CN104814972A - Ginsenoside-containing medicine composition - Google Patents
Ginsenoside-containing medicine composition Download PDFInfo
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- CN104814972A CN104814972A CN201510181848.3A CN201510181848A CN104814972A CN 104814972 A CN104814972 A CN 104814972A CN 201510181848 A CN201510181848 A CN 201510181848A CN 104814972 A CN104814972 A CN 104814972A
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- ginsenoside
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- cancer
- medicine composition
- arasaponin
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Abstract
The invention discloses a ginsenoside-containing medicine composition. The ginsenoside-containing medicine composition comprises the following active ingredients by weight percent: 20-70 percent of ginsenoside Rg, 10-40 percent of ginsenoside Rh2 and 20-50 percent of notoginsenoside ft1. The invention also provides application of the composition to drugs for preventing and treating cancers, auxiliary anti-cancer drugs and medicines or health products used for strengthening the organic immunity. The ginsenoside-containing medicine composition can effectively inhibit tumor cells and stimulate lymphocyte proliferation, has excellent pharmacological effects, and has better security on the basis of saving resources and taking better drug effects.
Description
Technical field
The invention belongs to medical art, be specifically related to a kind of pharmaceutical composition containing ginsenoside.
Background technology
Cancer is commonly encountered diseases, frequently-occurring disease, has serious threat to people's life and health, is also huge on the impact of the development of the national economy.The cancer morbidity of the whole world and China is obviously increasing year by year.Annual new cancer stricken about 1,600,000 people of China, die from cancer person about 1,300,000 people.The level of present China cancer mortality, the whole nation just has 2 people to die from cancer for every 1 minute, people more than 2800 being had every day to be seized life by cancer, within 1 year, having the city of a population of one million to be destroyed by being equivalent to one.In the U.S., annual treatment of cancer expense 83,000,000,000 dollars, accounts for 14% of national medical expense.Almost everyone experiences the threat of cancer.Because the whole world is every year because the number of cancer mortality is up to 6,300,000 people, and China is every year because the number of cancer mortality has reached 1,300,000 people, and cancer patient every year with 3% speed increase, be equivalent to just have 1 family to be subject to the threat of cancer in every 200 families.
At present, everybody " talks cancer complexion changed ", and how prevention and therapy cancer is a global difficult problem.Although there is very large cancer therapy drug clinically, a kind of medicine is not had to prevent completely and to cure cancer.Ginsenoside-Rh2 and-Rg3 are that first Japanese scholars Beichuan merit was prepared in 1980, and determine its molecular formula.The national scholar such as Japan, China, Korea S, Germany, the U.S. has also carried out to some extent to its research subsequently.Ginsenoside-Rh2 and-Rg3 Trace bio-element from Radix Ginseng Rubra (cultivated ginseng forms through drying or dry to steam again), its extraction ratio is only 0.001% and 0.003%, and because its content is too low, complex manufacturing, causes production cost higher.Ginsenoside-Rh2 and-Rg3 have significant antitumor and improve the activity of body immune function, and applicable early, middle and late phase tumor patient and immunocompromised prophylaxis of tumours crowd occur and take.Clinical experiment confirms that it has growth of cancer cells such as suppressing pulmonary carcinoma, hepatocarcinoma, gastric cancer, intestinal cancer, breast carcinoma preferably, obviously improves clinical symptoms, raising life quality, prevention and therapy cancer, cardiovascular function of improving, anti-platelet aggregation, protection cranial nerve cell, improves immunity of organisms.Directly take the effect with prophylaxis of cancer and Therapeutic cancer, be applicable to anxious, heavy, patient with advanced cancer, body constitution is weaker, takes and can improve autoimmune function, strengthens anti-tumor ability, alleviates toxic and side effects after chemotherapy.Ginsenoside rg3 and other Anticancer drug combination, its anticancer and improve body immune function aspect there is better effect.The Shenyi capsule effective ingredient used clinically is ginsenoside rg3, is mainly used in the auxiliary treatment of Therapeutic cancer and cancer.Ginsenoside Rh2 does not have independent patent medicine, sells using the present that it is main component pungent capsule as health food, is mainly used in the treatment and the auxiliary treatment that improve body's immunity and cancer.The pharmacologically active report of arasaponin ft1 is less.
