Gastrodin
(Synonyms: 天麻素; Gastrodine) 目录号 : GN10277
Gastrodin是一种酚性葡糖苷，是中草药天麻的主要活性成分，具有镇静催眠抗惊厥效果。
Cas No.:62499-27-8
Sample solution is provided at 25 µL, 10mM.
Gastrodin is a phenolic glucoside and the main active component of the Chinese herb Tianma and it has sedative, hypnotic and anticonvulsant effects [1]. Gastrodin can penetrate the blood-brain barrier and restore the imbalance between excitation and inhibition processes in the cerebral cortex, showing good antihypertensive, sedative and hypnotic effects, and having certain therapeutic effects on neurasthenia, insomnia and headache. It can also dilate blood vessels, improve microcirculation of the myocardium, relieve cerebral vasospasm, increase myocardial nutritional blood flow and enhance oxygen supply capacity. Gastrodin also has anti-inflammatory and anti-obesity effects [2]. Gastrodin can be used in the research of treatment for dizziness, epilepsy, stroke and dementia [3].
In vitro, Gastrodin (30, 40 and 60μM; 1h) pretreatment significantly inhibited the protein and mRNA expression levels of iNOS, COX-2, TNF-α, IL-1β and NF-κB in lipopolysaccharide (LPS)-stimulated microglia, and weakened the phosphorylation of extracellular signal-regulated kinase 1/2 (ERK1/2), c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase (p38MAPK) [4]. Gastrodin (5, 10 and 20μM; 1h) pretreatment significantly upregulated the (PI3-K)/Akt signaling pathway in LPS-induced H9c2 cardiomyocytes in a dose-dependent manner, while inhibiting the activation of NF-κB and MAPKs [5].
In vivo, Gastrodin (10, 50mg/kg/day; 2 weeks; i.p.) treatment significantly inhibited the loss of retinal ganglion cells (RGCs) in acute ocular hypertension (AOH) rats and reduced the number of Iba1-positive microglia in the retina [6]. Gastrodin (10, 20mg/kg/day; 28 days;) can improve the depressive-like behavior of depressed mice through oral administration, increase neurotransmitter levels, improve nerve cell damage, and inhibit the expression of Caspase-3 [7].
References:
[1] Liu Y, Gao J, Peng M, et al. A review on central nervous system effects of gastrodin[J]. Frontiers in pharmacology, 2018, 9: 24.
[2] Dai Y, Ban W, Yang Z. Gastrodin, a promising natural small molecule for the treatment of central nervous system disorders, and its recent progress in synthesis, pharmacology and pharmacokinetics[J]. International journal of molecular sciences, 2024, 25(17): 9540.
[3] Yang C S, Chiu S C, Liu P Y, et al. Gastrodin alleviates seizure severity and neuronal excitotoxicities in the rat lithium-pilocarpine model of temporal lobe epilepsy via enhancing GABAergic transmission[J]. Journal of ethnopharmacology, 2021, 269: 113751.
[4] Dai JN, Zong Y, Zhong LM, Li YM, Zhang W, Bian LG, Ai QL, Liu YD, Sun J, Lu D. Gastrodin inhibits expression of inducible NO synthase, cyclooxygenase-2 and proinflammatory cytokines in cultured LPS-stimulated microglia via MAPK pathways. PLoS One. 2011;6(7):e21891.
[5] Yang P, Han Y, Gui L, Sun J, Chen YL, Song R, Guo JZ, Xie YN, Lu D, Sun L. Gastrodin attenuation of the inflammatory response in H9c2 cardiomyocytes involves inhibition of NF-κB and MAPKs activation via the phosphatidylinositol 3-kinase signaling. Biochem Pharmacol. 2013 Apr 15;85(8):1124-33.
[6] Wang JW, Liu YM, Zhao XF, Zhang H. Gastrodin protects retinal ganglion cells through inhibiting microglial-mediated neuroinflammation in an acute ocular hypertension model. Int J Ophthalmol. 2017 Oct 18;10(10):1483-1489.
[7] Pei H, Shen H, Bi J, et al. Gastrodin improves nerve cell injury and behaviors of depressed mice through Caspase‐3‐mediated apoptosis[J]. CNS Neuroscience & Therapeutics, 2024, 30(3): e14444.
