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The limited application of garlic essential oil (GEO) is attributed to its pungent taste, poor water solubility and low bioavailability. Liposomes are nontoxic, biodegradable and biocompatible, and ß-cyclodextrin can inhibit undesirable odors and improve the stability and bioavailability. Thus a promising dual-layer GEO ß-cyclodextrin inclusion compound liposome (GEO-DCL) delivery system with both advantages was designed and prepared in this study. Experimental results indicated that the encapsulation efficiency of GEO-DCLs was 5% higher than that of GEO liposomes (GEO-CLs), reaching more than 88%. In vitro release experiment showed that the release rate of GEO in GEO-DCLs was 40% lower than that of GEO-CLs after incubation in gastric juice for 6-h, indicating that the stability of GEO-DCLs was better than GEO-CLs. Evaluation of the effects of GEO-DCLs on lowering blood lipid levels in hypercholesterolemia mice. GEO-DCLs could reduce the weight and fat deposition in hypercholesterolemia mice. Inhibiting the increase of TC, LDL-C, and decrease of HDL-C in mice. The degree of liver injury was decreased, the number of round lipid droplets in liver cytoplasm was reduced, and the growth of fat cells was inhibited. The lipid-lowering effects of GEO-DCLs were dose-dependent. GEO-DCL can improve the bioavailability of GEO and improve dyslipidemia. Based on GEO's efficacy in lowering blood lipids, this study developed a kind of GEO-DCL compound pomegranate juice beverage with good taste, miscibility and double effect of reducing blood lipids. This study lays a foundation for the application of GEO in the field of functional food.
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Alho , Hipercolesterolemia , Hiperlipidemias , Óleos Voláteis , beta-Ciclodextrinas , Camundongos , Animais , Lipossomos , Óleos Voláteis/farmacologia , AntioxidantesRESUMO
INTRODUCTION: The traditional Chinese medicine (TCM) Potentilla anserina L. can use both as food and medicine. At present, the market mainly depends on experience to identify the species and determine the production areas of P. anserina. To ensure the quality of P. anserina, it is essential to improve the level of quality control. OBJECTIVE: We aimed to establish a rapid and nondestructive discrimination model to identify P. anserina from different production areas by near-infrared spectroscopy. METHODS: The spectra of complete P. anserina medicinal materials and their powder of the same variety from four production areas were collected, and principal component analysis discriminant analysis and partial least squares discriminant analysis (PLS-DA) were conducted based on different pretreatment methods and band selection methods. Then, the spectra of complete medicinal materials were converted into the spectra of medicinal powder for nondestructive identification. RESULTS: The correct recognition rate (CRR) of the PLS-DA discriminant model was the best after spectral preprocessing using autoscaling and competitive adaptive reweighted sampling for band selection. The CRRs of the calibration set and validation set were 100%, the CRRs of the external test set were 95%, 90%, 82%, and 88%, respectively, and the CRRs of the transfer external test set were 84%, 80%, 82%, and 86%, respectively. CONCLUSION: We realized the nondestructive and effective identification of P. anserina from different origins and laid a foundation for the industrialization and upgrading of TCM.
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Potentilla , Análise de Componente Principal , Espectroscopia de Luz Próxima ao Infravermelho , Potentilla/química , Espectroscopia de Luz Próxima ao Infravermelho/métodos , Análise dos Mínimos Quadrados , Análise Discriminante , Medicina Tradicional Chinesa , Medicamentos de Ervas Chinesas/químicaRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Acute lung injury (ALI) is an aggressive inflammatory disease of the lungs characterized by a high mortality rate. More and more researchers have found that herbal medicines are highly effective in preventing and treating inflammatory lung diseases. Among them, Dachengqi Decoction (DCQD) is considered to be the representative prescription of "lung-intestine combined treatment" in traditional Chinese medicine, and its potential protective mechanism against ALI is worthy of further study. AIM OF THE STUDY: Based on the theory of "lung-intestine combined treatment", the protective effect and molecular mechanism of DCQD in alleviating ALI were verified by network pharmacology and experiments. MATERIALS AND METHODS: The active ingredients of DCQD were obtained by UPLC-MS. Network pharmacology and molecular docking techniques were used to screen the active ingredient-target pathway of DCQD for ALI treatment. Additionally, the ALI model was constructed and verified in vivo according to the predicted results. RESULTS: 34 active components and 570 potential targets of DCQD were selected by network pharmacological analysis. In addition, 950 target genes of ALI and 2095 target genes related to sepsis were obtained, and 570 interlinked target genes of the two were identified. We finally screened out 199 common target genes critical to DCQD treatment of ALI and sepsis, and then enriched them with GO and KEGG. In the ALI model, studies have found that DCQD alleviates the inflammatory response of ALI, possibly by inhibiting HIF-1α-mediated glycolysis. CONCLUSION: This study confirmed the preventive effect of DCQD on ALI, and found that DCQD can improve the protective mechanism of ALI by regulating the expression of HIF-1α, down-regulating glycolysis and reducing inflammation.
