Monoterpenoid indole alkaloids from the fruits of Gelsemium elegans and their anti-inflammatory activities

作者：Li, Ni-Ping; Liu, Jun-Shan; Liu, Jiao-Wen; Tian, Hai-Yan; Zhou, Hong-Ling; Zheng, Yuan-Ru; Huang, Xiao-Jun; Cao, Jia-Qing; Ye, Wen-Cai^*; Wang, Lei^*

来源：Bioorganic Chemistry, 2021, 107: 104624.

DOI：10.1016/j.bioorg.2020.104624

• Gelsemium elegans
• Monoterpenoid indole alkaloid
• Anti-inflammatory activity

Two novel monoterpenoid indole alkaloids (MIAs), gelsechizines A-B (1-2), along with four known ones (3-6) were isolated from the fruits of Gelsemium elegans. Compound 1 features a new carbon skeleton with two additional carbon atoms forming a 4-methylpyridine unit. Their structures with absolute configurations were elucidated by NMR, MS, X-ray diffraction and electronic circular dichroism (ECD) calculations. Compounds 1-3 showed significant anti-inflammatory effects in vivo and in vitro, which may be related to the inhibition of the trecruitment of neutrophils and macrophages as well as the secretion of TNF-alpha and IL-6. Preliminary structure-activity relationship analysis revealed that the beta-N-acrylate moiety plays an important role in the anti-inflammatory effect.

• 单位
  南方医科大学