摘要
鹅脱氧胆酸的含氮衍生物能抑制多种癌细胞的增殖作用并能够诱导多种癌细胞的凋亡.从鹅去氧胆酸出发,经过酯化、Jones试剂氧化、还原等反应,分别在鹅去氧胆酸甾核的3-位或7-位引进肟基、甲氧肟基、苄氧肟基和含有不同取代基的氨基硫脲等含氮基团,通过IR、NMR及Ms等现代分析方法对合成物进行了结构表征.同时,分别采用人胃癌细胞(SGC-7901)、人肝癌细胞(Bel-7404)和前列腺癌细胞(PC-3)对合成产物及部分合成中间体进行体外抑制肿瘤细胞生长增殖活性研究,结果表明某些鹅脱氧胆酸含氮化合物对前列腺癌细胞(PC-3)和人体肝癌细胞(Bel 7404)具有较好的抑制作用.
Chenodeoxycholic acid nitrogen-containing derivatives display anti-tumor activities and induce apoptosis of the cacer cells. Some chenodeoxycholic acid derivatives possessing various nitrogen-containing substituent in 3- or 7-position of steroidal nucleus were designed and synthesized using chenodeoxycholic acid as starting materials. Their structures were characterized by IR, NMR and MS. Antiproliferative activities of the compounds were assayed against human gastric cancer cells（SGC-7901）, human hepatic cancer（Bel-7404） and prostate cancer cell（PC-3） by MTT method. The results showed that some nitrogen-containing derivatives of chenodeoxycholic acid had better antiproliferative activities against Bel-7404 and PC-3cells.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2015年第10期2168-2175,共8页
Chinese Journal of Organic Chemistry
基金
国家自然科学基金(No.21462009)
广西高校北部湾石油天然气资源有效利用重点实验室开放课题(No.2014KLOG09)资助项目~~
关键词
鹅脱氧胆酸
含氮化合物
抗肿瘤活性
生理活性
chenodeoxycholic acid
nitrogen-containing compounds
antiproliferative activity
bioactivity