Pass through pharmacological experiment, the compositions active anticancer of ginsenoside-Rh2 and-Rg3 and arasaponin ft1 and enhancing human body immunity functional activity are all strong with-Rg3 than being used alone ginsenoside-Rh2, both explanations combination has collaborative pharmacological action, and this discovery has positive effect to the medicine of prevention and therapy cancer and health product exploitation aspect.
Summary of the invention
The object of this invention is to provide a kind of new pharmaceutical composition, said composition comprises ginsenoside Rg3, ginsenoside Rh2 and arasaponin ft1, by extensive and deep research, inventor finds that three carries out prescription at certain weight ratio and has collaborative pharmacological action, there is excellent pharmacological effect effect, at saving resource, have on the basis of better drug action, active ingredient composition has better safety.
The present invention realizes especially by following technical scheme:
A pharmaceutical composition containing ginsenoside, percentage composition comprises active component ginsenoside Rg3 20% ~ 70%, ginsenoside Rh2 10% ~ 40%, arasaponin ft120% ~ 50% by weight.
Preferably, a kind of pharmaceutical composition containing ginsenoside, percentage composition comprises active component ginsenoside Rg3 30% ~ 50%, ginsenoside Rh2 20% ~ 30%, arasaponin ft1 30% ~ 40% by weight.
Most preferred, a kind of pharmaceutical composition containing ginsenoside, percentage composition comprises active component ginsenoside Rg3 40%, ginsenoside Rh2 25%, arasaponin ft1 35% by weight.
The present composition can be processed into any oral and upper acceptable dosage form of injection on demand, and present composition oral agents can be made into tablet, sugar coated tablet, film coated tablet, enteric coated tablet, capsule, decoction, oral liquid, sucks agent, granule, electuary, pill, powder, sublimed preparation; Injection preparation can be made into freeze-dried powder, vein emulsion, injection, transfusion.Oral formulations is preferably tablet, capsule, granule; Injection preparation is preferably freeze-dried powder, vein emulsion, injection.
Its preparation of the present composition can be prepared by common processing method known in those skilled in the art, after mixing with liquid flux or solid carrier by active component, then add one or more in filler, binding agent, wetting agent, disintegrating agent, absorption enhancer, solvent, surfactant, flavouring agent, antiseptic, lubricant, sweeting agent or pigment.
Present invention also offers described compositions in prevention and therapy cancer and anticancer ancillary drug and the application that improves in the medicine of immunity of organisms or health product.
Beneficial effect of the present invention is: the present composition can effective inhibition tumor cell B16 and HepG2 through test proof, half-inhibition concentration IC50 is all at 40 below μ g/ml, lymphopoiesis can be stimulated simultaneously, enhancing human body immunity answering, have the known small dose group compound of experimental data all not stimulate the ability of lymphocytic emiocytosis IL-2 and IFN-γ, heavy dose of compositions has obvious stimulation to stimulate lymphocytic emiocytosis IL-2 and IFN-γ.
Detailed description of the invention
Below in conjunction with embodiment, the present invention is described further, the following stated, only to preferred embodiment of the present invention, not do other forms of restriction to the present invention, any those skilled in the art may utilize the technology contents of above-mentioned announcement to be changed to the Equivalent embodiments of equal change.Everyly do not depart from the present invention program's content, any simple modification done following examples according to technical spirit of the present invention or equivalent variations, all drop in protection scope of the present invention.
