CN102232957A - Antitumor activities of 3-acetoxyl-8,24-lanostadiene-21-acid and use of 3-acetoxyl-8, 24-lanostadiene-21-acid in medicines - Google Patents
Antitumor activities of 3-acetoxyl-8,24-lanostadiene-21-acid and use of 3-acetoxyl-8, 24-lanostadiene-21-acid in medicines Download PDFInfo
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Abstract
The invention discloses the in-vivo and in-vitro antitumor activities of 3-acetoxyl-8,24-lanostadiene-21-acid. Researches indicate that the compound has remarkable suppressing effect on H22 borne tumor and has desirable killing effect on human liver cancer cells SMMC-7721 and human breast cancer cells MCF-7. The invention belongs to the extraction and preparation of active ingredients of Chinese medicines and the using method of the active ingredients in fields of medicines and health-care products. And a theoretical basis is provided for the use of the 3-acetoxyl-8,24-lanostadiene-21-acid in prevention and treatment of tumors and functional health-care products for preventing and treating tumors.
Description
Technical field:
The invention discloses 3-acetoxyl group-8, the inside and outside anti-tumor activity of 24-lanostadiene-21-acid studies show that this chemical compound is to H
22The lotus tumor has good inhibitory effect, and human liver cancer cell SMMC-7721 and human breast cancer cell MCF-7 are all had lethal effect preferably.Belong to preparation of Chinese medicine extracts active ingredients and the application in medicine and field of health care products thereof.
Background technology:
3-acetoxyl group-8,24-lanostadiene-21-acid is a kind of tetracyclic triterpene acid.Modern study shows that it has the activity that suppresses the bacillus subtilis growth.
Cancer also claims malignant tumor, and the control growth and proliferation of cell mechanism of serving as reasons is not normal and the disease that causes is one of important diseases of present harm humans health even life.In recent years, because the influence of factors such as environmental pollution, chemical contamination and ionizing radiation, the sickness rate of cancer is rapid ascendant trend.According to incompletely statistics, the annual newly-increased cancer patient 1,800,000 of China, dead 1,400,000, average per minute just has 1.3 people to die from cancer.The treatment cancer mostly is the method that medicine combines with chemotherapy at present, and this many tools of method toxic and side effects.
Triterpene substance has effects such as the growth of tumour cell of inhibition, pain relieving, calmness, antiallergic, antiinflammatory, detoxifcation, hepatoprotective, blood pressure lowering, blood fat reducing.But about 3-acetoxyl group-8, the 24-lanostadiene-anti-tumor activity of 21-acid and the research of application thereof are not but seen so far report.
Summary of the invention:
The invention discloses 3-acetoxyl group-8, the inside and outside anti-tumor activity of 24-lanostadiene-21-acid, this chemical compound can improve body's immunity significantly and kill and wound effect such as cancerous cell.
Press practice of pharmacy, can be with 3-acetoxyl group-8 of the present invention, 24-lanostadiene-21-processed with acid becomes the medicine of various clinical pharmaceutical dosage form as the treatment tumor, and said medicament is a said dosage form on any pharmaceutics
Pharmaceutical composition of the present invention contains the 3-acetoxyl group-8 of effective in cure effective dose, and 24-lanostadiene-21-acid is active component, and contains one or more pharmaceutically acceptable carriers.
Above-mentioned carrier is meant the pharmaceutical carrier of pharmaceutical field routine, comprises diluent, excipient, filler, adhesive, wetting agent, disintegrating agent, absorption enhancer, surfactant, absorption carrier.
The present invention can compositions form be applied to the patient of this treatment by oral, vein, intramuscular injection or parenteral mode.Conventional production method according to pharmaceutical field prepares various dosage forms such as tablet, granule, electuary, capsule, suppository, spray, slow releasing agent and injection.Also can make its active component and one or more carriers or drug regimen, make required dosage form.
Following pharmacological evaluation has confirmed 3-acetoxyl group-8, and 24-lanostadiene-21-acid has the pharmacologically active of treatment and prophylaxis of tumours.
3-acetoxyl group-8, the detection of the inside and outside anti-tumor activity of 24-lanostadiene-21-acid
Method of abstracting: adopt H
22Bearing mouse model and mtt assay have detected 3-acetoxyl group-8, the inside and outside anti-tumor activity of 24-lanostadiene-21-acid.The result: 1. the result shows that tumour inhibiting rate can reach 52.31% when dosage is 10mg/kg/d in the body; Can improve the mice body's immunity significantly.2. results of in vitro studies shows that this chemical compound all has lethal effect preferably to human liver cancer cell SMMC-7721 and human breast cancer cell MCF-7, and its cell killing rate maximum is respectively 77.97% and 90%.
Conclusion: 3-acetoxyl group-8,24-lanostadiene-21-acid has inside and outside anti-tumor activity preferably, can improve body's immunity significantly and kill and wound cancerous cell.
1 material
1.1 medicine: 3-acetoxyl group-8,24-lanostadiene-21-acid is obtained by the separation of this laboratory;
Cyclophosphamide for injection (CTX), lot number 09090521, Hengrui Medicine Co., Ltd., Jiangsu Prov.'s product; 5-fluorouracil (5-Fu) is purchased the tumour hospital in Jilin Province.
