CN1623553A - Anticancer auxiliary medicine using 20 (S)-panaxcoside Rg3 as effertive component and its application - Google Patents
Anticancer auxiliary medicine using 20 (S)-panaxcoside Rg3 as effertive component and its application Download PDFInfo
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Abstract
An auxiliary anticancer medicine for increasing the curative effect of other anticancer medicines, decreasing their toxic, and preventing and treating the leukocytopenia caused by radiotherapy or chemicotherapy features that its active component is 20(s)-ginsenoside-Rg3. It is applied by injection or oral taking.
Description
Technical field
The present invention relates to a kind of cancer therapy drug curative effect that is used to strengthen, reduce the anticancer ancillary drug of the leucocytes reduction that toxicity of anticancer agents, prevention and treatment chemicotherapy cause, belong to the field of medicaments of treatment of cancer.
Background technology
Cancer is one of three big diseases of harm humans health, and its sickness rate and mortality rate have risen to the 1st in some country.Therefore develop cancer therapy drug and be one of key subjects that vast medical worker faces.A lot of cancer therapy drugs of succeeding in developing at present though therapeutic effect is become better and better, because the toxic and side effects of medicine itself is too strong, cause clinical practice to be restricted.Therefore, cancer therapy drug research at present continues to seek outside the medicine of kill cancer cell on the one hand, and exploitation is that the anticancer ancillary drug of main effect also more and more comes into one's own to strengthen the curative effect of cancer therapy drug, to reduce its toxic and side effects.
Radix Ginseng is a kind of famous and precious nourishing medicine, has strongly invigorating primordial QI, and multiple arteries and veins takes off admittedly, invigorating the spleen to benefit the lung, and function such as promote the production of body fluid, calm the nerves is used to improve cancer patient's body's immunity, the aspects such as leucocytes reduction that prevention and treatment cause because of chemicotherapy clinically.20 (S)-ginsenoside-Rg3 extract from Stem and leaf of Radix Ginseng and through transforming the tetracyclic triterpenes panoxadiol type saponin monomer effective ingredient that obtains.
20 (S)-ginsenoside-Rg3 structural formula (R:-glu-o-glu; R1:-OH; R2:-CH3)
It is reported, Rg3 has antitumor, suppresses effects such as new vessels generation, antiinflammatory, but have the cancer therapy drug of enhancing curative effect about 20 (S)-ginsenoside-Rg3, leucocytes reduction that reduction toxicity of anticancer agents, prevention and treatment chemicotherapy cause and the effect that strengthens cancer patient's body's immunity but do not appear in the newspapers; Although disclose the medical usage of 20 (S)-ginsenoside-Rg3 in preparation treatment pulmonary carcinoma, melanoma, S180 sarcoma among the open text CN 1092204C of Chinese patent, our research but find 20 (S) though-ginsenoside-Rg3 has certain active anticancer, but its effect that kills and wounds cancerous cell can not show a candle to chemical synthetic drug, as cyclophosphamide, 5-fluorouracil, cisplatin etc.; We find that also it has very significantly efficacy enhancing and toxicity reducing effect to cancer therapy drug, also can improve cancer patient's immunity of organisms simultaneously.In addition, numerous 20 (R)-ginsenoside-Rg3 that studies show that have notable antitumor activity, even calendar year 2001 China take the lead in ratifying as a kind new medicine (Chinese medicine) of effective ingredient " join a capsule " trial production and at home the listing, but it is very weak that its antitumor action is found in clinical practice, therefore, description is revised as " element culturing fixed folder, benefiting vital QI and blood when trial production is become a full member.Suppress tumor growth,, help to improve the curative effect of primary lung cancer, hepatocarcinoma, can improve the deficiency of vital energy symptom of tumor patient, improve immunity " with the chemotherapy drug combination.Promptly not being re-used as simple cancer therapy drug treats.Based on this, the inventor is by a large amount of experimentatioies, invented and a kind ofly be the medicine of effective ingredient and strengthening the cancer therapy drug curative effect, reducing its toxicity, the medical usage of the aspects such as leucocytes reduction that prevention and treatment chemicotherapy cause with 20 (S)-ginsenoside-Rg3.
Summary of the invention
The invention provides a kind of is effective ingredient with 20 (S)-ginsenoside-Rg3, is used to strengthen the cancer therapy drug curative effect, the medicine of the leucocytes reduction that reduction toxicity of anticancer agents, prevention and treatment chemicotherapy cause.
