JOURNAL OF ETHNOPHARMACOLOGY
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2023
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IF 5.4
Honghua Zhang,Yunting Sun,Yuqing Zou,Cheng Chen,Shuling Wang
Ethnopharmacological relevance Banxia baizhu tianma decoction (BBTD) originated from the Qing Dynasty Chinese medicine book “Medical Xinwu”, which has a clinical application history of more than 300 years. It's a classic prescription for expelling phlegm, extinguishing wind, strengthening the spleen (traditional Chinese medicine, ie, TCM, refers to the spleen channel) and dissipating excessive fluid based on TCM theory. BBTD is particularly effective in the treatment of excessive phlegm-dampness hypertension. However, the precise pharmacological effect of each herb of BBTD on hypertension treatment is not yet fully understood. Aim of the study To investigate the pharmacological effects of each herb in BBTD on hypertension treatment and to explore the mechanisms behind them. Materials and methods A high-fat-diet fed animal model was developed to evaluate the efficacy of different groups of drugs in BBTD for the treatment of hypertension. Untargeted metabolism was used to detect the metabolic changes after modeling and drug intervention. Then, Stigmasterol (STI) and gastrodin (GAS), major components of Pinellia Ternate Makino and Gastrodia elata Blume, were selected for treatment on HepG2 cell steatosis model. Real-time quantitative polymerase chain reaction and Western blotting were used to detect changes of corresponding gene and protein after drug intervention to explore the exam anti-hyperlipidemia mechanism of STI and GAS combination. Results The weight gain, elevated blood pressure and increased blood lipids induced by high-fat-diet were significantly decreased ( p < 0.05) after each prescription medicine intervention in a dose-dependent manner. In addition, 28 differential metabolites (DMs) were detected after modeling and were regulated to normal at varying degrees after each drug group treatment. In addition, eight of the 28 DMs were significantly different from the model group after the full prescription drug intervention, primarily related to four metabolic pathways, while only two metabolites were significantly different from the model group after the unprincipled drug intervention, related to one metabolic pathway. In HepG2 hyperlipidemia cell model, STI, GAS and their combination significantly decreased TC , TG levels and lipid accumulation ( p < 0.05), and decreased sterol regulatory element-binding protein 1c (SREBP-1c), fatty acid synthase (FAS), stearoyl-CoA desaturase-1 (SCD1) and their protein expressions ( p < 0.05), increased adenosine monophosphate-activated protein kinase (AMPK) and it's protein expression ( p < 0.05). The two drugs work better in combination than alone. Conclusion BBTD has been shown to be effective in reducing lipid accumulation in a high-fat rat model, as well as in restoring the model-induced abnormal metabolites to normal levels in a dose-dependent manner. Pinellia ternata Makino and Gastrodia elata Blume, the main components of BBTD, may regulate lipid metabolism through fatty acid biosynthesis, arginine and proline metabolism. Their main active agents, STI and GAS, effectively reduce lipid accumulation and lipid content in cells and regulate the expression levels of genes and proteins associated with lipid metabolism. These results suggest that BBTD may regulate lipid metabolism via AMPK/SREBP-1c pathway.
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高影响因子
MOLECULES
·
2019
·Vol. 24
·期 3
·547
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IF 3.06
Minhui Hu,Hui Yan,Yuanyuan Fu,Yulan Jiang,Weifeng Yao,Sheng Yu,Li Zhang,Qinan Wu,Anwei Ding,Mingqiu Shan
Gastrodia elatatuber (GET) is a popular traditional Chinese medicines (TCMs). In this study, response surface methodology (RSM) with a Box–Behnken design (BBD) was performed to optimize the extraction parameters of gastrodin-type components (gastrodin, gastrodigenin, parishin A, parishin B, parishin C and parishin E). Different from the conventional studies that merely focused on the contents of phytochemical, we gave consideration to both quantitative analysis of the above six components by HPLC and representative bioactivities of GET, including antioxidation and protection of human umbilical vein endothelial cells (HUVEC). Four independent variables (ethanol concentration, liquid-material ratio, soaking time and extraction time) were investigated with the integrated evaluation index of phytochemical contents. With the validation experiments, the optimal extraction parameters were as follows: ethanol concentration of 41%, liquid–solid ratio of 28.58 mL/g, soaking time of 23.91 h and extraction time of 46.60 min. Under the optimum conditions, the actual standardized comprehensive score was 1.8134 ± 0.0110, which was in accordance with the predicted score of 1.8100. This firstly established method was proved to be feasible and reliable to optimize the extraction parameters of the bioactive components from GET. Furthermore, it provides some reference for the quality control and extraction optimization of TCMs.Keywords:Gastrodia elatatuber (GET);Response surface methodology;Antioxidation;HUVEC;Gastrodin-type components
