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Angelicae Dahuricae Radix (ADR) holds a prominent place in traditional medicine for its remarkable antioxidative, anti-allergic, and antiproliferative capabilities. Recognized within the Korean Pharmacopoeia (KP 12th), Angelica dahurica (Hoffm.) Benth. and Hook.f. ex Franch. and Sav. (AD) and Angelica dahurica var. formosana (H. Boissieu) Yen (ADF) serve as the botanical origins for ADR. Differentiating these two varieties is crucial for the formulation and quality control of botanical drugs, as they are categorized under the same medicinal label. This research utilized two-dimensional high-performance thin-layer chromatography (2D-HPTLC) to effectively distinguish AD from ADF. Additionally, a quantitative analysis reveals significant differences in the concentrations of key active constituents such as oxypeucedanin, imperatorin, and isoimperatorin, with AD showing higher total coumarin levels. We further enhanced our investigative depth by incorporating a DPPH bioautography, which confirmed known antioxidant coumarins and unearthed previously undetected antioxidant profiles, including byakangelicin, byakangelicol, falcarindiol in both AD and ADF, and notably, 2-linoleoyl glycerol detected only in AD as an antioxidant spot. This comprehensive approach affords a valuable tool set for botanical drug development, emphasizing the critical need for accurate source plant identification and differentiation in ensuring the efficacy and safety of herbal medicine products.
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So Shiho Tang (SSHT) is a traditional herbal medicine commonly used in Asian countries. This study evaluated the anti-inflammatory effect of SSHT and the associated mechanism using lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages and murine dextran sodium sulfate (DSS)-induced ulcerative colitis models. Pre-treatment of RAW 264.7 macrophages with SSHT significantly reduced LPS-induced inflammation by decreasing nitrite production and regulating the mitogen-activated protein kinase pathway. Meanwhile, in mice, DSS-induced colitis symptoms, including colon shortening and body weight loss, were attenuated by SSHT. Moreover, representative compounds of SSHT, including glycyrrhizic acid, ginsenoside Rb1, baicalin, saikosaponin A, and saikosaponin B2, were quantified, and their effects on nitrite production were measured. A potential anti-inflammatory effect was detected in LPS-induced RAW 264.7 cells. Our findings suggest that SSHT is a promising anti-inflammatory agent. Its representative components, including saikosaponin B2, ginsenoside Rb1, and baicalin, may represent the key active compounds responsible for eliciting the anti-inflammatory effects and can, therefore, serve as quality control markers in SSHT preparations.
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Antiinflamatorios , Sulfato de Dextran , Lipopolisacáridos , Macrófagos , Animales , Ratones , Lipopolisacáridos/farmacología , Células RAW 264.7 , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Antiinflamatorios/farmacología , Antiinflamatorios/uso terapéutico , Medicamentos Herbarios Chinos/farmacología , Medicamentos Herbarios Chinos/uso terapéutico , Inflamación/tratamiento farmacológico , Inflamación/inducido químicamente , Inflamación/patología , Colitis/inducido químicamente , Colitis/tratamiento farmacológico , Colitis/patología , Masculino , Ginsenósidos/farmacología , Ginsenósidos/uso terapéutico , Ácido Oleanólico/análogos & derivados , Ácido Oleanólico/farmacologíaRESUMEN
Panax ginseng has been widely applied as an important herb in traditional medicine to treat numerous human disorders. However, the inflammatory regulation effect of P. ginseng distillate (GSD) has not yet been fully assessed. To determine whether GSD can ameliorate inflammatory processes, a GSD was prepared using the vacuum distillation process for the first time, and the regulation effect on lipopolysaccharide-induced macrophages was assessed. The results showed that GSD effectively inhibited nitric oxide (NO) formation and activation of inducible nitric oxide synthase (iNOS) mRNA in murine macrophage cell, but not cyclooxygenase-2 production. The mRNA expression pattern of tumor necrosis factor alpha and IL-6 were also reduced by GSD. Furthermore, we confirmed that GSD exerted its anti-inflammatory effects by downregulating c-Jun NH2-terminal kinase (JNK) phosphorylation, the extracellular signal-regulated kinase phosphorylation, and signaling pathway of nuclear factor kappa B (NF-κB). Our findings revealed that the inflammatory regulation activity of GSD could be induced by iNOS and NO formation inhibition mediated by regulation of nuclear factor kappa B and p38/JNK MAPK pathways.
