2. Academic Validation
  3. A Novel Prenylflavonoid Icariside I Ameliorates Estrogen Deficiency-Induced Osteoporosis via Simultaneous Regulation of Osteoblast and Osteoclast Differentiation

A Novel Prenylflavonoid Icariside I Ameliorates Estrogen Deficiency-Induced Osteoporosis via Simultaneous Regulation of Osteoblast and Osteoclast Differentiation

  • ACS Pharmacol Transl Sci. 2023 Jan 13;6(2):270-280. doi: 10.1021/acsptsci.2c00192.
Chuan Chen 1 2,  Mengjing Wu 1,  Hehua Lei 1,  Zheng Cao 1 2,  Fang Wu 1 2,  Yuchen Song 1 2,  Ce Zhang 1 2,  Mengyu Qin 1,  Cui Zhang 1 2,  Ruichen Du 1 2,  Jinlin Zhou 3 4,  Yujing Lu 3 5,  Denghui Xie 6,  Limin Zhang 1 2 4
Affiliations

Affiliations

  • 1 State Key Laboratory of Magnetic Resonance and Atomic and Molecular Physics, National Centre for Magnetic Resonance in Wuhan, Innovation Academy of Precision Measurement Science and Technology, CAS, Wuhan 430071, China.
  • 2 University of Chinese Academy of Sciences, Beijing 100049, China.
  • 3 Golden Health (Guangdong) Biotechnology Co., Ltd., Foshan 528225, China.
  • 4 Engineering Research Academy of High Value Utilization of Green Plants, Meizhou 514021, China.
  • 5 School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, China.
  • 6 Department of Joint Surgery, Center for Orthopaedic Surgery, The Third Affiliated Hospital of Southern Medical University, Guangzhou 510515, China.
PMID: 36798476 DOI: 10.1021/acsptsci.2c00192
Abstract

Regulation of osteoblast-mediated bone formation and osteoclast-mediated bone resorption is crucial for bone health. Currently, most clinical drugs for osteoporosis treatment such as bisphosphonates are commonly used to inhibit bone resorption but unable to promote bone formation. In this study, we discovered for the first time that icariside I (GH01), a novel prenylflavonoid isolated from Epimedium, can effectively ameliorate estrogen deficiency-induced osteoporosis with enhancement of trabecular and cortical bone in an ovariectomy (OVX) mouse model. Mechanistically, our in vitro results showed that GH01 repressed osteoclast differentiation and resorption through inhibition of RANKL-induced TRAF6-MAPK-p38-NFATc1 cascade. Simultaneously, we also found that GH01 dose-dependently promoted osteoblast differentiation and formation by inhibiting adipogenesis and accelerating energy metabolism of osteoblasts. In addition, both in vitro and in vivo studies also suggested that GH01 is not only a non-toxic natural small molecule but also beneficial for restoration of liver injury in OVX mice. These results demonstrated that GH01 has great potential for osteoporosis treatment by simultaneous regulation of osteoblast and osteoclast differentiation.

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