CN1008183B - Prodn. method of a new pattern medicine fulingsu - Google Patents
Prodn. method of a new pattern medicine fulingsuInfo
- Publication number
- CN1008183B CN1008183B CN 88100033 CN88100033A CN1008183B CN 1008183 B CN1008183 B CN 1008183B CN 88100033 CN88100033 CN 88100033 CN 88100033 A CN88100033 A CN 88100033A CN 1008183 B CN1008183 B CN 1008183B
- Authority
- CN
- China
- Prior art keywords
- fuling
- medicine
- present
- fulingsu
- suction filtration
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention discloses a novel medicine named Fulingsu which has the functions of resisting tumours and activating immunity. The novel medicine of the present invention is a tetracyclic-triterpane compound which is an effective ingredient extracted from tuckahoe. The preparation method of the medicine of the present invention discloses in the flowchart, and the product quality is detected by ultraviolet absorption quantitative measurement, thin layer scanning content analysis and bioactivity measurement of nucleoside transportation. Compared with the Tuckahoe which is a traditional Chinese medicine, the Fulingsu prepared by the method of the present invention has the advantages of obvious clinical adaptability, wide action range, few used curative doses, etc.
Description
Su-fuling is the one group of tetracyclic triterpenes effective ingredient for preparing from the Chinese medicine Poria cocos, and its molecular weight is about 500.
Poria cocos is China's traditional Chinese medicine, has hundreds of years and uses history, still continues to use tame sclerotium so far as raw material, makes medicine materical crude slice, adds in the Chinese medicine preparation and uses, and its efficacy of drugs is mainly diuresis according to record and relieves oedema or abdominal distension through diuresis or purgation, the peaceful heart of invigorating the spleen.The research of relevant Poria cocos mainly concentrates on Pachymose 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 cocos is come out, and by test, further develops the pharmacological function of Poria cocos, 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 4.5l95% ethanol, 0.5l0.5N hydrochloric acid stirred four hours, and suction filtration separates filtrate and filter cake.
Filter cake adds 4.5l95% ethanol again, and 0.5l0.5N hydrochloric acid stirred four hours, suction 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, suction 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. quality product detection method:
(1), ultraviolet absorption method (quantitative assay): quantitatively take by weighing sample, use 95% dissolve with ethanol, making and surveying periodic strength of solution is 50 μ g/ml, be placed in the optical path 1cm quartz cuvette, on ultraviolet spectrophotometer, use the 243nm wavelength, measure its optical density (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% Xylo-Mucine, the long 20 * 5cm of plate.
Solvent system: sherwood oil: benzene: ethyl acetate: ethanol: glacial acetic acid is 4: 6: 4: 0.2: 0.1.
Point sample: put 15 μ l samples on the thin layer plate for preparing in advance with microsyringe.
Advance: carry out with above-mentioned solvent system
Scanning: Tianjin, island thin layer chromatography scanner, the condition of scanning:
Sample wavelength 240nm
Reference wavelength 375nm
Sweep velocity 80mm/min
Recording paper 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):
Specimen preparation: quantitatively take by weighing product,, with 6NHCl PH is proofreaied and correct to about 7.5 again with the 0.15NNaOH dissolving.
Mouse leukemia L1210 cell preparation: the L1210 cell preservation of in the DBA/2 mouse, 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 nutrient solutions, uses 1000rpm at every turn, remove supernatant liquor 30 seconds, cell is diluted to 10 with 199 nutrient solutions again
7Ml
-1
The composition of cell culture tube (plate):
Cell suspension (10
6Cell) 100 μ l
Calf serum 100 μ l
199 nutrient solutions, 700 μ l
Medicine (100-800 μ g ml
-1) 100 μ l
Control group replaces medicine with salt solution.
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.
Isotropic substance participates in: every pipe (hole) adds 2 μ Ci
2The H-thymidine, mixing was cultivated 5 minutes in water-bath again, took out and put into ice-water bath immediately.
Numeration: the sample suction filtration with salt washing 6 times, is used 10% trichlorine pickling once again on filter paper, 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 different concns drug effect
3The H-thymidine participates in L1210 cell inhibiting rate, is abscissa with the drug level, and inhibiting rate 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 activate 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 nucleosides, therefore can suppress the synthetic of tumour cell DNA, and the growth to tumour cell in the body has certain restraining effect.Sarcoma 180 inhibiting rate 70%, ehrlich ascites tumor 100%.