The preparation of embodiment 1 injection
Take arginine 50g, etc. the water of quality, stir, add ginsenoside Rg3 100g, ginsenoside Rh2 62g, arasaponin ft1 88g, be heated to 50 DEG C, stirring and dissolving, with containing 9% salt aqueous acid adjust pH to 4.6, add water to full dose, stir; Add the active carbon of dosing amount 0.l% (g/ml) again, stir 25 minutes, coarse filtration takes off charcoal; Cross 0.22 μm of filter membrane, obtain fine straining liquid; Embedding, every bottled amount 2mL; 118 DEG C of pressure sterilizings 18 minutes, inspection, packaging, warehouse-in.
The preparation of embodiment 2 tablet
1) ginsenoside Rg3 16g, ginsenoside Rh2 10g, arasaponin ft1 14g are stirred after mixing, obtain pulverulent solids;
2) mixed homogeneously with lactose 60g, carboxymethyl starch sodium 3g and micropowder silica gel 4.5g by the powder of step (1) gained, add arginine 60g and make suitable soft material, 20 mesh sieves are granulated;
3) the dry granule of carboxymethyl starch sodium 5.5g and micropowder silica gel 2.1g and step (2) gained mixes, and tabletting, obtains tablet.
Prepared by embodiment 3 capsule
Take ginsenoside Rg3 16g, ginsenoside Rh2 10g, arasaponin ft1 14g, add starch 274g, mixing, sieves, with ethanol water as binding agent, make suitable soft material, 18 mesh sieves are granulated, 60 DEG C of oven dryings 5 hours, 16 mesh sieve granulate, add 2g magnesium stearate, mixing, obtained capsule.
Below in conjunction with the application at anti-tumor aspect of the concrete description of test present composition.
Laboratory animal: kunming mice is bought from unming Medical College's Experimental Animal Center.
Cell: B16 melanoma cell (B16melanoma cell) and human liver cancer cell (HepG2) cell are bought from American Type Cell storehouse (ATCC, Hanassas, VA, USA) and obtained.
Culture medium: cell culture DMEM liquid cultivates (FBS; HyClone, Logan, UT, USA), culture fluid adds 10% hyclone (FBS; HyClone, Logan, UT, USA), 0.03%L – glutamine, the blue or green enzyme element of 100U/L, 100mg/L streptomycin, 5%NaCO
2adjust pH to 6.8 – 7.0.
Sample: experimental group 1: ginsenoside Rg3 30%, ginsenoside Rh2 40%, arasaponin ft1 30%; Experimental group 2: ginsenoside Rg3 50%, ginsenoside Rh2 25%, arasaponin ft1 25%; Experimental group 3: ginsenoside Rg3 70%, ginsenoside Rh2 15%, arasaponin ft1 15%.Compositions 20 μ l dimethyl sulfoxide (DMSO) dissolve, for configuring the DMEM cell culture medium of variable concentrations.Paclitaxel (TAX:Paclitaxel) and cisplatin (PPD:Cisplatin) are purchased from Sigma Chemical company (St.Louis, MO).
Equipment: instrument: microplate reader Bio-RAD 680 (USA); CO2 incubator ThermoForma 3310 (U.S.); Inverted biological microscope XD-101 type (Nanjing) etc.
The growth inhibited evaluation of embodiment 4 pairs of tumor cells
The normal Kunming mouse nephrocyte of original cuiture, B16 cell and HepG2 cell with cell density for 1 × 10
4/ ml is inoculated in 96 orifice plates and cultivates after 24 hours, it is 0 μ g that common DMEM culture medium is changed to containing final concentration, 25 μ g, 50 μ g, 75 μ g, the DMEM culture medium of 100 μ g difference group chemical combination, each concentration establishes 3 holes, and detect the activity of cell at 24 hours later with mtt assay, cell inhibitory activity inhibition concentration IC
50(median inhibitoryconcentration) represents.Inhibition concentration (IC
50) be drug level when cytoactive suppression ratio is 50%, computational methods are IC
50=(A
cell controls group-A
test sample group)/A
cell controls group-A
blank group) × 100%.
