CN102872077B - Application of Houttuynoid B in drugs for treating endometrial cancer - Google Patents
Application of Houttuynoid B in drugs for treating endometrial cancer Download PDFInfo
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- CN102872077B CN102872077B CN 201210417498 CN201210417498A CN102872077B CN 102872077 B CN102872077 B CN 102872077B CN 201210417498 CN201210417498 CN 201210417498 CN 201210417498 A CN201210417498 A CN 201210417498A CN 102872077 B CN102872077 B CN 102872077B
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- Prior art keywords
- houttuynoid
- endometrial cancer
- drugs
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- 206010014759 Endometrial neoplasm Diseases 0.000 title claims abstract description 25
- 206010014733 Endometrial cancer Diseases 0.000 title claims abstract description 22
- OXBQNNYXKZSXES-RDHYKQKTSA-N 5,7-dihydroxy-2-(7-hydroxy-2-nonyl-1-benzofuran-4-yl)-3-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxychromen-4-one Chemical compound C1=CC(O)=C2OC(CCCCCCCCC)=CC2=C1C=1OC2=CC(O)=CC(O)=C2C(=O)C=1O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O OXBQNNYXKZSXES-RDHYKQKTSA-N 0.000 title abstract description 42
- 239000003814 drug Substances 0.000 title abstract description 8
- 229940079593 drug Drugs 0.000 title abstract description 8
- 239000003560 cancer drug Substances 0.000 claims abstract description 9
- 150000001875 compounds Chemical class 0.000 claims description 16
- 238000002360 preparation method Methods 0.000 claims description 14
- 229930190556 houttuynoid Natural products 0.000 claims description 4
- 230000012010 growth Effects 0.000 abstract description 7
- 230000000694 effects Effects 0.000 abstract description 5
- 230000002401 inhibitory effect Effects 0.000 abstract description 3
- 230000005764 inhibitory process Effects 0.000 abstract description 3
- 238000011161 development Methods 0.000 abstract description 2
- 238000011156 evaluation Methods 0.000 abstract description 2
- OAVCWZUKQIEFGG-UHFFFAOYSA-O 2-(5-methyl-2H-tetrazol-1-ium-1-yl)-1,3-thiazole Chemical compound CC1=NN=N[NH+]1C1=NC=CS1 OAVCWZUKQIEFGG-UHFFFAOYSA-O 0.000 abstract 1
- 230000000118 anti-neoplastic effect Effects 0.000 abstract 1
- 201000003914 endometrial carcinoma Diseases 0.000 description 11
- 208000009889 Herpes Simplex Diseases 0.000 description 4
- 241000700584 Simplexvirus Species 0.000 description 4
- 230000003602 anti-herpes Effects 0.000 description 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- 240000000691 Houttuynia cordata Species 0.000 description 3
- 235000013719 Houttuynia cordata Nutrition 0.000 description 3
- 239000002246 antineoplastic agent Substances 0.000 description 3
- 229940041181 antineoplastic drug Drugs 0.000 description 3
- 229930003935 flavonoid Natural products 0.000 description 3
- 150000002215 flavonoids Chemical class 0.000 description 3
- 235000017173 flavonoids Nutrition 0.000 description 3
- 239000001963 growth medium Substances 0.000 description 3
- 206010028980 Neoplasm Diseases 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 230000001093 anti-cancer Effects 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 230000031700 light absorption Effects 0.000 description 2
- 229930014626 natural product Natural products 0.000 description 2
- 230000004083 survival effect Effects 0.000 description 2
- 241001597008 Nomeidae Species 0.000 description 1
- 229930012538 Paclitaxel Natural products 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 230000001464 adherent effect Effects 0.000 description 1
- 230000000259 anti-tumor effect Effects 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 230000010261 cell growth Effects 0.000 description 1
- 239000012531 culture fluid Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 231100000206 health hazard Toxicity 0.000 description 1
- 150000002611 lead compounds Chemical class 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000011275 oncology therapy Methods 0.000 description 1
- 229960001592 paclitaxel Drugs 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 230000000452 restraining effect Effects 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses an application of Houttuynoid B in drugs for treating endometrial cancer, belonging to the technical field of a new application of drugs. Through external MTT (Methyl Thiazolyl Tetrazolium) antineoplastic activity evaluation, the invention discovers that Houttuynoid B also has an obvious inhibition effect on the growth of human endometrial cancer strains ISK and RL95-2. Thus, Houttuynoid B can be applied to preparing anti-endometrial cancer drugs and has good development and application prospects. The application of Houttuynoid B in drugs for treating endometrial cancer disclosed by the invention is publicized for the first time; and as the skeleton type is brand new, Houttuynoid B has an unexpectedly strong inhibitory activity to endometrial cancer cells.
Description
Technical field
The present invention relates to the new purposes of compound H outtuynoid B, relate in particular to the application of Houttuynoid B 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 B that the present invention relates to is one and delivered (Chen in 2012, S. D. et al., 2012. Houttuynoid B_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 B_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 B 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 B in the preparation antitumor drug.
The present invention adopts following technical scheme: the application of Houttuynoid B in the anti-endometrium cancer drug of preparation, and the structural formula of Houttuynoid B is shown in formula I:
The present invention finds that by external MTT anti-tumor activity evaluation the growth of the people's endometrial carcinoma cell of Houttuynoid B strain ISK and RL95-2 also has significant inhibitory effect, suppresses the IC of this 2 strain cell growth
50Value is respectively 0.14 ± 0.07 μ M and 0.17 ± 0.06 μ M.Therefore, Houttuynoid B can have the excellent development application prospect for the preparation of anti-endometrium cancer drug.
The purposes of the Houttuynoid B 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 B involved in the present invention is referring to document (Chen, S. D. et al., 2012. Houttuynoid B_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 B tablet involved in the present invention:
Get 20 and digest compound Houttuynoid B, add conventional adjuvant 180 grams of preparation tablet, mixing, conventional tablet machine are made 1000.
Embodiment 2: the preparation of compound H outtuynoid B capsule involved in the present invention:
Get 20 and digest compound Houttuynoid B, 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 B 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 B 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 B 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: 0.14 ± 0.07 μ M and 0.17 ± 0.06 μ M.
Shown that by above-described embodiment the growth of Houttuynoid B of the present invention people's endometrial carcinoma cell strain ISK and RL95-2 has the good restraining effect.Prove that thus Houttuynoid B 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 B in preparation treatment endometrium cancer drug, described compound H outtuynoid B structure as
Formula IShown in:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210417498 CN102872077B (en) | 2012-10-27 | 2012-10-27 | Application of Houttuynoid B in drugs for treating endometrial cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210417498 CN102872077B (en) | 2012-10-27 | 2012-10-27 | Application of Houttuynoid B in drugs for treating endometrial cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102872077A CN102872077A (en) | 2013-01-16 |
| CN102872077B true CN102872077B (en) | 2013-08-28 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201210417498 Expired - Fee Related CN102872077B (en) | 2012-10-27 | 2012-10-27 | Application of Houttuynoid B in drugs for treating endometrial cancer |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102872077B (en) |
-
2012
- 2012-10-27 CN CN 201210417498 patent/CN102872077B/en not_active Expired - Fee Related
Non-Patent Citations (2)
| 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN102872077A (en) | 2013-01-16 |
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