Stigmasterol 

Stigmasterol is an orally acitve, immunomodulatory agent with anti-inflammatory and neuroprotective effect, as well as able to cross the blood-brain barrier. Stigmasterol activates AMPK, which in turn inhibits NF-κB and NLRP3 signaling pathways, reduces microglia-mediated neuroinflammation, and alleviates cognitive impairment and Alzheimer's disease. Stigmasterol regulates M1/M2 polarization of microglia through the TLR4/ NF-κB pathway, thereby reducing neuropathic pain. Stigmasterol can be used for neurodegenerative diseases, inflammatory diseases, and pain management, among others^{[1][2][3][4][5]}.

Preincubation of Stigmasterol to IL-1beta-treated cells shows signi cant reduction of MMP-3 mRNA in human and mouse, MMP-3 protein in mouse, MMP-13 mRNA in mouse and human, ADAMTS-4 mRNA in human, PGE2 protein in human and mouse. Stigmasterol is also capable of counteracting the IL-1beta-induced NF-κB pathway^[1].

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

Stigmasterol (50 mg/kg; gavage; once a day; one month) alleviates cognitive deficits in mice, reduced Aβ42 concentrations in the cerebral cortex and hippocampus, and inhibits neuroinflammation by reducing proinflammatory cytokine levels and microglial activation^[1].
Stigmasterol (40 mg/kg; gavage; twice a day; 21 days) reduces thermal and mechanical hyperalgesia, serum IL-1β and IL-8 levels, and increased serum IL-4 and TGF-β levels in rats with chronic constriction injury (CCI). Stigmasterol also reduces the expression of IL-1β, COX-2, and TLR4 in the right sciatic nerve and IL-1β in the spinal cord, and promoted the transformation of M1 microglia to M2 microglia in the spinal cord^[2].
Stigmasterol (50-100 mg/kg; intraperitoneal injection; injected before LPS treatment, single dose) can reduce the total febrile response induced by LPS in rats and mice, inhibit the proliferation of neutrophils in the blood and peritoneal fluid of mice, control lung and liver damage, and inhibit the lethal effect of LPS^[3].
Stigmasterol (20-80 mg/kg; intraperitoneal injection; injected 2 hours after ischemia, single dose) can effectively reduce neurological deficits and infarct damage, improve tissue pathological changes, restore the level of endogenous antioxidant defense system, reduce the expression level of beclin1 and the conversion of LC3 I to LC3 II, promote the phosphorylation of mTOR, and inhibit the phosphorylation of AMPK and JNK and the expression of JNK induced by 24 hours of reperfusion in the rat cerebral ischemia-reperfusion injury model^[4].
Stigmasterol (10 mg/kg; oral; single dose) significantly alleviates scopolamine-induced memory impairment in the passive avoidance and Morris water maze tasks, and increases the phosphorylation levels of ERK and CREB in the hippocampus in the scopolamine-induced memory impairment model in mice. This improvement can be blocked by dizocilpine (HY-15084B) and tamoxifen (HY-13757A)^[5].

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

412.69

C₂₉H₄₈O

83-48-7

Solid

White to off-white

C[C@H](/C=C/[C@@H](CC)C(C)C)[C@H]1CC[C@@]2([H])[C@]3([H])CC=C4C[C@@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C

Room temperature in continental US; may vary elsewhere.

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

• [1]. Jie F, et al. Stigmasterol attenuates inflammatory response of microglia via NF-κB and NLRP3 signaling by AMPK activation. Biomed Pharmacother. 2022 Sep;153:113317.  [Content Brief]

  [2]. Si W, et al. Stigmasterol regulates microglial M1/M2 polarization via the TLR4/NF-κB pathway to alleviate neuropathic pain. Phytother Res. 2024 Jan;38(1):265-279.  [Content Brief]

  [3]. Antwi AO, et al. Stigmasterol inhibits lipopolysaccharide-induced innate immune responses in murine models. Int Immunopharmacol. 2017 Dec;53:105-113.  [Content Brief]

  [4]. Sun J, et al. Stigmasterol Exerts Neuro-Protective Effect Against Ischemic/Reperfusion Injury Through Reduction Of Oxidative Stress And Inactivation Of Autophagy. Neuropsychiatr Dis Treat. 2019 Oct 18;15:2991-3001.  [Content Brief]

  [5]. Park SJ, et al. The ameliorating effects of stigmasterol on scopolamine-induced memory impairments in mice. Eur J Pharmacol. 2012 Feb 15;676(1-3):64-70.  [Content Brief]