Objective To study the therapeutic effects of Ginsenoside Rg-1 and Gastrodine on rats model of Alzheimer’s disease(AD). Methods Aggregated β-Amyloid peptide (25-35) was injected into the lateral ventricle of rats to...Objective To study the therapeutic effects of Ginsenoside Rg-1 and Gastrodine on rats model of Alzheimer’s disease(AD). Methods Aggregated β-Amyloid peptide (25-35) was injected into the lateral ventricle of rats to establish AD models. Ginsenoside Rg-1, Gastrodine and Ginsenoside Rg-1+Gastrodine were intraperitoneally injected into rats of each test group(Ginsenoside Rg-1∶10mg/kg·day; Gastrodine 100mg/kg·day) for 4 weeks, the rats of control group received equal volume of saline. Passive avoidance task and Morris maze test were done to assess the ability of learning and memory. The content of superoxide dismutase (SOD), malondiadehyde (MDA), total-antioxidative capability (T-AOC), Choline acetyltransferase (ChAT) and acetylcholinesterase (AchE) in brain tissue were measured. Results Ginsenoside Rg-1 and Gastrodine significantly improved learning and memory deficits in the rats with AD induced by β-Amyloid peptide (25-35) (P<0.05). Ginsenoside Rg-1+Gastrodine group were better than Ginsenoside Rg-1 group and Gastrodine group (P<0.05). Ginsenoside Rg-1 reduced the increase of SOD, MDA, but inhibited the decrease of T-AOC, AchE and ChAT; Gastrodine reduced the increase of SOD, MDA, while inhibited the decrease of T-AOC. Gastrodine could also prevent the activity of ChAT and AchE decline in AD rats. Conclusion Both Ginsenoside Rg-1 and Gastrodine have therapeutic effects on rats with AD; Ginsenoside Rg-1 and Gastrodine injection at the same time were better than only using one of them. Their mechanisms might different. Ginsenoside Rg-1 can not only inhibit peroxidation but also increase the activity of AchE and ChAT in brain tissue, while Gastrodine can inhibit peroxidation only, but it can’t prevent the decline of ChAT and AchE activity in AD rats.展开更多
Gastrodia elata,a traditional Chinese medicine belonging to the Orchidaceae family,contains several major components such as gastrodin,polysaccharides of Gastrodia elata,and parishin.The pharmacological studies conduc...Gastrodia elata,a traditional Chinese medicine belonging to the Orchidaceae family,contains several major components such as gastrodin,polysaccharides of Gastrodia elata,and parishin.The pharmacological studies conducted on Gastrodia elata have revealed a variety of therapeutic properties,including antihypertensive,hypolipidemic,analgesic,and sedative-hypnotic properties.Thus,in this paper,we summarized the pharmacological effects of Gastrodia elata’s major components,namely gastrodin,polysaccharides of Gastrodia elata,parishin,and different types of Gastrodia elata extracts,on cardiovascular diseases such as atherosclerosis,hypertension,hyperglycemia,myocardial ischemia,myocardial hypoxia,myocarditis,and heart failure.Additionally,we conclude the mechanisms through which these active ingredients exert their therapeutic effects,including antioxidants,anti-inflammatory,and nitric oxide regulation.We provide insights into the therapeutic potential of Gastrodia elata with a detailed review of its pharmacological effects and molecular targets in cardiovascular disease protection and therapy,and can better understand the effect of traditional medicines in cardiovascular disease.展开更多
Objective:To observe the effects of perfusion of the gastrodin in abdominal aorta for alleviating the spinal cord ischemia reperfusion injury(SCIRI).Methods:A total of 36 New Zealand white rabbits were divided randoml...Objective:To observe the effects of perfusion of the gastrodin in abdominal aorta for alleviating the spinal cord ischemia reperfusion injury(SCIRI).Methods:A total of 36 New Zealand white rabbits were divided randomly into sham-operated group(group S),control group(group C) and gastrodin group(group G),12 rabbits for each group.Aorta abdominalis infrarenalis blocking method was applied to establish the SCIRI model.The changes of motor evoked potentials(MEPs) before the ischemia and on 30 min,60 min,6 h,12 h and 24 h of reperfusion of the gastrodin were respectively recorded,and the neurologic function score before the ischemia,on the 6 h,12 h and 24 h of the reperfusion of the gastrodin were assessed.And the changes of the concentration of serum neuron specific enolase(NSE),interleukin(IL)-l β and IL-8 were measured before the ischemia,after 45 min of ischemia,and on 30 min,60 min,6 h,12 h and 24 h of reperfusion of gastrodin.Then the levels of spinal cord nerve cells mitochondrial superoxide dismutase(SOD),reactive oxygen species(ROS),glutathione peroxidase(GSH-PX),malondialdehyde(MDA),total antioxidant capacity(T-AOC) and mitochondrial swelling degree(MSD) were tested and the histopathologic changes in spinal cord tissues were observed.Results:The levels of the NSE,IL-lfter the ischemβ,IL-8,ROS,MDA and MSD of group C were all significantly elevated aia(P<0.01);the levels of the spinal nerve cell mitochondria SOD,GSH-PX and T-AOC were all significantly reduced(P<0.01),MEPs and spinal cord tissue pathology were damaged significantly(P<0.01).The rate of motor neuron abnormalities and the damages of spinal cord tissue pathology of group G were significantly milder than those of group C(P<0.01);the levels of NSE,IL-lROS,MDA and MSD were significantly lower than those of group C(P< 0.01),but tβ,IL-8,he levels of SOD,GSH-PX and T-AOC were all significantly higher than those of group C(P<0.01),and the recovery of neurologic function score during the reperfusion of gastrodin was significantly faster than group C(P<0.01).Conclusions:Perfusion of the gastrodin in abdominal aorta can alleviate the spinal cord ischemiare perfusion injury by promoting the mitochondrial antioxidant capacity and inhibiting the inflammatory reaction.展开更多
