CN107213146A - Application of the wogonin in treatment colon cancer drug is prepared - Google Patents
Application of the wogonin in treatment colon cancer drug is prepared Download PDFInfo
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- CN107213146A CN107213146A CN201710406070.0A CN201710406070A CN107213146A CN 107213146 A CN107213146 A CN 107213146A CN 201710406070 A CN201710406070 A CN 201710406070A CN 107213146 A CN107213146 A CN 107213146A
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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
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Abstract
The present invention relates to application of the wogonin in treatment colon cancer drug is prepared, wherein shown in the chemical structural formula of described wogonin such as following formula (I).The effect of wogonin treatment colon cancer in application of the present invention significantly, there is very strong inhibitory action to Growth of Colon Cancer Cells in vitro, and can suppress colon cancer cell HCT116 autophagy, promotes Apoptosis；The growth to chemical induction tumor model has good inhibitory action in vivo.
Description
Technical field：
The present invention relates to the pharmaceutical product containing heterocyclic compound, and in particular to from labiate flavonoid
The anti-tumor medicinal preparation of thing.
Background technology：
Colon cancer is one of big common cancer of China nine.In China, colon cancer morbidity is in rising trend in recent years.
Counted according to Cancer in China, estimation will have 2814000 Chinese for 2015 and die from cancer.Masculinity and femininity death rate highest
Cancer is：Lung and bronchiolar carcinoma, stomach cancer, liver cancer, cancer of the esophagus, colorectal cancer, have accounted for 3/4ths of all cancer mortalities.
Because of colon cancer died, male occupies the 5th of mortality of malignant tumors, and women occupies the 6th.Therefore, new effective colon is sought
Cancer medicine, improves clinical efficacy, be it is current in the urgent need to research the problem of.With the development of China's traditional Chinese medicine, from medium-height grass
Seek in medicine with efficiently, low toxicity, it is stable the features such as antineoplastic be one of means for being particularly suitable for.
Wogonin (Wogonin) is one of active component of Chinese traditional herbs radix scutellariae, its chemical constitution such as following formula (I) institute
Show, find 41 kinds of flavone compounds from radix scutellariae at present, wherein content is higher and has being mainly for obvious pharmacological action
Scutelloside (baicalin), baicalein (baicalein), wogonin (wogonin), wogonoside (wogonoside) and
Oroxylin (oroxylin A) etc..In recent years, domestic and international researcher never Tongfang in face of wogonin antitumaous effect and
Mechanism of action is conducted in-depth research, it is found that wogonin has its unique mechanism to the lethal effect of tumour cell.
Wogonin is contained flavone compound in labiate radix scutellariae and the root for belonging to various plants together, its chemistry
Entitled 5,7- dihydroxy -8- methoxyl groups -2- phenyl -4H-1- benzofuran -4- ketone, molecular formula is C16H12O5, and molecular weight is
284.26.Wogonin be it is a kind of be dissolved in organic solvent and water insoluble yellow needles thing, now there are some researches show the Chinese is yellow
A kind of reed mentioned in ancient books have multiple pharmacological effect, including antioxidation, and blood coagulation resisting function, spasmolysis additionally wants antibacterial, antivirus action
And diuresis etc..But, have not yet to see the report that the extract described in similar invention is acted on colon cancer.
The content of the invention
The technical problem to be solved in the present invention is to provide the new application of wogonin, i.e., the new application in pharmacy.
The new application of above-mentioned wogonin is that wogonin is preparing the application in treating colon cancer drug, wherein described
Wogonin chemical structural formula such as following formula (I) shown in,
In above-mentioned application, described medicine is made up of wogonin and medically acceptable auxiliary material.
In above-mentioned application, described medicine is nano emulsion injection, capsule or tablet.
The effect of wogonin treatment colon cancer in application of the present invention is notable, in vitro to Growth of Colon Cancer Cells
There is very strong inhibitory action, and colon cancer cell HCT116 autophagy can be suppressed, promote Apoptosis；Chemistry is lured in vivo
Leading the growth of tumor model has good inhibitory action.