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Medicamentos Herbarios Chinos , FN-kappa B , Panax , Extractos Vegetales , Humanos , Animales , Ratones , FN-kappa B/metabolismo , Lipopolisacáridos/farmacología , Vacio , Antiinflamatorios/farmacología , Células RAW 264.7 , Óxido Nítrico Sintasa de Tipo II/metabolismo , Ciclooxigenasa 2/genética , Ciclooxigenasa 2/metabolismo , Panax/metabolismo , ARN Mensajero , Óxido Nítrico/metabolismoRESUMEN
Introduction: Sasang Constitutional Medicine (SCM) is a type of traditional Korean medicine where patients are classified as one of four Sasang constitution types (Sasang type) and medications consisting of medicinal herbs are prescribed according to the Sasang type. Despite the importance of personalized medicine, the operation mechanism is largely unknown. To gain a better understanding, we investigated the compound information that composes Sasang type-specific personalized herbal medicines on both multivariate and univariate levels. Methods: Five machine learning classifiers including extremely randomized trees (ERT) were trained to investigate whether the Sasang type can be explained by compound information at the multivariate level. Hierarchical clustering was conducted to determine whether compounds are processed distributedly or specifically. Taxonomic and biosynthetic analyses were conducted on these compounds. A univariate level statistical test was conducted to provide more robust Sasang type-specific compound information. Results: Using the trained ERT classifier, sixty important compounds were extracted. The sixty compounds were clustered into three groups, corresponding to each Sasang type-prominent compounds, suggesting that most compounds have specific preference for the Sasang type. Structural and biosynthetic characteristics of these Sasang type-prominent compounds were determined based on taxonomy and pathway analyses. Fourteen compounds showed statistically significant relevance with the Sasang type. Additionally, we predicted the Sasang type of unknown herbs, which were confirmed by their biological effects in functional assays. Conclusion: This study investigated the personalized herbal medicines of the SCM using compound information. This study provided information on the chemical characteristics of the compounds that are essential for classifying the Sasang type of medicinal herbs, as well as predictions regarding the Sasang type of the commonly used but unidentified medicinal herbs.
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Repetitive exposure to ultraviolet B (UVB) is one of the main causes of skin photoaging. We previously reported that dieckol isolated from Eisenia bicyclis extract has potential anti-photoaging effects in UVB-irradiated Hs68 cells. Here, we aimed to evaluate the anti-photoaging activity of dieckol in a UVB-irradiated hairless mouse model. In this study, hairless mice were exposed to UVB for eight weeks. At the same time, dieckol at two doses (5 or 10 mg/kg) was administered orally three times a week. We found that dieckol suppressed UVB-induced collagen degradation and matrix metalloproteinases (MMPs)-1, -3, and -9 expression by regulating transforming growth factor beta (TGF-ß)/Smad2/3 and mitogen-activated protein kinases (MAPKs)/activator protein-1 (AP-1) signaling. In addition, dieckol rescued the production of hyaluronic acid (HA) and effectively restored the mRNA expression of hyaluronan synthase (HAS)-1/-2 and hyaluronidase (HYAL)-1/-2 in UVB-irradiated hairless mice. We observed a significant reduction in transepidermal water loss (TEWL), epidermal/dermal thickness, and wrinkle formation in hairless mice administered dieckol. Based on these results, we suggest that dieckol, due to its anti-photoaging role, may be used as a nutricosmetic ingredient for improving skin health.
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Benzofuranos , Proteínas Quinasas Activadas por Mitógenos , Envejecimiento de la Piel , Proteínas Smad , Factor de Transcripción AP-1 , Factor de Crecimiento Transformador beta , Animales , Ratones , Ratones Pelados , Proteínas Quinasas Activadas por Mitógenos/metabolismo , Transducción de Señal , Piel/efectos de los fármacos , Piel/metabolismo , Envejecimiento de la Piel/efectos de los fármacos , Factor de Transcripción AP-1/metabolismo , Factor de Crecimiento Transformador beta/metabolismo , Rayos Ultravioleta/efectos adversos , Benzofuranos/aislamiento & purificación , Benzofuranos/farmacología , Proteínas Smad/metabolismoRESUMEN
Scientific regulatory systems with suitable analytical methods for monitoring quality, safety, and efficacy are essential in medicinal plant drug discovery. There have been only few attempts to adopt the analytical quality by design (AQbD) strategy in medicinal plants analysis over the last few years. AQbD is a holistic method and development approach that understands analytical procedure, from risk assessment to lifecycle management. The enhanced AQbD approach reduces the time and effort necessary to develop reliable analytical methods, leads to flexible change control through the method operable design region (MODR), and lowers the out-of-specification (OOS) results. However, it is difficult to follow all the AQbD workflow steps in the field of medicinal plants analysis, such as defining the analytical target profiles (ATPs), identifying critical analytical procedure parameters (CAPPs), among others, because the complexity of chemical and biological properties in medicinal plants acts as a barrier. In this review, various applications of AQbD to medicinal plant analytical procedures are discussed. Unlike the analysis of a single compound, medicinal plant analysis is characterized by analyzing multiple components contained in biological materials, so it will be summarized by focusing on the following points: Analytical methods showing correlations within analysis parameters for the specific medicinal plant analysis, plant raw material diversity, one or more analysis targets defined for multiple phytochemicals, key analysis attributes, and analysis control strategies. In addition, the opportunities available through the use of design-based quality management techniques and the challenges that coexist are also discussed.
