Gastrodin

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Cat Number

PIPE-0758

CAS Number

62499-27-8

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CAS Number

62499-27-8

EINECS

683-202-7

Storage

2-8℃

Synonyms

4-(β-D-Glucopyranosyloxy)benzyl alcohol; p-(Hydroxymethyl)phenyl β-D-glucopyranoside; (2R,3S,4S,5R,6S)-2-(hydroxymethyl)-6-[4-(hydroxymethyl)phenoxy]oxane-3,4,5-triol

Molecular Formula

C13H18O7

Molecular Weight

286.28

Smiles

C1=CC(=CC=C1CO)O[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O

Appearance

White to off-white solid

Melting Point

153-155 ℃

Boiling Point

563.2 ℃

General Description

Gastrodin is a phenolic glycoside, extracted from the medicinal orchid Gastrodia elata as its major active ingredient. Gastrodin is widely used as an important pharmaceutical intermediate as well as a nutraceutical ingredient. Gastrodin easily penetrates through the blood-brain barrier, therefore it is broadly used for manufacturing neurological drugs as well as nutritional supplements that support brain health.

Mechanism of Action

Gastrodin acts on the receptors of various neurotransmitters that either promote or inhibit neurotransmission. Gastrodin has shown to enhance the expression of GABA and suppresses GABA transaminase activity which results in a sedative effect on the CNS. It has also shown strong antioxidant activity and down-regulates pro-inflammatory cytokines like TNF-α and IL-1β. Gastrodin protects the mitochondrial membrane from oxidative damage and neurons from glutamate-mediated excitotoxicity on the intracellular level.

Application

Used as an active pharmaceutical ingredient in medications designed to treat migraines, dizziness, epilepsy and neurasthenia. Used as an active nutraceutical ingredient in brain health supplements aiming to improve memory and concentration as well as decrease mental fatigue.

Network pharmacology was combined with in vivo and in vitro studies to reveal the antihypertension mechanism of Gastrodin. Online databases PharmMapper, OMIM and GeneCards were screened in silico, yielding 151 common targets. After the PPI network was constructed, AKT1, TNF and MMP9 were identified as hub nodes and KEGG enrichment showed that the PI3K/AKT signaling pathway was repeatedly enriched. Experiments found that oral Gastrodin administration for ten consecutive weeks greatly reduced systolic blood pressure (SBP), diastolic blood pressure (DBP) and mean arterial pressure (MAP) in SHRs. Moreover, pulse-wave velocity and thickening of the abdominal aorta were relieved, but body weight was unchanged. Pathological changes of hypertension in vascular tissues were improved.
Gastrodin inhibited the proliferation of AngII-induced vascular smooth muscle cells in vitro, decreasing cell confluence, cell number and CCK-8 absorbance values. In addition, the expression of PCNA proteins was down-regulated by Gastrodinn in a dose-dependent manner. Western blot showed that Gastrodin reduced the protein level of phosphorylated PI3K (p-PI3K) and phosphorylated AKT (p-AKT) without changing the total protein levels.

Fig. 1 Gastrodin suppresses the PI3K/AKT pathway to exert antiproliferative effects. (Shen A.; et al. 2023)

References

Shen A.; et al. Based on network pharmacology, gastrodin attenuates hypertension-induced vascular smooth muscle cell proliferation and PI3K/AKT pathway activation. Scientific Reports, 2023, 13(1): 12140.

Mitochondria-directed Gastrodin nanoconstructs were designed for protection against gastric lesions induced by ethanol. Nanoparticles containing Gastrodin (Gas-NPs) were synthesized by enzymatic reaction and modified with (5-carboxypentyl)(triphenyl)phosphonium bromide (TPP) via an amide linkage to produce GT-NPs. The generated GT-NPs exhibited a spherical structure with a uniform size distribution and excellent loading efficiency.
In vitro studies showed GT-NPs were quickly internalized by human gastric epithelial GES-1 cells, localized in mitochondria, and had enhanced reactive-oxygen-species (ROS) scavenging capacity than gastrodin alone. The gastrodin release kinetics from GT-NPs showed a sustained release pattern in SGF. In a ethanol-induced gastric ulcer mouse model, GT-NPs administered orally decreased the gastric mucosal injury score and oxidative stress levels, inhibited inflammatory cell infiltration and apoptosis.

Fig. 2 Gastrodin-based nanocarrier system for gastric ulcers. (Li Y.; et al. 2025)

References

Li Y.; et al. Construction of Gastrodin Nanocarriers and Their Improving Effect on Gastric Ulcers. ACS Applied Materials & Interfaces, 2025, 17(49): 67112-67122.

Where does Gastrodin come from?

Dried radix gastrodiae, dried rhizome of orchid Gastrodia elata Blume.

How does Gastrodin work in the brain?

It can penetrate into the brain through the blood-brain barrier to regulate GABA levels, so it has sedative, analgesic and neuroprotective functions.

Is Gastrodin water-soluble?

Soluble in water and methanol.

Can Gastrodin help with migraines?

Clinically, gastrodin can help ease vascular headaches and migraines, and decrease the frequency and severity of these conditions.