CN102872122B - Application of Houttuynoid B in medicament for treating pancreatic cancer - Google Patents

Application of Houttuynoid B in medicament for treating pancreatic cancer Download PDF

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CN102872122B
CN102872122B CN 201210419443 CN201210419443A CN102872122B CN 102872122 B CN102872122 B CN 102872122B CN 201210419443 CN201210419443 CN 201210419443 CN 201210419443 A CN201210419443 A CN 201210419443A CN 102872122 B CN102872122 B CN 102872122B
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houttuynoid
pancreatic cancer
medicament
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preparing
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CN102872122A (en
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俞骁
施桦
吴俊华
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Liu Jun
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吴俊华
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Abstract

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

Description

The application of Houttuynoid B in preparation treatment cancer of pancreas medicine
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-cancer of pancreas 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 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 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 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 cancer of pancreas medicine, because framework types belongs to brand-new framework types, and its inhibition for pancreatic 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 cancer of pancreas obviously has significant progress.
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-cancer of pancreas medicine of preparation, and the structural formula of Houttuynoid B is as shown in formula I:
Figure BDA0000231837311
The present invention finds by external MTT anti-tumor activity evaluation, and Houttuynoid B also has significant inhibitory action to the growth of human pancreas cancer cell strain PANC-1 and BXPC-3, suppresses the IC of this 2 strain Growth of Cells 50Value is respectively 1.11 ± 0.17 μ M and 1.43 ± 0.21 μ M.Therefore, Houttuynoid B can for the preparation of anti-cancer of pancreas medicine, have good development prospect.
Belong to open first for the purposes of the Houttuynoid B that the present invention relates in preparation treatment cancer of pancreas medicine, because framework types belongs to brand-new framework types, and its inhibition for pancreatic 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 cancer of pancreas 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 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 that prepare 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 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 B to the growth inhibited effect of human pancreas cancer cell strain
1. method: the cell that is in the growth logarithmic (log) phase: human pancreas cancer cell strain PANC-1 and BXPC-3(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 B 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 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 pancreas cancer cell strain PANC-1 and BXPC-3.This compound suppresses the IC of human pancreas cancer cell strain PANC-1 and BXPC-3 growth 50Value is respectively 1.11 ± 0.17 μ M and 1.43 ± 0.21 μ M.
Shown by above-described embodiment, Houttuynoid B of the present invention has good inhibitory action to the growth of human pancreas cancer cell strain PANC-1 and BXPC-3.Prove thus, it is active that Houttuynoid B of the present invention has anti-cancer of pancreas, can be for the preparation of anti-cancer of pancreas medicine.

Claims (1)

1.Houttuynoid the application of B in preparation treatment cancer of pancreas medicine, described compound H outtuynoid B structure as Formula IShown in:
Figure 45742DEST_PATH_IMAGE001
Formula I.
CN 201210419443 2012-10-27 2012-10-27 Application of Houttuynoid B in medicament for treating pancreatic cancer Active CN102872122B (en)

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Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
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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