Synthesis and evaluation of benzylisoquinoline derivatives for their inhibition on pancreatic lipase and preadipocyte proliferation  

作　　者：TIAN Feng LV Hao-Yu ZOU Ji-Long WANG Yi DUAN Meng-Jun CHU Xiao-Qin LI Dan ZHU Liang JIANG Jian-Qin 

机构地区：[1]Department of Natural Medicinal Chemistry, China Pharmaceutical University [2]Department of Pharmacology and Chemical Biology, Shanghai Jiao Tong University School of Medicine

出　　处：《Chinese Journal of Natural Medicines》2016年第5期382-390,共9页中国天然药物（英文版）

基　　金：supported by the Graduate Students Scientific Research Innovation Projects of Jiangsu Province(No:CXZZ11-0804)

摘　　要：The present study was designed to synthesize and evaluate a series of benzylisoquinoline derivatives. These compounds were synthesized by Bischler-Napieralski cyclization to yield 1-benzyl-3,4-dihydroisoquinolines, and the products were obtained by reductions. All these compounds were identified by MS, 1H NMR and 13 C NMR. The inhibitory activities on pancreatic lipase and preadipocyte proliferation for the synthesized compounds and alkaloids from Nulembo nucifera were assessed in vitro. Most of the compounds showed inhibitory activities on both pancreatic lipase and preadipocyte proliferation. Particularly, compounds 7p-7u and 9d-9f exhibited significant inhibitory activity on pancreatic lipase while compounds 7c, 7d, 7f, 7g, 7i, and 7j potently inhibited the proliferation of 3T3-L1 preadipocytes. Our results provided a basis for future evaluation and development of these compounds as leads for therapeutics for human diseases.The present study was designed to synthesize and evaluate a series of benzylisoquinoline derivatives. These compounds were synthesized by Bisehler-Napieralski cyclization to yield 1-benzyl-3,4-dihydroisoquinolines, and the products were obtained by reductions. All these compounds were identified by MS, 1H NMR and 13C NMR. The inhibitory activities on pancreatic lipase and preadipocyte proliferation for the synthesized compounds and alkaloids from Nulembo nuciJera were assessed in vitro. Most of the compounds showed inhibitory activities on both pancreatic lipase and preadipocyte proliferation. Particularly, compounds 7p-7u and 9d-9f exhibited significant inhibitory activity on pancreatic lipase while compounds 7c, 7d, 7f, 7g, 7i, and 7j potently inhibited the proliferation of 3T3-L1 preadipocytes. Our results provided a basis for future evaluation and development of these compounds as leads for therapeutics for human diseases.

关 键 词：Nelumbo nucifera Benzylisoquinoline alkaloid ANTI-OBESITY Pancreatic lipase inhibitor Adipocyte proliferation 

分 类 号：R284[医药卫生—中药学]