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Fufang Xiling Jiedu capsule (FXJC), a traditional Chinese medicine that evolved from "Yinqiao Powder", is widely used for the treatment of cold and influenza. However, due to a lack of in vivo metabolism research, the chemical components responsible for the therapeutic effects still remain unclear. Hence, this study aimed to describe the metabolic profiles of the FXJC in rat plasma, urine, and feces. A combined data mining strategy based on ultra-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry was employed and 201 xenobiotics, including 117 prototype components and 84 metabolites were detected. Phenolic acids, flavonoids, triterpenes, and lignans were prominent ingredients absorbed in vivo, and the major metabolic pathways of the detected metabolites were glucuronidation, sulfation, methylation, and oxidation. This is the first systematic study on the metabolism of the FXJC in vivo, providing valuable information for future studies on the efficacy, toxicity, and mechanism of the FXJC.
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Medicamentos de Ervas Chinesas , Espectrometria de Massas em Tandem , Ratos , Animais , Espectrometria de Massas em Tandem/métodos , Ratos Sprague-Dawley , Cromatografia Líquida de Alta Pressão/métodos , Administração Oral , Medicamentos de Ervas Chinesas/análise , MetabolomaRESUMO
Introduction: Traditional Chinese medicine (TCM) has the advantages of syndrome differentiation and rapid determination of etiology, and many TCM prescriptions have been applied to the clinical treatment of coronavirus disease 2019 (COVID-19). Among them, Jinbei Oral Liquid (Jb.L) has also shown an obvious curative effect in the clinic, but the related material basic research is relatively limited. Methods: Therefore, in this process, a systematic data acquisition and mining strategy was established using ultra-high- performance liquid chromatography coupled with quadruple time-of-flight mass spectrometry (UPLC-Q-TOF-MS). Results and Discussion: With the optimized conditions, a total of 118 peaks were tentatively characterized, including 43 flavonoids, 26 phenylpropanoids, 14 glycosides, 9 phthalides, 8 alkaloids and others. To determine the content of relevant pharmacological ingredients, we firstly exploited the ultra-performance liquid chromatography method coupled with triple-quadrupole tandem mass spectrometry (UPLC-QqQ-MS/MS) method for simultaneous detection of 31 active ingredients within 17 min, and the validation of methodology showed that this method has good precision and accuracy. Moreover, analyzing the pharmacology of 31 individual of the medicinal material preliminarily confirmed the efficacy of Jb.L and laid a foundation for an in-depth study of network pharmacology.
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CONTEXT: Zhishi Rhubarb Soup (ZRS) is a traditional Chinese medicine formula used in the clinic to treat acute cerebral infarction (ACI) for many years. However, the exact mechanism of the treatment remains unclear. OBJECTIVE: This study elucidates the multitarget mechanisms underlying the effects of ZRS on ACI using network pharmacology analysis and verify its effect by performing animal experiments. MATERIALS AND METHODS: Using the network pharmacology approach, the multiple components, critical targets and potential mechanisms of ZRS against ACI were investigated. Six herbal names of ZRS and 'acute cerebral infarction' were used as keywords to search the relevant databases. In addition, we established the MCAO model to verify the results of network pharmacology enrichment analysis. ZRS (10 g crude drug/kg) was gavaged once per day for 7 consecutive days beginning 3 h after model establishment. After ZRS treatment, TTC staining, Western blot analysis, IHC and ELISA were conducted to further explore the mechanism of ZRS intervention in ACI. RESULTS: The network pharmacology approach identified 69 key targets, 10 core genes and 169 signalling pathways involved in the treatment of ACI with ZRS. In vivo experiment showed that ZRS treatment significantly reduced cerebral infarction volume (42.76%). It also reduced the expression level of AGE, RAGE and P65; and inhibited the expression of inflammatory MMP-9 and IFN-γ. CONCLUSIONS: This study demonstrated that ZRS improved cerebral ischaemic injury by inhibiting neuroinflammation partly via the AGE-RAGE signalling pathway. It provides a theoretical basis for the clinical application of ZRS in the treatment of ACI.
