CN1035051A - A kind of manufacture method of newtype drug su-fuling - Google Patents
A kind of manufacture method of newtype drug su-fuling Download PDFInfo
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- CN1035051A CN1035051A CN 88100033 CN88100033A CN1035051A CN 1035051 A CN1035051 A CN 1035051A CN 88100033 CN88100033 CN 88100033 CN 88100033 A CN88100033 A CN 88100033A CN 1035051 A CN1035051 A CN 1035051A
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Abstract
A kind of newtype drug su-fuling with antitumor and immune activation effect is the effective ingredient tetracyclic triterpenoid that extracts from the Chinese medicine Poria, and its manufacture method is shown in flow chart:
The product quality detection method is uv absorption quantitative assay, thin slice scan analysis of components and nucleoside transporting biological activity determination.Advantage and good effects such as the su-fuling that the present invention obtains has more obvious clinical indication than Chinese medicine Poria, and sphere of action is more extensive, and the effective dose of use is very little.
Description
Su-fuling is the one group of tetracyclic triterpenes active ingredient for preparing from the Chinese medicine Poria, and its molecular weight is about 500.
Poria is China's Chinese medicine, has hundreds of years and uses history, still continues to use tame sclerotium so far as raw material, makes decoction pieces, adds in the Chinese medicinal formulae and uses, and its efficacy of drugs is mainly diuresis according to record and relieves oedema or abdominal distension through diuresis or purgation, the spleen invigorating mind calming.The research of relevant Poria mainly concentrates on pachyman at present both at home and abroad, comprises aspects such as its preparation, structure determination, chemical improvement, antitumor action.But the research of relevant su-fuling composition does not see that as yet report is arranged in nearly ten years.
Purpose of the present invention is that the extracts active ingredients in the Poria is come out, and by test, further develops the pharmacological function of Poria, and is used for the specific indication of clinical solution by the doctor trained in Western medicine mode.
Subject matter of the present invention:
1. the preparation flow of su-fuling: the 1kg Poria powder, add 4.5195% ethanol, 0.510.5N hydrochloric acid stirred four hours, sucking filtration, separately filtrate and filter cake.
Filter cake adds 4.5195% ethanol again, and 0.510.5N hydrochloric acid stirred four hours, sucking filtration, and filter cake discards, and filtrate is used for the extraction of following batch raw material.
Primary filtrate is transferred between the PH to 7-8 concentrating under reduced pressure (bath temperature is 50 ℃) with the about 26ml of 10N sodium hydroxide solution, concentrated solution is blown away residual ethanol, transfers PH to 10, filters, to PH2.5-3.0, su-fuling promptly is precipitated out filtrate, standing over night in refrigerator with the 6N hcl acidifying, make precipitation fully, sucking filtration is used a small amount of water washing and precipitating, in vacuum drying oven, drain, grind into powder promptly gets the su-fuling goods, and yield is 2/1000ths to three.
2. product quality detection method:
(1), ultraviolet absorption method (quantitative assay): quantitatively take by weighing sample, use 95% dissolve with ethanol, making and surveying periodic solution concentration is 50 μ g/ml, be placed in the optical path 1cm quartz cuvette, on ultraviolet spectrophotometer, use the 243nm wavelength, measure its trap (A) numerical value, with the percentage composition of su-fuling in the following formula calculation sample.
The percentage composition of su-fuling in the sample=[(A value * 200)/99.48] * 100%
The A of su-fuling
1% 1cm(λ 243nm)=99.48
(2), thin layer chromatography scanning (analysis of components): quantitatively take by weighing sample, be mixed with 10mg/ml solution with 95% ethanol.
Plate-making method: the 2g silica GF254 adds the 7ml0.5% sodium carboxymethyl cellulose, the long 20 * 5cm of plate.
Solvent system: petroleum ether: benzene: ethyl acetate: ethanol: glacial acetic acid is 4:6:4:0.2:0.1.
Point sample: put 15 μ l samples on the lamellae for preparing in advance with microsyringe.
Advance: carry out with above-mentioned solvent system
Scanning: Tianjin, island thin-layer chromatogram scanner, the condition of scanning:
Sample wavelength 240nm
Reference wavelength 375nm
Scanning speed 80mm/min
Recorder chart speed 40mm/min
Slit 10 * 0.4mm
Scanning result is directly got the content of each component by printer.
(3), nucleoside transporting method (biological activity):
Sample preparation: quantitatively take by weighing product, with the 0.15NNaOH dissolving, reuse 6NHCl proofreaies and correct PH to about 7.5.
Mouse leukemia L1210 cell preparation: the L1210 cell preservation of in the DBA/2 mice, going down to posterity, extract 6-8 days oncocyte of growth from the abdominal cavity during use, it is inferior to give a baby a bath on the third day after its birth with 199 culture fluid, uses 1000rpm at every turn, remove supernatant 30 seconds, cell reuse 199 culture fluid are diluted to 10
7Ml
-1
The composition of cell culture tube (plate):
Cell suspension (10
6Cell) 100 μ l
Calf serum 100 μ l
199 culture fluid, 700 μ l
Medicine (100-800 μ g ml
-1) 100 μ l
Matched group replaces medicine with saline.
