RESUMO
The polysaccharide glucan was extracted from Gastrodia elata Blume, and its structural characterizations and beneficial effects against acute dextran sulfate sodium (DSS)-induced ulcerative colitis were investigated. The results showed that a polysaccharide GP with a molecular weight of 811.0 kDa was isolated from G. elata Blume. It had a backbone of α-D-1,4-linked glucan with branches of α-d-glucose linked to the C-6 position. GP exhibited protective effects against DSS-induced ulcerative colitis, and reflected in ameliorating weight loss and pathological damages in mice, increasing colon length, inhibiting the expression of inflammatory cytokines tumor necrosis factor-α (TNF-α) and interleukin-1ß (IL-1ß), decreasing the levels of inflammatory related proteins NLRP3 and ASC, and elevating the anti-inflammatory cytokine interleukin-10 (IL-10) level in mouse colon tissues. GP supplementation also reinforced the intestinal barrier by promoting the expression of ZO-1, Occludin, and MUC2 of colon tissues, and positively regulated intestinal microbiota. Thus, GP treatment possessed a significant improvement in ulcerative colitis in mice, and it was expected to be developed as a functional food.
Assuntos
Sulfato de Dextrana , Gastrodia , Glucanos , Animais , Sulfato de Dextrana/efeitos adversos , Glucanos/química , Glucanos/farmacologia , Camundongos , Gastrodia/química , Colite/tratamento farmacológico , Colite/induzido quimicamente , Masculino , Microbioma Gastrointestinal/efeitos dos fármacos , Citocinas/metabolismo , Colite Ulcerativa/tratamento farmacológico , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/patologia , Modelos Animais de Doenças , Colo/efeitos dos fármacos , Colo/patologia , Colo/metabolismo , Peso MolecularRESUMO
Gastrodin, a bioactive compound derived from the rhizome of the orchid Gastrodia elata, exhibits a diverse range of biological activities. With documented neuroprotective, anti-inflammatory, antioxidant, anti-apoptotic, and anti-tumor effects, gastrodin stands out as a multifaceted therapeutic agent. Notably, it has demonstrated efficacy in protecting against neuronal damage and enhancing cognitive function in animal models of Alzheimer's disease, Parkinson's disease, and cerebral ischemia. Additionally, gastrodin showcases immunomodulatory effects by mitigating inflammation and suppressing the expression of inflammatory cytokines. Its cytotoxic activity involves the inhibition of angiogenesis, suppression of tumor growth, and induction of apoptosis. This comprehensive review seeks to elucidate the myriad potential effects of Gastrodin, delving into the intricate molecular mechanisms underpinning its pharmacological properties. The findings underscore the therapeutic potential of gastrodin in addressing various conditions linked to neuroinflammation and cancer.
Assuntos
Álcoois Benzílicos , Glucosídeos , Fármacos Neuroprotetores , Álcoois Benzílicos/farmacologia , Álcoois Benzílicos/química , Glucosídeos/farmacologia , Glucosídeos/química , Humanos , Animais , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Gastrodia/química , Antioxidantes/farmacologia , Antioxidantes/química , Apoptose/efeitos dos fármacos , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Neoplasias/metabolismoRESUMO
Tianma is the dried tuber of Gastrodia elata Blume (G. elata), which is frequently utilized in clinical practice as a traditional Chinese medicine. Gastrodin (GAS) is the main active ingredient of Tianma, which has good pharmacological activity. Therefore, for the first time, this review focused on the extraction, synthesis, pharmacological effects, and derivatives of GAS and to investigate additional development options for GAS. The use of microorganisms to create GAS is a promising method. GAS has good efficacy in the treatment of neurological diseases, cardiovascular diseases, endocrine diseases, and liver diseases. GAS has significant anti-inflammatory, antioxidant, neuroprotective, vascular protective, blood sugar lowering, lipid-regulating, analgesic, anticancer, and antiviral effects. The mechanism involves various signaling pathways such as Nrf2, NF-κB, PI3K/AKT, and AMPK. In addition, the derivatives of GAS and biomaterials synthesized by GAS and PU suggested a broader application of GAS. The research on GAS is thoroughly summarized in this paper, which has useful applications for tackling a variety of disorders and exhibits good development value.
