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Issue 11, 2012
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Novel nano-materials, RGD-tetrapeptide-modified 17β-amino-11α-hydroxyandrost-1,4-diene-3-one: synthesis, self-assembly based nano-images and in vivo anti-osteoporosis evaluation

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Abstract

To find novel nano-materials with anti-osteoporosis activity and without side effects three novel anti-osteoporosis active amphiphiles, 17β-(RGD-AA-amido)-11α-hydroxyandrost-1,4-diene-3-one (5a: AA = Ser, 5b: AA = Val, 5c: AA = Phe), were constructed by coupling the bone resorption inhibiting active RGD-peptides and anti-osteoporosis active 17β-amino-11α-hydroxyandrost-1,4-diene-3-one. In the solid state 5a, 5b and 5c exist as dispersed globes of 300 nm–14 μm in diameter, dispersed eggs of 110 nm–19 μm in diameter and beads of 238 nm–22 μm in diameter, respectively. In ultrapure water 1.1 μM of 5a, 5b and 5c form nano-globes of 33–400 nm, 16–278 nm and 54–187 nm in diameter, respectively. At an oral dose of 110 nmol kg−15a–c effectively inhibited mice from developing osteoporosis. In contrast to estradiol, 5a–c did not induce mice to develop endometrial hyperplasia and thrombus.

Graphical abstract: Novel nano-materials, RGD-tetrapeptide-modified 17β-amino-11α-hydroxyandrost-1,4-diene-3-one: synthesis, self-assembly based nano-images and in vivo anti-osteoporosis evaluation

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Supplementary files

Article information


Submitted
16 Aug 2011
Accepted
13 Dec 2011
First published
25 Jan 2012

J. Mater. Chem., 2012,22, 4652-4659
Article type
Paper

Novel nano-materials, RGD-tetrapeptide-modified 17β-amino-11α-hydroxyandrost-1,4-diene-3-one: synthesis, self-assembly based nano-images and in vivo anti-osteoporosis evaluation

Y. Wang, J. Wu, G. Kang, M. Zhao, L. Gui, N. Li, L. Peng, X. Zhang, L. Li and S. Peng, J. Mater. Chem., 2012, 22, 4652
DOI: 10.1039/C2JM13983A

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