Gastrodin是一种酚性葡糖苷，是中草药天麻的主要活性成分，具有镇静催眠抗惊厥效果 [1]。Gastrodin可以穿透血脑屏障，可恢复大脑皮质兴奋与抑制过程间的平衡失调，具有较好的降压，镇静、催眠作用，对神经衰弱、失眠头痛有一定疗效，还能扩张血管、改善心肌微循环、缓解脑血管痉挛、增加心肌营养性血流量提高供氧能力。Gastrodin还具有抗炎和抗肥胖作用 [2]。Gastrodin可用于头晕，癫痫，中风和痴呆症的治疗研究 [3]。
在体外，Gastrodin（30, 40和60μM; 1h）预处理显著抑制了脂多糖（LPS）刺激的小胶质细胞中的iNOS、COX-2、TNF-α、IL-1β和NF-κB的蛋白和mRNA表达水平，并减弱了细胞外信号调节激酶1/2（ERK1/2）、c-Jun N端蛋白激酶（JNK）和p38丝裂原活化蛋白激酶（p38MAPK）的磷酸化 [4]。Gastrodin（5, 10和20μM; 1h）预处理以剂量依赖性方式明显上调了LPS诱导的H9c2心肌细胞中(PI3-K)/Akt信号传导，而抑制NF-κB和MAPKs的激活 [5]。
在体内，Gastrodin（10, 50mg/kg/day;2 weeks; i.p.）治疗剂量依赖性显著抑制了急性高眼压症（AOH）大鼠的视网膜神经节细胞（RGC）的丢失，并减少视网膜Iba1阳性小胶质细胞数量 [6]。Gastrodin（10, 20mg/kg/day; 28 days; ）通过口服治疗能够改善抑郁症小鼠的抑郁样行为，提高了神经递质水平，改善了神经细胞损伤，并抑制其Caspase-3表达 [7]。
| Cell experiment [1]: | |
Cell lines | Mouse microglial cell line BV-2 cells |
Preparation Method | Cells were cultured in Dulbecco's modified Eagle's medium containing 2% fetal bovine serum and antibiotics (100IU/ml penicillin and 100µg/ml streptomycin) and maintained at 37°C in a humidified incubator with 5% CO2. Cells (approximately 1×106 cells/ml) were seeded in six-well plates before being subjected to treatments. Five groups of BV-2 cells were subjected to various treatments. In group 1, the cells were incubated in serum-free DMEM. In group 2, the cells were treated with 1µg/ml lipopolysaccharide (LPS). In groups 3, 4, and 5, the cells were treated with 30µM, 40µM, and 60µM Gastrodin for 1h and then stimulated with LPS (1µg/ml). After incubation of the cells for 30min to 4h, reverse transcription polymerase chain reaction (RT-PCR) and protein blotting analysis were performed. |
Reaction Conditions | 30, 40 and 60μM; 1h |
Applications | Gastrodin pretreatment significantly inhibited the protein and mRNA expression levels of iNOS, COX-2, TNF-α, IL-1β and NF-κB in microglial cells stimulated by LPS. |
| Animal experiment [2]: | |
Animal models | SD rats (acute ocular hypertension (AOH) model) |
Preparation Method | All the operations were performed under general anesthesia with intraperitoneal injection of chloral hydrate (400mg/kg) and additional topical anesthesia (0.5% proparacaine hydrochloride eye drops). The anterior chamber of a randomly chosen eye was cannulated with a 30-Gauge infusion needle connected with a 500mL saline-filled bottle. By keeping the bottle to a height of 1500mm above the eye, the Intraocular pressure (IOP) could rise to 110mm Hg. The IOP was monitored using a Tono-Pen and continuously maintained for 60min. The rats with only anterior chamber penetration and without IOP elevation were served as the control group. After 60min, the needle was removed from the anterior chamber and the rats were intraperitoneally injected with Gastrodin at 10mg/kg (G10 group), 50mg/kg (G50 group) and 0.9% NS (NS group), respectively, once a day for the next 2wk. The loss of RGCs and the number of Iba1-positive retina microglia were determined at 2wk after rapid ocular hypertension. |
Dosage form | 10, 50mg/kg/day; 2 weeks; i.p. |
Applications | Gastrodin treatment dose-dependently significantly inhibited the loss of retinal ganglion cells (RGCs) in AOH rats, and reduced the number of Iba1-positive microglia in the retina. |
References: | |
| Cas No. | 62499-27-8 | SDF | |
| 别名 | 天麻素; Gastrodine | ||
| 化学名 | (2R,3S,4S,5R,6S)-2-(hydroxymethyl)-6-[4-(hydroxymethyl)phenoxy]oxane-3,4,5-triol | ||
| Canonical SMILES | C1=CC(=CC=C1CO)OC2C(C(C(C(O2)CO)O)O)O | ||
| 分子式 | C13H18O7 | 分子量 | 286.28 |
| 溶解度 | Water : 100 mg/mL (349.31 mM); DMSO : >50 mg/mL (174.65 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4931 mL | 17.4654 mL | 34.9308 mL |
| 5 mM | 698.6 μL | 3.4931 mL | 6.9862 mL |
| 10 mM | 349.3 μL | 1.7465 mL | 3.4931 mL |
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- Purity: >99.50%
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