Columbamine chloride is an organic heterocyclic alkaloid and a metabolite of berberine which is widely found in Ranunculaceae plants such as Coptis and Phellodendron. Columbamine chloride induces apoptosis in cancer cells and exhibits anticancer activity. Columbamine chloride inhibits the cytochrome P450 (CYP) subtype CYP3A4 (IC50 = 30.6 µM). Columbamine chloride possesses various biological activities, including antioxidant, anti-inflammatory, antifungal, antiprotozoal, hepatoprotective, neuroprotective, lipid-lowering, and hypoglycemic effects.

CYP3A4:30.6 µM

Methods: HCT116 cells were treated with Columbamine chloride (0, 20, 30, 40 μM) for 48 hours, and apoptosis was assessed by TUNEL staining and flow cytometry.
Results: Columbamine chloride induced concentration-dependent cell death in HCT116 cells. [1]
Methods: Columbamine chloride (15 μM) was added to Hep G2 cells and incubated for 24 hours; real-time quantitative PCR was used to detect changes in the mRNA expression of ACC, FAS, GPAT, HMGCR, and mCAD.
Results: Columbamine chloride significantly inhibited the mRNA expression of the lipid synthesis-related genes ACC, FAS, GPAT, and HMGCR, and increased the mRNA expression of the fatty acid oxidation-related gene mCAD. [2]

Methods: To investigate the tumor growth-inhibiting effects of Columbamine chloride, BALB/c nude mice were selected and subcutaneously injected with HCT116 cells. Following successful tumor engraftment, Columbamine chloride (5, 10, 20 mg/kg) was administered for 23 consecutive days.
Results: Columbamine chloride inhibited tumor growth in a dose-dependent manner. [1]

DMSO: 4 mg/mL (10.7 mM), Sonication is recommended.