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摘要
To find novel nano-materials with anti-osteoporosis activity and without side effects three novel anti-osteoporosis active amphiphiles, 17 beta-(RGD-AA-amido)-11 alpha-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 17 beta-amino-11 alpha-hydroxyandrost-1,4-diene-3-one. In the solid state 5a, 5b and 5c exist as dispersed globes of 300 nm-14 mu m in diameter, dispersed eggs of 110 nm-19 mu m in diameter and beads of 238 nm-22 mu m in diameter, respectively. In ultrapure water 1.1 mu M 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(-1) 5a-c effectively inhibited mice from developing osteoporosis. In contrast to estradiol, 5a-c did not induce mice to develop endometrial hyperplasia and thrombus.
- 出版日期2012
- 单位首都医科大学
