CN103463058B - The application of Lycojaponicumin A in treatment cancer of biliary duct medicine - Google Patents
The application of Lycojaponicumin A in treatment cancer of biliary duct medicine Download PDFInfo
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- CN103463058B CN103463058B CN201310443201.4A CN201310443201A CN103463058B CN 103463058 B CN103463058 B CN 103463058B CN 201310443201 A CN201310443201 A CN 201310443201A CN 103463058 B CN103463058 B CN 103463058B
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Abstract
The invention discloses the application of Lycojaponicumin A in preparation treatment human bile duct cancer medicine, belong to technical field of new application of medicine.The present invention is found by external MTT antineoplastic activity evaluation, and the growth of Lycojaponicumin A to human bile duct carcinoma strain RBE also has significant inhibitory action.Therefore, Lycojaponicumin A for the preparation of anti-cancer of biliary duct medicine, can have good development prospect.Belong to first public for the purposes of the Lycojaponicumin A that the present invention relates in preparation treatment human bile duct cancer medicine, because framework types belongs to brand-new framework types, and its inhibit activities for human bile duct carcinoma is unexpectedly strong.
Description
Technical field
The present invention relates to the novelty teabag of compound L ycojaponicumin A, particularly relate to the application of Lycojaponicumin A in the anti-cancer of biliary duct medicine of preparation.
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 A 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 Unprecedented Skeleton fromLycopodium japonicum.Organic Letters14 (10), New skeleton compound 2614-2617.), this compound has brand-new framework types, the purposes in preparation treatment cancer of biliary duct medicine that the present invention relates to is belonged to first public, because framework types belongs to brand-new framework types, and its inhibit activities for cholangiocarcinoma cell is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control simultaneously for cancer of biliary duct obviously has significant progress.
Summary of the invention
The invention provides compound L ycojaponicumin A and prepare the application in antitumor drug.
The present invention adopts following technical scheme: the application of Lycojaponicumin A in the anti-cancer of biliary duct medicine of preparation, and the structural formula of Lycojaponicumin A is as shown in formula I:
The present invention is found by external MTT antineoplastic activity evaluation, and the growth of Lycojaponicumin A to human bile duct carcinoma strain RBE also has significant inhibitory action, suppresses the IC of this 1 strain Growth of Cells
50value is 4.67 ± 0.33 μMs.Therefore, Lycojaponicumin A for the preparation of anti-cancer of biliary duct medicine, can have good development prospect.
The purposes of the Lycojaponicumin A that the present invention relates in preparation treatment cancer of biliary duct medicine belongs to first public, because framework types belongs to brand-new framework types, and its inhibit activities for cholangiocarcinoma 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 cancer of biliary duct 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 A involved in the present invention is see 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 by 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 g of compound Lycojaponicumin A, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound L ycojaponicumin A capsule involved in the present invention:
Get 20 g of compound Lycojaponicumin A, 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 A to the growth inhibited effect of human bile duct carcinoma strain
1. method: the cell being in growth logarithmic (log) phase: human bile duct carcinoma strain RBE(buys from Chinese Academy of Sciences's cell bank) 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 LycojaponicuminA 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 A to human bile duct carcinoma strain RBE has significant inhibitory action.This compound suppresses the IC of human bile duct carcinoma strain RBE growth
50value is: 4.67 ± 0.33 μMs.
Shown by above-described embodiment, the growth of Lycojaponicumin A of the present invention to human bile duct carcinoma strain RBE has good inhibitory action.Prove thus, it is active that Lycojaponicumin A of the present invention has anti-cancer of biliary duct, can for the preparation of anti-cancer of biliary duct medicine.
Claims (1)
- The application of 1.Lycojaponicumin A in preparation treatment cancer of biliary duct medicine, described compound L ycojaponicumin A structure as formula Ishown in:formula I.
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| CN201310443201.4A CN103463058B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin A in treatment cancer of biliary duct medicine |
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| CN103463058A CN103463058A (en) | 2013-12-25 |
| CN103463058B true CN103463058B (en) | 2015-08-19 |
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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 |
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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 (1)
| Title |
|---|
| Nine new lycopodine-type alkaloids from Lycopodium japonicum;WANG Xiaojing等;《tetrahedron》;20130513;第69卷;6234-6240 * |
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Address after: 546200 building 3, Chengnan Industrial Park, Chengguan Town, Xincheng County, Laibin City, Guangxi Zhuang Autonomous Region Patentee after: Wang Xiaoyan Address before: No. 45 Beihai 536000 the Guangxi Zhuang Autonomous Region jinhaian Road (Beihai high tech Zone) Patentee before: Wang Xiaoyan |
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