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TOXICOLOGY AND APPLIED PHARMACOLOGY
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2025
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IF 3.4
Ruijing Li,Weili Yang,Lijuan Zheng,Xingxue Yan,Cuihua Liu,Yaodong Zhang,Jitong Li
Prenatal alcohol exposure is a leading cause of developmental abnormalities and neurobehavioral deficits, collectively known as fetal alcohol spectrum disorder (FASD). The underlying molecular mechanisms, however, are not fully elucidated, hindering the development of effective therapeutic strategies. Ferroptosis, an iron-dependent form of regulated cell death driven by lipid peroxidation, has emerged as a key pathological process in various diseases. Gastrodin (GAS), the primary bioactive component of Gastrodia elata , has demonstrated potent antioxidant and neuroprotective properties. This study aimed to investigate the protective effects of GAS against alcohol-induced developmental and neurotoxic damage and to elucidate the underlying molecular mechanisms. Using a zebrafish larval model, we found that exposure to 200 mM alcohol from 2 to 24 hours post-fertilization (hpf) induced significant developmental toxicity, including a decreased hatching rate, body length and eye diameter, and increased morphological malformations in larvae. Alcohol-exposed larvae also exhibited severe neurobehavioral deficits, characterized by a reduction in movement distance and average velocity in dark conditions. Mechanistically, alcohol exposure triggered ferroptosis, evidenced by an increase in intracellular Fe 2+ , malondialdehyde (MDA), and reactive oxygen species (ROS) levels, alongside a decrease in the levels of glutathione (GSH) and reduced glutathione peroxidase 4 (GPX4) and the nuclear factor erythroid 2-related factor 2 (Nrf2) activities. Co-treatment with GAS (200 mg/L) significantly ameliorated these alcohol-induced developmental and neurobehavioral defects. GAS administration effectively suppressed the hallmarks of ferroptosis by restoring the ROS level and altering the expression of genes related to oxidative stress. In addition, GAS suppressed alcohol-induced cell apoptosis, downregulated caspase3b , bax , caspase8 , and upregulated bcl2 in mRNA levels. Molecular analysis revealed that GAS exerts its anti-ferroptotic effect by activating Nrf2/GPX4 signaling pathway, which was suppressed by alcohol. Our findings indicate that ferroptosis plays a key role in alcohol-induced developmental neurotoxicity, and GAS provides protection by activating the Nrf2/GPX4 axis. This suggests that GAS could be a potential therapeutic option for reducing the negative effects of prenatal alcohol exposure.
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JOURNAL OF CHROMATOGRAPHY A
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2014
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IF 4.258
Wenhua Ji,Lingxiao Chen,Xiuli Ma,Xiao Wang,Qianshan Gao,Yanling Geng,Luqi Huang
Molecular imprinted polymers (MIPs) with high selectivity and affinity to gastrodin in water were designed using allyl 2,3,4,6-tetra- O -acetyl-glucopyranoside (TAGL) and 1,2,3,4,5-pentafluoro-6-vinylbenzene (PFVB) as novel functional monomers. Binding characterization of pre-polymerization complexes was researched by nuclear magnetic resonance (NMR) and the MIPs were characterized by scanning electron microscopy (SEM). The properties involving adsorption isotherm, adsorption kinetics and selective recognition capacity were evaluated. The MIPs/TAGL exhibited good site accessibility in which it only took 30 min to achieve adsorption equilibrium and highly selective recognition for the template. Furthermore, the performance of the MIPs/TAGL as solid phase extraction material was investigated in detail and hot water at 50 °C served as the eluting solvent. Pure gastrodin with the recovery of 76.6% was obtained from the aqueous extract of Gastrodia elata roots.
