Synthesis Of Matrine Derivatives And Its Anti-Hepatoma Effect In Vivo

Matrine is widely found in flavescent sophora, sophora alopecuroides L and radix sophorae subprostrata. The modern medical research indicated that the important components of these medicines, matrine, has a good effect on lowing temperature, antipyretic effect, sedation, tramadol, antiarrhythmic, protecting myocardial ischemia, besides, matrine show a variety of pharmac ological activity on treating chronic hepatitis B, inducing proliferation, differentiation, and apoptosis in tumor cell. So it has a new medicine development prospect in the treatment of tumors, hepatitis B and other deseases. The widespread use of matrine is limited because its poor chemical stabilityis, low bioavailability and toxic side effects on central nervo us system. However we can use some chemical ways to change its stucture so as to enhanced pharmacological activity and reduced toxicity.Considering the pharmacological activity and the structure of matrine, twenty-eight novel structure of matrine derivatives have been designed and synthesized. All the compounds were identified by1HNMR,MS and IR.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 RWOl to RW22, RW24to RW27is the same as the reference substances of matrine. The activity of RW23, RW28is the same as the reference substances of cyclophosphamide, higer than cyclophospha mide.