多巴胺-β-环糊精/α-生育酚的分子识别及包结物性能  

Molecular recognition of dopamine-β-cyclodextrin derivative/α-tocopherol and performance of inclusion complex

作　　者：张冬梅 杨成 ZHANG Dongmei;YANG Cheng(Key Laboratory of Synthetic and Biological Colloids,Ministry of Education,School of Chemical and Material Engineering,Jiangnan University,Wuxi 214122,Jiangsu,China)

机构地区：[1]合成与生物胶体教育部重点实验室,江南大学化学与材料工程学院,江苏无锡214122

出　　处：《精细化工》2020年第7期1454-1460,共7页Fine Chemicals

基　　金：中央高校基本科研基金(JUSRP21937,JUSRP11931)。

摘　　要：为了提升α-生育酚(α-TOC)在环境中的稳定性,增强其包封率及药物有效利用,以多巴胺(DA)改性的β-环糊精(b-CD-6-DA)为包结物主体分子对α-TOC进行主-客体分子识别,得到稳定的包结复合物β-CD-6-DA/α-TOC。采用UV-Vis、2D-NOESY与连续变量Job’s法探究了β-CD-6-DA的疏水空腔对α-TOC的包封率、分子识别行为及主客体包结比。结果表明,改性后的β-CD-6-DA对α-TOC的包封率高达99.3%±0.7%,促进了α-TOC进入疏水空腔中的深度,并将包结物的包结比由2∶1提升至1∶1。此外,对β-CD-6-DA/α-TOC包结物的生物性能进行探讨,发现其在35℃下具有响应性释放能力,并展现出了高于80%的细胞相容性以及优异的体外抗氧化能力。To improve the stability ofα-tocopherol(α-TOC)under natural environment and enhance its encapsulation rate and drug utilization,b-cyclodextrin derivative(β-CD-6-DA)modified by dopamine(DA)was used as host molecule to self-embedα-TOC,thereby obtaining stable inclusion complex(β-CD-6-DA/α-TOC).The encapsulation rate,molecular recognition behaviors and inclusion proportion ofβ-CD-6-DA toα-TOC were investigated by UV-vis,2 D-NOESY,and continuous variable Job’s methods.The results showed thatβ-CD-6-DA had an encapsulation rate toα-TOC up to 99.3%±0.7%,which promoted the embedded depth ofα-TOC inside hydrophobic cavity,and increased inclusion proportion from 2∶1 to 1∶1.The biological properties of inclusion complexβ-CD-6-DA/α-TOC were discussed.It was found that this inclusion complex had a controlled release ability at 35℃.In addition,inclusion complexβ-CD-6-DA/α-TOC showed up to 80%cytocompatibility,and exhibited excellent antioxidant capacity in vitro.

关 键 词：多巴胺-β-环糊精 Α-生育酚 主客体包结物 包封率 可控释放 抗氧化性 医药原料 

分 类 号：TQ460.1[化学工程—制药化工]