Mtt assay: according to the cytotoxicity (Y.Nakajima, Y.Saton, M.Katsumata, K.Tsujiyama, Y.Ida, and J.Shoji, Phytochemistry 1994,36,119-127) of the mtt assay detection of drugs that Mosmann sets up.Concrete grammar is: in the cell hole sucking supernatant, add 0.4mg/mL MTT, 0.1mL/ hole, 37 DEG C of 5%CO
2cultivate 4h, remove supernatant, every hole adds 0.1mL dimethyl sulfoxide (DMSO), hatches 10min, and microplate reader measures the absorbance of solution under 570nm.
The half-inhibition concentration IC50 (μ g/mL) of table 1 pair tumor cell
Experimental result is as shown in table 1, and positive controls (TAX, PPD) and three experimental grouies all have inhibitory action to B16 and HepG2 cell.To the half-inhibition concentration IC of two tumor cells
50all at 40 below μ g/ml.Further, all relevant sets all do not have toxicity to normal mouse kidney cell.
Embodiment 5 immunoregulatory activity detects
Be divided at random according to often organizing 5 by 125 18 ~ 20g kunming mices: normal saline group, the test group of 12 groups of 1mg/kg and 12 group 4mg/kg, experimental group is: experimental group 1: ginsenoside Rg3 30%, and ginsenoside Rh2 40%, arasaponin ft1 30%; Experimental group 2: ginsenoside Rg3 50%, ginsenoside Rh2 25%, arasaponin ft1 25%; Experimental group 3: ginsenoside Rg3 70%, ginsenoside Rh2 15%, arasaponin ft1 15%.Distinguish the compound group of intraperitoneal injection of saline or 4mg/kg every day.Put to death after 7 days, and experiment below spleen preparation is got in dislocation.
1) mtt assay measures lymphopoiesis ability
Asepticly prepare splenocyte suspension, adjust cell concentration to be 1 × 10
7/ mL.Every hole 100 μ L.If cell control well (adding DMEM culture fluid) and Con A Concanavalin (ConA) stimulate hole (concentration of ConA is 5mg/L).In 37 DEG C of CO
2cultivate 48h, add the MTT solution of 5mg/mL, 37 DEG C, 5%CO
2cultivate 4h, remove supernatant, every hole adds 100 μ L dimethyl sulfoxide (DMSO), hatches 10min, and microplate reader measures the absorbance A of solution under 570nm.Calculate stimulation index (SI).SI=stimulates hole A meansigma methods/control wells A meansigma methods.
Experimental result is in table 2, and positive controls (TAX, PPD) does not all stimulate lymphopoietic effect, and three experimental grouies all can stimulate lymphopoiesis.
2) NK cells against tumor cells kills and wounds toxicity test
By 100 μ L mouse boosting cell (1x10
7/ mL) add 96 orifice plates with 100 μ L YAC-1 cells in the ratio of cell concentration 50:1.If target cell (YAC-1 cell) contrast, effector lymphocyte's (each compound group mouse boosting cell) contrast, each 3 multiple holes.In 37 DEG C, 5%CO
2incubator cultivates 18h, adds MTT solution, measures A570 value.Calculate NK cell toxicant percentage rate: NK cell toxicant percentage rate=[1-(effect wad cutter A value-effect control wells A value)/target control wells A value] x100%.
Experimental result is in table 2, and positive controls (TAX, PPD) does not all strengthen the effect that NK cells against tumor cells kills and wounds.NK cells against tumor cells kills and wounds toxicity test and shows, low dose of experimental group all can strengthen the lethal of NK cell, all has comparatively strong active.
Table 2 lymphopoiesis ability (SI) and NK cells against tumor cells kill and wound toxicity impact (%) (n=5,
* expression and stimulating group compare P<0.05)
3) in spleen cell cultures supernatant, IL-2 and IFN-γ secretes mensuration
IL-2 determination of activity adopts mice T lymphoblast method of proliferating, and mtt assay surveys A570 value and IL-2 activity is proportionate, IFN-gamma activity mensuration employing L929 cytopathic-effect inhibition assay, violet staining survey the height that A540 value size reflects IFN-gamma activity.Joined by spleen cell cultures supernatant in mice T lymphoblast or L929 cell, the upgrowth situation of two kinds of cells reflects corresponding cytokine content.
