CN106309441A - Application of Fistulains A in preparation of drugs for treating cervical cancer - Google Patents
Application of Fistulains A in preparation of drugs for treating cervical cancer Download PDFInfo
- Publication number
- CN106309441A CN106309441A CN201610890869.7A CN201610890869A CN106309441A CN 106309441 A CN106309441 A CN 106309441A CN 201610890869 A CN201610890869 A CN 201610890869A CN 106309441 A CN106309441 A CN 106309441A
- Authority
- CN
- China
- Prior art keywords
- fistulains
- cervical cancer
- preparation
- drugs
- application
- 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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Classifications
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- 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
Abstract
The invention discloses application of Fistulains A in the preparation of drugs for treating cervical cancer, belonging to the technical field of novel use of the drugs. In-vitro MTT antitumor activity evaluation finds that the Fistulains A also has remarkable inhibition effects to the growth of human cervical cancer cell strains HELA, HELA229, HCE1 and CASKI. Therefore, the Fistulains A can be used for preparing the anti-cervical cancer drugs and has relatively good development and application prospects. The application of the Fistulains A in the preparation of the drugs for treating the cervical cancer is disclosed for the first time, and the inhibitory activity of the Fistulains A to cervical cancer cells is unexpectedly strong.
Description
Technical field
The present invention relates to the new application of compound Fistulains A, particularly relate to Fistulains A in preparation treatment palace
Application in neck cancer medicine.
Background technology
Cancer is one of disease maximum to human life's health hazard, has substantial amounts of people to die from cancer every year.Anticancer
The focus of the research and development of medicine always study of pharmacy.Having 74% in antitumor drug is natural product or derivatives thereof, such as Ramulus et folium taxi cuspidatae
Alcohol and derivant thereof are exactly the antitumor drug that application effectiveness comparison is good the most clinically.Therefore, from natural product, searching is anti-
Chemical compound for treating cancer or lead compound have great importance.
The compound Fistulains A that the present invention relates to be one within 2015, deliver (Min Zhou, et al.,
Fistulains A and B,New Bischromones from the Bark of Cassia fistula,and Their
Activities.Org.Lett.2015,17,2638-2641.) noval chemical compound, this compound has brand-new framework types,
There is suppression hepatitis B virus effect (Min Zhou, et al., Fistulains A and B, New Bischromones from
The Bark of Cassia fistula, and Their Activities.Org.Lett.2015,17,2638-2641.),
The Fistulains A that the present invention relates to purposes in preparation treatment cervical cancer medicine is belonged to first public, owing to belonging to
Brand-new structure type, and it is unexpectedly strong for the inhibitory activity of cervical cancer cell, does not exist by other compounds
Providing the possibility of any enlightenment, possess prominent substantive distinguishing features, the preventing and treating being simultaneously used for cervical cancer obviously has significantly to enter
Step.
Summary of the invention
Do not find in it is an object of the invention to study according to existing Fistulains A that it has anti-cervical cancer activity
The present situation of report, it is provided that Fistulains A application in preparing medicament for resisting cervical cancer.
Described compound Fistulains A, structure is as shown in formula I:
Described Fistulains A application in treatment cervical cancer medicine, cervical cancer cell is human cervical carcinoma cell lines
HELA, HELA229, HCE1 and CASKI.
One treats cervical cancer medicine, Fistulains A be that active component interpolation adjuvant is prepared from, preparation method
For taking 5 g of compound Fistulains A, adding 195 grams of dextrin, mixing, conventional tablet presses makes 1000.
One treats cervical cancer medicine, Fistulains A be that active component interpolation adjuvant is prepared from, preparation method
For taking 5 g of compound Fistulains A, add starch 195 grams, mixing, encapsulated make 1000.
The present invention is found by external MTT antineoplastic activity evaluation, Fistulains A to human cervical carcinoma cell lines HELA,
The growth of HELA229, HCE1 and CASKI also has significant inhibitory action, and the IC50 value suppressing this 4 strain cell to grow is respectively
4.89 ± 1.75 μMs, 4.24 ± 2.43 μMs, 5.55 ± 1.68 μMs and 4.46 ± 2.96 μMs.Therefore, Fistulains A can be used for
Prepare medicament for resisting cervical cancer, there is good development prospect.
The Fistulains A that the present invention relates to purposes in preparation treatment cervical cancer medicine is belonged to first public,
Owing to framework types belongs to brand-new framework types, and it is unexpectedly strong, no for the inhibitory activity of cervical cancer cell
There is the possibility being provided any enlightenment by other compounds, possess prominent substantive distinguishing features, be simultaneously used for the preventing and treating of cervical cancer
Obviously have the most progressive.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by concrete real
Execute any restriction of example, but be defined in the claims.
Detailed description of the invention
The preparation method of compound Fistulains A involved in the present invention see document (Min Zhou, et al.,
Fistulains A and B,New Bischromones from the Bark of Cassia fistula,and Their
Activities.Org.Lett.2015,17,2638-2641.)
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by concrete real
Execute any restriction of example, but be defined in the claims.
