CN103463049B - The application of Lycojaponicumin B in preparation treatment breast cancer medicines - Google Patents

The application of Lycojaponicumin B in preparation treatment breast cancer medicines Download PDF

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CN103463049B
CN103463049B CN201310436783.3A CN201310436783A CN103463049B CN 103463049 B CN103463049 B CN 103463049B CN 201310436783 A CN201310436783 A CN 201310436783A CN 103463049 B CN103463049 B CN 103463049B
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breast cancer
lycojaponicumin
application
preparation treatment
present
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CN103463049A (en
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江春平
张广
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Shanghai Institute of Biological Products Co.,Ltd.
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Nanjing Guangkangxie Biomedical Technology Co Ltd
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Abstract

The invention discloses the application of Lycojaponicumin B in preparation treatment breast cancer medicines, belong to technical field of new application of medicine.The present invention is found by external MTT antineoplastic activity evaluation, and Lycojaponicumin B also has significant inhibitory action to the growth of Breast cancer lines 4T1, MCF-7, MDA-MB-231 and MCF-7B.Therefore, Lycojaponicumin B for the preparation of anti-breast cancer medicines, can have good development prospect.Belong to first public for the purposes of the Lycojaponicumin B that the present invention relates in preparation treatment breast cancer medicines, because framework types belongs to brand-new framework types, and its inhibit activities for breast cancer cell is unexpectedly strong.

Description

The application of Lycojaponicumin B in preparation treatment breast cancer medicines
Technical field
The present invention relates to the novelty teabag of compound L ycojaponicumin B, particularly relate to Lycojaponicumin B and preparing the application in anti-breast cancer medicines.
Technical background
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 L ycojaponicumin B that the present invention relates to is one and delivers (Wang in 2012, X.J.et al., 2012.Lycojaponicumins A-C, Three Alkaloids with an UnprecedentedSkeleton from Lycopodium japonicum.Organic Letters 14 (10), New skeleton compound 2614-2617.), this compound has brand-new framework types, the purposes of the LycojaponicuminB that the present invention relates in preparation treatment breast cancer medicines is belonged to first public, because framework types belongs to brand-new framework types, and its inhibit activities for breast cancer cell is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control simultaneously for breast carcinoma obviously has significant progress.
Summary of the invention
The invention provides compound L ycojaponicumin B and prepare the application in antitumor drug.
The present invention adopts following technical scheme: Lycojaponicumin B is preparing the application in anti-breast cancer medicines, and the structural formula of Lycojaponicumin B is as shown in formula I:
The present invention is found by external MTT antineoplastic activity evaluation, and Lycojaponicumin B also has significant inhibitory action to the growth of Breast cancer lines 4T1, MCF-7, MDA-MB-231 and MCF-7B, suppresses the IC of this 4 strain Growth of Cells 50value is respectively 3.12 ± 0.13 μMs, 2.31 ± 0.25 μMs, 1.24 ± 0.17 μMs and 4.17 ± 0.37 μMs.Therefore, Lycojaponicumin B for the preparation of anti-breast cancer medicines, can have good development prospect.
The purposes of the Lycojaponicumin B that the present invention relates in preparation treatment breast cancer medicines belongs to first public, because framework types belongs to brand-new framework types, and its inhibit activities for breast 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 breast 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 L ycojaponicumin B involved in the present invention is see document (Wang, X.J.et al., 2012.Lycojaponicumins A-C, Three Alkaloids with an Unprecedented Skeleton from Lycopodiumjaponicum.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 by 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 g of compound Lycojaponicumin B, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound L ycojaponicumin B capsule involved in the present invention:
Get 20 g of compound Lycojaponicumin B, add prepare capsule customary adjuvant as starch 180 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example: adopt mtt assay assessing compound Lycojaponicumin B to the growth inhibited effect of Breast cancer lines
1. method: the cell being in growth logarithmic (log) phase: Breast cancer lines 4T1, MCF-7, MDA-MB-231 and MCF-7B (buying from Chinese Academy of Sciences's cell bank) are 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 Lycojaponicumin B 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 Lycojaponicumin B to Breast cancer lines 4T1, MCF-7, MDA-MB-231 and MCF-7B has significant inhibitory action.This compound suppresses the IC of Breast cancer lines 4T1, MCF-7, MDA-MB-231 and MCF-7B growth 50value is respectively: 3.12 ± 0.13 μMs, 2.31 ± 0.25 μMs, 1.24 ± 0.17 μMs and 4.17 ± 0.37 μMs.
Shown by above-described embodiment, the growth of Lycojaponicumin B of the present invention to Breast cancer lines 4T1, MCF-7, MDA-MB-231 and MCF-7B has good inhibitory action.Prove thus, Lycojaponicumin B of the present invention has anti-breast cancer activity, can for the preparation of anti-breast cancer medicines.

Claims (1)

1.Lycojaponicumin B preparation treatment breast cancer medicines in application, described compound L ycojaponicumin B structure as formula Ishown in:
formula I.
CN201310436783.3A 2013-09-23 2013-09-23 The application of Lycojaponicumin B in preparation treatment breast cancer medicines Active CN103463049B (en)

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CN201310436783.3A CN103463049B (en) 2013-09-23 2013-09-23 The application of Lycojaponicumin B in preparation treatment breast cancer medicines

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CN103463049B true CN103463049B (en) 2015-08-19

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Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Lycojaponicumins A-c,Three Alkaloids with an Unprecedented Skeleton from Lycopodium japonicum;Xiao-Jing Wang, et al;《Organic Letters》;20120508;第14卷(第10期);2614-2617 *

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Effective date of registration: 20170411

Address after: 200051 Anshun Road, Shanghai, No. 350, No.

Patentee after: Shanghai Institute of Biological Products Co.,Ltd.

Address before: Metro Technology Building No. 69 Olympic Avenue in Jianye District of Nanjing city in Jiangsu province 210019 01 5 storey buildings

Patentee before: Nanjing Guangkangxie Biomedical Technology Co., Ltd.