CN102885806B - Application of Aphanamixoid A in preparation of drug for treating laryngeal cancers - Google Patents
Application of Aphanamixoid A in preparation of drug for treating laryngeal cancers Download PDFInfo
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- CN102885806B CN102885806B CN201210412954.4A CN201210412954A CN102885806B CN 102885806 B CN102885806 B CN 102885806B CN 201210412954 A CN201210412954 A CN 201210412954A CN 102885806 B CN102885806 B CN 102885806B
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- Prior art keywords
- aphanamixoid
- drug
- preparation
- laryngeal
- application
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- 229930193702 aphanamixoid Natural products 0.000 title claims abstract description 24
- 239000003814 drug Substances 0.000 title claims abstract description 16
- 238000002360 preparation method Methods 0.000 title claims abstract description 14
- 206010023841 laryngeal neoplasm Diseases 0.000 title abstract description 14
- 229940079593 drug Drugs 0.000 title abstract description 8
- 201000005264 laryngeal carcinoma Diseases 0.000 claims description 11
- 206010023825 Laryngeal cancer Diseases 0.000 abstract description 10
- 230000012010 growth Effects 0.000 abstract description 7
- 230000002401 inhibitory effect Effects 0.000 abstract description 4
- 230000005764 inhibitory process Effects 0.000 abstract description 3
- 238000011161 development Methods 0.000 abstract description 2
- 238000011156 evaluation 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
- 230000000118 anti-neoplastic effect Effects 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 description 9
- 240000003906 Aphanamixis grandifolia Species 0.000 description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 3
- 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
- 150000002630 limonoids Chemical class 0.000 description 3
- 230000003389 potentiating effect Effects 0.000 description 3
- 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
- 230000000694 effects 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
- 230000004083 survival effect Effects 0.000 description 2
- UXFQHRONALVRMZ-UHFFFAOYSA-N CC1=CCCC2C1=CCC2 Chemical compound CC1=CCCC2C1=CCC2 UXFQHRONALVRMZ-UHFFFAOYSA-N 0.000 description 1
- 241000238631 Hexapoda Species 0.000 description 1
- 241001597008 Nomeidae Species 0.000 description 1
- 229930012538 Paclitaxel Natural products 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
- 230000001887 anti-feedant 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
- 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
- 238000012545 processing Methods 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 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
Abstract
The invention discloses application of Aphanamixoid A to preparation of a drug for treating laryngeal cancers, belonging to the technical field of novel pharmaceutical use. Through in vitro MTT (methyl thiazolyl tetrazolium) antineoplastic activity evaluation, Aphanamixoid A is found to have remarkable inhibition on growth of human laryngeal cancer cell strains HEP-2, TU686, M2e and M4e. Thus, Aphanamixoid A can be used for preparing the drug for fighting the laryngeal cancers and has excellent development and application prospects. The application of Aphanamixoid A to preparation of the drug for treating the laryngeal cancers is firstly publicized; and as a framework type belongs to a brand-new framework type, the framework type has unexpectedly strong inhibitory activity on laryngeal cancer cells.
Description
Technical field
The present invention relates to the new purposes of compd A phanamixoid A, relate in particular to the application of Aphanamixoid A in the anti-laryngeal carcinoma medicine of preparation.
Technical background
Cancer is to one of disease of human life's health hazard maximum, 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.In antitumor drug, have 74% to be natural product or derivatives thereof, if paclitaxel and derivant thereof are exactly the reasonable antitumor drug of effect clinically at present.Therefore, from natural product, find anticancer compound or lead compound has great importance.
The compd A phanamixoid A the present invention relates to is one and within 2012, delivers (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.) New skeleton compound, this compound has brand-new framework types, current purposes only relates to insect antifeedant activity (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.), purposes for the Aphanamixoid A the present invention relates in preparation treatment laryngeal carcinoma medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for laryngeal cancer cell is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control for laryngeal carcinoma simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of compd A phanamixoid A in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Aphanamixoid A in the anti-laryngeal carcinoma medicine of preparation, and the structural formula of Aphanamixoid A is as shown in formula I:
The present invention finds by the evaluation of external MTT anti-tumor activity, and Aphanamixoid A also has significant inhibitory action to the growth of people's laryngeal cancer cell strain HEP-2, TU 686, M2e and M4e, suppresses the IC of this 4 strain Growth of Cells
50value is respectively 0.53 ± 0.05 μ M, 0.23 ± 0.09 μ M, 0.32 ± 0.02 μ M and 0.19 ± 0.02 μ M.Therefore, Aphanamixoid A can, for the preparation of anti-laryngeal carcinoma medicine, have good development prospect.