AIM:To investigate the neuroprotective effect of gastrodin on retinal ganglion cells(RGCs) in an acute ocular hypertension(AOH) rat model and to identify its possible mechanism.METHODS:AOH rat model was performed in a...AIM:To investigate the neuroprotective effect of gastrodin on retinal ganglion cells(RGCs) in an acute ocular hypertension(AOH) rat model and to identify its possible mechanism.METHODS:AOH rat model was performed in a randomly selected eye by anterior chamber perfusion and either received an intraperitoneal injection with various concentrations of gastrodin or normal saline.After 2 wk,the rats were sacrificed.Fluoro Gold was used to label survival RGCs.Immunostaining with anti-Iba1 in the retinal flat mounts to calculate the microglia density in the ganglion cell layer(GCL).Changes in microglial cytokines,tumour necrosis factor-alpha(TNF-α) and inducible NO synthase(i NOS) were examined with Western blot and reverse transcriptionquantitative polymerase chain reaction.Expression levels of total and phosphorylated p38 mitogen activated protein kinase(MAPK) were determined by Western blot.RESULTS:Results showed that AOH induced significant loss of RGCs and severe microglia activation in the GCL.Besides,AOH increased the phosphorylation of p38 MAPK and promoted the release of microglial cytokines in the retinas.Intraperitoneal injection with dose-dependent gastrodin significantly reduced the loss of RGCs and inhibited retinal microglia activation,accompanied with the decreased expression levels of microglial cytokines and p38 MAPK phosphorylation.CONCLUSION:Gastrodin exerts a neuroprotective effect on RGCs in an acute glaucoma animal model viainhibiting microglia activation and microglial-mediated neuroinflammation.The finding demonstrates the potential application of gastrodin in the neuroprotective therapy of acute glaucoma and other retinal neurodegenerative diseases characterized by microglia activation and RGCs death.展开更多
Cardiovascular diseases cause significant morbidity and mortality worldwide,incurring a major public health burden.Gastrodia elata Blume is a traditional Chinese herbal medicine that has been widely used to treat cent...Cardiovascular diseases cause significant morbidity and mortality worldwide,incurring a major public health burden.Gastrodia elata Blume is a traditional Chinese herbal medicine that has been widely used to treat central nervous system and cardiovascular diseases.Gastrodin,as the major active component in Gastrodia elata Blume,can confer protection against cardiovascular diseases.In this review,we summarize the anti-inflammatory actions,anti-cardiac hypertrophy,anti-hypertension,anti-atherosclerosis,and angiogenic effects of gastrodin,as well as its protective effects on vascular cells and against myocardial ischemia-reperfusion injury.The medical potential of gastrodin in diabetes-related cardiovascular diseases is also discussed.展开更多
Nine new gastrodin derivatives,including seven p-hydroxybenzyl-modified gastrodin ethers(1-7),6′-O-acetylgastrodin(8),and 4-[α-d-glucopyranosyl-(1→6)-β-d-glucopyranosyloxy]benzyl alcohol(9),together with seven kno...Nine new gastrodin derivatives,including seven p-hydroxybenzyl-modified gastrodin ethers(1-7),6′-O-acetylgastrodin(8),and 4-[α-d-glucopyranosyl-(1→6)-β-d-glucopyranosyloxy]benzyl alcohol(9),together with seven known derivatives,were isolated from an aqueous extract of Gastrodia elata(“tian ma”)rhizomes.Their structures were determined by spectroscopic and chemical methods as well as single crystal X-ray diffraction.Compounds 1-4,7,10,and 11 were also isolated from a reaction mixture by refluxing gastrodin and p-hydroxybenzyl alcohol in H2O.As both gastrodin and p-hydroxybenzyl alcohol exist in the plant,the reaction results provide evidence for the production and increase/decrease of potential effective/toxic components when“tian ma”is decocted solely or together with ingredients in Chinese traditional medicine formulations,though the isolates were inactive in the preliminarily cell-based assays at concentrations of 10μM.Moreover,using ultra-performance liquid chromatography high-resolution electrospray ionization mass spectrometry(UPLC-HRESIMS),4,7,10,and 11,as well as component variations,were detectable in the freshly prepared extracts of different types of samples,including the freeze-dried fresh G.elata rhizomes.展开更多
Objective Effects of Remifentanil combined with Gastrodin injection on cerebral oxygen metabolism and early postoperative cognitive function in patients undergoing laparoscopic surgery for cervical cancer.Methods 107 ...Objective Effects of Remifentanil combined with Gastrodin injection on cerebral oxygen metabolism and early postoperative cognitive function in patients undergoing laparoscopic surgery for cervical cancer.Methods 107 cases of laparoscopic cervical carcinoma were randomly divided into observation group(54 cases)and control group(53 cases),the control group received anesthesia induction therapy based on Remifentanil,the observation group was given intravenous Gastrodin injection to 120h after operation on the basis of control group.the brain oxygen metabolism and brain injury related indexes 6h,12h,72h and 120h after operation were observed,and the preoperative cognitive function and postoperative cognitive function of two groups after 6h,1d,3d and 5d were evaluated by using Mini-Mental State Examination(MMSE)test method.Results Compared to the preoperative data,the oxygen saturation of the internal jugular vein(SjvO22)and cerebral oxygen saturation(rSO2)of two groups after 6h of operation was significantly decreased(p<0.05),and the indexes all back to normal after 120h,and observation group’s indexes were higher than that in control group(P<0.05);and the Cerebral arterial-venous oxygen content difference(Da-jvO2)and Cerebral Oxygen extraction rate(CERO2)of two groups after 6h of operation was significantly increased(P<0.05),and the indexes all back to normal after 120h and observation group’s indexes were lower than that in control group(P<0.05);serum neuron specific enolase(NSE)and S100B protein level of two groups after 6h of operation was significantly increased and back to normal after 120h,and observation group’s indexes were lower than that in control group(P<0.05);The MMSE score of 6h,12h,72h and 120h were higher in the observation group than in the control group,and the incidence of postoperative cognitive dysfunction(POCD)was lower than that in the control group(P-<0.05).Conclusion In the anesthesia induction program based on Remifentanil,the use of Gastrodin injection can reduce the incidence of cognitive dysfunction after laparoscopic surgery for cervical cancer,and its mechanism may be related to the improvement of brain metabolism and the reduction of hypoxia injury in neurons of cranial nerves.展开更多
