CN102872072B - Application of Houttuynoid B to preparing drugs for treating kidney cancer - Google Patents
Application of Houttuynoid B to preparing drugs for treating kidney cancer Download PDFInfo
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- CN102872072B CN102872072B CN 201210417092 CN201210417092A CN102872072B CN 102872072 B CN102872072 B CN 102872072B CN 201210417092 CN201210417092 CN 201210417092 CN 201210417092 A CN201210417092 A CN 201210417092A CN 102872072 B CN102872072 B CN 102872072B
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- Prior art keywords
- houttuynoid
- kidney cancer
- application
- drugs
- preparing
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- 206010038389 Renal cancer Diseases 0.000 title claims abstract description 25
- 239000003814 drug Substances 0.000 title claims abstract description 17
- 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 40
- 229940079593 drug Drugs 0.000 title abstract description 9
- 208000008839 Kidney Neoplasms Diseases 0.000 title abstract description 8
- 201000010982 kidney cancer Diseases 0.000 title abstract description 8
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 17
- 201000010174 renal carcinoma Diseases 0.000 claims description 17
- 150000001875 compounds Chemical class 0.000 claims description 16
- 238000002360 preparation method Methods 0.000 claims description 10
- 229930190556 houttuynoid Natural products 0.000 claims description 4
- 230000012010 growth Effects 0.000 abstract description 7
- 230000000694 effects Effects 0.000 abstract description 6
- 230000002401 inhibitory effect Effects 0.000 abstract description 4
- 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
- 238000000338 in vitro Methods 0.000 abstract 1
- 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
- 201000011510 cancer Diseases 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 230000031700 light absorption Effects 0.000 description 2
- 239000000203 mixture Substances 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
- 230000001093 anti-cancer 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
- 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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- Medicinal Preparation (AREA)
- Medicines Containing Plant Substances (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses application of Houttuynoid B to preparing drugs for treating kidney cancer, belonging to technical field of new uses of the drugs. According to the invention, found by in vitro methyl thiazolyl tetrazolium (MTT) antineoplastic activity evaluation, Houttuynoid B also has remarkable inhibition effect on the growth of human kidney cancer cell line KC. Therefore, Houttuynoid B can be used for preparing the drugs of resisting the kidney cancer and has good development and application prospects. The application of Houttuynoid B to preparing the drugs for treating the kidney cancer, disclosed by the invention, is firstly published; the framework type is brand new; and the activity of inhibiting the kidney cancer cells is unexpectedly strong.
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-renal 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.In antitumor drug, have 74% to be the natural product or derivatives thereof, as paclitaxel and derivant thereof are exactly the reasonable antitumor drug of effect clinically at present.Therefore, from natural product, searching anticancer compound or lead compound have great importance.
The compound H outtuynoid B the present invention relates to is one and within 2012, delivers (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.) New skeleton compound, this compound has brand-new framework types, current 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.), purposes for the Houttuynoid B the present invention relates in preparation treatment renal carcinoma medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for kidney cancer cell is active unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control for renal carcinoma simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of compound H outtuynoid B in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Houttuynoid B in the anti-renal carcinoma medicine of preparation, and the structural formula of Houttuynoid B is as shown in formula I:
Formula I
The present invention finds by external MTT anti-tumor activity evaluation, and Houttuynoid B also has significant inhibitory action to the growth of human renal carcinoma cell strain KC, suppresses the IC of this 1 strain Growth of Cells
50value is respectively 1.71 μ M.Therefore, Houttuynoid B can, for the preparation of anti-renal carcinoma medicine, have good development prospect.
The purposes of the Houttuynoid B the present invention relates in preparation treatment renal carcinoma medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for kidney cancer cell is active unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control for renal carcinoma simultaneously obviously has significant progress.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be 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 subject to any restriction of specific embodiment, but be 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 that prepare tablet, mix, conventional tablet machine is 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 the conventional adjuvant for preparing capsule as starch 180 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: adopt the growth inhibited effect of mtt assay assessing compound Houttuynoid B to the human renal carcinoma cell strain
1. method: in the cell of growth logarithmic (log) phase: human renal carcinoma cell strain KC(buys 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 containing 10% hyclone; It is 100 μ M that the drug treating group is changed containing concentration, 50 μ M, 10 μ M, 1 μ M, 0.1 μ M, 0.01 μ M, 0.001 μ M, the culture medium of the Houttuynoid B of 0.0001 μ M and 0.00001 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 dark place, utilize microplate reader (Sunrise company product) to measure light absorption value (wavelength 570nm), 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 B has significant inhibitory action to the growth of human renal carcinoma cell strain KC.This compound suppresses the IC of human renal carcinoma cell strain KC growth
50value is respectively: 1.71 ± 0.12 μ M.
By above-described embodiment, shown, Houttuynoid B of the present invention has good inhibitory action to the growth of human renal carcinoma cell strain KC.Prove thus, Houttuynoid B of the present invention has anti-renal carcinoma activity, can be for the preparation of anti-renal carcinoma medicine.
Claims (1)
1.Houttuynoid the application of B in preparation treatment renal carcinoma medicine, described compound H outtuynoid B structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210417092 CN102872072B (en) | 2012-10-27 | 2012-10-27 | Application of Houttuynoid B to preparing drugs for treating kidney cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201210417092 CN102872072B (en) | 2012-10-27 | 2012-10-27 | Application of Houttuynoid B to preparing drugs for treating kidney cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102872072A CN102872072A (en) | 2013-01-16 |
| CN102872072B true CN102872072B (en) | 2013-12-18 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 201210417092 Expired - Fee Related CN102872072B (en) | 2012-10-27 | 2012-10-27 | Application of Houttuynoid B to preparing drugs for treating kidney cancer |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102872072B (en) |
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2012
- 2012-10-27 CN CN 201210417092 patent/CN102872072B/en not_active Expired - Fee Related
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| Publication number | Publication date |
|---|---|
| CN102872072A (en) | 2013-01-16 |
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Owner name: JIANGSU KANGHENG CHEMICAL CO., LTD. Free format text: FORMER OWNER: WU JUNHUA Effective date: 20141127 |
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Effective date of registration: 20141127 Address after: 226500, Jiangsu, Rugao town (Rugao port area) 8 West Hong Kong Road (Fine Chemical Industry Park) Patentee after: Jiangsu Kangheng Chemical Co., Ltd. Address before: 210009 No. 22, Hankou Road, Gulou District, Jiangsu, Nanjing Patentee before: Wu Junhua |
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Granted publication date: 20131218 Termination date: 20191027 |