Ascomycotols A-C: Rare Sulfur/Sulfone-Containing Scaffolds from Mushroom Endophytes with Dual Anti-inflammatory and Antirenal Fibrosis Effects.

Endophytic fungal natural products, especially sulfur- or sulfone-containing scaffolds, have attracted increasing attention as a valuable resource for drug development. Ascomycotol A (), a polyketide with an unprecedented 4-oxa-12-thiabicyclo[7.3.1]tridecane sulfur-containing scaffold, and ascomycotols B () and C () featuring rare sulfone functional moieties, were purified from the mushroom ( species)-associated endophytic sp. GLQ01 and GLQ03. Their chemical structures were assigned using nuclear magnetic resonance data, electronic circular dichroism calculations, and X-ray diffraction methods. A possible biosynthetic pathway of compounds - was speculated, involving two consecutive S-nucleophilic addition reactions and atypical incorporation of both l-Phe and d-Phe residues. Finally, biological activity studies revealed that compounds and (+)- exhibit the potential of anti-inflammatory activity, and compound has a dose-dependent protective effect on age-related renal fibrosis .