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Isoscopoletin is a coumarin derivative and a natural plant metabolite found, for example, in Artemisia argyi leaves, coriander, and eggplant[4][12]. It is a primary metabolite of scoparone[1]. In preclinical studies, isoscopoletin has demonstrated significant anti-proliferative activity against several cancer cell lines, including hepatocellular carcinoma (HCC), leukemia (CCRF-CEM), lung cancer, and colon cancer, with an IC50 of 4.0 μM in CCRF-CEM cells[1][11]. The primary mechanism of action in HCC appears to be via inhibition of glycolysis by directly binding to and regulating the levels of glycolysis-related proteins, specifically GPD2, GPI, Hsp90α, and PGK2, leading to reduced glucose consumption and lactate production in cancer cells[1]. Isoscopoletin also inhibits hepatitis B virus (HBV) replication[5][13]. It possesses anti-inflammatory, antioxidant, and smooth muscle relaxant properties, and has been investigated for effects in chronic bronchitis and bronchial asthma[6]. However, isoscopoletin is not an approved pharmaceutical and remains primarily a research compound with diverse biological activities.
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