Assuntos
Álcoois Benzílicos , Glucosídeos , Glucosídeos/farmacologia , Glucosídeos/uso terapêutico , Álcoois Benzílicos/farmacologia , Álcoois Benzílicos/uso terapêutico , Humanos , Animais , Gastrodia/química , Transdução de Sinais/efeitos dos fármacosRESUMO
Gastrodia elata ("Tian Ma" in Chinese) is used as a food and medical ingredient in traditional Chinese medicine. In this study, to enhance the anti-breast cancer activity of Gastrodia elata polysaccharide (GEP), GEPs were modified via sulfidation (SGEP) and acetylation (AcGEP). The physicochemical properties (such as solubility and substitution degree) and structural information (such as molecular weight Mw and radius of gyration Rg) of GEP derivatives were determined by Fourier transformed infrared (FTIR) spectroscopy and asymmetrical flow field-flow fractionation (AF4) coupled online with multiangle light scattering (MALS) and differential refractive index (dRI) detectors (AF4-MALS-dRI). The effects of the structural modification of GEP on the proliferation, apoptosis, and cell cycle of MCF-7 cell were studied systematically. The ability of MCF-7 cell for the uptake of GEP was studied by laser scanning confocal microscopy (LSCM). The results suggested that the solubility and anti-breast cancer activity of GEP were enhanced and the average Rg and Mw of GEP decreased after chemical modification. The AF4-MALS-dRI results showed that the chemical modification process simultaneously caused the degradation and aggregation of GEPs. The LSCM results revealed that more SGEP can enter the MCF-7 cell interior compared with AcGEP. The results indicated that the structure of AcGEP could play a dominating role in antitumor activity. The data obtained in this work can be used as a starting point for investigating the structure-bioactivity of GEPs.
Assuntos
Fracionamento por Campo e Fluxo , Gastrodia , Neoplasias , Humanos , Gastrodia/química , Polissacarídeos/farmacologia , Medicina Tradicional Chinesa , Fracionamento por Campo e Fluxo/métodosRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Gastrodia elata Bl. (GE) is one of the rare Chinese medicinal materials with a long history of medicine and cooking. It consists of a variety of chemical components, including aromatic compounds, organic acids and esters, steroids, saccharides and their glycosides, etc., which has medicinal and edible value, and is widely used in various diseases, such as infantile convulsions, epilepsy, tetanus, headache, dizziness, limb numbness, rheumatism and arthralgia. It is also commonly used in health care products and cosmetics. Thus, its chemical composition and pharmacological activity have attracted more and more attention from the scientific community. AIM: In this review, the processing methods, phytochemistry and pharmacological activities of GE were comprehensively and systematically summarized, which provides a valuable reference for researchers the rational of GE. MATERIALS AND METHODS: A comprehensive search of published literature and classic books from 1958 to 2023 was conducted using online bibliographic databases PubMed, Google Scholar, ACS, Science Direct Database, CNKI and others to identify original research related to GE, its processing methods, active ingredients and pharmacological activities. RESULTS: GE is traditionally used to treat infantile convulsion, epilepsy, tetanus, headache, dizziness, limb numbness, rheumatism and arthralgia. To date, more than 435 chemical constituents were identified from GE including 276 chemical constituents, 72 volatile components and 87 synthetic compounds, which are the primary bioactive compounds. In addition, there are other biological components, such as organic acids and esters, steroids and adenosines. These extracts have nervous system and cardiovascular and cerebrovascular system activities such as sedative-hypnotic, anticonvulsant, antiepileptic, neuron protection and regeneration, analgesia, antidepressant, antihypertensive, antidiabetic, antiplatelet aggregation, anti-inflammatory, etc. CONCLUSION: This review summarizes the processing methods, chemical composition, pharmacological activities, and molecular mechanism of GE over the last 66 years, which provides a valuable reference for researchers to understand its research status and applications.
