L48H37 is a Curcumin analogue exhibiting enhanced chemical stability. It acts as a potent and selective inhibitor of myeloid differentiation protein 2 (MD2), effectively disrupting the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is employed in research for the treatment of sepsis or lung injury[1].
体内研究
L48H37 (intraperitoneal injection; 5 mg or 10 mg/kg; once daily; 11‐day) suppresses the growth of H460 xenograft tumors and demonstrates anti-tumor efficacy in mice[1].
体外研究
L48H37 suppresses LPS-induced inflammation, notably inhibiting TNF-α and IL-6 production as well as gene expression in mouse macrophages[1].
L48H37 (0-20 µM; 24 hours) reduces the viability of A549 and H460 cells, with IC50 values of 5.3 µM and 2.3 µM, respectively, surpassing the efficacy of curcumin in lung cancer cells. It exhibits minimal cytotoxicity on normal human lung epithelial cells (BEAS-2B), with an IC50 of 21 μM[2].
L48H37 (1, 2, or 4 µM; 16 hours) dose-dependently suppressed the expression of p-Cdc2 and Cdc2, while enhancing the expression of p53. Additionally, it elevated levels of cleaved poly (ADP-ribose) polymerase (PARP) and decreased levels of the anti-apoptotic protein Bcl-2 in H460 and A549 cells[2].
L48H37 (4 µM; 16 hours) dose-dependently triggers a rapid increase in intracellular ROS levels, as evidenced by elevated DCF levels in H460 and A549 cells[2].
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