CN103405418A - Application of Chukrasone B in medicine for treating breast cancer - Google Patents
Application of Chukrasone B in medicine for treating breast cancer Download PDFInfo
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- CN103405418A CN103405418A CN2013103860965A CN201310386096A CN103405418A CN 103405418 A CN103405418 A CN 103405418A CN 2013103860965 A CN2013103860965 A CN 2013103860965A CN 201310386096 A CN201310386096 A CN 201310386096A CN 103405418 A CN103405418 A CN 103405418A
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- Prior art keywords
- chukrasone
- breast cancer
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- medicine
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- 206010006187 Breast cancer Diseases 0.000 title claims abstract description 25
- 208000026310 Breast neoplasm Diseases 0.000 title claims abstract description 25
- 229930187319 chukrasone Natural products 0.000 title claims abstract description 25
- 239000003814 drug Substances 0.000 title claims abstract description 17
- 229940079593 drug Drugs 0.000 claims abstract description 13
- 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
- 238000002360 preparation method Methods 0.000 abstract description 10
- 230000012010 growth Effects 0.000 abstract description 7
- 230000000694 effects Effects 0.000 abstract description 5
- 230000005764 inhibitory process Effects 0.000 abstract description 4
- 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
- 238000000338 in vitro Methods 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 description 9
- 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
- 230000002401 inhibitory effect Effects 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
- 201000008275 breast carcinoma Diseases 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 239000002775 capsule Substances 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
- 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
- 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
- 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 application of Chukrasone B in preparation of a medicine for treating breast cancer, and belongs to the technical field of new application of medicines. The in-vitro MTT (3-4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide) antitumor evaluation shows that Chukrasone B has remarkable inhibition effect on the growth of human breast cancer cell lines 4T1, MCF-7, MDA-MB-231 and MCF-7B, so that Chukrasone B has a good development and application prospect and can be applied to the preparation of the medicine for treating breast cancer. The application of Chukrasone B in the preparation of the medicine for treating breast cancer is disclosed for the first time; the framework type of Chukrasone B is brand new; Chukrasone B brings unexpected inhibition activity for breast cancer cells.
Description
Technical field
The present invention relates to the new purposes of Compound C hukrasone B, relate in particular to the application of Chukrasone B in preparing anti-breast cancer medicines.
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 B the present invention relates to is one and delivered (Liu in 2012, H.B.et al., 2012.Chukrasones 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 B the present invention relates in preparation treatment breast cancer medicines, belong to open first, because framework types belongs to brand-new framework types, and its inhibition for breast 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 breast carcinoma simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of Compound C hukrasone B in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Chukrasone B in preparing anti-breast cancer medicines, and the structural formula of Chukrasone B is as shown in formula I:
Formula I
The present invention finds by external MTT anti-tumor activity evaluation, and Chukrasone B also has significant inhibitory action to the growth of human breast cancer cell strain 4T1, MCF-7, MDA-MB-231 and MCF-7B, suppresses the IC of this 4 strain Growth of Cells
50Value is respectively 1.11 ± 0.19 μ M, 1.35 ± 0.16 μ M, 1.21 ± 0.15 μ M and 1.19 ± 0.16 μ M.Therefore, Chukrasone B can, for the preparation of anti-breast cancer medicines, have good development prospect.
The purposes of the Chukrasone B the present invention relates in preparation treatment breast cancer medicines belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for breast 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 breast 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 B involved in the present invention is referring to document (Liu, H.B.et al., 2012.Chukrasones 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 B tablet involved in the present invention:
Get 20 and digest compound Chukrasone B, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of Compound C hukrasone B capsule involved in the present invention:
Get 20 and digest compound Chukrasone B, 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 B to the human breast cancer cell strain
1. method: the cell that is in the growth logarithmic (log) phase: human breast cancer cell strain 4T1, MCF-7, MDA-MB-231 and MCF-7B(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 B 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 B has significant inhibitory action to the growth of human breast cancer cell strain 4T1, MCF-7, MDA-MB-231 and MCF-7B.This compound suppresses the IC of human breast cancer cell strain 4T1, MCF-7, MDA-MB-231 and MCF-7B growth
50Value is respectively: 1.11 ± 0.19 μ M, 1.35 ± 0.16 μ M, 1.21 ± 0.15 μ M and 1.19 ± 0.16 μ M.
By above-described embodiment, shown, Chukrasone B of the present invention has good inhibitory action to the growth of human breast cancer cell strain 4T1, MCF-7, MDA-MB-231 and MCF-7B.Prove thus, Chukrasone B of the present invention has the anti-breast cancer activity, can be for the preparation of anti-breast cancer medicines.
Claims (1)
1.Chukrasone B is in the application for the treatment of in breast cancer medicines, described Compound C hukrasone B structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013103860965A CN103405418A (en) | 2013-08-29 | 2013-08-29 | Application of Chukrasone B in medicine for treating breast cancer |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013103860965A CN103405418A (en) | 2013-08-29 | 2013-08-29 | Application of Chukrasone B in medicine for treating breast cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103405418A true CN103405418A (en) | 2013-11-27 |
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ID=49598493
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013103860965A Pending CN103405418A (en) | 2013-08-29 | 2013-08-29 | Application of Chukrasone B in medicine for treating breast cancer |
Country Status (1)
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| CN (1) | CN103405418A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113368113A (en) * | 2020-03-10 | 2021-09-10 | 四川大学 | Anti-tumor application of benzothiadiazoloquinazolinone compound |
-
2013
- 2013-08-29 CN CN2013103860965A patent/CN103405418A/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》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113368113A (en) * | 2020-03-10 | 2021-09-10 | 四川大学 | Anti-tumor application of benzothiadiazoloquinazolinone compound |
| CN113368113B (en) * | 2020-03-10 | 2022-04-22 | 四川大学 | Anti-tumor application of benzothiadiazoloquinazolinone compound |
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Application publication date: 20131127 |