The application of Houttuynoid D in treatment endometrium cancer drug
Technical field
The present invention relates to the new purposes of compound H outtuynoid D, relate in particular to the application of Houttuynoid D 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 present reasonable antitumor drug of effect clinically such as paclitaxel and derivant thereof.Therefore, searching anticancer compound or lead compound have great importance from natural product.
The compound H outtuynoid D that the present invention relates to is one and delivered (Chen in 2012, S. D. et al., 2012. Houttuynoid D_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.) New skeleton 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 D_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 D 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 simultaneously carcinoma of endometrium obviously has significant progress.
Summary of the invention
The invention provides the application of compound H outtuynoid D in the preparation antitumor drug.
The present invention adopts following technical scheme: the application of Houttuynoid D in the anti-endometrium cancer drug of preparation, and the structural formula of Houttuynoid D is shown in formula I:
Formula I
The present invention finds by external MTT anti-tumor activity evaluation, and Houttuynoid D 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 0.19 ± 0.09 μ M and 0.23 ± 0.06 μ M.Therefore, Houttuynoid D can for the preparation of anti-endometrium cancer drug, have good development prospect.
The purposes of the Houttuynoid D 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 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 compound H outtuynoid D involved in the present invention is referring to document (Chen, S. D. et al., 2012. Houttuynoid D_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 D tablet involved in the present invention:
Get 20 and digest compound Houttuynoid D, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid D capsule involved in the present invention:
Get 20 and digest compound Houttuynoid D, 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 mtt assay assessing compound Houttuynoid D 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 Houttuynoid D 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 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: Houttuynoid D has significant inhibitory action to the growth of people's Endometrial carcinoma cell line ISK and RL95-2.This chemical compound suppresses the IC of people Endometrial carcinoma cell line ISK and RL95-2 growth
50Value is respectively: 0.19 ± 0.09 μ M and 0.23 ± 0.06 μ M.
Shown by above-described embodiment, Houttuynoid D 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 Houttuynoid D of the present invention has anti-carcinoma of endometrium, can be for the preparation of anti-endometrium cancer drug.