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Lesão Pulmonar Aguda , Medicamentos de Ervas Chinesas , Sepse , Humanos , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Simulação de Acoplamento Molecular , Cromatografia Líquida , Espectrometria de Massas em Tandem , Extratos Vegetais/farmacologia , Lesão Pulmonar Aguda/tratamento farmacológico , Sepse/tratamento farmacológicoRESUMO
Colorectal cancer (CRC) is the most prevalent cancer of the digestive tract. Herba Patriniae (also known as Bai Jiang Cao, HP) have been widely used to manage diarrhea, ulcerative colitis, and several cancers, including CRC. Nonetheless, the molecular mechanisms underlying the pharmacological action of HP on CRC remain unclear. This study investigated the underlying mechanisms of HP against CRC using network pharmacology analysis and in vitro and in vivo experiments. The results revealed nine bioactive compounds of HP. Furthermore, 3460 CRC-related targets of the identified active compounds were predicted from the Gene Expression Omnibus (GEO) database. Furthermore, 65 common targets were identified through the intersection of two related targets. Moreover, ten hub genes, including CDK4, CDK2, CDK1, CCND1, CCNB1, CCNA2, MYC, E2F1, CHEK1, and CDKN1A were identified through the topological analysis. Meanwhile, the GO and KEGG pathway analysis revealed that the core target genes were majorly enriched in the p53 and HIF-1 signaling pathways. Moreover, HP promoted apoptosis and suppressed cell proliferation by activating the p53 signaling pathway in a dose-dependent manner, while a similar effect was observed for Isovitexin (the primary component of HP). Overall, this study provides valuable insights into the underlying mechanisms of HP and its component Isovitexin against CRC, providing a theoretical foundation for additional experimental verification of its clinical application.
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Neoplasias Colorretais , Medicamentos de Ervas Chinesas , Proteína Supressora de Tumor p53 , Apoptose , Pontos de Checagem do Ciclo Celular , Genes cdc , Proteína Supressora de Tumor p53/genética , Neoplasias Colorretais/tratamento farmacológico , Neoplasias Colorretais/patologia , Humanos , Medicamentos de Ervas Chinesas/farmacologia , Antineoplásicos Fitogênicos/farmacologiaRESUMO
Species of genus Morus (family Moraceae) have been used as traditional medicinal and edible resources since ancient times. Genus Morus has been acknowledged as a promising resource for the exploration of novel compounds with various bioactivities. Phytochemical investigations of the genus have led to the discovery of more than approximately 453 natural products from 2011 to 2023, mainly including flavonoids, Diels-Alder adducts, 2-arylbenzfuran, alkaloids and stilbenes. Bioactive constituents and extracts of this genus displayed a wide range of impressive biological properties including antidiabetic, anti-inflammatory, antioxidant, anti-cancer, hepatoprotective, renoprotective, and some other activities. Herein, the research progress of this genus Morus from 2011 to 2023 on phytochemistry and pharmacology are systematically presented and discussed for the first time. This current review provides the easiest access to the information on genus Morus for readers and researchers in view of enhancing the continuity on research done on this genus.