Objective:To explore^1H nuclear magnetic resonance-based metabolomics on sex-specific metabolic changes of gastrodin intervention in rats.Methods:In this research,~1H NMR-based metabolomics was used for the first time...Objective:To explore^1H nuclear magnetic resonance-based metabolomics on sex-specific metabolic changes of gastrodin intervention in rats.Methods:In this research,~1H NMR-based metabolomics was used for the first time to investigate metabolic changes following chronic intervention with gastrodin in rats.Results:24 endogenous metabolites were identified.Body weight.daily diet and the total volume of urine in in each day of each rat were measured synchronously.Modifications in 12 metabolites were observsd following gastrodin intervention,indicating gastrodin-induced alterations in carbohydrate and energy metabolism.Interestingly,these metabolic changes were not totally identical in female and male rats.Some metabolic changes arising from gastrodin intervention showed sexual dimorphism including LDL/VLDL and lactate which were on the decrease in the female but on the increase in the male,together with arginine/ornithine,creatine,and glycerol which were on the increase in the female but on the decrease in the male.While the decrease in pyruvate,succinate and glutamate was only shown in the male and the increase in valine,α-ketoglutarate and glucose was only in the female.Conclusions:This resesrch shows the sex-specific metabolic response to GAS intervention,weather GAS is a healthy dietary supplement for the male merits further展开更多
[Objectives]The research aimed to establish a high performance liquid chromatography method for the content determination of gastrodin in Jingtianshenma Tablets.[Methods]A phenomenex Luna C18(250 mm×4.6 mm,5μm)c...[Objectives]The research aimed to establish a high performance liquid chromatography method for the content determination of gastrodin in Jingtianshenma Tablets.[Methods]A phenomenex Luna C18(250 mm×4.6 mm,5μm)column was used;the mobile phase was acetonitrile-0.05%phosphoric acid solution(3∶97);the detection wavelength was 220 nm,and the column temperature was set at 25℃.[Results]Gastrodin showed a good linear relationship in the range of 0.0984-0.5904μg with the peak area,and regression equation was Y=2000000X-51999(r=0.9999).The limits of detection and quantification for gastrodin were 2.50 and 4.20 ng respectively,and the average recovery rate was 95.95%.[Conclusions]This method is sensitive,accurate and reproducible,with good linearity,and it is suitable for the content determination of gastrodin in health food Jingtianshenma Tablets.展开更多
Acrylamide(AA)is ubiquitous in packaging materials,paints,cosmetics,food and drinking water.However,AA has obvious neurotoxicity,reproductive toxicity and carcinogenicity,which seriously endangers human health.As one ...Acrylamide(AA)is ubiquitous in packaging materials,paints,cosmetics,food and drinking water.However,AA has obvious neurotoxicity,reproductive toxicity and carcinogenicity,which seriously endangers human health.As one of precious traditional Chinese medicines,Gastrodia elata Bl.has been mainly used to lower blood pressure and resist myocardial ischemia.However,the antioxidant activity of Gastrodia elata Bl.on AA-induced DNA damage has not been reported.We found that AA(25,30 and 50 mg/kg)could cause DNA damage and the damage was time/dose dependent.After AA administration,Tail moment,micronuclei formation rate,8-OHdG and MDA level were significantly increased and SOD activity was decreased.Gastrodia elata Bl.decoction,gastrodin and vitamin C could reduce AA-induced DNA damage by decreasing AA-induced increment of tail moment and micronuclei formation rate.What’s more,Gastrodia elata Bl.decoction,gastrodin and vitamin C could lower 8-OHdG and MDA level and improve SOD activity.In conclusion,our research showed that Gastrodia elata Bl.decoction and gastrodin had protective effects on AA-induced DNA damage,and the potential protective mechanism might be related to anti-oxidative stress.展开更多
Gastrodin(4-hydroxymethylphenyl-β-d-glucopyranoside)is an active ingredient with high content,which is isolated from the rhizome of Gastrodia elata.Gastrodin injections,tablets and capsules are currently the main gas...Gastrodin(4-hydroxymethylphenyl-β-d-glucopyranoside)is an active ingredient with high content,which is isolated from the rhizome of Gastrodia elata.Gastrodin injections,tablets and capsules are currently the main gastrodin-related preparations in clinical practice,and gastrodin injections are the most widely used.This article will summarize pharmacology and adverse reactions of gastrodin to evaluate its safety,effectiveness and quality control.Gastrodin has pharmacological effects on central nervous system(vertigo,headache,insomnia,neurasthenia,convulsions and epilepsy,etc.),cardiovascular system and other diseases(osteoporosis,osteoarthritis and bone injury,etc.),but we still need to pay attention to its clinical adverse reactions(some patients may have dry mouth and nose,dizziness and stomach discomfort).In addition,further research is needed in other fields,such as health products,food,cosmetics,etc.We also need to further develop and explore the new pharmacological effects of gastrodin and expand its medicinal value.展开更多
Objective: To explore the influence of gastrodin on IL-10, JAK2 and STAT3 in hippocampus of epileptic rats induced by pentylenetetrazol and the role of the IL-10 pathway in epilepsy. Methods: 50 adult male Wistar rats...Objective: To explore the influence of gastrodin on IL-10, JAK2 and STAT3 in hippocampus of epileptic rats induced by pentylenetetrazol and the role of the IL-10 pathway in epilepsy. Methods: 50 adult male Wistar rats were randomly divided into 5 groups: normal control group (NC Group), epilepsy model group (EP Group), low doses of gastrodin + EP Group (GE1 Group), medium doses of gastrodin + EP Group (GE2 Group), high doses of gastrodin + EP Group (GE3 Group). EP group and GE Groups were injected subthreshold doses of pentylenetetrazole (PTZ) by intraperitoneal once a day until reaching the ignited standards. GE groups were respectively injected 4, 6, 8 mg/kg gastrodin by intraperitoneal. All groups were administered for 28 consecutive days. The behavioral changes of the rats were observed and recorded daily 1 hour after the injection. mRNAs of IL-10, STAT3 and JAK2 in hippocampus were measured by RT-qPCR, and proteins by Western blot. Results: Compared GE2 group with EP group, the incubation of seizure was significantly prolonged (P Conclusions: Gastrodin can increase the expression of IL-10, and reduce the expression of STAT3 and JAK2, which may play an antiepileptic effect through regulating JAK2/STAT3 signaling pathways by IL-10.展开更多
