Synthesis Of Piperazine Matrine Derivatives And Their Activities In Anti-Tumor

Matrine, which is an effectively active constituent of traditional medicine herb Kushen, was extracted from Sophora alopecuroides L, Sophorae Subprostrata and Sophorae flavescentis,et al. Matrine has many pharmacological activities such as detoxification anti-tumor, anti-arrhythmia and anti-inflammatory et al. Matrine is widespread use of in the clinical, but its bioavailability is not particularly high, and there is toxic side effects on the central nervous system. So it is frequently allied with other drugs for the treatment of patients. thus that reasons Limits its use.In this paper, on the basis of the biological activity and structure of Matraine to improve the anti-cancer activity of matrine, and what’s more, hope to get some novel matrine derivatives as new leads for drug discovery. and the carbon-nitrogen ring compounds has a special biological activity, such as N-phenyl-piperazine. Twenty-seven novel matrine derivatives were designed and synthesized by the chemical reaction between matrine and piperazine group. The structure of the target compounds were confirmed by IR, MS, and1H NMR.The results of the initial anti-tumor tests showed that some compounds had significant effect in anti-tumor. By comparing their Cell viability (50μM), we found the activities of M13、M17、M22、M26and M26was higher than the activities of the comparison drug matrine and cis-Dichlorodiamineplatinum (Ⅱ) on7402cells. Particularly, compounds M3、M9、M10、M17、M18and M24showed better anti-tumor activity on7402cells and RKO cells than comparison drug matrine. Then, their anti-tumor activity is the same as cis-Dichlorodiamineplatinum(II).The results of the initial anti-hepatoma in vivo tests showed that all the compounds had effect in anti-hepatoma in different degree. By comparing their inhibition rate, we found the activity of Ml to M27are the same as the reference substances of matrine. The activity of M4、M7、M8、M11、M14and M20are higer than matrine.