Assuntos
Epilepsia , Gastrodia , Tétano , Humanos , Etnofarmacologia , Fitoterapia , Gastrodia/química , Tontura/tratamento farmacológico , Hipestesia/tratamento farmacológico , Tétano/tratamento farmacológico , Epilepsia/tratamento farmacológico , Anticonvulsivantes/farmacologia , Anticonvulsivantes/uso terapêutico , Cefaleia/tratamento farmacológico , Artralgia/tratamento farmacológico , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/química , Extratos Vegetais/farmacologiaRESUMO
BACKGROUND: Cyclophosphamide (CTX) is a widely used chemotherapeutic agent for the treatment of malignant tumors and autoimmune diseases. However, it can cause immunosuppression and damage the intestinal mucosa. The development of new agents to counteract these side effects is becoming increasingly important. Previous studies have shown that the polysaccharides from Gastrodia elata (GEPs) have strong immune-enhancing effects; however, their functions regarding the intestines and the underlying mechanism are still unclear. In this study, the effects of GEPs on immunomodulatory activity, intestinal barrier function, and gut microbiota regulation were investigated in a mouse model of CTX-induced immunosuppression. RESULTS: Gastrodia elata polysaccharides attenuated the CTX-induced decrease in organ indices of the thymus and spleen, and promoted the secretion of immune-related cytokines and immunoglobulins in the serum. They also improved the intestinal pathology and restored the intestinal barrier function by elevating the expression of intestinal tight junction proteins, occludin and ZO-1. Moreover, GEPs restored the composition and abundance of the gut microbiota and increased the short-chain fatty acid (SCFA) content in the colon. The abundance of SCFA-producing bacteria (Muribaculaceae, Prevotellaceae, and Bacteroidaceae) also increased. CONCLUSIONS: Gastrodia elata polysaccharides can effectively alleviate immunosuppression and regulate the intestinal barrier integrity and the structure of gut microbiota in CTX-treated mice. They may be used as ingredients to develop functional foods for intestinal health. © 2023 Society of Chemical Industry.
Assuntos
Gastrodia , Microbioma Gastrointestinal , Camundongos , Animais , Gastrodia/química , Ciclofosfamida/efeitos adversos , Intestinos , Polissacarídeos/farmacologia , Polissacarídeos/químicaRESUMO
As both a traditional medicine and food material, fresh Gastrodia elata requires a curing process for quality improvement. The effects of steaming and various drying methods (sun-, hot-air-, microwave-vacuum-, freeze- and vacuum-drying) on the total phenolic, total flavonoid, ascorbic acid, adenosine, and phenolic compound contents, antioxidant activities (scavenging DPPHâ¢, ABTS+â¢, OH⢠and reducing power) and microstructures were investigated in this study. The contents of adenosine and individual phenolic compounds were analyzed using high-performance liquid chromatography. The results showed that steaming had adverse effects on the total phenolic, total flavonoid, adenosine, parishin C, vanillyl alcohol, quercetin and cinnamic acid contents, while subsequent hot-air- and freeze-drying showed compensatory effects. Steaming significantly increased the levels of gastrodin, p-hydroxybenzylalcohol, p-hydroxybenzaldehyde, parishins (A, B and E) and catechin (by 3.4-, 1.1-, 1.1-, 3.8-, 6-, 1.4- and 1.5-fold, respectively, p < 0.05) compared to the fresh samples, which were further increased by hot-air- and freeze-drying. Hot-air- and freeze-drying significantly increased the levels of adenosine, gastrodin, p-hydroxybenzylalcohol, p-hydroxybenzaldehyde, parishins (A, B and C), vanillyl alcohol, catechin, caffeic acid, quercetin and cinnamic acid by 1.1-11.6-fold (p < 0.05) compared to steaming treatment. Steaming reduced all the antioxidant activities, which were restored partially by hot-air- and freeze-drying. Principal component and clustering analyses revealed the relationship among the samples, phenolics, and antioxidant activities, which suggested a steaming-then-drying action mechanism in which steaming changes enzymes and starch hydrolysis and drying promote condensation reactions. Collectively, steaming-then-hot-air- or freeze-drying is a promising method for enhancing the quality of Gastrodia elata for food applications.
Assuntos
Catequina , Gastrodia , Adenosina , Antioxidantes/química , Gastrodia/química , Fenóis , Extratos Vegetais/química , Quercetina , VaporRESUMO
As an important active ingredient in the rare Chinese herb Gastrodiae Rhizoma and also the main precursor for gastrodin biosynthesis, 4-hydroxybenzyl alcohol has multiple pharmacological activities such as anti-inflammation, anti-tumor, and anti-cerebral ischemia. The pharmaceutical products with 4-hydroxybenzyl alcohol as the main component have been increasingly favored. At present, 4-hydroxybenzyl alcohol is mainly obtained by natural extraction and chemical synthesis, both of which, however, exhibit some shortcomings that limit the long-term application of 4-hydroxybenzyl alcohol. The wild and cultivated Gastrodia elata resources are limited. The chemical synthesis requires many steps, long time, and harsh reaction conditions. Besides, the resulting by-products are massive and three reaction wastes are difficult to treat. Therefore, how to artificially prepare 4-hydroxybenzyl alcohol with high yield and purity has become an urgent problem facing the medical researchers. Guided by the theory of microbial metabolic engineering, this study employed the genetic engineering technologies to introduce three genes ThiH, pchF and pchC into Escherichia coli for synthesizing 4-hydroxybenzyl alcohol with L-tyrosine. And the fermentation conditions of engineering strain for producing 4-hydroxybenzyl alcohol in shake flask were also discussed. The experimental results showed that under the conditions of 0.5 mmol·L~(-1) IPTG, 15 â induction temperature, and 40 â transformation temperature, M9 Y medium containing 200 mg·L~(-1) L-tyrosine could be transformed into(69±5)mg·L~(-1) 4-hydroxybenzyl alcohol, which has laid a foundation for producing 4-hydroxybenzyl alcohol economically and efficiently by further expanding the fermentation scale in the future.