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Produtos Biológicos , Morus , Plantas Medicinais , Morus/química , Produtos Biológicos/farmacologia , Plantas Medicinais/química , Extratos Vegetais/química , Flavonoides/farmacologia , Compostos Fitoquímicos/farmacologia , Etnofarmacologia , FitoterapiaRESUMO
BACKGROUND: The incidence of colorectal cancer and cancer death rate are increasing every year, and the affected population is becoming younger. Traditional Chinese medicine therapy has a unique effect in prolonging survival time and improving the prognosis of patients with colorectal cancer. Oridonin has been reported to have anti-cancer effects in a variety of tumors, but the exact mechanism remains to be investigated. METHODS: Cell Counting Kit-8 assay (CCK8) and 5-Ethynyl-2'-deoxyuridine (EdU) staining assay, Tranwell, and Wound healing assays were performed to measure cell proliferation, invasion, and migration capacities, respectively. The protein and mRNA expression levels of various molecules were reflected by Western blot and Reverse Transcription quantitative Polymerase Chain Reaction (qRT-PCR). Transcription Factor 4 (TCF4) and its target genes were analyzed by Position Weight Matrices (PWMs) software and the Gene Expression Omnibus (GEO) database. Immunofluorescence (IF) was performed to visualize the expression and position of Endoplasmic Reticulum (ER) stress biomarkers. The morphology of the ER was demonstrated by the ER tracker-red. Reactive Oxygen Species (ROS) levels were measured using a flow cytometer (FCM) or fluorescent staining. Calcium ion (Ca2+) concentration was quantified by Fluo-3 AM staining. Athymic nude mice were modeled with subcutaneous xenografts. RESULTS: Oridonin inhibited the proliferation, invasion, and migration of colorectal cancer, and this effect was weakened in a concentration-dependent manner by ER stress inhibitors. In addition, oridonin-induced colorectal tumor cells showed increased expression of ER stress biomarkers, loose morphology of ER, increased vesicles, and irregular shape. TCF4 was identified as a regulator of ER stress by PWMs software and GEO survival analysis. In vitro and in vivo experiments confirmed that TCF4 inhibited ER stress, reduced ROS production, and maintained Ca2+ homeostasis. In addition, oridonin also activated TP53 and inhibited TCF4 transactivation, further exacerbating the elevated ROS levels and calcium ion release in tumor cells and inhibiting tumorigenesis in colorectal cancer cells in vivo. CONCLUSIONS: Oridonin upregulated TP53, inhibited TCF4 transactivation, and induced ER stress dysregulation in tumor cells, promoting colorectal cancer cell death. Therefore, TCF4 may be one of the important nodes for tumor cells to regulate ER stress and maintain protein synthesis homeostasis. And the inhibition of the TP53/TCF4 axis plays a key role in the anti-cancer effects of oridonin.
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Apoptose , Neoplasias Colorretais , Animais , Camundongos , Humanos , Fator de Transcrição 4/genética , Espécies Reativas de Oxigênio/metabolismo , Cálcio/metabolismo , Camundongos Nus , Ativação Transcricional , Linhagem Celular Tumoral , Neoplasias Colorretais/tratamento farmacológico , Neoplasias Colorretais/genética , Neoplasias Colorretais/metabolismo , Estresse do Retículo Endoplasmático , Proliferação de Células , Proteína Supressora de Tumor p53/metabolismoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Astragali Radix (AR) is the dry root of the leguminous plants Astragalus membranaceus (Fisch) Beg. var. mongholicus (Beg) Hsiao, and Astragalus membranaceus (Fisch) Bge., being used as a medicinal and edible resource. AR is used in traditional Chinese medicine prescriptions to treat hyperuricemia, but this particular effect is rarely reported, and the associated mechanism of action is still need to be elucidated. AIM OF THE STUDY: To research the uric acid (UA)-lowering activity and mechanism of AR and the representative compounds through the constructed hyperuricemia mouse and cellular models. MATERIALS AND METHODS: In our study, the chemical profile of AR was analysed by UHPLC-QE-MS, as well as the mechanism of action of AR and the representative compounds on hyperuricemia was studied through the constructed hyperuricemia mouse and cellular models. RESULTS: The main compounds in AR were terpenoids, flavonoids and alkaloids. Mice group treated with the highest AR dosage showed significantly lower (p < 0.0001) serum uric acid (208 ± 9 µmol/L) than the control group (317 ± 11 µmol/L). Furthermore, UA increased in a dose-dependence manner in urine and faeces. Serum creatinine and blood urea nitrogen standards, as well as xanthine oxidase in mice liver, decreased (p < 0.05) in all cases, indicating that AR could relieve acute hyperuricemia. UA reabsorption protein (URAT1 and GLUT9) was down-regulated in AR administration groups, while the secretory protein (ABCG2) was up-regulated, indicating that AR could promote the excretion of UA by regulating UA transporters via PI3K/Akt signalling pathway. CONCLUSION: This study validated the activity, and revealed the mechanism of AR in reducing UA, which provided experimental and clinical basis for the treatment of hyperuricemia with it.