Gastrodin is a phenolic glycoside that has been demonstrated to provide neuroprotection in preclinical models of central nervous system disease, but its effect in subarachnoid hemorrhage(SAH) remains unclear. In this ...Gastrodin is a phenolic glycoside that has been demonstrated to provide neuroprotection in preclinical models of central nervous system disease, but its effect in subarachnoid hemorrhage(SAH) remains unclear. In this study, we showed that intraperitoneal administration of gastrodin(100 mg/kg per day) significantly attenuated the SAH-induced neurological deficit, brain edema, and increased blood-brain barrier permeability in rats. Meanwhile, gastrodin treatment significantly reduced the SAHinduced elevation of glutamate concentration in the cerebrospinal fluid and the intracellular Ca2+ overload.Moreover, gastrodin suppressed the SAH-induced microglial activation, astrocyte activation, and neuronal apoptosis. Mechanistically, gastrodin significantly reduced the oxidative stress and inflammatory response, up-regulated the expression of nuclear factor erythroid 2–related factor2, heme oxygenase-1, phospho-Akt and B-cell lymphoma2, and down-regulated the expression of BCL2-associated X protein and cleaved caspase-3. Our results suggested that the administration of gastrodin provides neuroprotection against early brain injury after experimental SAH.展开更多
Borneol is a traditional Chinese medicine that can promote drug absorption from the gastrointestinal tract and distribution to the brain.However,stomach irritation may occur when high doses of borneol are used.In the ...Borneol is a traditional Chinese medicine that can promote drug absorption from the gastrointestinal tract and distribution to the brain.However,stomach irritation may occur when high doses of borneol are used.In the present work,gastrodin,the main bioactive ingredient of the traditional Chinese drug“Tianma”(Rhizoma Gastrodiae)was used as a model drug to explore reasonable application of borneol.Sustained-release solid dispersions(SRSDs)for co-loading gastrodin and borneol were prepared using ethylcellulose as a sustained release matrix and hydroxy-propyl methylcellulose as a retarder.The dispersion state of drug within the SRSDs was analyzed by using scanning electron microscopy,differential scanning calorimetry,and powder X-ray diffractometry.The results indicated that both gastrodin and borneol were molecularly dispersed in an amorphous form.Assay of in vitro drug release demonstrated that the dissolution profiles of gastrodin and borneol from the SRSDs both fitted the Higuchi model.Subsequently,gastric mucosa irritation and the brain targeting of the SRSDs were evaluated.Compared with the free mixture of gastrodin and borneol,brain targeting of SRSDs was slightly weaker(brain targeting index:1.83 vs.2.09),but stomach irritation obviously reduced.Sustained-release technology can be used to reduce stomach irritation caused by borneol while preserving sufficient transport capacity for oral brain-targeting drug delivery.展开更多
Vascular grafts must avoid negative inflammatory responses and thrombogenesis to prohibit fibrotic deposition immediately upon implantation and promote the regeneration of small diameter blood vessels(<6 mm inner d...Vascular grafts must avoid negative inflammatory responses and thrombogenesis to prohibit fibrotic deposition immediately upon implantation and promote the regeneration of small diameter blood vessels(<6 mm inner diameter).Here,polyurethane(PU)elastomers incorporating anti-coagulative and anti-inflammatory Gastrodin were fabricated.The films had inter-connected pores with porosities equal to or greater than 86%and pore sizes ranging from 250 to 400μm.Incorporation of Gastrodin into PU films resulted in desirable mechanical properties,hydrophilicity,swelling ratios and degradation rates without collapse.The released Gastrodin maintained bioactivity over 21 days as assessed by its anti-oxidative capability.The Gastrodin/PU had better anti-coagulation response(less observable BSA,fibrinogen and platelet adhesion/activation and suppressed clotting in whole blood).Red blood cell compatibility,measured by hemolysis,was greatly improved with 2Gastrodin/PU compared to other Gastrodin/PU groups.Notably,Gastrodin/PU upregulated anti-oxidant factors Nrf2 and HO-1 expression in H2O2 treated HUVECs,correlated with decreasing pro-inflammatory cytokines TNF-αand IL-1β in RAW 264.7 cells.Upon implantation in a subcutaneous pocket,PU was encapsulated by an obvious fibrous capsule,concurrent with a large amount of inflammatory cell infiltration,while Gastrodin/PU induced a thinner fibrous capsule,especially 2Gastrodin/PU.Further,enhanced adhesion and proliferation of HUVECs seeded onto films in vitro demonstrated that 2Gastrodin/PU could help cell recruitment,as evidenced by rapid host cell infiltration and substantial blood vessel formation in vivo.These results indicate that 2Gastrodin/PU has the potential to facilitate blood vessel regeneration,thus providing new insight into the development of clinically effective vascular grafts.展开更多
Peripheral nerve regeneration and functional recovery remain a major clinical challenge.Nerve guidance conduit(NGC)that can regulate biological behavior of Schwann cells(SCs)and facilitate axonal regeneration through ...Peripheral nerve regeneration and functional recovery remain a major clinical challenge.Nerve guidance conduit(NGC)that can regulate biological behavior of Schwann cells(SCs)and facilitate axonal regeneration through microenvironmental remodeling is beneficial for nerve regeneration and functional recovery.Gastrodin,a main constituent of a Chinese traditional herbal medicine,has been known to display several biological and pharmacological properties,especially antioxidative,anti-inflammatory and nerve regeneration.Herein,polyurethane(PU)NGCs modified by different weight ratio of Gastrodin(0,1 and 5 wt%)were designed for sequential and sustainable drug release,that created a favorable microenvironment for nerve regeneration.The scaffold showed suitable pore structure and biocompatibility in vitro,and evidently promoted morphological and functional recovery of regenerated sciatic nerves in vivo.Compared to the PU and 1% Gastrodin/PU scaffolds,the 5% Gastrodin/PU significantly enhanced the proliferation,migration and myelination of SCs and up-regulated expression of neurotrophic factors,as well as induction of the differentiation of PC12 cells.Interestingly,the obvious anti-inflammatory response was observed in 5% Gastrodin/PU by reduced expression of TNF-α and iNOS,which also evidenced by the few fibrous capsule formation in the subcutaneous implantation.Such a construct presented a similarity to autograft in vivo repairing a 10 mm sciatic nerve defects.It was able to not only boost the regenerated area of nerve and microvascular network,but also facilitate functional axons growth and remyelination,leading to highly improved functional restoration.These findings demonstrate that the 5% Gastrodin/PU NGC efficiently promotes nerve regeneration,indicating their potential for use in peripheral nerve regeneration applications.展开更多