The invention provides a kind of is the application of medicine in the medicine that strengthens the cancer therapy drug curative effect of effective ingredient with 20 (S)-ginsenoside-Rg3.
The invention provides a kind of is the application of medicine in the medicine that reduces toxicity of anticancer agents of effective ingredient with 20 (S)-ginsenoside-Rg3.
The invention provides a kind of is the application of medicine in the medicine of the leucocytes reduction that prevents and treat chemicotherapy to cause of effective ingredient with 20 (S)-ginsenoside-Rg3.
The invention provides a kind of with 20 (S)-ginsenoside-Rg3 be the medicine of effective ingredient when being used for above-mentioned arbitrary purposes, its using dosage scope is 1mg～2000mg, the preferred dose scope is 20mg～500mg.
Medicine provided by the invention can be with oral or injection administration, and drug administration by injection can be for injecting in intravenous injection, intramuscular injection, lumbar injection, subcutaneous injection or the tumor body.Oral formulations can be tablet, capsule, pill, granule, drop pill, soft capsule, suspension, solution, syrup, capsule, granule, drop pill; Injection preparation can be freeze-dried powder, injection vein emulsion, injection, transfusion.Oral formulations is preferably tablet, capsule, granule; The preferred freeze-dried powder of injection preparation, injection vein emulsion.
Various pharmaceutical dosage form provided by the present invention all can be prepared from the pharmacy conventional method.
The inventor confirms with 20 (S)-ginsenoside-Rg3 to be that the medicine of effective ingredient has the cancer therapy drug of enhancing curative effect, reduces its toxicity by following test, leukopenic effect that prevention and treatment chemicotherapy cause, the following examples are used for more detailed description the present invention, but and do not mean that the present invention only limits to this.Testing 20 used (S)-ginsenoside-Rg3 is provided by natural drug Engineering Technical Research Centre Natural Medicine Chemistry research department, Shandong Province, through HPLC detection level 〉=90%, reference substance is provided by natural drug Engineering Technical Research Centre pharmaceutical analysis research department, Shandong Province.
The specific embodiment:
Preparation embodiment 1: injection preparation prepares embodiment
Take by weighing 1.00g 20 (S)-ginsenoside-Rg3, the propylene glycol that adds 20ml n-butyl alcohol and 30ml melts saponin fully, and the citric acid of 0.15g tetracaine hydrochloride, 0.02g is joined in the 40ml water for injection, makes dissolving fully, and above-mentioned aqueous solution joined in the drug solution mix homogeneously; Regulating pH value with Borax and boric acid is 5.5 ± 1.0; 85 ℃ of insulations of the needle-use activated carbon of adding 0.1% 30 minutes, the G3 sintered glass funnel filters, the filtering with microporous membrane of 0.22um; Filtrate is sub-packed in the 7ml cillin bottle, and (directly tamponade of the injection that branch installs, jewelling cover into injection to every loading amount 2ml; Or make freeze-dried powder through the freeze dryer lyophilizing.)。
Preparation embodiment 2: preparation tablets embodiment
Take by weighing 10.00g 20 (S)-ginsenoside-Rg3, add starch 90 grams, mixing, sieve, mixed powder; Ethanol water is made binding agent, the suitable soft material of system, and 18 mesh sieves are granulated, 60 ℃ of oven dryings 2 hours, 16 order nylon mesh granulate add magnesium stearate, mixing, the heavily about 100mg/ sheet of tabletting, sheet.
Press down the tumor experiment in test example 1 20 (S)-ginsenoside-Rg3 body
1, test material
1.1 medicine and reagent: injection 20 (S)-ginsenoside-Rg3, the Shandong Province natural drug Engineering Technical Research Centre Drug Manufacturing Room provide lot number: 20020525,20mg/ml, 5ml/ props up.Cyclophosphamide, Hualian Pharmaceutical Co., Ltd., Shanghai produces, lot number: 000205.
1.2 animal: Kunming mouse, 5 ~ 8 ages in week, body weight 18 ~ 22g, Shandong Province's natural drug Engineering Technical Research Centre animal center provides, the quality certification number: (matter) word 20010603 is moved in the Shandong.The male and female dual-purpose, same sex is adopted in every batch of experiment.The C57BL/6 mouse inbred lines, 5 ~ 8 ages in week, body weight 18 ~ 22g, Chinese Academy of Medical Sciences's laboratory animal breeding field provides, the quality certification number: SCX11-00-0006.
