Moreover, 1 and 5 restrained the expression and nuclear translocation of NF-κB, as well as its downstream signaling proteins COX-2 and iNOS. Besides, 1 and 5 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. Additionally, compounds 1 and 5 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. Among those, compounds 1 and 5 showed a significant inhibitory effect on NO production with IC 50 values of 1.49 ± 0.31 and 3.41 ± 0.85 μM, respectively. All of the isolates were evaluated for anti-inflammatory activity against the production of nitric oxide (NO) in lipopolysaccharide (LPS)-induced RAW264.7 cells. Compound 2 was constructed by five continuous quaternary carbon atoms, which occur rarely in natural products. Structurally, compounds 1 and 2 belonged to the polyketide family and were from different origins. 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. Their structures were extensively elucidated via HRESIMS, 1D, and 2D NMR analysis. Two new polyketide compounds, asperulosins A and B ( 1– 2), and one new prenylated small molecule, asperulosin C ( 3), along with nine known compounds ( 4– 12), were isolated and identified from a fungus Aspergillus rugulosa. 3Maternal and Child Health Hospital of Hubei Province, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.1Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.Qianqian Xu 1 †, Yuben Qiao 1 †, Zijun Zhang 1 †, Yanfang Deng 1, Tianqi Chen 1, Li Tao 2, Qiaoxin Xu 1, Junjun Liu 1, Weiguang Sun 1, Ying Ye 1, Yuanyuan Lu 3*, Changxing Qi 1* and Yonghui Zhang 1*
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