CN103463045A - Application of Lycojaponicumin A in drugs for treating ileocecal carcinoma - Google Patents
Application of Lycojaponicumin A in drugs for treating ileocecal carcinoma Download PDFInfo
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- CN103463045A CN103463045A CN2013104366474A CN201310436647A CN103463045A CN 103463045 A CN103463045 A CN 103463045A CN 2013104366474 A CN2013104366474 A CN 2013104366474A CN 201310436647 A CN201310436647 A CN 201310436647A CN 103463045 A CN103463045 A CN 103463045A
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- lycojaponicumin
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Abstract
The invention discloses application of Lycojaponicumin A in preparation of drugs for treating ileocecal carcinoma and belongs to the technical field of new application of drugs. In vitro MTT anticancer activity evaluation discovers that Lycojaponicumin A shows remarkable inhibitory effects on growth of a human ileocecal carcinoma cell line HCT-8. Therefore, the Lycojaponicumin A can be used for preparing anti-ileocecal carcinoma drugs and has good development and application prospects. Application of the Lycojaponicumin A in preparation of drugs for treating ileocecal carcinoma is disclosed for the first time; and because skeleton type is completely new, inhibitory activity on human ileocecal carcinoma cells is extraordinary strong.
Description
Technical field
The present invention relates to the new purposes of compound L ycojaponicumin A, relate in particular to the application of Lycojaponicumin A in the anti-ileocecum cancer drug 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 L ycojaponicumin A 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 A the present invention relates in preparation treatment ileocecum cancer drug belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for the ileocecum cancerous 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 the ileocecum cancer simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of compound L ycojaponicumin A in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Lycojaponicumin A in the anti-ileocecum cancer drug of preparation, and the structural formula of Lycojaponicumin A is as shown in formula I:
The present invention finds by external MTT anti-tumor activity evaluation, and Lycojaponicumin A also has significant inhibitory action to the growth of human ileocecal carcinoma cell strain HCT-8, suppresses the IC of this 1 strain Growth of Cells
50value is 1.15 ± 0.17 μ M.Therefore, Lycojaponicumin A can, for the preparation of anti-ileocecum cancer drug, have good development prospect.
The purposes of the Lycojaponicumin A the present invention relates in preparation treatment ileocecum cancer drug belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for the ileocecum cancerous 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 the ileocecum 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 A 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 A tablet involved in the present invention:
Get 20 and digest compound Lycojaponicumin A, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound L ycojaponicumin A capsule involved in the present invention:
Get 20 and digest compound Lycojaponicumin 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 Lycojaponicumin A to the human ileocecal carcinoma cell strain
1. method: in the cell of growth logarithmic (log) phase: human ileocecal carcinoma cell strain HCT-8(buys 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, 0.01 μ M, 0.001 μ M, the culture medium of the Lycojaponicumin A of 0.0001 μ M and 0.00001 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 A has significant inhibitory action to the growth of human ileocecal carcinoma cell strain HCT-8.This compound suppresses the IC of human ileocecal carcinoma cell strain HCT-8 growth
50value is: 1.15 ± 0.17 μ M.
By above-described embodiment, shown, Lycojaponicumin A of the present invention has good inhibitory action to the growth of human ileocecal carcinoma cell strain HCT-8.Prove thus, Lycojaponicumin A of the present invention has anti-ileocecum cancer activity, can be for the preparation of anti-ileocecum cancer drug.
Claims (1)
1.Lycojaponicumin the application of A in treatment ileocecum cancer drug, described compound L ycojaponicumin A structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310436647.4A CN103463045B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin A in preparation treatment blindgut cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310436647.4A CN103463045B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin A in preparation treatment blindgut cancer |
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| CN103463045A true CN103463045A (en) | 2013-12-25 |
| CN103463045B CN103463045B (en) | 2015-08-19 |
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| CN201310436647.4A Active CN103463045B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin A in preparation treatment blindgut cancer |
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Citations (1)
| 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 |
-
2013
- 2013-09-23 CN CN201310436647.4A patent/CN103463045B/en active Active
Patent Citations (1)
| 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 (2)
| Title |
|---|
| WANG XIAOJING等: "Nine new lycopodine-type alkaloids from Lycopodium japonicum", 《TETRAHEDRON》, vol. 69, 13 May 2013 (2013-05-13), pages 1 * |
| XIAO-JING WANG,ET AL.: "Lycojaponicumin 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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| CN103463045B (en) | 2015-08-19 |
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Address after: Tiefu iron rich street Pizhou city 221331 Jiangsu city of Xuzhou Province Patentee after: Nanjing Guangkangxie Biomedical Technology 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. |
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Inventor after: Zhang Fusheng Inventor before: Jiang Chunping Inventor before: Wang Zezheng |
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Effective date of registration: 20171227 Address after: The 404600 Chongqing city Fengjie County Zhenping on Village 7 Patentee after: FENGJIE DONGYANG BUILDING MATERIALS CO., LTD. Address before: Tiefu iron rich street Pizhou city 221331 Jiangsu city of Xuzhou Province Patentee before: Nanjing Guangkangxie Biomedical Technology Co., Ltd. |