Page 13 of 15
Journal of Materials Chemistry B
3.
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C.Cui, Y. Wang, K. Yang, Y. Wang, J. Yang, J. Xi, M. Zhao,
supination, nor occurred death. Therefore, IQCA-TASS is
J. Wu and S. Peng, J Biomed Nanotechnol, 2015, 11, 70-80.
comparatively non-toxic, and the LD50 value of IQCA-TASS
Y. Song and S. Peng, J. Mater. Chem.DBO,I:21001.150,339,/C926T6B00-92270658A.
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Fig.10 Serum Cr (A), AST (B)and ALT (C) of health ICR mice
treated with NS and 1 μmol/kg of IQCA-TASS, n=12. Note:
normal levels of the serum Cr, AST and ALT of male ICR mice are
17.6 - 35.36 μM, 40 - 100 IU/L and 26 - 59 IU/L, respectively. 41
Conclusions
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By coupling anti-thrombotic pharmacophore IQCA and
GPIIb/IIIa recognizing sequence TARGD(S)S, tailor-designed
IQCA-TASS was prepared as a nano-scaled P-selectin inhibitor.
In vivo IQCA-TASS is able to target thrombus thereby releasing
IQCA and TASS, and to offer excellent anti-thrombotic and
anti-inflammatory actions. At high dose (10 nmol/kg)
IQCA-TASS does not injure the liver and the kidney of
inflammatory mice, at 1 μmol/kg, 1000 times of the minimal
effective dose (1 nmol/kg), IQCA-TASS still induces no toxic
reaction to the liver, kidney and nerve of health ICR mice.
These findings suggest that IQCA-TASS is worthy of
developing towards a nano-scaled anti-thrombotic drug.
Acknowledgements
The authors thank BMSTC, China (Z141100002114049);
TJSHG, China (201310025008); Project of Construction of
Innovative Teams and Teacher Career Development for
Universities and Colleges under Beijing Municipality; NSFC,
China (81270046, 81273379, 81373264 and 81373265); BNSF,
China (7162025); 863 Program, China (AA2015020902);
2015ZR15 and 2016ZR22 for financialsupport.
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