CN105153131B - A kind of pharmaceutical composition that human glioma is treated in nursing - Google Patents
A kind of pharmaceutical composition that human glioma is treated in nursing Download PDFInfo
- Publication number
- CN105153131B CN105153131B CN201510603092.7A CN201510603092A CN105153131B CN 105153131 B CN105153131 B CN 105153131B CN 201510603092 A CN201510603092 A CN 201510603092A CN 105153131 B CN105153131 B CN 105153131B
- Authority
- CN
- China
- Prior art keywords
- human glioma
- pharmaceutical composition
- compound
- nursing
- treated
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
Abstract
The present invention relates to a kind of pharmaceutical composition that human glioma is treated in nursing, described pharmaceutical composition includes the compound and pharmaceutically acceptable carrier of effective dose, and the compound has having structure：
Description
Technical field
The present invention relates to field of medicaments, a kind of drug regimen that human glioma is treated in nursing is related in particular to
Thing.
Background technology
Glioma is also known as spongiocytoma, is the various tumours for betiding neuroderm, in the various swollen of encephalic
Most commonly seen in knurl, due to nervous system and the anatomic characteristic on head, glioma is seldom transferred to by vascular system
Its hetero-organization, majority is Brain metastases.
At present, the treatment means to neuroglial cytoma include operation, radiotherapy etc., but general curative effect is still undesirable, lead to
Cross after ocal resection tissue, the high metastatic neuroglial cytoma having can be even transferred at a distance by vascular system
Other organs, but these transfers neuroglial cytoma usually to radiotherapy, chemotherapy etc. is insensitive, thus is difficult to be uprooted, hidden
Show when suffering from.Therefore, clinically need to continually develop new effective medicine.
The content of the invention
It is an object of the invention to provide a kind of pharmaceutical composition that human glioma is treated in nursing.
In order to realize the purpose of the present invention, the present invention provides a kind of compound that human glioma is treated in nursing,
The compound has having structure：
The present invention also provides a kind of pharmaceutical composition that human glioma is treated in nursing, described pharmaceutical composition bag
Compound and pharmaceutically acceptable carrier containing effective dose, the compound have having structure：
Preferably, the pharmaceutically acceptable carrier is diluent, disintegrant, adhesive, lubricant, stabilizer or rectified
Positive agent.
Preferably, the diluent is sugar derivatives, starch derivatives or cellulose derivative.
Preferably, the diluent is lactose.
Preferably, described pharmaceutical composition is powder, fine granule, granule, capsule or tablet.
The present invention also provides compound and is preparing the purposes during the medicine of human glioma is treated in nursing, the chemical combination
Thing has having structure：
The present invention also provides compound in the external medicine for suppressing human glioma cell's U87 growth activities is prepared
Purposes, the compound has having structure：
Term " pharmaceutically acceptable " used herein refer to the biological activity that does not eliminate compound as described herein or
The material of property, such as carrier or diluent.This kind of material, which is applied to individual, does not cause undesirable biological action or not
Interacted with any component in harmful way and the composition comprising it.
Term " pharmaceutically acceptable carrier " as used herein includes any and all solvent, decentralized medium, bag
Clothing material, surfactant, antioxidant, preservative (such as antiseptic, antifungal agent), isotonic agent, absorption delaying agent, salt,
Preservative, drug stabilizing agent, adhesive, excipient, disintegrant, lubricant, sweetener, flavouring, dyestuff etc. and its combination, this
It is well-known to those skilled in the art (for example, see Remington's Pharmaceutical Sciences, 18th
Ed.Mack Printing Company,1990,pp.1289-1329).In addition to the carrier incompatible with active component, controlling
Consider to use any conventional carrier in treatment or pharmaceutical composition.
The compound of the present invention has growth inhibitory activity to human glioma cell.
Embodiment
The present invention is further illustrated below by embodiment.It should be understood that embodiments of the invention are to be used to illustrate
The present invention rather than limitation of the present invention.The present invention is belonged to according to the simple modifications that the essence of the present invention is carried out to the present invention
Claimed scope.Unless otherwise stated, the percentage in the present invention is percetage by weight.