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Medicamentos de Ervas Chinesas , Hiperuricemia , Camundongos , Animais , Ácido Úrico , Hiperuricemia/tratamento farmacológico , Hiperuricemia/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Medicamentos de Ervas Chinesas/química , Proteínas de Membrana TransportadorasRESUMO
Swertia mussotii Franch. (SMF), a traditional Tibetan medicine, which has miraculous effect on treating hepatitis diseases. However, there is no research on its entire production process, and invisible production process has seriously hindered the SMF modern development. In this study, principal component analysis (PCA), subtractive spectroscopy, and two-dimensional correlation spectroscopy (2D-COS) were used to explain changes of characteristic groups in the extraction process. Four main characteristic peaks at 1884 nm, 1944 nm, 2246 nm and 2308 nm were identified to describe the changes of molecular structure information of total active components in SMF extraction process. In addition, multi critical quality attributes (CQAs) models were established by near-infrared spectroscopy (NIRS) combined with the total quantum statistical moment (TQSM). The coefficients of determination (R2eval and R2ival) were both greater than 0.99. The ratios of the standard deviation of validation to the standard error of the prediction (RPDe and RPDi) were greater than five. The quantitative model of AUCT could save time on primary data measurement by not requiring determination of indicator components compared with others. In conclusion, these results demonstrated that it was feasible to understand the SMF extraction process through AUCT and characteristic groups. These could realize the visual digital characterization and quality stability of the SMF extraction process.
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Swertia , Swertia/química , Espectroscopia de Luz Próxima ao InfravermelhoRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Sijunzi Decoctionï¼SJZDï¼, as a famous classical prescription for the treatment of colorectal cancer(CRC) in the traditional Chinese medicine (TCM), has achieved good curative effects in clinical practice. However, its specific ingredients and molecular mechanisms is still unclear. AIM OF THE STUDY: To analyze the effective ingredients and molecular mechanisms of SJZD in the treatment of CRC through network pharmacology technology and experimental validation. MATERIALS AND METHODS: First, the TCM Systems Pharmacology database and analysis platform database were searched to screen the effective chemical components of SJZD. Swiss Target Prediction was used to predict corresponding potential target genes of compounds. After that, we constructed a components and corresponding target network by Cytoscape. Simultaneously, 5 disease databases were used to search and filter CRC targets, and then we constructed a drug-disease target protein-protein interaction (PPI) network. Cytoscape 3.7 was used for visualization and cluster analysis, and Metascape database was used for GO and KEGG enrichment analysis. We drew the main pathway-target network diagram. Autodock vina1.5.6 was applied to molecular docking for the main compounds and target proteins. Subsequently, the potential mechanism of SJZD on colon cancer predicted by network pharmacological analysis was experimentally studied and verified in vivo and in vitro. RESULTS: 144 effective active chemical components, 897 potential targets, and 2584 CRC target genes were screened out. The number of common targets between the SJZD and CRC was 414.3250 GO biological process items and 186 KEGG signal pathways were obtained after analysis. The main compounds and the target protein had a good binding ability in molecular docking. The results of cell and animal experiments showed that SJZD could promote apoptosis and autophagy of CRC cells through PI3K/Akt/mTOR pathway. CONCLUSIONS: SJZD can treat CRC through multiple components, multiple targets and multiple pathways. We initially revealed the effective components and molecular mechanisms of SJZD in the treatment of CRC, and we used molecular docking and experiment for preliminary verification.
