CN103462974A - Application of Incarviatone A in medicaments for treating ovarian cancer - Google Patents
Application of Incarviatone A in medicaments for treating ovarian cancer Download PDFInfo
- Publication number
- CN103462974A CN103462974A CN2013104340065A CN201310434006A CN103462974A CN 103462974 A CN103462974 A CN 103462974A CN 2013104340065 A CN2013104340065 A CN 2013104340065A CN 201310434006 A CN201310434006 A CN 201310434006A CN 103462974 A CN103462974 A CN 103462974A
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- China
- Prior art keywords
- incarviatone
- ovarian cancer
- medicaments
- application
- preparation
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 206010033128 Ovarian cancer Diseases 0.000 title claims abstract description 19
- 206010061535 Ovarian neoplasm Diseases 0.000 title claims abstract description 19
- 239000003814 drug Substances 0.000 title claims abstract description 17
- 150000001875 compounds Chemical class 0.000 claims description 17
- 238000002360 preparation method Methods 0.000 abstract description 9
- 230000012010 growth Effects 0.000 abstract description 7
- 108700024827 HOC1 Proteins 0.000 abstract description 6
- 101100178273 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) HOC1 gene Proteins 0.000 abstract description 6
- 230000002401 inhibitory effect Effects 0.000 abstract description 5
- 230000000259 anti-tumor effect Effects 0.000 abstract description 2
- 238000011161 development Methods 0.000 abstract description 2
- 238000011156 evaluation Methods 0.000 abstract description 2
- OAVCWZUKQIEFGG-UHFFFAOYSA-O 2-(5-methyl-2H-tetrazol-1-ium-1-yl)-1,3-thiazole Chemical compound CC1=NN=N[NH+]1C1=NC=CS1 OAVCWZUKQIEFGG-UHFFFAOYSA-O 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 229940079593 drug Drugs 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 229930014626 natural product Natural products 0.000 description 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- 239000002246 antineoplastic agent Substances 0.000 description 3
- 229940041181 antineoplastic drug Drugs 0.000 description 3
- 239000001963 growth medium Substances 0.000 description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 2
- 241001121991 Incarvillea delavayi Species 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 230000031700 light absorption Effects 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 238000001228 spectrum Methods 0.000 description 2
- 230000004083 survival effect Effects 0.000 description 2
- 241001597008 Nomeidae Species 0.000 description 1
- 229930012538 Paclitaxel Natural products 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 230000001464 adherent effect Effects 0.000 description 1
- 230000001093 anti-cancer Effects 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 230000010261 cell growth Effects 0.000 description 1
- 239000012531 culture fluid Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 231100000206 health hazard Toxicity 0.000 description 1
- 150000002611 lead compounds Chemical class 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000011275 oncology therapy Methods 0.000 description 1
- 229960001592 paclitaxel Drugs 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention discloses an application of Incarviatone A in preparation of medicaments for treating ovarian cancer, and belongs to the technical field of a new application of medicaments. In-vitro methyl thiazolyl tetrazolium (MTT) anti-tumor activity evaluation discovers that the Incarviatone A has a prominent inhibiting effect on growth of human ovarian cancer cell strains HO-8910, HOC1 and OVAC. Therefore, the Incarviatone A can be used for preparing anti-ovarian cancer medicaments, and has a good development and application prospect. The application of the Incarviatone A in preparation of the medicaments for treating the ovarian cancer is made public for the first time, the skeleton type is completely novel, and the Incarviatone A has an unexpectedly strong human ovarian cancer cell inhibiting activity.
Description
Technical field
The present invention relates to the new purposes of Compound I ncarviatone A, relate in particular to the application of Incarviatone A in preparing ovarian cancer resistance medicament.
Technical background
Cancer is to one of disease of human life's health hazard maximum, and annual have a large amount of people to die from cancer.The research and development of cancer therapy drug are the focuses of study of pharmacy always.In antitumor drug, have 74% to be the natural product or derivatives thereof, as paclitaxel and derivant thereof are exactly the reasonable antitumor drug of effect clinically at present.Therefore, from natural product, searching anticancer compound or lead compound have great importance.
The Compound I ncarviatone A the present invention relates to is one and within 2012, delivers (Shen, Y.H.et al., 2012.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.RSC Advances2, 4175 – 4180.) New skeleton compound, this compound has brand-new framework types, there is no at present the report about this compound activity aspect, purposes for the Incarviatone A the present invention relates in preparation treatment ovarian cancer medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for ovarian cancer cell is active unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control for ovarian cancer simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of Compound I ncarviatone A in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Incarviatone A in preparing ovarian cancer resistance medicament, and the structural formula of Incarviatone A is as shown in formula I:
The present invention finds by external MTT anti-tumor activity evaluation, and Incarviatone A also has significant inhibitory action to the growth of human oophoroma cell line HO-8910, HOC1 and OVAC, suppresses the IC of this 3 strain Growth of Cells
50value is respectively 1.21 ± 0.09 μ M, 0.39 ± 0.05 μ M and 0.54 ± 0.05 μ M.Therefore, Incarviatone A can, for the preparation of ovarian cancer resistance medicament, have good development prospect.
