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

【摘要】 Semicarbazide-sensitive amine oxidase ( SSAO) has been considered to be associated with the metabolism of glucose and fat,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 1 5 anti-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 3 1 . 9 % and 1 8 . 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 1 5 . 6 % on serum SSAO. Caffeine provides a natural source of inhibition of SSAO activity and may be a promising inhibitor for the study of SSAO.更多还原

【Abstract】 Semicarbazide-sensitive amine oxidase ( SSAO) has been considered to be associated with the metabolism of glucose and fat,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 1 5 anti-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 3 1.9 % and 1 8.8 % 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 1 5.6 % on serum SSAO. Caffeine provides a natural source of inhibition of SSAO activity and may be a promising inhibitor for the study of SSAO.更多还原