It is easy to the public to more fully understand, below by effect experiment and embodiment further illustrates the present invention
Beneficial effect.
Brief description of the drawings：
Fig. 1 is bar chart of the wogonin to colon cancer cell effect of vigor.
Fig. 2 is the electrophoretogram that wogonin suppresses colon cancer cell HCT116 autophagy.
Fig. 3 is the electrophoretogram that wogonin promotes Apoptosis of Colon Cancer Cells.
Fig. 4 is that wogonin suppresses the design sketch of its tumour growth, the figure be chemical induction colon cancer mouse model group and
The colon lengths figure of drug-treated group.
Embodiment：
Experimental example 1：Inhibitory action of the wogonin to external colon cancer cell
Take the logarithm the tumour cell in growth period, be inoculated in 4000/ hole in 96 orifice plate culture plates, overnight incubation, cell life
After long status is good, original culture medium is discarded, then according to the drug concentration of design：Wogonin 0,1,2,4,10,20,
40,80 μM act on stopping culture after HCT116 cells 72h, then add MTT (0.5mg/ml) solution in 100 μ l/ holes, handle
After 4h, supernatant is abandoned, the DMSO vibrations for being eventually adding 150 μ l are mixed, be placed in ELIASA and determine its absorbance (determining wavelength is
570nm).As a result as shown in figure 1, wogonin can substantially suppress colon cancer cell HCT116 growth.
Experimental example 2：Wogonin suppresses colon cancer cell HCT116 autophagy
Take the logarithm growth period HCT116 cells with 5 × 104Individual/hole is inoculated in 6 well culture plates, incubated overnight, treats thin
When born of the same parents' adhered state is preferable, culture medium is discarded, add the fresh culture continuation of wogonin containing various concentrations (0,5,10 μM)
Cultivate after 72h, digestion, collection cell, centrifugation, PBS are washed 2 times, are washed supernatant off, are then added appropriate RIPA and 1% albumen
After enzyme inhibitor PMSF, cell lysis 45min, collect supernatant and determine protein content, use Western blotting's
Method detects the expression of autophagy GAP-associated protein GAP.As a result as shown in Fig. 2 wogonin is acted on after HCT116 cells to suppress
The expression of its autophagy GAP-associated protein GAP.
Experimental example 3：Wogonin can promote Apoptosis of Colon Cancer Cells
Take the logarithm growth period HCT116 cells with 5 × 104Individual/hole is inoculated in 6 well culture plates, incubated overnight, treats thin
When born of the same parents' adhered state is preferable, culture medium is discarded, add the fresh culture continuation of wogonin containing various concentrations (0,5,10 μM)
Cultivate after 72h, digestion, collection cell, centrifugation, PBS are washed 2 times, are washed supernatant off, are then added appropriate RIPA and 1% albumen
After enzyme inhibitor PMSF, cell lysis 45min, collect supernatant and determine protein content, use Western blotting's
Method detects the expression of apoptosis-related protein.As a result as shown in figure 3, wogonin is acted on after HCT116 cells to promote
The expression of its apoptosis-related protein.
Experimental example 4：Wogonin plays the role of to suppress its tumour growth to the tumor model of chemical induction
Set up the animal model of chemical induction colon cancer.It is from the female C57BL/6 mouse of 4 to 6 week old, mouse is random
It is divided into 4 groups, every group 20, is respectively：1. blank control group；2. wogonin dosage administration group (50mg/kg)；3. wogonin
Dosage administration group (100mg/kg)；4. model group.Except another 3 groups of blank control group in the 5th week intraperitoneal injection AOM once, the 2nd,
3rd, 4 groups in the 6th, added in its drinking water within 9,12 weeks 2% DSS, DSS solutions for administration one week changes once for three days, replacing every time
Fresh configuration, administration group set time gastric infusion 1 time (50,100mg/kg) weekly since the 5th week, is weighed for during which every 3 days
Mouse weight 1 time, monitoring amount of drinking water, food-intake, monitors excrement index, still evaluates stool in mice according to DAI scorings, observes DSS
After reparation state after damage terminated to administration in the 25th week, mouse is put to death, takes small intestine, the heart, liver, spleen, lung, kidney, thymus gland etc. to organize
And preserve.As a result as shown in figure 4, wogonin can suppress the growth of colon cancer, the mouse Colon section of administration group is compared with model group more
Long, inflammation is lighter, with antitumor active in vivo.