MTT (Sigma); DMSO (Beijing Chemical Plant);
1.2 animal: 50 of kunming mices, male, body weight 18～22g.Available from Jilin University's preclinical medicine animal center.
1.3 instrument: microplate reader (Multiskan); Centrifuge (SORVALL); CO2 gas incubator (NAPCO France).
2 methods and result
2.1 method
2.1.1 anti-tumor in vivo method: after animal was bought, first breeding observing conformed for 1 week it.Get the ascites of ascitic type tumor-bearing mice of inoculation 7d under the aseptic condition, be diluted to cell suspension at 1: 3 with normal saline, it is subcutaneous to be inoculated in mice left hind axillary fossa with every Mus 0.1mL.Be divided at random then: the normal control group; The normal saline model control group; Positive control drug cyclophosphamide 20mg/kg/d group; 3-acetoxyl group-8,24-lanostadiene-21-acid 5mg/kg/d and 10mg/kg/d group, totally 5 groups, 10 every group.Remove the 1st treated animal and normally raise, outside normal control; Cyclophosphamide group lumbar injection every other day gives cyclophosphamide, 3-acetoxyl group-8,24-lanostadiene-21-acid group gastric infusion every day; The normal saline matched group gavages normal saline every day.Each is organized mice and freely gets food drinking-water.Observe the state of mice every day, 10d behind the last administration 24h, weighs continuously, and mice is plucked eyeball and gets blood 0.5～1mL, and room temperature leaves standstill 2h, and the centrifugal 20min of 1000r/min gets serum IL-2 content to be measured.Simultaneously, the mice of getting behind the blood is put to death, complete tumor piece, thymus and the spleen won weighed respectively, calculates tumour inhibiting rate and organ index of immunity (index and spleen index and thymus index).
Result of calculation and statistics: tumor control rate=(the average tumor of the average tumor weight-administration of matched group group is heavy)/average tumor of matched group heavy * 100%.Heavy (the mg)/body weight (g) of thymus index=thymus, heavy (the mg)/body weight (g) of index and spleen index=spleen.
The IL-2 assay adopts double-antibody sandwich enzyme linked immunosorbent assay (ELISA) to detect, and operating procedure is carried out according to explanation.After adding stop buffer, mix gently, 450nm reads at the place absorption value (OD) on microplate reader.Establishing criteria product OD value adopts ELISA standard curve software for drawing to make standard curve, the IL-2 content of each sample of establishing criteria curve calculation.
Experimental data is used
Expression, and adopt SPSS18.0for Windows statistical software to analyze.P＜0.05 explanation is remarkable difference statistically, and P＜0.01 explanation is utmost point significant difference statistically.
2.1.2 vitro cytotoxicity experimental technique: adopt mtt assay, experimental procedure is as follows, adopts SMMC-7721 and the MCF-7 cell of exponential phase of growth, and being configured to concentration is 4 * 10
4The cell suspension of individual/mL, every hole 100 μ L are inoculated in 96 orifice plates, after 37 ℃, 5% saturated humidity are cultivated 24h, add by design concentration and to be subjected to reagent, and every hole adds dose 100 μ L, 4 parallel holes of each dosage.After cultivating 72h again, add the every hole 20 μ L of MTT, after continuing to cultivate 4h, supernatant discarded, every hole adds 150 μ LDMSO, and micro oscillator concussion 10min puts mensuration absorbance in 492nm wavelength place on the microplate reader.
Result of calculation and statistics: suppression ratio=(OD
Negative-OD
Be subjected to reagent)/OD
Negative* 100%.The OD value is with mean+SD
Represent.And adopt SPSS18.0for Windows statistical software to analyze.
P＜0.05 explanation is remarkable difference statistically, and P＜0.01 explanation is utmost point significant difference statistically.
2.2 result
2.2.1 anti-tumor in vivo experiment
2.2.1.1 to H
22The inhibitory action of tumor-bearing mice tumor
3-acetoxyl group-8,24-lanostadiene-21-acid is to H
22The inhibitory action result of tumor-bearing mice tumor is as shown in table 1.As can be known, this material presents than obvious suppression effect (P＜0.05) the growth of mice-transplanted tumor from table.When dosage was 10mg/kg/d, tumour inhibiting rate was 52.31% to the maximum, and compared with matched group, had significant difference (P＜0.01).
