CN103405451B - The application of Chukrasone A in preparation treatment tongue cancer drug - Google Patents
The application of Chukrasone A in preparation treatment tongue cancer drug Download PDFInfo
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- CN103405451B CN103405451B CN201310384603.1A CN201310384603A CN103405451B CN 103405451 B CN103405451 B CN 103405451B CN 201310384603 A CN201310384603 A CN 201310384603A CN 103405451 B CN103405451 B CN 103405451B
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- chukrasone
- cancer drug
- tongue cancer
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Abstract
The invention discloses the application of Chukrasone A in preparation treatment tongue cancer drug, belong to technical field of new application of medicine.The present invention is found by external MTT antineoplastic activity evaluation, and the growth of Chukrasone A to people's longue carcinoma Tca8113 and T6 also has significant inhibitory action.Therefore, Chukrasone A for the preparation of anti-tongue cancer drug, can have good development prospect.Belong to first public for the purposes of the Chukrasone A that the present invention relates in preparation treatment tongue cancer drug, because framework types belongs to brand-new framework types, and its inhibit activities for Human Tongue Carcinoma Lines is unexpectedly strong.
Description
Technical field
The present invention relates to the novelty teabag of Compound C hukrasone A, particularly relate to the application of Chukrasone A in the anti-tongue cancer drug of preparation.
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 C hukrasone A that the present invention relates to is one and delivers (Liu in 2012, H.B.et al., 2012.Chukrasone A and B:Potential Kv1.2Potassium Channel Blockers withNew 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 inhibit activities, the purposes of the Chukrasone A that the present invention relates in preparation treatment tongue cancer drug is belonged to first public, because framework types belongs to brand-new framework types, and its inhibit activities for Human Tongue Carcinoma Lines is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control simultaneously for carcinoma of tongue obviously has significant progress.
Summary of the invention
The invention provides Compound C hukrasone A and prepare the application in antitumor drug.
The present invention adopts following technical scheme: the application of Chukrasone A in the anti-tongue cancer drug of preparation, and the structural formula of Chukrasone A is as shown in formula I:
The present invention is found by external MTT antineoplastic activity evaluation, and the growth of Chukrasone A to people's longue carcinoma Tca8113 and T6 also has significant inhibitory action, suppresses the IC of this 2 strain Growth of Cells
50value is respectively 1.59 ± 0.37 μMs and 2.19 ± 0.51 μMs.Therefore, Chukrasone A for the preparation of anti-tongue cancer drug, can have good development prospect.
The purposes of the Chukrasone A that the present invention relates in preparation treatment tongue cancer drug belongs to first public, because framework types belongs to brand-new framework types, and its inhibit activities for Human Tongue Carcinoma Lines is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously for carcinoma of tongue 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 C hukrasone A involved in the present invention is see document (Liu, H.B.et al., 2012.Chukrasone A and B:Potential Kv1.2Potassium Channel Blockers with New Skeletons fromChukrasia 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 by 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 g of compound Chukrasone A, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of Compound C hukrasone A capsule involved in the present invention:
Get 20 g of compound Chukrasone A, 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 Chukrasone A to the growth inhibited effect of people's longue carcinoma
1. method: the cell being in growth logarithmic (log) phase: people's longue carcinoma Tca8113 and T6 (buying from Chinese Academy of Sciences's cell bank) is 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 Chukrasone A 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 L DMSO, 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. result: the growth of Chukrasone A to people's longue carcinoma Tca8113 and T6 has significant inhibitory action.This compound suppresses the IC of people's longue carcinoma Tca8113 and T6 growth
50value is respectively: 1.59 ± 0.37 μMs and 2.19 ± 0.51 μMs.
Shown by above-described embodiment, the growth of Chukrasone A of the present invention to people's longue carcinoma Tca8113 and T6 has good inhibitory action.Prove thus, it is active that Chukrasone A of the present invention has anti-carcinoma of tongue, can for the preparation of anti-tongue cancer drug.
Claims (1)
1.Chukrasone A preparation treatment tongue cancer drug in application, described Compound C hukrasone A structure as
formula Ishown in:
formula I
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310384603.1A CN103405451B (en) | 2013-08-29 | 2013-08-29 | The application of Chukrasone A in preparation treatment tongue cancer drug |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310384603.1A CN103405451B (en) | 2013-08-29 | 2013-08-29 | The application of Chukrasone A in preparation treatment tongue cancer drug |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103405451A CN103405451A (en) | 2013-11-27 |
| CN103405451B true CN103405451B (en) | 2015-10-07 |
Family
ID=49598525
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310384603.1A Expired - Fee Related CN103405451B (en) | 2013-08-29 | 2013-08-29 | The application of Chukrasone A in preparation treatment tongue cancer drug |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103405451B (en) |
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2013
- 2013-08-29 CN CN201310384603.1A patent/CN103405451B/en not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| Chukrasones A and B: Potential Kv1.2 Potassium Channel Blockers with New Skeletons from Chukrasia tabularis;Hong-Bing Liu等;《Org. Lett》;20121008;第14卷(第17期);4438–4441 * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN103405451A (en) | 2013-11-27 |
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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 for invention or patent application | ||
| CB03 | Change of inventor or designer information |
Inventor after: Wu Junhua Inventor after: Wang Zhongxia Inventor after: Wu Junyi Inventor after: Zhang Guang Inventor after: Huang Rong Inventor after: Wang Hui Inventor after: Jiang Chunping Inventor before: Huang Rong Inventor before: Wang Hui Inventor before: Wu Junyi Inventor before: Zhang Guang Inventor before: Jiang Chunping Inventor before: Wu Junhua |
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| COR | Change of bibliographic data |
Free format text: CORRECT: INVENTOR; FROM: HUANG RONG WANG HUI WU JUNYI ZHANG GUANG JIANG CHUNPING WU JUNHUA TO: WU JUNHUA WANG ZHONGXIA WU JUNYI ZHANG GUANG HUANG RONG WANG HUI JIANG CHUNPING |
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| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| 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: 20151007 Termination date: 20160829 |