Agrimonolide, a compound derived from isocoumarins and found mainly in the herb Agrimonia pilosa Ledeb, has significant biological activity. agrimonolide exerts anti-inflammatory effects by inhibiting lipopolysaccharide (LPS)-induced activation of JAK-STATs and p38 MAPKs signaling pathways. Agrimonolide and its derivative, desmethyl agonolide, have been shown to be effective in increasing insulin-mediated glycogen levels in hepatocytes and may play a key role in regulating insulin-resistant HepG2 cells. agrimonolide exhibits inhibitory effects on cancer progression and induction of cell death and apoptosis by targeting SCD1 in ovarian cancer cells. In particular, Agrimonolide exhibited a dose-dependent inhibition of proliferation, migration and invasion of A2780 and SKOV-3 cells, while promoting apoptosis. The compound was also found to induce iron-mediated cell death while increasing reactive oxygen species (ROS) and total iron levels.Agrimonolide readily crosses the blood-brain barrier, suggesting its potential for therapeutic applications in neurological disorders.

通过柱色谱法从AP中分离出五种化合物，包括Agrimonolide (K1)、desmethylAgrimonolide (K2)、tormentic acid (K3)、ursolic acid (K4)和quercetin (K5)。在胰岛素抵抗性的HepG2细胞中评估了糖代谢效果。K1和K2有效提高了肝细胞中胰岛素介导的糖原水平。在20μM的浓度水平下，K1显著提高了肝细胞葡萄糖激酶(GK)活性(3.0 U min-1 mg-1蛋白质)，与对照组相比。K1显著降低了糖酵解-6-磷酸酶(G6Pase)活性，并显著改变了磷酸烯醇式丙酮酸羧化酶(PEPCK)的活性。[1] Agrimonolide在A2780和SKOV-3细胞中剂量依赖性地抑制增殖、迁移和侵袭，并促进凋亡。Agrimonolide通过增加ROS、总铁和Fe2+水平以及下调铁死亡指标(SLC7A11和GPX4)诱导了肿瘤细胞的铁死亡。此外，Agrimonolide减缓了SKOV-3异种移植模型中卵巢癌的肿瘤生长，并在肿瘤组织中显著下调SCD1表达。[2]