CN103520175B - The application of a kind of compound in preparation treatment cervical cancer medicine - Google Patents
The application of a kind of compound in preparation treatment cervical cancer medicine Download PDFInfo
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- CN103520175B CN103520175B CN201310529111.7A CN201310529111A CN103520175B CN 103520175 B CN103520175 B CN 103520175B CN 201310529111 A CN201310529111 A CN 201310529111A CN 103520175 B CN103520175 B CN 103520175B
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- cervical cancer
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- asperterpenols
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Abstract
The invention discloses the application of a kind of compound in preparation treatment cervical cancer medicine, 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 cervical carcinoma cell lines HELA, HELA229, HCE1 and CASKI.Therefore, Asperterpenols? A for the preparation of medicament for resisting cervical cancer, can have good development prospect.For the Asperterpenols that the present invention relates to? the purposes of A in preparation treatment cervical cancer medicine belongs to first public, and its inhibit activities for cervical 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 compd A sperterpenolsA in preparation treatment cervical cancer medicine.
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 cervical cancer medicine 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 anti-cervical cancer activity according in existing AsperterpenolsA research, provide AsperterpenolsA and preparing the application in medicament for resisting cervical cancer.
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 cervical carcinoma cell lines HELA, HELA229, HCE1 and CASKI, suppresses the IC50 value of this 2 strain Growth of Cells to be respectively 4.14 ± 1.47 μMs, 4.25 ± 2.74 μMs, 5.78 ± 1.23 μMs and 4.85 ± 2.27 μMs.Therefore, AsperterpenolsA for the preparation of medicament for resisting cervical cancer, can have good development prospect.
The purposes of the AsperterpenolsA that the present invention relates in preparation treatment cervical cancer medicine is belonged to first public, because framework types belongs to brand-new framework types, and its inhibit activities for cervical cancer cell is strong, possess outstanding substantive distinguishing features, the control simultaneously for cervical 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 20 g of compound AsperterpenolsA, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compd A sperterpenolsA capsule involved in the present invention:
Get 20 g of compound AsperterpenolsA, 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 AsperterpenolsA to the growth inhibited effect of human cervical carcinoma cell lines
1. method: the cell being in growth logarithmic (log) phase: human cervical carcinoma cell lines HELA, HELA229, HCE1 and CASKI(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 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: AsperterpenolsA to human cervical carcinoma cell lines HELA, HELA229, HCE1 and CASKI has significant inhibitory action.This compound suppresses the IC50 value of human cervical carcinoma cell lines HELA, HELA229, HCE1 and CASKI growth to be respectively 4.14 ± 1.47 μMs, 4.25 ± 2.74 μMs, 5.78 ± 1.23 μMs and 4.85 ± 2.27 μMs.
Shown by above-described embodiment, the growth of AsperterpenolsA of the present invention to human cervical carcinoma cell lines HELA, HELA229, HCE1 and CASKI has good inhibitory action.Prove thus, AsperterpenolsA of the present invention has anti-cervical cancer activity, can for the preparation of medicament for resisting cervical cancer.
Claims (1)
1. the application of compound in preparation treatment cervical cancer medicine, described compd A sperterpenolsA structure is as shown in formula I:
Formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201310529111.7A CN103520175B (en) | 2013-10-31 | 2013-10-31 | The application of a kind of compound in preparation treatment cervical cancer medicine |
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| CN201310529111.7A CN103520175B (en) | 2013-10-31 | 2013-10-31 | The application of a kind of compound in preparation treatment cervical cancer medicine |
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| Publication Number | Publication Date |
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| CN103520175A CN103520175A (en) | 2014-01-22 |
| CN103520175B true CN103520175B (en) | 2016-04-13 |
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| CN201310529111.7A Active CN103520175B (en) | 2013-10-31 | 2013-10-31 | The application of a kind of compound in preparation treatment cervical cancer medicine |
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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 |
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2013
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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;20130502;《Organic Letters》;20130502;第15卷(第10期);2522–2525 * |
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| CN103520175A (en) | 2014-01-22 |
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| C41 | Transfer of patent application or patent right or utility model | ||
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Inventor after: Wang Xianrong Inventor before: Zhang Zhilian |
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Effective date of registration: 20160315 Address after: 311827 Zhejiang city of Shaoxing province Zhuji City Road No. 32 two floor in town Applicant after: Wang Xianrong Address before: The 3 groups after the deep Tangxia village of Yiwu city street 322008 Zhejiang city of Jinhua Province Applicant before: Zhang Zhilian |
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Inventor after: Mo Xiaojun Inventor after: Huang Mingjun Inventor before: Wang Xianrong |
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Effective date of registration: 20170118 Address after: Chancheng District of Guangdong city in Foshan province 528010 Tang Road No. 19 Room 301 Patentee after: Mo Xiaojun Address before: 311827 Zhejiang city of Shaoxing province Zhuji City Road No. 32 two floor in town Patentee before: Wang Xianrong |