缬氨酸冰片酯合成及生物活性研究  

Synthesis and bioactivity of valine borneol ester

作　　者：匡新谋[1] 汤志敏 李浩 申小兰 史海波[1] 李爱元[1] 吴志革 KUANG Xin-mou;TANG Zhi-min;LI Hao;SHENG Xiao-lan;SHI Hai-bo;LI Ai-yuan;WU Zhi-ge(School of chemical engineering,Ningbo Polytechnic,Ningbo 315800,China;College of Biology and Chemical Engineering,Ningbo Institute of Technology,Zhejiang University,Ningbo 315100,China)

机构地区：[1]宁波职业技术学院化学工程学院,浙江宁波315800 [2]浙江大学宁波理工学院生物与化学工程学院,浙江宁波315100

出　　处：《化学研究与应用》2019年第10期1793-1797,共5页Chemical Research and Application

基　　金：国家自然科学基金项目(81502421)资助;国家星火计划项目(2015GA701022)资助;宁波市科技惠民计划项目(2015C50042)资助;宁波市自然科学基金项目(2018A610280)资助;宁波市工业重大科技专项项目(2017C110017)资助;宁波职业技术学院2018年度课题项目(NZ18006)资助;2018年浙江省大学生科技创新活动计划(新苗人才计划)项目(2018R459012)资助

摘　　要：本文从N-boc-L-缬氨酸和冰片出发,以DCC/DMAP作为催化剂合成了缬氨酸冰片酯(BPX),并采用IR、NMR、MS等方法对其结构进行了表征。进一步电休克惊厥实验及抑制HeLa细胞活力实验分别对缬氨酸冰片酯的抗癫痫及体外抑制肿瘤活性进行了初步研究,结果表明缬氨酸冰片酯显示出了明显的生物抗癫痫活性及抑制HeLa细胞增殖的能力。在最大电休克惊厥实验中,腹腔给药,当小鼠的BPX给药量为50mg·kg^-1及以上时,与对照组相比,显示出了与卡马西平类似甚至更好的抗癫痫活性;在体外抗肿瘤活性实验中,与对照组相比,BPX抑制率最高达57%,具备抑制HeLa细胞的增殖的能力。When N-boc-L-valine and borneol were used as material,the valine borneol ester(BPX)was synthesized by DCC/DMAP as catalyst. Its structure was characterized by IR,NM R and MS. Further animal anticonvulsant and tumor cell experiments showed that valine borneol ester had significant anti epileptic and anti tumor cell proliferation activity. When valine melaminate was dosed at 50 mg·kg^-1 and above,in the maximal electrical shock convulsion experiment,mice were injected intraperitoneally,compared with saline and carbamazepine groups,which showed similar,even better antiepileptic activity. In the antitumor experiments,growth of HeLa cells were significantly inhibited,and the highest inhibition rate was 57%.

关 键 词：缬氨酸冰片酯 DCC/DMAP 生物活性 

分 类 号：O626[理学—有机化学]