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Updated: May 23, 2025
A Novel in vivo Gene Transfer Technique and in vitro Cell Based Assays for the Study of Bone Loss in Musculoskeletal Disorders
Published on: June 8, 2014
RGDS-modified ursolic acid: insights into self-assembly, nano-properties, osteoporosis inhibition and molecular
Xiaoxiao Yuan1,2, Xiaoyi Zhang1,2, Yifan Yang1,2
1Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Capital Medical University, No. 10, Youanmenwaixitoutiao, Fengtai District, Beijing 100069, People's Republic of China. zhaomingccmu@ccmu.edu.cn.
Abstract:
Herein, a novel anti-osteoporosis agent is presented, namely, RGDS (Arg-Gly-Asp-Ser)-conjugated UA (ursolic acid) (abbreviated as UA-RGDS). In ultrapure water, UA-RGDS existed as a tetramer. In the serum of ovariectomized (OVX) mice and at 10-4 M concentration, the self-assembled UA-RGDS formed nano-particles of 16-156 nm in height, suitable for transportation in blood circulation. In vivo bio-distribution data showed that UA-RGDS was only distributed in the femur of OVX mice, while null distribution was found in the blood and other organs. These observations suggested that UA-RGDS can target the femur, thereby preventing bone loss. ELISA results showed that as an anti-osteoporosis agent, UA-RGDS downregulated the expressions of IL-1β in the serum of OVX mice. Thus, serum IL-1β levels could be a biomarker to clinically detect menopause, and UA-RGDS could help prevent bone loss.