文摘Objective To study the therapeutic effects of Ginsenoside Rg-1 and Gastrodine on rats model of Alzheimer’s disease(AD). Methods Aggregated β-Amyloid peptide (25-35) was injected into the lateral ventricle of rats to establish AD models. Ginsenoside Rg-1, Gastrodine and Ginsenoside Rg-1+Gastrodine were intraperitoneally injected into rats of each test group(Ginsenoside Rg-1∶10mg/kg·day; Gastrodine 100mg/kg·day) for 4 weeks, the rats of control group received equal volume of saline. Passive avoidance task and Morris maze test were done to assess the ability of learning and memory. The content of superoxide dismutase (SOD), malondiadehyde (MDA), total-antioxidative capability (T-AOC), Choline acetyltransferase (ChAT) and acetylcholinesterase (AchE) in brain tissue were measured. Results Ginsenoside Rg-1 and Gastrodine significantly improved learning and memory deficits in the rats with AD induced by β-Amyloid peptide (25-35) (P<0.05). Ginsenoside Rg-1+Gastrodine group were better than Ginsenoside Rg-1 group and Gastrodine group (P<0.05). Ginsenoside Rg-1 reduced the increase of SOD, MDA, but inhibited the decrease of T-AOC, AchE and ChAT; Gastrodine reduced the increase of SOD, MDA, while inhibited the decrease of T-AOC. Gastrodine could also prevent the activity of ChAT and AchE decline in AD rats. Conclusion Both Ginsenoside Rg-1 and Gastrodine have therapeutic effects on rats with AD; Ginsenoside Rg-1 and Gastrodine injection at the same time were better than only using one of them. Their mechanisms might different. Ginsenoside Rg-1 can not only inhibit peroxidation but also increase the activity of AchE and ChAT in brain tissue, while Gastrodine can inhibit peroxidation only, but it can’t prevent the decline of ChAT and AchE activity in AD rats.
基金This study was funded by the National Natural Science Foundation of China(82260096)the Science and Technology Foundation of Basic Research Program of Guizhou Province([2023]General 371,[2020]1Y381)the Science and Technology Foundation of Health Commission of Guizhou Province(2022XMSB00037954).
文摘Gastrodia elata,a traditional Chinese medicine belonging to the Orchidaceae family,contains several major components such as gastrodin,polysaccharides of Gastrodia elata,and parishin.The pharmacological studies conducted on Gastrodia elata have revealed a variety of therapeutic properties,including antihypertensive,hypolipidemic,analgesic,and sedative-hypnotic properties.Thus,in this paper,we summarized the pharmacological effects of Gastrodia elata’s major components,namely gastrodin,polysaccharides of Gastrodia elata,parishin,and different types of Gastrodia elata extracts,on cardiovascular diseases such as atherosclerosis,hypertension,hyperglycemia,myocardial ischemia,myocardial hypoxia,myocarditis,and heart failure.Additionally,we conclude the mechanisms through which these active ingredients exert their therapeutic effects,including antioxidants,anti-inflammatory,and nitric oxide regulation.We provide insights into the therapeutic potential of Gastrodia elata with a detailed review of its pharmacological effects and molecular targets in cardiovascular disease protection and therapy,and can better understand the effect of traditional medicines in cardiovascular disease.
基金supported by National Natural Science Foundation of China (Grant number:30672025)Science and Technology Department of Guizhou Province Foundation Project (Grant number:Qinkehe SY[2013]3063,Qinheke J[2013]2179,Qinkehe LH[2014]7021)
文摘Objective:To observe the effects of perfusion of the gastrodin in abdominal aorta for alleviating the spinal cord ischemia reperfusion injury(SCIRI).Methods:A total of 36 New Zealand white rabbits were divided randomly into sham-operated group(group S),control group(group C) and gastrodin group(group G),12 rabbits for each group.Aorta abdominalis infrarenalis blocking method was applied to establish the SCIRI model.The changes of motor evoked potentials(MEPs) before the ischemia and on 30 min,60 min,6 h,12 h and 24 h of reperfusion of the gastrodin were respectively recorded,and the neurologic function score before the ischemia,on the 6 h,12 h and 24 h of the reperfusion of the gastrodin were assessed.And the changes of the concentration of serum neuron specific enolase(NSE),interleukin(IL)-l β and IL-8 were measured before the ischemia,after 45 min of ischemia,and on 30 min,60 min,6 h,12 h and 24 h of reperfusion of gastrodin.Then the levels of spinal cord nerve cells mitochondrial superoxide dismutase(SOD),reactive oxygen species(ROS),glutathione peroxidase(GSH-PX),malondialdehyde(MDA),total antioxidant capacity(T-AOC) and mitochondrial swelling degree(MSD) were tested and the histopathologic changes in spinal cord tissues were observed.Results:The levels of the NSE,IL-lfter the ischemβ,IL-8,ROS,MDA and MSD of group C were all significantly elevated aia(P<0.01);the levels of the spinal nerve cell mitochondria SOD,GSH-PX and T-AOC were all significantly reduced(P<0.01),MEPs and spinal cord tissue pathology were damaged significantly(P<0.01).The rate of motor neuron abnormalities and the damages of spinal cord tissue pathology of group G were significantly milder than those of group C(P<0.01);the levels of NSE,IL-lROS,MDA and MSD were significantly lower than those of group C(P< 0.01),but tβ,IL-8,he levels of SOD,GSH-PX and T-AOC were all significantly higher than those of group C(P<0.01),and the recovery of neurologic function score during the reperfusion of gastrodin was significantly faster than group C(P<0.01).Conclusions:Perfusion of the gastrodin in abdominal aorta can alleviate the spinal cord ischemiare perfusion injury by promoting the mitochondrial antioxidant capacity and inhibiting the inflammatory reaction.
