CN103405453A - Application of Chukrasone A in medicaments for treating pancreatic carcinoma - Google Patents
Application of Chukrasone A in medicaments for treating pancreatic carcinoma Download PDFInfo
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- CN103405453A CN103405453A CN201310385600XA CN201310385600A CN103405453A CN 103405453 A CN103405453 A CN 103405453A CN 201310385600X A CN201310385600X A CN 201310385600XA CN 201310385600 A CN201310385600 A CN 201310385600A CN 103405453 A CN103405453 A CN 103405453A
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- Prior art keywords
- chukrasone
- pancreatic carcinoma
- application
- medicaments
- cancer
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- 239000003814 drug Substances 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
- 208000008443 pancreatic carcinoma Diseases 0.000 title abstract description 14
- 208000021045 exocrine pancreatic carcinoma Diseases 0.000 title abstract 6
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 19
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 19
- 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
- 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
- 230000002946 anti-pancreatic effect Effects 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
- 230000001093 anti-cancer Effects 0.000 description 6
- 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
- 102000006628 Kv1.2 Potassium Channel Human genes 0.000 description 2
- 108010087141 Kv1.2 Potassium Channel Proteins 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
- 229930014626 natural product Natural products 0.000 description 2
- 201000002528 pancreatic cancer Diseases 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
- 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
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Investigating Or Analysing Biological Materials (AREA)
Abstract
The invention discloses an application of Chukrasone A in preparing medicaments for treating pancreatic 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 pancreatic carcinoma cell strains PANC-1 and BXPC-3. Therefore, the Chukrasone A can be used for preparing anti-pancreatic carcinoma medicaments, and has a good development and application prospect. The application of Chukrasone A in preparing medicaments for treating pancreatic 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 pancreatic 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-cancer of pancreas 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 Kv1.2Potassium Channel Blockers with New Skeletons from Chukrasia tabularis.Organic Letters14 (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 cancer of pancreas medicine, belong to open first, because framework types belongs to brand-new framework types, and its inhibition for pancreatic 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 cancer of pancreas 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-cancer of pancreas 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 human pancreas cancer cell strain PANC-1 and BXPC-3, suppresses the IC of this 2 strain Growth of Cells
50Value is respectively 2.19 ± 0.16 μ M and 1.31 ± 0.28 μ M.Therefore, Chukrasone A can, for the preparation of anti-cancer of pancreas medicine, have good development prospect.
For the purposes of the Chukrasone A the present invention relates in preparation treatment cancer of pancreas medicine, belong to open first, because framework types belongs to brand-new framework types, and its inhibition for pancreatic 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 cancer of pancreas 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 Kv1.2Potassium Channel Blockers with New Skeletons from Chukrasia tabularis.Organic Letters14 (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 human pancreas cancer cell strain
1. method: the cell that is in the growth logarithmic (log) phase: human pancreas cancer cell strain PANC-1 and BXPC-3(buy from Chinese Academy of Sciences's cell bank) with 1.5 * 10
4The concentration kind is in 96 orifice plates.After cell culture 24h is 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 48h, add the MTT of concentration 5mg/mL, continue to be put in CO
2Incubator is cultivated 4h, then along culture fluid top, suck 100 μ L supernatants, 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: Chukrasone A has significant inhibitory action to the growth of human pancreas cancer cell strain PANC-1 and BXPC-3.This compound suppresses the IC of human pancreas cancer cell strain PANC-1 and BXPC-3 growth
50Value is respectively 2.19 ± 0.16 μ M and 1.31 ± 0.28 μ M.
By above-described embodiment, shown, Chukrasone A of the present invention has good inhibitory action to the growth of human pancreas cancer cell strain PANC-1 and BXPC-3.Prove thus, Chukrasone A of the present invention has anti-cancer of pancreas activity, can be for the preparation of anti-cancer of pancreas medicine.
Claims (1)
1.Chukrasone the application of A in treatment cancer of pancreas medicine, described Compound C hukrasone A structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310385600.XA CN103405453B (en) | 2013-08-29 | 2013-08-29 | The application of Chukrasone A in preparation treatment pancreatic cancer drug |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310385600.XA CN103405453B (en) | 2013-08-29 | 2013-08-29 | The application of Chukrasone A in preparation treatment pancreatic cancer drug |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103405453A true CN103405453A (en) | 2013-11-27 |
| CN103405453B CN103405453B (en) | 2015-10-07 |
Family
ID=49598527
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310385600.XA Active CN103405453B (en) | 2013-08-29 | 2013-08-29 | The application of Chukrasone A in preparation treatment pancreatic cancer drug |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103405453B (en) |
-
2013
- 2013-08-29 CN CN201310385600.XA patent/CN103405453B/en active Active
Non-Patent Citations (1)
| Title |
|---|
| HONG-BING LIU等: "Chukrasones A and B: Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis", 《ORG. LETT.》 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN103405453B (en) | 2015-10-07 |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C53 | Correction of patent of invention or patent application | ||
| CB03 | Change of inventor or designer information |
Inventor after: Wu Junhua Inventor after: Tao Gaojian Inventor after: Jiang Chunping Inventor after: Zhang Guang Inventor after: Wu Junyi Inventor after: Huang Rong Inventor before: Jiang Chunping Inventor before: Zhang Guang Inventor before: Wang Zezheng Inventor before: Wu Junhua |
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| COR | Change of bibliographic data |
Free format text: CORRECT: INVENTOR; FROM: JIANG CHUNPING ZHANG GUANG WANG ZEZHENG WU JUNHUA TO: WU JUNHUA TAO GAOJIAN JIANG CHUNPING ZHANG GUANG WU JUNYI HUANG RONG |
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| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant |