CN105412120A - Application of Epishionol in preparing drugs for treating lung cancer - Google Patents
Application of Epishionol in preparing drugs for treating lung cancer Download PDFInfo
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- CN105412120A CN105412120A CN201510908117.4A CN201510908117A CN105412120A CN 105412120 A CN105412120 A CN 105412120A CN 201510908117 A CN201510908117 A CN 201510908117A CN 105412120 A CN105412120 A CN 105412120A
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- epishionol
- lung
- lung cancer
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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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses the application of Epishionol in preparing drugs for treating lung cancer and belongs to the technical field of novel application of drugs. The compound has high anti-lung-cancer activity and can be used for preparing drugs for treating lung cancer. Epishionol can remarkably restrain in-vitro cultured non-small cell lung cancer cells A549, large cell lung cancer cells NCI-H460, lung squamous carcinoma cells HTB-8 and human lung epidermoid carcinoma cells QG-5, and has a small restraining effect on human normal hepatic cells LO2 and peripheral blood lymphocytes, and remarkable selectivity is realized. The application of Epishionol in preparing drugs for treating lung cancer is disclosed for the first time, a novel framework type is adopted, and the lung cancer cell inhibitory activity of Epishionol is surprisingly high.
Description
Technical field
The present invention relates to the novelty teabag of compd E pishionol, particularly relate to the application of Epishionol in preparation treatment lung-cancer medicament.
Background technology
Malignant tumor is the disease of serious threat human life health, and current clinical conventional chemotherapeutics, while killing tumor cell, has also damaged normal structure and cell greatly, which limits its application.Searching is efficient, the medicine of the treatment tumor of low toxicity has become the research of current cancer therapy drug direction and urgent task.Searching is efficient, low toxicity antitumor drug has been considered to a kind of effective approach.
The present invention confirms that Epishionol has significant inhibitory action to the non-small cell lung cancer cell A549 of In vitro culture, maxicell lung carcinoma cell NCI-H460, Lung Squamous Carcinoma Cells HTB-8 and people's lung squamous epithelium cancerous cell QG-5 by experiment, and little on the impact of Human normal hepatocyte strain L02 and peripheral blood lymphocyte, show obvious selectivity.
The compd E pishionol that the present invention relates to is one and delivers (Wen-BingZhou in 2013, etal., AstataricusonesA – DandAstataricusolA, FiveNewAnti-HBVShionane-TypeTriterpenesfromAstertataricu sL.f..Molecules2013, 18, 14585-14596.) noval chemical compound, this compound has brand-new framework types, current purposes suppresses hepatitis B virus (Wen-BingZhou, etal., AstataricusonesA – DandAstataricusolA, FiveNewAnti-HBVShionane-TypeTriterpenesfromAstertataricu sL.f..Molecules2013, 18, 14585-14596.), the purposes in preparation treatment lung-cancer medicament that the present invention relates to is belonged to first public, because framework types belongs to brand-new framework types, and its cytotoxicity for lung carcinoma cell is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, treatment simultaneously for pulmonary carcinoma obviously has significant progress.
Summary of the invention
The object of the invention is, by research Epishionol anti-lung cancer activity in vitro, to provide the application of Epishionol in anti-pulmonary carcinoma pharmacy
The invention provides the application of Epishionol as preparation treatment lung-cancer medicament.
Described compd E pishionol, structure is as shown in formula I:
The application of described Epishionol in treatment lung-cancer medicament, lung carcinoma cell is non-small cell non-cancerous cells, maxicell non-cancerous cells NCI-H460, Lung Squamous Carcinoma Cells HTB-8, people's lung squamous epithelium cancerous cell QG-5, normal liver cell LO2, human peripheral lymphocyte.
One treats lung-cancer medicament, and be that active component interpolation adjuvant is prepared from by Epishionol, preparation method, for getting 5 g of compound Epishionol, adds 195 grams, dextrin, and mixing, conventional tablet presses makes 1000.
One treats lung-cancer medicament, and be that active component adds adjuvant and is prepared from by Epishionol, preparation method, for getting 20 g of compound Epishionol, adds starch 195 grams, and mixing, encapsulatedly makes 1000.
The purposes of the Epishionol that the present invention relates in preparation treatment lung-cancer medicament belongs to first public, because framework types belongs to brand-new framework types, and its cytotoxicity for lung carcinoma cell is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the treatment simultaneously for pulmonary carcinoma obviously has significant progress.
