CN106580976A - Application of tabersonine in preparing medicines for preventing and treating cancers - Google Patents
Application of tabersonine in preparing medicines for preventing and treating cancers Download PDFInfo
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- CN106580976A CN106580976A CN201611064554.3A CN201611064554A CN106580976A CN 106580976 A CN106580976 A CN 106580976A CN 201611064554 A CN201611064554 A CN 201611064554A CN 106580976 A CN106580976 A CN 106580976A
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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
- A61K31/4353—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
- A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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Abstract
The invention provides an application of tabersonine in preparing medicines for preventing and treating cancers. The tabersonine can be used for effectively preventing and treating the cancers. According to the invention, the tabersonine is used for preventing the cancers on the basis of the principle that the tabersonine has an obvious inhibitory effect on proliferation of cancer cells, so that the cancer cells become shrunken and diminished in volume, accompanied with karyopyknosis, and finally, cancer cell apoptosis is achieved. Based upon a cytotoxicity test, IC50 value of an inhibitory effect of the tabersonine on a hepatoma cell line SMMC7721 is 12.866-13.230 [mu]mol/L and IC50 value of an inhibitory effect of the tabersonine on a hepatoma cell line Bel7402 is 14.810-15.342 [mu]mol/L, IC50 value of an inhibitory effect on a gastric carcinoma cell line SGC7901 is 11.696-11.910 [mu]mol/L, IC50 value of an inhibitory effect on an ovarian carcinoma cell line SKOV3 is 24.383-24.703 [mu]mol/L and IC50 value of an inhibitory effect on an ovarian carcinoma cell line Hey is 14.669-14.977 [mu]mol/L, showing that the tabersonine has an excellent effect of preventing and treating the cancers.
Description
Technical field
The invention belongs to biomedicine technical field, more particularly to tabersonine answering in the medicine for preparing anti-curing cancers
With.
Background technology
Tumor is a kind of commonly encountered diseases, frequently-occurring disease, and wherein malignant tumor is the class disease for endangering human health most serious at present
Disease.According to the data that China Ministry of Public Health is announced, China's malignant tumor mortality rate in rural area and urban population in 2006 occupies the
One.And in many malignant tumor, hepatocarcinoma, gastric cancer and ovarian cancer belong to a most refractory class, reason is still lacked so far
The medicine thought, the mortality rate of patient remains high throughout the year, and 5 annual survival rates are low.The whole world annual newfound hepatocarcinoma, gastric cancer
Occur in China with human ovarian cancer patients 30～50%, and the age mostly is 40～50 years old.The early stage of hepatocarcinoma, gastric cancer and ovarian cancer is general
Without clinical symptoms, once there is typical clinical manifestation, middle and advanced stage is generally already belonged to, there occurs cancerometastasis.
Tabersonine is a kind of chemical substance, and molecular formula is C21H24N2O2, can extract from African Wo Kanjia seeds, have
Blood pressure lowering, blood sugar lowering, diuresis and depressed, the Jiao that cause for apoplexy sequela, ischemic hypertensive encephalopathy, cerebrovascular
Consider uneasy, emotional lability, be suitable to the symptom eliminates of senilism brain degeneration, such as dizziness, headache, hypomnesis, attention does not collect
In, aphasia, Andre Meynier syndrome etc.；Can also be used for retinal hemorrhage, nerves tachycardia and other plant function of nervous system disorderly
Disorderly etc..But the report that tabersonine is capable of anti-curing cancers is not related in prior art.
The content of the invention
In view of this, present invention aims to the deficiencies in the prior art, and provide tabersonine prepare it is anti-for cancer
Application in the medicine of disease, enables the effectively anti-curing cancers of tabersonine.
In order to realize foregoing invention purpose, the present invention provides technical scheme below：
The invention provides application of the tabersonine in the medicine for preparing anti-curing cancers.
Preferably, the cancer includes hepatocarcinoma, gastric cancer or ovarian cancer.
Preferably, the hepatocarcinoma is the hepatocarcinoma that hepatoma cell strain SMMC7721 or/and hepatoma cell strain Bel7402 cause.
Preferably, the gastric cancer is the gastric cancer that stomach cancer cell line SGC7901 causes.
Preferably, the ovarian cancer is the ovarian cancer that Ovarian Cancer Cells SKOV3 or/and Ovarian Cancer Cells Hey cause.
Preferably, the dosage form of the medicine includes liquid preparation, granule, slow releasing agent, electuary, tablet or soft gelatin capsule.
Preferably, the medicine contains tabersonine pharmaceutically acceptable adjuvant.
