Traditional medicine-derived natural products as anti-osteoporotic Agents: A review on structural modifications,
Yinhua Ji1, Shikun Ji2, Xueting Bao2
1Fujian University of Traditional Chinese Medicine, No.1 Qiuyang Road, Fuzhou, 350122, People's Republic of China; The Research Center of Chiral Drugs, Innovation Research Institute of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, People's Republic of China.
Abstract:
Osteoporosis is a chronic disease affecting over 200 million people globally. It imposes a heavy burden on healthcare systems, societies, and families. Currently, clinical anti-osteoporotic drugs have various adverse effects limiting long-term use; although natural products from traditional medicines show therapeutic potential, their clinical translation is restricted by poor druggability. This article highlights how targeted chemical modifications, including heterocycle fusion, side-chain optimization, and functional group introduction, can significantly enhance anti-osteoporotic activity, improve pharmacokinetics, and reduce toxicity. Key compound classes discussed include terpenoids, alkaloids, flavonoids, coumarins, and polyphenols, with a focus on their mechanisms involving the RANKL/RANK/OPG, NF-κB, MAPK, and Wnt/β-catenin signaling pathways. The review underscores the potential of structure-activity relationship-guided design to transform traditional medicine-derived leads into promising drug candidates for osteoporosis treatment.
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