Experimental example the compounds of this invention is in the external medicine for suppressing human glioma cell's U87 growth activities is prepared
The research of purposes
Compound has having structure in the present invention：
Test principle
Mtt assay (the micro enzyme reaction colorimetric method of tetramethyl azo azoles salt) be using analyze metabolism reduction tetramethyl azo azoles salt as
Basis.In vitro under environment, living cells can be by the effect of dehydrogenase during mitochondrial, by the MTT of yellow
The formazan of insoluble bluish violet is reduced to, and the enzyme of this in dead cell disappears, MTT is not reduced.Therefore, it is molten by determining
The change of liquid shade can reflect that (Tan Weidong, golden red, Luo Dixiang wait antineoplastics to sieve to the impacted situation of tumour cell
Choose comparison [J] research and development of natural products of mtt assay and srb assay, 1999,11 (3):17-22.).Mtt assay operation letter
Just, sensitive, repeatability and S-N ratio are good.
Cell culture
Take the logarithm the human glioma cell (U87, purchased from abundant bio tech ltd of upper Hisense) in growth period, within
RPMI-1640 nutrient solutions containing 10% (v/v) hyclone (fetal bovine serum) (agree strong instrument limited purchased from Shanghai
Company) it is diluted to 5 × 104Individual/L cell suspending liquid, is inoculated in 96 orifice plates, 100 μ L/ holes, be placed in 37 DEG C, saturated humidity,
5%CO224h is cultivated in incubator.
After the compounds of this invention is dissolved with DMSO, with the RPMI-1640 nutrient solutions (purchase containing 10% (v/v) hyclone
From Shanghai Ken Qiang Instrument Ltd.) 100,80,60,40,20,10 μ g/ml, six gradients.Above-mentioned pastille nutrient solution is added 96
In orifice plate, it is positioned in the incubator with cell culture the same terms and cultivates 48h, to be used as administration group.To add the life of same amount
Manage salt solution person as a control group.Then add MTT to dye 4 hours, OD values are determined under 570nm using ELIASA.Data analysis
Calculate in accordance with the following methods：Inhibitory rate of cell growth=[1- administration groups OD values/control group OD values] × 100%
As a result
For U87, the inhibitory rate of cell growth of 100,80,60,40,20,10 six gradients of μ g/ml is respectively 55.6%,
47.5%th, 41.9%, 36.2%, 33.1% and 30.1%.Test result indicates that, the compounds of this invention is in vitro for people's neuroglia
Matter oncocyte U87 has growth inhibiting, and toxicity test shows that toxicity is smaller, is adapted to continual exploitation to prepare new medicine
Thing.
Claims (1)
1. purposes of the compound in the external medicine for suppressing human glioma cell's U87 growth activities is prepared, its feature exists
In the compound has having structure：
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510603092.7A CN105153131B (en) | 2015-09-21 | 2015-09-21 | A kind of pharmaceutical composition that human glioma is treated in nursing |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510603092.7A CN105153131B (en) | 2015-09-21 | 2015-09-21 | A kind of pharmaceutical composition that human glioma is treated in nursing |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105153131A CN105153131A (en) | 2015-12-16 |
| CN105153131B true CN105153131B (en) | 2017-10-17 |
Family
ID=54794222
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510603092.7A Expired - Fee Related CN105153131B (en) | 2015-09-21 | 2015-09-21 | A kind of pharmaceutical composition that human glioma is treated in nursing |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105153131B (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105348270B (en) * | 2015-11-09 | 2018-01-09 | 吕显艳 | A kind of pharmaceutical composition for preventing and treating tooth body infections of dental pulp |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20080096950A1 (en) * | 2006-10-19 | 2008-04-24 | Karl Richard Gibson | Compounds Useful In Therapy |
| US20100056524A1 (en) * | 2008-04-02 | 2010-03-04 | Mciver Edward Giles | Compound |
| CN105940004B (en) * | 2014-01-29 | 2018-02-02 | 葛兰素史密斯克莱知识产权发展有限公司 | Compound |
-
2015
- 2015-09-21 CN CN201510603092.7A patent/CN105153131B/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CN105153131A (en) | 2015-12-16 |
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| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20171017 Termination date: 20180921 |