CN103463034A - Application of Lycojaponicumin B to medicament for treating oophoroma - Google Patents

Application of Lycojaponicumin B to medicament for treating oophoroma Download PDF

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CN103463034A
CN103463034A CN2013104361945A CN201310436194A CN103463034A CN 103463034 A CN103463034 A CN 103463034A CN 2013104361945 A CN2013104361945 A CN 2013104361945A CN 201310436194 A CN201310436194 A CN 201310436194A CN 103463034 A CN103463034 A CN 103463034A
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lycojaponicumin
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medicine
oophoroma
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CN103463034B (en
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江春平
张广
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Anhui Creative Technology Transfer Service Co.,Ltd.
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Nanjing Guangkangxie Biomedical Technology Co Ltd
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Abstract

The invention discloses an application of Lycojaponicumin B in preparation of a medicine for treating oophoroma, belonging to the technical field of new applications of medicines. According to the application disclosed by the invention, the in-vitro MTT (methyl thiazolyl tetrazolium) anti-tumor activity evaluation discovers that the Lycojaponicumin B also has an obvious inhibitory effect on the growth of human ovarian carcinoma cell lines including HO-8910, HOC1 and OVAC. Thus, the Lycojaponicumin B can be used for preparing an anti-oophoroma medicine and has good prospects in development and application. The application of the Lycojaponicumin B in preparation of medicine for treating oophoroma, disclosed by the invention, is disclosed for the first time. The skeleton type of the Lycojaponicumin B belongs to a brand new skeleton type, and the inhibitory activity of the Lycojaponicumin B on human ovarian carcinoma cells is unexpectedly strong.

Description

The application of Lycojaponicumin B in treatment ovarian cancer medicine
Technical field
The present invention relates to the new purposes of compound L ycojaponicumin B, relate in particular to the application of Lycojaponicumin B in preparing ovarian cancer resistance medicament.
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 L ycojaponicumin B the present invention relates to is one and within 2012, delivers (Wang, X. J. et al., 2012. Lycojaponicumins A-C, Three Alkaloids with an Unprecedented Skeleton from Lycopodium japonicum. Organic Letters 14 (10), 2614-2617.) New skeleton compound, this compound has brand-new framework types, purposes for the Lycojaponicumin B the present invention relates in preparation treatment ovarian cancer medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for ovarian 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 ovarian cancer simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of compound L ycojaponicumin B in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Lycojaponicumin B in preparing ovarian cancer resistance medicament, and the structural formula of Lycojaponicumin B is as shown in formula I:
Figure BDA0000385855441
The present invention finds by external MTT anti-tumor activity evaluation, and Lycojaponicumin B also has significant inhibitory action to the growth of human oophoroma cell line HO-8910, HOC1 and OVAC, suppresses the IC of this 3 strain Growth of Cells 50value is respectively 1.21 ± 0.11 μ M, 2.37 ± 0.14 μ M and 2.14 ± 0.12 μ M.Therefore, Lycojaponicumin B can, for the preparation of ovarian cancer resistance medicament, have good development prospect.
The purposes of the Lycojaponicumin B the present invention relates in preparation treatment ovarian cancer medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for ovarian 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 ovarian cancer 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 L ycojaponicumin B involved in the present invention is referring to document (Wang, X. J. et al., 2012. Lycojaponicumins A-C, Three Alkaloids with an Unprecedented Skeleton from Lycopodium japonicum. Organic Letters 14 (10), 2614-2617.).
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 L ycojaponicumin B tablet involved in the present invention:
Get 20 and digest compound Lycojaponicumin B, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound L ycojaponicumin B capsule involved in the present invention:
Get 20 and digest compound Lycojaponicumin B, 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 Lycojaponicumin B to the human oophoroma cell line
1. method: in the cell of growth logarithmic (log) phase: human oophoroma cell line HO-8910, HOC1 and OVAC(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 24 h are 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 Lycojaponicumin B of 0.01 μ M and 0.001 μ M.After cultivating 48 h, add the MTT of concentration 5mg/mL, continue to be put in CO 2incubator is cultivated 4 h, then suck 100 μ L supernatants along culture fluid top, 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 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: Lycojaponicumin B has significant inhibitory action to the growth of human oophoroma cell line HO-8910, HOC1 and OVAC.This compound suppresses the IC of human oophoroma cell line HO-8910, HOC1 and OVAC growth 50value is respectively: 1.21 ± 0.11 μ M, 2.37 ± 0.14 μ M and 2.14 ± 0.12 μ M.
By above-described embodiment, shown, Lycojaponicumin B of the present invention has good inhibitory action to the growth of human oophoroma cell line HO-8910, HOC1 and OVAC.Prove thus, Lycojaponicumin B of the present invention has the ovarian cancer resistance activity, can be for the preparation of ovarian cancer resistance medicament.

Claims (1)

1.Lycojaponicumin the application of B in treatment ovarian cancer medicine, described compound L ycojaponicumin B structure as formula Ishown in:
Figure 359644DEST_PATH_IMAGE001
formula I.
CN201310436194.5A 2013-09-23 2013-09-23 The application of Lycojaponicumin B in preparation treatment ovarian cancer Active CN103463034B (en)

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103059043A (en) * 2011-10-24 2013-04-24 中国医学科学院药物研究所 Clavatine A-C and preparation method as well as pharmaceutical composition and application thereof

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103059043A (en) * 2011-10-24 2013-04-24 中国医学科学院药物研究所 Clavatine A-C and preparation method as well as pharmaceutical composition and application thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
XIAO-JING WANG, ET AL: "Lycojaponicumins A-c,Three Alkaloids with an Unprecedented Skeleton from Lycopodium japonicum", 《ORGANIC LETTERS》, vol. 14, no. 10, 8 May 2012 (2012-05-08), pages 2614 - 2617, XP055066237, DOI: 10.1021/ol3009478 *

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