NDLI: IQCA-TASS: a nano-scaled P-selectin inhibitor capable of targeting thrombus and releasing IQCA/TARGD(S)S <i>in vivo</i>

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Journal of Materials Chemistry B Vol - 5 Issue - 4

Journal of Materials Chemistry B Vol - 5 Issue - 3

Journal of Materials Chemistry B Vol - 5 Issue - 2

Journal of Materials Chemistry B Vol -4

Journal of Materials Chemistry B Vol -3

Journal of Materials Chemistry B Vol -2

Journal of Materials Chemistry B Vol -1

IQCA-TASS: a nano-scaled P-selectin inhibitor capable of targeting thrombus and releasing IQCA/TARGD(S)S in vivo

Content Provider	Royal Society of Chemistry (RSC)
Author	Yang, Guodong Zhao, Ming Gui, Lin Wu, Jianhui Wang, Yaonan Zhang, Xiaoyi Wang, Yuji Peng, Shiqi Zhao, Shurui Zhu, Haimei
Copyright Year	2017
Abstract	Thrombosis is a serious threat to human health worldwide. Tetrahydroisoquinoline-3-carboxylic acid (IQCA) is an antithrombotic agent, while Thr-Ala-Arg-Gly-Asp(Ser)-Ser (TASS) can target thrombus. Herein, tetrahydro-isoquinoline-3-carbonyl-Thr-Ala-Arg-Gly-Asp(Ser)-Ser (IQCA-TASS) was designed with the aim towards the discovery of a nano-delivery system for targeting thrombus. In vitro, IQCA-TASS acted on P-selectin and down-regulated P-selectin expression. The IC50 values of IQCA-TASS against the platelet aggregation induced by four aggregators were less than 0.45 nM. In vivo, IQCA-TASS targeted thrombus, released IQCA and TASS inside the thrombus, showed dose-dependent anti-thrombotic action, of which the minimal effective dose was 1 nmol kg−1, and showed anti-inflammatory action. Even with the dose up to 1 μmol kg−1, a dose of 1000 times the minimal effective dose, IQCA-TASS still induced no toxic reaction. In rat plasma, IQCA-TASS formed nanoparticles with diameters of less than 41 nm. The interactions of the nanoparticles with both resting and activated platelets were imaged. IQCA-TASS should be a safe nano-medicine capable of targeting thrombus and releasing anti-thrombotic/anti-inflammatory pharmacophores in disease sites.
Starting Page	917
Ending Page	927
Page Count	11
File Format	HTM / HTML PDF
ISSN	2050750X
Volume Number	5
Issue Number	5
Journal	Journal of Materials Chemistry B
DOI	10.1039/c6tb02705a
Language	English
Publisher	Royal Society of Chemistry
Access Restriction	Open
Subject Keyword	TASS IQCA Tetrahydroisoquinoline Carboxylic acid Thrombosis Thrombus P-selectin IC50 Platelet Effective dose (radiation) Blood plasma
Content Type	Text
Resource Type	Article
Subject	Chemistry Medicine Materials Science Biomedical Engineering

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IQCA-TASS: a nano-scaled P-selectin inhibitor capable of targeting thrombus and releasing IQCA/TARGD(S)S in vivo

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IQCA-TASS: a nano-scaled P-selectin inhibitor capable of targeting thrombus and releasing IQCA/TARGD(S)S in vivo