Review Article

Neuropharmacological Potential of Gastrodia elata Blume and Its Components

Table 2

Pharmacological effects of GE and its components on neurodegeneration.

Target pathwayInducer(s)Extracts/componentsDose/route/regimenAnimals or cellsHistological and biochemical evaluationReferences

NeurotransmissionPTZEFME of GE rhizome500 mg/kg, p.o., for 10 daysSD ratsRecovery of brain GABA contents[30]

NeurotransmissionStroking of the backGastrodin60 mg/kg, p.o., for 1 weekMongolian gerbilsDecreased GABA-T immunoreactivity
Decreased SSADH, SSAR immunoreactivity
[57]

NeurotransmissionCocaine GE rhizome—methanol extract500 or 1000 mg/kg, p.o., 5 times every 12 h before cocaine treatmentC57BL/6J miceAttenuation of cocaine-induced seizure via , but not receptor activation[29]

NeurotransmissionPentobarbitalGE rhizome—ethanol extract25, 50, and 100 mg/kg, p.o., 1 h before pentobarbital injectionICR mice, primary culture of cerebellar granule cellsProlonged total sleep time
Reduced sleep latency
Increased GAD and receptor subtype expression
[58]

Neurotransmission and antioxidationTransient global ischemiaVanillin,
4-HBAL, and
4-HBA
40 mg/kg, s.c., 30 min before and 30 min, 3, 6, 9, and 24 h after ischemia
0.016, 0.08, 0.4, 2, and 10 μM, for 2 h
Mongolian gerbils, PC12 cellsDownregulated 8-OHdG immunoreactivity
Increased GABA-T in the early stage after ischemia
Antioxidant activity on lipid peroxidation
[38]

AntioxidationGlutamateGastrodin0.1, 1, and 10 μMPC12 cellsInhibited ROS production
Inhibited MDA, MMP, and SOD levels
Blocked glutamate-induced influx
Blocked CaMKII, ASK-1, and phosphorylation of MAPK
[59]

AntioxidationMPP+Gastrodin1, 5, and 25 μM, 4 h prior to MPP+ exposureSH-SY5Y cellsDecreased ROS production
Induced HO-1 expression through p38 MAPK/Nrf2 signaling pathway
[54]

AntioxidationMPP+GE rhizome—ethanol extract10, 100, and 200 μg/mL, 4 h prior to MPP+ exposureSH-SY5Y cellsInhibited ROS production
Inhibited Bax/Bcl-2 ratio, cleaved caspase-3, and PARP proteolysis
[53]

AntioxidationMPP+GE rhizome—ethanol extract Vanillyl alcohol10, 100, and 200 μg/mL
1, 10, and 100 μM
MN9D cellsInhibited ROS production
Inhibited Bax/Bcl-2 ratio, cleaved caspase-3, and PARP proteolysis
[55]

AntioxidationAβ (25–35)GE rhizome—aqueous extract20 μM, for 48 hPC12 cellsDecreased ROS production
Upregulated enzymatic activities of catalase, SOD, and glutathione peroxidase
[60]

AntioxidationMCAOGE rhizome—aqueous extract
4-HBA
500 mg/kg, i.p.
25 mg/kg, i.p., 3 days prior to MCAO
SD ratsIncreased levels of genes related to antioxidant system (protein disulfide isomerase and 1-Cys peroxiredoxin)[61]

Anti-inflammationCUSGastrodin50, 100, and 200 mg/kg, i.p., for 14 days
5, 10, 20, and 50 μg/mL
SD rats
Primary hippocampal cells
Upregulated neural stem cell proliferation
Reduced NF-κB and IL-1β
[62]

Anti-inflammationLPSGastrodin30, 40, and 60 μM, 1 h prior to LPS exposureBV-2 cellsDecreased levels of proinflammatory enzymes (iNOS, COX-2) and proinflammatory cytokines (TNF-α, IL-1β)
Reduced phosphorylation of ERK1/2, JNK, p38 MAPK, and CREB
[63]

Anti-inflammationRotenoneGastrodin0.2 g/kg, p.o.Wistar ratsSuppressed microglial activation
Reduced IL-1β expression
[64]

Anti-inflammationKAGE rhizome—ethanol extract0.5, 1 g/kg, p.o., 30 min prior to KA injectionSD ratsDecreased microglial activation (ED1)
Reduced nNOS activation
[65]

Anti-inflammation and antioxidationLPSGE rhizome—ethanol extract0.25, 0.5, and 1 μg/mL, for 24 hRAW264.7 cellsInhibited NO production
Reduced iNOS and COX-2 expression
[66]

Anti-inflammation and antioxidationLPSGE rhizome—ethanol extract
4-HBA
1, 10, and 100 μg/mL
50, 100, and 200 nM
BV-2 cellsInhibited JNK and NF-κB signaling pathways
Inhibited NO and iNOS
[18]

4-HBA: 4-hydroxybenzyl alcohol; 4-HBAL: 4-hydroxybenzaldehyde; 8-OHdG: 8-hydroxy-2′-deoxyguanosine; ASK-1: apoptosis signal-regulating kinase-1; CaMKII: Ca2+/calmodulin-dependent kinase II; COX-2: cyclooxygenase-2; CUS: chronic unpredictable stress; EFME: ether fraction of methanol extract; ERK: extracellular signal-regulated kinase; GABA-T: gamma aminobutyric acid transaminase; GAD: glutamate decarboxylase; GE: Gastrodia elata; GREE: Gastrodia elata rhizome ethanol extract; iNOS: inducible nitric oxide synthase; JNK: c-jun N-terminal kinases; KA: kainic acid; LPS: lipopolysaccharide; MAPK: mitogen-activated protein kinase; MCAO: middle cerebral artery occlusion; MDA: malondialdehyde; MMP: mitochondrial membrane potential; nNOS: neuronal nitric oxide synthase; NO: nitric oxide; PTZ: pentylenetetrazole; ROS: reactive oxygen species; SOD: superoxide dismutase; SSADH: succinic semialdehyde dehydrogenase; SSAR: succinic semialdehyde reductase.