Embodiment 1: the preparation of compound Fistulains A tablet involved in the present invention:
Taking 5 g of compound Fistulains A, add 195 grams of dextrin, mixing, conventional tablet presses makes 1000.
Embodiment 2: the preparation of compound Fistulains A capsule involved in the present invention:
Take 5 g of compound Fistulains A, add starch 195 grams, mixing, encapsulated make 1000.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example: use mtt assay to evaluate the compound Fistulains A growth inhibited effect to human cervical carcinoma cell lines
1. method: be in the cell of growth logarithmic (log) phase: human cervical carcinoma cell lines HELA, HELA229, HCE1 and CASKI (purchase
Buy from Chinese Academy of Sciences's cell bank) with 1.5 × 104Concentration kind is in 96 orifice plates.Original training is sucked after cell cultivation 24h is adherent
Support base.Test is divided into blank group, drug treating group.Blank group changes 1640 culture medium containing 10% hyclone；Medicine
It is 100 μMs that process group is changed containing concentration, 50 μMs, 10 μMs, 1 μM, 0.1 μM, the training of the Fistulains A of 0.01 μM and 0.001 μM
Support base.After cultivating 48h, add the MTT of concentration 5mg/mL, continue to be put in CO2Incubator cultivates 4h, then along culture fluid top
Sucking 100 μ L of supernatant, add 100 μ L DMSO, 10min is placed in dark place, utilizes microplate reader (Sunrise Products) to measure and inhales
Light value (wavelength 570nm), and calculate cell survival according to light absorption value, each process sets 6 repeating holes.Cell survival rate
(%)=Δ OD drug treating/Δ OD blank × 100.
2. result: the growth of human cervical carcinoma cell lines HELA, HELA229, HCE1 and CASKI is had by Fistulains A
Significantly inhibitory action.The IC50 value of this compound suppression human cervical carcinoma cell lines HELA, HELA229, HCE1 and CASKI growth
It is respectively 4.89 ± 1.75 μMs, 4.24 ± 2.43 μMs, 5.55 ± 1.68 μMs and 4.46 ± 2.96 μMs.
Shown by above-described embodiment, the Fistulains A of the present invention to human cervical carcinoma cell lines HELA, HELA229,
The growth of HCE1 and CASKI has good inhibiting effect.Thus proving, the Fistulains A of the present invention has anti-cervical cancer
Activity, can be used for preparing medicament for resisting cervical cancer.
Claims (4)
1.Fistulains A application in treatment cervical cancer medicine, described compound Fistulains A structure such as formula I
Shown in:
Formula I.
2. Fistulains A application in treatment cervical cancer medicine as claimed in claim 1, it is characterised in that cervical cancer is thin
Born of the same parents are human cervical carcinoma cell lines HELA, HELA229, HCE1 and CASKI.
3. a treatment cervical cancer medicine, it is characterised in that be that active component adds by the Fistulains A described in claim 1
Adding adjuvant to be prepared from, preparation method, for taking 5 g of compound Fistulains A, adds 195 grams of dextrin, mixing, Conventional compression
Machine makes 1000.
4. a treatment cervical cancer medicine, it is characterised in that be that active component adds by the Fistulains A described in claim 1
Adding adjuvant to be prepared from, preparation method, for taking 5 g of compound Fistulains A, adds starch 180 grams, mixing, encapsulated system
Become 1000.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610890869.7A CN106309441A (en) | 2016-10-12 | 2016-10-12 | Application of Fistulains A in preparation of drugs for treating cervical cancer |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610890869.7A CN106309441A (en) | 2016-10-12 | 2016-10-12 | Application of Fistulains A in preparation of drugs for treating cervical cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106309441A true CN106309441A (en) | 2017-01-11 |
Family
ID=57821090
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610890869.7A Pending CN106309441A (en) | 2016-10-12 | 2016-10-12 | Application of Fistulains A in preparation of drugs for treating cervical cancer |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106309441A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108893518A (en) * | 2018-07-12 | 2018-11-27 | 吉首大学 | A kind of drug and detection method that can inhibit human cervical carcinoma cell proliferation |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105294720A (en) * | 2015-05-08 | 2016-02-03 | 云南民族大学 | Dimerization chromone alkaloid compound as well as preparation method and application thereof |
-
2016
- 2016-10-12 CN CN201610890869.7A patent/CN106309441A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105294720A (en) * | 2015-05-08 | 2016-02-03 | 云南民族大学 | Dimerization chromone alkaloid compound as well as preparation method and application thereof |
Non-Patent Citations (2)
| Title |
|---|
| MIN ZHOU, ET AL.: "Fistulains A and B, New Bischromones from the Bark of Cassia fistula, and Their Activities", 《ORG. LETT.》 * |
| 王月德等: "傣药腊肠树枝中1 个新的三环生物碱类化合物及其细胞毒活性", 《中草药》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108893518A (en) * | 2018-07-12 | 2018-11-27 | 吉首大学 | A kind of drug and detection method that can inhibit human cervical carcinoma cell proliferation |
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| PB01 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20170111 |
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| RJ01 | Rejection of invention patent application after publication |