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Isquemia Encefálica , Medicamentos de Ervas Chinesas , Rheum , Acidente Vascular Cerebral , Animais , Isquemia Encefálica/tratamento farmacológico , Infarto Cerebral/tratamento farmacológico , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Farmacologia em Rede , Acidente Vascular Cerebral/tratamento farmacológicoRESUMO
Vitamin D deficiency has become a widespread public health problem owing to its potential adverse health effects. Generally, the nutritional status of vitamin D depends on sunlight exposure and dietary or supplementary intake. However, recent studies have found that exercise can influence circulating 25(OH)D levels; although, the results have been inconclusive. In this review, we focused on the effect of exercise on circulating vitamin D metabolites and their possible mechanisms. We found that endurance exercise can significantly increase serum 25(OH)D levels in vitamin D-deficient people but has no significant effect on vitamin D-sufficient people. This benefit has not been observed with resistance training. Only chronic endurance exercise training can significantly increase serum 1,25(OH)2D, and the effect may be sex-dependent. Exercise may influence 25(OH)D levels in the circulation by regulating either the vitamin D metabolites stored in tissues or the utilization by target tissues. The effects of exercise on 25(OH)D levels in the circulation may be dependent on many factors, such as the vitamin D nutritional status, exercise type and intensity, and sex. Therefore, further research on the effects and mechanisms of exercise on vitamin D metabolites is required.
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Deficiência de Vitamina D , Vitamina D , Exercício Físico , Humanos , Estado Nutricional , VitaminasRESUMO
BACKGROUND: Stroke has always been a major threat worldwide but is most severe in China, with 2.5 million new stroke cases each year and 7.5 million stroke survivors, placing a heavy burden on the social and national health care systems. Zhishi Rhubarb Soup (ZRS) is a traditional Chinese medicine (TCM) that has been used clinically for many years in China. To explore the potential mechanism of ZRS in the treatment of stroke, liquid chromatography with mass spectrometry (LC-MS) was performed. METHODS: In this study, a quantitative proteomic method with LC-MS was used to analyse the proteomic differences between MACO samples treated with ZRS and those without ZRS treatment. RESULTS: Liquid chromatography with mass spectrometry (LC-MS) analysis led to the identification of 35,006 peptides, with 5160.0 proteins identified and 4094.0 quantified. Significantly differentially expressed proteins were identified through data analysis, and the difference was found to be more than 1.2 times (P < 0.05). The Gene Ontology (GO) analysis provided a summary of the dysregulated protein expression in the biological process (BP), cell component (CC), and molecular function (MF) categories. Proteins related to brain repair, including BDNF, IL-10, IL-6, and TGF-ß, were found to change significantly, partially demonstrating the effectiveness of ZRS to attenuate tissue injury. CONCLUSION: In this study, LC-MS/MS was performed to assess the effects of ZRS on differentially expressed proteins in rats with cerebral infarction. These promising results could help to improve the understanding of the effects of drugs on stroke.
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1. Morin, a natural flavonol, is present in many plants. It has anti-inflammatory and immunomodulatory activities and is often used as an adjuvant treatment for arthritis. Diclofenac sodium is the first-choice drug in the treatment of rheumatoid arthritis. However, the herb-drug interaction (HDI) between morin and diclofenac sodium remains unclear.2. The aim of the present research was to investigate whether and how morin affect the pharmacokinetic profile of diclofenac sodium.3. The enzyme kinetic and pharmacokinetic studies showed that morin significantly accelerated the metabolism and reduced systemic exposure of diclofenac sodium. Interestingly, the effect of morin on the pharmacokinetic profile of diclofenac sodium was not in a dose-dependent manner. Therefore, the effect of morin on P-glycoprotein (P-gp) was further investigated.4. The results implied that the influence mechanism of morin on the pharmacokinetic of diclofenac sodium might be related to CYP2C9 and P-gp. Attention should be paid to the risk of HDI between morin and diclofenac sodium in clinical practice.
