CN103446123A - Application of Lycojaponicumin B in colorectal cancer treatment drug - Google Patents
Application of Lycojaponicumin B in colorectal cancer treatment drug Download PDFInfo
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- CN103446123A CN103446123A CN 201310435097 CN201310435097A CN103446123A CN 103446123 A CN103446123 A CN 103446123A CN 201310435097 CN201310435097 CN 201310435097 CN 201310435097 A CN201310435097 A CN 201310435097A CN 103446123 A CN103446123 A CN 103446123A
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- lycojaponicumin
- colorectal cancer
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- cancer treatment
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Abstract
The invention discloses application of Lycojaponicumin B in preparation of a colorectal 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 Lycojaponicumin B also has remarkable inhabiting effect on growth of human colorectal cancer cell strains LOVE1, LoVo, SW620 and SW480. Therefore, the Lycojaponicumin B can be used for preparation of an anti-colorectal cancer drug and has good development and application prospect. The application of the Lycojaponicumin B in the preparation of the colorectal 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 colorectal cancer cell inhibiting activity of the Lycojaponicumin B is previously unimagined.
Description
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 resistive connection rectal cancer medicine.
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 Letters14 (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 colorectal cancer medicine belongs to open first, and because framework types belongs to brand-new framework types, there do not is the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control for colorectal 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 resistive connection rectal cancer medicine, and the structural formula of Lycojaponicumin B is as shown in formula I:
The present invention finds by external MTT anti-tumor activity evaluation, and Lycojaponicumin B also has significant inhibitory action to the growth of Human colorectal cancer cells strain LOVE1, LoVo, SW620 and SW480, suppresses the IC of this 4 strain Growth of Cells
50value is respectively 1.21 ± 0.11 μ M, 2.35 ± 0.21 μ M, 0.79 ± 0.07 μ M and 2.86 ± 0.22 μ M.Therefore, Lycojaponicumin B can, for the preparation of resistive connection rectal cancer medicine, have good development prospect.
The purposes of the Lycojaponicumin B the present invention relates in preparation treatment colorectal cancer medicine belongs to open first, and because framework types belongs to brand-new framework types, there do not is the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control for colorectal 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 Letters14 (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 colorectal cancer cells strain
1. method: in the cell of growth logarithmic (log) phase: Human colorectal cancer cells strain LOVE1, LoVo, SW620 and SW480(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 Lycojaponicumin B 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: Lycojaponicumin B has significant inhibitory action to the growth of Human colorectal cancer cells strain LOVE1, LoVo, SW620 and SW480.This compound suppresses the IC of Human colorectal cancer cells strain LOVE1, LoVo, SW620 and SW480 growth
50value is respectively: 1.21 ± 0.11 μ M, 2.35 ± 0.21 μ M, 0.79 ± 0.07 μ M and 2.86 ± 0.22 μ M.
By above-described embodiment, shown, Lycojaponicumin B of the present invention has good inhibitory action to the growth of Human colorectal cancer cells strain LOVE1, LoVo, SW620 and SW480.Prove thus, Lycojaponicumin B of the present invention has resistive connection rectal cancer activity, can be for the preparation of resistive connection rectal cancer medicine.
Claims (1)
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CN 201310435097 CN103446123A (en) | 2013-09-23 | 2013-09-23 | Application of Lycojaponicumin B in colorectal cancer treatment drug |
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CN 201310435097 CN103446123A (en) | 2013-09-23 | 2013-09-23 | Application of Lycojaponicumin B in colorectal cancer treatment drug |
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CN 201310435097 Pending CN103446123A (en) | 2013-09-23 | 2013-09-23 | Application of Lycojaponicumin B in colorectal cancer treatment drug |
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Application publication date: 20131218 |