New Polyketides With Anti-Inflammatory Activity From the Fungus .

Two new polyketide compounds, asperulosins A and B (-), and one new prenylated small molecule, asperulosin C (), along with nine known compounds (-), were isolated and identified from a fungus . Their structures were extensively elucidated HRESIMS, 1D, and 2D NMR analysis. The absolute configurations of the new compounds were determined by the comparison of their electronic circular dichroism (ECD), calculated ECD spectra, and the detailed discussion with those in previous reports. Structurally, compounds and belonged to the polyketide family and were from different origins. Compound was constructed by five continuous quaternary carbon atoms, which occur rarely in natural products. All of the isolates were evaluated for anti-inflammatory activity against the production of nitric oxide (NO) in lipopolysaccharide (LPS)-induced RAW264.7 cells. Among those, compounds and showed a significant inhibitory effect on NO production with IC values of 1.49 ± 0.31 and 3.41 ± 0.85 M, respectively. Additionally, compounds and markedly increased the secretion of anti-inflammatory cytokine IL10 while suppressing the secretion of pro-inflammatory cytokines IL6, TNF-α, IFN-γ, MCP-1, and IL12. Besides, and inhibited the transcription level of pro-inflammatory macrophage markers IL6, IL1β, and TNF-α while remarkably elevating the anti-inflammatory factor IL10 and M2 macrophage markers ARG1 and CD206. Moreover, and restrained the expression and nuclear translocation of NF-κB, as well as its downstream signaling proteins COX-2 and iNOS. All these results suggest that and have potential as anti-inflammatory agents, with better or comparable activities than those of the positive control, dexamethasone.