Assuntos
Gastrodia , Engenharia Metabólica , Álcoois Benzílicos , Escherichia coli/genética , Escherichia coli/metabolismo , Gastrodia/química , Tirosina/metabolismoRESUMO
Parishin compounds are rare polyphenolic glucosides mainly found in the rhizome of the traditional Chinese medicinal plant, Gastrodia elata. These constituents are reported to have several biological and pharmacological activities. In the present study, two novel parishin derivatives not previously reported as plant-based phytochemicals were identified from a twig of Maclura tricuspidata (MT) and two new compounds were elucidated as 1-(4-(ß-d-glucopyranosyloxy)benzyl)-3-hydroxy-3-methylpentane-1,5-dioate (named macluraparishin E) and 1,3-bis(4-(ß-d-glucopyranosyloxy)benzyl)-3-hydroxy-3-methylpentane- 1,5-dioate (macluraparishin C), based on the experimental data obtained by UV-Visible (UV-Vis) spectroscopy, high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (HPLC-QTOF-MS) and nuclear magnetic resonance (NMR) spectroscopy. Additionally, gastrodin, parishin A and parishin B were positively identified by spectroscopic evidence and the comparison of HPLC retention time with the corresponding authentic standards. Gastrodin, parishin A and parishin B, macluraparishin E and macluraparishin C were found to be the most abundant constituents in the MT twig. The compositions and contents of these constituents were found to vary depending on the different parts of the MT plant. In particular, the contents of parishin A, parishin B, macluraparishin C and macluraparishin E were higher in the twig, bark and root than in the leaves, xylem and fruit.
Assuntos
Gastrodia , Maclura , Plantas Medicinais , Extratos Vegetais/química , Plantas Medicinais/química , Cromatografia Líquida de Alta Pressão/métodos , Gastrodia/químicaRESUMO
Atherosclsis is a critical actuator causing cardiac-cerebral vascular disease with a complicated pathogeneon, refered to the disorders of intestinal flora and persistent inflammation. Gastrodin (4-(hydroxymethyl) phenyl-ß-D- Glucopyranoside) is the most abundant glucoside extracted from the Gastrodiaelata, which is a traditional Chinese herbal medicine for cardiac-cerebral vascular disease, yet its mechanisms remain little known. In the present study, the gastrodia extract and gastrodin attenuate the lipid deposition and foam cells on the inner membrane of the inner membrane of the thoracic aorta in the early atherosclerosis mice. Blood lipid detection tips that TC and LDL-C were reduced in peripheral blood after treatment with the gastrodia extract and gastrodin. Furthermore, unordered gut microbes are remodeled in terms of bacterial diversity and abundance at family and genus level. Also, the intestinal mucosa damage and permeability were reversed, accompaniedwith the reducing of inflammatory cytokines. Our findings revealed that the functions of gastrodia extract and gastrodin in cardiac-cerebral vascular disease involved to rescued gut microbes and anti-inflammation may be the mechanismof remission lipid accumulation.
