CN102872141B - Application of Houttuynoid E in drug for treating liver cancer - Google Patents

Application of Houttuynoid E in drug for treating liver cancer Download PDF

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CN102872141B
CN102872141B CN201210419604.0A CN201210419604A CN102872141B CN 102872141 B CN102872141 B CN 102872141B CN 201210419604 A CN201210419604 A CN 201210419604A CN 102872141 B CN102872141 B CN 102872141B
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houttuynoid
liver cancer
drug
preparing
application
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CN102872141A (en
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李丽丽
朱磊磊
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 E in preparing a drug for treating liver cancer, belonging to the technical field of the new use of the drug. Houttuynoid E is found to have obvious inhibition effect on the growth of human liver cancer cell lines HepG2, MHCC-LM3, Bel-7402 and HuH-7 through MTT (Methyl Thiazolyl Ternzolinm) anticancer activity evaluation in vitro. Therefore, Houttuynoid E can be used for preparing the anti-liver cancer drug and has excellent prospects in development and application. The use of Houttuynoid E in preparing the drug for treating the liver cancer involved in the invention is disclosed for the first time; the framework type of Houttuynoid E is a brand new framework type; and Houttuynoid E has an unexpectedly high inhibition activity for the liver cancer cells.

Description

The application of Houttuynoid E in Hepatoma therapy medicine
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 preparing medicines resistant to liver cancer.
Technical background
Cancer is to one of disease of human life's health hazard maximum, has a large amount of people to die from cancer every year.The research and development of cancer therapy drug are the focuses of study of pharmacy always.In antitumor drug, have 74% to be natural product or derivatives thereof, if paclitaxel and derivant thereof are exactly the reasonable antitumor drug of effect clinically at present.Therefore, from natural product, find anticancer compound or lead compound has great importance.
The compound H outtuynoid E the present invention relates to is one and within 2012, delivers (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.) 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 E_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.), for the purposes in preparing Hepatoma therapy medicine the present invention relates to, belong to open first, and because framework types belongs to brand-new framework types, there is not the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control for hepatocarcinoma simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of compound H outtuynoid E in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Houttuynoid E in preparing medicines resistant to liver cancer, and the structural formula of Houttuynoid E is as shown in formula I:
Figure BDA0000231839571
Formula I
The present invention finds by the evaluation of external MTT anti-tumor activity, and Houttuynoid E also has significant inhibitory action to the growth of HepG2 cell lines, MHCC-LM3, Bel-7402 and HuH-7, suppresses the IC of this 4 strain Growth of Cells 50value is respectively 2.29 ± 0.37 μ M, 1.49 ± 0.49 μ M, 3.44 ± 0.61 μ M and 2.22 ± 0.55 μ M.Therefore, Houttuynoid E can, for the preparation of medicines resistant to liver cancer, have good development prospect.
The present invention relates to the purposes of Houttuynoid E in preparing Hepatoma therapy medicine and belong to open first, because framework types belongs to brand-new framework types, and its inhibition for hepatoma carcinoma 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 for hepatocarcinoma 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 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 subject to any restriction of specific embodiment, but be 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 180 grams of conventional adjuvants preparing tablet, mix, conventional tablet machine is 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 of preparing capsule as 180 grams of starch, mix, encapsulatedly make 1000.
Below by pharmacodynamic experiment, further illustrate its pharmaceutically active.
Experimental example: adopt the growth inhibited effect of mtt assay assessing compound Houttuynoid E to human hepatoma cell strain
1. method: the cell in growth logarithmic (log) phase: HepG2 cell lines, MHCC-LM3, Bel-7402 and HuH-7(buy from Chinese Academy of Sciences's cell bank) with 1.5 * 10 4concentration kind is in 96 orifice plates.After cell culture 24 h are adherent, suck original culture medium.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 drug treating group is changed containing 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.Cultivate after 48 h, add the MTT of concentration 5mg/mL, continue to be put in CO 2incubator is cultivated 4 h, then along culture fluid top, suck 100 μ L supernatants, 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 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 HepG2 cell lines, MHCC-LM3, Bel-7402 and HuH-7.This compound suppresses the IC of HepG2 cell lines, MHCC-LM3, Bel-7402 and HuH-7 growth 50value is respectively: 2.29 ± 0.37 μ M, 1.49 ± 0.49 μ M, 3.44 ± 0.61 μ M and 2.22 ± 0.55 μ M.
By above-described embodiment, shown, Houttuynoid E of the present invention has good inhibitory action to the growth of HepG2 cell lines, MHCC-LM3, Bel-7402 and HuH-7.Prove thus, Houttuynoid E of the present invention has resisting liver cancer activity, can be for the preparation of medicines resistant to liver cancer.

Claims (1)

  1. The application of 1.Houttuynoid E in preparing the medicine of Hepatoma therapy, described compound H outtuynoid E structure as formula Ishown in:
    Figure 803550DEST_PATH_IMAGE001
    formula I.
CN201210419604.0A 2012-10-27 2012-10-27 Application of Houttuynoid E in drug for treating liver cancer Expired - Fee Related CN102872141B (en)

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