CN105311026A - Application of Leuconoxine in preparation of medicines for treating pancreatic cancer - Google Patents
Application of Leuconoxine in preparation of medicines for treating pancreatic cancer Download PDFInfo
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- CN105311026A CN105311026A CN201510907979.5A CN201510907979A CN105311026A CN 105311026 A CN105311026 A CN 105311026A CN 201510907979 A CN201510907979 A CN 201510907979A CN 105311026 A CN105311026 A CN 105311026A
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- leuconoxine
- pancreatic cancer
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Abstract
The invention discloses an application of Leuconoxine in preparation of medicines for treating pancreatic cancer, and belongs to the technical field of new applications of medicines. An in vitro MTT anti-tumor activity evaluation shows that the Leuconoxine also has a significant inhibition effect on growth of human pancreatic cancer cell lines PANC-1 and BXPC-3. Therefore, the Leuconoxine can be used for preparing anti-pancreatic cancer medicines, and has a good development and application prospect. The application of the Leuconoxine in preparation of the medicines for treating the pancreatic cancer related to the invention belongs to first publication, and the inhibitory activity of the Leuconoxine on pancreatic cancer cells is unexpectedly high.
Description
Technical field
The present invention relates to the novelty teabag of compound L euconoxine, particularly relate to the application of Leuconoxine in preparation treatment pancreatic 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 L euconoxine 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 Leuconoxine that the present invention relates in preparation treatment pancreatic cancer drug is belonged to first public, owing to belonging to brand-new structure type, and its inhibit activities for pancreatic 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 cancer of pancreas 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-cancer of pancreas activity according in existing Leuconoxine research, provide the application of Leuconoxine in the anti-pancreatic cancer drug of preparation.
Described compound L euconoxine, structure is as shown in formula I:
The application of described Leuconoxine in preparation treatment pancreatic cancer drug, pancreatic cancer cell is human pancreas cancer cell strain PANC-1 and BXPC-3.
One treats pancreatic cancer drug, and be that active component interpolation adjuvant is prepared from by Leuconoxine, preparation method, for getting 5 g of compound Leuconoxine, adds 195 grams, dextrin, and mixing, Conventional compression makes 1000.
One treats pancreatic cancer drug, and be that active component adds adjuvant and is prepared from by Leuconoxine, preparation method, for getting 5 g of compound Leuconoxine, adds starch 195 grams, and mixing, encapsulatedly makes 1000.
The present invention is found by external MTT antineoplastic activity evaluation, Leuconoxine also has significant inhibitory action to the growth of human pancreas cancer cell strain PANC-1 and BXPC-3, suppresses the IC50 value of this 2 strain Growth of Cells to be respectively 1.89 ± 0.51 μMs and 1.72 ± 0.48 μMs.Therefore, Leuconoxine for the preparation of anti-pancreatic cancer drug, can have good development prospect.
The purposes of the Leuconoxine that the present invention relates in preparation treatment pancreatic cancer drug is belonged to first public, because framework types belongs to brand-new framework types, and its inhibit activities for pancreatic 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 cancer of pancreas 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 euconoxine 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 L euconoxine tablet involved in the present invention:
Get 20 g of compound Leuconoxine, add the customary adjuvant 180 grams preparing tablet, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound L euconoxine capsule involved in the present invention:
Get 20 g of compound Leuconoxine, 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 Leuconoxine to the growth inhibited effect of human pancreas cancer cell strain
1. method: the cell being in growth logarithmic (log) phase: human pancreas cancer cell strain PANC-1 and BXPC-3 (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 Leuconoxine 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: Leuconoxine to human pancreas cancer cell strain PPANC-1 and BXPC-3 has significant inhibitory action.This compound suppresses the IC50 value of human pancreas cancer cell strain PANC-1 and BXPC-3 growth to be respectively 1.89 ± 0.51 μMs and 1.72 ± 0.48 μMs.
Shown by above-described embodiment, the growth of Leuconoxine of the present invention to human pancreas cancer cell strain PANC-1 and BXPC-3 has good inhibitory action.Prove thus, it is active that Leuconoxine of the present invention has anti-cancer of pancreas, can for the preparation of anti-pancreatic cancer drug.
Claims (4)
- The application of 1.Leuconoxine in treatment pancreatic cancer drug, described compound L euconoxine structure is as shown in formula I:
- 2. the application of Leuconoxine in treatment pancreatic cancer drug as claimed in claim 1, is characterized in that pancreatic cancer cell is human pancreas cancer cell strain PANC-1 and BXPC-3.
- 3. treat a pancreatic cancer drug, it is characterized in that by Leuconoxine described in claim 1 being that active component interpolation adjuvant is prepared from, preparation method, for getting 5 g of compound Leuconoxine, adds 195 grams, dextrin, and mixing, Conventional compression makes 1000.
- 4. treat a pancreatic cancer drug, it is characterized in that by Leuconoxine described in claim 1 being that active component adds adjuvant and is prepared from, preparation method, for getting 5 g of compound Leuconoxine, adds starch 195 grams, and mixing, encapsulatedly makes 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510907979.5A CN105311026A (en) | 2015-12-10 | 2015-12-10 | Application of Leuconoxine in preparation of medicines for treating pancreatic cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN201510907979.5A CN105311026A (en) | 2015-12-10 | 2015-12-10 | Application of Leuconoxine in preparation of medicines for treating pancreatic cancer |
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| CN105311026A true CN105311026A (en) | 2016-02-10 |
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| CN201510907979.5A Pending CN105311026A (en) | 2015-12-10 | 2015-12-10 | Application of Leuconoxine in preparation of medicines for treating pancreatic cancer |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105596334A (en) * | 2016-02-02 | 2016-05-25 | 南京正亮医药科技有限公司 | Application of Leuconoxine in preparation of medicine for treating breast cancer |
-
2015
- 2015-12-10 CN CN201510907979.5A patent/CN105311026A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105596334A (en) * | 2016-02-02 | 2016-05-25 | 南京正亮医药科技有限公司 | Application of Leuconoxine in preparation of medicine for treating breast cancer |
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Application publication date: 20160210 |