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.