CN102872109B - Application of Houttuynoid A in medicament for treating prostate cancer - Google Patents

Application of Houttuynoid A in medicament for treating prostate cancer Download PDF

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CN102872109B
CN102872109B CN 201210419335 CN201210419335A CN102872109B CN 102872109 B CN102872109 B CN 102872109B CN 201210419335 CN201210419335 CN 201210419335 CN 201210419335 A CN201210419335 A CN 201210419335A CN 102872109 B CN102872109 B CN 102872109B
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houttuynoid
prostate cancer
medicament
application
preparing
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CN102872109A (en
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邱翔宇
王慧
吴俊华
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Jiangsu Kangheng Chemical Co., Ltd.
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吴俊华
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Abstract

The invention discloses application of Houttuynoid A in preparing a medicament for treating prostate cancer, and belongs to the technical field of new use of medicament. Houttuynoid A is found to have an obvious inbibitional effect on the growth of human prostate cancer cell lines ALVA, gpc-1, 9L-B and Du145 through MTT (Methyl Thiazolyl Ternzolinm) anticancer activity evaluation in vitro. Therefore, Houttuynoid A can be used for preparing the anti-prostate cancer medicament and has excellent prospects in development and application. The use of Houttuynoid A in preparing the medicament for treating the prostate cancer involved in the invention is disclosed for the first time; the framework type of Houttuynoid A is a brand new framework type; and Houttuynoid A has an unexpectedly high inhibition activity for the prostate cancer cells.

Description

The application of Houttuynoid A in preparation treatment carcinoma of prostate medicine
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 preparation antiprostate 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 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 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 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 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 carcinoma of prostate medicine, because framework types belongs to brand-new framework types, and its inhibition for prostate gland cancer 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 prostate obviously has significant progress.
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 preparation antiprostate cancer, and the structural formula of Houttuynoid A is shown in formula I:
Figure BDA0000231843321
Formula I
The present invention finds that by external MTT anti-tumor activity evaluation Houttuynoid A also has significant inhibitory action to the growth of human prostate cancer cell line ALVA, gpc-1,9L-B and Du145, suppresses the IC of this 4 strain Growth of Cells 50Value is respectively 0.39 ± 0.03 μ M, 0.15 ± 0.06 μ M, 0.13 ± 0.05 μ M and 0.14 ± 0.06 μ M.Therefore, Houttuynoid A can for the preparation of antiprostate cancer, have good development prospect.
The purposes of the Houttuynoid A that the present invention relates in preparation treatment carcinoma of prostate medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for prostate gland cancer 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 prostate 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 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 mtt assay assessing compound Houttuynoid A to the growth inhibited effect of human prostate cancer cell line
1. method: the cell that is in the growth logarithmic (log) phase: human prostate cancer cell line ALVA, gpc-1,9L-B and Du145(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 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 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 A has significant inhibitory action to the growth of human prostate cancer cell line ALVA, gpc-1,9L-B and Du145.This chemical compound suppresses the IC of human prostate cancer cell line ALVA, gpc-1,9L-B and Du145 growth 50Value is respectively: 1.76 ± 0.36 μ M, 1.76 ± 0.36 μ M, 1.76 ± 0.36 μ M and 3.56 ± 0.42 μ M.
Shown that by above-described embodiment Houttuynoid A of the present invention has good inhibitory action to the growth of human prostate cancer cell line ALVA, gpc-1,9L-B and Du145.Prove that thus Houttuynoid A of the present invention has the anti-prostate cancer activity, can be for the preparation of antiprostate cancer.

Claims (1)

1.Houttuynoid the application of A in preparation treatment carcinoma of prostate medicine, described compound H outtuynoid A structure as Formula IShown in:
Figure 555554DEST_PATH_IMAGE001
Formula I.
CN 201210419335 2012-10-27 2012-10-27 Application of Houttuynoid A in medicament for treating prostate cancer Expired - Fee Related CN102872109B (en)

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Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Houttuynoids A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata;Shao-Dan Chen等;《Organic Letters》;20120313;第14卷(第7期);1772-1775 *
Shao-DanChen等.HouttuynoidsA-E Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata.《Organic Letters》.2012

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