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Neoplasias do Colo , Medicamentos de Ervas Chinesas , Animais , Simulação de Acoplamento Molecular , Farmacologia em Rede , Fosfatidilinositol 3-Quinases , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Medicina Tradicional ChinesaRESUMO
Background: Colorectal cancer (CRC) is a common digestive tract malignancy with rising incidence and morbidity worldwide during recent years. Yi-Yi-Fu-Zi-Bai-Jiang-San (YYFZBJS), a traditional Chinese medicine formula, has showed positive effects against cancers. However, the mechanisms underlying its anticancer effects requires investigation. Methods: Information on bioactive compounds, potential YYFZBJS targets, and CRC-associated genes, was obtained from public databases. The key targets and ingredients as well their corresponding signaling pathways were identified using bioinformatic approaches, including Kyoto encyclopedia of genes and genomes (KEGG) analyses, gene ontology (GO), and protein-protein interaction (PPI). Subsequently, molecular docking was used to verify the main compounds-targets. Potential YYFZBJS therapeutic effects against CRC were validated in vitro and in vivo. Results: Using pharmacological network analysis, 40 YYFZBJS active compounds and 21 potential anti-CRC targets were identified. YYFZBJS was an important regulator of CRC through various targets and signaling pathways, particularly the cell cycle and PI3K/AKT pathway. Additionally, YYFZBJS suppressed the proliferation of CRC cells. Flow cytometry showed that YYFZBJS induced apoptosis and cell cycle arrest in the G2/M phase. Western blotting analysis indicated that YYFZBJS reduced the protein levels of CDK1, p-AKT, and p-PI3K, without altering total PI3K and AKT protein levels. In vivo analysis found that YYFZBJS inhibited tumor growth and PI3K/AKT signaling in a mouse model of CRC. Conclusion: As predicted by network pharmacology and validated by the experimental results, YYFZBJS inhibited proliferation, induced apoptosis and arrested cell cycle progression in CRC by modulating the CDK1/PI3K/Akt signaling pathway.
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Good sleep quality is essential for maintaining the body's attention during wakefulness, which is easily affected by external factors such as an ambient temperature. However, the mechanism by which an ambient temperature influences sleep-wake behaviors remains unclear. The dorsomedial hypothalamus (DMH) has been reported to be involved in thermoregulation. It also receives projection from the preoptic area, which is an important region for sleep and energy homeostasis and the suprachiasmatic nucleus-a main control area of the clock rhythm. Therefore, we hypothesized that the DMH plays an important role in the regulation of sleep related to ambient temperatures. In this study, we found that cold exposure (24/20/16/12 °C) increased wakefulness and decreased non-rapid eye movement (NREM) sleep, while warm exposure (32/36/40/44 °C) increased NREM sleep and decreased wakefulness compared to 28 °C conditions in wild-type mice. Then, using non-specific and specific apoptosis, we found that lesions of whole DMH neurons and DMH γ-aminobutyric acid (GABA)-ergic neurons induced by caspase-3 virus aggravated the fluctuation of core body temperature after warm exposure and attenuated the change in sleep-wake behaviors during cold and warm exposure. However, chemogenetic activation or inhibition of DMH GABAergic neurons did not affect the sleep-wake cycle. Collectively, our findings reveal an essential role of DMH GABAergic neurons in the regulation of sleep-wake behaviors elicited by a change in ambient temperature.
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Neurônios GABAérgicos/metabolismo , Hipotálamo/metabolismo , Sono/fisiologia , Animais , Regulação da Temperatura Corporal/fisiologia , Temperatura Baixa , Núcleo Hipotalâmico Dorsomedial , Neurônios GABAérgicos/fisiologia , Temperatura Alta , Hipotálamo Médio/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Qualidade do Sono , Sono REM , Temperatura , Vigília/fisiologiaRESUMO
Obesity has been reported to be associated with gut microbiome dysbiosis. seabuckthorn fruits have traditionally been used in Tibetan foods and medicines for thousands of years. Seabuckthorn polysaccharide (SP) is one of the main functional components in seabuckthorn fruits. However, the effects of SP on a high-fat diet (HFD)-induced obesity have not yet been elucidated. The purpose of this study is to explore the amelioration effect of SP on obesity induced by HFD and to reveal its mechanism of gut microbiota and its metabolites. Results showed that 12-week SP (0.1%, w/w) dietary supplementation could significantly reduce body weight gain, serum lipid level and liver triglycerides level in obese mice. Notably, the SP treatment elevated p-AMPKα and PPARα proteins expression stimulated the phosphorylation of ACC1 and inhibited the protein expression of FAS, PPARγ, and CD36 in the mice liver. Further, SP also reorganized the gut microbiome by up-regulating the proportion of Muribaculaceae_unclassified, Bifidobacterium, Rikenellaceae_RC9_gut_group, Alistipes, and Bacteroides, and down-regulating the abundance of Lactobacillus, Firmicutes_unclassified, Dubosiella Bilophila, and Streptococcus in HFD-induced obese mice. Moreover, the production of microbial metabolites short-chain fatty acids (SCFAs) in feces has also increased. In addition, correlation analysis results showed that obesity-ameliorating effects of SP were highly associated with levels of SCFAs in feces. Therefore, the regulation of SP on liver lipid metabolism may be due to the variation of the gut microbiome and raised production of SCFAs. These results indicate that SP could play the part of a potential nutraceutical for ameliorating obesity through regulation of the gut-liver axis.
