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Cardenolides; calotropin and gomphogenin from Calotropis procera (Aiton) mitigate bone turnover in ovariectomized
Walaa S A Mettwally1, Rehab A Hussein2, Gehad A Abdel Jaleel3
1Chemistry of Natural and Microbial Products Department, Pharmaceutical and Drug Industries Research Institute, National Research Centre, Dokki, Giza 12622, Egypt.
Insights
Calotropis procera extract, calotropin (CLT), and gomphogenin (GPG) show potential in treating osteoporosis by regulating bone turnover and increasing mineralization. Calotropin demonstrated superior efficacy in preventing bone loss in ovariectomized rats.
Area of Science:
- Pharmacology
- Biochemistry
- Osteoporosis Research
Background:
- Osteoporosis is a significant skeletal disorder characterized by decreased bone mineral density and increased fracture risk.
- Ovariectomy-induced osteoporosis in rats serves as a standard preclinical model to evaluate potential therapeutic agents.
- Calotropis procera and its cardenolides are investigated for their potential bone-protective effects.
Purpose of the Study:
- To investigate the efficacy of Calotropis procera extract, calotropin (CLT), and gomphogenin (GPG) in an ovariectomy-induced osteoporosis rat model.
- To elucidate the underlying mechanisms, including effects on bone turnover biomarkers and hormonal levels.
Main Methods:
- Ovariectomized rats were treated with C. procera extract, CLT, or GPG for 14 days.
- Bone resorption/formation biomarkers (BALP, OPG, RANKL), serum calcium, phosphorus, estradiol (E2), and catalase were assessed.
- Histopathological, histomorphometric, and immunohistochemical analyses were performed; molecular docking was utilized.
Main Results:
- C. procera extract, CLT, and GPG treatments restored estradiol levels and regulated the RANKL/OPG axis.
- Serum calcium and phosphorus levels increased, while bone-specific alkaline phosphatase (BALP) decreased.
- Calotropin (CLT) exhibited superior efficacy compared to gomphogenin (GPG) and the C. procera extract, supported by molecular docking studies.
Conclusions:
- Calotropis procera, particularly calotropin and gomphogenin, effectively suppresses bone turnover and enhances mineralization in osteoporotic rats.
- The compounds act by decreasing osteoclastic activity and increasing calcium mineralization, potentially via binding to ER-α and the RANKL/OPG complex.
- These findings suggest therapeutic potential for C. procera constituents in managing osteoporosis.
Abstract:
The present study aimed to examine the effect of Calotropis procera (Aiton) and its major cardenolides; calotropin and gomphogenin on ovariectomy-induced osteoporosis in rats. Osteoporotic rats were orally treated with C. procera alcoholic extract (100 mg/kg), calotropin (CLT; 100 μg/kg) and gomphogenin (GPG; 100 μg/kg) for 14 consecutive days. Bone resorption/formation biomarkers; bone specific alkaline phosphatase (BALP), osteoprotegerin (OPG) and nuclear factor-κβ ligand (RANKL) as well as serum calcium and phosphorus were assessed 24 h after last doses of treatments. Serum levels of estradiol (E2) and catalase were also measured. Oral treatment with C. procera extract, CLT and GPG caused E2 restoration to normal level with a marked regulation in the RANKL/OPG axis. Serum phosphorus and calcium were up-leveled whereas BALP was downregulated. Histopathological examination, bone histomorphometric analysis and immunohistochemical staining for osteopontin (OPN) inspection further emphasized the aforementioned outcomes. The results revealed the superiority of CLT and to a lesser extent GPG osteoporotic effect over C. procera extract. Molecular docking of the two compounds on ER-α and RANKL/OPG complex showed noteworthy binding affinities which also confirmed the supremacy of CLT due to the additional hydrogen bonding of the hydroxyl groups of the sugar moiety with RANKL/OPG complex. Finally, it is concluded that CLT and GPG from C. procera hinder bone turnover by decreasing osteoclastic bone cells activity and increasing calcium mineralization thus suppressing bone remodeling and preventing bone infirmity in OVX osteoporotic rats directly via binding to RANKL/OPG complex and ER-α and indirectly through elevating level of E2.
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