Stepharine

Stepharine, an natural alkaloid, directly interactes with TLR4 and binds to the TLR4/MD2 complex (TLR4 inhibitor). Stepharine possesses anti-aging, anti-viral and anti-hypertensive effects[1].

Signaling Pathways >> Immunology/Inflammation >> Toll-like Receptor (TLR)

Research Areas >> Cardiovascular Disease

Research Areas >> Inflammation/Immunology

Stepharine (10, 30 μM) substantially inhibits nitric oxide (NO) release as well as the mRNA and protein expression of pro-inflammatory mediators [inducible nitric oxide synthase, interleukin (IL)-6, tumor necrosis factor (TNF)-α, IL-1β] in LPS-activated BV-2 cells[1]. Stepharine (10, 30 μM) inhibits LPS-induced increase of TLR4 expression, IκBα phosphorylation, and NF-κB p65 nuclear translocation[1]. Stepharine exhibits neuroprotective effects on SH-SY5Y cells cultured with LPS-treated conditioned medium. Stepharine has also shown to inhibit cholinesterase in vitro[1].

Stepharine (500 μg/kg) inhibited NeuN+ cells loss and Iba-1+ cells increase in the MCAO ischemic cortex[1]. Animal Model: Middle cerebral artery occlusion (MCAO) rat model[1]. Dosage: 500 μg/kg (20 μL). Administration: Intranasally injected into rats 1h after MCAO. Result: Attenuated the neuronal loss induced by MCAO (MCAO+ stepharine) group.

[1]. Tingyu Hao, et al. Inflammatory mechanism of cerebral ischemia-reperfusion injury with treatment of stepharine in rats. Phytomedicine. 2020 Dec;79:153353.