Litcius/Paper detail

Anti-Neuroinflammatory Components from Clausena lenis Drake

Si-Si Zhu, Yifan Zhang, Meng Ding, Ke‐Wu Zeng, Pengfei Tu, Yong Jiang

2022Molecules11 citationsDOIOpen Access PDF

Abstract

Clausena lenis Drake (C. lenis) is a folk medicinal herb to treat influenza, colds, bronchitis, and malaria. The 95% and 50% ethanol extract of C. lenis showed significant nitric oxide (NO) inhibition activity in BV-2 microglial cells stimulated by lipopolysaccharide (LPS). Bio-guided isolation of the active extract afforded five new compounds, including a chlorine-containing furoquinoline racemate, (±)-claulenine A (1), an amide alkaloid, claulenine B (2), a prenylated coumarin, claulenin A (3), a furocoumarin glucoside, clauleside A (4), and a multi-prenylated p-hydroxybenzaldehyde, claulenin B (5), along with 33 known ones. Their structures were determined via spectroscopic methods, and the absolute configurations of new compounds were assigned via the electronic circular dichroism (ECD) calculations and single-crystal X-ray diffraction analysis. Compounds 2, 23, 27, 28, 33, and 34 showed potent anti-neuroinflammatory effects on LPS-induced NO production in BV-2 microglial cells, with IC50 values in the range of 17.6–40.9 μM. The possible mechanism was deduced to interact with iNOS through molecular docking.

Topics & Concepts

ChemistryStereochemistryCoumarinAmideNitric oxideBiochemistryOrganic chemistryPlant chemical constituents analysisAlkaloids: synthesis and pharmacologyNatural product bioactivities and synthesis