The purposes of the Incarviatone A the present invention relates in preparation treatment ovarian cancer medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for ovarian cancer cell is active unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control for ovarian cancer simultaneously obviously has significant progress.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
The specific embodiment
The preparation method of Compound I ncarviatone A involved in the present invention is referring to document (Shen, Y.H.et al., 2012.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.RSC Advances2,4175 – 4180.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of Compound I ncarviatone A tablet involved in the present invention:
Get 20 and digest compound Incarviatone A, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of Compound I ncarviatone A capsule involved in the present invention:
Get 20 and digest compound Incarviatone A, add the conventional adjuvant for preparing capsule as starch 180 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: adopt the growth inhibited effect of mtt assay assessing compound Incarviatone A to the human oophoroma cell line
1. method: in the cell of growth logarithmic (log) phase: human oophoroma cell line HO-8910, HOC1 and OVAC(buy from Chinese Academy of Sciences's cell bank) with 1.5 * 10
4the concentration kind is in 96 orifice plates.Suck original culture medium after cell culture 24h is adherent.Test is divided into blank group, drug treating group.Blank group is changed 1640 culture medium containing 10% hyclone; It is 100 μ M that the drug treating group is changed containing concentration, 50 μ M, 10 μ M, 1 μ M, 0.1 μ M, the culture medium of the Incarviatone A of 0.01 μ M and 0.001 μ M.After cultivating 48h, add the MTT of concentration 5mg/mL, continue to be put in CO
2incubator is cultivated 4h, then suck 100 μ L supernatants along culture fluid top, add 100 μ L DMSO, 10min is placed in dark place, utilize microplate reader (Sunrise company product) to measure light absorption value (wavelength 570nm), and calculating the cell survival situation according to light absorption value, 6 repeating holes are established in each processing.Cell survival rate (%)=Δ OD
drug treating/ Δ OD
blank* 100.
2. result: Incarviatone A has significant inhibitory action to the growth of human oophoroma cell line HO-8910, HOC1 and OVAC.This compound suppresses the IC of human oophoroma cell line HO-8910, HOC1 and OVAC growth
50value is respectively: 1.21 ± 0.09 μ M, 0.39 ± 0.05 μ M and 0.54 ± 0.05 μ M.
By above-described embodiment, shown, Incarviatone A of the present invention has good inhibitory action to the growth of human oophoroma cell line HO-8910, HOC1 and OVAC.Prove thus, Incarviatone A of the present invention has the ovarian cancer resistance activity, can be for the preparation of ovarian cancer resistance medicament.
Claims (1)
1.Incarviatone the application of A in treatment ovarian cancer medicine, described Compound I ncarviatone A structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310434006.5A CN103462974B (en) | 2013-09-22 | 2013-09-22 | The application of Incarviatone A in preparation treatment ovarian cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310434006.5A CN103462974B (en) | 2013-09-22 | 2013-09-22 | The application of Incarviatone A in preparation treatment ovarian cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103462974A true CN103462974A (en) | 2013-12-25 |
| CN103462974B CN103462974B (en) | 2015-08-19 |
Family
ID=49788172
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310434006.5A Expired - Fee Related CN103462974B (en) | 2013-09-22 | 2013-09-22 | The application of Incarviatone A in preparation treatment ovarian cancer |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103462974B (en) |
-
2013
- 2013-09-22 CN CN201310434006.5A patent/CN103462974B/en not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| SHEN Y.H.ET AL: ""Incarviatone A,astructurally unique natural product hybrid with a new carbon skeleton from Incarvillea delavayi,and its absolute configuration via calculated electronic circular dichroic spectra"", 《RSC ADVANCES 2》, 31 December 2012 (2012-12-31), pages 4175 - 4180 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN103462974B (en) | 2015-08-19 |
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| C06 | Publication | ||
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| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CP02 | Change in the address of a patent holder |
Address after: Tiefu iron rich street Pizhou city 221331 Jiangsu city of Xuzhou Province Patentee after: Nanjing Guangkangxie Biomedical Technology Co., Ltd. Address before: Metro Technology Building No. 69 Olympic Avenue in Jianye District of Nanjing city in Jiangsu province 210019 01 5 storey buildings Patentee before: Nanjing Guangkangxie Biomedical Technology Co., Ltd. |
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| CP02 | Change in the address of a patent holder | ||
| CB03 | Change of inventor or designer information | ||
| CB03 | Change of inventor or designer information |
Inventor after: Lu Hongxian Inventor before: Jiang Chunping Inventor before: Huang Rong |
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| TR01 | Transfer of patent right | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20171218 Address after: 535000 the Guangxi Zhuang Autonomous Region, Qinzhou, Qinnan District Building Street, No. 9 Patentee after: Qinzhou Industry Research Institute Address before: Tiefu iron rich street Pizhou city 221331 Jiangsu city of Xuzhou Province Patentee before: Nanjing Guangkangxie Biomedical Technology Co., Ltd. |
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| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20150819 Termination date: 20180922 |