Study On Anti-tumor Active Constituents Of Gentiana Guan

Gentiana scabra belongs to the Gentiana, family of Gentianaceae. It has rich resources in Jilin Province. It is the genuine herbs of Changbai Mountain and has better anti-tumor effect in the civil. Antineoplastic agents are mostly syntehtic drugs and have great said effects, such as suppressed immune function and damaged liver and kidney function etc. at present. So look for the traditional Chinese medicine of natural, effective and lowtoxicity becomes medical research focus in modern. In resent yeas, national researchers isolated multiple secoiridoids, triterp-enoids, flavonoids and other compounds. Japanese scholars studied chemical compositions of triterpenoids and secoiridoids of Jilin Gentiana, while, there is no any reports about the active compositions of Gentiana scabra on anti-tumor effect in domestic. Therefore, in order to develop and use of Gentiana scabra, and find out chemical compounds with anti-tumor activity, this study made systemic research with Gentiana scabra whitch was collected from Hudian, Jilin.This study take the modle of mouse S180 sarcoma in vivo, to obersve the Anti-tumor Effect of the ethanol extract of Gentiana scabra and the results show that it has better tumor inhibition. On the basis of this research, the ethanol extract of alcohol refluxing and methanol extract of methanol ouenching were extracted with petroleum ether, ethyl acetate and n-butanol. The each fraction of the alcohol reflux extraction by means of gastric cancer (MGC-803), cervical(Hela) and liver cancer(HepG-2) cells in vitro cytotoxicity and mouse S180 sarcoma inhibition experiments in vivo, to select active fractions of Gentiana scabra on anti-tumor effect were fractions of petroleum ether and ethyl acetate, in particular, the ethyl acetate exeract.Twelve compounds were isolated from the active fractions by silica gel chromatography. The structures of eleven compounds were identified as Chirat-17(22)-en-3-one(Ⅰ), Chiratol (Ⅱ),β-sitosterol(Ⅲ), a-Amyrinpalmitate(Ⅳ), Chirat-16-en-3-one(Ⅴ), Chiratenol(Ⅵ),3,4-dih-ydro-1H,6H,8H-naphtho[1,2-c:4,5-c',d']dipyrano-1,8-dione(Ⅶ), (3-daucosterol(Ⅷ), Cholesterol (Ⅹ), Ggentiopicroside(Ⅺ), D-sucurose(Ⅻ) by spectroscopic(1H-NMR,13C-NMR, DEPT, HMBC, HSQC,'H-'H COSY, GC-MS et.al) and chemical means. Among them, CompoundsⅡ,Ⅳ,Ⅶ,Ⅹand XH were isolated from this plant for the first time. CompoundsⅤ,Ⅵ,ⅦandⅫ exhibited moderrate anti-tumor effect (69.94,52.31,51.74 and 50.93% inhibition at a dose of 100μg-mL-1 respectively) against Hela.This study not only improvesthe understanding about chemical compounds and anti-tumor activites of Gentiana scabra, but also provides scientific evidence for further research and develop Gentiana scabra.