Description
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.
Structural Formula
Stepharine
Solubility
DMSO : 25 mg/mL(84.08 mM;Need ultrasonic)
Source
Plants >other families
Storage
4℃, protect from light
Shipping
Room temperature in continental US; may vary elsewhere.
SMILES
COC1=C2C3(C=CC(C=C3)=O)C[C@]4([H])C2=C(CCN4)C=C1OC
In Vivo
Stepharine (500 μg/kg) inhibited NeuN+ cells loss and Iba-1+ cells increase in the MCAO ischemic cortex.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.
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