CN103520178B - The application of a kind of compound in preparation treatment ovarian cancer - Google Patents
The application of a kind of compound in preparation treatment ovarian cancer Download PDFInfo
- Publication number
- CN103520178B CN103520178B CN201310530481.2A CN201310530481A CN103520178B CN 103520178 B CN103520178 B CN 103520178B CN 201310530481 A CN201310530481 A CN 201310530481A CN 103520178 B CN103520178 B CN 103520178B
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- ovarian cancer
- compound
- asperterpenols
- preparation treatment
- present
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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
- 150000001875 compounds Chemical class 0.000 title claims abstract description 14
- 238000002360 preparation method Methods 0.000 title claims abstract description 14
- 239000003814 drug Substances 0.000 abstract description 9
- 230000000694 effects Effects 0.000 abstract description 7
- 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
- 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
- 229930183110 asperterpenol Natural products 0.000 abstract 4
- 229940079593 drug Drugs 0.000 description 4
- 239000001963 growth medium Substances 0.000 description 3
- 206010028980 Neoplasm Diseases 0.000 description 2
- 239000002246 antineoplastic agent Substances 0.000 description 2
- 229940041181 antineoplastic drug Drugs 0.000 description 2
- 201000011510 cancer Diseases 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
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 241001597008 Nomeidae Species 0.000 description 1
- 229930012538 Paclitaxel Natural products 0.000 description 1
- 206010039966 Senile dementia Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 description 1
- 229960004373 acetylcholine Drugs 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
- 239000002775 capsule Substances 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 230000010261 cell growth Effects 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 239000012531 culture fluid Substances 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000002329 esterase inhibitor Substances 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
- 238000011160 research Methods 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
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses the application of a kind of compound in preparation treatment ovarian cancer, does is compound Asperterpenols? A, belongs to technical field of new application of medicine.Is the present invention found by external MTT antineoplastic activity evaluation, Asperterpenols? A also has significant inhibitory action to the growth of human oophoroma cell line HO-8910, HOC1 and OVAC.Therefore, Asperterpenols? A for the preparation of ovarian cancer resistance medicament, can have good development prospect.For the Asperterpenols that the present invention relates to? the purposes of A in preparation treatment ovarian cancer belongs to first public, and its inhibit activities for ovarian cancer cell is strong, has significant progress.
Description
Technical field
The present invention relates to a kind of novelty teabag of compound, particularly relate to the application of AsperterpenolsA in preparation treatment ovarian cancer.
Background technology
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 compd A sperterpenolsA that the present invention relates to be one within 2013, deliver (Ze ' enXiao, etal., AsperterpenolsAandB, NewSesterterpenoidsIsolatedfromaMangroveEndophyticFungus Aspergillussp.085242.OrganicLetters, 2013, 15(10) 2522 – 2525.) noval chemical compound, this compound has brand-new framework types, this compound energy acetylcholine esterase inhibition, have anti-senile dementia effect (Ze ' enXiao, etal., AsperterpenolsAandB, NewSesterterpenoidsIsolatedfromaMangroveEndophyticFungus Aspergillussp.085242.OrganicLetters, 2013, 15(10) 2522 – 2525.), the purposes of the AsperterpenolsA that the present invention relates in preparation treatment ovarian cancer belongs to first public.
Summary of the invention
The object of the invention is to not find that it has the present situation of the report of ovarian cancer resistance activity according in existing AsperterpenolsA research, provide AsperterpenolsA and preparing the application in ovarian cancer resistance medicament.
Described compd A sperterpenolsA structure is as shown in formula I:
Formula I
The present invention is found by external MTT antineoplastic activity evaluation, AsperterpenolsA also has significant inhibitory action to the growth of human oophoroma cell line HO-8910, HOC1 and OVAC, suppresses the IC50 value of this 3 strain Growth of Cells to be respectively 3.64 ± 1.36 μMs, 4.75 ± 1.37 μMs and 1.65 ± 0.36 μMs.Therefore, AsperterpenolsA for the preparation of ovarian cancer resistance medicament, can have good development prospect.
