA arrangement.Phytochemistry,89(2013)
71–77.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by specific reality
Any restrictions of example are applied, but are defined in the claims.
Embodiment 1：The preparation of compound Apigenin tablets involved in the present invention：
Take 5 g of compound Apigenin to add 195 grams of starch, mix, conventional tablet presses are made 1000.
Embodiment 2：The preparation of compound Apigenin capsules involved in the present invention：
Take 5 g of compound Apigenin to add 195 grams of dextrin, mix, it is encapsulated to be made 1000.
Its pharmaceutical activity is further illustrated below by pharmacodynamic experiment.
Experimental example：Growth inhibition effects of the compound Apigenin to Breast cancer lines is evaluated using mtt assay
1. method：Cell in growth logarithmic phase：Breast cancer lines 4T1, MCF-7, MDA-MB-231 and MCF-
7B (buying from Chinese Academy of Sciences's cell bank) is with 1.5 × 104Concentration kind is in 96 orifice plates.Original is sucked after cell culture 24h is adherent
The culture medium come.Experiment is divided into blank control group, drug-treated group.Blank group changes 1640 cultures containing 10% hyclone
Base；Drug-treated group is changed containing the Apigenin that concentration is 100 μM, 50 μM, 10 μM, 1 μM, 0.1 μM, 0.01 μM and 0.001 μM
Culture medium.After cultivating 48h, concentration 5mg/mL MTT is added, continues to be put in CO2Incubator culture 4h, then along nutrient solution
Top sucks 100 μ L of supernatant, adds 100 μ L DMSO, and 10min is placed in dark place, is surveyed using ELIASA (Sunrise Products)
Determine light absorption value (wavelength 570nm), and cell survival is calculated according to light absorption value, each processing sets 6 repeating holes.Cell survival
Rate (%)=Δ OD drug-treateds/Δ OD blank control × 100.
2. result：Growth tools of the Apigenin to Breast cancer lines P 4T1, MCF-7, MDA-MB-231 and MCF-7B
There is significant inhibitory action.The compound suppresses Breast cancer lines 4T1, MCF-7, MDA-MB-231 and MCF-7B growth
IC50 values are respectively 0.49 ± 0.31 μM, 0.83 ± 0.52 μM, 0.49 ± 0.23 μM and 0.81 ± 0.57 μM.
Shown by above-described embodiment, Apigenin of the invention is to Breast cancer lines 4T1, MCF-7, MDA-MB-231
Growth with MCF-7B has good inhibiting effect.Thus prove, Apigenin of the invention has anti-breast cancer activity, energy
For preparing anti-breast cancer medicines.
Claims (4)
- Applications of the 1.Apigenin in breast cancer medicines are treated, shown in the compound Apigenin structures such as formula (I)：
- 2. applications of the Apigenin as claimed in claim 1 in breast cancer medicines are treated, it is characterised in that breast cancer cell is Breast cancer lines 4T1, MCF-7, MDA-MB-231 and MCF-7B.
- 3. one kind treats breast cancer medicines, it is characterised in that the Apigenin as described in claim 1 is that active component adds auxiliary material It is prepared, preparation method adds 195 grams of dextrin, mixed, Conventional compression is made 1000 to take 5 g of compound Apigenin.
- 4. one kind treats breast cancer medicines, it is characterised in that the Apigenin as described in claim 1 is that active component adds auxiliary material It is prepared, preparation method adds 195 grams of starch, mixing is encapsulated to be made 1000 to take 5 g of compound Apigenin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610849064.8A CN107865855A (en) | 2016-09-24 | 2016-09-24 | Apigenin is preparing the application in treating breast cancer medicines |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610849064.8A CN107865855A (en) | 2016-09-24 | 2016-09-24 | Apigenin is preparing the application in treating breast cancer medicines |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107865855A true CN107865855A (en) | 2018-04-03 |
Family
ID=61750719
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610849064.8A Pending CN107865855A (en) | 2016-09-24 | 2016-09-24 | Apigenin is preparing the application in treating breast cancer medicines |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107865855A (en) |
-
2016
- 2016-09-24 CN CN201610849064.8A patent/CN107865855A/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20180403 |
|
| WD01 | Invention patent application deemed withdrawn after publication |