Gardenin A 是一种口服有效的、合成的 PMF 类似物，对神经突生长和神经元分化具有神经营养作用。Gardenin A 通过激活 PC12 细胞中的MAPK/ERK、PKC和PKA信号通路促进神经细胞的发生，但不激活 TrkA、CREB 信号通路。Gardenin A 也有镇静、抗焦虑、抗抑郁和抗惊厥作用。
| 生物活性 | 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 activatingMAPK/ERK,PKC, andPKA, but notTrkA, CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects[1][2]. |
体外研究
(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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体内研究
(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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| 来源 | - Plants
- Rutaceae
- Citrus reticulataBlanco
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