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Diclofenaco , Flavonoides , Membro 1 da Subfamília B de Cassetes de Ligação de ATP , Animais , Anti-Inflamatórios não Esteroides , Interações Ervas-Drogas , RatosRESUMO
Diabetes is a group of metabolic disorders with an increased risk of developing cognitive impairment and dementia. The hippocampus in the forebrain contains an abundance of insulin receptors related to cognitive function and plays an important role in the pathophysiology of neurodegenerative disorders. Berberine from traditional Chinese medicine has been used to treat diabetes and diabetic cognitive impairment, although its related mechanisms are largely unknown. In this study, a STZ diabetes rat model feeding with a high-fat diet was used to test the effects of berberine compared with metformin. Oral glucose tolerance and hyperinsulinemic-euglycemic clamp were used for glucose metabolism and insulin resistance. The Morris water maze was used to observe the compound effects on cognitive impairment. Serum and hippocampal [Formula: see text]-amyloid peptide (A[Formula: see text], Tau and phosphorylated Tau protein deposition in the hippocampi were measured. The TUNEL assay was used to detect the neuronal apoptosis, supported by histomorphological changes and transmissional electron microscopy (TEM) image. Our data showed that the diabetic rats had a significantly cognitive impairment. In addition to improving glucose metabolism and reducing insulin resistance, berberine significantly improved the cognitive function in the rat. Berberine also effectively decreased the expression of hippocampal tau protein, phosphorylated Tau, and increased insulin receptor antibodies. Moreover, berberine downregulated the abnormal phosphorylation of A[Formula: see text] and Tau protein and improved hippocampal insulin signaling. The TUNEL assay confirmed that berberine reduced hippocampal neuronal apoptosis supported by TEM. Thus, berberine significantly improved the cognitive function in diabetic rats by changing the peripheral and central insulin resistance. The reduction of neuronal injury, A[Formula: see text] deposition, abnormal phosphorylation of Tau protein, and neuronal apoptosis in the hippocampus were observed as the related mechanisms of action.
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Berberina/farmacologia , Disfunção Cognitiva/tratamento farmacológico , Diabetes Mellitus Experimental/tratamento farmacológico , Metformina/farmacologia , Animais , Apoptose/efeitos dos fármacos , Dieta Hiperlipídica , Modelos Animais de Doenças , Hipocampo/efeitos dos fármacos , Hipoglicemiantes/farmacologia , Resistência à Insulina/fisiologia , Masculino , Ratos , Ratos Sprague-Dawley , Estreptozocina , Proteínas tau/efeitos dos fármacosRESUMO
BACKGROUND: The ZaoRenDiHuang (ZRDH) capsule is widely used in clinical practice and has significant therapeutic effects on insomnia. However, its active ingredients and mechanisms of action for insomnia remain unknown. In this study, network pharmacology was employed to elucidate the potential anti-insomnia mechanisms of ZRDH. METHODS: The potential active ingredients of ZRDH were obtained from the Traditional Chinese Medicine Systems Pharmacology Database. Possible targets were predicted using SwissTargetPrediction tools. The insomnia-related targets were identified using the therapeutic target database, Drugbank database, Online Mendelian Inheritance in Man database, and gene-disease associations database. A compound-target-disease network was constructed using Cytoscape for visualization. Additionally, the protein functional annotation and identification of signaling pathways of potential targets were performed using Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses using the Metascape platform. RESULTS: In this study, 61 anti-insomnia components and 65 anti-insomnia targets of ZRDH were filtered through database mining. The drug-disease network was constructed with five key components. Sixty-five key targets were identified using topological analysis. Docking studies indicated that bioactive compounds could stably bind to the pockets of target proteins. Through data mining and network analysis, the GO terms and KEGG annotation suggested that the neuroactive ligand-receptor interaction, serotonergic synapse CAMP signaling, HIF-1a signaling, and toll-like receptor signaling pathways play vital roles against insomnia. CONCLUSION: The potential mechanisms of ZRDH treatment for insomnia involve multiple components, targets, and pathways. These findings provide a reference for further investigations into the mechanisms underlying ZRDH treatment of insomnia.
