Dihydroberberine

Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy^[1][2]. In Vitro: Dihydroberberine has a synergistic effect with sunitinib, and when mixed together, it exhibits anti-cancer effects in human non-small cell lung cancer cell lines (NSCLC), A549, NCI-H460 and NCI-H1299 cells. Dihydroberberine (25 μM; 48 h) inhibits NCI-H460 cell proliferation and colony formation^[2].
NCI-H460 cells were treated with a mixture (DCS) of Dihydroberberine (25 μM) and Sunitinib (2 μM) to arrest the cell cycle in the G1 phase. DCS regulates JNK/p38 MAPK signaling and plays a role in inducing apoptosis^[2].
In Vivo: Dihydroberberine (250 mg/kg; intragastric gavage, once every other day for 14 days) effectively inhibits tumor growth and proliferation in the mouse NCI-H460 xenograft model and exhibits synergistic with Sunitini^[2].