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Frontiers in Cellular Neuroscience
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2022
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IF 6.147
Yuhong Wang,Kaixuan Luo,Junrui Li,Yehui Liao,Chengde Liao,Wen-Shiang Chen,Moxian Chen,Lijuan Ao
Parkinson’s disease (PD) is the second most common chronic neurodegenerative disease globally; however, it lacks effective treatment at present. Focused ultrasound (FUS) combined with microbubbles could increase the efficacy of drug delivery to specific brain regions and is becoming a promising technology for the treatment of central nervous system diseases. In this study, we explored the therapeutic potential of FUS-mediated blood–brain barrier (BBB) opening of the left striatum to deliver gastrodin (GAS) in a subacute PD mouse model induced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). The concentration of GAS in the left hemisphere was detected by ultra-high performance liquid chromatography electrospray Q-Orbitrap mass spectrometry (UHPLC/ESI Q-Orbitrap) and the distribution of tyrosine hydroxylase (TH) neurons was detected by immunohistochemical staining. The expression of TH, Dopamine transporter (DAT), cleaved-caspase-3, B-cell lymphoma 2 (Bcl-2), brain-derived neurotrophic factor (BDNF), postsynaptic density protein 95 (PSD-95), and synaptophysin (SYN) protein were detected by western blotting. Analysis showed that the concentration of GAS in the left hemisphere of PD mice increased by approximately 1.8-fold after the BBB was opened. FUS-mediated GAS delivery provided optimal neuroprotective effects and was superior to the GAS or FUS control group. In addition, FUS enhanced GAS delivery significantly increased the expression of Bcl-2, BDNF, PSD-95, and SYN protein in the left striatum ( P < 0.05) and reduced the levels of cleaved-caspase-3 remarkably ( P = 0.001). In conclusion, the enhanced delivery by FUS effectively strengthened the protective effect of GAS on dopaminergic neurons which may be related to the reinforcement of the anti-apoptotic activity and the expression of synaptic-related proteins in the striatum. Data suggests that FUS-enhanced GAS delivery may represent a new strategy for PD treatment.
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高影响因子
MOLECULES
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2022
·Vol. 27
·期 4
·1230
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IF 4.927
Li Jiang,Yanling Xiong,Yu Tu,Wentong Zhang,Qiyun Zhang,Peng Nie,Xiaojun Yan,Hongning Liu,Ronghua Liu,Guoliang Xu
Puerarin (PUR) and gastrodin (GAS) are often used in combined way for treating diseases caused by microcirculation disorders. The current study aimed to investigate the absorption and transportation mechanism of PUR and GAS and their interaction via Caco-2 monolayer cell model. In this work, the concentration in Caco-2 cell of PUR and GAS was determined by HPLC method. The bidirectional transport of PUR and GAS and the inhibition of drug efflux including verapamil and cyclosporine on the transport of these two components were studied. The mutual influence between PUR and GAS, especially the effect of the latter on the former of the bidirectional transport were also investigated. The transport of 50 μg·mL−1PUR in Caco-2 cells has no obvious directionality. While the transport of 100 and 200 μg·mL−1PUR presents a strong directionality, and this directionality can be inhibited by verapamil and cyclosporine. When PUR and GAS were used in combination, GAS could increase the absorption of PUR while PUR had no obvious influence on GAS. Therefore, the compatibility of PUR and GAS is reasonable, and GAS can promote the transmembrane transport of PUR, the effect of which is similar to that of verapamil.Keywords:transport mechanism;puerarin;gastrodin;absorption;Caco-2 cell monolayer
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Bioactive Materials
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2024
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IF 18
Shiwei Niu,Fan Li,Zhi Lin,Bo Chen,Lechun Lyu,Yongliang Jiang,Wanting Li,Jianlin Jiao,Yi Han,Di Lu,Lin Sun
Since inferior biomimetic fabrication and anti-thrombosis process always lead to the implantation failure of artificial vascular grafts, the development of bioactive platform which can promote endothelialization is fundamental in the research for blood vessel substitutes to overcome the low-efficiency or hyperplasia. To solve the limitation of insufficient autologous sources of small blood vessels, this study prepared a tri-layer small diameter vascular based on citrate, followed by covalently immobilizing of specific peptides to achieve in situ cells enrichment. The natural carbohydrate of carboxymethyl chitosan is creatively used as the inner layer of tubular graft, thus exerting the anti-thrombosis effect. Moreover, the gastrodin coating was employed to alleviate the inflammation response and increase the safety of this surgically implanted vascular scaffold. The synthesis process was characterized, its biocompatibility, hierarchically cell induction capacity, anticoagulant effect and the ability to promote neovascularization were evaluated. In such way, we hope to prepare a biodegradable small-diameter artificial vascular for the clinical application.