基金Supported by the Natural Science Foundation of Shandong Province,China(No.ZR2017BH049)
文摘AIM:To investigate the neuroprotective effect of gastrodin on retinal ganglion cells(RGCs) in an acute ocular hypertension(AOH) rat model and to identify its possible mechanism.METHODS:AOH rat model was performed in a randomly selected eye by anterior chamber perfusion and either received an intraperitoneal injection with various concentrations of gastrodin or normal saline.After 2 wk,the rats were sacrificed.Fluoro Gold was used to label survival RGCs.Immunostaining with anti-Iba1 in the retinal flat mounts to calculate the microglia density in the ganglion cell layer(GCL).Changes in microglial cytokines,tumour necrosis factor-alpha(TNF-α) and inducible NO synthase(i NOS) were examined with Western blot and reverse transcriptionquantitative polymerase chain reaction.Expression levels of total and phosphorylated p38 mitogen activated protein kinase(MAPK) were determined by Western blot.RESULTS:Results showed that AOH induced significant loss of RGCs and severe microglia activation in the GCL.Besides,AOH increased the phosphorylation of p38 MAPK and promoted the release of microglial cytokines in the retinas.Intraperitoneal injection with dose-dependent gastrodin significantly reduced the loss of RGCs and inhibited retinal microglia activation,accompanied with the decreased expression levels of microglial cytokines and p38 MAPK phosphorylation.CONCLUSION:Gastrodin exerts a neuroprotective effect on RGCs in an acute glaucoma animal model viainhibiting microglia activation and microglial-mediated neuroinflammation.The finding demonstrates the potential application of gastrodin in the neuroprotective therapy of acute glaucoma and other retinal neurodegenerative diseases characterized by microglia activation and RGCs death.
文摘Cardiovascular diseases cause significant morbidity and mortality worldwide,incurring a major public health burden.Gastrodia elata Blume is a traditional Chinese herbal medicine that has been widely used to treat central nervous system and cardiovascular diseases.Gastrodin,as the major active component in Gastrodia elata Blume,can confer protection against cardiovascular diseases.In this review,we summarize the anti-inflammatory actions,anti-cardiac hypertrophy,anti-hypertension,anti-atherosclerosis,and angiogenic effects of gastrodin,as well as its protective effects on vascular cells and against myocardial ischemia-reperfusion injury.The medical potential of gastrodin in diabetes-related cardiovascular diseases is also discussed.
基金Financial support from the National Natural Science Foundation of China(81630094,81502942,and 81730093)CAMS Innovation Fund for Medical Science of China(2016-I2M-1-004,2017-I2M-3-010,and 2016-I2M-1-010)Drug Innovation Major Project(2018ZX09711001-001-001,China)is gratefully acknowledged.
文摘Nine new gastrodin derivatives,including seven p-hydroxybenzyl-modified gastrodin ethers(1-7),6′-O-acetylgastrodin(8),and 4-[α-d-glucopyranosyl-(1→6)-β-d-glucopyranosyloxy]benzyl alcohol(9),together with seven known derivatives,were isolated from an aqueous extract of Gastrodia elata(“tian ma”)rhizomes.Their structures were determined by spectroscopic and chemical methods as well as single crystal X-ray diffraction.Compounds 1-4,7,10,and 11 were also isolated from a reaction mixture by refluxing gastrodin and p-hydroxybenzyl alcohol in H2O.As both gastrodin and p-hydroxybenzyl alcohol exist in the plant,the reaction results provide evidence for the production and increase/decrease of potential effective/toxic components when“tian ma”is decocted solely or together with ingredients in Chinese traditional medicine formulations,though the isolates were inactive in the preliminarily cell-based assays at concentrations of 10μM.Moreover,using ultra-performance liquid chromatography high-resolution electrospray ionization mass spectrometry(UPLC-HRESIMS),4,7,10,and 11,as well as component variations,were detectable in the freshly prepared extracts of different types of samples,including the freeze-dried fresh G.elata rhizomes.
文摘Objective Effects of Remifentanil combined with Gastrodin injection on cerebral oxygen metabolism and early postoperative cognitive function in patients undergoing laparoscopic surgery for cervical cancer.Methods 107 cases of laparoscopic cervical carcinoma were randomly divided into observation group(54 cases)and control group(53 cases),the control group received anesthesia induction therapy based on Remifentanil,the observation group was given intravenous Gastrodin injection to 120h after operation on the basis of control group.the brain oxygen metabolism and brain injury related indexes 6h,12h,72h and 120h after operation were observed,and the preoperative cognitive function and postoperative cognitive function of two groups after 6h,1d,3d and 5d were evaluated by using Mini-Mental State Examination(MMSE)test method.Results Compared to the preoperative data,the oxygen saturation of the internal jugular vein(SjvO22)and cerebral oxygen saturation(rSO2)of two groups after 6h of operation was significantly decreased(p<0.05),and the indexes all back to normal after 120h,and observation group’s indexes were higher than that in control group(P<0.05);and the Cerebral arterial-venous oxygen content difference(Da-jvO2)and Cerebral Oxygen extraction rate(CERO2)of two groups after 6h of operation was significantly increased(P<0.05),and the indexes all back to normal after 120h and observation group’s indexes were lower than that in control group(P<0.05);serum neuron specific enolase(NSE)and S100B protein level of two groups after 6h of operation was significantly increased and back to normal after 120h,and observation group’s indexes were lower than that in control group(P<0.05);The MMSE score of 6h,12h,72h and 120h were higher in the observation group than in the control group,and the incidence of postoperative cognitive dysfunction(POCD)was lower than that in the control group(P-<0.05).Conclusion In the anesthesia induction program based on Remifentanil,the use of Gastrodin injection can reduce the incidence of cognitive dysfunction after laparoscopic surgery for cervical cancer,and its mechanism may be related to the improvement of brain metabolism and the reduction of hypoxia injury in neurons of cranial nerves.