The invention provides application of the tabersonine in the medicine for preparing anti-curing cancers, tabersonine can effectively prevent for cancer
Disease.The present inventor's research finds that tabersonine has obvious inhibitory action to cancer cell multiplication, makes cancerous cell shrinkage, volume diminish,
With karyopycnosis, cancer cell-apoptosis are finally made, reach the purpose for the treatment of cancer.The present invention has carried out cytotoxicity reality to tabersonine
Test, as a result show, tabersonine is to the hepatoma cell strain SMMC7721 and IC of hepatoma cell strain Bel7402 inhibitory action50Value difference
For 12.866～13.230 μm of ol/L and 14.810～15.342 μm of ol/L, the IC to stomach cancer cell line SGC7901 inhibitory action50
It is worth for 11.696～11.910 μm of ol/L, to the Ovarian Cancer Cells SKOV3 and IC of Ovarian Cancer Cells Hey inhibitory action50Value
Respectively 24.383～24.703 μm ol/L and 14.669～14.977 μm of ol/L, from the IC of the cancerous cell for obtaining50Value, it may be said that
Bright tabersonine has good prevention effect to cancer.
Description of the drawings
Fig. 1 be tabersonine to hepatoma cell strain SMMC7721, hepatoma cell strain Bel7402, stomach cancer cell line SGC7901,
The suppression curve of Ovarian Cancer Cells SKOV3 and Ovarian Cancer Cells Hey；
Fig. 2 is phases of the hepatoma cell strain SMMC7721 Jing after the tabersonine effect 48h that concentration is 6 μm of ol/L and 24 μm of ol/L
Difference microscopic findings, are from left to right control, and concentration is 6 μm of ol/L and concentration is 24 μm of ol/L；
Fig. 3 is phases of the hepatoma cell strain Bel7402 Jing after the tabersonine effect 48h that concentration is 6 μm of ol/L and 24 μm of ol/L
Difference microscopic findings, are from left to right control, and concentration is 6 μm of ol/L and concentration is 24 μm of ol/L；
Fig. 4 is phases of the stomach cancer cell line SGC7901 Jing after the tabersonine effect 48h that concentration is 6 μm of ol/L and 24 μm of ol/L
Difference microscopic findings, are from left to right control, and concentration is 6 μm of ol/L and concentration is 24 μm of ol/L；
Fig. 5 is phases of the Ovarian Cancer Cells SKOV3 Jing after the tabersonine effect 48h that concentration is 6 μm of ol/L and 24 μm of ol/L
Difference microscopic findings, are from left to right control, and concentration is 6 μm of ol/L and concentration is 24 μm of ol/L；
Fig. 6 is differences of the Ovarian Cancer Cells Hey Jing after the tabersonine effect 48h that concentration is 6 μm of ol/L and 24 μm of ol/L
Microscopic findings, are from left to right control, and concentration is 6 μm of ol/L and concentration is 24 μm of ol/L；
Fig. 7 is hepatoma cell strain SMMC7721 Jing after the tabersonine effect 48h that concentration is 6 μm of ol/L and 12 μm of ol/L, AO/
EB coloration results, are from left to right control, and concentration is 6 μm of ol/L and 12 μm of ol/L；
Fig. 8 is stomach cancer cell line SGC7901 Jing after the tabersonine effect 48h that concentration is 6 μm of ol/L and 12 μm of ol/L, AO/
EB coloration results, are from left to right control, and concentration is 6 μm of ol/L and 12 μm of ol/L.
Specific embodiment
The invention provides application of the tabersonine in the medicine for preparing anti-curing cancers.Specifically, in the present invention, it is described
Cancer includes hepatocarcinoma, gastric cancer or ovarian cancer.
In the present invention, the tabersonine has structure shown in Formulas I：
The present invention does not have particular/special requirement to the source of the tabersonine, using the commercially available of those skilled in the art's routine selection
Commodity, the such as product of Tianyitang's production.
The present invention does not have special restriction to the dosage form of the medicine, is using dosage form well known to those skilled in the art
Can, in the present invention, the dosage form of the tabersonine can be liquid agent, granule, slow releasing agent, electuary, tablet or soft gelatin capsule.This
The bright adjuvant to above-mentioned dosage form is not particularly limited, using those skilled in the art's pharmaceutically acceptable adjuvant.This
Invention is not particularly limited to the preparation method of above-mentioned dosage form, the method for routinely preparing above-mentioned dosage form using those skilled in the art
.
In the present invention, when the tabersonine is prepared into liquid agent, granule, slow releasing agent, electuary, tablet or soft gelatin capsule,
The preparation method of the liquid agent, granule, slow releasing agent, electuary, tablet or soft gelatin capsule is not particularly limited, using this area skill
The method that art personnel routinely prepare.
