Suppression of lipopolysaccharide-induced COX-2 expression via p38MAPK, JNK, and C/EBPβ phosphorylation inhibition by furomagydarin A, a benzofuran glycoside from Magydaris pastinacea

Abstract

The phytochemical investigation of the methanol extract of the seeds of Magydaris pastinacea afforded two undescribed benzofuran glycosides, furomagydarins A-B (1, 2), together with three known coumarins. The structures of the new isolates were elucidated after extensive 1D and 2D NMR experiments as well as HR MS. Compound 1 was able to inhibit the COX-2 expression in RAW264.7 macrophages exposed to lipopolysaccharide, a pro-inflammatory stimulus. RT-qPCR and luciferase reporter assays suggested that compound 1 reduces COX-2 expression at the transcriptional level. Further studies highlighted the capability of compound 1 to suppress the LPS-induced p38MAPK, JNK, and C/EBPβ phosphorylation, leading to COX-2 down-regulation in RAW264.7 macrophages.

Keywords:

• COX-2
• benzofurans
• Magydaris pastinacea
• p38MAPK
• JNK
• C/EBPβ

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

Financial support from the MIUR, Rome, by the University of Cagliari (FIR 2020). This research was also funded by the National Science and Technology Council [MOST 110–2320-B-038–035-MY3 and NSTC 112–2320-B-038–041]. We acknowledge the CeSAR (Centro Servizi Ricerca d’Ateneo) core facility of the University of Cagliari and Dr. Sandrina Lampis for recording NMR spectra.