CN103405406B - The application of a kind of compound in preparation treatment endometrial cancer drug - Google Patents

The application of a kind of compound in preparation treatment endometrial cancer drug Download PDF

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Publication number
CN103405406B
CN103405406B CN201310370859.7A CN201310370859A CN103405406B CN 103405406 B CN103405406 B CN 103405406B CN 201310370859 A CN201310370859 A CN 201310370859A CN 103405406 B CN103405406 B CN 103405406B
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China
Prior art keywords
nardoaristolones
cancer drug
endometrial cancer
compound
preparation treatment
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Expired - Fee Related
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CN201310370859.7A
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Chinese (zh)
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CN103405406A (en
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刘美福
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Taizhou hi tech new technology development center high port intellectual property consulting office
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YIWU LVMEI BIOTECHNOLOGY Co Ltd
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Abstract

The invention discloses the application of Nardoaristolones A in preparation treatment endometrial cancer drug, belong to technical field of new application of medicine.The present invention is found by external MTT antineoplastic activity evaluation, and the growth of Nardoaristolones A to people's Endometrial carcinoma cell line ISK and RL95-2 also has significant inhibitory action.Therefore, Nardoaristolones A for the preparation of anti-endometrial cancer drug, can have good development prospect.For the Nardoaristolones A that the present invention relates to, the purposes in preparation treatment endometrial cancer drug belongs to first public.

Description

The application of a kind of compound in preparation treatment endometrial cancer drug
Technical field
The present invention relates to the novelty teabag of compound N ardoaristolones A, particularly relate to the application of Nardoaristolones A in preparation treatment endometrial cancer drug.
Background technology
Cancer is to one of maximum disease of human life's health hazard, 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.74% is had to be natural product or derivatives thereof in antitumor drug, if paclitaxel and derivant thereof are exactly the current reasonable antitumor drug of effect clinically.Therefore, from natural product, anticancer compound is found or lead compound has great importance.
The compound N ardoaristolones A that the present invention relates to is one and delivers (Ming-Li Liu in 2013, Ying-Hui Duan, Yun-Long Hou, et al.Nardoaristolones A and B, Two Terpenoids with Unusual Skeletons from Nardostachys chinensis Batal.Organic Letters, 2013, noval chemical compound 15(5): 1000 – 1003.), this compound has brand-new framework types, current purposes only has protective effect (Ming-Li Liu to the myocardial damage of hydrogen peroxide induction, Ying-Hui Duan, Yun-Long Hou, et al.Nardoaristolones A and B, Two Terpenoids with Unusual Skeletons from Nardostachys chinensis Batal.Organic Letters, 2013, 15(5): 1000 – 1003.), the purposes of the Nardoaristolones A that the present invention relates in preparation treatment endometrial cancer drug belongs to first public.
Summary of the invention
The object of the invention is to not find that it has the present situation of the report of anti-carcinoma of endometrium activity according in existing Nardoaristolones A research, provide the application of Nardoaristolones A in the anti-endometrial cancer drug of preparation.
Described compound N ardoaristolones A structure is as shown in formula I:
The present invention is found by external MTT antineoplastic activity evaluation, the growth of Nardoaristolones A to people's Endometrial carcinoma cell line ISK and RL95-2 also has significant inhibitory action, suppresses the IC50 value of this 2 strain Growth of Cells to be respectively 1.94 ± 0.32 μMs and 0.69 ± 0.27 μM.Therefore, Nardoaristolones A for the preparation of anti-endometrial cancer drug, can have good development prospect.
The purposes of the Nardoaristolones A that the present invention relates in preparation treatment endometrial cancer drug is belonged to first public, because framework types belongs to brand-new framework types, and its inhibit activities for endometrial carcinoma cell is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control simultaneously for carcinoma of endometrium obviously has significant progress.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Detailed description of the invention
The preparation method of compound N ardoaristolones A involved in the present invention is see document (Ming-Li Liu, Ying-Hui Duan, Yun-Long Hou, et al.Nardoaristolones A and B, Two Terpenoids with Unusual Skeletons from Nardostachys chinensis Batal.Organic Letters, 2013,15(5): 1000 – 1003.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of compound N ardoaristolones A tablet involved in the present invention:
Get 5 g of compound Nardoaristolones A and add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compound N ardoaristolones A capsule involved in the present invention:
Get 5 g of compound Nardoaristolones A and add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example: adopt mtt assay assessing compound Nardoaristolones A to the growth inhibited effect of people's Endometrial carcinoma cell line
1. method: the cell being in growth logarithmic (log) phase: people's Endometrial carcinoma cell line ISK and RL95-2(buys from Chinese Academy of Sciences's cell bank) with 1.5 × 10 4concentration kind is in 96 orifice plates.Original culture medium is sucked after cell culture 24h is adherent.Test is divided into blank group, drug treating group.Blank group changes 1640 culture medium containing 10% hyclone; It is 100 μMs that drug treating group is changed containing concentration, 50 μMs, 10 μMs, 1 μM, 0.1 μM, the culture medium of the Nardoaristolones A of 0.01 μM and 0.001 μM.After cultivating 48h, add the MTT of concentration 5mg/mL, continue to be put in CO 2incubator cultivates 4h, then 100 μ L supernatants are sucked along culture fluid top, add 100 μ L DMSO, 10min is placed in dark place, microplate reader (Sunrise Products) is utilized to measure light absorption value (wavelength 570nm), and calculating cell survival according to light absorption value, 6 repeating holes are established in each process.Cell survival rate (%)=Δ OD drug treating/Δ OD blank × 100.
2. result: the growth of Nardoaristolones A to people's Endometrial carcinoma cell line P ISK and RL95-2 has significant inhibitory action.This compound suppresses the IC50 value of people's Endometrial carcinoma cell line ISK and RL95-2 growth to be respectively 1.94 ± 0.32 μMs and 0.69 ± 0.27 μM.
Shown by above-described embodiment, the growth of Nardoaristolones A of the present invention to people's Endometrial carcinoma cell line ISK and RL95-2 has good inhibitory action.Prove thus, it is active that Nardoaristolones A of the present invention has anti-carcinoma of endometrium, can for the preparation of anti-endometrial cancer drug.

Claims (1)

  1. The application of 1.Nardoaristolones A in preparation treatment endometrial cancer drug, described compound N ardoaristolones A structure is as shown in formula I:
CN201310370859.7A 2013-08-22 2013-08-22 The application of a kind of compound in preparation treatment endometrial cancer drug Expired - Fee Related CN103405406B (en)

Priority Applications (1)

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CN201310370859.7A CN103405406B (en) 2013-08-22 2013-08-22 The application of a kind of compound in preparation treatment endometrial cancer drug

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Application Number Priority Date Filing Date Title
CN201310370859.7A CN103405406B (en) 2013-08-22 2013-08-22 The application of a kind of compound in preparation treatment endometrial cancer drug

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CN103405406B true CN103405406B (en) 2015-09-09

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Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Asperterpenols A and B, New Sesterterpenoids Isolated from a Mangrove Endophytic Fungus Aspergillus sp. 085242;Ze’en Xiao et al.;《Org. Lett.》;20130305;第15卷(第10期);2522–2525 *

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