In the present invention, the liver that the hepatocarcinoma is caused by hepatoma cell strain SMMC7721 or/and hepatoma cell strain Bel7402
Cancer.
In the present invention, the gastric cancer that the gastric cancer is caused by stomach cancer cell line SGC7901.
In the present invention, the ovum that the ovarian cancer is caused by Ovarian Cancer Cells SKOV3 or/and Ovarian Cancer Cells Hey
Nest cancer.
Carry out in detail with reference to application of the embodiment to the tabersonine of present invention offer in the medicine for preparing anti-curing cancers
Thin explanation, but they can not be interpreted as limiting the scope of the present invention.
Embodiment 1
1st, determination of cytotoxic activity
Assay method：
Tabersonine is first dissolved with DMSO, then concentration is configured to culture medium and be respectively 6,12,18,24,30 and 36 μm of ol/
The solution of L, the solution is used as sample determination liquid.By hepatoma cell strain SMMC7721, hepatoma cell strain in exponential phase
Bel7402, stomach cancer cell line SGC7901, Ovarian Cancer Cells SKOV3 and Ovarian Cancer Cells Hey are respectively according to every hole 2500
Individual cell strain is inoculated with 96 orifice plates, in 5%CO2In incubator, 37 DEG C of incubation 24h are subsequently adding containing above-mentioned variable concentrations ladder
The μ L of culture medium 200 of degree sample determination liquid continue to cultivate.Plus tabersonine group and negative control group are all provided with 4 multiple holes, each plate is equal
8 blank control wells are provided with, blank control group is not added with cancer cell and tabersonine only adds the culture medium of equivalent, negative control group to add
Plus the culture medium of cancer cell and equivalent, without tabersonine.
Supernatant is sopped up after 48h, the concentration that 100 μ L are added per hole incubates 4～8h for the MTT of 5mg/L in 37 DEG C, terminates training
Support, careful suction abandons supernatant, add the DMSO of 100 μ L crystal is fully dissolved per hole, vibrated with microwell plate fast oscillator
20min, determines the light absorption value A in each hole under 570nm.
The component of culture medium is：RPMI-1640 is 9 with the volume ratio of hyclone:1.
2nd, cytotoxic activity
The relative inhibition of the cell strain after tabersonine effect is calculated according to absorbance A.Computing formula is：
According to determination data and value of calculation draw tabersonine to hepatoma cell strain SMMC7721, hepatoma cell strain Bel7402,
The suppression curve of stomach cancer cell line SGC7901, Ovarian Cancer Cells SKOV3 and Ovarian Cancer Cells Hey, is as a result shown in Fig. 1.And profit
Half suppression ratio IC of each tabersonine sample to cancer cell is calculated with SPSS statistical softwares50Value, the results are shown in Table 1.
The IC that the tabersonine of table 1. is acted on each inhibition of cancer cell50Value
Can be drawn according to table 1 and Fig. 1, tabersonine presses down to hepatoma cell strain SMMC7721 and hepatoma cell strain Bel7402
The IC of making50Value is respectively 12.866～13.230 μm of ol/L and 14.810～15.342 μm of ol/L, to stomach cancer cell line
The IC of SGC7901 inhibitory action50It is worth for 11.696～11.910 μm of ol/L, to Ovarian Cancer Cells SKOV3 and ovarian cancer cell
The IC of strain Hey inhibitory action50Value is respectively 24.383～24.703 μm of ol/L and 14.669～14.977 μm of ol/L.
Embodiment 2
Difference microexamination and AO/EB carry out cancerous cell dyeing
Determined by MTT and shown, tabersonine has obvious inhibitory action to different cancer cell multiplications.Further to analyze this
Plant inhibitory action and be derived from necrocytosiss or inducing cell apoptosis, confirmed from morphocytology.It is 6 or 24 μ by concentration
After the tabersonine effect 48h of mol/L, difference microexamination finds cell shrinkage, and volume diminishes, with karyopycnosis, in culture fluid
There are a large amount of cell debriss, cell is presented typical apoptotic body.And cellular control unit is full unfolds, adherent growth in blocks；AO/
The apoptotic cell of EB dyeing is rendered as sending out Chinese red fluorescence or dyeing enhancing, and fluorescence more becomes clear, the round shape of uniformity or solid
Contracting shape, crumb structure, non-apoptotic nucleus are presented the deep mixed structure like feature of fluorescence.Difference microscopic findings are shown in figure
2 (SMMC7721), Fig. 3 (Bel7402), Fig. 4 (SGC7901), Fig. 5 (SKOV3) and Fig. 6 (Hey).AO/EB cancerous cell dyeing knot
Fruit sees Fig. 7 (SMMC7721) and Fig. 8 (SGC7901).Morphocytology research shows that tabersonine can pass through inducing cell apoptosis
To suppress the propagation of cancer cell.
