以硫磺素T为母体,合成和表征了一种苯并噻唑类双功能荧光螯合剂ZY5,并考察了它与金属-Aβ(amyloid-β)聚集体的相互作用。结果表明:ZY5的荧光强度在p H 4.0~10.0的范围内基本稳定,基本不受时间和光照的影响。ZY5符合严格的Lipinski类药标准,能识别和解聚金属-Aβ42聚集体,在一定程度上可抑制由Cu-Aβ42聚集体产生的毒性。
A thioflavin T -based bifunctional fluorescent chelator ZY5 was synthesized and characterized, its interaction with metal - Aβ( amyloid - [5) aggregates was also investigated. The results showed that the fluo- rescent intensity of ZY5 was almost stable in the range of pH value from 4.0 to 10.0, and it was hardly affect- ed by time and light. ZY5 fulfilled strict drug - like criteria, and it can recognize and disaggregate metal - Aβ42 aggregates. The cytotoxicity of the Cu - Aβ42 aggregates could be inhibited by ZY5 to some extent.