Azaphilone Alkaloids with Anti-inflammatory Activity from Fungus Penicillium sclerotiorum cib-411

Nine new azaphilone alkaloids, penazaphilones
A–I (1–9), were isolated from
the solid fermented
rice culture of Penicillium sclerotiorum cib-411.
The structures of compounds 1–9 were
elucidated based on HRESIMS, NMR, and CD spectroscopic data. The structures
of 5 and 8 were confirmed by X-ray crystallographic
analyses. Biological evaluation showed that compounds 1, 5, 6, and 8 inhibited the
production of nitric oxide (NO) on RAW 264.7 cells stimulated by lipopolysaccharide
with IC50 values of 15.29, 9.34, 9.50, and 7.05 μM,
respectively. Meanwhile, they did not exhibit obvious cytotoxicity
at a concentration of 50.0 μM.

从固态发酵糙米培养基中分离得到九种新的呋喃香豆素类生物碱，即A-I（1-9）型。基于高分辨质谱（HRESIMS）、核磁共振（NMR）和圆二色光谱（CD）数据，确定了化合物1-9的结构。通过X射线晶体学分析，确认了化合物5和8的结构。生物活性评估表明，化合物1、5、6和8在50.0 μM的浓度下对RAW 264.7细胞中由脂多糖刺激产生的氮氧化物（NO）的产生具有抑制作用，其半抑制浓度（IC50）值分别为15.29、9.34、9.50和7.05 μM。与此同时，这些化合物在该浓度下并未表现出明显的细胞毒性。