基金funded by the National Science Foundation of China(81173526)the Fundamental Research Funds for the Central Universities(No.30920130112014)+2 种基金the Program for New Century Excellent Talents in University,State Education Ministry of China(#NCET-11-0738)the Program for Changjiang Scholars and Innovative Research Team in University(PCSIRT-IRT1193)the Priority Academic Program Development of Jiangsu Higher Education Institutions(PAPD)
文摘Objective:To explore^1H nuclear magnetic resonance-based metabolomics on sex-specific metabolic changes of gastrodin intervention in rats.Methods:In this research,~1H NMR-based metabolomics was used for the first time to investigate metabolic changes following chronic intervention with gastrodin in rats.Results:24 endogenous metabolites were identified.Body weight.daily diet and the total volume of urine in in each day of each rat were measured synchronously.Modifications in 12 metabolites were observsd following gastrodin intervention,indicating gastrodin-induced alterations in carbohydrate and energy metabolism.Interestingly,these metabolic changes were not totally identical in female and male rats.Some metabolic changes arising from gastrodin intervention showed sexual dimorphism including LDL/VLDL and lactate which were on the decrease in the female but on the increase in the male,together with arginine/ornithine,creatine,and glycerol which were on the increase in the female but on the decrease in the male.While the decrease in pyruvate,succinate and glutamate was only shown in the male and the increase in valine,α-ketoglutarate and glucose was only in the female.Conclusions:This resesrch shows the sex-specific metabolic response to GAS intervention,weather GAS is a healthy dietary supplement for the male merits further
基金School-level Scientific Research Fund of Langfang Normal University-Doctoral Research Startup Project(XBQ202032)Self Raised Project of Langfang Science and Technology Bureau(2019012001)the Project of Langfang Key Laboratory of Food Nutrition and Safety.
文摘[Objectives]The research aimed to establish a high performance liquid chromatography method for the content determination of gastrodin in Jingtianshenma Tablets.[Methods]A phenomenex Luna C18(250 mm×4.6 mm,5μm)column was used;the mobile phase was acetonitrile-0.05%phosphoric acid solution(3∶97);the detection wavelength was 220 nm,and the column temperature was set at 25℃.[Results]Gastrodin showed a good linear relationship in the range of 0.0984-0.5904μg with the peak area,and regression equation was Y=2000000X-51999(r=0.9999).The limits of detection and quantification for gastrodin were 2.50 and 4.20 ng respectively,and the average recovery rate was 95.95%.[Conclusions]This method is sensitive,accurate and reproducible,with good linearity,and it is suitable for the content determination of gastrodin in health food Jingtianshenma Tablets.
文摘Acrylamide(AA)is ubiquitous in packaging materials,paints,cosmetics,food and drinking water.However,AA has obvious neurotoxicity,reproductive toxicity and carcinogenicity,which seriously endangers human health.As one of precious traditional Chinese medicines,Gastrodia elata Bl.has been mainly used to lower blood pressure and resist myocardial ischemia.However,the antioxidant activity of Gastrodia elata Bl.on AA-induced DNA damage has not been reported.We found that AA(25,30 and 50 mg/kg)could cause DNA damage and the damage was time/dose dependent.After AA administration,Tail moment,micronuclei formation rate,8-OHdG and MDA level were significantly increased and SOD activity was decreased.Gastrodia elata Bl.decoction,gastrodin and vitamin C could reduce AA-induced DNA damage by decreasing AA-induced increment of tail moment and micronuclei formation rate.What’s more,Gastrodia elata Bl.decoction,gastrodin and vitamin C could lower 8-OHdG and MDA level and improve SOD activity.In conclusion,our research showed that Gastrodia elata Bl.decoction and gastrodin had protective effects on AA-induced DNA damage,and the potential protective mechanism might be related to anti-oxidative stress.
文摘Gastrodin(4-hydroxymethylphenyl-β-d-glucopyranoside)is an active ingredient with high content,which is isolated from the rhizome of Gastrodia elata.Gastrodin injections,tablets and capsules are currently the main gastrodin-related preparations in clinical practice,and gastrodin injections are the most widely used.This article will summarize pharmacology and adverse reactions of gastrodin to evaluate its safety,effectiveness and quality control.Gastrodin has pharmacological effects on central nervous system(vertigo,headache,insomnia,neurasthenia,convulsions and epilepsy,etc.),cardiovascular system and other diseases(osteoporosis,osteoarthritis and bone injury,etc.),but we still need to pay attention to its clinical adverse reactions(some patients may have dry mouth and nose,dizziness and stomach discomfort).In addition,further research is needed in other fields,such as health products,food,cosmetics,etc.We also need to further develop and explore the new pharmacological effects of gastrodin and expand its medicinal value.
文摘Objective: To explore the influence of gastrodin on IL-10, JAK2 and STAT3 in hippocampus of epileptic rats induced by pentylenetetrazol and the role of the IL-10 pathway in epilepsy. Methods: 50 adult male Wistar rats were randomly divided into 5 groups: normal control group (NC Group), epilepsy model group (EP Group), low doses of gastrodin + EP Group (GE1 Group), medium doses of gastrodin + EP Group (GE2 Group), high doses of gastrodin + EP Group (GE3 Group). EP group and GE Groups were injected subthreshold doses of pentylenetetrazole (PTZ) by intraperitoneal once a day until reaching the ignited standards. GE groups were respectively injected 4, 6, 8 mg/kg gastrodin by intraperitoneal. All groups were administered for 28 consecutive days. The behavioral changes of the rats were observed and recorded daily 1 hour after the injection. mRNAs of IL-10, STAT3 and JAK2 in hippocampus were measured by RT-qPCR, and proteins by Western blot. Results: Compared GE2 group with EP group, the incubation of seizure was significantly prolonged (P Conclusions: Gastrodin can increase the expression of IL-10, and reduce the expression of STAT3 and JAK2, which may play an antiepileptic effect through regulating JAK2/STAT3 signaling pathways by IL-10.
基金supported by funds from the Project of Medical and Health Technology Development Program in Shandong Province,China(2016WS0196)
文摘Gastrodin is a phenolic glycoside that has been demonstrated to provide neuroprotection in preclinical models of central nervous system disease, but its effect in subarachnoid hemorrhage(SAH) remains unclear. In this study, we showed that intraperitoneal administration of gastrodin(100 mg/kg per day) significantly attenuated the SAH-induced neurological deficit, brain edema, and increased blood-brain barrier permeability in rats. Meanwhile, gastrodin treatment significantly reduced the SAHinduced elevation of glutamate concentration in the cerebrospinal fluid and the intracellular Ca2+ overload.Moreover, gastrodin suppressed the SAH-induced microglial activation, astrocyte activation, and neuronal apoptosis. Mechanistically, gastrodin significantly reduced the oxidative stress and inflammatory response, up-regulated the expression of nuclear factor erythroid 2–related factor2, heme oxygenase-1, phospho-Akt and B-cell lymphoma2, and down-regulated the expression of BCL2-associated X protein and cleaved caspase-3. Our results suggested that the administration of gastrodin provides neuroprotection against early brain injury after experimental SAH.
