CN103432116A - Application of Chukrasone B in medicament for treating tongue cancer - Google Patents
Application of Chukrasone B in medicament for treating tongue cancer Download PDFInfo
- Publication number
- CN103432116A CN103432116A CN2013103853548A CN201310385354A CN103432116A CN 103432116 A CN103432116 A CN 103432116A CN 2013103853548 A CN2013103853548 A CN 2013103853548A CN 201310385354 A CN201310385354 A CN 201310385354A CN 103432116 A CN103432116 A CN 103432116A
- Authority
- CN
- China
- Prior art keywords
- chukrasone
- application
- tongue cancer
- tongue
- 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.)
- Pending
Links
- 229930187319 chukrasone Natural products 0.000 title claims abstract description 23
- 239000003814 drug Substances 0.000 title claims abstract description 17
- 206010062129 Tongue neoplasm Diseases 0.000 title abstract 5
- 201000006134 tongue cancer Diseases 0.000 title abstract 5
- 206010043966 Tongue neoplasm malignant stage unspecified Diseases 0.000 claims description 11
- 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 11
- 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
- 238000011161 development 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
- 238000002841 anti-cancer assay Methods 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 description 9
- 208000025358 tongue carcinoma Diseases 0.000 description 8
- 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
- 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
- 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
- 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)
- Medicinal Preparation (AREA)
Abstract
The invention discloses application of Chukrasone B in preparation of medicaments for treating tongue cancer, and belongs to the technical field of novel application of medicaments. An in-vitro MTT (methyl thiazolyl tetrazolium) anticancer activity evaluation discovers that Chukrasone B has a remarkable inhibition effect on the growth of human tongue cancer cell strains Tca8113 and T6. Therefore, Chukrasone B can be used for preparing anti-tongue cancer medicaments, and has an excellent development application prospect. The application of Chukrasone B in preparation of medicament for treating tongue caner is disclosed for the first time, and the frame type belongs to a brand-new frame type, so that the inhibition activity of the Chukrasone B to tongue cancer cells is unexpectedly strong.
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 the anti-carcinoma of tongue 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, 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 C hukrasone B the present invention relates to is one and within 2012, delivers (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.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to potassium-channel and suppresses active, purposes for the Chukrasone B the present invention relates in preparation treatment carcinoma of tongue medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for Human Tongue Carcinoma Lines 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 carcinoma of tongue 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 the anti-carcinoma of tongue medicine of preparation, 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 people's Human Tongue Carcinoma Lines strain Tca8113 and T6, suppresses the IC of this 2 strain Growth of Cells
50value is respectively 1.33 ± 0.21 μ M and 2.41 ± 0.31 μ M.Therefore, Chukrasone B can, for the preparation of anti-carcinoma of tongue medicine, have good development prospect.
The purposes of the Chukrasone B the present invention relates in preparation treatment carcinoma of tongue medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for Human Tongue Carcinoma Lines 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 carcinoma of tongue 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 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 subject 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 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 Chukrasone B to the strain of people's Human Tongue Carcinoma Lines
1. method: in the cell of growth logarithmic (log) phase: people's Human Tongue Carcinoma Lines strain Tca8113 and T6(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 ChukrasoneB 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: Chukrasone B has significant inhibitory action to the growth of people's Human Tongue Carcinoma Lines strain Tca8113 and T6.This compound suppresses the IC of people Human Tongue Carcinoma Lines strain Tca8113 and T6 growth
50value is respectively: 1.33 ± 0.21 μ M and 2.41 ± 0.31 μ M.
By above-described embodiment, shown, Chukrasone B of the present invention has good inhibitory action to the growth of people's Human Tongue Carcinoma Lines strain Tca8113 and T6.Prove thus, Chukrasone B of the present invention has anti-carcinoma of tongue activity, can be for the preparation of anti-carcinoma of tongue medicine.
Claims (1)
1.Chukrasone the application of B in treatment carcinoma of tongue medicine, described Compound C hukrasone B structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013103853548A CN103432116A (en) | 2013-08-29 | 2013-08-29 | Application of Chukrasone B in medicament for treating tongue cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2013103853548A CN103432116A (en) | 2013-08-29 | 2013-08-29 | Application of Chukrasone B in medicament for treating tongue cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103432116A true CN103432116A (en) | 2013-12-11 |
Family
ID=49685903
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013103853548A Pending CN103432116A (en) | 2013-08-29 | 2013-08-29 | Application of Chukrasone B in medicament for treating tongue cancer |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103432116A (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1357311A (en) * | 2001-12-20 | 2002-07-10 | 武汉大学 | Medical application of ursolic acid |
-
2013
- 2013-08-29 CN CN2013103853548A patent/CN103432116A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1357311A (en) * | 2001-12-20 | 2002-07-10 | 武汉大学 | Medical application of ursolic acid |
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", 《ORGANIC LETTERS》, vol. 14, no. 17, 31 December 2012 (2012-12-31), pages 4438 - 4441 * |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN103432140A (en) | Application of Chukrasone A in preparation of medicaments for treating endometrial cancer | |
| CN103405418A (en) | Application of Chukrasone B in medicine for treating breast cancer | |
| CN103462960A (en) | Application of Incarviatone A in medicaments for treating prostatic cancer | |
| CN102872139B (en) | Application of Houttuynoid C in drug for treating tongue cancer | |
| CN102872142B (en) | Application of Houttuynoid D in drug for treating ovarian cancer | |
| CN103405424A (en) | Application of Chukrasone B in medicine for treating colorectal cancer | |
| CN103432116A (en) | Application of Chukrasone B in medicament for treating tongue cancer | |
| CN103432115A (en) | Application of Chukrasone B in preparation of medicaments for treating skin cancer | |
| CN103432141A (en) | Application of Chukrasone A in preparation of medicaments for treating ovarian cancer | |
| CN103462958A (en) | Application of Incarviatone A in medicaments for treating tongue cancer | |
| CN103432143A (en) | Application of Chukrasone A in preparation of medicaments for treating blindgut cancer | |
| CN103405451A (en) | Application of Chukrasone A in medicaments for treating tongue carcinoma | |
| CN103462961A (en) | Application of Incarviatone A in medicaments for treating bladder cancer | |
| CN103463056A (en) | Application of Lycojaponicumin A in drugs for treating tongue cancer | |
| CN103446101A (en) | Application of Chukrasone B in medicament for treating liver cancer | |
| CN103405421A (en) | Application of Chukrasone B in medicine for treating cervical cancer | |
| CN103463051A (en) | Application of Lycojaponicumin A in medicaments for treating nasopharyngeal cancer | |
| CN103463052A (en) | Application of Lycojaponicumin A in drugs for treating cervical cancer | |
| CN103462966A (en) | Application of Incarviatone A in medicaments for treating colorectal cancer | |
| CN103446133A (en) | Application of Lycojaponicumin B in tongue cancer treatment drug | |
| CN103479633A (en) | Application of Lycojaponicumin B in preparation of drugs for treating nasopharyngeal carcinoma | |
| CN103405414A (en) | Application of Chukrasone B in medicine for treating ileocecal cancer | |
| CN103462974A (en) | Application of Incarviatone A in medicaments for treating ovarian cancer | |
| CN103405413A (en) | Application of Chukrasone B in medicaments for treating bladder cancer | |
| CN103479632A (en) | Application of Lycojaponicumin B in preparation of drugs for treating cervical carcinoma |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20131211 |