CN103463034B - The application of Lycojaponicumin B in preparation treatment ovarian cancer - Google Patents
The application of Lycojaponicumin B in preparation treatment ovarian cancer Download PDFInfo
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- CN103463034B CN103463034B CN201310436194.5A CN201310436194A CN103463034B CN 103463034 B CN103463034 B CN 103463034B CN 201310436194 A CN201310436194 A CN 201310436194A CN 103463034 B CN103463034 B CN 103463034B
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- ovarian cancer
- lycojaponicumin
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- preparation treatment
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- 206010033128 Ovarian cancer Diseases 0.000 title claims abstract description 17
- 206010061535 Ovarian neoplasm Diseases 0.000 title claims abstract description 17
- 238000002360 preparation method Methods 0.000 title claims abstract description 13
- 229930185194 lycojaponicumin Natural products 0.000 title abstract description 6
- 150000001875 compounds Chemical class 0.000 claims description 16
- 239000003814 drug Substances 0.000 abstract description 12
- 230000012010 growth Effects 0.000 abstract description 7
- 108700024827 HOC1 Proteins 0.000 abstract description 6
- 101100178273 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) HOC1 gene Proteins 0.000 abstract description 6
- 230000000694 effects Effects 0.000 abstract description 6
- 230000002401 inhibitory effect Effects 0.000 abstract description 4
- 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
- 230000002611 ovarian Effects 0.000 abstract 1
- 230000035755 proliferation Effects 0.000 abstract 1
- 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
- PZRZBYZBJWANQI-MZBWQEOASA-N C[C@@H](C[C@H]1[C@H]([C@H]2O)O)C[C@]1(CC[C@@H]1NCC3)[C@]21[C@H]3P Chemical compound C[C@@H](C[C@H]1[C@H]([C@H]2O)O)C[C@]1(CC[C@@H]1NCC3)[C@]21[C@H]3P PZRZBYZBJWANQI-MZBWQEOASA-N 0.000 description 1
- 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
Abstract
Do you the invention discloses Lycojaponicumin? the application of B in preparation treatment human ovarian cancer medicine, belongs to technical field of new application of medicine.Is the present invention found by external MTT antineoplastic activity evaluation, Lycojaponicumin? B also has significant inhibitory action to the growth of human oophoroma cell line HO-8910, HOC1 and OVAC.Therefore, Lycojaponicumin? B for the preparation of ovarian cancer resistance medicament, can have good development prospect.For the Lycojaponicumin that the present invention relates to? the purposes of B in preparation treatment human ovarian cancer medicine belongs to first public, and because framework types belongs to brand-new framework types, and its inhibit activities for Proliferation of Human Ovarian Cell is unexpectedly strong.
Description
Technical field
The present invention relates to the novelty teabag of compound L ycojaponicuminB, particularly relate to LycojaponicuminB and preparing the application in ovarian cancer resistance medicament.
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 ycojaponicuminB 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 LycojaponicuminB that the present invention relates in preparation treatment ovarian cancer is belonged to first public, because framework types belongs to brand-new framework types, and its inhibit activities for ovarian 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 ovarian cancer obviously has significant progress.
Summary of the invention
The invention provides compound L ycojaponicuminB and prepare the application in antitumor drug.
The present invention adopts following technical scheme: LycojaponicuminB is preparing the application in ovarian cancer resistance medicament, and the structural formula of LycojaponicuminB is as shown in formula I:
The present invention is found by external MTT antineoplastic activity evaluation, and LycojaponicuminB also has significant inhibitory action to the growth of human oophoroma cell line HO-8910, HOC1 and OVAC, suppresses the IC of this 3 strain Growth of Cells
50value is respectively 1.21 ± 0.11 μMs, 2.37 ± 0.14 μMs and 2.14 ± 0.12 μMs.Therefore, LycojaponicuminB for the preparation of ovarian cancer resistance medicament, can have good development prospect.
The purposes of the LycojaponicuminB that the present invention relates in preparation treatment ovarian cancer belongs to first public, because framework types belongs to brand-new framework types, and its inhibit activities for ovarian 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 ovarian cancer 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 ycojaponicuminB 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 ycojaponicuminB tablet involved in the present invention:
Get 20 g of compound LycojaponicuminB, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound L ycojaponicuminB capsule involved in the present invention:
Get 20 g of compound LycojaponicuminB, 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 LycojaponicuminB to the growth inhibited effect of human oophoroma cell line
1. method: the cell being in growth logarithmic (log) phase: human oophoroma cell line HO-8910, HOC1 and OVAC (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 LycojaponicuminB 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: LycojaponicuminB to human oophoroma cell line HO-8910, HOC1 and OVAC has significant inhibitory action.This compound suppresses the IC of human oophoroma cell line HO-8910, HOC1 and OVAC growth
50value is respectively: 1.21 ± 0.11 μMs, 2.37 ± 0.14 μMs and 2.14 ± 0.12 μMs.
Shown by above-described embodiment, the growth of LycojaponicuminB of the present invention to human oophoroma cell line HO-8910, HOC1 and OVAC has good inhibitory action.Prove thus, LycojaponicuminB of the present invention has ovarian cancer resistance activity, can for the preparation of ovarian cancer resistance medicament.
Claims (1)
1.LycojaponicuminB preparation treatment ovarian cancer in application, described compound L ycojaponicuminB structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310436194.5A CN103463034B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin B in preparation treatment ovarian cancer |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310436194.5A CN103463034B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin B in preparation treatment ovarian cancer |
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| Publication Number | Publication Date |
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| CN103463034A CN103463034A (en) | 2013-12-25 |
| CN103463034B true CN103463034B (en) | 2015-12-02 |
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|---|---|---|---|
| CN201310436194.5A Active CN103463034B (en) | 2013-09-23 | 2013-09-23 | The application of Lycojaponicumin B in preparation treatment ovarian cancer |
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| Country | Link |
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| CN (1) | CN103463034B (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 CN201310436194.5A patent/CN103463034B/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 (1)
| Title |
|---|
| Lycojaponicumins A-c,Three Alkaloids with an Unprecedented Skeleton from Lycopodium japonicum;Xiao-Jing Wang, et al;《Organic Letters》;20120508;第14卷(第10期);第2614-2617页 * |
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| Publication number | Publication date |
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| CN103463034A (en) | 2013-12-25 |
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Effective date of registration: 20151103 Address after: 325011, building 1112, building A, 209 Wenchang Road, hi tech Zone, Longwan District, Zhejiang, Wenzhou Applicant after: Wenzhou Chengqiao 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 Applicant before: Nanjing Guangkangxie Biomedical Technology Co., Ltd. |
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