CN1132841C - Total triterpenoid saponin in coral ardisa root or other plants in same family and preparing process thereof - Google Patents

Total triterpenoid saponin in coral ardisa root or other plants in same family and preparing process thereof Download PDF

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CN1132841C
CN1132841C CN 99105451 CN99105451A CN1132841C CN 1132841 C CN1132841 C CN 1132841C CN 99105451 CN99105451 CN 99105451 CN 99105451 A CN99105451 A CN 99105451A CN 1132841 C CN1132841 C CN 1132841C
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saponin
triterpenoid saponin
described total
ardisia
root
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CN1270174A (en
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边宝林
王素芬
杨健
王宏杰
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Institute of Materia Medica of CAMS
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Traditional Chinese Medicine Inst China Academy Of Traditional Chinese Medicin
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Abstract

The present invention relates to an antineoplastic Chinese drug preparation which is made by extracting the component of total triterpenoid saponin from ardisia crenata, etc. by macroporous resin in an etanol reflux or a methanol reflux mode. Plants in myrsinaceae ardisia, such ardisia. Crenate, A. japonica, A. crispa, A. quinquengona, A. pusilla, etc. contain the component of total triterpenoid saponin which contains 2 to 5% of pentacyclic triterpene. The component of the class has obvious tumor inhibition effect on various mouse transplant tumours (tests in vivo) and various human tumor cells (tests in vitro). The clinical examination results of the oral administration tests of a plurality of cases of tumour patients show that the present invention has certain antineoplastic activity.

Description

Total triterpenoid saponin and preparation method in Root of Coral Ardisia and the congener
The invention belongs to technical field of traditional Chinese medicines, particularly relate to a kind of antitumor Chinese medicine total triterpenoid saponin and preparation method, total triterpenoid saponin derives from Myrsinacea Ardisa plant Root of Coral Ardisia (Ardisia.crenate), the Japanese Ardisia Herb (A.japonica) Root of Crispateleaf Ardisia (A..crispa), A..quinquengona (A..quinquengona), Ardisia pusilla (A.pusilla).Tumour is one of high disease kind of the human mortality ratio of our times scope, and people drop into a large amount of manpower and materials and research and develop antineoplastic new drug for this reason.Searching good effect, the antitumor drug that toxicity is little, domestic and international vast drug research person, separation and Extraction has obtained some chemical substances from plant, but the quantity that really can develop patent medicine is few.And the screening expense is very high.It is very big to drop into manpower and materials.So seek safety, effectively drop into suitable antitumor drug and be still current very important task.The objective of the invention is to set up a kind of method that can extract antitumor total triterpenoid saponin in Root of Coral Ardisia and the congener, its development is become anti-cancer agent.Root of Coral Ardisia is the root of Myrsinacea Ardisa plant (Ardisia crenata Sims), beginning is stated from Compendium of Material Medica, have effects such as clearing heat and detoxicating, blood stasis removing analgesic, the clinical diseases such as sense, tonsillitis, diphtheria, erysipelas, poradenolymphitis, rheumatism, wound that are used for.This paper is on the basis of summing up medication experience among the people, Root of Coral Ardisia, the Japanese Ardisia Herb, Root of Crispateleaf Ardisia, A..quinquengona, Ardisia pusilla total triterpenoid saponin have been carried out multinomial anti-tumor experiment, the result shows stronger anti-tumor activity: external pharmacodynamics shows that total triterpenoid saponin has obvious restraining effect to leukemia cell (HL-60), lung carcinoma cell (PG), oral squamous carcinoma cell (KB).2mg-200mg/kg dosage is used in the mice transplanted tumor experiment, and S180-sarcoma, U14-uterine neck knurl, liver H22 tumour, lung cancer etc. are all had restraining effect.LD 50=1802mg/kg is 10 times of the highest effective dose, and to compare its toxicity not very big with antitumor drug, has the good prospect of the Chinese medicine of making antineoplastic new.
Total triterpenoid saponin is to the heavy inhibiting rate (%) of mouse tumor knurl
Knurl strain kind Inhibiting rate
The S180-sarcoma 30~40%
U14-uterine neck knurl 25~30%
Liver H22 tumour 35~50%
Lewis lung cancer 40~60%
The total triterpenoid saponin extraction process:
Root of Coral Ardisia or congener root are cleaned, pulverized 20 mesh sieves, take by weighing 1 kilogram and put into the refluxing extraction device, add 10%-100% ethanol or methyl alcohol, reflux 30-60 minute, leach extracting solution, residue according to said method extracts one time again, leach extracting solution and extracting solution merging for the first time, united extraction liquid is evaporated to 1 liter, centrifugal 25 minutes (3000 rev/mins) incline and supernatant liquor, join on 4 liters of macroporous resins (HP-20) post, earlier with 25 liters of flushing with clean water, again with 20 liters of 50%-100% ethanol elutions and collect elutriant, with the elutriant concentrating under reduced pressure at the 1.5-1.6 liter, the reduced vacuum drying is (55-60 ℃ then, 0.08MPa more than) take out and to be ground into fine powder, add 10 times of amount 85%-100% ethanol of fine powder, stirring and dissolving is placed and is spent the night, and centrifugal 15 minutes (300rpm) inclines and supernatant liquor, be evaporated to 90-100ml, (60-65 ℃ of reduced vacuum drying, 0.08MPa more than), take out and pulverize, get the Root of Coral Ardisia total triterpenoid saponin.Technical process is as follows:
Root of Coral Ardisia (Ardisia crenata sims) or congener root
↓ wash-out
The 10%-100% alcohol reflux
Concentrated solution
Macroporous resin (HP-20)
Water elution
The 50%-100% ethanol elution
Concentrate eluant
The drying under reduced pressure concentrated solution
Total triterpenoid saponin
Through our test for many years, from Root of Coral Ardisia and congener, separate obtaining multiple saponin, its basic structure is triterpenoid saponin (structural formula is attached).From plant, separate the antineoplastic component that obtains at present and mostly be biological alkali class and diterpene-kind compound, the antitumor research of triterpenoid saponin chemical ingredients is also few, so the antitumor Chinese medicine that total triterpenoid saponin is developed into can be subjected to the extensive patients welcome and have vast market prospect.Total triterpenoid saponin can be made into Chinese medicine various formulations, for example capsule formulation, granule, tablet, electuary etc. commonly used.
Figure C9910545100061

