CN105596334A - Application of Leuconoxine in preparation of medicine for treating breast cancer - Google Patents
Application of Leuconoxine in preparation of medicine for treating breast cancer Download PDFInfo
- Publication number
- CN105596334A CN105596334A CN201610072623.9A CN201610072623A CN105596334A CN 105596334 A CN105596334 A CN 105596334A CN 201610072623 A CN201610072623 A CN 201610072623A CN 105596334 A CN105596334 A CN 105596334A
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- leuconoxine
- breast cancer
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- application
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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 Leuconoxine in preparation of a medicine for treating breast cancer, and belongs to the technical field of a new application of medicines. In-vitro MTT anti-tumor activity evaluation shows that the Leuconoxine has a significant inhibition effect on growth of human breast cancer cell lines 4T1, MCF-7, MDA-MB-231 and MCF-7B. Therefore, the Leuconoxine can be used for preparing an anti-breast cancer medicine, and has good development and application prospects. The application of the Leuconoxine in preparation of the medicine for treating the breast cancer is disclosed for the first time; and furthermore, the inhibitory activity on breast cancer cells is unexpectedly good.
Description
Technical field
The present invention relates to the new purposes of compound L euconoxine, relate in particular to Leuconoxine at preparation treatment breast cancer medicineApplication in thing.
Background technology
Cancer is one of disease to human life's health hazard maximum, has a large amount of people to die from cancer every year. Cancer therapy drugResearch and development are the focuses of study of pharmacy always. In antineoplastic, have 74% to be natural products or derivatives thereof, as taxol and spread outBiology is exactly the reasonable antineoplastic of effect clinically at present. Therefore, from natural products, find anticancer compound orLead compound has great importance.
The compound L euconoxine the present invention relates to is one and within 2014, delivers (AtsushiUmehara, etal., TotalSynthesesofLeuconoxine,LeuconodineB,andMelodinineEbyOxidativeCyclicAminalFormationandDiastereoselectiveRing-ClosingMetathesis.Org.Lett.2014,16,2526-2529.) noval chemical compound, this compound has brand-new framework types (AtsushiUmehara, etal., TotalSynthesesofLeuconoxine,LeuconodineB,andMelodinineEbyOxidativeCyclicAminalFormationandDiastereoselectiveRing-ClosingMetathesis.Org.Lett.2014,16,2526-2529.), the purposes for the Leuconoxine the present invention relates in preparation treatment breast cancer medicines belongs to open first,Owing to belonging to brand-new structure type, and its inhibition for breast cancer cell is active unexpectedly strong, does not exist by otherCompound provides the possibility of any enlightenment, possesses outstanding substantive distinguishing features, obviously has significantly for the control of breast cancer simultaneouslyProgress.
Summary of the invention
The object of the invention is to according to not finding showing of its report with anti-breast cancer activity in existing Leuconoxine researchShape, provides Leuconoxine in the application of preparing in anti-breast cancer medicines.
Described compound L euconoxine, structure is suc as formula shown in (I):
The application of described Leuconoxine in preparation treatment breast cancer medicines, breast cancer cell behaviour breast carcinoma cell strain 4T1,MCF-7, MDA-MB-231 and MCF-7B.
One is treated breast cancer medicines, is that active component interpolation auxiliary material is prepared from by Leuconoxine, and preparation method is for getting 5Digest compound Leuconoxine, add 195 grams, dextrin, mix, conventional compressing tablet is made 1000.
One is treated breast cancer medicines, is that active component interpolation auxiliary material is prepared from by Leuconoxine, and preparation method is for getting 5Digest compound Leuconoxine, add 195 grams of starch, mix, encapsulatedly make 1000.
The present invention finds by external MTT antitumor activity evaluation, Leuconoxine to human breast cancer cell strain 4T1, MCF-7,The growth of MDA-MB-231 and MCF-7B also has significant inhibitory action, suppresses the IC50 value of this 4 strain Growth of Cells respectivelyBe 1.34 ± 0.43 μ M, 2.15 ± 0.47 μ M, 1.53 ± 0.37 μ M and 1.48 ± 0.31 μ M. Therefore, LeuconoxineCan be for the preparation of anti-breast cancer medicines, there is good development prospect.
Purposes for the Leuconoxine the present invention relates in preparation treatment breast cancer medicines belongs to open first, due to boneFrame type belongs to brand-new framework types, and its inhibition for breast cancer cell is active unexpectedly strong, does not exist by itHis compound provides the possibility of any enlightenment, possesses outstanding substantive distinguishing features, obviously has aobvious for the control of breast cancer simultaneouslyThe progress of work.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to specific embodimentAny restriction, but be limited by claim.
Detailed description of the invention
The preparation method of compound L euconoxine involved in the present invention referring to document (AtsushiUmehara, etal.,TotalSynthesesofLeuconoxine,LeuconodineB,andMelodinineEbyOxidativeCyclicAminalFormationandDiastereoselectiveRing-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 subject to specific embodimentAny restriction, but be limited by claim.
