Structure of Gastrodin
CAS No.: 62499-27-8
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Gastrodin, an anti-inflammatory polyphenol isolated and purified from the Chinese natural herbal Gastrodia elata Blume., benefits neurodegenerative diseases.
Synonyms: Gastrodine
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| CAS No. : | 62499-27-8 |
| Formula : | C13H18O7 |
| M.W : | 286.28 |
| SMILES Code : | OCC1=CC=C(C=C1)O[C@@H]2O[C@H](CO)[C@H]([C@@H]([C@H]2O)O)O |
| Synonyms : |
Gastrodine
|
| MDL No. : | MFCD00272169 |
| InChI Key : | PUQSUZTXKPLAPR-UJPOAAIJSA-N |
| Pubchem ID : | 115067 |
| GHS Pictogram: |
|
| Signal Word: | Warning |
| Hazard Statements: | H302 |
| Precautionary Statements: | P280-P305+P351+P338 |
In Vitro:
|
Cell Line
|
Concentration | Treated Time | Description | References |
| SCC25-CR cells | 20 µM | 12 hours | Inhibited glycolysis and HK2 expression | Cell Death Discov. 2023 Oct 2;9(1):364. |
| Neonatal rat cardiomyocytes (NRCMs) | 100 µM | 12 hours | Gastrodin alleviated phenylephrine-induced cardiomyocyte hypertrophy, as indicated by reduced cell surface area and decreased ANF and cTnT protein expression | Front Pharmacol. 2017 Apr 25;8:222. |
| SCC4-CR cells | 10, 20, 40 µM | 24 hours | Inhibited glycolysis and HK2 expression, promoted apoptosis | Cell Death Discov. 2023 Oct 2;9(1):364. |
| CAL27-CR cells | 10, 20, 40 µM | 24 hours | Inhibited glycolysis and HK2 expression, promoted apoptosis | Cell Death Discov. 2023 Oct 2;9(1):364. |
| HepG2 cells | 10, 30, 100 µM | 24 hours | Gastrodin alleviated insulin resistance by increasing glucose consumption, glucose uptake, and glycogen content in dexamethasone-induced HepG2 cells. The Western blotting results showed that gastrodin upregulated the expression of insulin receptors and ubiquitin-specific protease 4 (USP4) and increased the phosphorylation of GATA binding protein 1 (GATA1) and protein kinase B (AKT) in vivo and in vitro. | Front Pharmacol. 2021 Sep 16;12:710722. |
| Rat kidney fibroblast cell lines (NRK-49F) | 25-100 µM | 24 hours | To evaluate the effect of gastrodin on the expression of α-SMA, fibronectin, collagen I, and p-Smad2/p-Smad3 proteins in TGF-β1-stimulated NRK-49F cells. Results showed gastrodin significantly reversed their upregulation without affecting cell viability. | Front Pharmacol. 2023 Jan 17;14:1082281. |
| PC12 cells | 0.1–100 µM | 24–48 hours | Evaluate the effect of Gastrodin on the survival rate of PC12 cells, results showed that 0.1–100 µM Gastrodin had no significant effect on the survival rate of Q23 and Q74 PC12 cells after 24–48 h of incubation | Int J Mol Sci. 2024 Jul 14;25(14):7709. |
| Q74 PC12 cells | 1, 5, 25 µM | 36 hours | Gastrodin significantly reduces the expression levels of mHtt and polyQ proteins in a dose-dependent manner | Int J Mol Sci. 2024 Jul 14;25(14):7709. |
| Q74 PC12 cells | 25 µM | 36 hours | Gastrodin promotes neurite outgrowth in Q74 PC12 cells and improves cell morphology | Int J Mol Sci. 2024 Jul 14;25(14):7709. |
| H9c2 cardiomyocytes | 20, 50, 100 µM | 4 hours | GAS pretreatment significantly ameliorated the decrease in cell viability and increase in apoptosis of H9c2 cells treated with 400 μM H2O2 for 3 h. | Acta Pharmacol Sin. 2020 Oct;41(10):1314-1327. |
| Neonatal rat cardiac fibroblasts (CFs) | 1 µM or 5 µM | 48 hours | To evaluate the inhibitory effect of gastrodin on high glucose and high palmitic acid (HG-PA)-induced differentiation, collagen synthesis, and cell migration in cardiac fibroblasts. Results showed that gastrodin significantly inhibited the increase in α-SMA protein and mRNA levels, as well as the expression of collagen I and collagen III induced by HG-PA. | Chin Med. 2024 Nov 22;19(1):164. |