B. use 4-8mg/Kg dosage, ten days, su-fuling can act synergistically with multiple anticarcinogen, improves the inhibition ability to tumour.Therefore might develop into anticancer synergist.
C. use 4-8mg/Kg dosage, ten days, Poria cocos 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 cocos have the promotion Differentiation.Do exhausted human leukemia HL-60 cell 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 activating cells film on Na
+K
+The ATP enzyme promotes K
+Absorption, therefore the effect that improves heart disorder is arranged, can be developed to the ARR medicine of treatment.
(4) diuresis, elimination oedema: use 8-16mg/kg dosage, ten days, experimentation on animals 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(PG).Prostaglandin(PG) is a secondary medium hypersensitive.Therefore, su-fuling suppresses anaphylactoid effect, might prevent or treat type clinically.
(6). antivirus action: use 25-50mg/Kg dosage, five days, through su-fuling activatory scavenger cell, can suppress the growth of simplexvirus significantly, also observe the growth that it can suppress duck hepatitis virus in vivo.
4, preclinical pharmacology research (toxicology):
(1). lethal dose (LD50) mouse
Vein 370mg/Kg
Abdominal cavity 670mg/Kg
Oral＞5000mg/Kg.
(2), subacute toxicity: rat and dog 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 tract, the recycle system, urinary system all less than the influence.
Advantage of the present invention is with positively effect: compare with the traditional Chinese medicine Poria cocos, su-fuling not only can regulate heart rate, improve sleep and appetite, eliminate oedema, the Ammonium Glycyrrhizate reaction, experimentation on animals shows, use su-fuling also can suppress murine sarcoma 180, inhibiting rate 70% separately, ehrlich carcinoma inhibiting rate 100%, lung cancer metastasis model inhibiting rate 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 inhibiting rate, and the coupling collar phosphamide uses, and the efficient 100%(of reaching uses the inhibiting rate of endoxan to be 20-30% separately).Therefore, su-fuling has tangible indication, acts on more extensive than Poria cocos.The su-fuling consumption is 8-50mg/Kg, people's consumption be 400mg/ days-2500mg/ days, directly use the Chinese medicine Poria cocos to be difficult to the dosage that reaches such.
Claims (1)
1, a kind of manufacture method with newtype drug su-fuling of antitumor and immune activation effect, it is characterized in that it being that the 1Kg Poria powder is added 4.5L95% ethanol, 0.5L0.5N hydrochloric acid, stirred the companion 4 hours, suction filtration, the ethanolic soln of the polysaccharide that is removed is with 10N sodium hydroxide solution 26ml, transfer between the PH to 7-8, concentrating under reduced pressure (bath temperature is 50 ℃) is blown away residual ethanol, transfers PH to 10 to filter, obtain su-fuling solution, to PH2.5-3, su-fuling is precipitated comes out, and it is inserted refrigerator overnight with the 6N hcl acidifying, make its precipitation cmpletely, suction filtration is used the less water washing precipitation then, and is dry in vacuum drying oven, grind into powder is the su-fuling goods.
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 CN1035051A (en) | 1989-08-30 |
| CN1008183B true 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 (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1326554C (en) * | 2001-04-02 | 2007-07-18 | 李洪芬 | Antitumour medicine |
| EP1535619B1 (en) * | 2003-11-25 | 2008-03-19 | Sinphar Pharmaceutical Co., Ltd. | Poria extract devoid of secolanostane derivatives comprising lanostane derivatives for immunity enhancement |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| CN113527424B (en) * | 2021-07-16 | 2023-04-14 | 福建掌链科技有限公司 | Poria polypeptide and antiviral effect thereof |
-
1988
- 1988-01-12 CN CN 88100033 patent/CN1008183B/en not_active Expired
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1326554C (en) * | 2001-04-02 | 2007-07-18 | 李洪芬 | Antitumour medicine |
| EP1535619B1 (en) * | 2003-11-25 | 2008-03-19 | Sinphar Pharmaceutical Co., Ltd. | Poria extract devoid of secolanostane derivatives comprising lanostane derivatives for immunity enhancement |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1035051A (en) | 1989-08-30 |
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