Cultivate: above-mentioned cultivation suspension was cultivated 3 hours earlier down at 37 ℃, took out and put into 37 ℃ of waters bath with thermostatic control.
Isotope participates in: every pipe (hole) adds 2 μ Ci
3The H-thymidine, mixing was cultivated 5 minutes in water-bath again, took out and put into ice-water bath immediately.
Numeration: the sample sucking filtration is on filter paper, and with salt washing 6 times, reuse 10% trichlorine pickling once, dehydrated alcohol is washed once, drains, and takes out the scraps of paper and puts into the numeration bottle, add 2ml mixing scintillation solution, count on FJ-2100 type liquid scintillation numeration instrument, it is right to calculate under the variable concentrations drug effect
3The H-thymidine participates in L1210 cell inhibiting rate, is abscissa with the drug level, and suppression ratio is an ordinate, and the IC50(half-inhibition concentration is obtained in drawing from figure).The half-inhibition concentration of su-fuling is about the every ml10 of 35-37 μ g/ml(
6The L1210 cell).
3, biological activity:
(1) immune activation effect: at 10-15mg/Kg dosage, in three days, su-fuling can live mouse macrophage and lymphocyte.
(2), antitumor action:
A. use 35-37 μ g/ml, three hours, su-fuling can suppress the transhipment of tumor cell membrane to nucleoside, therefore can suppress the synthetic of tumor cell DNA, and the growth to tumor cell in the body has certain inhibitory action.Sarcoma 180 suppression ratio 70%, ehrlich ascites tumor 100%.
B. use 4-8mg/Kg dosage, ten days, su-fuling can with multiple anticarcinogen synergism, improve inhibition ability to tumor.Therefore might develop into anticancer synergist.
C. use 4-8mg/Kg dosage, ten days, Poria have the effect of leukocyte increasing, when share with anticarcinogen, can prevent by the caused leukopenia of anticarcinogen.
D. use 10-100 μ g/ml, ten days, Poria have the promotion differentiation.Do exhausted human leukemia HL-60 cell's strain through su-fuling, not only form can be observed differentiating phenomenon, and cell enzyme activity and cell function all have recovery.
(3). improve heart rate: use 8-16mg/Kg dosage, ten days, su-fuling can the active cell film on Na
+K
+The ATP enzyme promotes K
+Absorption, therefore the effect that improves arrhythmia is arranged, can be developed to the ARR medicine of treatment.
(4) diuresis, elimination edema: use 8-16mg/kg dosage, ten days, zoopery showed that su-fuling can be eliminated ascites significantly, can be developed to diuresis, consumer edema medicine.
(5). anti-allergic effects: use 60mg/Kg dosage, seven days, su-fuling can promote the rising of cell CAMP, improved the ratio of CAMP/CGMP.CAMP raises and can suppress the release of histamine (former medium hypersensitive).Su-fuling can also suppress disengaging of prostaglandin.Prostaglandin is a secondary medium hypersensitive.Therefore, su-fuling suppresses anaphylactoid effect, might prevent or treat anaphylaxis clinically.
(6). antivirus action: use 25-50mg/Kg dosage, five days, through the activatory macrophage of su-fuling, can suppress the growth of herpesvirus significantly, also observe the growth that it can suppress DHV in vivo.
4, preclinical pharmacology research (toxicology):
(1). fatal dose (LD50) mice
Vein 370mg/Kg
Abdominal cavity 670mg/Kg
Oral〉5000mg/Kg.
(2), subacute toxicity: rat and Canis familiaris L. 50,200,500mg/Kg, oral administration two months there is no overt toxicity reaction, tissue slice is no abnormality seen also.
(3), experimental result, do not observe teratogenesis, cause prominent, carcinogenesis.
(4), general pharmacology, to respiratory system, digestive system, blood circulation, urinary system all less than the influence.
Advantage of the present invention is with good effect: compare with the Chinese medicine Poria, su-fuling not only can regulate heart rate, improve sleep and appetite, eliminate edema, the Polyglucan reaction, zoopery shows, use su-fuling also can suppress murine sarcoma 180, suppression ratio 70% separately, ehrlich carcinoma suppression ratio 100%, lung cancer metastasis model suppression ratio 40-60%; Share with multiple anticarcinogen, all show the obvious synergistic effect, can prevent the leukopenia that anticarcinogen causes; Experiment showed, the 25-50mg/Kg administration five days with duck hepatitis model, can obviously suppress viral growth; The rat autoimmune disease model experiment showed, that independent use su-fuling is 50% to autoimmune disease morbidity suppression ratio, and the coupling collar phosphamide uses, and effective percentage reaches 100%(and uses the suppression ratio of cyclophosphamide to be 20-30% separately).Therefore, su-fuling has tangible indication, acts on more extensive than Poria.The su-fuling consumption is 8-50mg/Kg, people's consumption be 400mg/ days-2500mg/ days, directly use the Chinese medicine Poria to be difficult to the dosage that reaches such.
