Liensinine

Liensinine is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke^{[1][2][3][4][5]}. In Vitro:Liensinine (5-80 μM; 24 h) reduces the viability of SaOS-2, MG-63, 143B and U-2OS osteosarcoma cells in a dose-dependent manner, but has no effect on the viability of hFOB 1.19 normal osteoblasts^[1].
Liensinine (40-80 μM; 24 h) inhibits the proliferation and colony-forming ability of SaOS-2 and 143B osteosarcoma cells, induces apoptosis, and causes G0/G1 cell cycle arrest in a dose-dependent manner^[1].
Liensinine (40-80 μM; 24 h) increases intracellular ROS production in SaOS-2 and 143B osteosarcoma cells in a dose-dependent manner, but does not affect ROS levels in hFOB 1.19 normal osteoblasts^[1].
Liensinine (40-80 μM; 24 h) disrupts the GSH/GSSG redox balance in SaOS-2 and 143B osteosarcoma cells in a dose-dependent manner by decreasing GSH levels, increasing GSSG levels, and elevating the GSSG/GSH ratio^[1].
Liensinine (40-80 μM; 24 h) induces the loss of mitochondrial membrane potential in SaOS-2 and 143B osteosarcoma cells in a dose-dependent manner^[1].
Liensinine (40-80 μM; 24 h) dose-dependently regulates the expression of apoptosis- and cell cycle-related proteins in SaOS-2 and 143B osteosarcoma cells in vitro, and inhibits the activation of the JAK2/STAT3 pathway, but exerts no effect on the aforementioned proteins in hFOB 1.19 normal osteoblasts^[1].
Liensinine (20 μM; 24 h) enhances cell viability, reduces apoptosis and cytotoxicity, and inhibits autophagy in an in vitro oxygen-glucose deprivation/reoxygenation ischemia-reperfusion model^[3]. In Vivo:Liensinine (20 mg/kg; i.p.; once daily; for 21 consecutive days) significantly inhibits the growth of subcutaneous hepatocellular carcinoma (HCC) xenografts in male BALB/c nude mice, reduces tumor vascular density, and reshapes the tumor immune microenvironment into an anti-tumor phenotype^[5].
Liensinine (20 mg/kg; i.p.; once daily for 16 consecutive days) significantly inhibits orthotopic HCC tumor progression in male C57BL/6 mice, induces tumor metabolic reprogramming, reduces tumor vascular density, regulates macrophage polarization, and downregulates PD-L1 expression^[5].