Assuntos
Aterosclerose/tratamento farmacológico , Medicamentos de Ervas Chinesas/farmacologia , Gastrodia/química , Microbioma Gastrointestinal/efeitos dos fármacos , Inflamação/tratamento farmacológico , Ácido Acético/metabolismo , Animais , Aorta/efeitos dos fármacos , Aorta/metabolismo , Aorta/patologia , Aterosclerose/microbiologia , Aterosclerose/patologia , Álcoois Benzílicos/farmacologia , Álcoois Benzílicos/uso terapêutico , Ácido Butírico/metabolismo , Modelos Animais de Doenças , Ácidos Graxos Voláteis/metabolismo , Microbioma Gastrointestinal/genética , Glucosídeos/farmacologia , Glucosídeos/uso terapêutico , Inflamação/microbiologia , Molécula 1 de Adesão Intercelular/sangue , Interleucina-1beta/sangue , Mucosa Intestinal/efeitos dos fármacos , Mucosa Intestinal/patologia , Lipídeos/sangue , Camundongos Endogâmicos C57BL , Propionatos/metabolismo , Proteínas de Junções Íntimas/metabolismo , Fator de Necrose Tumoral alfa/sangueRESUMO
BACKGROUND: Gastrodiae Rhizoma (Tianma), the dried tuber of Gastrodia elata Bl. (Orchidaceae), is listed as a top-grade herbal medicine in Shen-nong Ben-ts'ao Jing and has been used for treating headaches, dizziness, vertigo and convulsion. It has a neuroprotective effect and extends the lifespan in mouse models of Huntington's disease and Niemann-Pick type C disease. However, its effect on senescence remains unknown. PURPOSE: This study aimed to investigate the anti-aging effects and the underlying mechanism of Gastrodiae Rhizoma. METHODS: D-galactose (D-gal)- and BeSO4-induced cellular senescence and senescence-associated ß-galactosidase (SA-ß-gal) activity were evaluated in SH-SY5Y and PC12 cells. D-gal-induced aging mice were used as an in vivo model. Animal behaviors including nesting and burrowing and Morris water maze were conducted. Neurogenesis in the hippocampus was assessed by immunohistochemistry and confocal microscopy, and the aging-related proteins were assessed by Western blot analysis. The potential neuritogenesis activity of the partially purified fraction of Gastrodiae Rhizoma (TM-2) and its major ingredients were investigated in PC12 cells. RESULTS: TM-2 could improve D-gal-induced learning and memory impairement by inhibiting oxidative stress, increasing hippocampal neurogenesis and regulating the SH2B1-Akt pathway. Moreover, N6-(4-hydroxybenzyl)adenine riboside (T1-11) and parishins A and B, three constituents of TM-2, had anti-aging activity, as did T1-11 and parishin A induced neuritogenesis. CONCLUSION: Our data suggested that TM-2 slowed down D-gal-induced cellular and mouse brain aging. These results indicate that Gastrodiae Rhizoma has a beneficial effect on senescence. It may be used for neuroprotection and promoting neurogenesis.
Assuntos
Envelhecimento/efeitos dos fármacos , Senescência Celular/efeitos dos fármacos , Gastrodia/química , Hipocampo/efeitos dos fármacos , Rizoma/química , Animais , Comportamento Animal/efeitos dos fármacos , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas/farmacologia , Galactose , Hipocampo/citologia , Hipocampo/fisiologia , Masculino , Camundongos , Neurogênese/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Células PC12 , RatosRESUMO
According to the previously described anti-photoaging effect of the enzyme-processed Panax ginseng extract and Gastrodia elata extract, we hypothesized that the combination of the two extracts would have superior effect to protect human skin from UVB radiation. Besides, the mixture of active components isolated from herbal extracts, ginsenoside F2, and α-gastrodin was investigated on the photo-protective capability. The expression of aging-related markers including matrix metalloproteinase-1 (MMP-1), interleukin-6 (IL-6), and procollagen type 1 was evaluated using ELISA kits. It was reported that the herbal extract at a Panax ginseng extract to Gastrodia elata extract ratio of 1:10 (w/w) and the compound mixture with equal proportion of ginsenoside F2 and α-gastrodin exhibited significant inhibition of MMP-1 and IL-6 production, and marked upregulation of procollagen type 1 formation. Thus, the combination of either the enzyme-processed herbal extracts or their active components would enhance the properties of prevention and treatment of UVB-induced skin damage.