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Reproductive Biology
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2023
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IF 2.1
Yulu Cao,Jingjing Wang,Xiaoxiao Li,Biyun Liu,Chongjun Li,Yijin Sun,Kang Zou
Zearalenone (ZEA) is a prevalent mycotoxin found in moldy diets and is associated with reproductive dysfunction. However, the molecular underpinning of ZEA in impairment of spermatogenesis remains largely unknown. To unveil the toxic mechanism of ZEA, we established a co-culture model using porcine Sertoli cells and porcine spermatogonial stem cells (pSSCs) to investigate the impact of ZEA on these cell types and their associated signaling pathways . Our findings showed that low concentration of ZEA inhibited cell apoptosis , while high concentration induced cell apoptosis. Furthermore, the expression levels of Wilms’ tumor 1 (WT1), proliferating cell nuclear antigen (PCNA) and glial cell line-derived neurotrophic factor (GDNF) were significantly decreased in ZEA treatment group, while concurrently upregulating the transcriptional levels of the NOTCH signaling pathway target genes HES1 and HEY1 . The addition of the NOTCH signaling pathway inhibitor DAPT (GSI-IX) alleviated the damage to porcine Sertoli cells caused by ZEA. Gastrodin (GAS) significantly increased the expression levels of WT1, PCNA and GDNF, and inhibited the transcription of HES1 and HEY1 . GAS also efficiently restored the decreased expression levels of DDX4, PCNA and PGP9.5 in co-cultured pSSCs suggesting its potential in ameliorating the damage caused by ZEA to Sertoli cells and pSSCs. In conclusion, the present study demonstrates that ZEA disrupts pSSCs self-renewal by affecting the function of porcine Sertoli cell, and highlights the protective mechanism of GAS through the regulation of the NOTCH signaling pathway. These findings may offer a novel strategy for alleviating ZEA-induced male reproductive dysfunction in animal production.
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NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
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2026
·
IF 4
Song Jia-Lin,Wu Rui-Cong,Sun Rui,Gao Ya-Xin,He Bing-Qin,Xie Yan-Jie,Xie Jie-Shan,Li Xi-Rui,Tong Fei-Xiang,Liu Yan,Li Hui,Wang Zeng-Qin
Inflammatory bowel disease (IBD) patients frequently suffer from emotional disturbances, predominantly anxiety- and depression-like symptoms, and may also have cognitive dysfunction, but the mechanisms remain unclear, and no therapies targeting the gut or nervous system exist. Gastrodin (GAS), the primary active component of Gastrodia elata , has anti-inflammatory and neuroprotective effects. Whether GAS can alleviate acute colitis with comorbid anxiety- and depression-like behaviours or cognitive dysfunction via the gut–brain axis is unknown. Using a 3% dextran sulfate sodium (DSS)–induced mouse model, we administered GAS (240 mg/kg) by gavage for 7 days. The open field, elevated plus maze, tail suspension, and forced swimming tests showed that GAS improved behavioural abnormalities (including anxiety- and depression-like behaviours); it also restored colon length and reduced colonic histopathological injury. Metagenomic sequencing revealed that GAS reshaped the gut microbiota, increasing Sporosarcina and Nitrospirae while decreasing Clostridiaceae and Lachnospiraceae. Untargeted metabolomics indicated that GAS shifted the metabolic profile away from DSS and normalized taurine levels, and KEGG pathway analysis suggested that GAS may partially ameliorate DSS-induced metabolic disturbances by downregulating virulence-related pathways and upregulating energy metabolic pathways such as the TCA cycle and oxidative phosphorylation relative to DSS. Western blot confirmed that GAS restored the tight junction protein Occludin and decreased TNF-α. Quantitative proteomics demonstrated that GAS reversed the aberrant expression of 191 colonic proteins. These results demonstrate correlative associations between GAS treatment and the alleviation of acute colitis and behavioural abnormalities, alongside concurrent changes in gut microbiota composition, metabolite profiles, and intestinal barrier proteins. Whether these associations reflect a causal gut-brain axis mechanism requires direct experimental validation. GAS modulates the microbiota, partially restores metabolism, repairs the gut barrier, and suppresses local inflammation, suggesting a potential gut-brain axis mechanism. These findings position GAS as a promising candidate for further mechanistic and translational investigation in IBD-associated behavioural comorbidities.