Experimental example 5：The preparation example of pharmaceutical preparation
Example 1 (nano emulsion injection agent)
Wogonin 25mg is taken, with Tween-80：Medium chain triglyceride (MCT)：The mass ratio of n-butanol is 4:1：0.9 claims
It is 35mg to take gross mass, and 50 DEG C of heating water bath dissolvings obtain the solution of homogeneous transparent.Under under the conditions of the magnetic agitation, normal temperature is noted
Penetrate and the solution is added with water 100ml, emulsify 30min, form faint yellow, clear wogonin nano-emulsion.In clean ring
Under border, filtrate is potted in sterilized 2mL, 5mL ampoule by 0.22 μm of filtering with microporous membrane, draws envelope.The good Chinese of embedding is yellow
121 DEG C of nano emulsion injection of a kind of reed mentioned in ancient books element, 0.1MPa pressure sterilizing 15min, are produced.
Example 2 (from micro emulsion enteric hard wafer)
1. the preparation of sealing solution.Bone gelatin is dissolved in into 60 DEG C of water separately sodium carboxymethylcellulose is scattered in ethanol,
The two is mixed under agitation again, keeping temperature is about 50 DEG C, standby.
2. the preparation of preparation.After 24mg wogonins are mixed with Tween-80 18mg and PEG-400 6mg again with soybean
Oily 10mg mixing, while stirring by medicine liquid irrigation be loaded in hollow enteric hard capsule with the sealing solution prepared to capsule fore shaft at
Progress sealing dries at room temperature to be produced.
Example 3 (tablet)
Wogonin 40g is taken, lactose 480g, starch 1100g is added and is well mixed, with 7% starch slurry 300g as viscous
Mixture wet granulation, drying adds magnesium stearate 16g mixing, is pressed into the every 4mg containing wogonin 10000, tablet, often
Piece net weight 0.17g.
Claims (2)
1. application of the wogonin in treatment colon cancer drug is prepared, wherein the chemical structural formula of described wogonin is as follows
Shown in formula (I),
2. application according to claim 1, it is characterised in that described medicine is nano emulsion injection, capsule or piece
Agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710406070.0A CN107213146A (en) | 2017-06-02 | 2017-06-02 | Application of the wogonin in treatment colon cancer drug is prepared |
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| CN201710406070.0A CN107213146A (en) | 2017-06-02 | 2017-06-02 | Application of the wogonin in treatment colon cancer drug is prepared |
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| CN201710406070.0A Pending CN107213146A (en) | 2017-06-02 | 2017-06-02 | Application of the wogonin in treatment colon cancer drug is prepared |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111529572A (en) * | 2020-06-18 | 2020-08-14 | 山西中医药大学 | Scutellaria baicalensis extract self-microemulsion with biological antibacterial activity |
-
2017
- 2017-06-02 CN CN201710406070.0A patent/CN107213146A/en active Pending
Non-Patent Citations (1)
| Title |
|---|
| 李瑶瑶等: "汉黄芩素调控Ywhaz蛋白抑制结肠癌细胞增殖及侵袭转移", 《中国实验方剂学杂志》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111529572A (en) * | 2020-06-18 | 2020-08-14 | 山西中医药大学 | Scutellaria baicalensis extract self-microemulsion with biological antibacterial activity |
| CN111529572B (en) * | 2020-06-18 | 2023-11-24 | 山西中医药大学 | A Scutellariae radix extract self-microemulsion with biological antibacterial effect |
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Application publication date: 20170929 |