Assuntos
Colágeno Tipo I/metabolismo , Fibroblastos/efeitos dos fármacos , Gastrodia/química , Interleucina-6/metabolismo , Metaloproteinase 1 da Matriz/metabolismo , Panax/química , Extratos Vegetais/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Fibroblastos/citologia , Fibroblastos/metabolismo , Fibroblastos/efeitos da radiação , Humanos , Protetores contra Radiação/farmacologia , Pele/citologia , Raios Ultravioleta/efeitos adversosRESUMO
Gastrodiae Rhizoma is a highly valuable traditional herbal medicine commonly used to treat neurological disorders. The present study is designed to determine the antidepressant-like effect of the Gastrodiae Rhizoma water extract (GRWE) on a depression model and the potential mechanisms. The chronic unpredictable mild stress (CUMS) rat model was used to induce depression. The sucrose preference test, open field test, forced swimming test, and tail suspension test were performed to assess the depressive-like behaviors, respectively. Hypothalamic-pituitary-adrenal (HPA) function was measured via plasma corticosterone (CORT), adrenocorticotrophic hormone (ACTH), hypothalamic corticotropin-releasing factor (CRF), and glucocorticoid receptor (GR) concentrations. Plasma concentrations of proinflammatory cytokines including interleukin-1ß (IL-1ß), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α) were also evaluated. The results showed that GRWE significantly attenuates the behavioral abnormalities in CUMS rats, as shown by elevated sucrose consumption, raised locomotor activity, and reduced immobility duration. Moreover, GRWE treatment reduced CORT, ACTH, CRF, and GR levels and decreased the plasma IL-1ß, IL-6, and TNF-α concentrations. These findings indicate that GRWE improves depressive behaviors in a chronic stress model of rats; its effect may be ascribed to the modulation of the HPA axis activity and inflammatory response.
Assuntos
Medicamentos de Ervas Chinesas/farmacologia , Sistema Hipotálamo-Hipofisário/efeitos dos fármacos , Inflamação/metabolismo , Sistema Hipófise-Suprarrenal/efeitos dos fármacos , Estresse Psicológico/metabolismo , Animais , Comportamento Animal/efeitos dos fármacos , Doença Crônica , Citocinas/metabolismo , Modelos Animais de Doenças , Gastrodia/química , Masculino , Ratos , Ratos Sprague-DawleyRESUMO
Aging is a natural human process. It is uniquely individual, taking into account experiences, lifestyle habits and environmental factors. However, many disorders and syndromes, such as osteoporosis, neurodegenerative disorders, cognitive decline etc., often come with aging. The present study was designed to investigate the possible anti-aging effect of N6-(4-hydroxybenzyl)adenine riboside (T1-11), an adenosine analog isolated from Gastrodia elata, in a mouse model of aging created by D-galactose (D-gal) and the underlying mechanism, as well as explore the role of adenosine signaling in aging. T1-11 activated A2AR and suppressed D-gal- and BeSO4-induced cellular senescence in vitro. In vivo results in mice revealed that T1-11 abated D-gal-induced reactive oxygen species generation and ameliorated cognitive decline by inducing neurogenesis and lowering D-gal-caused neuron death. T1-11 could be a potent agent for postponing senility and preventing aging-related neuroinflammation and neurodegeneration.
Assuntos
Adenosina/análogos & derivados , Adenosina/metabolismo , Envelhecimento/efeitos dos fármacos , Disfunção Cognitiva/prevenção & controle , Hipocampo/efeitos dos fármacos , Adenosina/administração & dosagem , Envelhecimento/imunologia , Animais , Senescência Celular/efeitos dos fármacos , Senescência Celular/imunologia , Disfunção Cognitiva/imunologia , Disfunção Cognitiva/patologia , Modelos Animais de Doenças , Galactose/administração & dosagem , Galactose/toxicidade , Gastrodia/química , Hipocampo/citologia , Hipocampo/imunologia , Hipocampo/patologia , Humanos , Masculino , Camundongos , Neurogênese/efeitos dos fármacos , Neurogênese/imunologia , Neurônios/efeitos dos fármacos , Neurônios/imunologia , Neurônios/patologia , Estresse Oxidativo/efeitos dos fármacos , Estresse Oxidativo/imunologia , Espécies Reativas de Oxigênio/metabolismoRESUMO
An investigation of a co-culture of the Armillaria sp. and endophytic fungus Epicoccum sp. YUD17002 associated with Gastrodia elata led to the isolation of eight new compounds, including five protoilludane-type sesquiterpenes (1-5) and three aryl esters (6-8), together with six known analogues (9-14). The assignments of their structures were conducted via extensive analyses of the spectroscopic data and comparison of experimental and calculatedelectronic circular dichroism(ECD)data. Notably, these new compounds were not present in the pure culture controls and were only detected in the co-cultures. Compound 4 is the first example of an ent-protoilludane sesquiterpenoid scaffold bearing a five-membered lactone. Compound 6 exhibited moderate in vitro cytotoxic activities against five human cancer cell lines (HL-60, A549, MCF-7, SMMC-7721, and SW480) with IC50 values ranging from 15.80 to 23.03 µM. Moreover, 6 showed weak acetylcholinesterase inhibitory activity (IC50 value of 23.85 µM).
