CN103446092B - The application of Incarviatone A in preparation treatment cervical cancer medicine - Google Patents
The application of Incarviatone A in preparation treatment cervical cancer medicine Download PDFInfo
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- CN103446092B CN103446092B CN201310432223.0A CN201310432223A CN103446092B CN 103446092 B CN103446092 B CN 103446092B CN 201310432223 A CN201310432223 A CN 201310432223A CN 103446092 B CN103446092 B CN 103446092B
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- incarviatone
- cervical cancer
- cervical carcinoma
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- human cervical
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Abstract
Do you the invention discloses Incarviatone? the application of A in preparation treatment human cervical carcinoma medicine, belongs to technical field of new application of medicine.Is the present invention found by external MTT antineoplastic activity evaluation, Incarviatone? A also has significant inhibitory action to the growth of Human cervical carcinoma cell line HeLa, HeLa229, HCE1 and CaSKi.Therefore, Incarviatone? A for the preparation of medicament for resisting cervical cancer, can have good development prospect.For the Incarviatone that the present invention relates to? the purposes of A in preparation treatment human cervical carcinoma medicine belongs to first public, and because framework types belongs to brand-new framework types, and its inhibit activities for human cervical carcinoma cell is unexpectedly strong.
Description
Technical field
The present invention relates to the novelty teabag of Compound I ncarviatoneA, particularly relate to IncarviatoneA and preparing the application in medicament for resisting cervical cancer.
Technical background
Cancer is to one of maximum disease of human life's health hazard, has a large amount of people to die from cancer every year.The research and development of cancer therapy drug are the focuses of study of pharmacy always.74% is had to be natural product or derivatives thereof in antitumor drug, if paclitaxel and derivant thereof are exactly the current reasonable antitumor drug of effect clinically.Therefore, from natural product, anticancer compound is found or lead compound has great importance.
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 of the IncarviatoneA that the present invention relates in preparation treatment cervical cancer medicine is belonged to first public, because framework types belongs to brand-new framework types, and its inhibit activities for cervical cancer cell is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control simultaneously for cervical cancer obviously has significant progress.
Summary of the invention
The invention provides Compound I ncarviatoneA and prepare the application in antitumor drug.
The present invention adopts following technical scheme: IncarviatoneA is preparing the application in medicament for resisting cervical cancer, and the structural formula of IncarviatoneA is as shown in formula I:
The present invention is found by external MTT antineoplastic activity evaluation, and IncarviatoneA also has significant inhibitory action to the growth of Human cervical carcinoma cell line HeLa, HeLa229, HCE1 and CaSKi, suppresses the IC of this 4 strain Growth of Cells
50value is respectively 1.21 ± 0.11 μMs, 1.03 ± 0.13 μMs, 1.27 ± 0.17 μMs and 1.36 ± 0.14 μMs.Therefore, IncarviatoneA for the preparation of medicament for resisting cervical cancer, can have good development prospect.
The purposes of the IncarviatoneA that the present invention relates in preparation treatment cervical cancer medicine belongs to first public, because framework types belongs to brand-new framework types, and its inhibit activities for cervical cancer cell is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously for cervical cancer obviously has significant progress.
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.
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.
Experimental example: adopt mtt assay assessing compound IncarviatoneA to the growth inhibited effect of human cervical carcinoma cell lines
1. method: the cell being in growth logarithmic (log) phase: Human cervical carcinoma cell line HeLa, HeLa229, HCE1 and CaSKi (buying from Chinese Academy of Sciences's cell bank) are with 1.5 × 10
4concentration kind is in 96 orifice plates.Original culture medium is sucked after cell culture 24h is adherent.Test is divided into blank group, drug treating group.Blank group changes 1640 culture medium containing 10% hyclone; It is 100 μMs that drug treating group is changed containing concentration, 50 μMs, 10 μMs, 1 μM, 0.1 μM, the culture medium of the IncarviatoneA of 0.01 μM and 0.001 μM.After cultivating 48h, add the MTT of concentration 5mg/mL, continue to be put in CO
2incubator cultivates 4h, then 100 μ L supernatants are sucked along culture fluid top, add 100 μ LDMSO, 10min is placed in dark place, microplate reader (Sunrise Products) is utilized to measure light absorption value (wavelength 570nm), and calculating cell survival according to light absorption value, 6 repeating holes are established in each process.Cell survival rate (%)=Δ OD
drug treating/ Δ OD
blank× 100.
2. the growth of result: IncarviatoneA to Human cervical carcinoma cell line HeLa, HeLa229, HCE1 and CaSKi has significant inhibitory action.This compound suppresses the IC of Human cervical carcinoma cell line HeLa, HeLa229, HCE1 and CaSKi growth
50value is respectively: 1.21 ± 0.11 μMs, 1.03 ± 0.13 μMs, 1.27 ± 0.17 μMs and 1.36 ± 0.14 μMs.
Shown by above-described embodiment, the growth of IncarviatoneA of the present invention to Human cervical carcinoma cell line HeLa, HeLa229, HCE1 and CaSKi has good inhibitory action.Prove thus, IncarviatoneA of the present invention has anti-cervical cancer activity, can for the preparation of medicament for resisting cervical cancer.
Claims (1)
- The application of 1.IncarviatoneA in preparation treatment cervical cancer medicine, described Compound I ncarviatoneA structure as formula Ishown in:formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310432223.0A CN103446092B (en) | 2013-09-22 | 2013-09-22 | The application of Incarviatone A in preparation treatment cervical cancer medicine |
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| CN201310432223.0A CN103446092B (en) | 2013-09-22 | 2013-09-22 | The application of Incarviatone A in preparation treatment cervical cancer medicine |
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| Publication Number | Publication Date |
|---|---|
| CN103446092A CN103446092A (en) | 2013-12-18 |
| CN103446092B true CN103446092B (en) | 2015-11-25 |
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| CN201310432223.0A Expired - Fee Related CN103446092B (en) | 2013-09-22 | 2013-09-22 | The application of Incarviatone A in preparation treatment cervical cancer medicine |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005021496A2 (en) * | 2003-08-27 | 2005-03-10 | The Trustees Of Columbia University In The City Of New York | Synthesis of derivatives of ginkgolide c |
| EP1939166A1 (en) * | 2006-12-19 | 2008-07-02 | InterMed Discovery GmbH | Plants extracts for use in brain modulation |
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2013
- 2013-09-22 CN CN201310432223.0A patent/CN103446092B/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005021496A2 (en) * | 2003-08-27 | 2005-03-10 | The Trustees Of Columbia University In The City Of New York | Synthesis of derivatives of ginkgolide c |
| EP1939166A1 (en) * | 2006-12-19 | 2008-07-02 | InterMed Discovery GmbH | Plants extracts for use in brain modulation |
Non-Patent Citations (1)
| Title |
|---|
| ncarviatone 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;Shen,Y.H.et al.,;《RSC ADVANCES2》;20121231;4175-4180 * |
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| CN103446092A (en) | 2013-12-18 |
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| C41 | Transfer of patent application or patent right or utility model | ||
| CB03 | Change of inventor or designer information |
Inventor after: Zhao Jinyan Inventor after: Wang Meixiang Inventor after: Fu Xiaoli Inventor before: Jiang Chunping Inventor before: Huang Rong |
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Effective date of registration: 20151020 Address after: 261500 Shandong city of Weifang province Gaomi City Liquan Street Town Community Old Road No. 9 Shunhe No. 3 Building 1 unit 302 room Applicant after: Zhao Jinyan 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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