Description |
Gardenin A is an orally active and synthetic PMF analogue with the neurotrophic effect for neurite outgrowth and neuronal differentiation. Gardenin A promotes neuritogenesis via activating MAPK/ERK, PKC, and PKA, but not TrkA, CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects[1][2].
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Related Catalog |
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In Vitro |
Gardenin A (10-20 μM; 48 h) 可诱导 PC12 细胞神经突生长,(10 μM; 24 小时和 48 小时) 还增加神经元分化和突触形成标记蛋白、生长相关蛋白-43 (GAP-43) 和突触素的表达[1]。 Gardenin A (10 μM; 30-120分钟) 显著诱导环 AMP 反应元件结合蛋白(CREB) 的磷酸化和 CRE 介导的转录,这是通过抑制剂 2-萘酚AS-E 磷酸盐 (KG-501) 或使用 CREB siRNA 来抑制的[1]。 Gardenin A (10 μM; 15-120分钟) 增加 ERK 磷酸化水平,提高 PKA 和 PKC 活性[1]。 Cell Viability Assay[1] Cell Line: PC12 cells Concentration: 2, 5, 10, 20 μM Incubation Time: 48 hours Result: showed cell growth supporting effect at higher concentrations (10-20 µM) and did not exert detectable 237 cytotoxicity on PC12 cells after 48 h incubation in low serum medium. Western Blot Analysis[1] Cell Line: PC12 cells Concentration: 10 μM Incubation Time: 0, 15, 30, 60, and 120 min Result: Significantly increased the phosphorylation of ERK1/2 (Thr202/Tyr204) at 15 min, subsequently reduced after 30 min. Increased PKC and PKA activity peaked at 15 min.Increased CREB phosphorylation.
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In Vivo |
Gardenin A (0.1-25 mg/kg; 口服; 单剂量) 具有神经药理作用,包括镇静、抗焦虑、抗抑郁和抗惊厥作用的小鼠[2]。 栀子苷A (1-10 mg/kg; 口服; 单次剂量) 不影响小鼠的运动协调和延迟惊厥的发生[2]。 Animal Model: Male Balb/c mice (24-32 g)[2] Dosage: 1 mg/kg, 10 mg/kg, 25 mg/kg Administration: Oral gavage; single dose Result: Showed sedative effects at a dose of 25 mg/kg, which increased the duration of sleep but did not alter sleep onset.
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References |
[1]. Chiu SP, et al. Neurotrophic action of 5-hydroxylated polymethoxyflavones: 5-demethylnobiletin and gardenin A stimulate neuritogenesis in PC12 cells. J Agric Food Chem. 2013 Oct 2;61(39):9453-63. [2]. Alonso-Castro AJ, et al. Evaluation of the neuropharmacological effects of Gardenin A in mice. Drug Dev Res. 2020 Aug;81(5):600-608.
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