CN102872089B - Application of Houttuynoid E in preparing medicines for treating skin cancer - Google Patents
Application of Houttuynoid E in preparing medicines for treating skin cancer Download PDFInfo
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- CN102872089B CN102872089B CN 201210418675 CN201210418675A CN102872089B CN 102872089 B CN102872089 B CN 102872089B CN 201210418675 CN201210418675 CN 201210418675 CN 201210418675 A CN201210418675 A CN 201210418675A CN 102872089 B CN102872089 B CN 102872089B
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Abstract
The invention discloses an application of Houttuynoid E in preparing medicines for treating skin cancer, and belongs to the technical field of new applications of medicines. In vitro MTT (Methyl Thiazolyl Tetrazolium) antineoplastic activity evaluation finds that Houttuynoid E has remarkable inhibition effect on the growth of human skin cancer cell lines A431, HME1, A375 and SK23, so that Houttuynoid E can be used to prepare medicines for inhibiting skin cancer and has good development application prospect. The application of Houttuynoid E in medicines for treating skin cancer is disclosed for the first time, and has extremely high inhibitory activity to skin cancer cells as the skeleton type belongs to a completely novel skeleton type.
Description
Technical field
The present invention relates to the new purposes of compound H outtuynoid E, relate in particular to the application of Houttuynoid E in the anti-skin carcinoma 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 compound H outtuynoid E that the present invention relates to is one and delivered (Chen in 2012, S. D. et al., 2012. Houttuynoid E_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.) New skeleton compound, this compound has brand-new framework types, present purposes only relates to anti-herpes simplex virus activity (Chen, S. D. et al., 2012. Houttuynoid E_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 E that the present invention relates in preparation treatment skin carcinoma medicine, because framework types belongs to brand-new framework types, and its inhibition for skin 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 skin carcinoma obviously has significant progress.
Summary of the invention
The invention provides the application of compound H outtuynoid E in the preparation antitumor drug.
The present invention adopts following technical scheme: the application of Houttuynoid E in the anti-skin carcinoma medicine of preparation, and the structural formula of Houttuynoid E is as shown in formula I:
Formula I
The present invention finds by external MTT anti-tumor activity evaluation, and Houttuynoid E also has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23, suppresses the IC of this 4 strain Growth of Cells
50Value is respectively 0.13 ± 0.02 μ M, 1.12 ± 0.03 μ M, 1.22 ± 0.07 μ M and 0.47 ± 0.06 μ M.Therefore, Houttuynoid E can for the preparation of anti-skin carcinoma medicine, have good development prospect.
The purposes of the Houttuynoid E that the present invention relates in preparation treatment skin carcinoma medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for skin 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 skin carcinoma 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 E involved in the present invention is referring to document (Chen, S. D. et al., 2012. Houttuynoid E_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 E tablet involved in the present invention:
Get 20 and digest compound Houttuynoid E, add conventional adjuvant 180 grams that prepare tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid E capsule involved in the present invention:
Get 20 and digest compound Houttuynoid E, 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 Houttuynoid E to the growth inhibited effect of application on human skin JEG-3
1. method: the cell that is in the growth logarithmic (log) phase: application on human skin JEG-3 A431, HME1, A375 and SK23(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 E 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: Houttuynoid E has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23.This compound suppresses the IC of application on human skin JEG-3 A431, HME1, A375 and SK23 growth
50Value is respectively: 0.13 ± 0.02 μ M, 1.12 ± 0.03 μ M, 1.22 ± 0.07 μ M and 0.47 ± 0.06 μ M.
Shown by above-described embodiment, Houttuynoid E of the present invention has good inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23.Prove thus, it is active that Houttuynoid E of the present invention has anti-skin carcinoma, can be for the preparation of anti-skin carcinoma medicine.
Claims (1)
1.Houttuynoid the application of E in preparation treatment skin carcinoma medicine, described compound H outtuynoid E structure as
Formula IShown in:
Formula I.
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| Application Number | Priority Date | Filing Date | Title |
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| CN 201210418675 CN102872089B (en) | 2012-10-27 | 2012-10-27 | Application of Houttuynoid E in preparing medicines for treating skin cancer |
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| CN 201210418675 CN102872089B (en) | 2012-10-27 | 2012-10-27 | Application of Houttuynoid E in preparing medicines for treating skin cancer |
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| CN102872089A CN102872089A (en) | 2013-01-16 |
| CN102872089B true CN102872089B (en) | 2013-05-15 |
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN103127080A (en) * | 2012-10-25 | 2013-06-05 | 吴俊华 | Application of Aphanamixoid A in medicines curing skin cancer |
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Non-Patent Citations (2)
| Title |
|---|
| Chen, Shao-Dan等.Houttuynoids A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata.《Organic Letters》.2012,第14卷(第7期),1772-1775. |
| Houttuynoids A-E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata;Chen, Shao-Dan等;《Organic Letters》;20120313;第14卷(第7期);1772-1775 * |
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| CN102872089A (en) | 2013-01-16 |
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