Guaianolides from Artemisia codonocephala suppress interleukine-1β secretion in macrophages

Sesquiterpene lactones supply a variety of scaffolds for the development of anti-inflammatory drugs. In this study, eight undescribed guaianolides, i.e., lavandolides A ‒ H, were isolated from the whole plants of Artemisia codonocephala , together with five known analogues. Their planar structures and relative configurations were elucidated by spectroscopic measurements, and their absolute configurations were determined by electronic circulardichroism spectra and single crystal X-ray diffraction experiments. The nitric oxide inhibitory effect of all the isolates was assessed on lipopolysaccharide stimulated THP-1 macrophages. Lavandolide D showed a potent inhibitory effect on NO production, with IC 50 values of 3.31 ± 0.74 μ M. Furthermore, lavandolide D inhibited NOD-, LRR- and pyrin domain-containing protein 3 inflammasome-mediated interleukin-1β production through activating autophagy. • Eight undescribed guaianolides were isolated from Artemisia lavandulifolia. • Most absolute configurations were confirmed by single crystal X-ray diffraction. • Lavandolide D shows inhibition on NO production with a IC 50 value of 3.31 μ M. • Lavandolide D inhibits NLRP3-mediated IL-1β production by activating autophagy.