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.
In Vitro
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. Stepharine (10, 30 μM) inhibits LPS-induced increase of TLR4 expression, IκBα phosphorylation, and NF-κB p65 nuclear translocation. Stepharine exhibits neuroprotective effects on SH-SY5Y cells cultured with LPS-treated conditioned medium. Stepharine has also shown to inhibit cholinesterase in vitro. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Stepharine (500 μg/kg) inhibited NeuN + cells loss and Iba-1 + cells increase in the MCAO ischemic cortex . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Middle cerebral artery occlusion (MCAO) rat model . 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.