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Medicamentos de Ervas Chinesas , Distúrbios do Início e da Manutenção do Sono , Cápsulas , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Humanos , Medicina Tradicional Chinesa , Simulação de Acoplamento Molecular , Distúrbios do Início e da Manutenção do Sono/tratamento farmacológicoRESUMO
Rhizoma coptidis (Huang-lian) and Asian ginseng have been widely used in the treatment of diabetes and other concurrent diseases with apparent effects. This study investigated the effects of the active ingredients of R. coptidis and ginseng, berberine and ginsenoside Rb1, on depression-like behavior in a rat diabetes model. The animal model was established via a high-fat diet and intraperitoneal injection of streptozotocin, while the animal's depression-like behavior was induced via chronic unpredictable mild stress. These experimental rats were divided into four groups: control, depression-like behavior (DLB), metformin plus fluoxetine hydrochloride (M+FH), and berberine plus ginsenoside Rb1 (B+GRb1) groups. Glucose metabolism and insulin resistance were evaluated by oral glucose test and glucose clamp study. Depression-like behavior was evaluated via behavioral analyses, including forced swim, sucrose preference, elevated plus maze, and open-field tests. HE and Nissl staining, plasma cortisol expression of adrenocorticotropic hormone, and brain-derived neurotrophic factor (BDNF) levels were assayed to explore the mechanisms of action. Compared with the control, rats in the DLB group had a significant increase in the levels of blood glucose and depression-like behavior. The B+GRb1 group significantly improved glucose metabolism and insulin resistance, reduced depression-like behavior, downregulated levels of plasma cortisol and adrenocorticotropic hormone under stress, and upregulated BDNF protein expression compared to the DLB rats. HE and Nissl staining data revealed that B+GRb1 protected neurons from pathological and morphological changes. Thus, berberine and ginsenoside Rb1 not only improved glucose metabolism in diabetic rats but also ameliorated their depression-like behavior under chronic unpredictable stress. Mechanistically, studied data with plasma hormonal levels and brain neuronal pathological/morphological changes supported the observed effects. The combination of berberine and ginsenoside Rb1 may have a clinical value in the management of diabetic patients with depression.
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Berberina/farmacologia , Depressão/tratamento farmacológico , Diabetes Mellitus Experimental/tratamento farmacológico , Ginsenosídeos/farmacologia , Medicina Tradicional Chinesa/métodos , Animais , Glicemia/efeitos dos fármacos , Dieta Hiperlipídica , Quimioterapia Combinada , Resistência à Insulina , Masculino , Ratos , Ratos Sprague-Dawley , EstreptozocinaRESUMO
BACKGROUND: It is well known that Alzheimer's disease (AD) is a progressive neurodegenerative disease characterized by memory deficits and cognitive decline. Amyloid-ß (Aß) deposition and synaptic dysfunction play important roles in the pathophysiology of Alzheimer's disease (AD). The Huatuo Zaizao pill (HT) is a Traditional Chinese Medicine (TCM) that has been used clinically for many years in China, mainly for post-stroke rehabilitation and cognitive decline; however, the mechanism of cognitive function is not clear. In this study, we investigated the effect of HT on hippocampal synaptic function, Amyloid-ß (Aß) deposition in APP/PS1 AD transgenic mice. METHOD: Six-month-old APP/PS1 transgenic (Tg) mice were randomly divided into control, HT-treated, and memantine (MEM)-treated groups. Then, these groups were orally administered vehicle (for the control), HT (0.25 g/kg) and MEM (5 mg/kg) respectively for 4 weeks. The Morris water maze, Novel Object Recognition, and Open field tests were used to assess cognitive behavioral changes. We evaluated the effects of HT on neuronal excitability, membrane ion channel activity, and synaptic plasticity in acute hippocampal slices by combining electrophysiological extracellular tests. Synaptic morphology in the hippocampus was investigated by electron microscopy. Western blotting was used to assess synaptic-associated protein and Aß production and degrading levels. Immunofluorescence staining was used to determine the relative integrated density. RESULTS: HT can ameliorate hippocampus-dependent memory deficits and improve synaptic dysfunction by reversing LTP impairment in APP/PS1 transgenic mice. Moreover, HT reduces amyloid plaque deposition by regulating α-secretase and γ-secretase levels. CONCLUSION: HT can improve the learning and memory function of APP/PS1 transgenic mice by improving synaptic function and reducing amyloid plaque deposition.