1.3 cell strain: rat liver cancer H22, mouse cervical cancer U14, murine melanoma B16, Mice Bearing Lewis Lung Cancer, available from institute of materia medica, Chinese Academy of Medical Sciences Beijing.
1.4 analysis on hemogram instrument: AITAIKE BLOOD CELL COUNTER CA-500
1.5 the medicine preparation: mice all is made into respective concentration with the injection normal saline with each medicine.
2, content of the test: H22 hepatocarcinoma and the inoculation of U14 cervical cancer: be taken at the above-mentioned tumor-bearing mice that the Kunming mouse intraperitoneal inoculation was gone down to posterity seven days, behind the sterilization skin of abdomen, extract ascites, add the long-pending injection normal saline dilution of triploid, sterilization Mus armpit skin, every mice is in the oxter
Injection tumor cell suspension 0.2ml, 50 mices are inoculated in each tumor strain respectively.
B16 melanoma and Lewis lung cancer inoculation: get the good mice of Lewis lung cancer, growth conditions that inoculates 10 days, taking off neck puts to death, after disinfecting skin in alcohol, strip tumor tissues, grind to form homogenate with Potter-Elvehjem Tissue Grinders, 100 order sterilizing stainless steel net filtrations behind the normal saline of five times of weight of adding.Every mice left side axil skin of sterilizing, inoculation tumor liquid 0.2ml.50 mices are inoculated in each tumor strain respectively.
Connect after the tumor second day and be divided into following 5 groups and administration at random:
Solvent control group: the normal saline solution that gives the equivalent adjuvant
Positive drug contrast: give cyclophosphamide 20mg/kg
Medicine small dose group: give 20 (S)-ginsenoside-Rg33.75mg/kg
Dosage group in the medicine: give 20 (S)-ginsenoside-Rg37.5mg/kg
The heavy dose of group of medicine agent: give 20 (S)-ginsenoside-Rg315mg/kg
Intravenously administrable is 10 days continuously, puts to death mice in 24 hours after the last administration, strips tumor tissue and weighs.Calculate tumour inhibiting rate.
Data are represented with X ± SD, carry out statistical procedures with the t check.
3, result of the test
3.1 20 (S)-ginsenoside-Rg3 are to the inhibitory action of mice H22 liver cancer growth
The result shows that 20 (S)-ginsenoside-Rg3 are the dose-dependent inhibition effect to mice H22 liver cancer growth, and administration group and solvent control group have significant difference (heavy dose of and middle dosage group: P＜0.01; Low dose group: P＜0.05); 20 (S)-ginsenoside-Rg3 respectively organize the mice body weight and the solvent control group compares, there was no significant difference, and cyclophosphamide group mice body weight and solvent control group relatively have significant difference to the results are shown in Table 1.
Table 1.20 (S)-ginsenoside-Rg3 is to the inhibitory action of mice H22 liver cancer growth
| Group | The Mus number | Dosage (mg/kg) | Body weight (g) | Tumor heavy (g) | Tumour inhibiting rate (%) |
| The solvent control group | 10 | ?—— | ?29.5±2.2 | 2.54±0.68 | |
| The cyclophosphamide group | 10 | ?20 | ?24.8±1.7** | 0.84±0.53** | 66.8 |
| Rg3 | 10 | ?15 | ?28.5±2.3## | 1.45±0.55** | 43.0 |
| 10 | ?7.5 | ?29.1±2.4## | 1.66±0.61** | 34.8 | |
| 10 | ?3.75 | ?29.7±2.6## | 1.81±0.48* | 28.8 |
Compare with the solvent control group: * *, P＜0.01; *, P＜0.05; Compare with the cyclophosphamide group: ##, P＜0.01; #, P＜0.05
3.2 20 (S)-ginsenoside-Rg3 are to the inhibitory action of mice U14 cervical cancer growth
The result shows that growth is the dose-dependent inhibition effect to 20 (S)-ginsenoside-Rg3 to mice U14 cervical cancer, and administration group and solvent control group have significant difference (heavy dose of and middle dosage group: P＜0.01; Low dose group: P＜0.05); 20 (S)-ginsenoside-Rg3 respectively organize the mice body weight and the solvent control group compares, there was no significant difference, and cyclophosphamide group mice body weight and solvent control group relatively have significant difference to the results are shown in Table 2.