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Fármacos Antiobesidade/farmacologia , Suplementos Nutricionais , Hippophae , Polissacarídeos/farmacologia , Animais , Fármacos Antiobesidade/administração & dosagem , Fármacos Antiobesidade/química , Dieta Hiperlipídica , Modelos Animais de Doenças , Microbioma Gastrointestinal/efeitos dos fármacos , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/prevenção & controle , Polissacarídeos/administração & dosagem , Polissacarídeos/química , Aumento de Peso/efeitos dos fármacosRESUMO
As an important method to accurately and timely diagnose stroke and study physiological characteristics and pathological mechanism in it, imaging technology has gone through more than a century of iteration. The interaction of cells densely packed in the brain is three-dimensional (3D), but the flat images brought by traditional visualization methods show only a few cells and ignore connections outside the slices. The increased resolution allows for a more microscopic and underlying view. Today's intuitive 3D imagings of micron or even nanometer scale are showing its essentiality in stroke. In recent years, 3D imaging technology has gained rapid development. With the overhaul of imaging mediums and the innovation of imaging mode, the resolution has been significantly improved, endowing researchers with the capability of holistic observation of a large volume, real-time monitoring of tiny voxels, and quantitative measurement of spatial parameters. In this review, we will summarize the current methods of high-resolution 3D imaging applied in stroke.
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Encéfalo/irrigação sanguínea , Imageamento Tridimensional/métodos , Acidente Vascular Cerebral/diagnóstico por imagem , Animais , Meios de Contraste/química , HumanosRESUMO
Young Prunus persica fruits (YPF) contain substances that are distinct from those found in the mature fruits. Response surface methodology was used to explore the influences of extraction conditions including ultrasonic time (X1), ethanol proportion (X2), liquid-to-solid ratio (X3) and temperature (X4) on UV-absorbing components from YPF. To purify the extract, the adsorption/desorption properties of 280 nm-absorbing components on AB-8 resin were investigated. A total of 11 metabolites (amino acids, glycosylated amino acids and phenolics) were identified in the UV-absorbing fraction of YPF (YPF-F) based on LC-MS/MS assays. In a study of in vivo anti-inflammatory activity, YPF-F significantly decreased the number of inflammatory cells that migrated to the lateral line location in CuSO4-induced transgenic fluorescent zebrafish. YPF should be utilized as a high value resource of functional foods.[Formula: see text].
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Prunus persica , Aminoácidos/análise , Animais , Cromatografia Líquida , Etanol/análise , Frutas/química , Extratos Vegetais/química , Prunus persica/química , Espectrometria de Massas em Tandem , Peixe-ZebraRESUMO
Panax quinquefolius, a popular medicinal herb, has been cultivated in China for many years. In this work, the region-specific profiles of metabolites in P. quinquefolius from Wendeng was investigated using liquid-chromatography-quadrupole-time-of-flight-(LC-Q-TOF)-based metabolomics analysis. The three most abundant biomarkers, identified as ginsenoside Rb3, notoginsenoside R1, and ginsenoside Rc, were the representative chemical components employed in the network pharmacology analysis. In addition, molecular docking and western blotting analyses revealed that the three compounds were effective binding ligands with Hsp90α, resulting in the inactivation of SRC and PI3K kinase, which eventually led to the inactivation of the Akt and ERK pathways and lung cancer suppression. The outcomes obtained herein demonstrated the intriguing chemical characteristics and potential functional activities of P. quinquefolius from Wendeng.