Claims (13)

1, a kind of method of extracting Root of Coral Ardisia and congener total triterpenoid saponin thereof is characterized in that: water or ethanol, methanol extraction, through resin, ethanol, methanol-eluted fractions, powder process gained; The saponin structure of isolating is in the Ardisa Root of Coral Ardisia:
Figure C9910545100021
2, by the described total triterpenoid saponin extracting method of claim 1, wherein ethanol or methanol concentration are 10~100%.
3, by the described total triterpenoid saponin extracting method of claim 1, wherein resin is the macroporous resin class.
4, by the described total triterpenoid saponin wash-out of claim 1 with ethanol or methanol concentration 50~100%.
5,, wherein need to concentrate or drying under reduced pressure by the described total triterpenoid saponin extracting method of claim 1.
6, by the described total triterpenoid saponin method of claim 1, wherein total saponin content is 10~100%.
7, mice transplanted tumor is had in the inhibiting medicine in preparation by claim 1 or 6 described total saponins and use.
8, be to mouse S in preparation by the described application of claim 7 180Sarcoma, liver H 22, uterus U 14, Lewis tumour, leukemia, Ehrlich press ascitic tumor to have in the inhibiting medicine and use.
9, be application in vitro inhibition HL-60 cell, PG cell, KB cell by the described application of claim 7.
10, a kind of capsule wherein contains the described total saponin of claim 1.
11, a kind of granule wherein contains the described total saponin of claim 1.
12, a kind of tablet wherein contains the described total saponin of claim 1.
13, a kind of electuary wherein contains the described total saponin of claim 1.
CN 99105451 1999-04-08 1999-04-08 Total triterpenoid saponin in coral ardisa root or other plants in same family and preparing process thereof Expired - Fee Related CN1132841C (en)

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Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101157717B (en) * 2006-10-04 2011-05-11 薛永新 Preparation method of Ardisia mamillata B and uses thereof
CN101333242B (en) * 2008-08-04 2011-05-04 中国人民解放军第四军医大学 New antineoplastic compounds of triterpenoid saponin
CN101381391B (en) * 2008-08-04 2011-04-13 中国人民解放军第四军医大学 Triterpene saponins compounds extracted from ardipusilloside
CN104306260B (en) * 2014-10-23 2018-03-09 桂林莱茵生物科技股份有限公司 Extract containing galloyl Bergenin and its preparation method and application
CN107669772A (en) * 2017-11-23 2018-02-09 陈子豪 A kind of Chinese medicine preparation for alleviating early carcinoma of stomach patient's anorexia

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