Abstract

The well-known toxic medicine Gelsemium elegans is widely and historically used to treat bone fracture and skin ulcers by the folk people of China. Two new monoterpenoid indole alkaloids, gelselegandines D and E, together with the known analogue gelegamine A were isolated from G. elegans. Their structures were elucidated by means of spectroscopic techniques and quantum chemical calculations. All isolated compounds were tested for the effects on RANKL-induced osteoclast formation. Interestingly, gelselegandine E and gelegamine A, respectively, showed significant promoting and inhibitory activities on osteoclastogenesis, while gelselegandine D had no activity under the same concentration. This work suggested the different configurations for the carbons near the C-19/20 oxygen rings of the isolated compounds may be the key active groups on osteoclast formation and provided the evidence for the rationality as the traditional treatment for bone-related diseases of G. elegans.

Highlights

  • Enlightened by the clinical practice of star natural products, pharmacists and chemists are always fascinated with their complicated structures as well as potent biological activities [1,2,3]

  • The effects of compounds 1–3 on osteoclastogenesis assay induced by RANKL were tested

  • Two new monoterpenoid indole alkaloids, gelselegandines D and E, together with the known analogue gelegamine A were isolated from G. elegans

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Summary

Introduction

Enlightened by the clinical practice of star natural products, pharmacists and chemists are always fascinated with their complicated structures as well as potent biological activities [1,2,3]. G. elegans is widely and historically used to treat bone fracture and skin ulcers by the folk. G. elegans is widely and historically used to treat bone fracture and skin ulcers by the folk people of Guizhou province, China [14]. In our continuing research on MIAs medicine, gelseleparts of G. elegans [12,13]. In our continuing research on MIAs medicine, gelselegandines D gandines D (1) and E (2), two new monoterpenoid indole alkaloids together with the (1). All isolated compounds were tested for the effects on the receptor activator on the receptor activator for NF-κB ligand (RANKL)-induced osteoclast formation. MayThis be the key active groups osteoclast formation.

Structure Elucidation
Calculated
The Effects of Compounds 1–3 on Osteoclastogenesis Induced by RANKL
Effects
General Experimental Procedures
Plant Material
Extraction and Isolation
ECD Calculation
Cell Culture and Cell Viability Assay
Osteoclastogenesis Assay In Vitro
Conclusions
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