New oxindole alkaloids with selective osteoclast inhibitory activity from Gelsemium elegans.

A new alkaloid 14-hydroxygelseziridine (1), along with four known oxindoles (2-5), was isolated and characterized from the well-known toxic medicine Gelsemium elegans. Their structures were elucidated by means of spectroscopic techniques and quantum chemistry calculations. Structurally, new compound 1 has a three membered oxygen ring at N-4/C-20. All compounds were tested for osteoclast (MOC-1) inhibitory activity in vitro. Compound 2 exhibited the selective osteoclast inhibitory activity. Flow cytometry revealed that the apoptosis of osteoclasts induced by 2. Furthermore, the PCR bioassay suggested that compound 2 may activate the apoptotic pathway of osteoclasts by reducing the expression of IL-6 and c-Jun, and increasing caspase 9. This work provided the evidence for the rationality as the traditional treatment for bone related diseases of G. elegans, and shed a new light on its further research.

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Xin Wei, Xiao-Teng Huang, Li-Yan Zhang, Xin-Yue Hu, Wei Zhang, Yong-Qiang Zhou, Hao-Fei Yu, Cai-Feng Ding, Lan-Chun Zhang, Xia Liu, Ying Zhou. New oxindole alkaloids with selective osteoclast inhibitory activity from Gelsemium elegans. Natural product research. 2022 May;36(10):2630-2636

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PMID: 33908330

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