CN105287521A - Application of Nagelamides Y in preparation of endometrial cancer treating medicine - Google Patents
Application of Nagelamides Y in preparation of endometrial cancer treating medicine Download PDFInfo
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- CN105287521A CN105287521A CN201510745379.3A CN201510745379A CN105287521A CN 105287521 A CN105287521 A CN 105287521A CN 201510745379 A CN201510745379 A CN 201510745379A CN 105287521 A CN105287521 A CN 105287521A
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- endometrial cancer
- nagelamides
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Abstract
The invention discloses application of Nagelamides Y in preparation of endometrial cancer treating medicine, and belongs to the technical field of new medicine application. It is found through in-vitro MTT antineoplastic activity evaluation that Nagelamides Y has a remarkable effect on restraining growth of human endometrial cancer cell strains ISK and RL95-2. Thus, Nagelamides Y can be used for preparing endometrial cancer resisting medicine and has good development and application prospects. The application of Nagelamides Y in preparation of endometrial cancer treating medicine is disclosed for the first time, and Nagelamides Y is unexpectedly high in endometrial cancer cell restraining activity.
Description
Technical field
The present invention relates to the novelty teabag of compound N agelamidesY, particularly relate to the application of NagelamidesY in preparation treatment endometrial cancer drug.
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 compound N agelamidesY that the present invention relates to is one and delivers (NaonobuTanaka in 2013, etal., NagelamidesXZ, DimericBromopyrroleAlkaloidsfromaMarineSpongeAgelassp.Or ganicLetters13 (15), 3262 – 3265.) noval chemical compound, this compound has brand-new framework types, current purposes only relates to antibacterial (NaonobuTanaka, etal., NagelamidesXZ, DimericBromopyrroleAlkaloidsfromaMarineSpongeAgelassp.Or ganicLetters13 (15), 3262 – 3265.), the purposes of the NagelamidesY that the present invention relates in preparation treatment endometrial cancer drug is belonged to first public, owing to belonging to brand-new structure type, and its inhibit activities for endometrial carcinoma cell is unexpectedly strong, there is not the possibility being provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control simultaneously for carcinoma of endometrium obviously has significant progress.
Summary of the invention
The object of the invention is to not find that it has the present situation of the report of anti-carcinoma of endometrium activity according in existing NagelamidesY research, provide the application of NagelamidesY in the anti-endometrial cancer drug of preparation.
Described compound N agelamidesY structure is as shown in formula I:
The present invention is found by external MTT antineoplastic activity evaluation, the growth of NagelamidesY to people's Endometrial carcinoma cell line ISK and RL95-2 also has significant inhibitory action, suppresses the IC50 value of this 2 strain Growth of Cells to be respectively 1.89 ± 0.26 μMs and 0.73 ± 0.52 μM.Therefore, NagelamidesY for the preparation of anti-endometrial cancer drug, can have good development prospect.
The purposes of the NagelamidesY that the present invention relates in preparation treatment endometrial cancer drug is belonged to first public, because framework types belongs to brand-new framework types, and its inhibit activities for endometrial carcinoma 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 carcinoma of endometrium 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 N agelamidesY involved in the present invention is see document (NaonobuTanaka, etal., NagelamidesXZ, DimericBromopyrroleAlkaloidsfromaMarineSpongeAgelassp.Or ganicLetters13 (15), 3262 – 3265.)
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 N agelamidesY tablet involved in the present invention:
Get 20 g of compound NagelamidesY and add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound N agelamidesY capsule involved in the present invention:
Get 20 g of compound NagelamidesY 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 NagelamidesY to the growth inhibited effect of people's Endometrial carcinoma cell line
1. method: the cell being in growth logarithmic (log) phase: people's Endometrial carcinoma cell line ISK and RL95-2 (buying from Chinese Academy of Sciences's cell bank) is 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 NagelamidesY 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: NagelamidesY to people's Endometrial carcinoma cell line PISK and RL95-2 has significant inhibitory action.This compound suppresses the IC50 value of people's Endometrial carcinoma cell line ISK and RL95-2 growth to be respectively 1.89 ± 0.26 μMs and 0.73 ± 0.52 μM.
Shown by above-described embodiment, the growth of NagelamidesY of the present invention to people's Endometrial carcinoma cell line ISK and RL95-2 has good inhibitory action.Prove thus, it is active that NagelamidesY of the present invention has anti-carcinoma of endometrium, can for the preparation of anti-endometrial cancer drug.
Claims (1)
- The application of 1.NagelamidesY in treatment endometrial cancer drug, described compound N agelamidesY structure is as shown in formula I:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510745379.3A CN105287521A (en) | 2015-11-05 | 2015-11-05 | Application of Nagelamides Y in preparation of endometrial cancer treating medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510745379.3A CN105287521A (en) | 2015-11-05 | 2015-11-05 | Application of Nagelamides Y in preparation of endometrial cancer treating medicine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105287521A true CN105287521A (en) | 2016-02-03 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510745379.3A Withdrawn CN105287521A (en) | 2015-11-05 | 2015-11-05 | Application of Nagelamides Y in preparation of endometrial cancer treating medicine |
Country Status (1)
| Country | Link |
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| CN (1) | CN105287521A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102861099A (en) * | 2012-10-27 | 2013-01-09 | 吴俊华 | Application of Houttuynoid D in medicine for treating endometrial cancer |
| CN103349668A (en) * | 2013-08-05 | 2013-10-16 | 淄博齐鼎立专利信息咨询有限公司 | Application of Polyflavanostilbene A in preparing drug for treating endometrial cancer |
-
2015
- 2015-11-05 CN CN201510745379.3A patent/CN105287521A/en not_active Withdrawn
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102861099A (en) * | 2012-10-27 | 2013-01-09 | 吴俊华 | Application of Houttuynoid D in medicine for treating endometrial cancer |
| CN103349668A (en) * | 2013-08-05 | 2013-10-16 | 淄博齐鼎立专利信息咨询有限公司 | Application of Polyflavanostilbene A in preparing drug for treating endometrial cancer |
Non-Patent Citations (1)
| Title |
|---|
| NAONOBU TANAKA，等: "Nagelamides X Z, Dimeric Bromopyrrole Alkaloids from a Marine Sponge Agelas sp.", 《ORGANIC LETTERS》 * |
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Application publication date: 20160203 |
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