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ACS Omega
·
2021
·
IF 3.512
Jun Lu,Xin Ma,Wen-Cong Gao,Xin Zhang,Yuanling Fu,Qian Liu,Lixiang Tian,Xiao-Dan Qin,Weimin Yang,Hong-Yi Zheng,Chang-Bo Zheng
Pathological cardiac hypertrophy is commonly associated with an upregulation of fetal genes, fibrosis, cardiac dysfunction, and heart failure. Previous studies have demonstrated that gastrodin (GAS) exerts cardioprotective action in the treatment of cardiac hypertrophy. However, the mechanism by which GAS protects against cardiac hypertrophy is yet to be elucidated. A mouse model of myocardial hypertrophy was established using an angiotensin II (Ang II) induction. GAS (5 or 50 mg/kg/d) was orally administered every day starting 7 days prior to the Ang II infusion combined with sham-operated controls. Heart samples from each group were collected for RNA sequencing. Using bioinformatics analysis, the key differentially expressed genes (DEGs) that are involved in reversing cardiac function were identified. Through bioinformatics analysis, the key DEGs that are involved in GAS’s inhibition of Ang II-induced abnormal gene expression within the heart were identified. This was further validated using quantitative real-time PCR and Western blotting in neonatal rat cardiomyocytes (NRCMs). Oral administration of GAS significantly suppressed the Ang II-induced increase in heart size and heart weight to body weight. Furthermore, pretreatment of the NRCMs with GAS led to a dose-dependent inhibition of Ang II-induced increases in Nppb mRNA expression. We identified 620 upregulated and 87 downregulated Ang II-induced DEGs II, among which the expression patterns of 58 and 146 genes were inverted by low-dose and high-dose GAS, respectively. These inverted DEGs were found to be mainly enriched in the biological processes of regulation of Ras protein signal transduction, heart contraction, covalent chromatin modification, glucose metabolism, and positive regulation of cell cycle. Among them, the insulin-like growth factor type 2 (Igf2) gene, which was found to be highly reversed and downregulated by GAS, served as a core gene linking energy metabolism, immune regulation, and systemic development. Subsequent functional verification demonstrated that IGF2, and its receptor IGF2R, is one of the targets of GAS that helps protect against cardiac hypertrophy. Taken together, we have identified, for the first time, IGF2/IGF2R as a potential target influenced by GAS in the prevention of cardiac hypertrophy.
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JOURNAL OF ETHNOPHARMACOLOGY
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2026
·
IF 6.8
Yonghao Wang,Mingheng Su,Zi Ye,Ziqian Jia,Qi Zhang
Ethnopharmacological relevance Gastrodia elata Blume ( G. elata ) is a traditional Chinese medicinal herb documented in the Compendium of Materia Medica and has been widely used for dizziness, convulsive disorders, vertigo, and neurological symptoms. Gastrodin (GAS), the principal bioactive constituent of G. elata , is known to exhibit anti-inflammatory, antioxidant, and neuroprotective properties. Nevertheless, whether GAS is beneficial for vascular cognitive impairment associated with dietary risk factors remains unclear. Clarifying this issue may help explain the pharmacological basis of the traditional neurological use of G. elata . Aim of the study This study investigated whether GAS could alleviate cognitive dysfunction aggravated by a high-salt diet (HSD) in chronic cerebral hypoperfusion (CCH) mice, and explored its possible involvement in cerebral blood flow (CBF) regulation, blood-brain barrier (BBB)-related structural preservation, and amyloidogenic processing. Materials and methods A mouse model of CCH combined with dietary risk was generated using bilateral common carotid artery stenosis (BCAS) and HSD exposure. Cognitive performance was assessed by the novel object recognition test, Y-maze test, and open field test. CBF was monitored using laser speckle imaging. Hippocampal transcriptomic sequencing was conducted to identify GAS-regulated pathways. Nissl staining, immunohistochemistry, Western blotting, and transmission electron microscopy were used to examine neuronal injury, BBB structure, and related protein expression. Serum Aβ and inflammatory cytokines were quantified by ELISA. Results HSD exposure further worsened BCAS-induced cerebral hypoperfusion and cognitive deficits. GAS administration restored CBF, improved behavioral performance, and showed a tendency toward partial improvement of hippocampal morphology. Transcriptomic analysis indicated that GAS-responsive differentially expressed genes were enriched in pathways associated with extracellular matrix interaction, tight junctions, vascular function, and PI3K-Akt signaling. Further experiments showed that GAS increased ZO-1, Occludin, and eNOS expression, preserved BBB-related ultrastructural features, restored Akt/mTOR pathway-associated phosphorylation, and attenuated BACE1/APP-, sAPPβ-, Aβ-, and serum TNF-α-related changes. Conclusion GAS ameliorates cognitive impairment induced by HSD exposure combined with BCAS, and this effect is associated with improved CBF, restoration of Akt/mTOR pathway-associated phosphorylation, eNOS-related endothelial regulation, preservation of BBB-related structural integrity, and attenuation of amyloidogenic processing-related and serum inflammatory marker changes. These results provide experimental support for the potential role of GAS in treating vascular cognitive impairment associated with dietary risk factors.
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