Table 2.20 (S)-ginsenoside-Rg3 is to the inhibitory action of mice U14 cervical cancer growth
| Group | The Mus number | Dosage (mg/kg) | Body weight (g) | Tumor heavy (g) | Tumour inhibiting rate (%) |
| The solvent control group | ?10 | —— | ?29.3±2.9 | ?1.88±0.63 | |
| The cyclophosphamide group | ?10 | 20 | ?25.3±1.9** | ?0.74±0.36** | 60.5 |
| Rg3 | ?10 | 15 | ?28.7±2.2## | ?1.04±0.34** | 45.0 |
| ?10 | 7.5 | ?28.6±2.4## | ?1.12±0.36** | 40.6 | |
| ?10 | 3.75 | ?29.3±2.6## | ?1.29±0.51* | 31.5 |
Compare with the solvent control group: *, P＜0.05; *, P＜0.01; Compare with the cyclophosphamide group: ##, P＜0.01.
3.3 20 (S)-ginsenoside-Rg3 are to the inhibitory action of Mice Bearing Lewis Lung Cancer growth
The result shows that growth is the dose-dependent inhibition effect to 20 (S)-ginsenoside-Rg3 to Mice Bearing Lewis Lung Cancer, and administration group and solvent control group have significant difference (heavy dose of and middle dosage group: P＜0.01; Low dose group: P＜0.05); 20 (S)-ginsenoside-Rg3 respectively organize the mice body weight and the solvent control group compares, there was no significant difference, and cyclophosphamide group mice body weight and solvent control group relatively have significant difference to the results are shown in Table 3.
Table 3 20 (S)-ginsenoside-Rg3 is to the inhibitory action of Mice Bearing Lewis Lung Cancer growth
| Group | The Mus number | Dosage (mg/kg) | Body weight (g) | Tumor heavy (g) | Tumour inhibiting rate (%) |
| The solvent control group | ?10 | —— | ?25.4±0.4 | 1.78±0.54 | |
| The cyclophosphamide group | ?10 | 20 | ?22.3±0.5** | 0.63±0.23** | 64.6 |
| Rg3 | ?10 | 15 | ?26.4±0.4## | 0.84±0.36** | 52.7 |
| ?10 | 7.5 | ?26.0±0.3## | 0.97±0.23** | 45.4 | |
| ?10 | 3.75 | ?25.5±0.2## | 1.19±0.41* | 33.3 |
Compare with the solvent control group: *, P＜0.05; *, P＜0.01; Compare with the cyclophosphamide group: ##, P＜0.01.
3.4 20 (S)-ginsenoside-Rg3 are to the inhibitory action of mice B16 melanoma growth
The result shows that growth is the dose-dependent inhibition effect to 20 (S)-ginsenoside-Rg3 to Mice Bearing Lewis Lung Cancer, and administration group and solvent control group have significant difference (heavy dose of and middle dosage group: P＜0.01; Low dose group: P＜0.05); 20 (S)-ginsenoside-Rg3 respectively organize the mice body weight and the solvent control group compares, there was no significant difference, and cyclophosphamide group mice body weight and solvent control group relatively have significant difference to the results are shown in Table 4.
Table 4 20 (S)-ginsenoside-Rg3 is to the inhibitory action of mice B16 melanoma growth
| Group | The Mus number | Dosage (mg/kg) | Body weight (g) | Tumor heavy (g) | Tumour inhibiting rate (%) |
| The solvent control group | 10 | —— | ?28.3±1.7 | 2.51±0.63 | |
| The cyclophosphamide group | 10 | 20 | ?25.5±1.3** | 0.99±0.36** | 60.7 |
| Rg3 | 10 | 15 | ?28.9±1.3### | 1.22±0.43** | 51.5 |
| 10 | 7.5 | ?28.0±1.6## | 1.38±0.64** | 44.8 | |
| 10 | 3.75 | ?28.3±1.8## | 1.60±0.43** | 36.2 |
Compare with the solvent control group: *, P＜0.05; *, P＜0.01; Compare with the cyclophosphamide group: ##, P＜0.01.
