1364570-26-2Relevant articles and documents
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
Wang, Yuji,Wu, Jianhui,Kang, Guifeng,Zhao, Ming,Gui, Lin,Li, Ning,Peng, Li,Zhang, Xiaoyi,Li, Li,Peng, Shiqi
, p. 4652 - 4659 (2012/06/29)
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.