| Macrophages | 10 µM or 100 µM | 6 hours or 12 hours | To evaluate the inhibitory effect of Gastrodin on VSV and HSV-1 infection. Results showed that Gastrodin significantly reduced the viral load of VSV and HSV-1 in macrophages. | Front Pharmacol. 2021 Feb 19;11:608707. |
| Human umbilical vein endothelial cells (HUVECs) | 50 µM and 100 µM | 6 hours pretreatment followed by 24 hours | To evaluate the effect of Gastrodin on H2O2-induced senescence in HUVECs. Results showed that Gastrodin reduced the proportion of SA β-gal positive cells, decreased the expression levels of p16 and p21 proteins, and enhanced the proliferation and migration ability of HUVECs. | J Cell Mol Med. 2024 Feb;28(3):e18089. |
In Vivo:
|
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
| C57BL/6J mice | Chronic unpredictable mouse stress (CUMS) model | Intragastric administration | 10 mg/kg and 20 mg/kg | Once daily for 28 consecutive days | Gastrodin improved depression-like behaviors and nerve cell injury in CUMS mice by inhibiting Caspase-3-mediated apoptosis | CNS Neurosci Ther. 2024 Mar;30(3):e14444 |
| C57BL/6J mice | VSV or HSV-1 infection model | Intraperitoneal injection | 10 mg/kg or 100 mg/kg | Single dose, observed for 96 hours | To evaluate the protective effect of Gastrodin on VSV and HSV-1 infected mice. Results showed that Gastrodin significantly improved the survival rate of infected mice and reduced viral load. | Front Pharmacol. 2021 Feb 19;11:608707. |
| Nude mice | CAL27-CR xenograft model | Intraperitoneal injection | 10 mg/kg, 30 mg/kg | Every two days until the end of the experiment | Inhibited tumor growth and glycolysis | Cell Death Discov. 2023 Oct 2;9(1):364. |
| B6-hHTT130-N transgenic mice | Huntington's disease model | Oral | 100 mg/kg | Once daily until 12 weeks of age | Gastrodin increases grip strength and attenuates mHtt aggregates in B6-hHTT130-N transgenic mice | Int J Mol Sci. 2024 Jul 14;25(14):7709. |
| Sprague-Dawley rats | Subarachnoid hemorrhage model | Intraperitoneal injection | 100 mg/kg/ day | Administered at 2, 24, and 48 hours after SAH | Gastrodin significantly attenuated SAH-induced neurological deficits, brain edema, and increased blood-brain barrier permeability, while reducing glutamate concentration in cerebrospinal fluid and intracellular Ca2+ overload, suppressing microglial and astrocyte activation, and neuronal apoptosis. | Neurosci Bull. 2019 Jun;35(3):461-470 |
| C57BL/6 mice | DSS-induced colitis model | Oral gavage | 20 mg/kg/day | Once daily for two weeks | Gastrodin alleviates DSS-induced colitis by strengthening intestinal barrier and modulating gut microbiota | Foods. 2024 Aug 3;13(15):2460 |
| ICR mice | D-galactose-induced Alzheimer's disease model | Oral gavage | 3 mg/kg, 90 mg/kg, 210 mg/kg | Daily for 9 weeks | Gastrodin improved memory dysfunction in D-galactose-induced AD mice by regulating gut microbiota composition and inhibiting neuronal inflammation. | Front Pharmacol. 2022 Jun 2;13:814271 |
| Spontaneously hypertensive rats (SHRs) | Hypertensive renal injury model | Intragastric administration | 3.5 mg/kg/day | Once daily for 10 weeks | To investigate the protective effects of gastrodin against hypertensive renal injury and fibrosis. Results demonstrated gastrodin attenuated renal injury, reduced collagen deposition, and downregulated TGF-β1/Smad2/3 signaling pathway proteins. | Front Pharmacol. 2023 Jan 17;14:1082281. |
| Wistar rats | Type 2 diabetes model | Oral gavage | 30, 60, 90 mg/kg | Once daily for 6 weeks | After 6 weeks of treatment with gastrodin, fasting blood glucose levels, blood lipid metabolism, and insulin sensitivity index values were remarkably reduced. Gastrodin also alleviated liver toxicity caused by diabetes and relieved pathological damage to the pancreas in T2DM rats. | Front Pharmacol. 2021 Sep 16;12:710722. |
