Design and synthesis of nanoscaled IQCA-TAVV as a delivery system capable of antiplatelet activation, targeting arterial thrombus and releasing IQCA

Jianhui Wu,1,2,* Haimei Zhu,1,2,* Guodong Yang,1 Jianhong He,3 Yuji Wang,1,2 Shurui Zhao,1,2 Xiaoyi Zhang,1,2 Lin Gui,1,2 Ming Zhao,1,2,4 Shiqi Peng1,2 1Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Educatio...

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Autores principales:	Wu J, Zhu H, Yang G, He J, Wang Y, Zhao S, Zhang X, Gui L, Zhao M, Peng S
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	arterial thrombosis thrombus targeting nano-delivery anti-thrombosis Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/408fb8d8bcf6477da84f7fa4ba80251e
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spelling	oai:doaj.org-article:408fb8d8bcf6477da84f7fa4ba80251e2021-12-02T08:06:25ZDesign and synthesis of nanoscaled IQCA-TAVV as a delivery system capable of antiplatelet activation, targeting arterial thrombus and releasing IQCA1178-2013https://doaj.org/article/408fb8d8bcf6477da84f7fa4ba80251e2018-02-01T00:00:00Zhttps://www.dovepress.com/design-and-synthesis-of-nanoscaled-iqca-tavv-as-a-delivery-system--cap-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Jianhui Wu,1,2,* Haimei Zhu,1,2,* Guodong Yang,1 Jianhong He,3 Yuji Wang,1,2 Shurui Zhao,1,2 Xiaoyi Zhang,1,2 Lin Gui,1,2 Ming Zhao,1,2,4 Shiqi Peng1,2 1Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing, China; 2Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, China; 3Department of Internal Medicine of TCM, The First Affiliated Hospital of Guanxi University of Chinese Medicine, Nanning, China; 4Department of Biomedical Science and Environmental Biology, Kaohsiung Medical University, Kaohsiung, Taiwan *These authors contributed equally to this work 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, antithrombosisWu JZhu HYang GHe JWang YZhao SZhang XGui LZhao MPeng SDove Medical Pressarticlearterial thrombosisthrombus targetingnano-deliveryanti-thrombosisMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 1139-1158 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	arterial thrombosis thrombus targeting nano-delivery anti-thrombosis Medicine (General) R5-920
spellingShingle	arterial thrombosis thrombus targeting nano-delivery anti-thrombosis Medicine (General) R5-920 Wu J Zhu H Yang G He J Wang Y Zhao S Zhang X Gui L Zhao M Peng S Design and synthesis of nanoscaled IQCA-TAVV as a delivery system capable of antiplatelet activation, targeting arterial thrombus and releasing IQCA
description	Jianhui Wu,1,2,* Haimei Zhu,1,2,* Guodong Yang,1 Jianhong He,3 Yuji Wang,1,2 Shurui Zhao,1,2 Xiaoyi Zhang,1,2 Lin Gui,1,2 Ming Zhao,1,2,4 Shiqi Peng1,2 1Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, Beijing, China; 2Beijing Laboratory of Biomedical Materials, College of Pharmaceutical Sciences, Capital Medical University, Beijing, China; 3Department of Internal Medicine of TCM, The First Affiliated Hospital of Guanxi University of Chinese Medicine, Nanning, China; 4Department of Biomedical Science and Environmental Biology, Kaohsiung Medical University, Kaohsiung, Taiwan *These authors contributed equally to this work 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
format	article
author	Wu J Zhu H Yang G He J Wang Y Zhao S Zhang X Gui L Zhao M Peng S
author_facet	Wu J Zhu H Yang G He J Wang Y Zhao S Zhang X Gui L Zhao M Peng S
author_sort	Wu J
title	Design and synthesis of nanoscaled IQCA-TAVV as a delivery system capable of antiplatelet activation, targeting arterial thrombus and releasing IQCA
title_short	Design and synthesis of nanoscaled IQCA-TAVV as a delivery system capable of antiplatelet activation, targeting arterial thrombus and releasing IQCA
title_full	Design and synthesis of nanoscaled IQCA-TAVV as a delivery system capable of antiplatelet activation, targeting arterial thrombus and releasing IQCA
title_fullStr	Design and synthesis of nanoscaled IQCA-TAVV as a delivery system capable of antiplatelet activation, targeting arterial thrombus and releasing IQCA
title_full_unstemmed	Design and synthesis of nanoscaled IQCA-TAVV as a delivery system capable of antiplatelet activation, targeting arterial thrombus and releasing IQCA
title_sort	design and synthesis of nanoscaled iqca-tavv as a delivery system capable of antiplatelet activation, targeting arterial thrombus and releasing iqca
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/408fb8d8bcf6477da84f7fa4ba80251e
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Design and synthesis of nanoscaled IQCA-TAVV as a delivery system capable of antiplatelet activation, targeting arterial thrombus and releasing IQCA

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