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Adenocarcinoma de Pulmão/tratamento farmacológico , Adenocarcinoma de Pulmão/metabolismo , Biomarcadores/metabolismo , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/metabolismo , Panax/química , Células A549 , Linhagem Celular Tumoral , China , Cromatografia Líquida de Alta Pressão/métodos , Ginsenosídeos/química , Ginsenosídeos/farmacologia , Humanos , Metabolômica/métodos , Simulação de Acoplamento Molecular/métodos , Raízes de Plantas/química , Plantas Medicinais/química , Saponinas/química , Saponinas/farmacologiaRESUMO
Objectives: Early-life stress and polyunsaturated fatty acids (PUFAs) have profound effects on brain development. Polyunsaturated fatty acids (PUFAs) are essential nutrients and normal components for development. The aims of this study are to investigate the effects of maternal deprivation (MD) stress and maternal dietary of n-3 PUFAs on the physical and neurobiological developments of offspring.Methods: According to the content of n-3 PUFAs in diets, female dams were divided into three groups (n = 6-7): deficiency, control and supplementary. MD paradigm was performed 6 h a day from postnatal days (PND) 1 to PND 14. The physical parameters and neurobehavioral tests were measured.Results: Different effects of MD stress, maternal diet and time on physical and neurobehavioral developments were observed. There was an interaction among stress, diet and time on body weight. MD stress markedly decreased weight among different diet groups, while deficiency diet significantly increased weight on PND 21 in N-MD pups and on PND 14 in MD pups. Moreover, MD stress delayed fur appearance and eye opening, whereas deficiency diet accelerated eye opening. On cliff avoidance and rearing frequency, MD pups performed worse; however a subtle delay on the surface righting was observed in supplementary group. Additionally, MD pups performed worse on PND 14 in forelimb grip. Unfortunately, there were no significant effects on incisor eruption, locomotion frequency and negative geotaxis.Discussion: This study suggests that early MD and inadequate intake of n-3 PUFAs are harmful to optimal growth and neurobehavioral development.
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Ácidos Graxos Ômega-3 , Privação Materna , Animais , Dieta , Ácidos Graxos Insaturados , Feminino , Masculino , Ratos , Ratos WistarRESUMO
Extraction process is not only a critical manufacturing unit but also the initial process of various extracts and preparations. Taking the most extensive Chinese herbal medicine Danshen (Salvia miltziorrhiza Bge) as an example, salvianolic acid B (Sal B) is its main active pharmaceutical ingredient but lacks accurate characterization of the extraction process. As one of process analytical technologies, near-infrared spectroscopy (NIRS) technology has been widely applied for monitoring pharmaceutical extraction process. In most past studies, water spectral information is often eliminated due to its high absorption. However, this study proposed a method of using water spectrum to understand the whole extraction process and to quickly determine the content of Sal B. Principal component analysis (PCA) was first utilized to investigate the whole extraction process, then the reconstructed spectrum based on PCA was established and analyzed by Aquaphotomics, and finally the partial least squares regression (PLSR) quantitative model of Sal B was established. PCA and Aquaphotomics results showed the whole extraction process could be considered as a dynamic change from structure breaker to structure maker, and the dominance of highly H-bonded water structures increases with the extraction time. Also, the Sal B quantitative model with water spectrum showed higher accuracy and stability than other methods, which parameters (RMSEC, RMSECV, RMSEP, R2c, R2cv, R2p, RPD) were 0.2408 mg/mL, 0.2939 mg/mL, 0.2584 mg/mL, 0.9536, 0.9300, 0.9494, 4.6298, respectively, and the paired t-test showed that Sal B content measured by NIR and HPLC methods had no significant differences (p > 0.05). In conclusion, all result indicated that water can be used as a probe to understand the traditional Chinese medicine extraction process with NIRS.
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Medicamentos de Ervas Chinesas , Salvia miltiorrhiza , Medicina Tradicional Chinesa , Espectroscopia de Luz Próxima ao Infravermelho , ÁguaRESUMO
INTRODUCTION: Gastroesophageal reflux is a physiologic occurrence in infants. Clinicians caring for neonates use histamine-2 receptor antagonists (H2As) or proton pump inhibitors (PPIs) for symptomatic reflux, apnea/bradycardia/desaturations, or irritability. Recent studies have shown that there is an increased incidence of infection, fracture, and mortality in neonates who receive antacids. METHODS: A multidisciplinary team aimed to decrease nonindicated antacid use in the NICU by 50% by April 2019. Outcome measures include the median number of inappropriate antacid prescriptions and patient-days on acid-suppressants. Interventions include education regarding use and risks of antacids, development of a list of indications deemed "appropriate" for starting an H2A or PPI, mandatory discussion on rounds when considering antacids, documentation of treatment goal, and indication, and an automatic drop-off in the electronic medical record. RESULTS: Baseline data (June-December 2017) showed 19 prescriptions of H2As or PPIs. Of those, 10 orders were deemed "inappropriate," according to our indicated uses. There were 407 total patient-days of medication-use (median: 51 patient-days). After the implementation of the interventions (October 2018-May 2019), there were 11 prescriptions of antacid medications, 3 of which were deemed "inappropriate." There were 206 total days of medication-use (median: 18.5 patient-days). CONCLUSIONS: A multidisciplinary agreement on indications for antacid use in neonates stimulates discussion and creates more purposeful use. Overall, we successfully decreased nonindicated antacid prescriptions in the NICU. For the next steps, we hope to educate physicians on the risks of antacid use and reduce prescriptions in other areas of the hospital and the outpatient setting.
