Gastrodin

Other Names

(2R,3S,4S,5R,6S)-2-(hydroxymethyl)-6-[4-(hydroxymethyl)phenoxy]oxane-3,4,5-triol4-(Hydroxymethyl)phenyl beta-D-glucopyranoside4-(β-D-Glucopyranosyl)-benzyl alcohol4-(β-D-Glucopyranosyloxy)benzyl alcohol4-Hydroxybenzyl alcohol 4-O-β-D-glucopyranosideCheon-maCheonmaChi JianChiqianDing Feng CaoDu Yao ZhiGastrodia RhizomeGastrodia RootGastrodia TuberGastrodiae RhizomaGastrodin HemihydrateGastrodineMing Tian Map-Hydroxybenzyl alcohol glucosideRhizoma GastrodiaeRhizoma Gastrodiae extractShui Yang YuTall GastrodiaTian MaTianma

Synopsis

Gastrodin: A Comprehensive Reference

1. Identity

Chemical and Botanical Names

Gastrodin is a chemical compound which is the glucoside of gastrodigenin. Chemically known as 4-hydroxybenzyl alcohol β-D-glucopyranoside, it is a phenolic glycoside with good water solubility and bioavailability, making it a prominent subject in modern pharmacological studies. Its CAS registry number is 62499-27-8. The aglycone released upon hydrolysis — that is, the sugar-free moiety — is gastrodigenin, also known as p-hydroxybenzyl alcohol (HBA) or p-HBA. Gastrodin is sometimes written as 4-[β-D-glucopyranosyloxy]benzyl alcohol in the chemical literature.

Natural Sources

Gastrodin has been isolated from the rhizomes of two orchid species, Gastrodia elata and Galeola faberi. The overwhelmingly predominant commercial and pharmacological source is Gastrodia elata Blume. G. elata, commonly known as Tianma, is a saprophytic perennial herb belonging to the genus Gastrodia, family Orchidaceae. It is primarily found in eastern Asia, specifically in the mountainous areas of China, Korea, Japan, and India. In China, it grows mainly in Sichuan, Guizhou, Yunnan, and other provinces. It grows in wet places with a lot of humus, especially in humid mountainous areas at an altitude of 400–3,200 m above sea level, and depends on the fungus Armillaria mellea for nutrients.

G. elata (Orchidaceae) is native to mountainous areas of Asia and is a plant species used in traditional medicine for more than two thousand years. The species has been reported to have many biological activities, such as neuroprotective, antioxidant, and anti-inflammatory activity. After many years of extensive exploitation from the wild, the plant was added to lists of endangered species.

The Medicinal Part

Rhizoma Gastrodiae is the dried tuber of Gastrodia elata Blume of the orchid family, which is a perennial parasitic botanical drug. The medicinal part is its tubers. Previous studies mainly focused on the tubers and have shown that G. elata mainly contains gastrodin and other natural products with benzyl alcohol as the basic unit.

Regulatory and Pharmacopeial Status

The G. elata rhizome is a herb used in traditional Chinese medicine to treat headache, and it is standardized in the Chinese Pharmacopoeia by gastrodin and gastrodigenin content. In line with this traditional use, gastrodin and its acetyl derivative (acetagastrodin) are used in China as an over-the-counter drug to treat neurasthenia, headache, and migraine. It is available as a dietary supplement in other countries. There are nine preparations listed in the Pharmacopoeia of the People's Republic of China, namely, Tianma Pills, Tianma Headache Tablets, Tianma Gouteng Granules, Tianma Shouwu Tablets, Tianma Qufeng Patches, Tianma Xingnao Capsules, Bantian Ma Pills, Quan Tianma Capsules, and Strong Tianma Duzhong Pills.