| Mice | 3xTg-AD mouse model | Intragastric | 50 mg/kg and 100 mg/kg | Once daily for 30 days | Gastrodin alleviates tau pathology by targeting FERMT2, reversing the reduction in brain viscoelasticity, and improving cognitive function and spatial recognition abilities. | CNS Neurosci Ther. 2025 Mar;31(3):e70283 |
| C57BL/6 mice | Pentylenetetrazole (PTZ)-induced seizure model | Intraperitoneal injection | 50 mg/kg, 100 mg/kg, 200 mg/kg | Single administration | Gastrodin attenuates PTZ-induced seizures by modulating MAPK-associated inflammatory responses, improving EEG patterns, reducing levels of pro-inflammatory cytokines IL-1β and TNF-α, increasing levels of anti-inflammatory cytokine IL-10, and inhibiting microglial activation. | Neurosci Bull. 2017 Jun;33(3):264-272 |
| C57 mice | Phenylephrine or angiotensin II-induced cardiac hypertrophy model | Intraperitoneal injection | 50 mg/kg/day | Once daily for 3 weeks | Gastrodin alleviated phenylephrine or angiotensin II-induced cardiac hypertrophy, as indicated by reduced heart size, decreased heart weight/body weight ratio, and reduced ANF and cTnT protein expression | Front Pharmacol. 2017 Apr 25;8:222. |
| C57BL/6 mice | Diabetic cardiomyopathy (DCM) model | Gavage | 50 mg/kg/day (low dose) or 100 mg/kg/day (high dose) | Once every two days for 12 weeks | To evaluate the effect of gastrodin on cardiac function and myocardial fibrosis in diabetic cardiomyopathy mice. Results showed that gastrodin significantly improved cardiac function, reduced myocardial fibrosis, and decreased the expression of KLK8 and PAR1. | Chin Med. 2024 Nov 22;19(1):164. |
| C57BL/6J mice | LPS-induced neuroinflammation and depressive-like behavior model | Intraperitoneal injection | 50, 100, 200 mg/kg | Single administration, behavioral tests performed at 6 and 24 hours post-administration | Gastrodin ameliorates LPS-induced neuroinflammation and depressive-like behaviors by downregulating miR-107-3p | Front Pharmacol. 2022 Dec 8;13:1044375 |
Clinical Trial:
| NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
| NCT03221894 | - | Recruiting | September 2017 | China ... More >> Dongzhimen Hospital Recruiting Beijing, China Contact: Jing Shi, M.D. 86-10-84013132 shijing87@hotmail.com Less << | |
| NCT00297245 | Cognitive Decline | Phase 4 | Unknown | - | China, Hubei ... More >> Department of Anesthesiology, Union Hospital Recruiting Wuhan, Hubei, China, 430022 Contact: Shihai Zhang, M.D., Ph.D. 862-785-726-834 zhangshh@public.wh.hb.cn Principal Investigator: Shihai Zhang, M.D., Ph.D. Less << |
| NCT02156024 | Masked Hypertension | Phase 4 | Unknown | - | China, Shanghai ... More >> Ruijin Hospital Recruiting Shanghai, Shanghai, China, 200025 Contact: Yan Li, doctor 021-64370045 ext 663228 liyanshcn@yahoo.com Principal Investigator: Yan Li, docter Less << |
| Bio Calculators | ||||
| Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
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1 mM 5 mM 10 mM |
3.49mL 0.70mL 0.35mL |
17.47mL 3.49mL 1.75mL |
34.93mL 6.99mL 3.49mL |
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| Dissolving Methods |
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:
in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day; The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
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Tags: Gastrodin | Gastrodine | Gastrodine | anti-inflammatory agent | neuroprotective | oxidative stress reduction | chronic inflammation | neurodegenerative diseases | arthritis | natural anti-inflammatory | orchid | 62499-27-8
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