CN103405421B - Application of Chukrasone B in medicine for treating cervical cancer - Google Patents
Application of Chukrasone B in medicine for treating cervical cancer Download PDFInfo
- Publication number
- CN103405421B CN103405421B CN201310386099.9A CN201310386099A CN103405421B CN 103405421 B CN103405421 B CN 103405421B CN 201310386099 A CN201310386099 A CN 201310386099A CN 103405421 B CN103405421 B CN 103405421B
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- CN
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- Prior art keywords
- chukrasone
- cervical cancer
- application
- medicine
- human cervical
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- 229930187319 chukrasone Natural products 0.000 title claims abstract description 25
- 206010008342 Cervix carcinoma Diseases 0.000 title claims abstract description 18
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 title claims abstract description 18
- 201000010881 cervical cancer Diseases 0.000 title claims abstract description 18
- 239000003814 drug Substances 0.000 title claims abstract description 17
- 238000002360 preparation method Methods 0.000 claims abstract description 12
- 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
- 230000000694 effects Effects 0.000 abstract description 8
- 230000012010 growth Effects 0.000 abstract description 7
- 101000963221 Homo sapiens mRNA guanylyltransferase Proteins 0.000 abstract description 6
- 102100039604 mRNA guanylyltransferase Human genes 0.000 abstract description 6
- 229940079593 drug Drugs 0.000 abstract description 5
- 238000011161 development Methods 0.000 abstract description 2
- 238000011156 evaluation Methods 0.000 abstract description 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 abstract 1
- 230000000259 anti-tumor effect Effects 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 208000025848 malignant tumor of nasopharynx Diseases 0.000 abstract 1
- 201000011216 nasopharynx carcinoma Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 description 9
- 208000019065 cervical carcinoma Diseases 0.000 description 6
- 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
- 238000000034 method Methods 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
- 230000000118 anti-neoplastic 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
- 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
- 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
- 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
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses application of Chukrasone B in preparation of a medicine for treating human cervical 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 activity evaluation shows that Chukrasone B has remarkable inhibition effect on the growth of human cervical cancer cell lines HeLa, HeLa229, HCE1 and CaSKi, so that Chukrasone B has a good development and application prospect and can be applied to the preparation of the medicine for treating nasopharynx cancer. The application of Chukrasone B in the preparation of the medicine for treating human cervical cancer is disclosed for the first time; the framework type of Chukrasone B is brand new; Chukrasone B brings unexpected inhibition activity for human cervical cancer cells.
Description
Technical field
The present invention relates to the novelty teabag of Compound C hukrasone B, particularly relate to Chukrasone B and preparing the application in medicament for resisting cervical cancer.
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 B that the present invention relates to is one and delivers (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 inhibit activities, the purposes of the Chukrasone B that the present invention relates in preparation treatment cervical cancer medicine is belonged to first public, because framework types belongs to brand-new framework types, and its inhibit activities for cervical cancer cell is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control simultaneously for cervical cancer obviously has significant progress.
Summary of the invention
The invention provides Compound C hukrasone B and prepare the application in antitumor drug.
The present invention adopts following technical scheme: Chukrasone B is preparing the application in medicament for resisting cervical cancer, and the structural formula of Chukrasone B is as shown in formula I:
The present invention is found by external MTT antineoplastic activity evaluation, and Chukrasone B also has significant inhibitory action to the growth of Human cervical carcinoma cell line HeLa, HeLa229, HCE1 and CaSKi, suppresses the IC of this 4 strain Growth of Cells
50value is respectively 0.67 ± 0.12 μM, 0.23 ± 0.02 μM, 0.72 ± 0.09 μM and 1.17 ± 0.16 μMs.Therefore, Chukrasone B for the preparation of medicament for resisting cervical cancer, can have good development prospect.
The purposes of the Chukrasone B that the present invention relates in preparation treatment cervical cancer medicine belongs to first public, because framework types belongs to brand-new framework types, and its inhibit activities for cervical cancer cell is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously for cervical cancer 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 B involved in the present invention is see 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 by 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 g of compound Chukrasone B, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of Compound C hukrasone B capsule involved in the present invention:
Get 20 g of compound Chukrasone B, 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 B to the growth inhibited effect of human cervical carcinoma cell lines
1. method: the cell being in growth logarithmic (log) phase: Human cervical carcinoma cell line HeLa, HeLa229, HCE1 and CaSKi(are bought from Chinese Academy of Sciences's cell bank) 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 B 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 B to Human cervical carcinoma cell line HeLa, HeLa229, HCE1 and CaSKi has significant inhibitory action.This compound suppresses the IC of Human cervical carcinoma cell line HeLa, HeLa229, HCE1 and CaSKi growth
50value is respectively: 0.67 ± 0.12 μM, 0.23 ± 0.02 μM, 0.72 ± 0.09 μM and 1.17 ± 0.16 μMs.
Shown by above-described embodiment, the growth of Chukrasone B of the present invention to Human cervical carcinoma cell line HeLa, HeLa229, HCE1 and CaSKi has good inhibitory action.Prove thus, Chukrasone B of the present invention has anti-cervical cancer activity, can for the preparation of medicament for resisting cervical cancer.
Claims (1)
- The application of 1.Chukrasone B in preparation treatment cervical cancer medicine, described Compound C hukrasone B structure as formula Ishown in:formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310386099.9A CN103405421B (en) | 2013-08-29 | 2013-08-29 | Application of Chukrasone B in medicine for treating cervical cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310386099.9A CN103405421B (en) | 2013-08-29 | 2013-08-29 | Application of Chukrasone B in medicine for treating cervical cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103405421A CN103405421A (en) | 2013-11-27 |
| CN103405421B true CN103405421B (en) | 2015-04-29 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310386099.9A Expired - Fee Related CN103405421B (en) | 2013-08-29 | 2013-08-29 | Application of Chukrasone B in medicine for treating cervical cancer |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103405421B (en) |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1759833A (en) * | 2005-09-30 | 2006-04-19 | 青岛大学 | Application of indole-2,3-diketone in preparing medication for antivirus or immunopotenfiator |
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2013
- 2013-08-29 CN CN201310386099.9A patent/CN103405421B/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1759833A (en) * | 2005-09-30 | 2006-04-19 | 青岛大学 | Application of indole-2,3-diketone in preparing medication for antivirus or immunopotenfiator |
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| Publication number | Publication date |
|---|---|
| CN103405421A (en) | 2013-11-27 |
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| CB03 | Change of inventor or designer information |
Inventor after: Wu Junhua Inventor after: Cao Yin Inventor after: Wang Hui Inventor after: Wang Zezheng Inventor after: Wu Junyi Inventor after: Zhang Guang Inventor after: Jiang Chunping Inventor before: Wang Hui Inventor before: Wang Zezheng 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: WANG HUI WANG ZEZHENG WU JUNYI ZHANG GUANG JIANG CHUNPING WU JUNHUA TO: WU JUNHUA CAO YIN WANG HUI WANG ZEZHENG WU JUNYI ZHANG GUANG JIANG CHUNPING |
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