Common Forms and Preparations

Gastrodin and its source herb are available in several forms across different markets:

Isolated gastrodin: Standardized oral capsules, tablets, and injectable solutions are used in China. The only marketed monomeric drugs are gastrodin and its derivative acetylgastrodin, while other products are formulations prepared from Gastrodia elata extracts combined with other botanical medicines.
Whole-herb preparations: Dried tuber (sliced or powdered) and water decoctions. Although EtOH or MeOH are common protocols used for extracting chemical components from plant material, in most cases herbal medicine is decocted with water, with the aqueous decoctions then applied to treat patients.
Dietary supplements (international markets): Capsules and powders standardized to a specified percentage of gastrodin.
Food and tonic products: A wide variety of G. elata health care products have been developed and sell well in China, such as Tianma health wine, Tianma health drinks, and Tianma candy.
Synthetic gastrodin: Gastrodin can be directly extracted from the original plant, but its direct extraction leads to low yield, high costs, and resource wastage. Moreover, the resources of wild G. elata Blume have become fewer and fewer due to overexploitation. Therefore, chemical synthesis and biotransformation methods have emerged in recent years.

2. Traditional and Historical Use

Earliest Records

Rhizoma Gastrodiae ("tian ma") is an important tonic herbal medicine derived from Gastrodia elata Blume (Orchidaceae) rhizomes. Its medicinal application for improving health conditions and treating neuralgic and nervous disorders can be traced back to the earliest Chinese pharmacopeia Shen Nong Ben Cao Jing. Rhizoma Gastrodiae was first recorded for treating primary headache in the famous compendium of Chinese medicines called Shen Nong's Herbal Classic in 25 AD to 220 AD.

Traditional Chinese Medicine (TCM) Framework

In TCM, the herb has sweet flavor and liver channel tropism and is neutral in nature. Traditional Chinese medicine believes that its main functions are to expel wind and relieve convulsion, calm the liver and suppress liver-yang, and expel wind evil and channel. In TCM terminology, it was specifically employed against patterns described as "liver wind stirring internally," associated with symptoms including dizziness, tremor, headache, spasm, and seizures.

It has been used to treat headaches, dizziness, stroke, epilepsy, amnesia, spasm, and other disorders since ancient times. Gastrodiae Rhizoma was commonly employed in ancient China due to its clear curative and non-toxic impact. It was blended with other drugs to create a variety of well-known, traditional medicinal prescriptions, which included Tianma Gouteng Yin (TGY), Banxia Baizhu Tianma Tang (BBTT), Tianma Xifeng Tang (TXT), and Tianma Zexie Tang (TZT).

The preparation "Tianma stewed pig brain" has an enriching essence and marrow effect, and is often used for headache, dizziness, easily angry temperament, palpitations, and insomnia insulted by liver fire. Influenced by the traditional Chinese culture and the medical system of TCM, application of G. elata as a therapeutic botanical drug is now popular in many Asian countries, especially in South Korea and Japan.

Modern Chinese Drug Status

Gastrodin, a main bioactive constituent of Rhizoma Gastrodiae, has been applied clinically to treat primary headache for more than 30 years in China due to its potential analgesic and anti-migraine mechanisms. Since identified in 1978, gastrodin has been extensively investigated on its pharmacological properties.

3. Key Constituents and Active Compounds

Phytochemical Profile of Gastrodia elata

Over 200 bioactive components and secondary plant metabolites have been isolated and identified from Gastrodia elata Blume (GEB), including gastrodin (GAS), gastrodigenin (p-hydroxybenzyl alcohol, HBA), GEB polysaccharides (PEG), vanillin, parishin, trace elements, amino acids, organic acids, and other compounds. Hundreds of compounds, including phenols, glycosides, polysaccharides, steroids, organic acids, and others, have been isolated and identified from this plant.

There are 23 chemical ingredients extracted from Gastrodia elata, including gastrodin, gastrodia glycosides, vanilla alcohol, vanilla aldehyde, beta steroid valley alcohol, p-hydroxybenzoic acid, carrot glycosides, and so on, among which the highest content single active ingredient is gastrodin. Parishin derivatives — parishin A, parishin B, parishin C, and parishin E — are also abundant phenolic glycosides that contribute to the extract's overall pharmacological profile.

