Synthesis And Antitumor Activity Of Oleanane-12-ene Derivatives

Adriamycin belongs to anthracycline broad-spectrum antitumor antibiotics.Its hydrochloride is often used in clinic and also called doxorubicin.It can produce a wide range of biological effects on the organism.It has strong cytotoxicity,and has good curative effect on liver cancer,thyroid cancer,lymphatic cancer and lung cancer.It also plays an important role in bladder cancer and bronchial carcinoma.However,intravenous injection of high dose of DOX can cause strong side effects.These shortcomings become the main factors limiting the clinical application of DOX.The main purpose of this study is to improve the efficacy,reduce the toxicity and side effects of doxorubicin,and to study the active targeting of tumor and its pharmacodynamics in vitro.Folic acid receptors are overexpressed on tumor cells,the specific affinity of folic acid as active targeting preparations of target vascular factors,by coupling agent specific,chemical modification of the coupling to doxorubicin albumin nanoparticles,in order to make agents active targeting tumor after release of Adriamycin and kill tumor cells.The main methods,results and conclusions of this paper include the following aspects:Aim:To preparation new of new high dose of folic acid-albumin nanoparticles loaded with doxorubicin FA-BSANPs/DOX utilizing folic acid-coupled bovine serum albumin as carrier material and investigate its anticancer activity in vitro.Method: FA-BSANPs / DOX with active anti-tumor adriamycin were obtained by the amino group of albumin nanoparticles of desolvation and the folic acid active ester.And the properities of FA-BSANPs / DOX were inspected.MTT method was applied to determine the in vitro anticancer activity of FA-BSANPs / DOX in HEPG2 and SGC7901 compared with DOX.Results: FA-BSANPs / DOX was successfully formulated.The particle size of FA-BSANPs / DOX was(277.43 ±0.67)nm with uniform particle size distribution,of which the entrapment efficiency was(70.43 ±0.67)% and the drug loading rate reached at(19.33±0.32)%.The result of the in vitro release of FA-BSANPs / DOX exhibited that cumulative release amount o 24 h was 26.7% indicating that FABSANPs / DOX had the good quality of delayd releasing.The pharmacodynamics in vitro experiment results revealed that the values of FA-BSANPs / DOX and DOX in HEPG2 were 4.98 ?mol/L and 5.13 ?mol/L,in SGC7901 were 4.85 ?mol/L and 5.02 ?mol/L,respectively.Conclusions: Albumin as a good biodegrdable carrier material can prepare the high drug-loading albumin nanoparticles.FA-BSANPs / DOX are more effective in killing HEPG2 and SGC7901 in vitro and show stronger antitumor effect comparing DOX.which may be hopeful to be a kind of potential preparation of albumin nanoparticles.