The purposes of the Aphanamixoid A the present invention relates in preparation treatment laryngeal carcinoma medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for laryngeal cancer cell is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control for laryngeal 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 subject to any restriction of specific embodiment, but be limited by claim.
The specific embodiment
The preparation method of compd A phanamixoid A involved in the present invention is referring to document (Cai, J. Y. et al., 2012. Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya. Organic Letters 14 (10), 2524 – 2527.).
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 compd A phanamixoid A tablet involved in the present invention:
Get 20 and digest compound Aphanamixoid A, add 180 grams of conventional adjuvants preparing tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compd A phanamixoid A capsule involved in the present invention:
Get 20 and digest compound Aphanamixoid A, add the conventional adjuvant of preparing capsule as 180 grams of starch, 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 Aphanamixoid A to the strain of people's laryngeal cancer cell
1. method: the cell in growth logarithmic (log) phase: people's laryngeal cancer cell strain HEP-2, TU 686, M2e and M4e(buy from Chinese Academy of Sciences's cell bank) with 1.5 * 10
4concentration kind is in 96 orifice plates.After cell culture 24 h are adherent, suck original culture medium.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 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 Aphanamixoid A of 0.01 μ M and 0.001 μ M.Cultivate after 48 h, add the MTT of concentration 5 mg/mL, continue to be put in CO
2incubator is cultivated 4 h, then along culture fluid top, suck 100 μ L supernatants, add 100 μ L DMSO, 10 min are placed in dark place, utilize microplate reader (Sunrise company product) to measure light absorption value (wavelength 570nm), and calculating 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: Aphanamixoid A has significant inhibitory action to the growth of people's laryngeal cancer cell strain HEP-2, TU 686, M2e and M4e.This compound suppresses the IC of people's laryngeal cancer cell strain HEP-2, TU 686, M2e and M4e growth
50value is respectively: 0.53 ± 0.05 μ M, 0.23 ± 0.09 μ M, 0.32 ± 0.02 μ M and 0.19 ± 0.02 μ M.
By above-described embodiment, shown, Aphanamixoid A of the present invention has good inhibitory action to the growth of people's laryngeal cancer cell strain HEP-2, TU 686, M2e and M4e.Prove thus, it is active that Aphanamixoid A of the present invention has anti-laryngeal carcinoma, can be for the preparation of anti-laryngeal carcinoma medicine.
Claims (1)
- The application of 1.Aphanamixoid A in preparation treatment laryngeal carcinoma medicine, described compd A phanamixoid A structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210412954.4A CN102885806B (en) | 2012-10-25 | 2012-10-25 | Application of Aphanamixoid A in preparation of drug for treating laryngeal cancers |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210412954.4A CN102885806B (en) | 2012-10-25 | 2012-10-25 | Application of Aphanamixoid A in preparation of drug for treating laryngeal cancers |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102885806A CN102885806A (en) | 2013-01-23 |
| CN102885806B true CN102885806B (en) | 2014-04-16 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201210412954.4A Active CN102885806B (en) | 2012-10-25 | 2012-10-25 | Application of Aphanamixoid A in preparation of drug for treating laryngeal cancers |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102885806B (en) |
-
2012
- 2012-10-25 CN CN201210412954.4A patent/CN102885806B/en active Active
Non-Patent Citations (2)
| Title |
|---|
| Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya;Jie-Yun Cai,et al;《ORGANIC LETTERS》;20120427;第14卷(第10期);第2524–2527页 * |
| Jie-Yun Cai,et al.Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya.《ORGANIC LETTERS》.2012,第14卷(第10期),第2524–2527页. |
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| Publication number | Publication date |
|---|---|
| CN102885806A (en) | 2013-01-23 |
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Effective date of registration: 20141226 Address after: 226400, No. 6, Southeast River, dug Town, Rudong County, Jiangsu Patentee after: Gu Yongliang Address before: 210093 Nanjing, Gulou District, Jiangsu, No. 22 Hankou Road Patentee before: Nanjing University |