Test example 2 20 (S)-ginsenoside-Rg33 is to the potentiation of chemotherapeutics
1, test material is with test example 1
2, content of the test
Set up transplanted tumor model in the mice body with mice H22 hepatocarcinoma and Lewis lung cancer, divide into groups and administration by following group:
Solvent control group: the normal saline solution that gives the equivalent adjuvant
Cyclophosphamide small dose group: give cyclophosphamide 5mg/kg
Cyclophosphamide low dose+medicine small dose group: give cyclophosphamide 5+20 (S)-ginsenoside-Rg33.75mg/kg
The heavy dose of group of cyclophosphamide low dose+medicine: give cyclophosphamide 5+20 (S)-ginsenoside-Rg315mg/kg and encircle phosphinylidyne
The heavy dose of group of amine: give cyclophosphamide 10mg/kg
Cyclophosphamide heavy dose+medicine small dose group: give cyclophosphamide 10+20 (S)-ginsenoside-Rg33.75mg/kg
The heavy dose of group of cyclophosphamide heavy dose+medicine: give cyclophosphamide 10+20 (S)-ginsenoside-Rg315mg/kg
Cyclophosphamide heavy dose+medicine injection high dose group: give cyclophosphamide 10+20 (S)-ginsenoside-Rg3150mg/kg
Cyclophosphamide heavy dose+drug oral high dose group: give cyclophosphamide 10+20 (S)-ginsenoside-Rg3300mg/kg
Medication as previously mentioned.Take off cervical vertebra after the last administration and put to death mice, get tumor and weigh, competitive list share each tumour inhibiting rate of organizing of treatment with cyclophosphamide 5mg/kg and 10mg/kg treatment with 20 (S)-ginsenoside-Rg33.75mg/kg and ginsenoside-Rg315mg/kg, observes 20 (S)-ginsenoside-Rg3 potentiation.
Data are represented with X ± SD, carry out statistical procedures with the t check.
3, result of the test
3.1 20 (S)-ginsenoside-Rg3 are to the potentiation of cyclophosphamide treatment mice H22 hepatocarcinoma
The result shows that cyclophosphamide 5mg/kg dosage group tumour inhibiting rate is 23.8%, and adds with behind 3.75mg/kg and 15mg/kg 20 (S)-ginsenoside-Rg3, has obviously improved the tumor killing effect of cyclophosphamide.Cyclophosphamide 10mg/kg is 32.2% to H22 hepatocarcinoma tumour inhibiting rate, adds with behind 3.75mg/kg, 15mg/kg, 150mg/kg, oral 3000mg/kg20 (S)-ginsenoside-Rg3, has obviously improved the tumor killing effect of cyclophosphamide, the results are shown in Table 5.
Table 5 cyclophosphamide and 20 (S)-ginsenoside-Rg3 use in conjunction is to the inhibitory action of mice H22 liver cancer growth
Heavy (g) tumour inhibiting rate (%) of rank dosage (mg/kg) tumor
Solvent control group 2.46 ± 0.68
Cyclophosphamide 5 1.87 ± 0.49 23.8
Cyclophosphamide 10 1.67 ± 0.51* 32.2
Cyclophosphamide+Rg3 5+3.75 1.33 ± 0.51**# 45.9
Cyclophosphamide+Rg3 5,+15 1.18 ± 0.34**## 52.0
Cyclophosphamide+Rg3 10+3.75 1.05 ± 0.28**# 57.2
Cyclophosphamide+Rg3 10,+15 0.83 ± 0.36**## 66.3
Cyclophosphamide+Rg3 10+,150 0.53 ± 0.30**## 78.5
Cyclophosphamide+oral Rg3 10+,300 0.73 ± 0.37**## 70.3
Compare with the solvent control group: * *, P＜0.01; *, P＜0.05.Compare with the cyclophosphamide group: ##, P＜0.01.
3.1 20 (S)-ginsenoside-Rg3 are to the potentiation of cyclophosphamide treatment Mice Bearing Lewis Lung Cancer
The result shows that cyclophosphamide 5mg/kg dosage group tumour inhibiting rate is 22.2%, and adds with behind 3.75mg/kg and 15mg/kg 20 (S)-ginsenoside-Rg3, has obviously improved the tumor killing effect of cyclophosphamide.Cyclophosphamide 10mg/kg is 34.4% to H22 hepatocarcinoma tumour inhibiting rate, adds with behind 3.75mg/kg, 15mg/kg, 15mg/kg 20 (S)-ginsenoside-Rg3, has obviously improved the tumor killing effect of cyclophosphamide, the results are shown in Table 6.
