Esculetin (Cichorigenin) is a coumarin derivative from various natural plant products with various biological and pharmaceutical properties including anti-edema, anti-inflammatory and anti-tumour effects. It inhibits lipoxygenases (LOs).

Esculetin通过诱导G1期细胞周期停滞减少细胞增殖，这与通过激活p27KIP[2]下调cyclin D1/CDK4和cyclin E/CDK2复合物有关。Esculetin显著以浓度和时间依赖的方式抑制HCC细胞的增殖，IC50值为2.24 mM。它阻断细胞周期在S期并在SMMC-7721细胞中诱导凋亡，显著提高caspase-3和caspase-9活性，但不影响caspase-8活性。Esculetin处理导致体内外线粒体膜电位崩溃，并伴随Bax表达上升及Bcl-2表达在转录和翻译水平上下降。Esculetin在体内外对肝细胞性肝癌具有抗增殖活性，其机制涉及启动线粒体介导的、依赖caspase的凋亡途径[3]。

Esculetin 在携带 Hepa1-6 细胞的小鼠中显著降低肿瘤生长。随着 esculetin 剂量的增加，肿瘤重量分别降低了20.33%，40.37%，和55.42%。值得注意的是，在这项动物研究中，esculetin 没有明显的毒性[3]。在由三硝基苯磺酸引起的大鼠炎症性肠病的实验模型中，以5 mg/kg的剂量，esculetin 显示出肠道抗炎作用[4]。

Tests are performed in 96-well plates. For mature adipocytes, cells are seeded (5000 cells/well), grown to confluency, induced to differentiate, and grown to maturation. For preadipocytes, a seeding density of 2500 cells/well is used, and cells are cultured overnight before treatment. Cells are incubated with either DMSO or increasing concentrations of esculetin for 6, 12, 24, or 48 hours. For the post-confluent preadipocytes, a seeding density of 2500 cells/well is used, and cells are grown to confluency before treatment. Esculetin (100 or 200 μM) in 0.01% DMSO carrier is added with the induction medium for Days 0 to 2, 2 to 4, and 4 to 6 of adipogenesis. Medium is changed every 2 days. Before assay for cell viability, cells are washed with DMEM/10% FBS three times, and 100 μL of DMEM/10% FBS medium is added to each well before treatment with 20 μL MTS assay solution per well. Cells are incubated for 1 hour at 37 °C; then 25 μL of 10% sodium dodecyl sulfate is added to each well. The absorbance is measured at 490 nm in a plate reader to determine the formazan concentration, which is proportional to the number of live cells.(Only for Reference)