CN103462973B - The application of Incarviatone A in preparation treatment lung-cancer medicament - Google Patents
The application of Incarviatone A in preparation treatment lung-cancer medicament Download PDFInfo
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- CN103462973B CN103462973B CN201310433118.9A CN201310433118A CN103462973B CN 103462973 B CN103462973 B CN 103462973B CN 201310433118 A CN201310433118 A CN 201310433118A CN 103462973 B CN103462973 B CN 103462973B
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- incarviatone
- cancer
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Abstract
Do you the invention discloses Incarviatone? the application of A in preparation treatment lung-cancer medicament, this compound shows good anti-lung cancer activity, can be used for preparing anti-lung-cancer medicament, belongs to technical field of new application of medicine.Incarviatone? A significantly can suppress the non-small cell lung cancer cell A of In vitro culture
549, 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.For the Incarviatone that the present invention relates to? the purposes of A in preparation treatment lung-cancer medicament belongs to first public, and because framework types belongs to brand-new framework types, and its inhibit activities for lung carcinoma cell is unexpectedly strong.
Description
Technical field
The present invention relates to field of antineoplastic medicaments, particularly relate to IncarviatoneA and preparing the application in antitumor drug.
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 the non-small cell lung cancer cell A of IncarviatoneA to In vitro culture by experiment
549, maxicell lung carcinoma cell NCI-H460, Lung Squamous Carcinoma Cells HTB-8 and people's lung squamous epithelium cancerous cell QG-5 have significant inhibitory action, and little on the impact of Human normal hepatocyte strain L02 and peripheral blood lymphocyte, shows obvious selectivity.
The Compound I ncarviatoneA that the present invention relates to is one and delivers (Shen in 2012, Y.H.etal., 2012.IncarviatoneA, astructurallyuniquenaturalproducthybridwithanewcarbonske letonfromIncarvilleadelavayi, anditsabsoluteconfigurationviacalculatedelectroniccircul ardichroicspectra.RSCAdvances2, 4175 – 4180.) New skeleton compound, this compound has brand-new framework types, report at present not in this compound activity, 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 IncarviatoneA anti-lung cancer activity in vitro, to provide the application of IncarviatoneA in anti-pulmonary carcinoma pharmacy
The invention provides the application of IncarviatoneA as preparation treatment lung-cancer medicament.
Described Compound I ncarviatoneA structure is as shown in formula I:
The purposes of the IncarviatoneA 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 Compound I ncarviatoneA involved in the present invention is see document (Shen, Y.H.etal., 2012.IncarviatoneA, astructurallyuniquenaturalproducthybridwithanewcarbonske letonfromIncarvilleadelavayi, anditsabsoluteconfigurationviacalculatedelectroniccircul ardichroicspectra.RSCAdvances2,4175 – 4180.).
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 Compound I ncarviatoneA tablet involved in the present invention:
Get 20 g of compound IncarviatoneA, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of Compound I ncarviatoneA capsule involved in the present invention:
Get 20 g of compound IncarviatoneA, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
The inhibited proliferation of experimental example: IncarviatoneA on the lung carcinoma cell of In vitro culture and the impact on human normal cell line
Take the logarithm lung carcinoma cell (the non-small cell lung cancer cell A of trophophase
549, maxicell lung carcinoma cell NCI-H460, Lung Squamous Carcinoma Cells HTB-8 and people's lung squamous epithelium cancerous cell QG-5) and human normal liver cell L 02 be inoculated on 96 well culture plates, 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, prepares individual cells suspension, adjust cell concentration to be 2 × 10 with the RPMI1640 containing 10% hyclone
5individual/mL, is inoculated in 96 well culture plates, every hole 100uL.After above-mentioned each culture plate cell culture 24h, experimental group adds the IncarviatoneA100uL 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.Absorbance (the A in each hole of 570nm is measured by microplate reader (BIO-RAD product)
570), average for each group, calculate suppression ratio: suppression ratio=(1-experimental group A
570/ control group A
570) × 100%.Carry out statistical analysis with SPSS13.0, and calculate IC
50.
Result: IncarviatoneA all has to above-mentioned lung carcinoma cell inhibitory action of significantly rising in value; And IncarviatoneA is to Human normal hepatocyte and peripheral blood lymphocyte inhibitory action less (table 1).Visible IncarviatoneA has obvious selective inhibitory to tumor cell.
Table 1IncarviatoneA is to tumor cell and Normocellular half-inhibition concentration
Conclusion: IncarviatoneA significantly can suppress the non-small cell lung cancer cell A of In vitro culture
549, 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 (1)
1.IncarviatoneA preparation treatment pulmonary carcinoma medicine in application, described Compound I ncarviatoneA structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310433118.9A CN103462973B (en) | 2013-09-22 | 2013-09-22 | The application of Incarviatone A in preparation treatment lung-cancer medicament |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310433118.9A CN103462973B (en) | 2013-09-22 | 2013-09-22 | The application of Incarviatone A in preparation treatment lung-cancer medicament |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103462973A CN103462973A (en) | 2013-12-25 |
| CN103462973B true CN103462973B (en) | 2016-02-17 |
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| CN201310433118.9A Expired - Fee Related CN103462973B (en) | 2013-09-22 | 2013-09-22 | The application of Incarviatone A in preparation treatment lung-cancer medicament |
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| Country | Link |
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| CN (1) | CN103462973B (en) |
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2013
- 2013-09-22 CN CN201310433118.9A patent/CN103462973B/en not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| Incarviatone A, a structurally unique natural product hybrid with a new carbon skeleton from Incarvillea delavayi, and its absolute configuration via calculated electronic circular dichroic spectra;Yun-Heng Shen等;《RSC Advances》;20120301;第2卷;4175–4180 * |
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| CN103462973A (en) | 2013-12-25 |
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| C41 | Transfer of patent application or patent right or utility model | ||
| CB03 | Change of inventor or designer information |
Inventor after: Liu Fengxia Inventor before: Jiang Chunping Inventor before: Huang Rong |
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| COR | Change of bibliographic data | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20151105 Address after: 250014, martyrs Road, Licheng District, Shandong, Ji'nan, 12, Shandong Applicant after: Liu Fengxia Address before: Metro Technology Building No. 69 Olympic Avenue in Jianye District of Nanjing city in Jiangsu province 210019 01 5 storey buildings Applicant before: Nanjing Guangkangxie Biomedical Technology Co., Ltd. |
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| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20160217 Termination date: 20160922 |