Table 6 cyclophosphamide and 20 (S)-ginsenoside-Rg3 use in conjunction is to the inhibitory action of Mice Bearing Lewis growth
Heavy (g) tumour inhibiting rate (%) of rank dosage (mg/kg) tumor
Solvent control group 1.93 ± 0.55
Cyclophosphamide 5 1.50 ± 0.35 22.2
Cyclophosphamide 10 1.26 ± 0.34* 34.4
Cyclophosphamide+Rg3 5+3.75 1.19 ± 0.22**# 38.5
Cyclophosphamide+Rg3 5,+15 1.05 ± 0.32**## 45.3
Cyclophosphamide+Rg3 10+3.75 0.89 ± 0.33**# 54.0
Cyclophosphamide+Rg3 10,+15 0.73 ± 0.24**## 62.1
Cyclophosphamide+Rg3 10+,150 0.56 ± 0.28**## 71.0
Cyclophosphamide+oral Rg3 10+,300 0.67 ± 0.32**## 65.3
Compare with the solvent control group: * *, P＜0.01; *, P＜0.05.Compare with the cyclophosphamide group: ##, P＜0.01.
Above results suggest, cyclophosphamide 5mg/kg is the ineffective dose of treatment mice H22 hepatocarcinoma and Lewis lung cancer, cyclophosphamide 10mg/kg dosage group is the effective dose of treatment hepatocarcinoma H22 and Lewis lung cancer, can obviously improve its tumour inhibiting rate after 20 (S)-ginsenoside-Rg3 and its use in conjunction, therapeutic alliance group and corresponding dosage cyclophosphamide group relatively have significance difference (P＜0.05).Show that 20 (S)-ginsenoside-Rg3 have obvious synergistic effect.
The reduction toxicity of anticancer agents effect of test example 3 20 (S)-ginsenoside-Rg3
1, test material is with test example 1
2, content of the test: set up transplanted tumor model in the mice body with mice H22 hepatocarcinoma and Lewis lung cancer, divide into groups and administration by following group: solvent control group: the normal saline solution that gives the equivalent adjuvant
Cyclophosphamide small dose group: give cyclophosphamide 10mg/kg
Cyclophosphamide low dose+medicine small dose group: give cyclophosphamide 10+20 (S)-ginsenoside-Rg33.75mg/kg
The heavy dose of group of cyclophosphamide low dose+medicine: give cyclophosphamide 10+20 (S)-ginsenoside-Rg315mg/kg
The heavy dose of group of cyclophosphamide: give cyclophosphamide 10mg/kg
Cyclophosphamide heavy dose+medicine small dose group: give cyclophosphamide 20+20 (S)-ginsenoside-Rg33.75mg/kg
The heavy dose of group of cyclophosphamide heavy dose+medicine: give cyclophosphamide 20+20 (S)-ginsenoside-Rg315mg/kg
Cyclophosphamide heavy dose+medicine high dose group: give cyclophosphamide 20+20 (S)-ginsenoside-Rg3150mg/kg
Cyclophosphamide heavy dose+drug oral high dose group: give cyclophosphamide 10+20 (S)-ginsenoside-Rg3300mg/kg
Medication as previously mentioned.Competitive list is treated together with cyclophosphamide 10mg/kg and 20mg/kg and 20 (S)-ginsenoside-Rg33.75mg/kg, Rg315mg/kg, Rg3150mg/kg, oral Rg3300mg/kg use in conjunction are treated the weight of animals, thymus index and spleen index between each group, with analysis on hemogram instrument counting peripheral blood leucocyte, leukocyte count between relatively each is organized.
Data are represented with X ± SD, carry out statistical procedures with the t check.
