α-Spinasterol

α-Spinasterol is an orally taken antagonist of transient receptor potential vanilloid 1 ( TRPV1), and it's also an inhibitor of COX-1 and COX-2, with IC₅₀ values of 16.17 μM and 7.76 μM, respectively. α-Spinasterol exhibits antibacterial, anti-inflammatory, antidepressant, and antioxidant effects, has the ability to cross the blood-brain barrier, and can improve diabetes in mice^{[1][2][3][4][5][6]}. In Vitro: α-Spinasterol has antimicrobial activity, with MIC values of 0.13, 0.24, 1.92 and 3.69 nM against E.coli, S.pneumoniae CAU0070, S.pullorum cvcc533, S.aureus, respectively^[1].
α-Spinasterol shows even better antibacterial effects when combined with ceftriaxone^[1].
α-Spinasterol (0-0.5 ng/mL, 24 h) inhibits glomerular mesangial cells (GMCs), with an IC₅₀ of 3.9×10^-12 g/mL^[2]. In Vivo: α-Spinasterol (0.5-2.5 mg/kg, oral, 6 weeks) lowers serum triglycerides in mice and improves symptoms of diabetes^[2].
α-Spinasterol (0.1-1 mg/kg, oral, 24 h) has anti-nociceptive effects in postoperative and neuropathic pain models in mice^[3].
α-Spinasterol (0-2 mg/kg, i.p., single dose) exhibits antidepressant effects in mice but does not show anxiolytic effects^[4].
α-Spinasterol (0.001-10 mg/kg, i.g., single dose) significantly reduces inflammatory cell infiltration induced by LPS (HY-D1056) in mice^[5].
α-Spinasterol (0.001-1 mg/kg, i.p., single dose) can inhibit leukocytes and mononuclear cells in mice, with ID₅₀ at 0.006 (0.002-0.01) mg/kg and 0.004 (0.002-0.007) mg/kg^[5].
α-Spinasterol (0.001-1 mg/kg, i.p., single dose) has anticonvulsant activity in mice without affecting their neuromuscular strength, impairing motor coordination, or changing body temperature^[6].