CN109925316A - A kind of drug for treating ulcerative colitis - Google Patents
A kind of drug for treating ulcerative colitis Download PDFInfo
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- CN109925316A CN109925316A CN201910235424.9A CN201910235424A CN109925316A CN 109925316 A CN109925316 A CN 109925316A CN 201910235424 A CN201910235424 A CN 201910235424A CN 109925316 A CN109925316 A CN 109925316A
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- ulcerative colitis
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Abstract
The invention discloses a kind of drug for treating ulcerative colitis, the structural formula of the drug is as follows:
Description
Technical field
The present invention relates to the drug for the treatment of colitis, especially a kind of drugs for treating ulcerative colitis.
Background technique
The treatment means of ulcerative colitis mainly have drug therapy and operative treatment.Drug therapy includes: (1) willow nitrogen sulphur
Amine pyridine, Salicylic Acid Formulations are to treat the key agents of ulcerative colitis, but its long-term treatment effects is poor；(2) cortex class
Sterol, such as dexamethasone or prednisone, however long-term hormone maintenance can not prevent ulcerative colitis from recurring；And chronic
Whether the phase can continue still is disagreed using hormone, and has certain side effect (danger that steroid medicine may will increase infection)；
(3) immunosuppressor, but its curative effect remain it is doubtful, it is also possible to will increase the risk of infection and cancer.In short, these treatments are burst at present
The drug of ulcer colitis cannot achieve the effect that prevent for a long time or treat；On the other hand, patients of ulcerative colitis into
After the treatment method that Colon and rectum of having gone is cut off entirely, patient is still to pay special attention to the nursing in life, centainly it is noted that work and rest knot
It closes, oneself can not be allowed too tired, especially some more serious patients of the state of an illness just should more lie up in time.
Summary of the invention
Based on the above issues, a kind for the treatment of is provided it is an object of the invention to overcome above-mentioned the deficiencies in the prior art place
The effective drug of ulcerative colitis.
To achieve the above object, the technical scheme adopted by the invention is as follows: a kind of drug for treating ulcerative colitis, it is special
Sign is that the structural formula of the drug (LY3009120) is as follows:
As advanced optimizing for above scheme, the dosage of the drug (LY3009120) is 20mg/KG weight.
It should be noted that as needed, the drug for the treatment of ulcerative colitis of the invention may be used also on the basis of LY3009120
To add corresponding auxiliary material, the forms such as tablet, pill or powder electuary are made.
As advanced optimizing for above scheme, the drug (LY3009120) is using intraperitoneal injection.
In conclusion the invention has the benefit that
There is significant curative effect using drug (LY3009120) treatment ulcerative colitis of the invention, including can be significant
The mitigation for inhibiting mouse weight, significantly improves the survival rate of mouse, and the mouse Colon for significantly inhibiting DSS induction shortens, significant to press down
The destruction of the mouse Colon epithelial cell barriers of DSS induction processed.
Detailed description of the invention
Fig. 1 is each group mouse weight result of variations figure in embodiment 1；
Fig. 2 is each group mouse survival rate result figure in embodiment 1；
Fig. 3 is each group mouse Colon length sequences figure in embodiment 2；
Fig. 4 is the extent of the destruction result figure of each group mouse Colon epithelial cell barriers in embodiment 3.
Specific embodiment
The present invention finds a kind of pair of ulcerative colitis with significant curative effect from the pathogenesis of ulcerative colitis
Compound L Y3009120, LY3009120 structural formula are as follows:
The compound (LY3009120) is a kind of anticarcinogen, has been applied to phase clinical trial.Present inventor's hair
Existing, the dosage of LY3009120 is 20mg/Kg mouse, when using intraperitoneal injection, has significant curative effect to ulcerative colitis,
It is embodied in the following aspects: the mitigation of mouse weight can be significantly inhibited, significantly improve the survival rate of mouse, significantly inhibit
The mouse Colon of DSS induction shortens, and significantly inhibits the destruction of the mouse Colon epithelial cell barriers of DSS induction.
To better illustrate the object, technical solutions and advantages of the present invention, below in conjunction with the drawings and specific embodiments pair
The present invention is described further.Unless otherwise instructed, the experimental method in the present invention is conventional method；Unless otherwise instructed,
Reagent concentration in the present invention is mass concentration；Unless otherwise instructed, the material in the present invention or reagent can from market or
Other open channels obtain.
1 LY3009120 of embodiment is to the DSS ulcerative colitis mouse weight variation induced and the research of survival rate
Experimental method: 22-24g male C57BL/6 mouse, be divided into 2 groups (every group of 8 mouse): (PBS contains Vehicle group
10%DMSO and 20%cyclodextrin) and LY3009120 group (20mg/Kg mice, is dissolved in PBS, containing 10%DMSO and
20%cyclodextrin).Daily feed 3%DSS (dextran sulfate sodium), and daily be injected intraperitoneally Vehicle or
LY3009120 (20mg/Kg mouse) removed DSS after seven days, continued that Vehicle or LY3009120 is injected intraperitoneally, after 3 days, no
It injects again.It weighs daily to mouse and counts dead mouse situation, test result is as illustrated in fig. 1 and 2.
