CN103735557A - Application of Ilexsaponin A1 in preparation of anti-tumor medicament - Google Patents
Application of Ilexsaponin A1 in preparation of anti-tumor medicament Download PDFInfo
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- CN103735557A CN103735557A CN201410007437.8A CN201410007437A CN103735557A CN 103735557 A CN103735557 A CN 103735557A CN 201410007437 A CN201410007437 A CN 201410007437A CN 103735557 A CN103735557 A CN 103735557A
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Abstract
The invention discloses novel medicinal application of a monomer component, namely, Ilexsaponin A1 derived from plants such as ilex hainanensis in the anti-tumor aspect, namely, application of the Ilexsaponin A1 in preparation of a medicament or health-care food for treating and preventing tumors. Meanwhile, the invention further discloses dosage forms such as capsules, tablets, drop pills and injections prepared by taking the Ilexsaponin A1 as raw materials. As proved by in-vitro experiments, the Ilexsaponin A1 has a very strong inhibiting function on various tumor cell lines. Thus, the Ilexsaponin A1 can be prepared into the anti-tumor medicament and a medicament or health-care food for preventing tumors.
Description
Technical field
The present invention relates to medical technical field, relate in particular to the anti-tumor activity of Ilexsaponin Ilexsaponin A1 and Ilexsaponin Ilexsaponin A1 in the new purposes of preparing in antitumor drug.
Background technology
Radix Ilicis Pubescentis is root or the leaf of Aquifoliaceae Holly Radix Ilicis Pubescentis, Ilexsaponin Ilexsaponin A1 be a kind of pentacyclic triterpene saponin of extracting from Radix Ilicis Pubescentis (Xiong Youxiang, etc. Chinese crude drug, 2002,25 (5): 371-374; Prosperous gorgeous, etc. modern combination of Chinese and Western medicine magazine, 2002,11 (21): 2198-2199).Report that in the past it has certain cardiovascular pharmacological effect, Mice Auricle microcirculation experiment show Ilexsaponin Ilexsaponin A1 can significant prolongation mice hemorrhage and clotting time, rat FeCl
3induction thrombosis experiment show Ilexsaponin A1 can reduce rat aorta thrombosis generate quality (Zhou Yuan, etc. Chinese crude drug, 2011,34 (5): 765-767).We study and find that Ilexsaponin Ilexsaponin A1 has good antitumor action, particularly to people's hepatocarcinoma and gastric cancer etc., within the scope of finite concentration, tumor cell are had lethal effect and do not affect vigor and the function of normal T cell.In addition, there is not yet bibliographical information Ilexsaponin Ilexsaponin A1 is prepared into antitumor drug.
Summary of the invention
One of the object of the invention provides the antineoplastic new usage of Ilexsaponin Ilexsaponin A1; Two of the object of the invention provides the pharmaceutical dosage form of Ilexsaponin Ilexsaponin A1.
The invention provides the purposes of Ilexsaponin Ilexsaponin A1 in medicine or the health food of preparation treatment and prophylaxis of tumours.
The kinds of tumors such as the tumor hepatocarcinoma of indication of the present invention, gastric cancer.Ilexsaponin Ilexsaponin A1 can dose dependent to suppress hepatocarcinoma, stomach cancer cell active but do not affect normal T cell differentiation on ground, therefore Ilexsaponin Ilexsaponin A1 has the features such as high efficiency anti-tumor and low toxicity.
Pharmaceutical excipient that pharmaceutical preparation of the present invention contains 1%～99% Ilexsaponin Ilexsaponin A1 and 99%～1% (comprising the medicine that other can prescription), preferably containing the pharmaceutical excipient of 30%～80% Ilexsaponin IlexsaponinA1 and 70%～20% (comprising the medicine that other can prescription), preferably contain the pharmaceutical excipient (comprising the medicine that other can prescription) of 60%～70% Ilexsaponin Ilexsaponin A1 and 40%～30%.