The impact (n=5, ± SD, * represent compare P<0.05 with stimulating group) that table 3 experimental group is secreted IL-2 and IFN-γ
Experimental result is in table 3, and positive controls (TAX, PPD) does not all stimulate the ability of lymphocytic emiocytosis IL-2 and IFN-γ.Three experimental group small dose group all do not stimulate the ability of lymphocytic emiocytosis IL-2 and IFN-γ, and heavy dose of group has obvious stimulation to stimulate lymphocytic emiocytosis IL-2 and IFN-γ.
Claims (5)
1. the pharmaceutical composition containing ginsenoside, is characterized in that percentage composition comprises active component ginsenoside Rg3 20% ~ 70%, ginsenoside Rh2 10% ~ 40%, arasaponin ft120% ~ 50% by weight.
2. a kind of pharmaceutical composition containing ginsenoside according to claim 1, is characterized in that percentage composition comprises active component ginsenoside Rg3 30% ~ 50%, ginsenoside Rh2 20% ~ 30%, arasaponin ft130% ~ 40% by weight.
3. a kind of pharmaceutical composition containing ginsenoside according to claim 2, is characterized in that percentage composition comprises active component ginsenoside Rg3 40%, ginsenoside Rh2 25%, arasaponin ft135% by weight.
4. the application of the compositions according to any one of claims 1 to 3 in the anticancer ancillary drug of preparation.
5. the application of the compositions according to any one of claims 1 to 3 in the medicine or health product of preparation raising immunity of organisms.
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Cited By (5)
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CN105832753A (en) * | 2016-03-17 | 2016-08-10 | 云南普优生物科技有限公司 | Composition containing ginsenoside Rg3 and notoginsenoside ft1 |
CN105832780A (en) * | 2016-05-25 | 2016-08-10 | 朱国平 | Medicinal composition capable of enhancing human body immunity and having anti-cancer effect and preparation method thereof |
CN106924275A (en) * | 2016-10-17 | 2017-07-07 | 云南农业大学 | Pharmaceutical composition containing (R) notoginsenoside of compound 20 Ft1 and its application in pharmacy |
CN106924276A (en) * | 2017-05-09 | 2017-07-07 | 西北大学 | A kind of Panaxsaponin composition and its application in leucoderma is treated |
CN115317496A (en) * | 2022-09-22 | 2022-11-11 | 云南农业大学 | Application of ginsenoside Rg3, notoginsenoside Ft1 and composition thereof in preparing medicine for treating prostatic hyperplasia |
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CN1981776A (en) * | 2005-12-15 | 2007-06-20 | 昆明维泰尔健康科技有限责任公司 | Composition containing rare ginseng saponin, its production and usage |
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Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
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CN105832753A (en) * | 2016-03-17 | 2016-08-10 | 云南普优生物科技有限公司 | Composition containing ginsenoside Rg3 and notoginsenoside ft1 |
CN105832780A (en) * | 2016-05-25 | 2016-08-10 | 朱国平 | Medicinal composition capable of enhancing human body immunity and having anti-cancer effect and preparation method thereof |
CN106924275A (en) * | 2016-10-17 | 2017-07-07 | 云南农业大学 | Pharmaceutical composition containing (R) notoginsenoside of compound 20 Ft1 and its application in pharmacy |
CN106924276A (en) * | 2017-05-09 | 2017-07-07 | 西北大学 | A kind of Panaxsaponin composition and its application in leucoderma is treated |
CN115317496A (en) * | 2022-09-22 | 2022-11-11 | 云南农业大学 | Application of ginsenoside Rg3, notoginsenoside Ft1 and composition thereof in preparing medicine for treating prostatic hyperplasia |
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Application publication date: 20150805 |