CN106491588A - Applications of the Linderolide H in treatment bladder cancer drug is prepared - Google Patents
Applications of the Linderolide H in treatment bladder cancer drug is prepared Download PDFInfo
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- CN106491588A CN106491588A CN201610815110.2A CN201610815110A CN106491588A CN 106491588 A CN106491588 A CN 106491588A CN 201610815110 A CN201610815110 A CN 201610815110A CN 106491588 A CN106491588 A CN 106491588A
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- Prior art keywords
- linderolide
- bladder cancer
- cancer drug
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- prepared
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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
- A61K31/365—Lactones
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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)
- Medicines Containing Plant Substances (AREA)
- Steroid Compounds (AREA)
Abstract
The invention discloses applications of the Linderolide H in treatment bladder cancer drug is prepared, belongs to technical field of new application of medicine.The present invention has found that by external MTT antineoplastic activity evaluation Linderolide H also have significant inhibitory action to the growth of human bladder cancer cell's strain T 24.Therefore, Linderolide H can be used for preparing anti-bladder cancer drug, with good development prospect.For Linderolide H according to the present invention belong to first public preparing the purposes in treatment bladder cancer drug, and which is unexpectedly strong for the inhibitory activity of transitional cell bladder carcinoma cell line.
Description
Technical field
The present invention relates to the new application of compound L inderolide H, more particularly to Linderolide H are in preparation treatment
Application in bladder cancer drug.
Background technology
Cancer is to endanger one of maximum disease to human life and health, 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 reasonable antineoplastic of application effect.Therefore, find from natural products anti-
Chemical compound for treating cancer or lead compound have great importance.
Compound L inderolide H according to the present invention be one deliver within 2014 (Qing Liu, et al.,
Sesquiterpene lactones from the roots of Lindera strychnifolia.Phytochemistry,
87 (2013) 112 118.) noval chemical compound, the compound have brand-new framework types, and current purposes is desinsection (Qing
Liu,et al.,Sesquiterpene lactones from the roots of Lindera strychnifol
Ia.Phytochemistry, 87 (2013) 112 118.), for Linderolide H according to the present invention are preparing treatment wing
Purposes in Guang cancer drug belongs to first public, and due to belonging to brand-new structure type, and which is for the suppression of transitional cell bladder carcinoma cell line
Activity processed is unexpectedly strong, and there is no the possibility for being provided any enlightenment by other compounds, possesses prominent substantive distinguishing features,
The preventing and treating for being simultaneously used for carcinoma of urinary bladder obviously has significant progress.
Content of the invention
It is an object of the invention to not finding in studying according to existing Linderolide H which has anti-bladder cancer activity
The present situation of report, there is provided applications of the Linderolide H in anti-bladder cancer drug is prepared.
Shown in the compound L inderolide H structures such as formula (I)：
By external MTT antineoplastic activity evaluation, the present invention has found that Linderol ide H are to human bladder cancer cell strain T-
24 growth also has significant inhibitory action, suppresses the IC50 values of this 1 plant of cell growth to be respectively 4.80 ± 1.45 μM.Cause
This, Linderolide H can be used for preparing anti-bladder cancer drug, with good development prospect.
For purposes of the Linderolide H according to the present invention in preparation treatment bladder cancer drug belongs to public first
Open, as framework types belong to brand-new framework types, and which is unexpectedly strong for the inhibitory activity of transitional cell bladder carcinoma cell line,
There is no the possibility that any enlightenment is provided by other compounds, possess prominent substantive distinguishing features, be simultaneously used for the anti-of carcinoma of urinary bladder
Control.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by concrete real
Any restriction of example is applied, but is defined in the claims.
Specific embodiment
The preparation method of compound L inderolide H involved in the present invention referring to document (Qing Liu, et al.,
Sesquiterpene lactones from the roots of Lindera
strychnifolia.Phytochemistry,87(2013)112–118.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by concrete real
Any restriction of example is applied, but is defined in the claims.
Embodiment 1：The preparation of compound L inderol ide H tablets involved in the present invention：
20 g of compound Linderol ide H are taken, addition prepares 180 grams of the customary adjuvant of tablet, mixed, Conventional compression
Machine makes 1000.
Embodiment 2：The preparation of compound L inderol ide H capsules involved in the present invention：
20 g of compound Linderol ide H are taken, addition prepares customary adjuvant such as 180 grams of the starch of capsule, are mixed,
Encapsulated make 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example：Compound L inderol ide H are evaluated using mtt assay to make the growth inhibition of human bladder cancer cell's strain
With
1. method：Cell in growth logarithmic phase：(purchase is from Chinese Academy of Sciences's cell for human bladder cancer cell strain T-24
Storehouse) with 1.5 × 104Concentration kind is in 96 orifice plates.Original culture medium is sucked after cell culture 24h is adherent.Test is divided into blank
Control group, drug-treated group.Blank group changes 1640 culture mediums containing 10% hyclone；Drug-treated group is changed
The culture medium of 100 μM, 50 μM, 10 μM, 1 μM, 0.1 μM, 0.01 μM and 0.001 μM of Linderolide H.After culture 48h, plus
Enter the MTT of concentration 5mg/mL, continue to be put in CO2Incubator culture 4h, sucks 100 μ L of supernatant then along nutrient solution top, plus
Enter 100 μ L DMSO, 10min is placed in dark place, light absorption value (wavelength 570nm) is determined using ELIASA (Sunrise Products),
And cell survival is calculated according to light absorption value, each process sets 6 repeating holes.At cell survival rate (%)=Δ OD medicines
Reason/Δ OD blank × 100.
2. result：Linderolide H have significant inhibitory action to the growth of human bladder cancer cell strain T-24.The change
Compound suppresses the IC50 values of human bladder cancer cell's strain T-24 growths to be respectively 4.80 ± 1.45 μM.
Shown by above-described embodiment, the Linderol ide H of the present invention have to the growth of human bladder cancer cell strain T-24
Good inhibiting effect.Thus prove, the Linderolide H of the present invention have anti-bladder cancer activity, can be used for preparing anti-wing
Guang cancer drug.
Claims (1)
- Applications of the 1.Linderolide H in treatment bladder cancer drug, the compound L inderolide H structures such as formula (I) shown in：
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610815110.2A CN106491588A (en) | 2016-09-11 | 2016-09-11 | Applications of the Linderolide H in treatment bladder cancer drug is prepared |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610815110.2A CN106491588A (en) | 2016-09-11 | 2016-09-11 | Applications of the Linderolide H in treatment bladder cancer drug is prepared |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106491588A true CN106491588A (en) | 2017-03-15 |
Family
ID=58291378
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610815110.2A Pending CN106491588A (en) | 2016-09-11 | 2016-09-11 | Applications of the Linderolide H in treatment bladder cancer drug is prepared |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106491588A (en) |
-
2016
- 2016-09-11 CN CN201610815110.2A patent/CN106491588A/en active Pending
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20170315 |