CN103462954B - Application of Nardoaristolones A in preparation of medicaments for treating skin cancer - Google Patents

Application of Nardoaristolones A in preparation of medicaments for treating skin cancer Download PDF

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Publication number
CN103462954B
CN103462954B CN201310405513.6A CN201310405513A CN103462954B CN 103462954 B CN103462954 B CN 103462954B CN 201310405513 A CN201310405513 A CN 201310405513A CN 103462954 B CN103462954 B CN 103462954B
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nardoaristolones
medicaments
application
preparation
skin cancer
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CN103462954A (en
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严建低
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Qinyan Haosheng Pharmaceutical (Shanghai) Co.,Ltd.
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SHENGZHOU LINMEI BIOTECHNOLOGY Co Ltd
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Abstract

The invention discloses application of Nardoaristolones A in preparation of medicaments for treating skin canner, and belongs to the technical field of new application of the medicaments. In vitro MTT (3-4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) anti-tumor activity evaluation discovers that Nardoaristolones A also has a remarkable effect on inhibiting the growth of human skin cancer cell strains A431, HME1, A375 and SK23, so that Nardoaristolones A can be used for preparing the medicaments for resisting the skin caner, and has a good development and application prospect, high inhibiting activity, prominent substantive features and significant progress.

Description

The application of Nardoaristolones A in preparation treatment skin carcinoma medicine
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 skin carcinoma medicine.
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 skin carcinoma medicine belongs to first public, belong to brand-new structure type.
Summary of the invention
The object of the invention is to not find that it has the present situation of the report of anti-skin carcinoma activity according in existing Nardoaristolones A research, provide the application of Nardoaristolones A in the anti-skin carcinoma medicine 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, Nardoaristolones A also has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23, suppresses the IC50 value of this 4 strain Growth of Cells to be respectively 2.75 ± 0.36 μMs, 1.78 ± 0.42 μMs, 1.65 ± 0.34 μMs and 1.87 ± 0.54 μMs.Therefore, Nardoaristolones A for the preparation of anti-skin carcinoma medicine, can have good development prospect.
The purposes of the Nardoaristolones A that the present invention relates in preparation treatment skin carcinoma medicine is belonged to first public, because framework types belongs to brand-new framework types, and its inhibit activities for skin cancer 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 skin carcinoma 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, 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, 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 application on human skin JEG-3
1. method: the cell being in growth logarithmic (log) phase: application on human skin JEG-3 A431, HME1, A375 and SK23(buy 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 application on human skin JEG-3 A431, HME1, A375 and SK23 has significant inhibitory action.This compound suppresses application on human skin JEG-3 A431, the IC50 value of HME1, A375 and SK23 growth is respectively 2.75 ± 0.36 μMs, 1.78 ± 0.42 μMs, 1.65 ± 0.34 μMs and 1.87 ± 0.54 μMs.
Shown by above-described embodiment, the growth of Nardoaristolones A of the present invention to application on human skin JEG-3 A431, HME1, A375 and SK23 has good inhibitory action.Prove thus, it is active that Nardoaristolones A of the present invention has anti-skin carcinoma, can for the preparation of anti-skin carcinoma medicine.

Claims (1)

  1. The application of 1.Nardoaristolones A in preparation treatment skin carcinoma medicine, described compound N ardoaristolones A structure is as shown in formula I:
    Formula I.
CN201310405513.6A 2013-09-06 2013-09-06 Application of Nardoaristolones A in preparation of medicaments for treating skin cancer Active CN103462954B (en)

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CN201310405513.6A CN103462954B (en) 2013-09-06 2013-09-06 Application of Nardoaristolones A in preparation of medicaments for treating skin cancer

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CN103462954B true CN103462954B (en) 2015-05-20

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Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Nardoaristolones A and B, Two Terpenoids with Unusual Skeletons from Nardostachys chinensis Batal;Ming-Li Liu, et al.;《ORGANIC LETTERS》;20130208;第15卷(第 5期);1000-1003 *
甘松属植物化学成分与药理作用;万新 等;《国外医药•植物药分册》;20071231;第22卷(第1期);1-6 *

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