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ETHNOPHARMACOLOGICAL RELEVANCE: Acanthus ilicifolius L. has been used as a folk medicine in the treatment of acute and chronic hepatitis in China for a long time. Phenylethanoid glycosides are one of main components in A. ilicifolius L. AIM OF THE STUDY: The aim of present study was to assess the hepatoprotective activities of total phenylethanoid glycosides from A. ilicifolius L. (APhGs) against carbon tetrachloride (CCl4)-induced liver injury in vivo and in vitro. MATERIALS AND METHOD: The APhGs was separated by resin column chromatography. The purity of total phenylethanoid glycosides was determined by UV-Vis spectrophotometry using acteoside as a standard. The hepatoprotective activities of APhGs against CCl4-induced liver injury were performed on experimental mice and L-02 hepatocytes. Moreover, the antioxidant activities of APhGs were tested in vitro. RESULTS: The results showed that pre-administration of APhGs to mice decreased alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels in serum, and improved superoxide dismutase (SOD) activity and decreased malondialdehyde (MDA) level in serum and liver tissue induced by CCl4. Specifically, the SOD activities of APhGs-H and APhGs-M treatment groups were stronger than that of silymarin treatment group. The protective activities of APhGs were confirmed by histopathological results. Moreover, immunohistochemical analysis showed that APhGs could remarkably down-regulate the protein expression of tumor necrosis factor-α (TNF-α) and interleukin-1ß (IL-1ß). In vitro experiment, APhGs was observed to increase L-02 hepatocyte viability against CCl4-induced hepatotoxicity. In addition, antioxidation assays revealed that APhGs showed 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, and ferric reducing ability. CONCLUSION: Overall, total phenylethanoid glycosides from A. ilicifolius L. displayed promising hepatoprotective effects. These results offer a support for the medicine uses of A. ilicifolius L.
Assuntos
Acanthaceae/química , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Glicosídeos/farmacologia , Fígado/efeitos dos fármacos , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Alanina Transaminase/metabolismo , Animais , Antioxidantes/farmacologia , Aspartato Aminotransferases/metabolismo , Tetracloreto de Carbono/farmacologia , Doença Hepática Induzida por Substâncias e Drogas/metabolismo , China , Feminino , Glucosídeos/farmacologia , Glutationa/metabolismo , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Fígado/metabolismo , Masculino , Malondialdeído/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , Fenóis/farmacologiaRESUMO
Le-Cao-Shi (LCS), a formula of Traditional Chinese Medicine (TCM), has been used as a folk medicine for protection and treatment of liver injury. However, scientific evidences on its hepatoprotective effects have not been investigated. In this study, hepatoprotective activities of LCS water extracts (LCS-W) and ethanol extracts (LCS-E) against carbon tetrachloride (CCl4)-induced liver damage were investigated in vivo and in vitro. In vivo experiments, pretreatment of LCS-W and LCS-E to rats significantly declined the levels of serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST), and markedly increased the activity of superoxide dismutase (SOD) and ameliorated the level of malondialdehyde (MDA) induced by CCl4 treatment. Especially, LCS-WM group significantly prevented the elevation of lipid peroxidation level induced by CCl4, with the MDA level closed to that of normal group. Histopathological examinations further confirmed that LCS-W and LCS-E could protect the liver cells from CCl4-induced damage. In addition, immunohistochemically analysis revealed that LCS-W could significantly down-regulated the hepatic protein expression of necrosis factor-α (TNF-α) and interleukin-1ß (IL-1ß). Correspondingly, LCS-W and LCS-E were observed to promote cell viability and decline the levels of ALT, AST, and lactate dehydrogenase (LDH) in vitro. It could be concluded that LCS can exert a protective effect against CCl4-induced hepatotoxicity, which might be a potential therapeutic prescription for preventing or treating liver injury. Notably, LCS-W displayed better hepatoprotective activity against CCl4-induced injury than that of LCS-E, suggesting that LCS extracted by water decoction has good development prospects. Our results contribute towards the validation of the traditional use of LCS in the treatment of liver disorders.