Embodiment 1: the preparation of compound L euconoxine tablet involved in the present invention:
Get 20 and digest compound Leuconoxine, add 180 grams of conventional auxiliary materials preparing tablet, mix, conventional tablet press machine is made1000.
Embodiment 2: the preparation of compound L euconoxine capsule involved in the present invention:
Get 20 and digest compound Leuconoxine, add the conventional auxiliary material of preparing capsule as 180 grams of starch, mix, dress glueCapsule is made 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: adopt the growth inhibition effect of mtt assay assessing compound Leuconoxine to human breast cancer cell strain
1. method: the cell in growth logarithmic phase: human breast cancer cell strain 4T1, MCF-7, MDA-MB-231 and MCF-7B(buying from Chinese Academy of Sciences's cell bank) is with 1.5 × 104Concentration kind is in 96 orifice plates. After cell cultivation 24h is adherent, suckCulture medium originally. Test is divided into blank group, drug-treated group. Blank group is changed 1640 trainings containing 10% hycloneSupport base; Drug-treated group change containing concentration be 100 μ M, 50 μ M, 10 μ M, 1 μ M, 0.1 μ M, 0.01 μ M andThe culture medium of the Leuconoxine of 0.001 μ M. Cultivate after 48h, add the MTT of concentration 5mg/mL, continue to be put inCO2Incubator is cultivated 4h, then sucks 100 μ L supernatants along nutrient solution top, adds 100 μ LDMSO, and put dark placePut 10min, utilize ELIASA (Sunrise company product) to measure light absorption value (wavelength 570nm), and according to light absorption value meterCalculate cell survival situation, 6 repeating holes are established in each processing. Cell survival rate (%)=Δ OD drug-treated/Δ OD blank×100。
2. the life of result: Leuconoxine to human breast cancer cell strain P4T1, MCF-7, MDA-MB-231 and MCF-7BLength has significant inhibitory action. This compound suppresses human breast cancer cell strain 4T1, MCF-7, MDA-MB-231 and MCF-7BThe IC50 value of growth is respectively 1.34 ± 0.43 μ M, 2.15 ± 0.47 μ M, 1.53 ± 0.37 μ M and 1.48 ± 0.31 μ M.
Shown by above-described embodiment, Leuconoxine of the present invention is to human breast cancer cell strain 4T1, MCF-7, MDA-MB-231There is good inhibitory action with the growth of MCF-7B. Prove thus, Leuconoxine of the present invention has anti-breast cancer and livesProperty, can be for the preparation of anti-breast cancer medicines.
Claims (4)
1.Leuconoxine is the application in breast cancer medicines in treatment, described compound L euconoxine structure suc as formulaShown in (I):
Formula (I).
2. the application of Leuconoxine in treatment breast cancer medicines as claimed in claim 1, is characterized in that mammary glandCancer cell behaviour breast carcinoma cell strain 4T1, MCF-7, MDA-MB-231 and MCF-7B.
3. a treatment breast cancer medicines, is characterized in that by Leuconoxine described in claim 1 be active componentAdd auxiliary material and be prepared from, preparation method digests compound Leuconoxine for getting 5, adds 195 grams, dextrin, mixes, normalRule compressing tablet is made 1000.
4. a treatment breast cancer medicines, is characterized in that by Leuconoxine described in claim 1 be active componentAdd auxiliary material and be prepared from, preparation method digests compound Leuconoxine for getting 5, adds 195 grams of starch, mix,Encapsulatedly make 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610072623.9A CN105596334A (en) | 2016-02-02 | 2016-02-02 | Application of Leuconoxine in preparation of medicine for treating breast cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610072623.9A CN105596334A (en) | 2016-02-02 | 2016-02-02 | Application of Leuconoxine in preparation of medicine for treating breast cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105596334A true CN105596334A (en) | 2016-05-25 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610072623.9A Pending CN105596334A (en) | 2016-02-02 | 2016-02-02 | Application of Leuconoxine in preparation of medicine for treating breast cancer |
Country Status (1)
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105311026A (en) * | 2015-12-10 | 2016-02-10 | 淄博齐鼎立专利信息咨询有限公司 | Application of Leuconoxine in preparation of medicines for treating pancreatic cancer |
-
2016
- 2016-02-02 CN CN201610072623.9A patent/CN105596334A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105311026A (en) * | 2015-12-10 | 2016-02-10 | 淄博齐鼎立专利信息咨询有限公司 | Application of Leuconoxine in preparation of medicines for treating pancreatic cancer |
Non-Patent Citations (3)
| Title |
|---|
| FUMIKO ABE等: "INDOLE ALKALOIDS FROM LEAVES AND STEMS OF LEUCONOTIS EUGENIFOLIUS", 《PHYTOCHEMISTRY》 * |
| JIAN-HUA SHANG等: "Pharmacological evaluation of Alstonia scholaris: Anti-inflammatory and analgesic effects", 《JOURNAL OF ETHNOPHARMACOLOGY》 * |
| 战淑珺 等: "COX-2抑制剂与乳腺癌关系研究进展", 《癌症进展杂志》 * |
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Application publication date: 20160525 |