Claims (9)
1, a kind of manufacture method with newtype drug su-fuling of antitumor and immune activation effect is characterized in that said method is to adopt the research means of modern medicine and pharmacology, extracts the effective ingredient tetracyclic triterpenoid from the Chinese medicine Poria.
2, according to the described manufacture method of claim 1, it is characterized in that the 1Kg Poria powder is added 4.5L95% ethanol, 0.5L0.5N hydrochloric acid stirred the companion 4 hours, sucking filtration, the alcoholic solution of the polysaccharide that is removed.
3, according to the described manufacture method of claim 2, it is characterized in that the ethanol filtrate that will obtain for the first time, with 10N sodium hydroxide solution 26ml, transfer between the PH to 7-8 concentrating under reduced pressure (bath temperature is 50 ℃).
4, according to the described manufacture method of claim 3, it is characterized in that concentrated solution is blown away residual ethanol, transfer PH to 10 to filter, obtain su-fuling solution.
5,, it is characterized in that with su-fuling solution with the 6N hcl acidifying that to PH2.5-3 su-fuling is precipitated comes out according to the described manufacture method of claim 4.
6,, it is characterized in that the su-fuling precipitation is put into refrigerator left standstill liquid, made its precipitation cmpletely according to the described manufacture method of claim 5, sucking filtration is used the low amounts of water washing precipitation then, and is dry in vacuum drying oven, grind into powder is the su-fuling goods, and total recovery is 2/1000ths to three.
7, according to the described manufacture method of claim 6, it is characterized in that the su-fuling goods that obtain, available ultraviolet absorption method is measured the content value of 243nm wavelength: [(A value * 200)/99.48] * 100%.
8, according to the described manufacture method of claim 6, it is characterized in that the su-fuling goods that obtain, its composition of available tlc scanning determination, scanning result demonstrates the percentage composition of each component.
9, according to the described manufacture method of claim 6, it is characterized in that the su-fuling goods that obtain, available nucleoside transporting method is measured its biological activity, and the result shows that it is the every ml10 of 35-37 μ g/ml(that its half suppresses dense
6The L1210 cell).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 88100033 CN1008183B (en) | 1988-01-12 | 1988-01-12 | Prodn. method of a new pattern medicine fulingsu |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 88100033 CN1008183B (en) | 1988-01-12 | 1988-01-12 | Prodn. method of a new pattern medicine fulingsu |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1035051A true CN1035051A (en) | 1989-08-30 |
| CN1008183B CN1008183B (en) | 1990-05-30 |
Family
ID=4831137
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 88100033 Expired CN1008183B (en) | 1988-01-12 | 1988-01-12 | Prodn. method of a new pattern medicine fulingsu |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1008183B (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103550265A (en) * | 2013-11-08 | 2014-02-05 | 山东省中医药研究院 | Extraction method of active ingredients of tuckahoe peels and tuckahoe peel extracts |
| US9370540B2 (en) | 2014-05-21 | 2016-06-21 | Sinphar Pahrmaceutical Co., Ltd. | K2 composition and the preparation method and use of the same |
| CN107373664A (en) * | 2017-07-18 | 2017-11-24 | 杏辉天力（杭州）药业有限公司 | A kind of composition with anti-PM2.5 particulate matters effect |
| CN113527424A (en) * | 2021-07-16 | 2021-10-22 | 福建掌链科技有限公司 | Poria polypeptide and antiviral effect thereof |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE319462T1 (en) * | 2001-04-02 | 2006-03-15 | Hongfen Li | ANTINEOPLASTIC DRUG |
| DE60319840T2 (en) * | 2003-11-25 | 2009-04-09 | Sinphar Pharmaceutical Co., Ltd. | Poria extract free of Secolanostanderivaten containing Lanostanderivate for immune enhancement |
-
1988
- 1988-01-12 CN CN 88100033 patent/CN1008183B/en not_active Expired
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103550265A (en) * | 2013-11-08 | 2014-02-05 | 山东省中医药研究院 | Extraction method of active ingredients of tuckahoe peels and tuckahoe peel extracts |
| CN103550265B (en) * | 2013-11-08 | 2015-07-01 | 山东省中医药研究院 | Extraction method of active ingredients of tuckahoe peels and tuckahoe peel extracts |
| US9370540B2 (en) | 2014-05-21 | 2016-06-21 | Sinphar Pahrmaceutical Co., Ltd. | K2 composition and the preparation method and use of the same |
| TWI547284B (en) * | 2014-05-21 | 2016-09-01 | 杏輝藥品工業股份有限公司 | Fu-ling extract and preparation method and use of the same |
| CN107373664A (en) * | 2017-07-18 | 2017-11-24 | 杏辉天力（杭州）药业有限公司 | A kind of composition with anti-PM2.5 particulate matters effect |
| CN107373664B (en) * | 2017-07-18 | 2021-02-05 | 杏辉天力（杭州）药业有限公司 | Composition with PM2.5 particle resistance effect |
| CN113527424A (en) * | 2021-07-16 | 2021-10-22 | 福建掌链科技有限公司 | Poria polypeptide and antiviral effect thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1008183B (en) | 1990-05-30 |
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