已发表论文

纳米级 IQCA-TAVV 的设计和合成,作为一种能够抗血小板活化、靶向动脉血栓并释放 IQCA 的递送系统

 

Authors Wu J, Zhu H, Yang G, He J, Wang Y, Zhao S, Zhang X, Gui L, Zhao M, Peng S

Received 28 August 2017

Accepted for publication 22 November 2017

Published 26 February 2018 Volume 2018:13 Pages 1139—1158

DOI https://doi.org/10.2147/IJN.S150205

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Akshita Wason

Peer reviewer comments 2

Editor who approved publication: Dr Linlin Sun

Background: Arterial thrombosis has been associated with a series of pathological conditions, and the discovery of arterial thrombosis inhibitor is of clinical importance.
Methods: By analyzing the pharmacophores of anti-platelet agents, thrombus targeting peptide and anti-thrombotic nano-systems 3S-1,2,3,4-tetrahydroisoquino- line-3-carbonyl-Thr-Ala-Arg-Gly-Asp(Val)-Val (IQCA-TAVV) was designed and prepared as a nano-scaled arterial thrombosis inhibitor. 
Results: In vitro the nanoparticles of IQCA-TAVV were able to adhere onto the surface of activated platelets, attenuate activated platelets to extend pseudopodia and inhibit activated platelets to form aggregators. In vivo IQCA-TAVV targeted arterial thrombus, dose dependently inhibited arterial thrombosis with a 1 nmol/kg of minimal effective dose, and the activity was ~1670 folds of that of aspirin. 
Conclusion: IQCA-TAVV represented the design, preparation and application of nanomedicine capable of adhering on the surface of activated platelets, attenuating platelet activation, targeting arterial thrombus and inhibiting arterial thrombosis.
Keywords: arterial thrombosis, thrombus targeting, nanodelivery, antithrombosis