Liensinine

Liensinine is an isoquinoline alkaloid that has been found in N. nucifera and has diverse biological activities.^1,2,3 It is an inhibitor of voltage-gated potassium channel 10.1 (K_v10.1; IC₅₀ = 0.24 µM).² It is selective for K_v10.1 over K_v11.1 (IC₅₀ = 67 µM), K_v7.1 at 10 µM, and inward-rectifier potassium channel 2.1 (K_ir2.1) at 10 µM. Liensinine is cytotoxic to A549, NCI H520, and SPC-A1 non-small cell lung cancer (NSCLC) cells when used at concentrations ranging from 20 to 100 µM and induces apoptosis and autophagosome accumulation in A549 and SPC-A1 cells at 20 µM.³ It also reduces the proliferation and migration of HepG2 and Huh-7 hepatocellular carcinoma cells in a concentration-dependent manner.² Liensinine (0.6 and 3 mg/kg) reduces tumor growth in a HepG2 mouse xenograft model. It reduces signs of renal damage, levels of blood urea nitrogen (BUN) and serum creatinine, and mRNA expression of IL-1b, TNF-α, IL-6, and NOS2I in a mouse model of LPS-induced acute kidney injury and sepsis.¹

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1. Zhang, W., Chen, H., Xu, Z., et al. Liensinine pretreatment reduces inflammation, oxidative stress, apoptosis, and autophagy to alleviate sepsis acute kidney injury. Int. Immunopharmacol. 122, 110563 (2023).

2. Ma, B., Shi, S., Guo, W., et al. Liensinine, a novel and food-derived compound, exerts potent antihepatoma efficacy via inhibiting the K_v10.1 channel. J. Agric. Food Chem. 72(9), 4689-4702 (2024).

3. Chang, M., Ding, S., Dong, X., et al. Liensinine inhibits cell growth and blocks autophagic flux in nonsmall-cell lung cancer. J. Oncol. 2022, 1533779 (2022).