CN102861056B - Application of Houttuynoid A in endometrial cancer treatment medicine - Google Patents

Application of Houttuynoid A in endometrial cancer treatment medicine Download PDF

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CN102861056B
CN102861056B CN 201210418196 CN201210418196A CN102861056B CN 102861056 B CN102861056 B CN 102861056B CN 201210418196 CN201210418196 CN 201210418196 CN 201210418196 A CN201210418196 A CN 201210418196A CN 102861056 B CN102861056 B CN 102861056B
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houttuynoid
application
cancer treatment
endometrial cancer
treatment medicine
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CN102861056A (en
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邱翔宇
王慧
吴俊华
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Jiangsu Newhope Renewable Energy Science & Technology Co., Ltd.
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吴俊华
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Abstract

The invention relates to application of Houttuynoid A in preparing endometrial cancer treatment medicine, which belongs to the technical field of new application of the medicine. According to the assessment on the antineoplastic activity through in-vitro MTT method, Houttuynoid A has an obvious inhibiting effect on the growth of human endometrium cancer cell strains ISK and RL95-2. Therefore, Houttuynoid A can be used for preparing the endometrial cancer treatment medicine, and has a favorable development and application prospect. The application of Houttuynoid A in preparing the endometrial cancer treatment medicine, which is provided by the invention, is disclosed for the first time, and because the skeleton type belongs to brand-new skeleton type, the inhibiting activity of Houttuynoid A to endometrium cancer cells is extremely strong.

Description

The application of Houttuynoid A in treatment endometrium cancer drug
Technical field
The present invention relates to the new purposes of compound H outtuynoid A, relate in particular to the application of Houttuynoid 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 the 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 compound H outtuynoid A that the present invention relates to is one and delivered (Chen in 2012, S. D. et al., 2012. Houttuynoid A_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.) new framework compound, this chemical compound has brand-new framework types, present purposes only relates to anti-herpes simplex virus activity (Chen, S. D. et al., 2012. Houttuynoid A_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.), belong to open first for the purposes of the Houttuynoid 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 chemical compounds, possess outstanding substantive distinguishing features, the control that is used for carcinoma of endometrium simultaneously obviously has obvious improvement.
Summary of the invention
The invention provides the application of compound H outtuynoid A in the preparation antitumor drug.
The present invention adopts following technical scheme: the application of Houttuynoid A in the anti-endometrium cancer drug of preparation, and the structural formula of Houttuynoid A is shown in formula I:
Figure BDA0000231844441
The present invention finds that by external MTT anti-tumor activity evaluation the growth of the people's endometrial carcinoma cell of Houttuynoid A strain ISK and RL95-2 also has significant inhibitory effect, suppresses the IC of this 2 strain cell growth 50Value is respectively 0.15 ± 0.07 μ M and 0.19 ± 0.06 μ M.Therefore, Houttuynoid A can have the excellent development application prospect for the preparation of anti-endometrium cancer drug.
The purposes of the Houttuynoid 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 chemical compounds, possess outstanding substantive distinguishing features, the control that is used for carcinoma of endometrium simultaneously obviously has obvious improvement.
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 compound H outtuynoid A involved in the present invention is referring to document (Chen, S. D. et al., 2012. Houttuynoid A_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.).
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 compound H outtuynoid A tablet involved in the present invention:
Get 20 and digest compound Houttuynoid A, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid A capsule involved in the present invention:
Get 20 and digest compound Houttuynoid A, add conventional adjuvant such as starch 180 grams of preparation capsule, mixing is encapsulatedly made 1000.
Further specify its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: adopt the growth inhibited effect of the people's endometrial carcinoma cell of mtt assay assessing compound Houttuynoid A strain
1. method: the cell that is in the growth logarithmic (log) phase: people's endometrial carcinoma cell strain 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.Cell culture 24 h inhale adherent back and go original culture medium.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 Houttuynoid 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, inhale along culture fluid top then and remove 100 μ L supernatants, 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 according to light absorption value calculating cell survival situation, 6 repeating holes are established in each processing.Cell survival rate (%)=Δ OD Drug treating/ Δ OD Blank* 100.
2. result: the growth of the people's endometrial carcinoma cell of Houttuynoid A strain ISK and RL95-2 has significant inhibitory effect.This chemical compound suppresses the IC of people endometrial carcinoma cell strain ISK and RL95-2 growth 50Value is respectively: 0.15 ± 0.07 μ M and 0.19 ± 0.06 μ M.
Shown that by above-described embodiment the growth of Houttuynoid A of the present invention people's endometrial carcinoma cell strain ISK and RL95-2 has the good restraining effect.Prove that thus Houttuynoid A of the present invention has anti-carcinoma of endometrium activity, can be for the preparation of anti-endometrium cancer drug.

Claims (1)

1.Houttuynoid the application of A in preparation treatment endometrium cancer drug, described compound H outtuynoid A structure as Formula IShown in:
Figure 926979DEST_PATH_IMAGE001
Formula I.
CN 201210418196 2012-10-27 2012-10-27 Application of Houttuynoid A in endometrial cancer treatment medicine Expired - Fee Related CN102861056B (en)

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JPWO2004069233A1 (en) * 2003-02-04 2006-05-25 株式会社ヤクルト本社 Breast cancer resistance protein inhibitor

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