Di-O-methylhonokiol shows diverse bioactivities and potential therapeutic effects. It promotes neurite growth in rat cortical neurons, with notable activity at concentrations of 0.1 µM and 1 µM, and enhances neurite length by about 111 µM. The compound exhibits inhibitory effects on inflammatory enzymes, including 45% inhibition of COX1 in ram seminal vesicle and 47.8% inhibition of COX2 in sheep placental vesicle at an 8 µM concentration, with IC50 values of 11400.0 nM and 7700.0 nM, respectively. It also inhibits 5LOX-mediated LTB4 formation in stimulated human polymorphonuclear leukocytes, with a 27.8% inhibition and an IC50 value of 15000.0 nM. In addition, Di-O-methylhonokiol modulates the GABAAalpha1beta2 receptor by potentiating GABA-induced chloride current, exhibiting an EC50 of 42100.0 nM and maximal potentiation of 368% at 30 µM concentration.
The compound has a high octanol-water partition coefficient (log P) of around 5.69, indicating higher hydrophobicity and potential for good membrane permeability. It shows antiproliferative activity against various human and mouse cell lines, including HUVEC, HepG2, LL/2, MCF7, CNE2Z, and I10 cells, with IC50 values indicating limited potency, generally above 100,000.0 nM. Di-O-methylhonokiol also demonstrates significant inhibition of LPS-induced COX2-mediated PGF1 production and NO production in mouse RAW264.7 cells, displaying cytotoxicity at higher concentrations. Furthermore, it acts as a CB2 receptor ligand with a Ki value of 1375.0 nM, showcasing its moderate affinity for this receptor.
Overall, Di-O-methylhonokiol demonstrates a broad spectrum of bioactivities, including inflammation modulation, receptor activity modulation, and limited antiproliferative effects, with moderate hydrophobicity and potential membrane permeability..
Note: Summary generated by AI. Data source: ChEMBL 