The primary bioactive compounds in their neuropharmacological context include:

Gastrodin — the principal phenolic glycoside; antioxidant, anti-inflammatory, anti-apoptotic, and neuroprotective. Mechanisms include scavenging reactive oxygen species (ROS), inhibiting NF-κB/NLRP3 pathways, modulating BDNF/TrkB signaling, and enhancing GABAergic transmission.
p-Hydroxybenzyl alcohol (gastrodigenin / HBA) — the aglycone metabolite of gastrodin; it reduces glutamate excitotoxicity, suppresses TNF-α/IL-6, and inhibits mitochondrial apoptosis (increasing Bcl-2, decreasing Bax/caspase-3).
Vanillyl alcohol — a phenolic derivative that potentiates GABA_A receptors and attenuates oxidative stress.
β-Sitosterol — a phytosterol that modulates cholesterol metabolism and neuronal membrane stability, synergizing with other compounds to attenuate apoptosis and mitochondrial dysfunction.
Parishin compounds — phenylpropanoid glycosides co-occurring with gastrodin in the rhizome, contributing to the broad activity profile of the crude extract.

Gastrodin as a Quality Marker

Currently, gastrodin is recognized as one of the most crucial active monomers in Gastrodia elata Blume. Gastrodin is a phenolic glycoside of 4-hydroxybenzyl alcohol and is selected as one of the standard compounds for evaluating the quality of GEB.

4. Mechanisms of Action

GABAergic and Neurotransmitter Modulation

Imbalance between the activities of inhibitory neurotransmitters and excitatory neurotransmitters is considered to be the key mechanism associated with the abnormality of neural activities. Gamma-aminobutyric acid (GABA) is the major inhibitory neurotransmitter in the brain, and enhancement of the activity of GABA would be useful to treat epilepsy. Gastrodin was able to lower the Glu/GABA ratio, and the results indicated that gastrodin could significantly inhibit the release of cerebral amino acids, especially the excitatory amino acids, thus modulating the imbalance between excitatory and inhibitory amino acids.

Anti-Inflammatory Pathways

The mechanisms of actions of gastrodin in CNS diseases include modulating neurotransmitters, antioxidative and anti-inflammatory effects, suppressing microglial activation, regulating mitochondrial cascades, and up-regulating neurotrophins. Gastrodin may exert its neuroprotective effects in ischemic stroke by modulating the NF-κB, NLRP3, AKT/Nrf2 inflammatory and oxidative stress pathways and promoting neural regeneration by neural-related signaling pathways such as PDE9-cGMP-PKG pathways.

Antioxidant Activity and Nrf2 Pathway

Gastrodin induces up-regulation and nuclear translocation of Nrf2, and subsequently increases the expression of anti-oxidative genes, such as HO-1 and GCLM, in astrocytes. This activation of the Nrf2 (nuclear factor erythroid 2-related factor 2) pathway represents one of the central antioxidative mechanisms through which gastrodin limits cellular damage from reactive oxygen species.

Anti-Epileptic Mechanisms

Gastrodin (GAS) may exert its antiepileptic properties by inhibiting inflammatory and oxidant reactions via the MAPK and GABA pathway. Gastrodin alleviates seizure severity and neuronal excitotoxicities in the rat lithium-pilocarpine model of temporal lobe epilepsy via enhancing GABAergic transmission.

Cardiovascular and Antihypertensive Mechanisms

Studies have shown that GAS can effectively intervene in the renin-angiotensin-aldosterone system (RAAS) and its resulting myocardial remodeling, thus playing a role in the treatment of hypertension. Previous studies have revealed that gastrodin promoted the opening of ATP-sensitive potassium channels in vascular smooth muscles by activating protein kinase A, leading to vasodilation and blood pressure decline. Gastrodin intervenes with the renin-angiotensin-aldosterone system (RAAS) and PPARγ effectively, indicating its antihypertensive mechanism.

Neuroprotective Mechanisms in Ischemia

GAS can prevent and treat cerebral ischemia/reperfusion-induced neurological injury by regulating a variety of molecular signals, exerting pharmacological effects such as anti-oxidative stress, inhibition of inflammatory response, inhibition of cell death, modulation of neurotransmitters, alleviation of neurotoxicity, promotion of neural repair, protection of the blood-brain barrier, and alleviation of cerebral edema.

Neurotrophic Factor Regulation

Gastrodin can play a neuroprotective role via anti-inflammation, antioxidation, and neurotrophic factor regulation. At the same time, gastrodin can treat or improve neurodegenerative diseases, emotional disorders, and cognitive impairment to some extent.

