CN103463044B - The application of Lycojaponicumin A in preparation treatment skin carcinoma medicine - Google Patents
The application of Lycojaponicumin A in preparation treatment skin carcinoma medicine Download PDFInfo
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- CN103463044B CN103463044B CN201310436646.XA CN201310436646A CN103463044B CN 103463044 B CN103463044 B CN 103463044B CN 201310436646 A CN201310436646 A CN 201310436646A CN 103463044 B CN103463044 B CN 103463044B
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- Prior art keywords
- lycojaponicumin
- application
- skin carcinoma
- preparation treatment
- medicine
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- 201000000849 skin cancer Diseases 0.000 title claims abstract description 18
- 239000003814 drug Substances 0.000 title claims abstract description 17
- 238000002360 preparation method Methods 0.000 title claims abstract description 15
- 201000008261 skin carcinoma Diseases 0.000 title claims abstract description 15
- WGVQKABRYXBLGW-WUZBVLBZSA-N (1R,2S,5S,7S,10S,13S)-7-hydroxy-7-methyl-17-oxa-14-azapentacyclo[12.2.1.02,10.02,13.05,10]heptadecane-3,9-dione Chemical compound O=C([C@@]12CC3)C[C@@](C)(O)C[C@H]1CC(=O)[C@@]12[C@H]3N2CC[C@H]1O2 WGVQKABRYXBLGW-WUZBVLBZSA-N 0.000 title claims description 17
- 150000001875 compounds Chemical class 0.000 claims description 16
- 230000012010 growth Effects 0.000 abstract description 7
- 102100027833 14-3-3 protein sigma Human genes 0.000 abstract description 6
- 101100107350 Homo sapiens SFN gene Proteins 0.000 abstract description 6
- 230000000694 effects Effects 0.000 abstract description 5
- 230000002401 inhibitory effect Effects 0.000 abstract description 4
- 208000000453 Skin Neoplasms Diseases 0.000 abstract description 3
- 230000000118 anti-neoplastic effect Effects 0.000 abstract description 2
- 238000011161 development Methods 0.000 abstract description 2
- 238000011156 evaluation Methods 0.000 abstract description 2
- 229930185194 lycojaponicumin Natural products 0.000 abstract 4
- 229940079593 drug Drugs 0.000 description 4
- 239000002246 antineoplastic agent Substances 0.000 description 3
- 229940041181 antineoplastic drug Drugs 0.000 description 3
- 239000001963 growth medium Substances 0.000 description 3
- 206010028980 Neoplasm Diseases 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 230000031700 light absorption Effects 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 229930014626 natural product Natural products 0.000 description 2
- 230000004083 survival effect Effects 0.000 description 2
- 241001597008 Nomeidae Species 0.000 description 1
- 229930012538 Paclitaxel Natural products 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 230000001464 adherent effect Effects 0.000 description 1
- 230000001093 anti-cancer Effects 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 230000010261 cell growth Effects 0.000 description 1
- 239000012531 culture fluid Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 231100000206 health hazard Toxicity 0.000 description 1
- 150000002611 lead compounds Chemical class 0.000 description 1
- 238000011275 oncology therapy Methods 0.000 description 1
- 229960001592 paclitaxel Drugs 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Do you the invention discloses Lycojaponicumin? the application of A in preparation treatment skin carcinoma medicine, belongs to technical field of new application of medicine.Is the present invention found by external MTT antineoplastic activity evaluation, Lycojaponicumin? A also has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23.Therefore, Lycojaponicumin? A for the preparation of anti-skin carcinoma medicine, can have good development prospect.For the Lycojaponicumin that the present invention relates to? the purposes of A in preparation treatment skin carcinoma medicine belongs to first public, and because framework types belongs to brand-new framework types, and its inhibit activities for skin cancer cell is unexpectedly strong.
Description
Technical field
The present invention relates to the novelty teabag of compound L ycojaponicuminA, particularly relate to the application of LycojaponicuminA in the anti-skin carcinoma 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 ycojaponicuminA that the present invention relates to is one and delivers (Wang in 2012, X.J.etal., 2012.LycojaponicuminsA-C, ThreeAlkaloidswithanUnprecedentedSkeletonfromLycopodiumj aponicum.OrganicLetters14 (10), New skeleton compound 2614-2617.), this compound has brand-new framework types, the purposes of the LycojaponicuminA that the present invention relates in preparation treatment skin carcinoma medicine is belonged to first public, because framework types belongs to brand-new framework types, and its inhibit activities for skin 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 skin carcinoma obviously has significant progress.
