CN103638008A - Application of Artoxanthochromane in skin cancer treatment drugs - Google Patents

Application of Artoxanthochromane in skin cancer treatment drugs Download PDF

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CN103638008A
CN103638008A CN201310634100.5A CN201310634100A CN103638008A CN 103638008 A CN103638008 A CN 103638008A CN 201310634100 A CN201310634100 A CN 201310634100A CN 103638008 A CN103638008 A CN 103638008A
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artoxanthochromane
application
skin cancer
drugs
cancer treatment
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CN103638008B (en
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陈军
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XI'AN LEKOU FUTAI BIOMEDICAL TECHNOLOGY Co.,Ltd.
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CHANGZHOU KELIXIN MEDICAL DEVICES Co Ltd
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Abstract

The invention discloses an application of Artoxanthochromane in preparation of skin cancer treatment drugs, belonging to the technical field of a new application of drugs. According to in-vitro MTT antitumor activity evaluation, the Artoxanthochromane has a remarkable inhibitory effect on the growth of human skin cancer cell strains A431, HME1, A375 and SK23. Therefore, the Artoxanthochromane can be used for preparing anti-skin cancer drugs and has a good prospect in development and application. The application of Artoxanthochromane in preparation of skin cancer treatment drugs is disclosed for the first time; the Artoxanthochromane has strong inhibitory activity on the skin cancer cells, and a remarkable progress is realized.

Description

The application of Artoxanthochromane in treatment skin carcinoma medicine
Technical field
The present invention relates to the new purposes of compd A rtoxanthochromane, relate in particular to the application of Artoxanthochromane in preparation treatment skin carcinoma medicine.
Background technology
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 compd A rtoxanthochromane the present invention relates to is one and within 2013, delivers (Horng-Huey Ko, et al., A Novel MonoterpeneStilbene Adduct with a4, 4-Dimethyl-2, 3-diphenylchromane Skeleton from Artocarpus xanthocarpus.chemistry & biodiversity, 2013 (10): noval chemical compound 1269-1275.), this compound has brand-new framework types, this compound can be removed oxygen-derived free radicals (Horng-Huey Ko, et al., A Novel MonoterpeneStilbene Adduct with a4, 4-Dimethyl-2, 3-diphenylchromane Skeleton from Artocarpus xanthocarpus.chemistry & biodiversity, 2013 (10): 1269-1275.), the purposes of the Artoxanthochromane the present invention relates in preparation treatment skin carcinoma medicine belongs to open first.
Summary of the invention
The object of the invention is to, according to not finding that it has the present situation of the report of anti-skin carcinoma activity in existing Artoxanthochromane research, provides the application of Artoxanthochromane in the anti-skin carcinoma medicine of preparation.
Described compd A rtoxanthochromane, structure is as shown in formula I:
Figure BDA0000427777670000011
Formula I
The present invention finds by the evaluation of external MTT anti-tumor activity, Artoxanthochromane also has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23, and the IC50 value that suppresses this 4 strain Growth of Cells is respectively 2.47 ± 0.45 μ M, 1.96 ± 0.26 μ M, 1.37 ± 0.22 μ M and 1.27 ± 0.85 μ M.Therefore, Artoxanthochromane can, for the preparation of anti-skin carcinoma medicine, have good development prospect.
Purposes for the Artoxanthochromane the present invention relates in preparation treatment skin carcinoma medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for skin cancer cell is active strong, possess outstanding substantive distinguishing features, the control for skin carcinoma 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 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 preparation method of compd A rtoxanthochromane involved in the present invention is referring to document (Horng-Huey Ko, et al., A Novel MonoterpeneStilbene Adduct with a4,4-Dimethyl-2,3-diphenylchromane Skeleton from Artocarpus xanthocarpus.chemistry & biodiversity, 2013 (10): 1269-1275.), prepare according to the method described above compd A rtoxanthochromane.
Embodiment 1: the preparation of compd A rtoxanthochromane tablet involved in the present invention:
Get 5 and digest compound Artoxanthochromane, add 195 grams, dextrin, mix, conventional tabletting is made 1000.
Embodiment 2: the preparation of compd A rtoxanthochromane capsule involved in the present invention:
Get 5 and digest compound Artoxanthochromane, add 195 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 Artoxanthochromane to application on human skin JEG-3
1. method: the cell 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.After cell culture 24h is 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 Artoxanthochromane of 0.01 μ M and 0.001 μ M.Cultivate after 48h, add the MTT of concentration 5mg/mL, continue to be put in CO 2incubator is cultivated 4h, then along culture fluid top, suck 100 μ L supernatants, add 100 μ L DMSO, 10min is 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: Artoxanthochromane has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23.The IC50 value that this compound suppresses application on human skin JEG-3 A431, HME1, A375 and SK23 growth is respectively 2.47 ± 0.45 μ M, 1.96 ± 0.26 μ M, 1.37 ± 0.22 μ M and 1.27 ± 0.85 μ M.
By above-described embodiment, shown, Artoxanthochromane of the present invention has good inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23.Prove thus, it is active that Artoxanthochromane of the present invention has anti-skin carcinoma, can be for the preparation of anti-skin carcinoma medicine.

Claims (1)

  1. The application of 1.Artoxanthochromane in treatment skin carcinoma medicine, described compd A rtoxanthochromane structure is as shown in formula I:
    Formula I.
CN201310634100.5A 2013-12-02 2013-12-02 The application of Artoxanthochromane in treatment skin carcinoma medicine Active CN103638008B (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9701655B2 (en) 2014-02-07 2017-07-11 Novogen Limited Functionalised benzopyran compounds and use thereof

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
HORNG-HUEY KO等: "a novel monoterpene-stilbene adduct with a 4,4-dimethyl-2,3-diphenylchromane skeleton from artocarpus xanthocarpus", 《CHEMISTRY & BIODIVERSITY》, vol. 10, no. 7, 12 July 2013 (2013-07-12), pages 1269 - 1275 *
崔剑 等: "自由基生物抗氧化与疾病", 《清华大学学报 自然科学版》, vol. 40, no. 6, 31 December 2000 (2000-12-31), pages 9 - 12 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9701655B2 (en) 2014-02-07 2017-07-11 Novogen Limited Functionalised benzopyran compounds and use thereof
US10370349B2 (en) 2014-02-07 2019-08-06 Kazia Therapeutics Limited Functionalised benzopyran compounds and use thereof

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