CN103446088A - Application of Incarviatone A in skin cancer treatment drug - Google Patents

Application of Incarviatone A in skin cancer treatment drug Download PDF

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Publication number
CN103446088A
CN103446088A CN2013104321825A CN201310432182A CN103446088A CN 103446088 A CN103446088 A CN 103446088A CN 2013104321825 A CN2013104321825 A CN 2013104321825A CN 201310432182 A CN201310432182 A CN 201310432182A CN 103446088 A CN103446088 A CN 103446088A
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China
Prior art keywords
incarviatone
skin cancer
application
preparation
cancer treatment
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CN2013104321825A
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CN103446088B (en
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江春平
黄蓉
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Anhui Bodhi biological medicine science and Technology Co Ltd
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Nanjing Guangkangxie Biomedical Technology Co Ltd
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Abstract

The invention discloses application of Incarviatone A in preparation of a skin cancer treatment drug and belongs to the technical field of novel medicine application. Evaluation of in-vitro thiazolyl blue (MTT) anti-tumor activity shows that the Incarviatone A also has remarkable inhabiting effect on growth of human skin cancer cell strains A431, HME1, A375 and SK23. Therefore, the Incarviatone A can be used for preparation of an anti-skin cancer drug and has good development and application prospect. The application of the Incarviatone A in the preparation of the skin cancer treatment drug is disclosed for the first time. Due to the fact that the fact that the skeleton type is a novel skeleton type, and the high skin cancer cell inhibiting activity of the Incarviatone A is previously unimagined.

Description

The application of Incarviatone A in treatment skin carcinoma medicine
Technical field
The present invention relates to the new purposes of Compound I ncarviatone A, relate in particular to the application of Incarviatone A in the anti-skin carcinoma medicine of preparation.
Technical background
Cancer is to one of disease of human life's health hazard maximum, and annual have a large amount of people to die from cancer.The research and development of cancer therapy drug are the focuses of study of pharmacy always.In antitumor drug, have 74% to be the natural product or derivatives thereof, as paclitaxel and derivant thereof are exactly the reasonable antitumor drug of effect clinically at present.Therefore, from natural product, searching anticancer compound or lead compound have great importance.
The Compound I ncarviatone A the present invention relates to is one and within 2012, delivers (Shen, Y.H.et al., 2012.Incarviatone A, a structurally unique natural product hybrid with a new carbon skeleton from Incarvillea delavayi, and its absolute configuration via calculated electronic circular dichroic spectra.RSC Advances2, 4175 – 4180.) New skeleton compound, this compound has brand-new framework types, there is no at present the report about this compound activity aspect, purposes for the Incarviatone A 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 unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control for skin carcinoma simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of Compound I ncarviatone A in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Incarviatone A in the anti-skin carcinoma medicine of preparation, and the structural formula of Incarviatone A is as shown in formula I:
Figure BDA0000385286180000021
The present invention finds by external MTT anti-tumor activity evaluation, and Incarviatone A also has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23, suppresses the IC of this 4 strain Growth of Cells 50value is respectively 1.23 ± 0.13 μ M, 2.24 ± 0.17 μ M, 1.21 ± 0.21 μ M and 2.10 ± 0.18 μ M.Therefore, Incarviatone A can, for the preparation of anti-skin carcinoma medicine, have good development prospect.
The purposes of the Incarviatone A 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 unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, 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 preparation method of Compound I ncarviatone A involved in the present invention is referring to document (Shen, Y.H.et al., 2012.Incarviatone A, a structurally unique natural product hybrid with a new carbon skeleton from Incarvillea delavayi, and its absolute configuration via calculated electronic circular dichroic spectra.RSC Advances2,4175 – 4180.).
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 I ncarviatone A tablet involved in the present invention:
Get 20 and digest compound Incarviatone A, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of Compound I ncarviatone A capsule involved in the present invention:
Get 20 and digest compound Incarviatone A, add the conventional adjuvant for preparing capsule as starch 180 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: adopt the growth inhibited effect of mtt assay assessing compound Incarviatone A to the application on human skin JEG-3
1. method: in the cell of 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 4the concentration kind is in 96 orifice plates.Suck original culture medium after cell culture 24h is adherent.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 the 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 Incarviatone A of 0.01 μ M and 0.001 μ M.After cultivating 48h, add the MTT of concentration 5mg/mL, continue to be put in CO 2incubator is cultivated 4h, then suck 100 μ L supernatants along culture fluid top, 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 the 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: Incarviatone A has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23.This compound suppresses the IC of application on human skin JEG-3 A431, HME1, A375 and SK23 growth 50value is respectively: 1.23 ± 0.13 μ M, 2.24 ± 0.17 μ M, 1.21 ± 0.21 μ M and 2.10 ± 0.18 μ M.
By above-described embodiment, shown, Incarviatone A 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, Incarviatone A of the present invention has anti-skin carcinoma activity, can be for the preparation of anti-skin carcinoma medicine.

Claims (1)

1.Incarviatone the application of A in treatment skin carcinoma medicine, described Compound I ncarviatone A structure as formula Ishown in:
formula I.
CN201310432182.5A 2013-09-22 2013-09-22 The application of Incarviatone A in preparation treatment skin carcinoma medicine Expired - Fee Related CN103446088B (en)

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005021496A2 (en) * 2003-08-27 2005-03-10 The Trustees Of Columbia University In The City Of New York Synthesis of derivatives of ginkgolide c
EP1939166A1 (en) * 2006-12-19 2008-07-02 InterMed Discovery GmbH Plants extracts for use in brain modulation

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005021496A2 (en) * 2003-08-27 2005-03-10 The Trustees Of Columbia University In The City Of New York Synthesis of derivatives of ginkgolide c
EP1939166A1 (en) * 2006-12-19 2008-07-02 InterMed Discovery GmbH Plants extracts for use in brain modulation

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SHEN,Y.H.ET AL.,: "ncarviatone A,a structurally unique natural product hybrid with a new carbon skeleton from Incarvillea delavayi,and its absolute configuration via calculated electronic circular dichroic spectra", 《RSC ADVANCES2》, 31 December 2012 (2012-12-31), pages 4175 - 4180 *

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