CN102861073B - Application of Houttuynoid A in medicine for treating colorectal cancer - Google Patents

Application of Houttuynoid A in medicine for treating colorectal cancer Download PDF

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CN102861073B
CN102861073B CN201210418622.7A CN201210418622A CN102861073B CN 102861073 B CN102861073 B CN 102861073B CN 201210418622 A CN201210418622 A CN 201210418622A CN 102861073 B CN102861073 B CN 102861073B
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houttuynoid
colorectal cancer
medicine
application
preparation
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CN102861073A (en
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江春平
张广
吴俊华
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Gu Yongliang
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Nanjing University
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Abstract

The invention discloses application of Houttuynoid A in preparation of a medicine for treating colorectal cancer, belonging to the technical field of new application of medicine. The invention discovers that Houttuynoid A has the remarkable inhibitory effects on the growth of human colorectal cancer cell strains including LOVE1, LoVo, SW620 and SW480 through the evaluation of in vitro MTT antineoplastic activity. Therefore, Houttuynoid A can be used for preparing the anti-colorectal cancer medicine and has good development and application prospects. The application of Houttuynoid A in preparation of the medicine for treating the colorectal cancer provided by the invention is disclosed firstly. The skeleton type belongs to new skeleton type, and the inhibitory activity of Houttuynoid A on colorectal cancer cells is unexpectedly strong.

Description

The application of Houttuynoid A in treatment colorectal cancer medicine
Technical field
The present invention relates to the new purposes of compound H outtuynoid A, relate in particular to Houttuynoid A in the application of preparing in resistive connection rectal cancer medicine.
Technical background
Cancer is one of disease to 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 A the present invention relates to is one and within 2012, delivers (Chen, S. D. et al., 2012. Houttuynoid A_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 A_E, Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata. Organic Letters 14 (7), 1772 – 1775.), purposes for the Houttuynoid A the present invention relates in preparation treatment colorectal cancer medicine belongs 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, for the control of colorectal cancer, obviously there is significant progress simultaneously.
Summary of the invention
The invention provides compound H outtuynoid A in the application of preparing in antitumor drug.
The present invention adopts following technical scheme: Houttuynoid A is in the application of preparing in resistive connection rectal cancer medicine, and the structural formula of Houttuynoid A is as shown in formula I:
Figure BDA0000231843081
The present invention finds by external MTT anti-tumor activity evaluation, and Houttuynoid A also has significant inhibitory action to the growth of Human colorectal cancer cells strain LOVE1, LoVo, SW620 and SW480, suppresses the IC of this 4 strain Growth of Cells 50value is respectively 3.12 ± 0.39 μ M, 1.77 ± 0.21 μ M, 1.83 ± 0.32 μ M and 5.49 ± 0.44 μ M.Therefore, Houttuynoid A can, for the preparation of resistive connection rectal cancer medicine, have good development prospect.
The purposes of the Houttuynoid A the present invention relates in preparation treatment colorectal cancer medicine belongs 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, possess outstanding substantive distinguishing features, for the control of colorectal cancer, obviously there is significant progress simultaneously.
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 A involved in the present invention is referring to document (Chen, S. D. et al., 2012. Houttuynoid A_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 A tablet involved in the present invention:
Get 20 and digest compound Houttuynoid A, add 180 grams of conventional adjuvants preparing tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound H outtuynoid A capsule involved in the present invention:
Get 20 and digest compound Houttuynoid A, 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 A to Human colorectal cancer cells strain
1. method: in growth logarithmic (log) phase cell: Human colorectal cancer cells strain LOVE1, LoVo, SW620 and SW480(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 A 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 A has significant inhibitory action to the growth of Human colorectal cancer cells strain LOVE1, LoVo, SW620 and SW480.This compound suppresses the IC of Human colorectal cancer cells strain LOVE1, LoVo, SW620 and SW480 growth 50value is respectively: 3.12 ± 0.39 μ M, 1.77 ± 0.21 μ M, 1.83 ± 0.32 μ M and 5.49 ± 0.44 μ M.
By above-described embodiment, shown, Houttuynoid A of the present invention has good inhibitory action to the growth of Human colorectal cancer cells strain LOVE1, LoVo, SW620 and SW480.Prove thus, Houttuynoid A of the present invention has resistive connection rectal cancer activity, can be for the preparation of resistive connection rectal cancer medicine.

Claims (1)

  1. The application of 1.Houttuynoid A in preparation treatment colorectal cancer medicine, described compound H outtuynoid A structure as formula Ishown in:
    Figure 516716DEST_PATH_IMAGE001
    formula I.
CN201210418622.7A 2012-10-27 2012-10-27 Application of Houttuynoid A in medicine for treating colorectal cancer Active CN102861073B (en)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108421009A (en) * 2018-06-20 2018-08-21 江苏省中医药研究院 A kind of Chinese medicine composition and preparation method thereof for treating colon cancer

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
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);第1772–1775页 *
Shao-DanChen等.HouttuynoidsA-E Anti-Herpes Simplex Virus Active Flavonoids with Novel Skeletons from Houttuynia cordata.《Organic Letters》.2012

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