1,4-Naphthoquinone

1,4-Naphthoquinone is an inhibitor with broad-spectrum inhibitory activity targeting DNA polymerase, NF-κB and monoamine oxidase (MAO-A/B), with antibacterial and anti-biofilm efficacy. 1,4-Naphthoquinone is a competitive inhibitor of MAO-B (Ki=1.4 μM) and a non-competitive inhibitor of MAO-A (Ki=7.7 μM). 1,4-Naphthoquinone inhibits DNA polymerase pol α, β, γ, δ, ε, λ with IC₅₀ ranging from 5.57-128 μM. 1,4-Naphthoquinone inhibits tumor cell proliferation, induces apoptosis and necrosis, and has anti-angiogenic and anti-inflammatory activities by inducing oxidative stress, depleting glutathione (GSH), inhibiting DNA polymerase-mediated DNA synthesis and blocking NF-κB nuclear translocation. 1,4-Naphthoquinone can be used in anti-bacterial , anti-tumor and anti-inflammatory studies, including inhibition of melanoma and colon cancer cell growth and endothelial cell function, as well as LPS-induced inflammation models^{[1][2][3][4][5]}. In Vitro:1,4-Naphthoquinone (5-20 μM; 1-48 h) dose-dependently reduces cell viability, induces oxidative stress (GSH depletion, ROS elevation) and DNA damage in B16F1 melanoma cells^[1].
1,4-Naphthoquinone (1-100 μM; 24-72 h) inhibits proliferation of human colon cancer cells (HCT116) and vascular endothelial cells (HUVEC), blocks HUVEC tube formation and inhibits their migration, and the LD₅₀ for HCT116 is approximately 4.5 μM^[2].
1,4-Naphthoquinone (10 μM; 0.5-24 h) significantly inhibits LPS (100 ng/mL)-induced TNF-α secretion and NF-κB nuclear translocation in RAW264.7 macrophages, showing anti-inflammatory activity^[3].
1,4-Naphthoquinone increases the permeability of the outer and inner membranes of Chromobacterium violaceum, inhibits biofilm formation, and produce a 25 mm inhibition zone. The minimum inhibitory concentration against Chromobacterium violaceum is 405 μM^[4]. In Vivo:1,4-Naphthoquinone (250-500 μg/ear; topical application in 20 μL; single dose) significantly inhibits TPA (HY-18739)-induced edema in a mouse ear inflammation model^[3].
1,4-Naphthoquinone (20 mg/kg; intraperitoneal injection; single dose) inhibits the increase in serum TNF-α levels induced by LPS in a mouse acute inflammation model^[3].