Press practice of pharmacy, Ilexsaponin Ilexsaponin A1 of the present invention can be prepared into multiple clinical medicine dosage forms for antitumor, comprise the dosage form of oral formulations and parenterai administration.The oral formulations of indication is selected from any one in capsule, tablet, drop pill, oral liquid, and the parenterai administration dosage form of indication is injection.
Adjuvant in antitumor drug of the present invention refers to conventional excipient, as solvent, disintegrating agent, correctives, antiseptic, coloring agent, binding agent etc.The medicine that other compatibilities in antitumor drug of the present invention are used, the Ilexsaponin Ilexsaponin A1 that refers to effective dose is certain medicine material, then compatibility other allowed the Chinese medicine or the chemical drugs that share.
Accompanying drawing explanation
Fig. 1 is the chemical structural formula of Ilexsaponin Ilexsaponin A1
Fig. 2 is that Ilexsaponin Ilexsaponin A1 acts on HepG2 cell lines (A) and SMMC77210～72h(B) suppression ratio figure.
Fig. 3 is the suppression ratio figure that Ilexsaponin Ilexsaponin A1 acts on human stomach cancer cell line SGC79010～72h.
Fig. 4 is the impact of Ilexsaponin Ilexsaponin A1 on the normal T cell differentiation of mice.
The specific embodiment
Below by specific embodiment, the present invention is further illustrated, but these embodiment are in order to illustrate, rather than limitation of the present invention.
The molecular formula C of Ilexsaponin Ilexsaponin A1
36h
56o
11, chemical constitution is as Fig. 1.
(the Ilexsaponin Ilexsaponin A1 that the present invention uses provides for professor Wang Qiang of crude drug teaching and research room of China Medicine University; Standard substance center, reference substance Sichuan can be bought)
Embodiment mono-: adopt the effect of vigor of MTT colorimetric determination Ilexsaponin Ilexsaponin A1 to HepG2 cell lines: the hepatoma cell strain HepG2 of the trophophase of taking the logarithm, 0.25% trypsinization, collect the cell under Digestive States, counting cells, is diluted to 10 by DMEM culture medium
3-10
4the single cell suspension of individual/100 μ l concentration, every hole 100 μ l, are inoculated on 96 orifice plates, put 37 ℃, and 5%CO2, in the cell culture incubator of saturated humidity, cultivates after 12h.Blank group adds buffer PBS, equal-volume DMEM culture fluid for negative control group, positive controls adds the cisplatin solution of variable concentrations, experimental group adds Ilexsaponin Ilexsaponin A1(20,40,80, the 160 μ g/ml of variable concentrations), each concentration is established 6 multiple holes, every hole 20 μ l.96 orifice plates are put 37 ℃, 5%CO
2, saturated humidity cell culture incubator in, cultivate after 4h, add 5mg/mlMTT, every hole 10 μ l, cultivate 4h, every hole adds 150 μ l DMSO, shaking table vibration 10min, measures its absorbance (A value) in microplate reader, absorbing wavelength is 570nm.Measure respectively 24,48, the OD value of 72h, and calculate relative inhibition, formula is as follows: suppression ratio (%)=(1-A experimental group/A matched group) × 100%.The results are shown in Figure 2A.
Conclusion: as shown in Figure 2 A, after Ilexsaponin Ilexsaponin A1 and HepG2 cytosis, with the increase of this Ilexsaponin Ilexsaponin A1, its suppression ratio rises, when 20 μ g/ml, 40 μ g/ml, 80 μ g/ml and 160 μ g/ml concentration, HepG2 cell proliferation is had to obvious inhibitory action, relatively there is significant difference (P<0.05) with negative control group, be dose-dependence; Meanwhile, along with passage of time, Ilexsaponin Ilexsaponin A1 progressively increases HepG2 cell inhibitory rate, is time-dependent relation.