The purposes of the AsperterpenolsA 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 strong, 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 compd A sperterpenolsA involved in the present invention see document (Ze ' enXiao, etal., AsperterpenolsAandB, NewSesterterpenoidsIsolatedfromaMangroveEndophyticFungus Aspergillussp.085242.OrganicLetters, 2013,15(10) 2522 – 2525.)
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 compd A sperterpenolsA tablet involved in the present invention:
Get 5 g of compound AsperterpenolsA, add 195 grams, dextrin, mixing, Conventional compression makes 1000.
Embodiment 2: the preparation of compd A sperterpenolsA capsule involved in the present invention:
Get 5 g of compound AsperterpenolsA, add starch 195 grams, mixing, encapsulatedly makes 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example: adopt mtt assay assessing compound AsperterpenolsA 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(buy 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 AsperterpenolsA of 0.01 μM and 0.001 μM.After cultivating 48h, add the MTT of concentration 5mg/mL, continue to be put in CO2 incubator and cultivate 4h, then 100 μ L supernatants are sucked along culture fluid top, add 100 μ LDMSO, 10min is placed in dark place, utilizes microplate reader (Sunrise Products) 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: AsperterpenolsA to human oophoroma cell line HO-8910, HOC1 and OVAC has significant inhibitory action.This compound suppresses the IC50 value of human oophoroma cell line HO-8910, HOC1 and OVAC growth to be respectively 3.64 ± 1.36 μMs, 4.75 ± 1.37 μMs and 1.65 ± 0.36 μMs.
Shown by above-described embodiment, the growth of AsperterpenolsA of the present invention to human oophoroma cell line HO-8910, HOC1 and OVAC has good inhibitory action.Prove thus, AsperterpenolsA of the present invention has ovarian cancer resistance activity, can for the preparation of ovarian cancer resistance medicament.
Claims (1)
1. the application of compound in preparation treatment ovarian cancer, described compd A sperterpenolsA structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310530481.2A CN103520178B (en) | 2013-10-30 | 2013-10-30 | The application of a kind of compound in preparation treatment ovarian cancer |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310530481.2A CN103520178B (en) | 2013-10-30 | 2013-10-30 | The application of a kind of compound in preparation treatment ovarian cancer |
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| Publication Number | Publication Date |
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| CN103520178A CN103520178A (en) | 2014-01-22 |
| CN103520178B true CN103520178B (en) | 2016-04-13 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310530481.2A Active CN103520178B (en) | 2013-10-30 | 2013-10-30 | The application of a kind of compound in preparation treatment ovarian cancer |
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| Country | Link |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102181370A (en) * | 2011-03-16 | 2011-09-14 | 中山大学 | South China sea mangrove endophytic fungus BL321 |
-
2013
- 2013-10-30 CN CN201310530481.2A patent/CN103520178B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102181370A (en) * | 2011-03-16 | 2011-09-14 | 中山大学 | South China sea mangrove endophytic fungus BL321 |
Non-Patent Citations (1)
| Title |
|---|
| Asperterpenols A and B,New Sesterterpenoids Isolated from a Mangrove Endophytic Fungus Aspergillus sp.085242;Ze’en Xiao,et al;《Organic Letters》;20130502;第15卷(第10期);2522–2525 * |
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| Publication number | Publication date |
|---|---|
| CN103520178A (en) | 2014-01-22 |
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Inventor after: Wang Xianrong Inventor before: Zhang Guanlian |
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Effective date of registration: 20160323 Address after: 311827 Zhejiang city of Shaoxing province Zhuji City Road No. 32 two floor in town Applicant after: Wang Xianrong Address before: The 1 group of Yiwu city residential streets in Zhejiang province Jinhua City mountain village 322008 Applicant before: Zhang Guanlian |
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Inventor after: Wang Xuegen Inventor after: Ye Qing Inventor after: Lv Huimin Inventor after: Chen Ding Inventor after: Sun Yijun Inventor before: Wang Xianrong |
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Effective date of registration: 20170307 Address after: Jiangning Science Park Road, Jiangning District of Nanjing city and Jiangsu province 211100 No. 18 Building No. 6 Patentee after: Jiangsu Kaiji biological technology Limited by Share Ltd Address before: 311827 Zhejiang city of Shaoxing province Zhuji City Road No. 32 two floor in town Patentee before: Wang Xianrong |
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