Abstract
Osteoporosis is a major age-related bone disease characterized by low bone mineral density and a high risk of fractures. Bisphosphonates are considered as effective agents treating osteoporosis. However, long-term use of bisphosphonates is associated with some serious side effects, which limits the widespread clinical use of bisphosphonates. Here, we demonstrate a novel type of bone-targeting anti-resorptive agent, bisphosphonate-enoxacin (BE). In this study, ovariectomized rat model was established and treated with PBS, zoledronate (50 μg/kg) and different dose of BE (5 mg/kg and 10 mg/kg), respectively. The rats subjected to sham-operation and PBS treatment were considered as control group. Then, micro-computed tomography scanning, biomechanical tests, nano-indentation test and Raman analysis were used to compare the effects of zoledronate and BE on cortical bone mass, strength, and composition in ovariectomized rats. We found that both zoledronate and BE were beneficial to cortical bone strength. Three-point bending and nano-indentation tests showed that zoledronate- and BE-treated groups had superior general and local biomechanical properties compared to the ovariectomized groups. Interestingly, it seemed that BE-treated group got a better biomechanical property than the zoledronate-treated group. Also, BE-treated group showed significantly increased proteoglycan content compared with the zoledronate-treated group. We hypothesized that the increased bone strength and biomechanical properties was due to altered bone composition after treatment with BE. BE, a new bone-targeting agent, may be considered a more suitable anti-resorptive agent to treat osteoporosis and other bone diseases associated with decreased bone mass.
Highlights
Bone mass is maintained by osteoblastic bone formation and osteoclastic bone resorption, which is called bone remodeling (Teitelbaum and Ross, 2003; Horne et al, 2005; Karsenty et al, 2009)
Our results showed that cortical bone thickness was significantly lower in the OVX groups compared to the sham groups
Zoledronate-treated groups showed superior cortical bone thickness compared to the groups treated with BE, though there was no significant difference between them (Figure 1B)
Summary
Bone mass is maintained by osteoblastic bone formation and osteoclastic bone resorption, which is called bone remodeling (Teitelbaum and Ross, 2003; Horne et al, 2005; Karsenty et al, 2009). An imbalance between bone formation and bone resorption causes bone diseases, such as osteoporosis, which has become a worldwide health concern, causing great medical, economic, and social burdens. Two major types of medication are focused on the treatment of osteoporosis, anti-resorptive and anabolic agents (Amugongo et al, 2014). Bisphosphonate (BP), the classical anti-resorptive agent, is effective in preventing the development of osteoporosis and in reducing the risk of fractures (Boivin et al, 2000; Zoehrer et al, 2006; Bala et al, 2011). There is an urgent need to develop a safe, alternative anti-resorptive agent
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
