School of Biological Science and Technology, University of Jinan, Jinan, 250022, P. R. China.
Shandong Provincial Hospital, Cheeloo College of Medicine, Shandong University, Jinan, 250021, P. R. China.
Chem Biodivers. 2021 Feb;18(2):e2000639. doi: 10.1002/cbdv.202000639. Epub 2021 Feb 3.
Fractionation of the ethanol extract of a marine fungus, Arthrinium sp., afforded a new pyridone alkaloid (arthpyrone L (1)), the structure with absolute configuration of which was established by comprehensive spectroscopic analyses. In vitro cell viability assays revealed that compound 1 showed antiproliferative effects toward human A549 (lung), MG63, U2OS (bone), MCF-7 and MDA-MB-231 (breast) cancer cells. MG63 cell lines were chosen for further biological evaluations and presented apoptosis and cell cycle arrest (G0/G1 phase) upon treatment of 1. Subsequent mechanism studies demonstrated that the growth inhibition of 1 against MG63 cells was via activation of caspase-modulated apoptotic pathway and inhibition of PI3K/Akt pathway.
从海洋真菌 Arthrinium sp. 的乙醇提取物中分离得到一种新的吡啶酮生物碱（arthpyrone L (1)），其绝对构型通过综合光谱分析确定。体外细胞活力测定表明，化合物 1 对人 A549（肺）、MG63、U2OS（骨）、MCF-7 和 MDA-MB-231（乳腺）癌细胞具有抗增殖作用。选择 MG63 细胞系进行进一步的生物学评估，结果表明 1 处理后细胞发生凋亡和细胞周期阻滞（G0/G1 期）。随后的机制研究表明，1 对 MG63 细胞的生长抑制作用是通过激活 caspase 调节的凋亡途径和抑制 PI3K/Akt 途径实现的。
