CN103446143A - Application of Lycojaponicumin C in gastric cancer treatment drug - Google Patents
Application of Lycojaponicumin C in gastric cancer treatment drug Download PDFInfo
- Publication number
- CN103446143A CN103446143A CN2013104351479A CN201310435147A CN103446143A CN 103446143 A CN103446143 A CN 103446143A CN 2013104351479 A CN2013104351479 A CN 2013104351479A CN 201310435147 A CN201310435147 A CN 201310435147A CN 103446143 A CN103446143 A CN 103446143A
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- CN
- China
- Prior art keywords
- lycojaponicumin
- gastric cancer
- application
- preparation
- cancer treatment
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 208000005718 Stomach Neoplasms Diseases 0.000 title claims abstract description 25
- 206010017758 gastric cancer Diseases 0.000 title claims abstract description 25
- 201000011549 stomach cancer Diseases 0.000 title claims abstract description 25
- 239000003814 drug Substances 0.000 title claims abstract description 16
- UULHZQYEEKIMDO-CLROSIBMSA-N lycojaponicumin C Natural products CN1CCC[C@@]23[C@@H]1CC[C@]24[C@@H](CC3=O)C(=CCC4=O)C UULHZQYEEKIMDO-CLROSIBMSA-N 0.000 title abstract description 20
- 229940079593 drug Drugs 0.000 title abstract description 7
- 150000001875 compounds Chemical class 0.000 claims description 16
- 229930185194 lycojaponicumin Natural products 0.000 claims description 3
- 238000002360 preparation method Methods 0.000 abstract description 12
- 230000002401 inhibitory effect Effects 0.000 abstract description 4
- 230000000259 anti-tumor effect Effects 0.000 abstract description 2
- 238000011161 development Methods 0.000 abstract description 2
- 238000011156 evaluation Methods 0.000 abstract description 2
- AZKSAVLVSZKNRD-UHFFFAOYSA-M 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide Chemical compound [Br-].S1C(C)=C(C)N=C1[N+]1=NC(C=2C=CC=CC=2)=NN1C1=CC=CC=C1 AZKSAVLVSZKNRD-UHFFFAOYSA-M 0.000 abstract 2
- 239000003560 cancer drug Substances 0.000 abstract 1
- 230000000459 effect on growth Effects 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 230000012010 growth Effects 0.000 description 6
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- 239000002246 antineoplastic agent Substances 0.000 description 3
- 229940041181 antineoplastic drug Drugs 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 239000001963 growth medium Substances 0.000 description 3
- 241000927897 Lycopodium japonicum Species 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 229930013930 alkaloid Natural products 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 230000031700 light absorption Effects 0.000 description 2
- 239000000203 mixture Substances 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
- 238000000034 method Methods 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
- 238000012545 processing Methods 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
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses application of Lycojaponicumin C in preparation of a gastric 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 C also has remarkable inhabiting effect on growth of human gastric cancer cell strains HGC-27, MGC-803, BGC-823 and SGC-7901. Therefore, the Lycojaponicumin C can be used for preparation of an anti-gastric cancer drug and has good development and application prospect. The application of the Lycojaponicumin C in the preparation of the gastric 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 gastric cancer cell inhibiting activity of the Lycojaponicumin C is previously unimagined.
Description
Technical field
The present invention relates to the new purposes of compound L ycojaponicumin C, relate in particular to the application of Lycojaponicumin C in the anti-gastric cancer medicine 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 C 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, belong to open first for the purposes in preparation treatment gastric cancer medicine the present invention relates to, because framework types belongs to brand-new framework types, and its inhibition for stomach cancer 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 gastric cancer simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of compound L ycojaponicumin C in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Lycojaponicumin C in the anti-gastric cancer medicine of preparation, and the structural formula of Lycojaponicumin C is as shown in formula I:
The present invention finds by external MTT anti-tumor activity evaluation, and Lycojaponicumin C also has significant inhibitory action to the growth of human stomach cancer cell line HGC-27, MGC-803, BGC-823 and SGC-7901, suppresses the IC of this 4 strain Growth of Cells
50value is respectively 3.21 ± 0.33 μ M, 1.12 ± 0.17 μ M, 0.87 ± 0.07 μ M and 1.33 ± 0.19 μ M.Therefore, Lycojaponicumin C can, for the preparation of anti-gastric cancer medicine, have good development prospect.
Purposes for the Lycojaponicumin C the present invention relates in preparation treatment gastric cancer medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for stomach cancer 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 gastric 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 C 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 C tablet involved in the present invention:
Get 20 and digest compound Lycojaponicumin C, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of compound L ycojaponicumin C capsule involved in the present invention:
Get 20 and digest compound Lycojaponicumin C, 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 C to human stomach cancer cell line
1. method: in the cell of growth logarithmic (log) phase: human stomach cancer cell line HGC-27, MGC-803, BGC-823 and SGC-7901(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 C 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 C has significant inhibitory action to the growth of human stomach cancer cell line HGC-27, MGC-803, BGC-823 and SGC-7901.This compound suppresses the IC of human stomach cancer cell line HGC-27, MGC-803, BGC-823 and SGC-7901 growth
50value is respectively: 3.21 ± 0.33 μ M, 1.12 ± 0.17 μ M, 0.87 ± 0.07 μ M and 1.33 ± 0.19 μ M.
By above-described embodiment, shown, Lycojaponicumin C of the present invention has good inhibitory action to the growth of human stomach cancer cell line HGC-27, MGC-803, BGC-823 and SGC-7901.Prove thus, Lycojaponicumin C of the present invention has anti-gastric cancer activity, can be for the preparation of anti-gastric cancer medicine.
Claims (1)
1.Lycojaponicumin the application of C in treatment gastric cancer medicine, described compound L ycojaponicumin C-structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310435147.9A CN103446143B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin C in preparation treatment gastric cancer medicament |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310435147.9A CN103446143B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin C in preparation treatment gastric cancer medicament |
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| Publication Number | Publication Date |
|---|---|
| CN103446143A true CN103446143A (en) | 2013-12-18 |
| CN103446143B CN103446143B (en) | 2015-12-09 |
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|---|---|---|---|
| CN201310435147.9A Expired - Fee Related CN103446143B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin C in preparation treatment gastric cancer medicament |
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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 CN201310435147.9A patent/CN103446143B/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 |
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| Publication number | Publication date |
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| CN103446143B (en) | 2015-12-09 |
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| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C41 | Transfer of patent application or patent right or utility model | ||
| CB03 | Change of inventor or designer information |
Inventor after: Li Yanliang Inventor after: Chen Pengfei Inventor before: Wu Junhua Inventor before: Liu Yang |
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| COR | Change of bibliographic data | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20151030 Address after: Huaiyin District sunshine new road Ji'nan City, Shandong province 250022 No. 21 No. 52 No. 809 Applicant after: Li Yanliang Address before: Metro Technology Building No. 69 Olympic Avenue in Jianye District of Nanjing city in Jiangsu province 210019 01 5 storey buildings Applicant before: Nanjing Guangkangxie Biomedical Technology Co., Ltd. |
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Effective date of registration: 20160310 Address after: Huaiyin District of Ji'nan City, Shandong province 250022 Yan Ji Road, No. 440 Patentee after: Shandong Inst. of Tumor Prevention and Cure Address before: Huaiyin District sunshine new road Ji'nan City, Shandong province 250022 No. 21 No. 52 No. 809 Patentee before: Li Yanliang |
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| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20151209 Termination date: 20170923 |