3, result of the test: in mice H22 hepatocarcinoma and Lewis lung cancer tumor model, cyclophosphamide 20mg/kg dosage group is also seen body weight, immune organ organ index and leukocyte number average obviously descend (P＜0.01) when pressing down tumor.Can obviously improve by the reduction of anti-caused by cyclophosphamide mice body weight, leukopenia and atrophy of immune organ after share with the ginsenoside, improve mouse thymus and spleen organ index (seeing Table 7,8).Show that 20 (S)-ginsenoside-Rg3 can obviously reduce by the caused by cyclophosphamide toxic and side effects.Table 7 20 (S)-ginsenoside-Rg3 is to the Attenuation of cyclophosphamide in treatment mice H22 hepatocarcinoma
Rank dosage (mg/kg) thymus index body weight (g) spleen index WBC (* 109)
Solvent control group 25.52 ± 6.87 29.2 ± 2.7 25.91 ± 4.80 8.88 ± 2.57
Cyclophosphamide 20 12.40 ± 4.25** 24.0 ± 2.5** 10.10 ± 2.60** 4.25 ± 1.82**
Cyclophosphamide+Rg3 10+3.75 14.80 ± 3.77# 26.4 ± 2.0# 16.30 ± 2.26# 6.90 ± 3.03#
Cyclophosphamide+Rg3 10,+15 19.80 ± 3.52## 27.9 ± 2.8## 19.00 ± 5.09## 8.02 ± 3.09##
Cyclophosphamide+Rg3 10+,150 21.80 ± 3.48## 28.9 ± 2.8## 21.08 ± 5.29## 8.52 ± 2.79##
Cyclophosphamide+oral Rg3 10+,300 20.30 ± 3.28## 28.5 ± 2.6## 20.08 ± 4.29## 8.12 ± 2.69##
Compare with the solvent control group: * *, P＜0.01; *, P＜0.05.Compare with the cyclophosphamide group: #, P＜0.05; ##, P＜0.01.
Table 8 20 (S)-ginsenoside-Rg3 is to the Attenuation of cyclophosphamide in the treatment Mice Bearing Lewis Lung Cancer
Rank dosage (mg/kg) thymus index body weight (g) spleen index WBC (* 109/L)
Solvent control group 24.22 ± 6.89 29.5 ± 2.5 26.91 ± 4.46 9.08 ± 2.29
Cyclophosphamide 20 12.00 ± 4.37** 24.3 ± 2.0** 10.30 ± 2.31** 4.45 ± 1.89**
Cyclophosphamide+Rg3 10+3.75 15.80 ± 3.01# 26.7 ± 1.7# 15.30 ± 4.52# 7.10 ± 2.96#
Cyclophosphamide+Rg3 10,+15 19.75 ± 3.52## 28.2 ± 2.9## 19.20 ± 5.13## 8.22 ± 3.02##
Cyclophosphamide+Rg3 10+,150 21.75 ± 3.32## 29.2 ± 2.7## 21.20 ± 5.23## 8.62 ± 2.02##
Cyclophosphamide+oral Rg3 10+,300 20.10 ± 3.18## 28.7 ± 2.2## 20.18 ± 4.39## 8.10 ± 2.59##
Compare with the solvent control group: * *, P＜0.01; *, P＜0.05.Compare with the cyclophosphamide group: #, P＜0.05; ##, P＜0.01.
Test example 4 20 (S)-ginsenoside-Rg3 is to the Attenuation of x-ray bombardment tumor-bearing mice
1, test material is with test example 1
2, content of the test
Illuminate condition: use the irradiation of Philips Stabilipan, voltage 220V, electric current 10mA..Animal places and carries out whole body dose rate 0.287Gy/min in the plastic casing, target skin distance 50cm, and accumulated dose 4Gy, solvent control group 1 gives false irradiation.
Test procedure: H22 hepatocarcinoma inoculation: be taken at the above-mentioned tumor-bearing mice that the Kunming mouse intraperitoneal inoculation was gone down to posterity seven days, behind the sterilization skin of abdomen, extract ascites, add the long-pending injection normal saline dilution of triploid, sterilization Mus armpit skin, every mice inoculates 70 mices respectively in oxter injection tumor cell suspension 0.2ml.
Connect after the tumor second day and be divided into following 5 groups and administration at random:
Solvent control group 1: the normal saline solution that gives the equivalent adjuvant
Solvent control group 2: the normal saline solution that gives the equivalent adjuvant
Medicine small dose group: give 20 (S)-ginsenoside-Rg33.75mg/kg
Dosage group in the medicine: give 20 (S)-ginsenoside-Rg37.5mg/kg
The heavy dose of group of medicine: give 20 (S)-ginsenoside-Rg315mg/kg
Medicine injection high dose group: give 20 (S)-ginsenoside-Rg3150mg/kg
Drug oral high dose group: give 20 (S)-ginsenoside-Rg3300mg/kg
Desolventized in the 6th day in administration and all to carry out x-ray bombardment outside the matched group 1, radiological dose is every Mus accumulated dose 4Gy, continues administration, gets blood on the 4th day in the radiation back and surveys the WBC number.