Detailed description of the invention
The preparation method of compd E pishionol involved in the present invention is see document (Wen-BingZhou, etal., AstataricusonesA – DandAstataricusolA, FiveNewAnti-HBVShionane-TypeTriterpenesfromAstertataricu sL.f..Molecules2013,18,14585-14596.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compd E pishionol tablet involved in the present invention:
Get 5 g of compound Epishionol, add 195 grams, dextrin, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compd E pishionol capsule involved in the present invention:
Get 5 g of compound Epishionol, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
The inhibited proliferation of experimental example: Epishionol on the lung carcinoma cell of In vitro culture and the impact on human normal cell line
The take the logarithm lung carcinoma cell (non-small cell lung cancer cell A549, maxicell lung carcinoma cell NCI-H460, Lung Squamous Carcinoma Cells HTB-8 and people's lung squamous epithelium cancerous cell QG-5) of trophophase and human normal liver cell L 02 is inoculated on 96 well culture plates, and every hole inoculum concentration is respectively 3000 ~ 4000/100uL and 6000/100uL; Aseptic collection healthy blood donor venous blood 15mL, anticoagulant heparin, is separated mononuclearcell with Ficoll density－gradient centrifuga－tion method, individual cells suspension is prepared with the RPMI1640 containing 10% hyclone, adjust cell concentration to be 2 × 105/mL, be inoculated in 96 well culture plates, every hole 100uL.After above-mentioned each culture plate cell culture 24h, experimental group adds the Epishionol100uL of variable concentrations, and each concentration does three multiple holes; Negative control group Ensure Liquid liquid 100uL, blank control wells Ensure Liquid liquid 100uL, returns to zero for instrument.After effect different time (48h and 72h), every hole adds the MTT20uL of 5mg/mL, continues to cultivate 4h, and get rid of supernatant, every hole adds dimethyl sulfoxine 150uL.Measure the absorbance (A570) in each hole of 570nm by microplate reader (BIO-RAD product), average for each group, calculate suppression ratio: suppression ratio=(1-experimental group A570/ control group A 570) × 100%.Carry out statistical analysis with SPSS13.0, and calculate IC50.
Result: Epishionol all has to above-mentioned lung carcinoma cell inhibitory action of significantly rising in value; And Epishionol is to Human normal hepatocyte and peripheral blood lymphocyte inhibitory action less (table 1).Visible HouttuynoidC has obvious selective inhibitory to tumor cell.
Table 1Epishionol is to tumor cell and Normocellular half-inhibition concentration
Conclusion: Epishionol significantly can suppress the non-small cell lung cancer cell A549 of In vitro culture, maxicell lung carcinoma cell NCI-H460, Lung Squamous Carcinoma Cells HTB-8 and people's lung squamous epithelium cancerous cell QG-5, and less to the inhibitory action of Human normal hepatocyte LO2 and peripheral blood lymphocyte, show obvious selectivity.Therefore, can be used for treating pulmonary carcinoma.
Claims (4)
- The application of 1.Epishionol in treatment lung-cancer medicament, described compd E pishionol structure is as shown in formula I:Formula I.
- 2. the application of Epishionol in treatment lung-cancer medicament as claimed in claim 1, is characterized in that lung carcinoma cell is non-small cell non-cancerous cells, maxicell non-cancerous cells NCI-H460, Lung Squamous Carcinoma Cells HTB-8, people's lung squamous epithelium cancerous cell QG-5, normal liver cell LO2, human peripheral lymphocyte.
- 3. treat a lung-cancer medicament, it is characterized in that by Epishionol according to claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound Epishionol, adds 195 grams, dextrin, and mixing, conventional tablet presses makes 1000.
- 4. treat a lung-cancer medicament, it is characterized in that by Epishionol according to claim 1 being that active component adds adjuvant and is prepared from, preparation method, for getting 5 g of compound Epishionol, adds starch 195 grams, and mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510908117.4A CN105412120A (en) | 2015-12-10 | 2015-12-10 | Application of Epishionol in preparing drugs for treating lung cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510908117.4A CN105412120A (en) | 2015-12-10 | 2015-12-10 | Application of Epishionol in preparing drugs for treating lung cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105412120A true CN105412120A (en) | 2016-03-23 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510908117.4A Pending CN105412120A (en) | 2015-12-10 | 2015-12-10 | Application of Epishionol in preparing drugs for treating lung cancer |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105412120A (en) |
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2015
- 2015-12-10 CN CN201510908117.4A patent/CN105412120A/en active Pending
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| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160323 |
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| WD01 | Invention patent application deemed withdrawn after publication |