Embodiment bis-, adopts the effect of vigor of MTT colorimetric determination Ilexsaponin Ilexsaponin A1 to SMMC-7721 human hepatocarcinoma cell: methodology part, with reference to embodiment mono-, the results are shown in Figure 2B.
Conclusion: as shown in Figure 2 A, after Ilexsaponin Ilexsaponin A1 and SMMC7721 cytosis, with the increase of this Ilexsaponin Ilexsaponin A1, its suppression ratio rises, when 20 μ g/ml, 40 μ g/ml, 80 μ g/ml and 160 μ g/ml concentration, SMMC7721 cell proliferation is had to obvious inhibitory action, relatively there is significant difference (P<0.05) with negative control group, be dose-dependence; Meanwhile, along with passage of time, Ilexsaponin Ilexsaponin A1 progressively increases SMMC7721 cell inhibitory rate, is time-dependent relation.
Embodiment tri-, adopts the effect of vigor of MTT colorimetric determination Ilexsaponin Ilexsaponin A1 to stomach cancer cell line SGC7901: methodology part, with reference to embodiment mono-, the results are shown in Figure 3.
Conclusion: as shown in Figure 3, after Ilexsaponin Ilexsaponin A1 and SGC7901 cytosis, with the increase of this Ilexsaponin Ilexsaponin A1, its suppression ratio rises, when 20 μ g/ml, 40 μ g/ml, 80 μ g/ml and 160 μ g/ml concentration, SGC7901 cell proliferation is had to obvious inhibitory action, relatively there is significant difference (P<0.05) with negative control group, be dose-dependence; Meanwhile, along with passage of time, Ilexsaponin Ilexsaponin A1 progressively increases SGC7901 cell inhibitory rate, is time-dependent relation.
4. embodiment tetra-, the impact of external Ilexsaponin Ilexsaponin A1 on T cell differentiation
The negative selection method of magnetic bead separates and obtains CD4+T cell, the initial CD4 of sorting according to a conventional method
+t cell is inoculated in 96 well culture plates with 109/L density, each condition of culture is established multiple hole, with containing L-glutaminate, the RPMI-1640 of hyclone is cultivated, culture plate is in advance with PBS4 ℃ of coated the spending the night containing 10 μ g/ml CD3 monoclonal antibodies, add again 2.0 μ g/ml CD28 solubility monoclonal antibodies to cultivate and make T cells activation, add TGF (5ng/ml) and variable concentrations (0, 10, 30, 100, 300 μ g/ml) Ilexsaponin Ilexsaponin A1, jointly hatch 72h, fixing, wear film, buffer processing, add PE-CD25, Percp5.5-CD4 and Foxp3-APC, carry out FACS detection, the results are shown in Figure 4.
Conclusion: in 0～300 μ g/ml concentration range, Ilexsaponin Ilexsaponin A1 does not affect normal T cell differentiation.
Embodiment 5. capsules prepare Ilexsaponin Ilexsaponin A1250g, starch 2500g, fully mixes dried starch with Ilexsaponin Ilexsaponin A1, crosses 120 mesh sieves, after fully mixing, prepare 1000 of capsules, every containing Ilexsaponin Ilexsaponin A1250mg.
The preparation 600g Polyethylene Glycol water-bath of embodiment 6. drop pill is dissolved, and adds Ilexsaponin Ilexsaponin A1200g, fully stirs and is placed in insulating tube, and rear employing liquid paraffin parcel adds a small amount of Pulvis Talci to mix after blotting paraffin oil, prepares drop pill 1000 balls
Embodiment 7. tablets prepare Ilexsaponin Ilexsaponin A1100g, starch 1000g, Icing Sugar 200g, after appropriate alcohol granulation, after pelletizing machine is processed, tabletting subpackage.
Embodiment 7. injections prepare Ilexsaponin Ilexsaponin A110g, propylene glycol 20ml, Polyethylene Glycol 40ml, water for injection 200ml, heating in water bath 0.5h after mixing, water for injection adds to 500ml, supersound process 10min, heating in water bath 0.5h, regulates PH5.5～6.5, filter clear and bright, embedding sterilizing and get final product.