Data are represented with X ± SD, carry out statistical procedures with the t check.
3, result of the test
By the visible mice of using the X ray total irradiation of 4Gy accumulated dose of table 9, through 20 (S)-ginsenoside-Rg3, can suppress to reduce because of radio-induced murine interleukin at the 10th day 20 (S)-ginsenoside-Rg33.75mg/kg, 7.5mg/kg, 15mg/kg, 150mg/kg, oral 300mg/kg.Prompting, 20 (S)-ginsenoside-Rg3 have obvious radiation resistance, help to strengthen the immunologic function of tumor-bearing mice self, improve its defence capability.
Table 9.20 (S)-ginsenoside-Rg3 is to the Attenuation of x-ray bombardment tumor-bearing mice
Group dosage (mg/kg) WBC (* 109/L)
Solvent control group 1----7.41 ± 1.59
Solvent control group 2----1.81 ± 0.87**
3.75????????????????????????3.15±1.56#
Rg3??????????????7.5?????????????????????????5.59±3.02##
15??????????????????????????6.39±2.01##
150?????????????????????????6.52±1.13##
Oral Rg3 300 6.41 ± 1.91##
*, p＜0.05, p＜0.01; Expression is compared * * with solvent control group 1; #p＜0.05, ##p＜0.01; Expression is compared with solvent control group 2
The acute toxicity test of test example 5 20 (S)-ginsenoside-Rg3
1, test material is with test example 1
2, content of the test
Get 50 of mices, body weight 18 ~ 22g, male and female half and half, divide 5 groups at random, dosage is 312.5mg/kg, 250mg/kg, 200mg/kg, 160mg/kg, 128mg/kg, administering mode: intravenous injection, administration volume: 0.4ml/20g, death appearred in 1 hour in mice after the administration, observed 7 days total death condition of mice, and the LD50 value is calculated with the Kou Shi improved method.
3, result of the test
By table 10 as seen, the dosage group is that 312.5mg/kg is all dead as a result, and the dosage group is dead 8 of 250mg/kg, and the dosage group is dead 3 of 200mg/kg,, the dosage group is that death does not appear in 160mg/kg, 128mg/kg.LD50 (95% fiducial limit): 218.7 ± 28.6mg/kg.The acute toxicity test of table 10:20 (S)-ginsenoside-Rg3
Dosage death toll mortality rate
312.5mg/kg??????????10???????????????1
250mg/kg????????????8????????????????0.8
200mg/kg????????????3????????????????0.3
160mg/kg????????????0????????????????0
128mg/kg????????????0????????????????0
Claims (8)
1. one kind with 20 (S)-ginsenoside-Rg
3Be effective ingredient, be used to strengthen the cancer therapy drug curative effect, the medicine of the leucocytes reduction that reduction toxicity of anticancer agents, prevention and treatment chemicotherapy cause.
2. medicine according to claim 1, it is by 20 (S)-ginsenoside-Rg
3Form with pharmaceutically acceptable carrier.
3. medicine according to claim 2, it can be with oral or injection administration, and drug administration by injection can be for injecting in intravenous injection, intramuscular injection, lumbar injection, subcutaneous injection or the tumor body.
4. medicine according to claim 3, oral formulations can be tablet, capsule, pill, granule, drop pill, soft capsule, suspension, solution, syrup, capsule, granule, drop pill; Injection preparation can be freeze-dried powder, injection vein emulsion, injection, transfusion.
5. medicine according to claim 4, oral formulations is preferably tablet, capsule, granule; The preferred freeze-dried powder of injection preparation, injection vein emulsion.
6.20 (S)-ginsenoside-Rg
3Has the application in the medicine that strengthens the cancer therapy drug curative effect, reduces the leucocytes reduction that toxicity of anticancer agents, prevention and treatment chemicotherapy cause in preparation.
7. application according to claim 6, its using dosage scope is 1mg～2000mg.
8. application according to claim 7, preferred dose scope are 20mg～500mg.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008010668A1 (en) * | 2006-07-18 | 2008-01-24 | Sk Chemicals Co., Ltd. | 20(s -ginsenoside rg3 as an anti-angiogenic composition |
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2003
- 2003-12-06 CN CN 200310114432 patent/CN1623553A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008010668A1 (en) * | 2006-07-18 | 2008-01-24 | Sk Chemicals Co., Ltd. | 20(s -ginsenoside rg3 as an anti-angiogenic composition |
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