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February 19, 2026Pharmaceuticals0 citationsOpen Access

Design, Synthesis and Biological Evaluation of Novel Furanocoumarin Derivatives: Validation of Anti-Osteoporotic Efficacy In Vitro and In Vivo

XCXiaoqi ChenSCShuirong ChenQGQi Gao

Key Points

  • The aim is to design and evaluate new furanocoumarin derivatives for their effectiveness in treating osteoporosis.
  • Designed and synthesized novel furanocoumarin derivatives.
  • Evaluated compound B15 in an ovariectomy (OVX) mouse model.
  • Assessed changes in bone microarchitecture and serum bone metabolism markers.
  • Analyzed histopathological features of bone tissue.
  • Compound B15 exhibits reduced toxicity and superior inhibition of osteoclast formation compared to isoimperatorin.
  • B15 decelerates osteoporosis progression in OVX mice.
  • B15 significantly increases estradiol levels in serum of OVX mice.

Abstract

Background/Objectives: Osteoporosis is a metabolic bone disease characterized by reduced bone mass and impaired bone microarchitecture. It has become a major clinical challenge due to the limitations of current therapeutic approaches. Isoimperatorin (ISO), a naturally occurring and biologically active furanocoumarin extracted from various traditional herbals, exhibits therapeutic potential in combating osteoporosis. However, toxicity limits its application. Methods: In vivo, compound B15 was evaluated in an Ovariectomy (OVX) mice model, where treatment was associated with changes in bone microarchitecture parameters, modulation of serum bone metabolism markers, and alterations in the histopathological features of bone tissue. Results: In this study, a new series of furanocoumarin derivatives was designed and synthesized for the treatment of osteoporosis. Compared with ISO, compound B15 has less toxicity and better ability to inhibit osteoclast formation in vitro. Compound B15 could decelerate the progression of osteoporosis in ovariectomized mice. It is worth mentioning that the expression of estradiol in the serum of mice with excised ovaries was significantly increased by compound B15. Conclusions: These results imply that the novel furanocoumarin derivative B15 is a promising therapeutic option for osteoporosis.

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Cite This Study

Chen et al. (2026) studied this question.

synapsesocial.com/papers/6996a7c3ecb39a600b3edb6ahttps://doi.org/10.3390/ph19020327
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