CN103120684A - Application of Aphanamixoid A in medicine for treating endometrial carcinoma - Google Patents

Application of Aphanamixoid A in medicine for treating endometrial carcinoma Download PDF

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CN103120684A
CN103120684A CN 201210414444 CN201210414444A CN103120684A CN 103120684 A CN103120684 A CN 103120684A CN 201210414444 CN201210414444 CN 201210414444 CN 201210414444 A CN201210414444 A CN 201210414444A CN 103120684 A CN103120684 A CN 103120684A
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aphanamixoid
endometrial carcinoma
medicine
application
preparation
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李丽丽
龚霞
冯怡
吴俊华
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吴俊华
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Abstract

The invention discloses an application of Aphanamixoid A in preparation of a medicine for treating endometrial carcinoma, and belongs to the technical field of new application of the medicine. The Aphanamixoid A has outstanding inhibiting effect on the growth of human endometrial carcinoma cell strains ISK and RL95-2 through in-vitro MTT antineoplastic activity evaluation. Thus, the Aphanamixoid A can be used for preparing the medicine for resisting the endometrial carcinoma and has good development and application prospect; and the application of the Aphanamixoid A in preparation of the medicine for treating the endometrial carcinoma is firstly disclosed because a skeleton type belongs to a fire-new skeleton type and the inhibitory activity of the Aphanamixoid A on endometrial carcinoma cells is inconceivably high.

Description

The application of Aphanamixoid A in treatment endometrium cancer drug
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-endometrium cancer drug 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 of the Aphanamixoid A that the present invention relates in preparation treatment endometrium cancer drug, because framework types belongs to brand-new framework types, and its inhibition for endometrial 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 carcinoma of endometrium 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-endometrium cancer drug of preparation, and the structural formula of Aphanamixoid A is as shown in formula I:
Figure BDA0000230638561
The present invention finds by external MTT anti-tumor activity evaluation, and Aphanamixoid A also has significant inhibitory action to the growth of people's Endometrial carcinoma cell line ISK and RL95-2, suppresses the IC of this 2 strain Growth of Cells 50Value is respectively 0.15 ± 0.07 μ M and 0.19 ± 0.06 μ M.Therefore, Aphanamixoid A can for the preparation of anti-endometrium cancer drug, have good development prospect.
The purposes of the Aphanamixoid A that the present invention relates in preparation treatment endometrium cancer drug belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for endometrial 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 carcinoma of endometrium 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 people's Endometrial carcinoma cell line
1. method: the cell that is in the growth logarithmic (log) phase: people's Endometrial carcinoma cell line ISK and RL95-2(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 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: Aphanamixoid A has significant inhibitory action to the growth of people's Endometrial carcinoma cell line ISK and RL95-2.This compound suppresses the IC of people Endometrial carcinoma cell line ISK and RL95-2 growth 50Value is respectively: 0.15 ± 0.07 μ M and 0.19 ± 0.06 μ M.
Shown by above-described embodiment, Aphanamixoid A of the present invention has good inhibitory action to the growth of people's Endometrial carcinoma cell line ISK and RL95-2.Prove thus, it is active that Aphanamixoid A of the present invention has anti-carcinoma of endometrium, can be for the preparation of anti-endometrium cancer drug.

Claims (1)

1.Aphanamixoid the application of A in treatment endometrium cancer drug, described compd A phanamixoid A structure is as shown in formula I:
Figure 2012104144440100001DEST_PATH_IMAGE001
Formula I.
CN 201210414444 2012-10-25 2012-10-25 Application of Aphanamixoid A in medicine for treating endometrial carcinoma Withdrawn CN103120684A (en)

Priority Applications (1)

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CN 201210414444 CN103120684A (en) 2012-10-25 2012-10-25 Application of Aphanamixoid A in medicine for treating endometrial carcinoma

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CN103120684A true CN103120684A (en) 2013-05-29

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CN (1) CN103120684A (en)

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Application publication date: 20130529