5. Pharmacokinetics

Absorption and Distribution

Gastrodin is rapidly absorbed and widely distributed in the body and can also penetrate the blood–brain barrier. To the best of published knowledge, the pharmacokinetic analysis of gastrodin in humans was considered in one clinical study, which included eighteen male subjects to whom a gastrodin capsule was orally administered at a dosage of 200 mg. According to the obtained results, gastrodin was rapidly absorbed into blood (t_1/2Ka = 0.18 h) and reached a peak concentration at 0.81 h. The gastrodin in blood reached a peak concentration of 24.1 µg/ml, whereas HBA attained a peak concentration of approximately 220-fold lower (0.109 µg/ml) at 15 min post-dose. The results of this pharmacokinetic study also suggested that the brain exposure to gastrodin far exceeds the brain exposure to HBA (more than 8.7-fold at 15 min after administration).

Blood-Brain Barrier Penetration

After being absorbed into the blood, gastrodin is widely distributed in various tissues and can enter the brain through the blood-brain barrier. However, the extensive application of GAS and its molecular mechanism of action remain significant challenges due to its favorable hydrophilicity, low blood-brain barrier (BBB) permeability, and poor bioavailability. Studies in ischemic models have shown that brain accumulation of these compounds was significantly increased in ischemic models, attributable to compromised blood-brain barrier integrity.

Metabolism and Excretion

The majority of GAS is excreted in its native form via urine, and a small proportion of GAS is reported to be excreted via bile; HBA is mainly excreted via the hepatobiliary system. Gastrodin is not rapidly eliminated from the body; it remains detectable in rat plasma for up to 8 h after oral administration.

Intranasal Route

Intranasal gastrodin administration (50 mg/kg) in animal studies provided an AUC in the cerebrospinal fluid comparable to that obtained by intravenous administration. Additionally, cerebrospinal fluid concentrations of gastrodin 60 min following intranasal administration were always higher than those achieved after intravenous administration, which suggested a direct nose-to-brain pathway to transport gastrodin from the nasal cavity to the brain.

6. Scientific Evidence by Area of Use

6.1 Headache and Migraine

Gastrodin has been applied clinically to treat primary headache for more than 30 years in China due to its potential analgesic and anti-migraine mechanisms. However, clinical evidence supporting its routine use in medication-overuse headache (MOH) is insufficient.

A 2022 meta-analysis published in Frontiers in Neurology (PMC9454298) examined gastrodin's effectiveness for migraine through systematically integrated clinical trials. The treatment group used gastrodin combined with conventional treatment for migraine; the control group used conventional treatment for migraine alone (calcium ion antagonists, calcium channel blockers, antiepileptic drugs, vasodilators, and pain killers). Clinical efficacy, pain score, frequency of headache, duration of headache, average blood flow velocity of cerebral artery, and adverse reactions were assessed. Acute toxicity tests showed that gastrodin and its metabolites were safe, and gastrodin preparations have been widely used in the clinical treatment of migraine. However, there is still insufficient evidence to evaluate the outcome of gastrodin for the treatment of migraine — indicating that while the clinical trial data trend positively, the evidence base is not yet at the level of established therapies.

A multicenter randomized double-blind placebo-controlled trial (the EASTERN study) is specifically targeting medication-overuse headache. A multicenter, randomized, double-blind, parallel, placebo-controlled trial design was registered. A target sample size of 186 patients fulfilling ICHD-3 criteria for MOH were to be recruited and randomly assigned to either gastrodin or placebo at a 1:1 ratio. Enrolled patients are assessed every 4 weeks during a 12-week double-blind phase and followed up at week 24. The primary endpoint is mean change in monthly headache day frequency, with secondary endpoints including proportion of remitted MOH, headache pain intensity change, HIT-6 score, 50% responder rate, and SF-36 score.

Evidence strength: Preliminary to moderate. Existing Chinese clinical trials are positive but limited by methodological heterogeneity. Rigorous multinational RCT data are lacking. The EASTERN trial is ongoing and its completion will be important for definitive conclusions.

