Journal of Materials Chemistry p. 21740 - 21748 (2012)
Update date:2022-08-02
Topics:
Kang, Guifeng
Wang, Yuji
Liu, Jiawang
Wu, Jianhui
Zhao, Ming
Li, Guochun
Li, Ning
Peng, Li
Zhang, Xiaoyi
Li, Li
Mair, Nathan
Peng, Shiqi
Three novel three-component conjugates of a succinyl spacer, a pharmacophore of 17β-amino-11α-hydroxyl-androst-1,4-diene-3-one, and a targeting sequence of RGD-tetrapeptide (peptide Arg-Gly-Asp-AA) were designed, synthesized, and evaluated. This paper presents evidence that inserting a succinyl functional group into the pharmacophore and the targeting sequence improves the oral anti-osteoporosis activities in mouse glucocorticoid model of secondary osteoporosis, which were reflected by dry weight, ash weight, Ca 2+ and bone mineral content of the femur of examined mice. These novel conjugates have no side effects on estrogen, and form nano-globes with a porous surface. This paper emphasizes that the hydrogen bond between the carbonyl group of the succinyl group and the carboxylic group of the C-terminal amino acid residue of RGD-tetrapeptides is the key to forming pores on the surface of the nano-globes of these novel conjugates.
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