CN103405457A - Application of Chukrasone A in medicaments for treating skin carcinoma - Google Patents
Application of Chukrasone A in medicaments for treating skin carcinoma Download PDFInfo
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- CN103405457A CN103405457A CN2013103859756A CN201310385975A CN103405457A CN 103405457 A CN103405457 A CN 103405457A CN 2013103859756 A CN2013103859756 A CN 2013103859756A CN 201310385975 A CN201310385975 A CN 201310385975A CN 103405457 A CN103405457 A CN 103405457A
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- Prior art keywords
- chukrasone
- skin carcinoma
- application
- medicaments
- treating skin
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- 201000000849 skin cancer Diseases 0.000 title claims abstract description 19
- 239000003814 drug Substances 0.000 title claims abstract description 17
- 201000008261 skin carcinoma Diseases 0.000 title claims abstract description 17
- HZUBWSRMDOJYPS-WPCVKUBSSA-N chukrasone A Natural products C=1([C@@H]2OC(=O)C[C@H]3[C@@]4(O)[C@H](O)C(=O)[C@@]5(O)[C@@H](OC(=O)C(C)C)C(C)(C)[C@@H]([C@]5([C@H]4[C@H](OC(C)=O)C[C@]32C)C)CC(=O)OC)C=COC=1 HZUBWSRMDOJYPS-WPCVKUBSSA-N 0.000 title abstract description 24
- LVTJOONKWUXEFR-FZRMHRINSA-N protoneodioscin Natural products O(C[C@@H](CC[C@]1(O)[C@H](C)[C@@H]2[C@]3(C)[C@H]([C@H]4[C@@H]([C@]5(C)C(=CC4)C[C@@H](O[C@@H]4[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@@H](O)[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@H](CO)O4)CC5)CC3)C[C@@H]2O1)C)[C@H]1[C@H](O)[C@H](O)[C@H](O)[C@@H](CO)O1 LVTJOONKWUXEFR-FZRMHRINSA-N 0.000 claims description 7
- 229930187319 chukrasone Natural products 0.000 claims 1
- 230000012010 growth Effects 0.000 abstract description 7
- 102100027833 14-3-3 protein sigma Human genes 0.000 abstract description 6
- 101100107350 Homo sapiens SFN gene Proteins 0.000 abstract description 6
- 230000002401 inhibitory effect Effects 0.000 abstract description 5
- 238000011161 development Methods 0.000 abstract description 2
- AZKSAVLVSZKNRD-UHFFFAOYSA-M 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide Chemical compound [Br-].S1C(C)=C(C)N=C1[N+]1=NC(C=2C=CC=CC=2)=NN1C1=CC=CC=C1 AZKSAVLVSZKNRD-UHFFFAOYSA-M 0.000 abstract 1
- 238000002841 anti-cancer assay Methods 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- BOLDJAUMGUJJKM-LSDHHAIUSA-N renifolin D Natural products CC(=C)[C@@H]1Cc2c(O)c(O)ccc2[C@H]1CC(=O)c3ccc(O)cc3O BOLDJAUMGUJJKM-LSDHHAIUSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 description 9
- 238000002360 preparation method Methods 0.000 description 9
- 229940079593 drug Drugs 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
- 230000000694 effects Effects 0.000 description 3
- 239000001963 growth medium Substances 0.000 description 3
- 241001156380 Chukrasia tabularis Species 0.000 description 2
- 108010087141 Kv1.2 Potassium Channel Proteins 0.000 description 2
- 102000006628 Kv1.2 Potassium Channel Human genes 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 208000000453 Skin Neoplasms 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
- 229930014626 natural product Natural products 0.000 description 2
- 239000003450 potassium channel blocker Substances 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
- 102000004257 Potassium Channel Human genes 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
- 230000000259 anti-tumor effect 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
- 238000011156 evaluation Methods 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
- 108020001213 potassium channel Proteins 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)
Abstract
The invention discloses an application of Chukrasone A in preparing medicaments for treating skin carcinoma, which belongs to the technical field of new applications of medicaments. According to the application disclosed by the invention, in-vitro MTT(3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anticancer activity evaluation finds that the Chukrasone A also has a significant inhibitory effect on the growth of human skin carcinoma cell strains A431, HME1, A375 and SK23. Therefore, the Chukrasone A can be used for preparing anti-skin carcinoma medicaments, and has a good development and application prospect. The application of Chukrasone A in preparing medicaments for treating skin carcinoma provided by the invention is disclosed for the first time, and as the skeleton type of the Chukrasone A belongs to a brand-new skeleton type, the Chukrasone A has an unexpectedly strong inhibitory activity to skin carcinoma cells.
Description
Technical field
The present invention relates to the new purposes of Compound C hukrasone A, relate in particular to the application of Chukrasone A in the anti-skin carcinoma medicine of preparation.