6.2 Epilepsy and Seizure Disorders

It was demonstrated that pretreatment with gastrodin could significantly prolong seizure latency as well as reduce seizure severity, shorten seizure duration, accelerate recovery, and decrease mortality rate in preclinical models. The mechanisms underlying the anticonvulsant effect of gastrodin were also explored in subsequent work. Gastrodin may exert its antiepileptic properties by inhibiting inflammatory and oxidant reactions via the MAPK and GABA pathway. However, future in vitro and clinical trials are needed to further investigate the specific effects of GAS on other aspects of GABA metabolism.

Evidence strength: Predominantly preclinical (animal models). Mechanistic data are substantive; however, robust human clinical trial evidence in epilepsy is not well-established in the Western literature. The Chinese literature reports some clinical use, but controlled trials meeting modern standards are limited.

6.3 Neurodegenerative Diseases

Parkinson's Disease

Parkinson's disease (PD) is a neurodegenerative disorder characterized by progressive loss of dopaminergic neurons in the pars compacta of the substantia nigra, which leads to clinical symptoms of rigidity, resting tremor, and bradykinesia. The MPTP toxin model is a known mitochondrial complex I inhibitor that selectively damages dopaminergic neurons and leads to depletion of dopamine. Antioxidant (ROS inhibition, SOD activity) and antiapoptotic activities (Bax/Bcl-2 mRNA, caspase-3, and cleaved PARP) were characterized in SH-SY5Y cells stressed with MPP+. MPTP-intoxicated C57BL/6 mice underwent behavioral, antioxidant, histochemical, and histobiological evaluations. The results reveal gastrodin as a potential candidate with neuroprotective and antiapoptotic activities and strongly suggest gastrodin as a clinical candidate for PD.

Evidence strength: Preclinical (cell culture and animal models). No dedicated high-quality randomized controlled trials in PD patients have been established in the Western peer-reviewed literature. Promising mechanistic rationale exists.

Alzheimer's Disease

Studies on the pharmacological effects of gastrodin on the CNS indicate that it may exert anti-neurodegenerative, cerebrovascular protective, and ameliorative effects on diabetic encephalopathy, perioperative neurocognitive dysfunction, epilepsy, Tourette's syndrome, depression and anxiety, and sleep disorders through various mechanisms. In Alzheimer's disease models, gastrodin's effects on β-amyloid and tau pathology have been studied using bioinformatics and machine learning approaches, with one study demonstrating that SNAP25 can be considered a key aging-related gene in AD, and that gastrodin could treat AD by targeting specific genes and signaling pathways, providing insights for future clinical application.

Evidence strength: Predominantly preclinical and computational/bioinformatic. Clinical human RCT evidence in AD is absent from the current literature reviewed.

6.4 Cerebrovascular Disease and Ischemic Stroke

In in vivo studies, gastrodin treatment, whether administered before or after the operation, was reported to improve neurological functions, decrease the infarct volume and edema volume in cerebral ischemia models. In a Sprague-Dawley rat model of stroke (transient middle cerebral artery occlusion), intraperitoneal administration of GAS (40 mg/kg) after MCAO reduced mean infarct volume to 30.1 ± 5.9% of that of MCAO controls, and this neuroprotective effect was accompanied by neurological function recoveries. GAS can prevent and treat cerebral ischemia/reperfusion-induced neurological injury by regulating a variety of molecular signals. Gastrodin has significant value in the treatment of CIRI and there is extensive evidence to support its use in CIRI.

Evidence strength: Strong preclinical evidence. Clinical studies on these preparations primarily focus on cardiovascular and cerebrovascular diseases and neuroprotection. Most studies adopt a placebo-controlled design, while a few use positive drug controls to observe enhanced efficacy. Clinical evidence in humans exists within the Chinese medical system but has not been independently replicated or validated in large international RCTs.

6.5 Vascular Dementia and Cognitive Function

Gastrodin has been used in the treatment of migraine, epilepsy, Parkinson's disease, dementia, and depression in recent years. It can improve cognitive function and related neuropsychiatric symptoms through various effects and is considered a promising treatment for dementia. Although there is still a lack of evidence-based explorations, published reviews have covered the mechanism and methods of gastrodin in the treatment of vascular dementia.

