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 higher disease kind of the interior 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 be developed to medicine is few, and the screening expense is very high, it is very big to drop into manpower and materials, is still current very important task so seek the antitumor drug safe and effective, that cost is suitable.
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 (Ardisia crenatesims) of Myrsinacea Ardisa plant, 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).The mice transplanted tumor experiment is used 2mg-200mg/kg dosage, to S
180-sarcoma, U
14-uterine neck knurl, liver H
22Tumour, lung cancer etc. all have restraining effect.LD
50=1802mg/kg is 10 times of the highest effective dose, and compare its toxicity with other antitumor drug less, can be made into anti-cancer agent.
Total triterpenoid saponin is to the heavy inhibiting rate (%) of mouse tumor knurl
Knurl strain kind | Inhibiting rate |
S
180-sarcoma
| ????30~40% |
U
14-uterine neck knurl
| ????25~30% |
Liver H
22Tumour
| ????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 minutes, leach extracting solution, residue according to said method extracts one time again, leaches extracting solution and extracting solution merging for the first time, and 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 1.5~1.6 liters, the reduced vacuum drying is (55~60 ℃ then, 0.08Mpa more than), take out and 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, centrifugal 15 minutes (3000rpm) inclines and supernatant liquor, is evaporated to 90-100ml, (60~65 ℃ of reduced vacuum dryings, 0.08Mpa more than), take out and pulverize, get the Root of Coral Ardisia total triterpenoid saponin.Through our experimental study for many years, from Root of Coral Ardisia and congener, separate obtaining total saponin, be meant triterpenoid saponin (structural formula is attached).
R
1??????????????????????R
2
CH
2OH?????????????????
CHO??????????????????????
CHO??????????????????????