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Doença de Alzheimer/metabolismo , Peptídeos beta-Amiloides/metabolismo , Disfunção Cognitiva/metabolismo , Medicamentos de Ervas Chinesas/farmacologia , Plasticidade Neuronal/efeitos dos fármacos , Animais , Comportamento Animal/efeitos dos fármacos , Região CA1 Hipocampal/química , Região CA1 Hipocampal/citologia , Região CA1 Hipocampal/efeitos dos fármacos , Modelos Animais de Doenças , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , Memória/efeitos dos fármacos , Camundongos , Camundongos TransgênicosRESUMO
BACKGROUND: Panaxatriol saponins (PTS), an extract from the traditional Chinese herb Panax notoginseng, which has been used to treat ischemic stroke for many years in China. However, the mechanism underlying the effects of PTS remains unclear. This study aimed to determine whether PTS can protect against ischemic brain injury by promoting angiogenesis and to explore the possible mechanism by which it promotes angiogenesis. METHODS: Middle cerebral artery occlusion (MCAO) was induced in rats, and neurological deficit scores and brain infarct volumes were assessed. Micro-Positron emission tomography (PET) was adopted to assess cerebral perfusion, and real-time PCR and western blotting were used to evaluate vascular growth factor and Sonic hedgehog (Shh) pathway component levels. Immunofluorescence staining was used to determine capillary densities in ischemic penumbrae. RESULTS: We showed that PTS improved neurological function and reduced infarct volumes in MCAO rats. Micro-PET indicated that PTS can significantly increase 18F-fluorodeoxyglucose (18F-PDG) uptake by ischemic brain tissue and enhance cerebral perfusion after MCAO surgery. Moreover, PTS was able to increase capillary densities and enhance angiogenesis in ischemic boundary zones and up-regulate vascular endothelial growth factor (VEGF) and Angiopoietin-1 (Ang-1) expression by activating the Shh signaling pathway. CONCLUSION: These findings indicate that PTS exerts protective effects against cerebral ischemic injury by enhancing angiogenesis and improving microperfusion.
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Circulação Cerebrovascular/efeitos dos fármacos , Ginsenosídeos/uso terapêutico , Neovascularização Fisiológica/efeitos dos fármacos , Fitoterapia , Acidente Vascular Cerebral/tratamento farmacológico , Proteínas Angiogênicas/metabolismo , Animais , Isquemia Encefálica/tratamento farmacológico , Proliferação de Células/efeitos dos fármacos , Córtex Cerebral/efeitos dos fármacos , Córtex Cerebral/metabolismo , Avaliação Pré-Clínica de Medicamentos , Células Endoteliais/efeitos dos fármacos , Ginsenosídeos/farmacologia , Proteínas Hedgehog/metabolismo , Masculino , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Distribuição Aleatória , Ratos Sprague-DawleyRESUMO
Nonalcoholic fatty liver disease (NAFLD) is defined by a nonalcohol relevant pathological accumulation of fat in the liver. Previous studies have shown that sesamin exerts antioxidant effects and improves lipid metabolism of the fatty liver. In this study, we hypothesized that sesamin improves lipid homeostasis of Sprague-Dawley rats fed a high-fat diet (HFD) by regulating the expression of genes related to de novo lipogenesis and ß-oxidation. We induced NAFLD in rats with HFD and examined the effect of sesamin in vivo. The results showed that HFD rats accumulated total cholesterol and triacylglycerols in the liver and developed inflammation, as evidenced by the elevation of interleukin-6 and tumor necrosis factor-α in the liver and serum. Sesamin attenuated the disease progression by improving the blood lipid profile in a dose-dependent manner. Sesamin reduced the serum levels of total cholesterol, triacylglycerols, low-density lipoprotein cholesterol, and free fatty acid, whereas it increased the level of high-density lipoprotein cholesterol. Meanwhile, sesamin increased the activities of hepatic glutathione peroxidase and superoxide dismutase while reducing the level of malonaldehyde and cytochrome P450 2E1. Furthermore, higher doses of sesamin reduced the expression of liver X receptor α and its downstream target genes, whereas it upregulated the peroxisome proliferator-activated receptor α-mediated signaling. These findings suggest that sesamin attenuates diet-induced dyslipidemia and inflammation of NAFLD in rats via mechanisms regulated by liver X receptor α and peroxisome proliferator-activated receptor α.