A randomized controlled trial cited in the literature evaluated gastrodin for cognitive decline following cardiac surgery with cardiopulmonary bypass (Zhang et al.), representing one of the more rigorous human studies available. Gastrodin has been studied in Chinese clinical trials for headache, dizziness, and cognitive function in vascular dementia with positive outcomes.

Evidence strength: Preliminary. Results from Chinese clinical trials are encouraging, but the body of evidence is not yet sufficient by international standards for formal clinical recommendations.

6.6 Hypertension and Cardiovascular Disease

A randomized controlled trial showed that daily intravenous injection of 1,000 mg gastrodin for 4 weeks significantly decreased systolic and diastolic blood pressures and reduced plasma endothelin (ET) levels but increased nitric oxide (NO) levels in older adults with refractory hypertension.

Gastrodin can improve cardiac hypertrophy in mice with transverse aortic constriction and reduce cardiomyocyte hypertrophy induced by both transverse aortic constriction and phenylephrine. Gastrodin also inhibited cell apoptosis induced by homocysteine, interleukin-1 beta (IL-1β), high glucose, and oxidative stress through various targets.

In spontaneously hypertensive rat (SHR) studies, researchers have discovered that Rhizoma Gastrodiae acidic polysaccharides and crude polysaccharides can reduce hypertension. These metabolites simultaneously increase high-density lipoprotein cholesterol (HDL-C) levels while lowering total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C) levels. They also inhibit de novo synthesis of total cholesterol and low-density lipoproteins in rats, thereby improving hemorheology through multiple pathways and reducing the incidence of cardiovascular diseases and atherosclerosis.

Evidence strength: Preclinical data are substantial. The single human RCT cited used intravenous gastrodin at a high dose (1,000 mg/day) in a specific clinical population (refractory hypertension); this is not directly applicable to supplemental use. Broader controlled clinical trial evidence in cardiovascular disease is limited.

6.7 Depression, Anxiety, and Mood Disorders

In preclinical pharmacological studies, Rhizoma Gastrodiae was shown to have various therapeutic effects including neuroprotective, anti-inflammatory, antioxidative, antiepileptic, anticonvulsive, antipsychotic, anxiolytic, antidepressant, and memory-improving effects. Gastrodin has great potential to be used as an adjunctive strategy to relieve the clinical symptoms of depression. Gastrodin is a glycoside of 4-HBA, and both have been investigated to have similar biological activities such as anti-oxidant, anti-inflammatory, anti-depressant, neuroprotective, and memory-enhancing effects.

Evidence strength: Predominantly preclinical and animal model-based. Some small Chinese clinical studies report positive findings in depression and anxiety when gastrodin preparations are used in combination regimens, but independent high-quality RCT evidence in affective disorders is lacking.

6.8 Sleep Disorders

Gastrodin has significant pharmacological effects on the central nervous system, such as sedation and improvement of sleep. It can also improve epilepsy, neurodegenerative diseases, emotional disorders and cognitive impairment to a certain extent. Studies on the pharmacological effects of gastrodin on the CNS indicate that it may exert ameliorative effects on sleep disorders through various mechanisms.

Evidence strength: Preliminary; largely based on mechanistic/preclinical data. Clinical trial evidence specific to primary sleep disorders is not robustly established in the Western peer-reviewed literature.

7. Dosage Forms and Reported Dosages

The following dosages are reported in published scientific sources and are not recommendations:

Oral capsule (human pharmacokinetic study): A single oral dose of 200 mg was used in the only human pharmacokinetic study identified, which enrolled eighteen male subjects.
Intravenous injection (clinical hypertension study): Daily intravenous injection of 1,000 mg gastrodin for 4 weeks was used in older adults with refractory hypertension.
Preclinical intraperitoneal (stroke model): Intraperitoneal administration of GAS at 40 mg/kg after MCAO was reported in a rat stroke model.
Multicenter headache trial: The treatment group used gastrodin with no specified dosage limitation in the migraine meta-analysis.
Chinese OTC drug use: As noted, gastrodin and acetagastrodin are used as OTC drugs in China, with dosages specified in Chinese national formulary standards, which vary by preparation and indication.

The dosage of gastrodin is always high in clinical use as well as in preclinical models, as gastrodin has been proven to be a non-toxic compound in acute and subacute toxicity studies.

