CN103127079A - Application of Aphanamixoid A in medicines curing stomach cancer - Google Patents
Application of Aphanamixoid A in medicines curing stomach cancer Download PDFInfo
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- CN103127079A CN103127079A CN2012104132301A CN201210413230A CN103127079A CN 103127079 A CN103127079 A CN 103127079A CN 2012104132301 A CN2012104132301 A CN 2012104132301A CN 201210413230 A CN201210413230 A CN 201210413230A CN 103127079 A CN103127079 A CN 103127079A
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- aphanamixoid
- stomach cancer
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Abstract
The invention discloses application of Aphanamixoid A in medicines curing stomach cancer and belongs to the medicines new use technical field. An external MTT antineoplastic activity evaluation shows that the Aphanamixoid A has evident inhibiting effect on growth of human stomach cancer cell strain HGC-27, MGC-803, BGC-823 and SGC-7901. Therefore, the Aphanamixoid A can be used for preparing stomach cancer resisting medicines, and has good development and application prospect. Due to the fact that use of the Aphanamixoid A in preparation of the medicines curing the stomach cancer is made public for the first time, and the Aphanamixoid A has an unexpectedly high stomach cancer inhibitory activity.
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-gastric cancer 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.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 treatment gastric cancer medicine that the present invention relates to, because framework types belongs to brand-new framework types, and its inhibition for stomach cancer 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 gastric cancer 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 anti-gastric cancer medicine of preparation, and the structural formula of Aphanamixoid A is as shown in formula I:
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 human stomach cancer cell line HGC-27, MGC-803, BGC-823 and SGC-7901, suppresses the IC of this 4 strain Growth of Cells
50Value is respectively 0.22 ± 0.03 μ M, 0.49 ± 0.09 μ M, 0.83 ± 0.03 μ M and 0.49 ± 0.04 μ M.Therefore, Aphanamixoid A can for the preparation of anti-gastric cancer medicine, have good development prospect.
Belong to open first for the purposes of the Aphanamixoid A that the present invention relates in preparation treatment gastric cancer medicine, because framework types belongs to brand-new framework types, and its inhibition for stomach 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 that is used for simultaneously gastric 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 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 stomach cancer cell line
1. method: the cell that is in the growth logarithmic (log) phase: human stomach cancer cell line HGC-27, MGC-803, BGC-823 and SGC-7901(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 5 mg/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 human stomach cancer cell line HGC-27, MGC-803, BGC-823 and SGC-7901.This compound suppresses the IC of human stomach cancer cell line HGC-27, MGC-803, BGC-823 and SGC-7901 growth
50Value is respectively: 0.22 ± 0.03 μ M, 0.49 ± 0.09 μ M, 0.83 ± 0.03 μ M and 0.49 ± 0.04 μ M.
Shown by above-described embodiment, Aphanamixoid A of the present invention has good inhibitory action to the growth of human stomach cancer cell line HGC-27, MGC-803, BGC-823 and SGC-7901.Prove thus, it is active that Aphanamixoid A of the present invention has anti-gastric cancer, can be for the preparation of anti-gastric cancer medicine.
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CN2012104132301A CN103127079A (en) | 2012-10-25 | 2012-10-25 | Application of Aphanamixoid A in medicines curing stomach cancer |
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CN2012104132301A CN103127079A (en) | 2012-10-25 | 2012-10-25 | Application of Aphanamixoid A in medicines curing stomach cancer |
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CN102861065A (en) * | 2012-10-27 | 2013-01-09 | 吴俊华 | Application of Houttuynoid E in medicine for treating gastric cancer |
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CN102861065A (en) * | 2012-10-27 | 2013-01-09 | 吴俊华 | Application of Houttuynoid E in medicine for treating gastric cancer |
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Application publication date: 20130605 |