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Dioxóis/uso terapêutico , Inflamação/tratamento farmacológico , Lignanas/uso terapêutico , Metabolismo dos Lipídeos/efeitos dos fármacos , Receptores X do Fígado/metabolismo , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , PPAR alfa/metabolismo , Sesamum/química , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Citocromo P-450 CYP2E1/metabolismo , Dieta Hiperlipídica/efeitos adversos , Dioxóis/farmacologia , Dislipidemias/tratamento farmacológico , Dislipidemias/etiologia , Dislipidemias/metabolismo , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico , Inflamação/sangue , Inflamação/etiologia , Interleucina-6/sangue , Lignanas/farmacologia , Metabolismo dos Lipídeos/genética , Lipídeos/sangue , Lipogênese/efeitos dos fármacos , Lipogênese/genética , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Hepatopatia Gordurosa não Alcoólica/etiologia , Hepatopatia Gordurosa não Alcoólica/metabolismo , Hepatopatia Gordurosa não Alcoólica/patologia , Estresse Oxidativo/efeitos dos fármacos , Fitoterapia , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos Sprague-Dawley , Fator de Necrose Tumoral alfa/sangueRESUMO
Flowering plant sperm cells transcribe a divergent and complex complement of genes. To examine promoter function, we chose an isopentenyltransferase gene known as PzIPT1. This gene is highly selectively transcribed in one sperm cell morphotype of Plumbago zeylanica, which preferentially fuses with the central cell during fertilization and is thus a founding cell of the primary endosperm. In transgenic Arabidopsis (Arabidopsis thaliana), PzIPT1 promoter displays activity in both sperm cells and upon progressive promoter truncation from the 5'-end results in a progressive decrease in reporter production, consistent with occurrence of multiple enhancer sites. Cytokinin-dependent protein binding motifs are identified in the promoter sequence, which respond with stimulation by cytokinin. Expression of PzIPT1 promoter in sperm cells confers specificity independently of previously reported Germline Restrictive Silencer Factor binding sequence. Instead, a cis-acting regulatory region consisting of two duplicated 6-bp Male Gamete Selective Activation (MGSA) motifs occurs near the site of transcription initiation. Disruption of this sequence-specific site inactivates expression of a GFP reporter gene in sperm cells. Multiple copies of the MGSA motif fused with the minimal CaMV35S promoter elements confer reporter gene expression in sperm cells. Similar duplicated MGSA motifs are also identified from promoter sequences of sperm cell-expressed genes in Arabidopsis, suggesting selective activation is possibly a common mechanism for regulation of gene expression in sperm cells of flowering plants.
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Alquil e Aril Transferases/genética , Arabidopsis/genética , Regulação da Expressão Gênica de Plantas/genética , Proteínas de Plantas/genética , Pólen/genética , Sequências Reguladoras de Ácido Nucleico/genética , Arabidopsis/citologia , Arabidopsis/metabolismo , Citocininas/farmacologia , Regulação da Expressão Gênica de Plantas/efeitos dos fármacos , Proteínas de Fluorescência Verde/genética , Proteínas de Fluorescência Verde/metabolismo , Microscopia Confocal , Mutação , Motivos de Nucleotídeos/genética , Reguladores de Crescimento de Plantas/farmacologia , Plantas Geneticamente Modificadas , Plumbaginaceae/genética , Pólen/citologia , Regiões Promotoras Genéticas/genética , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Sítio de Iniciação de TranscriçãoRESUMO
A total of 11 phenolic compounds, as well as sucrose (12) and tryptophan (13), were isolated from cold-pressed Perilla frutescens var. arguta seed flour using column chromatography, and their chemical structures were identified as 3'-dehydroxyl-rosmarinic acid-3-o-glucoside (1), rosmarinic acid-3-o-glucoside (2), rosmarinic acid (3), rosmarinic acid methyl ester (4), luteolin (5), luteolin-5-o-glucoside (6), apigenin (7), caffeic acid (8), caffeic acid-3-o-glucoside (9), vanillic acid (10) and cimidahurinine (11) using NMR and time-of-flight mass spectrometry. Of these components, compound 1 is novel, and this is the first report of compounds 10 and 11 in perilla seeds. HPLC quantification combined with antioxidant activity evaluation revealed that rosmarinic acid and rosmarinic acid-3-o-glucoside were the dominant phenolic antioxidants with strong antioxidant activities.