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, having 74% to be the natural product or derivatives thereof, is exactly the reasonable antitumor drug of effect clinically at present as paclitaxel and derivant thereof.Therefore, from searching anticancer compound or lead compound natural product, have great importance.
The Compound C hukrasone A the present invention relates to is one and delivered (Liu in 2012, H. B. et al., 2012. Chukrasone A and B:Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis. Organic Letters 14 (17), 4438 – 4441.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to potassium-channel and suppresses active, for the purposes of the Chukrasone A the present invention relates in preparation treatment skin carcinoma medicine, belong to open first, because framework types belongs to brand-new framework types, and its inhibition for skin 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 skin carcinoma simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of Compound C hukrasone A in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Chukrasone A in the anti-skin carcinoma medicine of preparation, and the structural formula of Chukrasone A is as shown in formula I:
The present invention finds by external MTT anti-tumor activity evaluation, and Chukrasone A also has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23, suppresses the IC of this 4 strain Growth of Cells
50Value is respectively 1.03 ± 0.12 μ M, 0.73 ± 0.13 μ M, 0.77 ± 0.11 μ M and 2.19 ± 0.28 μ M.Therefore, Chukrasone A can, for the preparation of anti-skin carcinoma medicine, have good development prospect.
The purposes of the Chukrasone A the present invention relates in preparation treatment skin carcinoma medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for skin 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 skin carcinoma 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 subjected to any restriction of specific embodiment, but be limited by claim.
The specific embodiment
The preparation method of Compound C hukrasone A involved in the present invention is referring to document (Liu, H. B. et al., 2012. Chukrasone A and B:Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis. Organic Letters 14 (17), 4438 – 4441.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subjected to any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of Compound C hukrasone A tablet involved in the present invention:
Get 20 and digest compound Chukrasone A, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of Compound C hukrasone A capsule involved in the present invention:
Get 20 and digest compound Chukrasone A, add the conventional adjuvant such as starch 180 grams that prepare capsule, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
Experimental example: adopt the growth inhibited effect of mtt assay assessing compound Chukrasone A to the application on human skin JEG-3
1. method: the cell that is in the growth logarithmic (log) phase: application on human skin JEG-3 A431, HME1, A375 and SK23(buy from Chinese Academy of Sciences's cell bank) with 1.5 * 10
4The concentration kind is in 96 orifice plates.After cell culture 24 h are adherent, suck original culture medium.Test is divided into blank group, drug treating group.Blank group is changed 1640 culture medium that contain 10% hyclone; It is 100 μ M that the replacing of drug treating group contains concentration, 50 μ M, 10 μ M, 1 μ M, 0.1 μ M, the culture medium of the Chukrasone A of 0.01 μ M and 0.001 μ M.After cultivating 48 h, add the MTT of concentration 5 mg/mL, continue to be put in CO
2Incubator is cultivated 4 h, then along culture fluid top, suck 100 μ L supernatants, add 100 μ L DMSO, 10 min are placed in dark place, utilize microplate reader (Sunrise company product) to measure light absorption value (wavelength 570 nm), 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: Chukrasone A has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23.This compound suppresses the IC of application on human skin JEG-3 A431, HME1, A375 and SK23 growth
50Value is respectively: 1.03 ± 0.12 μ M, 0.73 ± 0.13 μ M, 0.77 ± 0.11 μ M and 2.19 ± 0.28 μ M.
By above-described embodiment, shown, Chukrasone A of the present invention has good inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23.Prove thus, Chukrasone A of the present invention has anti-skin carcinoma activity, can be for the preparation of anti-skin carcinoma medicine.
Claims (1)
1.Chukrasone the application of A in treatment skin carcinoma medicine, described Compound C hukrasone A structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013103859756A CN103405457A (en) | 2013-08-29 | 2013-08-29 | Application of Chukrasone A in medicaments for treating skin carcinoma |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013103859756A CN103405457A (en) | 2013-08-29 | 2013-08-29 | Application of Chukrasone A in medicaments for treating skin carcinoma |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103405457A true CN103405457A (en) | 2013-11-27 |
Family
ID=49598531
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013103859756A Pending CN103405457A (en) | 2013-08-29 | 2013-08-29 | Application of Chukrasone A in medicaments for treating skin carcinoma |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103405457A (en) |
-
2013
- 2013-08-29 CN CN2013103859756A patent/CN103405457A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| LIU,H.B.ET AL.: "Chukrasone A and B:Potential Kv1.2Potassium Channel Blockers with New Skeletons from Chukrasia tabularis.", 《ORGANIC LETTERS》 * |
| 王冬艳，等: "钾离子通道作为肿瘤治疗靶点的研究", 《国外医学药学分册》 * |
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
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Application publication date: 20131127 |