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]}.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

412.69

C₂₉H₄₈O

481-18-5

Solid

White to off-white

CC[C@@H](C(C)C)/C=C/[C@@H](C)[C@H]1CC[C@@]2([H])C3=CC[C@@]4([H])C[C@@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Yang X, et al. A novel method for synthesis of α-spinasterol and its antibacterial activities in combination with ceftiofur. Fitoterapia. 2017 Jun;119:12-19.  [Content Brief]

  [2]. Seung I Jeong, et al. alpha-Spinasterol isolated from the root of Phytolacca americana and its pharmacological property on diabetic nephropathy. Planta Med. 2004 Aug;70(8):736-9.  [Content Brief]

  [3]. Brusco I, et al. α-Spinasterol: a COX inhibitor and a transient receptor potential vanilloid 1 antagonist presents an antinociceptive effect in clinically relevant models of pain in mice. Br J Pharmacol. 2017 Dec;174(23):4247-4262.  [Content Brief]

  [4]. Katarzyna Socała, et al. Evaluation of the antidepressant- and anxiolytic-like activity of α-spinasterol, a plant derivative with TRPV1 antagonistic effects, in mice. Behav Brain Res. 2016 Apr 15:303:19-25.  [Content Brief]

  [5]. Fabio R M Borges, et al. Anti-inflammatory action of hydroalcoholic extract, dichloromethane fraction and steroid α-spinasterol from Polygala sabulosa in LPS-induced peritonitis in mice. J Ethnopharmacol. 2014;151(1):144-50.  [Content Brief]

  [6]. Katarzyna Socała, et al. α-Spinasterol, a TRPV1 receptor antagonist, elevates the seizure threshold in three acute seizure tests in mice. Planta Med. 2004 Aug;70(8):736-9.  [Content Brief]