基金This study was supported by the grants of National Natural Science Foundation of China(30902009)the Key Scientific and Technological Innovation Programs of Higher Education Institutions in Guangdong(CXZD1121).
文摘Borneol is a traditional Chinese medicine that can promote drug absorption from the gastrointestinal tract and distribution to the brain.However,stomach irritation may occur when high doses of borneol are used.In the present work,gastrodin,the main bioactive ingredient of the traditional Chinese drug“Tianma”(Rhizoma Gastrodiae)was used as a model drug to explore reasonable application of borneol.Sustained-release solid dispersions(SRSDs)for co-loading gastrodin and borneol were prepared using ethylcellulose as a sustained release matrix and hydroxy-propyl methylcellulose as a retarder.The dispersion state of drug within the SRSDs was analyzed by using scanning electron microscopy,differential scanning calorimetry,and powder X-ray diffractometry.The results indicated that both gastrodin and borneol were molecularly dispersed in an amorphous form.Assay of in vitro drug release demonstrated that the dissolution profiles of gastrodin and borneol from the SRSDs both fitted the Higuchi model.Subsequently,gastric mucosa irritation and the brain targeting of the SRSDs were evaluated.Compared with the free mixture of gastrodin and borneol,brain targeting of SRSDs was slightly weaker(brain targeting index:1.83 vs.2.09),but stomach irritation obviously reduced.Sustained-release technology can be used to reduce stomach irritation caused by borneol while preserving sufficient transport capacity for oral brain-targeting drug delivery.
基金This research was supported by the National Natural Science Foundation of China(81760087/31760292/81860326/81560050)the Department of Science and Technology of Yunnan Province of China(2017FA035/2017FE467(-008)/2018FE001(-137)/2018FE001(-165)/2018FE001(-125)/2018IA048/2019ZF011-2)+1 种基金Major Program of Kunming Science and Technology Innovation Center(2019-1-N-25318000003568)Program for Innovative Research Team(in Science and Technology)in University of Yunnan Province(IRTSTYN).
文摘Vascular grafts must avoid negative inflammatory responses and thrombogenesis to prohibit fibrotic deposition immediately upon implantation and promote the regeneration of small diameter blood vessels(<6 mm inner diameter).Here,polyurethane(PU)elastomers incorporating anti-coagulative and anti-inflammatory Gastrodin were fabricated.The films had inter-connected pores with porosities equal to or greater than 86%and pore sizes ranging from 250 to 400μm.Incorporation of Gastrodin into PU films resulted in desirable mechanical properties,hydrophilicity,swelling ratios and degradation rates without collapse.The released Gastrodin maintained bioactivity over 21 days as assessed by its anti-oxidative capability.The Gastrodin/PU had better anti-coagulation response(less observable BSA,fibrinogen and platelet adhesion/activation and suppressed clotting in whole blood).Red blood cell compatibility,measured by hemolysis,was greatly improved with 2Gastrodin/PU compared to other Gastrodin/PU groups.Notably,Gastrodin/PU upregulated anti-oxidant factors Nrf2 and HO-1 expression in H2O2 treated HUVECs,correlated with decreasing pro-inflammatory cytokines TNF-αand IL-1β in RAW 264.7 cells.Upon implantation in a subcutaneous pocket,PU was encapsulated by an obvious fibrous capsule,concurrent with a large amount of inflammatory cell infiltration,while Gastrodin/PU induced a thinner fibrous capsule,especially 2Gastrodin/PU.Further,enhanced adhesion and proliferation of HUVECs seeded onto films in vitro demonstrated that 2Gastrodin/PU could help cell recruitment,as evidenced by rapid host cell infiltration and substantial blood vessel formation in vivo.These results indicate that 2Gastrodin/PU has the potential to facilitate blood vessel regeneration,thus providing new insight into the development of clinically effective vascular grafts.
基金supported by the National Natural Science Foundation of China(81960251/81460210/81860326)the Department of Science and Technology of Yunnan Province of China(2019ZF011-2/2017FF117(-062)/2018IA048/2018FE001(-029)/2018FE001(-024))+1 种基金Scientific Research Fund of Yunnan Provincial Education Commission(2021J0229)the 100 Talents Program of Kunming Medical University(Limei Li).
文摘Peripheral nerve regeneration and functional recovery remain a major clinical challenge.Nerve guidance conduit(NGC)that can regulate biological behavior of Schwann cells(SCs)and facilitate axonal regeneration through microenvironmental remodeling is beneficial for nerve regeneration and functional recovery.Gastrodin,a main constituent of a Chinese traditional herbal medicine,has been known to display several biological and pharmacological properties,especially antioxidative,anti-inflammatory and nerve regeneration.Herein,polyurethane(PU)NGCs modified by different weight ratio of Gastrodin(0,1 and 5 wt%)were designed for sequential and sustainable drug release,that created a favorable microenvironment for nerve regeneration.The scaffold showed suitable pore structure and biocompatibility in vitro,and evidently promoted morphological and functional recovery of regenerated sciatic nerves in vivo.Compared to the PU and 1% Gastrodin/PU scaffolds,the 5% Gastrodin/PU significantly enhanced the proliferation,migration and myelination of SCs and up-regulated expression of neurotrophic factors,as well as induction of the differentiation of PC12 cells.Interestingly,the obvious anti-inflammatory response was observed in 5% Gastrodin/PU by reduced expression of TNF-α and iNOS,which also evidenced by the few fibrous capsule formation in the subcutaneous implantation.Such a construct presented a similarity to autograft in vivo repairing a 10 mm sciatic nerve defects.It was able to not only boost the regenerated area of nerve and microvascular network,but also facilitate functional axons growth and remyelination,leading to highly improved functional restoration.These findings demonstrate that the 5% Gastrodin/PU NGC efficiently promotes nerve regeneration,indicating their potential for use in peripheral nerve regeneration applications.
