New oxindole alkaloids with selective osteoclast inhibitory activity from Gelsemium elegans

New oxindole alkaloids with selective osteoclast inhibitory activity from Gelsemium elegans
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DOI:
10.1080/14786419.2021.1913589
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发表时间:
2021-04-28
影响因子:
2.2
通讯作者:
Zhou, Ying
Zhou, Ying
中科院分区:
化学3区
文献类型:
--
作者:
Wei, Xin;Huang, Xiao-Teng;Zhou, Ying

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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.[GRAPHICS].