Abstract
Studies on the relationship of nitric oxide (NO) and inflammation have revealed that compounds with NO inhibitory effects are potentially useful for inflammation and related inflammatory disorders. A phytochemical investigation to obtain new NO inhibitors resulted in the isolation of two new cleistanthane diterpenoids (1 and 2) and 11 known terpenoids (3–13) from Trigonostemon heterophyllus. The structures of these terpenoids were established by analysis of their NMR, MS, and electronic circular dichroism (ECD) data. Compounds 1 and 2 possess rare 3,4-seco-cleistanthane diterpenoid skeletons. All of the isolates were evaluated biologically for their NO inhibitory effects in lipopolysaccharide (LPS)-induced murine microglial BV-2 cells and compounds 1, 6, and 8–10 showed strong NO inhibitory effects with IC 50 values less than 40 μM. Using Western blotting experiments and molecular docking, the possible mechanism of NO inhibition was investigated.
Original language | English |
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Pages (from-to) | 417-424 |
Number of pages | 8 |
Journal | Bioorganic Chemistry |
Volume | 87 |
DOIs | |
Publication status | Published - 2019 Jun |
Bibliographical note
Funding Information:This research was supported by the National Key Research and Development Program of China (No. 2018YFA0507204), Hundred Young Academic Leaders Program of Nankai University, the Natural Science Foundation of Tianjin, China (No. 16JCYBJC27700), National Natural Science Foundation of China (Nos. U1703107, 21642016, and 21372125), and State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Guangxi Normal University, No. CMEMR2018-B02).
Funding Information:
This research was supported by the National Key Research and Development Program of China (No. 2018YFA0507204 ), Hundred Young Academic Leaders Program of Nankai University, the Natural Science Foundation of Tianjin, China (No. 16JCYBJC27700 ), National Natural Science Foundation of China (Nos. U1703107 , 21642016 , and 21372125 ), and State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Guangxi Normal University, No. CMEMR2018-B02 ).
Publisher Copyright:
© 2019 Elsevier Inc.
Keywords
- Cleistanthane diterpenoids
- Inflammation
- Molecular docking
- NO inhibitors
- Trigonostemon heterophyllus
ASJC Scopus subject areas
- Biochemistry
- Molecular Biology
- Drug Discovery
- Organic Chemistry