NO inhibitors function as potential anti-neuroinflammatory agents for AD from the flowers of Inula japonica

Feng Liu, Bangjian Dong, Xueyuan Yang, Yuling Yang, Jie Zhang, Da Qing Jin, Yasushi Ohizumi, Dongho Lee, Jing Xu, Yuanqiang Guo

Research output: Contribution to journalArticlepeer-review

31 Citations (Scopus)


The extensive pathology studies revealed that Alzheimer's disease (AD) is closely related to neuroinflammation and anti-neuroinflammatory agents may be potentially useful for the treatment of AD. Inula japonica is a member of the Asteraceae plant family and its flowers have been used as a healthy tea and a traditional Chinese medicine. Our continuous search for new nitric oxide (NO) inhibitory substances as anti-neuroinflammatory agents for AD resulted in the isolation of two new sesquiterpenes and ten known terpenes from the flowers of I. japonica. Their structures were established on the basis of extensive analysis of NMR and MS spectroscopic data, as well as calculated and experimental electronic circular dichroism (ECD) spectra. Among these isolates, compound 1 is a new sesquiterpene with a rare tricyclic fused skeleton, and 2 processes a 1,10-seco-eudesmane skeleton. The anti-neuroinflammatory effects were examined by inhibiting NO release in LPS-induced murine microglial BV-2 cells. The possible mechanism of NO inhibition was also investigated using molecular docking, which revealed the interactions of bioactive compounds with the iNOS protein. The present study disclosed that the flowers of I. japonica as a healthy tea are potentially useful for AD and related neuroinflammatory diseases.

Original languageEnglish
Pages (from-to)168-175
Number of pages8
JournalBioorganic Chemistry
Publication statusPublished - 2018 Apr

Bibliographical note

Funding Information:
This work was supported by the National Natural Science Foundation of China (Nos. U1703107 , 21372125 , and 21642016 ), the Natural Science Foundation of Tianjin, China (No. 16JCYBJC27700 ), the Fundamental Research Funds for the Central Universities , Hundred Young Academic Leaders Program of Nankai University , and the State Key Laboratory of Medicinal Chemical Biology (No. 201602007 ).

Publisher Copyright:
© 2018 Elsevier Inc.


  • Anti-neuroinflammatory
  • Inula japonica
  • Molecular docking
  • NO inhibitory effects
  • Sesquiterpenes
  • iNOS

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Drug Discovery
  • Organic Chemistry


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