Higenamine

Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC₅₀=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases^{[1][2][3][4][5][6][7][8][9][10][11]}. IC50 & Target:β2-AR^[1] In Vitro:Higenamine (3-100 μM; 72 h) can inhibit the differentiation of MV4-11 and MOLM-13 cells by inhibiting the activity of LSD1^[1].
Higenamine (1-100μM; 8 h) can enhance the activity of HO-1 in C6 cells and protect brain cells from cell hypoxia damage ^[2].
Higenamine (10-50 μM; 8 h) can inhibit apoptosis in C6 cells^[2].
Higenamine (10-40 μM; 24 h) can inhibit the production of IL-1β-induced ROS and activate the ROS-mediated PI3K/Akt signaling pathway, which has anti-apoptotic activity in HNPCs^[3].
Higenamine (0.08-250 μM; 0.5-24 h) promotes phosphorylation of SMAD2/3 in a time- and dose-dependent manner in BMSCs^[6].
Higenamine (0-120 μM, 24 h) reverses H₂O₂ (250 μM, 24 h) induced cell death and apoptosis in neonatal rat ventricular myocytes (NRVMs)^[7].
In Vivo:Higenamine hydrochloride (10 mg/kg; Intraperitoneal injection; Single dose) can significantly reduce the inflammation and infarct size of cerebral ischemic injury caused by middle cerebral artery occlusion (MCAO) in Sprague-Dawley rats^[2].
Higenamine hydrochloride (0.5-4.5 mg/kg; Single dose) improves cardiac and renal function in rats with cardio-renal syndrome (CRS) and alleviates cardiac and renal fibrosis by targeting ASK1/MAPK (ERK, P38)/NF-kB signaling pathway in Sprague-Dawley rats^[4].
Higenamine hydrochloride (20 mg/kg-30 mg/kg; Intraperitoneal injection; Once daily for 60 days) promotes bone formation and prevents accelerated bone loss in SAMP6 mice^[6].
Higenamine (10 mg/kg, i.p., 2 h prior to the surgery) protects against I/R-induced myocardial infarction in mice bearing ischemia/reperfusion injury^[7].