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Armillaria/química , Ascomicetos/química , Inibidores da Colinesterase/farmacologia , Técnicas de Cocultura , Gastrodia/química , Sesquiterpenos Policíclicos/farmacologia , Acetilcolinesterase/metabolismo , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/isolamento & purificação , Proliferação de Células/efeitos dos fármacos , Inibidores da Colinesterase/química , Inibidores da Colinesterase/isolamento & purificação , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Estrutura Molecular , Sesquiterpenos Policíclicos/química , Sesquiterpenos Policíclicos/isolamento & purificação , Relação Estrutura-Atividade , Células Tumorais CultivadasRESUMO
Grifola frondosa (hen of the woods or maitake) is a famous culinary-medicinal mushroom, and its exopolysaccharides (EPSs) have biological activities with or without supplementation with exogenous additives. In this study, a Rhizoma gastrodiae extract was added to a G. frondosa fermentation system. P-hydroxylbenzaldehyde (HBA), the main product of R. gastrodiae, had the highest utilization rate in the fermentation process (42%). In addition, the EPSs of G. frondosa after addition of R. gastrodiae extract (REPS), of HBA (HEPS), or of a standard solution according to the main component ratio of R. gastrodiae extract (CEPS) were obtained. We then determined the antioxidant and immunomodulatory activities of EPS, REPS, HEPS, and CEPS. Overall, REPS showed the highest antioxidant activities compared with EPS and HEPS (P < 0.05) but similar to that of CEPS (P > 0.05). The half-inhibitory concentration (ED50) values of REPS (< 4 mg/mL) were lower than those of EPS, HEPS, and CEPS. Moreover, REPS was better able to stimulate phagocytosis and nitric oxide production of RAW 264.7 macrophages than were the others, without a significant difference from CEPS (P > 0.05). An interesting and important finding is that a R. gastrodiae extract can increase antioxidant and immunomodulatory activities of EPS preparations from G. frondosa, and the standard solution of the main components of the R. gastrodiae extract may be better for simulating fermentation performed by G. frondosa and biological activities of its major products.
Assuntos
Antioxidantes/farmacologia , Polissacarídeos Fúngicos/farmacologia , Gastrodia/química , Grifola/química , Fatores Imunológicos/farmacologia , Extratos Vegetais/farmacologia , Agaricales , Animais , Antioxidantes/isolamento & purificação , Citocinas/metabolismo , Fermentação , Polissacarídeos Fúngicos/isolamento & purificação , Fatores Imunológicos/isolamento & purificação , Macrófagos/efeitos dos fármacos , Camundongos , Fagocitose/efeitos dos fármacos , Extratos Vegetais/isolamento & purificação , Células RAW 264.7RESUMO
The present study aimed to evaluate the antimicrobial activity and the possible mechanisms of activity of polypeptideenriched Gastrodia elata extracts (GEP) against the gramnegative bacteria Escherichia coli and Pseudomonas aeruginosa, the grampositive bacterium Staphylococcus aureus and the fungus Candida albicans. The antimicrobial activity of GEP was first confirmed by determining the minimum inhibitory concentration by growth curve analysis. GEP was found to damage the cell wall and membrane of the microorganisms tested, as revealed by the morphological changes visible through scanning electron microscopy, and by the observed leakage of alkaline phosphatase and ßgalactosidase from cells. GEP was demonstrated to perturb the metabolism of the microorganisms, especially the tricarboxylic acid cycle, as indicated by the reduced intracellular activity of succinate dehydrogenase, malate dehydrogenase and ATPases, including the Na+/K+ATPase and the Ca2+ATPase. In addition, GEP caused the leakage of the genetic material of the bacteria and the fungus, as indicated by the increased OD260. The results of the present study indicated that GEP may exert its antimicrobial activity by damaging cell walls and membranes, causing the leakage of genetic material, and by perturbing cellular metabolism.