Experimental result: Fig. 1 shows that LY3009120 can significantly inhibit the mitigation of mouse weight, * P < 0.05, * * P <
0.01,***P<0.001；Fig. 2 shows that LY3009120 can significantly improve the survival rate of mouse.
Influence of 2 LY3009120 of embodiment to the DSS ulcerative colitis mouse Colon length induced
Experimental method: 22-24g male C57BL/6 mouse is divided into 3 groups: control group 4, and DMSO group 4, LY3009120
Group 4.Control group feeds water daily；Vehicle and LY3009120 group feeds 3%DSS daily, and Vehicle is injected intraperitoneally daily
Or LY3009120 (20mg/Kg mouse), after seven days, DSS is removed, measures mouse Colon length.Experimental result is as shown in figure 3, knot
Fruit shows that LY3009120 can significantly inhibit the mouse Colon that DSS is induced and shorten.
Influence of 3 LY3009120 of embodiment to the DSS ulcerative colitis enterocyte barrier breakdown induced
Experimental method: 22-24g male C57BL/6 mouse is divided into 3 groups: control group 4, and DMSO group 4, LY3009120
Group 4.Control group feeds water daily；Vehicle and LY3009120 group feeds 3%DSS daily, and Vehicle is injected intraperitoneally daily
Or LY3009120 (10mg/Kg mouse) removed DSS after seven days, took colonic tissue, 4% paraformaldehyde is fixed, HE dyeing.It is real
Result is tested as shown in figure 4, Fig. 4 shows that LY3009120 can significantly inhibit the broken of the mouse Colon epithelial cell barriers of DSS induction
It is bad.
Finally it should be noted that the above embodiments are merely illustrative of the technical solutions of the present invention rather than protects to the present invention
The limitation of range, although the invention is described in detail with reference to the preferred embodiments, those skilled in the art should be managed
Solution, can with modification or equivalent replacement of the technical solution of the present invention are made, without departing from technical solution of the present invention essence and
Range.
Claims (3)
1. a kind of drug for treating ulcerative colitis, which is characterized in that the structural formula of the drug is as follows:
2. drug according to claim 1, which is characterized in that the dosage of the drug is 20mg/KG weight.
3. drug according to claim 1 or 2, which is characterized in that the drug is using intraperitoneal injection.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910235424.9A CN109925316B (en) | 2019-03-26 | 2019-03-26 | Medicine for treating ulcerative colitis |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910235424.9A CN109925316B (en) | 2019-03-26 | 2019-03-26 | Medicine for treating ulcerative colitis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN109925316A true CN109925316A (en) | 2019-06-25 |
| CN109925316B CN109925316B (en) | 2021-09-14 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201910235424.9A Active CN109925316B (en) | 2019-03-26 | 2019-03-26 | Medicine for treating ulcerative colitis |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111803618A (en) * | 2020-06-03 | 2020-10-23 | 桂林医学院附属医院 | Application of GPRP acetate in preparation of medicine for treating ulcerative colitis |
| CN116509876A (en) * | 2023-04-24 | 2023-08-01 | 大连理工大学 | Corticosteroid drug loaded polycyclodextrin-tannic acid nanoparticle as well as preparation method and application thereof |
Citations (3)
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| WO2016184999A1 (en) * | 2015-05-20 | 2016-11-24 | Pamgene Bv | Method for predicting the response of melanoma patients to targeted pharmacotherapy |
| CN109072311A (en) * | 2016-04-15 | 2018-12-21 | 豪夫迈·罗氏有限公司 | Diagnostic and therapeutic method for cancer |
| CN109223790A (en) * | 2018-09-20 | 2019-01-18 | 广州医科大学附属第二医院 | UCF-101 is preparing the purposes in Traumatic Colon treatment or prevention drug |
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2019
- 2019-03-26 CN CN201910235424.9A patent/CN109925316B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016184999A1 (en) * | 2015-05-20 | 2016-11-24 | Pamgene Bv | Method for predicting the response of melanoma patients to targeted pharmacotherapy |
| CN109072311A (en) * | 2016-04-15 | 2018-12-21 | 豪夫迈·罗氏有限公司 | Diagnostic and therapeutic method for cancer |
| CN109223790A (en) * | 2018-09-20 | 2019-01-18 | 广州医科大学附属第二医院 | UCF-101 is preparing the purposes in Traumatic Colon treatment or prevention drug |
Non-Patent Citations (1)
| Title |
|---|
| 樊新龙等: "pan—RAF抑制剂LY3009120对分化型甲状腺癌细胞增殖、侵袭和迁移", 《MODEM 0NCOLOGY》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111803618A (en) * | 2020-06-03 | 2020-10-23 | 桂林医学院附属医院 | Application of GPRP acetate in preparation of medicine for treating ulcerative colitis |
| CN111803618B (en) * | 2020-06-03 | 2023-05-05 | 桂林医学院附属医院 | Application of GPRP acetate in preparation of medicines for treating ulcerative colitis |
| CN116509876A (en) * | 2023-04-24 | 2023-08-01 | 大连理工大学 | Corticosteroid drug loaded polycyclodextrin-tannic acid nanoparticle as well as preparation method and application thereof |
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| Publication number | Publication date |
|---|---|
| CN109925316B (en) | 2021-09-14 |
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