根皮素缩氨基硫脲合成及其抑制酪氨酸酶活性作用  

Synthesis and antityrosinase activities of phloretin thiosemicarbazone

作　　者：许宾宾[1] 曹树稳[1,2] 余燕影[2] 

机构地区：[1]南昌大学食品科学与技术国家重点实验室,江西南昌330047 [2]南昌大学化学系,江西南昌330031

出　　处：《南昌大学学报（理科版）》2013年第1期51-54,共4页Journal of Nanchang University(Natural Science)

基　　金：国家自然科学基金资助项目(20962014)

摘　　要：以根皮素为母体合成了根皮素缩氨基硫脲,采用UV,IR,1 H NMR,13 C NMR及MS等手段对产物进行结构表征。以L-多巴为底物研究了根皮素及根皮素缩氨基硫脲对酪氨酸酶的抑制作用。结果表明,相比于根皮素,根皮素缩氨基硫脲对酪氨酸酶表现出更强的抑制作用,其IC50值为57.81±1.46μM。酶学动力学研究表明,二者对酪氨酸酶的抑制作用均表现为混合型可逆抑制作用。Phloretin thiosemicarbazone was synthesized from the condensation of the phloretin template with thiosemicarbazide.Its structure was characterized thrugh ultraviolet spectra,Fourier-transform infrared,1H-and 13C-nuclear magnetic resonance,and mass spectra.Both phloretin and Phloretin thiosemicarbazone were evaluated for their inhibition activities on tyrosinase.Our results showed that PT possessed potent tyrosinase inhibitory activity（IC50=57.81±1.46 μM）,which was much better than phloretin（IC50=70.08±0.88 μM）.Kinetic analyses suggested that both compounds showed reversible inhibition and their mechanisms were mixed-type.Their inhibition constants were also determined and compared.

关 键 词：根皮素 根皮素缩氨基硫脲 酪氨酸酶 动力学 

分 类 号：R284.3[医药卫生—中药学]