摘要
This study identified six novel azaphilones,isochromophilones G-L(1-6),and three novel biosynthetically related congeners(7-9)from Diaporthe sp.SCSIO 41011.The structures and absolute configurations were elucidated through comprehensive spectroscopic analyses combined with experimental and calculated electronic circular dichroism(ECD)spectra.Significantly,three highly oxygenated azaphilones contain an acetyl group at the terminal chain(4)or linear conjugated polyenoid moieties(5 and 6),which occur infrequently in the azaphilone family.Additionally,several compounds demonstrated inhibition of lipopolysaccharide(LPS)-induced nuclear factor kappa-B(NF-κB)activation in RAW 264.7 macrophages at 20μmol·L^(-1).The novel compound(1)effectively inhibited receptor activator of NF-κB ligand(RANKL)-induced osteoclast differentiation without exhibiting cytotoxicity in bone marrow and RAW264.7 macrophages,indicating its potential as a promising lead compound for osteolytic disease treatment.This research presents the first documented evidence of azaphilone derivatives as inhibitors of RANKL-induced osteoclastogenesis.
基金
supported by the National Natural Science Foundation of China(No.82260692)
Guangxi Natural Science Foundation(No.2024GXNSFFA010004)
Bagui Youth Talent Development Program
High-Level Talent Training Project Foundation of Guangxi University of Chinese Medicine(Nos.202407 and 2022C038)
the Innovation Project of Guangxi Graduate Education(No.YCSW2025457)。