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Antioxidantes/química , Farinha/análise , Manipulação de Alimentos/métodos , Perilla frutescens/química , Fenóis/química , Extratos Vegetais/química , Sementes/química , Cromatografia Líquida de Alta Pressão , Temperatura BaixaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Cyclocarya paliurus Batal., a Chinese native plant, is the sole species in its genus and its leaves have been widely used as a remedy for diabetes in traditional folk medicine. The study was undertaken to evaluate the effects of Cyclocarya paliurus leaves extracts (CPE) on adipokine expression and insulin sensitivity in mice. MATERIALS AND METHODS: Mice were stimulated with conditioned medium (prepared from activated macrophages, Mac-CM) to induce adipose dysfunction and insulin resistance. Then mice were treated with CPE (100, 200 and 500 mg/kg, ig.) or metformin (200 mg/kg, ig.), followed by glucose and insulin intolerance, adipokine expression, phosphorylation of insulin receptor substrate (IRS-1) and glucose consumption measurement. RESULTS: CPE, as well as metformin effectively promoted glucose disposal in oral glucose tolerance test in normal mice. Mac-CM challenge induced glucose and insulin intolerance, but CPE reversed these alternations with increased glycogen content in muscle and liver, well demonstrating its beneficial effects on glucose homeostasis. RT-qPCR analysis showed that CPE inhibited TNF-a, IL-6, MCP-1 and resistin overexpression and effectively enhanced adiponectin expression in adipose tissue when mice were exposed to Mac-CM stimulation. Inflammation impaired insulin signaling in muscle, whereas CPE inhibited inflammation-induced serine phosphorylation of IRS-1 and effectively restored the phosphorylation of both IRS-1 at tyrosine residues and downstream Akt phosphorylation in response to insulin. Moreover, independently of insulin, CPE promoted glucose consumption in adipocytes under normal and inflammatory conditions. CONCLUSION: Above-mentioned results demonstrated that CPE beneficially regulated adipokines expression and ameliorated insulin resistance through inhibition of inflammation in mice.
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Adipocinas/biossíntese , Medicamentos de Ervas Chinesas/farmacologia , Regulação da Expressão Gênica , Resistência à Insulina/fisiologia , Células 3T3 , Animais , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Medicamentos de Ervas Chinesas/uso terapêutico , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Masculino , Camundongos , Folhas de PlantaRESUMO
The Chinese formula Tang-Min-Ling (TML), an improved product of the decoction of Dachaihu which has a history of more than 2000 years, has main constituents of Coptis chinensis Franch, Scutellaria baicalensis Georgi, Rheum officinale Baill and Bupleurum chinense DC. A multi-central randomized controlled investigation performed previously by us has showed that TML has positive effects on regulating glycometabolism in type 2 diabetes (T2DM) patients, but the mechanisms remain unclear. Using Otsuka Long-Evans Tokushima Fatty (OLETF) rats as an animal model with rosiglitazone as a positive control, we were able to detect TML's effect on the serum glucose, serum lipid, serum leptin and adiponcetin after oral administration for 12 weeks. We were also able to detect the insulin resistance level by a glucose clamp test and study the mechanisms of TML in improving insulin resistance by detecting skeletal muscle AMP-activated protein kinase (AMPK) and glucose transporter 4 (GLUT4). Results showed that TML significantly reduced the glucose area under a curve of the oral glucose tolerance test, and had a positive effect in regulating serum lipid metabolism. TML treatment also significantly reduced the serum leptin level, but it had no effect on the serum adiponectin level. The AMPK enzymatic activity and GLUT4 expression in Skeletal Muscle were also upregulated in the TML group. The results suggest that the Chinese medicine TML, which contains Coptis chinensis Franch as one of its components, improves glycometabolism and its possible mechanisms may involve in improvement of insulin resistance of OLETF rats.
