CN105456262A - Application of Melodinine E in preparing medicine for treating endometrial cancer - Google Patents
Application of Melodinine E in preparing medicine for treating endometrial cancer Download PDFInfo
- Publication number
- CN105456262A CN105456262A CN201510930553.1A CN201510930553A CN105456262A CN 105456262 A CN105456262 A CN 105456262A CN 201510930553 A CN201510930553 A CN 201510930553A CN 105456262 A CN105456262 A CN 105456262A
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- CN
- China
- Prior art keywords
- melodininee
- endometrial cancer
- melodinine
- application
- compound
- 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.)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses an application of Melodinine E in preparing a medicine for treating endometrial cancer, belonging to the technical field of novel applications of medicines. The in-vitro MTT anti-tumor activity evaluation shows that Melodinine E has an obvious inhibiting effect for the growth of human endometrial cancer cell strains ISK and RL95-2. Therefore, Melodinine E can be used for preparing the medicine for treating endometrial cancer, and has good development and application prospects. The application of Melodinine E in preparing the medicine for treating endometrial cancer in the invention is disclosed for the first time, and the inhibiting activity of Melodinine E for the endometrial cancer cells is extremely strong.
Description
Technical field
The present invention relates to the novelty teabag of compound MelodinineE, particularly relate to the application of MelodinineE 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 MelodinineE that the present invention relates to is one and delivers (AtsushiUmehara in 2014, etal., TotalSynthesesofLeuconoxine, LeuconodineB, andMelodinineEbyOxidativeCyclicAminalFormationandDiaster eoselectiveRing-ClosingMetathesis.Org.Lett.2014, 16, noval chemical compound 2526-2529.), this compound has brand-new framework types (AtsushiUmehara, etal., TotalSynthesesofLeuconoxine, LeuconodineB, andMelodinineEbyOxidativeCyclicAminalFormationandDiaster eoselectiveRing-ClosingMetathesis.Org.Lett.2014, 16, 2526-2529.), the purposes of the MelodinineE 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 MelodinineE research, provide the application of MelodinineE in the anti-endometrial cancer drug of preparation.
Described compound MelodinineE structure is as shown in formula I:
The application of described MelodinineE in preparation treatment endometrial cancer drug, endometrial carcinoma cell behaviour Endometrial carcinoma cell line ISK and RL95-2.
One treats endometrial cancer drug, and be that active component interpolation adjuvant is prepared from by MelodinineE, preparation method, for getting 5 g of compound MelodinineE, adds 195 grams, dextrin, and mixing, Conventional compression makes 1000.
One treats endometrial cancer drug, and be that active component adds adjuvant and is prepared from by MelodinineE, preparation method, for getting 5 g of compound MelodinineE, adds starch 195 grams, and mixing, encapsulatedly makes 1000.
The present invention is found by external MTT antineoplastic activity evaluation, the growth of MelodinineE 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 1.73 ± 0.52 μMs and 0.89 ± 0.43 μM.Therefore, MelodinineE for the preparation of anti-endometrial cancer drug, can have good development prospect.
The purposes of the MelodinineE 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 MelodinineE involved in the present invention is see document (AtsushiUmehara, etal., TotalSynthesesofLeuconoxine, LeuconodineB, andMelodinineEbyOxidativeCyclicAminalFormationandDiaster eoselectiveRing-ClosingMetathesis.Org.Lett.2014,16,2526-2529.)
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 MelodinineE tablet involved in the present invention:
Get 20 g of compound MelodinineE and add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound MelodinineE capsule involved in the present invention:
Get 20 g of compound MelodinineE 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 MelodinineE 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 MelodinineE 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: MelodinineE 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 1.73 ± 0.52 μMs and 0.89 ± 0.43 μM.
Shown by above-described embodiment, the growth of MelodinineE 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 MelodinineE of the present invention has anti-carcinoma of endometrium, can for the preparation of anti-endometrial cancer drug.
Claims (4)
- The application of 1.MelodinineE in treatment endometrial cancer drug, described compound MelodinineE structure is as shown in formula I:Formula I.
- 2. the application of MelodinineE in treatment endometrial cancer drug as claimed in claim 1, is characterized in that endometrial carcinoma cell behaviour Endometrial carcinoma cell line ISK and RL95-2.
- 3. a treatment endometrial cancer drug, it is characterized in that by MelodinineE described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound MelodinineE, adds 195 grams, dextrin, mixing, Conventional compression makes 1000.
- 4. treat an endometrial cancer drug, it is characterized in that by MelodinineE described in claim 1 being that active component adds adjuvant and is prepared from, preparation method, for getting 5 g of compound MelodinineE, adds starch 195 grams, and mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510930553.1A CN105456262A (en) | 2015-12-12 | 2015-12-12 | Application of Melodinine E in preparing medicine for treating endometrial cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510930553.1A CN105456262A (en) | 2015-12-12 | 2015-12-12 | Application of Melodinine E in preparing medicine for treating endometrial cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105456262A true CN105456262A (en) | 2016-04-06 |
Family
ID=55594729
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510930553.1A Pending CN105456262A (en) | 2015-12-12 | 2015-12-12 | Application of Melodinine E in preparing medicine for treating endometrial cancer |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105456262A (en) |
-
2015
- 2015-12-12 CN CN201510930553.1A patent/CN105456262A/en active Pending
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| C06 | Publication | ||
| PB01 | Publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160406 |
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| WD01 | Invention patent application deemed withdrawn after publication |