Novel semicarbazide-sensitive amine oxidase inhibitor screening from anti-obesity drugs using HPLC-MS based technique  

作　　者：车宝泉 王琳 张永谦 肖盛元 邓玉林 

机构地区：[1]School of Life Science,Beijing Institute of Technology [2]Beijing Institute for Drug Control

出　　处：《Journal of Beijing Institute of Technology》2013年第1期135-142,共8页北京理工大学学报（英文版）

基　　金：Supported by the Ministry of Science and Technology of China(2008AA12A218; 2009BAK59B01)

摘　　要：Semicarbazide-sensitive the metabolism of glucose and fat, amine oxidase （SSAO） has been considered to be associated with and elevated SSAO activity was observed in obese patients. In the present study, an in vitro SSAO activity-based method was developed to screen inhibitors from 15 an- ti-obesity drugs. Among the fifteen anti-obesity drugs, four drugs including caffeine, fenfluramine, bumetanide and amfebutamone inhibited SSAO activity, and caffeine was the most effective one. When the concentration of caffeine was 1.4 mmol/L, the inhibition ratio was 31.9% and 18.8% in rabbit serum and rat adipose tissue, respectively. Inhibition of SSAO activity by caffeine was also confirmed in the in vivo study, showing the inhibition ratio of 15.6% on serum SSAO. Caffeine pro- vides a natural source of inhibition of SSAO activity and may be a promising inhibitor for the study of SSAO.Semicarbazide-sensitive the metabolism of glucose and fat, amine oxidase （SSAO） has been considered to be associated with and elevated SSAO activity was observed in obese patients. In the present study, an in vitro SSAO activity-based method was developed to screen inhibitors from 15 an- ti-obesity drugs. Among the fifteen anti-obesity drugs, four drugs including caffeine, fenfluramine, bumetanide and amfebutamone inhibited SSAO activity, and caffeine was the most effective one. When the concentration of caffeine was 1.4 mmol/L, the inhibition ratio was 31.9% and 18.8% in rabbit serum and rat adipose tissue, respectively. Inhibition of SSAO activity by caffeine was also confirmed in the in vivo study, showing the inhibition ratio of 15.6% on serum SSAO. Caffeine pro- vides a natural source of inhibition of SSAO activity and may be a promising inhibitor for the study of SSAO.

关 键 词：anti-obesity drugs CAFFEINE enzyme inhibition HPLC-MS semicarbazide-sensitive a-mine oxidase 

分 类 号：R96[医药卫生—药理学]