The Glycosylated Modification Of Three Steroidal Compounds And The External Antitumor Activity Research

With the developing of human science and technology,the living environment of human bing is constantly harsh,haze?dust storm?ozone hole?water pollution and so on,human beings has being experienceed this kind of harsh living environment,human body is also being changed,but absolutely,the large number of the changes is the malignant mutation,the most representative of which is cancer,"cancer" has become a problem that people can not avoid.Cancer is a kind of tumor,the tumor is a serious harm disease to human health,chemotherapy as a major treatment of cancer is by chemical drugs.Now the antitumor drugs used in the clinical treatment of chemotherapy have the problems of poor efficacy and serious side effects.It is urgent to find a drug with specific selectivity,small damage to human normal cells and high anti-tumor effect.There are two main sources of medicine: chemical synthesis and separation of natural products.The experiment from the two sources of drugs.1)Three steroid compounds:Cholesterol,Pregnenolone,16,17-alpha Epoxypregnenolone were used as steroidal saponins by chemical synthesis.The saponins of six steroidal compounds modified with D-glucose,L-arabinose and L-rhamnose were synthesized by acetimido method,which were Cholesty-5-ene-3?-ol-3-O-?-D-pyranglucopyranoside,Progester-5,20-diene-3?-ol-3-O-?-D-pyranglucopyranoside,Cholesty-5-ene-3?-ol-3-O-?-D-pyranarabinoside,Progester-5,20-diene-3?-ol-3-O-?-D-pyranarabinoside,Cholesty-5-ene-3?-ol-3-O-?-D-pyranrhamnoside,16?,17?-epoxypregna-5,20-diene-3?-ol-3-O-?-D-pyranarabinoside,mouse neuroma cells as the test cells,the result of the six compounds in vitro antitumor activity test is no anti-tumor activity inhibition.2)Neuro-2a cells(mouse neuroma cells)were selected as the test cells from the natural product source by MTT method.The components of the crude product column chromatography were subjected to anti-tumor activity tracing,which was then isolated from pure substance with anti-tumor activity against Neuro-2a cells.A pure substance with high antitumor activity against Neuro-2a cells was isolated and the 24hIC50 reached 16 ?g / mL.Through the structure identified it is the known compounds-the Fungus.