CN106420708A - Application of Linderolide H in preparation of medicine for treating skin cancer - Google Patents
Application of Linderolide H in preparation of medicine for treating skin cancer Download PDFInfo
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- CN106420708A CN106420708A CN201610803502.7A CN201610803502A CN106420708A CN 106420708 A CN106420708 A CN 106420708A CN 201610803502 A CN201610803502 A CN 201610803502A CN 106420708 A CN106420708 A CN 106420708A
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- linderolide
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- skin cancer
- medicine
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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)
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- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses application of Linderolide H in preparation of medicine for treating skin cancer, and belongs to the technical field of new medicine application. In-vitro MTT antitumor activity evaluations show that Linderolide H has a remarkable inhibiting effect on growth of human skin cancer cell strains A431, HME1, A375 and SK23. In this way, Linderolide H can be used for preparing the medicine for resisting skin cancer and has good development and application prospects. The application of Linderolide H in preparation of the medicine for treating skin cancer is first disclosed, and Linderolide H has an unexpected strong effect on inhibition of skin cancer cell activity.
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 skin cancer drug.
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.74% is had to be natural product or derivatives thereof in antitumor drug, such as Ramulus et folium taxi cuspidatae
Alcohol and its derivant are exactly the current clinically reasonable antitumor drug of application effect.Therefore, find from natural product and resist
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, this compound has brand-new framework types, has sedation (Qing
Liu,et al.,Sesquiterpene lactones from the roots of Lindera
Strychnifolia.Phytochemistry, 87 (2013) 112 118.), for Linderolide H according to the present invention
Purposes in preparation treatment skin cancer drug belongs to first public, and due to belonging to brand-new structure type, and it is for skin
The inhibitory activity of skin cancerous cell is unexpectedly strong, and there is not the possibility being provided any enlightenment by other compounds, possesses prominent
Substantive distinguishing features, the preventing and treating being simultaneously used for skin carcinoma obviously has and significantly improves.
Content of the invention
It is an object of the invention to not finding in studying according to existing Linderolide H that it has anti-skin carcinoma activity
The present situation of report, there is provided application in preparation anti-skin carcinoma medicament for the Linderolide H.
Described compound L inderolide H, structure is as shown in formula I：
The present invention finds, Linderolide H is to application on human skin JEG-3 by external MTT antineoplastic activity evaluation
The growth of A431, HME1, A375 and SK23 also has significant inhibitory action, suppresses the IC50 value of this 4 plants of cell growths respectively
For 2.58 ± 0.36 μM, 1.98 ± 0.31 μM, 1.65 ± 0.27 μM and 1.80 ± 0.21 μM.Therefore, Linderolide H can use
In preparation anti-skin carcinoma medicament, there is good development prospect.
Purposes in preparation treatment skin cancer drug for the Linderolide H according to the present invention is belonged to public first
Open, because framework types belong to brand-new framework types, and it is unexpectedly strong for the inhibitory activity of skin cancer cell,
There is not the possibility being provided any enlightenment by other compounds, possess prominent substantive distinguishing features, be simultaneously used for the anti-of skin carcinoma
Control obviously to have and significantly improve.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to concrete reality
Apply any restriction of example, but be 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 subject to concrete reality
Apply any restriction of example, but be defined in the claims.
Embodiment 1：The preparation of compound L inderolide H tablet involved in the present invention：
Take 20 g of compound Linderolide H, 180 grams of the customary adjuvant of tablet is prepared in addition, mix, conventional tablet presses
Make 1000.
Embodiment 2：The preparation of compound L inderolide H capsule involved in the present invention：
Take 20 g of compound Linderolide H, customary adjuvant such as 180 grams of the starch of capsule is prepared in addition, mix, dress
Capsule makes 1000.
To further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example：The growth inhibition effect to application on human skin JEG-3 for the compound L inderolide H is evaluated using mtt assay
1. method：It is in the cell of growth logarithmic (log) phase：Application on human skin JEG-3 A431, HME1, A375 and SK23 (buy certainly
Chinese Academy of Sciences's cell bank) with 1.5 × 104Concentration kind is in 96 orifice plates.Original culture is sucked after cell culture 24h is adherent
Base.Test is divided into blank control group, drug treating group.Blank group changes 1640 culture medium containing 10% hyclone；At medicine
Reason group is changed and is 100 μM containing concentration, 50 μM, 10 μM, 1 μM, 0.1 μM, the training of 0.01 μM and 0.001 μM of Linderolide H
Foster base.After culture 48h, add the MTT of concentration 5mg/mL, continue to be put in CO2Incubator cultivates 4h, then along culture fluid top
Suck 100 μ L of supernatant, add 100 μ L DMSO, 10min is placed in dark place, measured using microplate reader (Sunrise Products) and inhale
Light value (wavelength 570nm), and cell survival is calculated according to light absorption value, each process sets 6 repeating holes.Cell survival rate
(%)=Δ OD drug treating/Δ OD blank × 100.
2. result：Linderolide H has aobvious to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23
The inhibitory action writing.This compound suppresses application on human skin JEG-3 A431, HME1, the IC50 value of A375 and SK23 growth to be respectively
2.58 ± 0.36 μM, 1.98 ± 0.31 μM, 1.65 ± 0.27 μM and 1.80 ± 0.21 μM.
Shown by above-described embodiment, the Linderolide H of the present invention is to application on human skin JEG-3 A431, HME1, A375
Growth with SK23 has good inhibiting effect.Thus prove, the Linderolide H of the present invention has anti-skin carcinoma and lives
Property, can be used for preparing anti-skin carcinoma medicament.
Claims (1)
- Application in preparation treatment skin cancer drug for the 1.Linderolide H, described compound L inderolide H structure is such as Shown in formula I：
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610803502.7A CN106420708A (en) | 2016-09-06 | 2016-09-06 | Application of Linderolide H in preparation of medicine for treating skin cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610803502.7A CN106420708A (en) | 2016-09-06 | 2016-09-06 | Application of Linderolide H in preparation of medicine for treating skin cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106420708A true CN106420708A (en) | 2017-02-22 |
Family
ID=58164001
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610803502.7A Pending CN106420708A (en) | 2016-09-06 | 2016-09-06 | Application of Linderolide H in preparation of medicine for treating skin cancer |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106420708A (en) |
-
2016
- 2016-09-06 CN CN201610803502.7A patent/CN106420708A/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: 20170222 |