8. Safety Considerations

Animal Toxicology

Acute toxicity experiments suggested that both gastrodin and 4-HBA are safe on oral administration at the dosage up to 5,000 mg/kg body weight in mice, which did not cause any mortality or apparent toxic effects. In subacute toxicity experiments, when gastrodin or 4-HBA was orally administered at the dosage of 75 mg/kg bw/day for 14 days in dogs, or at the dosage of 375 mg/kg bw/day for 60 days in mice, no significant adverse effects were found.

Reported Adverse Reactions in Humans

Although toxicity studies in animals revealed that gastrodin is relatively safe to use, cases of clinical adverse drug reaction (ADR) or event (ADE) induced by gastrodin were reported occasionally. In a retrospective study including 315 cases with ADR or ADE induced by gastrodin in Chongqing province of China from January 2008 to June 2014, the ADR or ADE mainly occurred in the gastrointestinal system, skin, and nervous system. The most frequently reported symptoms included rash, pruritus, dizziness, dry mouth, nausea, palpitation, vomiting, and headache.

Limitations of Current Safety Data

There is still a need for carrying out more detailed toxicity studies of gastrodin according to International Council for Harmonization (ICH) safety guidelines. Knowledge regarding the toxicology of water extract of G. elata is limited. Gastrodin has been determined to be safe for use in toxicity studies in animals, and occasionally reported adverse drug reactions or events (ADE) have been observed in clinical practice.

Gastrointestinal and Dermatological Reactions

Based on the retrospective ADR surveillance data from the Chinese pharmacovigilance system, cases of clinical adverse drug reaction or event induced by gastrodin were still reported occasionally, which mainly occurred in skin, gastrointestinal, and nervous systems. These are generally described as mild and reversible in the available reports.

Food and Traditional Safety Classification

Based on its history and traditional use, G. elata is recognised as safe and is used as an ingredient in Chinese dietary therapy or as a functional food.

Plant Availability and Quality Concerns

After many years of extensive exploitation from the wild, the plant was added to lists of endangered species. Since its desired cultivation is considered difficult, innovative cultivation methods that can reduce costs and avoid contamination with pathogens and chemicals are urgently needed on large scale. Variability in gastrodin content between samples grown in different conditions and collected in different seasons has been documented analytically, with implications for the consistency of preparations.

9. Regulatory and Research Landscape

The only marketed monomeric drugs are gastrodin and its derivative acetylgastrodin, while other products are formulations prepared from Gastrodia elata extracts combined with other botanical medicines. As of mid-2025, a search of China's medical information platform identified 163 registered preparations and related formulations.

Gastrodin is a promising natural small molecule. In vitro and in vivo analyses have shown the wide range of physiological activities of gastrodin in the CNS, and it may be useful in the treatment of sleep disorders, epilepsy, AD, and related conditions. Further understanding of the bioactivity and mechanisms of gastrodin in the CNS will be beneficial to its future clinical application and formulation development.

Outside of China, gastrodin is marketed as a dietary supplement in the United States, Europe, and other regions, where it is not approved as a drug and thus not subject to the same regulatory controls as the Chinese OTC monographs. No European Medicines Agency (EMA), European Food Safety Authority (EFSA), or U.S. FDA-approved drug indication for gastrodin exists as of the time of writing.

References

Health Conditions

Health conditions that Gastrodin may help support.

Parkinson's DiseaseScientific
Gastrodin, the primary bioactive glycoside of Gastrodia elata (a Chinese medicinal herb used in traditional medicine for neurological conditions), has shown neuroprotective effects in multiple PD animal models. It protects dopaminergic neurons, reduces neuroinflammation, and maintains dopamine homeostasis. Research is primarily preclinical with growing mechanistic clinical interest.
Vertigo & BalanceScientific
Gastrodin is the primary bioactive phenolic glycoside of Gastrodia elata (Tianma), used in Chinese medicine for vertigo for over 1,000 years. It has demonstrated vestibular-modulating, neuroprotective, and anti-vertigo pharmacological properties. Retrospective cohort data from China confirms positive clinical effects for dizziness and vertigo, and a comparative animal study shows vestibular improvement comparable to betahistine.

Body Systems

Body systems that Gastrodin may help support.

No body systems available.