Summary of the invention
The invention provides compound L ycojaponicuminA and prepare the application in antitumor drug.
The present invention adopts following technical scheme: the application of LycojaponicuminA in the anti-skin carcinoma medicine of preparation, and the structural formula of LycojaponicuminA is as shown in formula I:
The present invention is found by external MTT antineoplastic activity evaluation, and LycojaponicuminA also has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23, suppresses the IC of this 4 strain Growth of Cells
50value is respectively 1.23 ± 0.03 μMs, 1.13 ± 0.05 μMs, 2.22 ± 0.08 μMs and 1.17 ± 0.11 μMs.Therefore, LycojaponicuminA for the preparation of anti-skin carcinoma medicine, can have good development prospect.
The purposes of the LycojaponicuminA that the present invention relates in preparation treatment skin carcinoma medicine belongs to first public, because framework types belongs to brand-new framework types, and its inhibit activities for skin 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 skin 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 ycojaponicuminA involved in the present invention is see document (Wang, X.J.etal., 2012.LycojaponicuminsA-C, ThreeAlkaloidswithanUnprecedentedSkeletonfromLycopodiumj aponicum.OrganicLetters14 (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 ycojaponicuminA tablet involved in the present invention:
Get 20 g of compound LycojaponicuminA, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound L ycojaponicuminA capsule involved in the present invention:
Get 20 g of compound LycojaponicuminA, 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 LycojaponicuminA to the growth inhibited effect of application on human skin JEG-3
1. method: the cell being in growth logarithmic (log) phase: application on human skin JEG-3 A431, HME1, A375 and SK23 (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 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 LDMSO, 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. the growth of result: LycojaponicuminA to application on human skin JEG-3 A431, HME1, A375 and SK23 has significant inhibitory action.This compound suppresses the IC of application on human skin JEG-3 A431, HME1, A375 and SK23 growth
50value is respectively: 1.23 ± 0.03 μMs, 1.13 ± 0.05 μMs, 2.22 ± 0.08 μMs and 1.17 ± 0.11 μMs.
Shown by above-described embodiment, the growth of LycojaponicuminA of the present invention to application on human skin JEG-3 A431, HME1, A375 and SK23 has good inhibitory action.Prove thus, it is active that LycojaponicuminA of the present invention has anti-skin carcinoma, can for the preparation of anti-skin carcinoma medicine.
Claims (1)
- The application of 1.LycojaponicuminA in preparation treatment skin carcinoma medicine, described compound L ycojaponicuminA structure as formula Ishown in:formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310436646.XA CN103463044B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin A in preparation treatment skin carcinoma medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310436646.XA CN103463044B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin A in preparation treatment skin carcinoma medicine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103463044A CN103463044A (en) | 2013-12-25 |
| CN103463044B true CN103463044B (en) | 2015-12-09 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310436646.XA Expired - Fee Related CN103463044B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin A in preparation treatment skin carcinoma medicine |
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| Country | Link |
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| CN (1) | CN103463044B (en) |
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 CN201310436646.XA patent/CN103463044B/en not_active Expired - Fee Related
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 |
|---|
| Lycojaponicumins AC, Three Alkaloids;xiao-jing wang,etc;《organic letters》;20121231;第14卷(第10期);2614-2617 * |
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| Publication number | Publication date |
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| CN103463044A (en) | 2013-12-25 |
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Address after: 225327 Yongan City, Jiangsu province high port town of Taizhou Bridge Community Patentee after: Li Shulan Address before: 266000 Shandong province Qingdao city Licang District Road No. 1020 Laoshan two unit 302 Patentee before: Li Shulan |
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Effective date of registration: 20170911 Address after: Lotus area east high village 071000 Hebei city of Baoding province No. 153 Patentee after: Sun Shanshan Address before: 510640 Guangdong City, Tianhe District Province, No. five, road, public education building, unit 371-1, unit 2401 Patentee before: Guangdong Gaohang Intellectual Property Operation Co., Ltd. |
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Granted publication date: 20151209 Termination date: 20180923 |