Claims (7)
1. the purposes of Ilexsaponin Ilexsaponin A1 in preparation treatment and prophylaxis of tumours medicine or health food.
2. purposes according to claim 1, is characterized in that described antitumor hepatocarcinoma and gastric cancer.
3. a pharmaceutical preparation, the Ilexsaponin Ilexsaponin A1 that it is characterized in that containing dose therapeutically effective and one or more pharmaceutically acceptable pharmaceutical excipients, or can with the other drug of Ilexsaponin Ilexsaponin A1 prescription.
4. pharmaceutical preparation according to claim 3, is characterized in that containing the medicine that the pharmaceutical excipient of 1%～99% Ilexsaponin Ilexsaponin A1 and 99%～1% or other can prescriptions.
5. pharmaceutical preparation according to claim 4, is characterized in that containing the medicine that the pharmaceutical excipient of 30%～80% Ilexsaponin Ilexsaponin A1 and 70%～20% or other can prescriptions.
6. pharmaceutical preparation according to claim 5, is characterized in that containing the medicine that the pharmaceutical excipient of 60%～70% Ilexsaponin Ilexsaponin A1 and 40%～30% or other can prescriptions.
7. according to the pharmaceutical preparation described in right 3, it is characterized in that said pharmaceutical dosage form is selected from any in the middle of capsule, tablet, drop pill, oral liquid, injection.
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104398546A (en) * | 2014-12-15 | 2015-03-11 | 扬州大学 | Antineoplastic drug preparation using hainan holly leaf total triterpenes as raw material |
| CN104546958A (en) * | 2014-12-25 | 2015-04-29 | 扬州大学 | Application of ilex hainanensis merr total triterpenes and weight-reducing and lipid-regulating pharmaceutical preparation taking ilex hainanensis merr total triterpenes as raw materials |
| CN105640969A (en) * | 2014-11-10 | 2016-06-08 | 江苏省中国科学院植物研究所 | Anti-bacterial purpose of prosapogenin A |
| CN114939121A (en) * | 2022-04-11 | 2022-08-26 | 枣庄学院 | Application of pubescent holly root saponin A in preparation of ionizing radiation protection medicines |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102499926A (en) * | 2011-11-04 | 2012-06-20 | 刘国樵 | Application of ilexsaponin compound |
-
2014
- 2014-01-08 CN CN201410007437.8A patent/CN103735557A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102499926A (en) * | 2011-11-04 | 2012-06-20 | 刘国樵 | Application of ilexsaponin compound |
Non-Patent Citations (3)
| Title |
|---|
| 杨运云 等: "加速溶剂萃取/HPLC-MS对毛冬青药材中Ilexgenin A与Ilexsaponin A1含量的测定", 《分析测试学报》 * |
| 程齐来 等: "山绿茶中ilexgenin A抗大鼠移植性肝癌的作用", 《中国实验方剂学杂志》 * |
| 赵钟祥 等: "大鼠肠内菌对毛冬青皂苷ilexsaponin A1的代谢转化", 《中国药科大学学报》 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105640969A (en) * | 2014-11-10 | 2016-06-08 | 江苏省中国科学院植物研究所 | Anti-bacterial purpose of prosapogenin A |
| CN104398546A (en) * | 2014-12-15 | 2015-03-11 | 扬州大学 | Antineoplastic drug preparation using hainan holly leaf total triterpenes as raw material |
| CN104546958A (en) * | 2014-12-25 | 2015-04-29 | 扬州大学 | Application of ilex hainanensis merr total triterpenes and weight-reducing and lipid-regulating pharmaceutical preparation taking ilex hainanensis merr total triterpenes as raw materials |
| CN114939121A (en) * | 2022-04-11 | 2022-08-26 | 枣庄学院 | Application of pubescent holly root saponin A in preparation of ionizing radiation protection medicines |
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Application publication date: 20140423 |