Assuntos
Anti-Infecciosos , Peptídeos Catiônicos Antimicrobianos , Bactérias/metabolismo , Candida albicans/metabolismo , Gastrodia/química , Proteínas de Plantas , Anti-Infecciosos/química , Anti-Infecciosos/metabolismo , Anti-Infecciosos/farmacologia , Peptídeos Catiônicos Antimicrobianos/química , Peptídeos Catiônicos Antimicrobianos/metabolismo , Peptídeos Catiônicos Antimicrobianos/farmacologia , Proteínas de Bactérias/metabolismo , Membrana Celular/metabolismo , Parede Celular/metabolismo , Proteínas Fúngicas/metabolismo , Proteínas de Plantas/química , Proteínas de Plantas/metabolismo , Proteínas de Plantas/farmacologiaRESUMO
Aim: The primary objective of this study was to evaluate the effects of polypeptide-enriched Gastrodia elata extracts (GE) on vulvovaginal candidiasis (VVC). Materials & methods: A VVC model induced by Candida albicans (C. albicans) infection was successfully developed in BALB/c mice. After treatment, the colony-forming unit (CFU) of vaginal lavage was measured by plating. The extent of the inflammatory response was assessed by hematoxylin-eosin (H&E) staining and enzyme-linked immunosorbent assay (ELISA). Results: GE had an inhibitory effect on the proliferation of C. albicans and inflammatory reaction. Meanwhile, it had a potentially beneficial effect on the growth of Lactobacillus. Conclusion: These results showed the potential application of GE as an antifungal agent in VVC treatment.
Assuntos
Candida albicans/efeitos dos fármacos , Candidíase Vulvovaginal/tratamento farmacológico , Gastrodia/química , Peptídeos/farmacologia , Peptídeos/uso terapêutico , Animais , Antifúngicos/química , Antifúngicos/farmacologia , Antifúngicos/uso terapêutico , Candida albicans/crescimento & desenvolvimento , Candidíase Vulvovaginal/sangue , Candidíase Vulvovaginal/microbiologia , Candidíase Vulvovaginal/patologia , Modelos Animais de Doenças , Feminino , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Inflamação/patologia , Interleucinas/sangue , Interleucinas/metabolismo , Camundongos Endogâmicos BALB C , Peptídeos/química , Resultado do Tratamento , Vagina/metabolismo , Vagina/microbiologia , Vagina/patologiaRESUMO
Gastrodia elata Blume (G. elata) is a valuable Traditional Chinese Medicine (TCM) with a wide range of clinical applications. G. elata polysaccharides, as one of the main active ingredients of G. elata, have interesting extraction, purification, qualitative analysis, quantitative analysis, derivatization, and pharmacological activity aspects, yet a review of G. elata polysaccharides has not yet been published. Based on this, this article summarizes the progress of G. elata polysaccharides in terms of the above aspects to provide a basis for their further research and development.
Assuntos
Gastrodia/química , Polissacarídeos/análise , Polissacarídeos/farmacologia , Antineoplásicos/farmacologia , Peso Molecular , Fármacos Neuroprotetores/farmacologia , Polissacarídeos/isolamento & purificaçãoRESUMO
Epilepsy is a group of neurological disorders characterized by recurrent seizures that disturbs about 60 million people worldwide. In this article, a novel series of 3,4,5-trimethoxycinnamic acid (TMCA) ester derivatives 1-35 were designed inspired from the traditional Chinese herb pair drugs Polygala tenuifolia and Gastrodia elata and synthesized followed by in vivo and in silico evaluation of their anticonvulsant potential. All the synthesized derivatives were biologically evaluated for their anticonvulsant potential using two acute model of seizures induced in mice, the maximal electroshock (MES) and sc-pentylenetetrazole (PTZ) models. Simultaneously, the motor impairment as a surrogate of acute neurotoxicity and in vitro screening of cytotoxicity against HepG-2 cells line were assessed through the rotarod performance test and CCK-8 assay, respectively. In addition, the physicochemical and pharmacokinetic parameters of the active compounds were determined. Our results showed that compounds 5, 7, 8, 13, 20, 25, 28, 30 and 32 exhibited preferable anticonvulsant activity in primary evaluation, with compounds 28 and 32 being the most promising anticonvulsant agents in according to results of subsequent pharmacology and toxicity evaluation. Additionally, the molecular modeling experiments predicted good binding interactions of part of the obtained active molecules with the gamma-aminobutyric acid (GABA) transferas. Therefore, it could be concluded that the synthesized derivatives 28 and 32 would represent useful lead compounds for further investigation in the development of anticonvulsant agents.