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Coptis/química , Diabetes Mellitus Tipo 2/terapia , Medicamentos de Ervas Chinesas/farmacologia , Hiperlipidemias/tratamento farmacológico , Hipoglicemiantes/farmacologia , Resistência à Insulina , Fitoterapia , Proteínas Quinases Ativadas por AMP/metabolismo , Adiponectina/sangue , Animais , Área Sob a Curva , Glicemia/metabolismo , Bupleurum/química , Diabetes Mellitus Tipo 2/sangue , Medicamentos de Ervas Chinesas/uso terapêutico , Teste de Tolerância a Glucose , Transportador de Glucose Tipo 4/metabolismo , Hiperlipidemias/sangue , Hipoglicemiantes/uso terapêutico , Leptina/sangue , Metabolismo dos Lipídeos/efeitos dos fármacos , Lipídeos/sangue , Músculo Esquelético/metabolismo , Ratos , Ratos Endogâmicos OLETF , Rheum/química , Rosiglitazona , Scutellaria baicalensis/química , Tiazolidinedionas/farmacologia , Tiazolidinedionas/uso terapêuticoRESUMO
OBJECTIVE: To study the chemical constituents from flowers of Koelreuteria paniculata. METHODS: Column chromatography and spectral analysis were used to isolate and identify the constituents. RESULTS: The EtOAc fraction from flowers of Koelreuteria paniculata was separated and purified. Nine compounds were obtained and identified as:sitosterol glucoside (I), gallic acid (II), kaempferol (III), luteolin (IV), kaempferol-3-O-(6"-acetyl)-beta-D-glucopyranoside (V), hyperoside-2"-O-acetyl (VI), hyperoside-2"-O-galloyl (VII), hyperoside (VIII), kaempferol-3-O-D-glucopyranoside (IX). CONCLUSION: Nine compounds are isolated for the first time from flowers of Koelreuteria paniculata. Compounds IV, V, VI and IX are isolated from this genus for the first time.
Assuntos
Flavonoides/isolamento & purificação , Flores/química , Plantas Medicinais/química , Sapindaceae/química , Flavonoides/química , Ácido Gálico/química , Ácido Gálico/isolamento & purificação , Quempferóis/química , Quempferóis/isolamento & purificação , Luteolina/química , Luteolina/isolamento & purificação , Espectroscopia de Ressonância Magnética , Estrutura Molecular , Quercetina/análogos & derivados , Quercetina/química , Quercetina/isolamento & purificação , Sitosteroides/química , Sitosteroides/isolamento & purificaçãoRESUMO
Combining unique macro-fingerprint characteristics of infrared spectroscopy (IR) with the overall concept of traditional Chinese medicine (TCM) theory, the authors seek to establish a new, rapid and economic method for research on Chinese herb preparation (CHP), which could reflect the whole and integration concept of TCM theory and also be widely applied in TCM research. In the present paper, four coptidis-evodia couples, e.g. Zuo-jin-wan (coptidis : evodia = 6 : 1), Gan-lu-san (coptidis : evodia = 2 : 1), Zhu-yu-wan (coptidis : evodia = 1 : 1) and Fan-zuo-jin (coptidis : evodia = 1 : 6), were extracted by boiling water and 80% alcohol, and the FTIR spectra of those CHPs were compared and analyzed in detail. The characteristic absorbance bands of coptidis and evodia were assigned in the FTIR spectra of the four coptidis-evodia couples. The results showed that rhizoma coptidis owns absolute superiority in both extracts of Zuo-jin-wan and Gan-lu-san since the proportions of rhizoma coptidis in the two couples are higher than those of fructus evodiae. With regard to Zhu-yu-wan, the proportions of two ingredients are the same. However, the contribution rate of coptidis is higher than that of evodiae in water extract of Zhu-yu-wan. In addition, coptidis also shows higher contribution rate than that of evodia in alcohol extract of Fan-zuo-jin. The spectroscopic technique described here is a simple and rapid analytical technique, which could provide valuable chemical information about the whole coptidis-evodia CHPs.
Assuntos
Medicamentos de Ervas Chinesas/química , Evodia/química , Interações Ervas-Drogas , Álcoois/química , Química Farmacêutica , Coptis chinensis , Espectroscopia de Infravermelho com Transformada de Fourier , Água/químicaRESUMO
OBJECTIVE: To study the flavonoids compounds from the effective fraction of Thesium chinese in anti-inflammation. METHODS: The isolation and purification were carried out by many kinds of column chromatographic techniques. The flavonoids were analyzed by HPLC-DAD, and elucidated by 1H-NMR, 13C-NMR and ESI-MS. RESULTS: Five compounds were obtained and therir structures were determined as kaempferol-3-O-glucoside (I), rutinoside (II), luteolin-7-O-glucoside (III), kaempferyl 5-methyl ether (IV), apigenin-5-O-neohesperidoside (V). CONCLUSION: Compounds IV and V are isolated from this plant for the first time.