As seen from the above embodiment, the tabersonine that the present invention is provided has preventive and therapeutic effect to hepatocarcinoma, gastric cancer and ovarian cancer, to liver
The IC of JEG-3 SMMC7721 and hepatoma cell strain Bel7402 inhibitory action50Value is respectively 12.866～13.230 μm of ol/L
With 14.810～15.342 μm of ol/L, the IC to stomach cancer cell line SGC7901 inhibitory action50It is worth for 11.696～11.910 μ
Mol/L, to the Ovarian Cancer Cells SKOV3 and IC of Ovarian Cancer Cells Hey inhibitory action50Value is respectively 24.383～24.703
μm ol/L and 14.669～14.977 μm of ol/L, shows that tabersonine has good prevention effect to cancer.
The above is only the preferred embodiment of the present invention, it is noted that for the ordinary skill people of the art
For member, under the premise without departing from the principles of the invention, some improvements and modifications can also be made, these improvements and modifications also should
It is considered as protection scope of the present invention.
Claims (7)
1. application of the tabersonine in the medicine for preparing anti-curing cancers.
2. application according to claim 1, it is characterised in that the cancer includes hepatocarcinoma, gastric cancer or ovarian cancer.
3. application according to claim 2, it is characterised in that the hepatocarcinoma is hepatoma cell strain SMMC7721 or/and liver
The hepatocarcinoma that JEG-3 Bel7402 causes.
4. application according to claim 2, it is characterised in that the gastric cancer is the stomach that stomach cancer cell line SGC7901 causes
Cancer.
5. application according to claim 2, it is characterised in that the ovarian cancer is Ovarian Cancer Cells SKOV3 or/and ovum
The ovarian cancer that nest JEG-3 Hey causes.
6. the application according to Claims 1 to 5 any one, it is characterised in that the dosage form of the medicine includes liquid system
Agent, granule, slow releasing agent, electuary, tablet or soft gelatin capsule.
7. application according to claim 6, it is characterised in that it is pharmaceutically acceptable auxiliary that the medicine contains tabersonine
Material.
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| CN201611064554.3A CN106580976A (en) | 2016-11-28 | 2016-11-28 | Application of tabersonine in preparing medicines for preventing and treating cancers |
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| CN201611064554.3A CN106580976A (en) | 2016-11-28 | 2016-11-28 | Application of tabersonine in preparing medicines for preventing and treating cancers |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108853043A (en) * | 2018-09-28 | 2018-11-23 | 郑士平 | A kind of drug and application thereof for treating central diabetes insipidus |
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| WO2007031556A2 (en) * | 2005-09-14 | 2007-03-22 | Vib Vzw | Means and methods to enhance the production of vinblastine and vincristine in catharanthus roseus |
| CN102558178A (en) * | 2012-01-09 | 2012-07-11 | 中国科学院昆明植物研究所 | Tabersonine derivative, pharmaceutical compositions, preparing method and medical application thereof |
-
2016
- 2016-11-28 CN CN201611064554.3A patent/CN106580976A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007031556A2 (en) * | 2005-09-14 | 2007-03-22 | Vib Vzw | Means and methods to enhance the production of vinblastine and vincristine in catharanthus roseus |
| CN102558178A (en) * | 2012-01-09 | 2012-07-11 | 中国科学院昆明植物研究所 | Tabersonine derivative, pharmaceutical compositions, preparing method and medical application thereof |
Non-Patent Citations (4)
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|---|
| CAI XIANG-HAI等: "Cytotoxic Indole Alkaloids from Melodinus fusiformis and M. morsei", 《CHINESE JOURNAL OF NATURAL MEDICINES》 * |
| EBA ADOU: "I. ISOLATION AND CHARACTERIZATION OF BIOACTIVE COMPOUNDS FROM SURINAME AND MADAGASCAR FLORA. II. A SYNTHETIC APPROACH TO LUCILACTAENE", 《VIRGINIA TECH ELECTRONIC THESES AND DISSERTATIONS》 * |
| SHAO-SONG LIU等: "Anti-tumor,anti-oxidant activity and isolation of the anti-tumor active compounds from Voacanga Africana Stapf.seeds", 《中国化学会第十一届全国天然有机化学学术会议论文集》 * |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108853043A (en) * | 2018-09-28 | 2018-11-23 | 郑士平 | A kind of drug and application thereof for treating central diabetes insipidus |
| CN108853043B (en) * | 2018-09-28 | 2020-11-13 | 郑士平 | Medicine for treating central diabetes insipidus and application thereof |
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Application publication date: 20170426 |