Table 13-acetoxyl group-8,24-lanostadiene-21-acid is to the influence of tumor-bearing mice tumor
Table?1Anti-tumor?activity?of?3-acetoxylanosta-8，24-dien-21-oic?acid?in?H
22mice
Compare with matched group:
*P＜0.05;
*P＜0.01.Compared?with?the?control?group，
*P＜0.05；
**P＜0.01。
2.2.1.2 to H
22The influence of tumor-bearing mice immune organ
3-acetoxyl group-8,24-lanostadiene-21-acid is to H
22The tumor-bearing mice immune organ to influence the result as shown in table 2.As can be known, index and spleen index obviously raises behind the mouse-borne tumor from table, and thymus index descends.3-acetoxyl group-8, after 24-lanostadiene-21-acid effect, index and spleen index and thymus index are reduction in various degree and increase.Compare with normal raising group, 3-acetoxyl group-8, there is not significant difference in the thymus index of 24-lanostadiene-21-acid group, but all there is significant difference (P＜0.05) in index and spleen index; Compare with the normal saline matched group, 3-acetoxyl group-8, the index and spleen index of 24-lanostadiene-21-acid group is lower than the normal saline group, but does not all have significant difference (P＞0.05); Compare with the CTX group, index and spleen index is higher than the CTX group but does not have significant difference, and thymus index is higher than the CTX group and has significant difference.
Table 23-acetoxyl group-8,24-lanostadiene-21-acid is to the influence of tumor-bearing mice immune organ
Table2Effects?of?3-acetoxylanosta-8，24-dien-21-oic?acid?on?immune?organ?in?H
22mice
Annotate: compare with matched group:
*P＜0.05;
*P＜0.01; Compare with normal group,
#P＜0.05;
##P＜0.01; Compare with the CTX group:
Note:Compared with the controlgroup,
*P＜0.05;
*P＜0.01; Compared with the normal group,
#P＜0.05;
##P＜0.01; Compared with the CTX group,
2.2.1.3 to H
22The influence of IL-2 content in the tumor-bearing mice serum
3-acetoxyl group-8,24-lanostadiene-21-acid is to H
22In the tumor-bearing mice serum IL-2 to influence the result as shown in table 3.From table as can be known, 3-acetoxyl group-8, the content of IL-2 obviously raises in the serum of the tumor-bearing mice after the 24-lanostadiene-21-acid effect.
Table 33-acetoxyl group-8,24-lanostadiene-21-acid is to H
22The influence of IL-2 in the tumor-bearing mice serum
Table3Effects?of?3-acetoxylanosta-8，24-dien-21-oic?acid?on?content?of?IL-2in?H
22mice
Compare with normal group,
#P＜0.05;
##P＜0.01; Note:Compared with the normal group,
#P＜0.05;
##P＜0.01.
2.2.2 external inhibitory action to cancer cell multiplication
3-acetoxyl group-8,24-lanostadiene-21-acid is as shown in table 4 to the inhibition of proliferation effect of human liver cancer cell (SMMC-7721) and human breast cancer cell (MCF-7).As can be known, this material all presents inhibitory action to SMMC-7721 and MCF-7, and has certain dose-effect relationship from table; Compare with matched group, have significant difference (P＜0.01).
Table 43-acetoxyl group-8,24-lanostadiene-21-acid is to SMMC-7721 and the effect of MCF-7 cell inhibitory effect
Table4?Inhibitory?Effects?of?3-acetoxylanosta-8，24-dien-21-oic?acid?to?SMMC-7721and?MCF-7
Annotate: compare with matched group:
*P＜0.05;
*P＜0.01; Compare with the 5-FU group:
Note:Compared with the control group,
*P＜0.05;
*P＜0.01; Comparedwith the CTX group,
3 conclusions
By above result as can be known, 3-acetoxyl group-8,24-lanostadiene-21-acid can suppress H
22Growth of tumors in vivo, and can improve the mice body's immunological function significantly; In addition, this material can also suppress the cell proliferation of human liver cancer cell (SMMC-7721) and human breast cancer cell (MCF-7) significantly.
Above-mentioned experimental result shows, 3-acetoxyl group-8, and 24-lanostadiene-21-acid has the prophylactic treatment effect to tumor; And has the adjusting immunologic function.Therefore, can be used for the application of prophylactic treatment tumor and functional health product thereof.
Claims (2)
1.3-acetoxyl group-8,24-lanostadiene-21-acid in preparation prophylactic treatment cancer drug purposes and relevant application.
2. medicine according to claim 1 is characterized in that said medicament is a said dosage form on any pharmaceutics.
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108467421A (en) * | 2018-03-05 | 2018-08-31 | 佳木斯大学 | Lanostane-type triterpene compound and its preparation method and application |
| CN109985052A (en) * | 2017-12-29 | 2019-07-09 | 上海蓝木化工有限公司 | The new application of triterpene compound |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN101062045A (en) * | 2006-04-29 | 2007-10-31 | 华北制药集团新药研究开发有限责任公司 | Novel function of triterpene saponin compounds |
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| CN101062045A (en) * | 2006-04-29 | 2007-10-31 | 华北制药集团新药研究开发有限责任公司 | Novel function of triterpene saponin compounds |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109985052A (en) * | 2017-12-29 | 2019-07-09 | 上海蓝木化工有限公司 | The new application of triterpene compound |
| CN108467421A (en) * | 2018-03-05 | 2018-08-31 | 佳木斯大学 | Lanostane-type triterpene compound and its preparation method and application |
| CN108467421B (en) * | 2018-03-05 | 2019-07-09 | 佳木斯大学 | Lanostane-type triterpene compound and its preparation method and application |
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