CN103120678A - Application of Aphanamixoid A in medicine for treating liver cancer - Google Patents
Application of Aphanamixoid A in medicine for treating liver cancer Download PDFInfo
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- CN103120678A CN103120678A CN2012104137004A CN201210413700A CN103120678A CN 103120678 A CN103120678 A CN 103120678A CN 2012104137004 A CN2012104137004 A CN 2012104137004A CN 201210413700 A CN201210413700 A CN 201210413700A CN 103120678 A CN103120678 A CN 103120678A
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- aphanamixoid
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Abstract
The invention discloses an application of Aphanamixoid A in preparation of a medicine for treating liver cancer, and belongs to the technical field of new application of the medicine. The Aphanamixoid A has outstanding inhibiting effect on the growth of human liver cancer cell strains HepG2, MHCC-LM3, Bel-7402 and HuH-7 through in-vitro MTT (Methyl Thiazolyl Tetrazolium) antineoplastic activity evaluation. Thus, the Aphanamixoid A can be used for preparing the medicine for resisting the liver cancer and has good development and application prospect; and the application of the Aphanamixoid A in preparing the medicine for treating the liver cancer is firstly disclosed because a skeleton type belongs to a fire-new skeleton type and the inhibitory activity of the Aphanamixoid A on liver cancer cells is inconceivably high.
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 preparation medicines resistant to liver cancer.
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.Having 74% to be the natural product or derivatives thereof in antitumor drug, is exactly the reasonable antitumor drug of effect clinically at present as paclitaxel and derivant thereof.Therefore, searching anticancer compound or lead compound have great importance from natural product.
the compd A phanamixoid A that the present invention relates to is one and delivered (Cai in 2012, 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, present 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.), belong to open first for the purposes in preparation Hepatoma therapy medicine that the present invention relates to, because framework types belongs to brand-new framework types, and its inhibition for hepatoma carcinoma cell is active unexpectedly strong, there is not the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, the control that is used for simultaneously hepatocarcinoma obviously has significant progress.
Summary of the invention
The invention provides the application of compd A phanamixoid A in the preparation antitumor drug.
The present invention adopts following technical scheme: the application of Aphanamixoid A in the preparation medicines resistant to liver cancer, and the structural formula of Aphanamixoid A is as shown in formula I:
The present invention finds by external MTT anti-tumor activity evaluation, and Aphanamixoid A also has significant inhibitory action to the growth of HepG2 cell lines, MHCC-LM3, Bel-7402 and HuH-7, suppresses the IC of this 4 strain Growth of Cells
50Value is respectively 0.29 ± 0.07 μ M, 0.49 ± 0.09 μ M, 0.44 ± 0.04 μ M and 0.22 ± 0.05 μ M.Therefore, Aphanamixoid A can for the preparation of medicines resistant to liver cancer, have good development prospect.
The present invention relates to the purposes of Aphanamixoid A in preparation Hepatoma therapy medicine and belong to open first, because framework types belongs to brand-new framework types, and its inhibition for hepatoma carcinoma 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 that is used for simultaneously hepatocarcinoma 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 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 subjected to any restriction of specific embodiment, but 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 conventional adjuvant 180 grams that prepare tablet, mixing, conventional tablet machine are 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 such as starch 180 grams that prepare capsule, mixing is encapsulatedly made 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: adopt mtt assay assessing compound Aphanamixoid A to the growth inhibited effect of human hepatoma cell strain
1. method: the cell that is in the growth logarithmic (log) phase: HepG2 cell lines, MHCC-LM3, Bel-7402 and HuH-7(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 24 h are adherent.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 Aphanamixoid A of 0.01 μ M and 0.001 μ M.After cultivating 48 h, add the MTT of concentration 5mg/mL, continue to be put in CO
2Incubator is cultivated 4 h, then suck 100 μ L supernatants along culture fluid top, add 100 μ L DMSO, 10 min are placed in the dark place, utilize microplate reader (Sunrise company product) to measure light absorption value (wavelength 570 nm), 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: Aphanamixoid A has significant inhibitory action to the growth of HepG2 cell lines, MHCC-LM3, Bel-7402 and HuH-7.This compound suppresses the IC of HepG2 cell lines, MHCC-LM3, Bel-7402 and HuH-7 growth
50Value is respectively: 0.29 ± 0.07 μ M, 0.49 ± 0.09 μ M, 0.44 ± 0.04 μ M and 0.22 ± 0.05 μ M.
Shown by above-described embodiment, Aphanamixoid A of the present invention has good inhibitory action to the growth of HepG2 cell lines, MHCC-LM3, Bel-7402 and HuH-7.Prove thus, Aphanamixoid A of the present invention has resisting liver cancer activity, can be for the preparation of medicines resistant to liver cancer.
Claims (1)
1.Aphanamixoid the application of A in the Hepatoma therapy 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 |
|---|---|---|---|
| CN2012104137004A CN103120678A (en) | 2012-10-25 | 2012-10-25 | Application of Aphanamixoid A in medicine for treating liver cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012104137004A CN103120678A (en) | 2012-10-25 | 2012-10-25 | Application of Aphanamixoid A in medicine for treating liver cancer |
Publications (1)
| Publication Number | Publication Date |
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| CN103120678A true CN103120678A (en) | 2013-05-29 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2012104137004A Pending CN103120678A (en) | 2012-10-25 | 2012-10-25 | Application of Aphanamixoid A in medicine for treating liver cancer |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105079006A (en) * | 2015-09-09 | 2015-11-25 | 刘高志 | Application of aphanalide J to preparation of drugs for treating liver cancer |
-
2012
- 2012-10-25 CN CN2012104137004A patent/CN103120678A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| CAI, J. Y. ET AL: "Aphanamixoid A, a Potent Defensive Limonoid, with a New Carbon Skeleton from Aphanamixis polystachya", 《ORGANIC LETTERS》 * |
| 夏菠等: "类柠檬苦素的生物活性研究进展", 《农业品加工 学刊》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105079006A (en) * | 2015-09-09 | 2015-11-25 | 刘高志 | Application of aphanalide J to preparation of drugs for treating liver cancer |
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Application publication date: 20130529 |