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Aspergillus cristatus is a beneficial fungus of microbial fermented teas such as China's Fuzhuan brick tea and Pu-erh tea, and is commonly called golden flower fungus (GFF) because its cleistothecium has a yellow millet or sand grain shape. Since natural materials fermented with GFF exhibit various physiological activities, a new active cosmeceutical ingredient was developed by solid-state fermentation of ginseng, a famous active material for healthy skin, with GFF. The extract of solid-state fermented ginseng with GFF (GFFG) exhibited potent anti-aging efficacy on the skin such as the increase of hyaluronic acid synthesis, aquaporin expression, and mRNA level of filaggrin in HaCaT keratinocyte. GFFG also inhibited the expression of MMP-1 increased by TNF-α in human dermal fibroblast. Sophisticated chromatographic and spectroscopic studies have elucidated isodihydroauroglaucin and flavoglaucin as the metabolites which were not present in ginseng extract nor GFF extract alone. Bioassay of these metabolites revealed that these compounds were part of active principles of GFFG. These results suggest that GFFG would be a potential active ingredient in anti-aging cosmeceutical products.
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The flower buds of Daphne genkwa have been reported as a potent resource associated with anti-angiogenic, anti-tumor, anti-rheumatoid arthritis activities, as well as immunoregulation. This paper aimed to establish an optimal extraction method for flavonoids, as active phytochemicals, and to conduct a comparative analysis by profiling the different blooming stages. Optimized shaking extraction conditions from the design of experiments (DoE), such as minutely mixture design, 23 full factorial design, and polynomial regression analysis, involved an agitation speed of 150 rpm and temperature of 65 °C for 12 h in 56% (v/v) acetone solvent. After, a comparative analysis was performed on three blooming stages, juvenile bud, mature purple bud, and complete flowering, by ultra-high-performance liquid chromatography-photodiode array-mass spectrometry (UHPLC-PDA-MS). Most flavonoids increased during bud growth and then decreased when the bud opened for blooming. In particular, apigenin 7-O-glucuronide, genkwanin 5-O-primeveroside, and genkwanin strikingly showcased this pattern. Furthermore, the raw spectrometric dataset was subjected to orthogonal projection to latent structures discriminant analysis (OPLS-DA) to find significant differences in the flavonoids from the juvenile bud, mature purple bud, and complete flowering. In conclusion, the present study facilitates an understanding of flavonoid change at different blooming stages and provides a momentous reference in the research of D. genkwa.
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The hepatic adiponectin and farnesoid X receptor (FXR) signaling pathways play multiple roles in modulating lipid and glucose metabolism, reducing hepatic inflammation and fibrosis, and altering various metabolic targets for the management of non-alcoholic fatty liver disease (NAFLD). Alisma orientale (AO, Ze xie in Chinese and Taeksa in Korean) is an herbal plant whose tubers are enriched with triterpenoids, which have been reported to exhibit various bioactive properties associated with NAFLD. Here, the present study provides a preclinical evaluation of the biological functions and related signaling pathways of AO extract for the treatment of NAFLD in a Western diet (WD)-induced mouse model. The findings showed that AO extract significantly reversed serum markers (liver function, lipid profile, and glucose) and improved histological features in the liver sections of mice fed WD for 52 weeks. In addition, it also reduced hepatic expression of fibrogenic markers in liver tissue and decreased the extent of collagen-positive areas, as well as inhibited F4/80 macrophage aggregation and inflammatory cytokine secretion. The activation of adiponectin and FXR expression in hepatic tissue may be a major mechanistic signaling cascade supporting the promising role of AO in NAFLD pharmacotherapy. Collectively, our results demonstrated that AO extract improves non-alcoholic steatohepatitis (NASH) resolution, particularly with respect to NASH-related fibrosis, along with the regulation of liver enzymes, postprandial hyperglycemia, hyperlipidemia, and weight loss, probably through the modulation of the hepatic adiponectin and FXR pathways.
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Alisma , Dieta Occidental , Enfermedad del Hígado Graso no Alcohólico , Adiponectina/metabolismo , Alisma/química , Animales , Dieta Occidental/efectos adversos , Fibrosis , Ratones , Ratones Endogámicos C57BL , Enfermedad del Hígado Graso no Alcohólico/inducido químicamente , Enfermedad del Hígado Graso no Alcohólico/etiología , Extractos Vegetales/uso terapéuticoRESUMEN
Chronic exposure to ultraviolet B (UVB) is a major cause of skin aging. The aim of the present study was to determine the photoprotective effect of a 30% ethanol extract of Eisenia bicyclis (Kjellman) Setchell (EEB) against UVB-induced skin aging. By treating human dermal fibroblasts (Hs68) with EEB after UVB irradiation, we found that EEB had a cytoprotective effect. EEB treatment significantly decreased UVB-induced matrix metalloproteinase-1 (MMP-1) production by suppressing the activation of mitogen-activated protein kinase (MAPK)/activator protein 1 (AP-1) signaling and enhancing the protein expression of tissue inhibitors of metalloproteinases (TIMPs). EEB was also found to recover the UVB-induced degradation of pro-collagen by upregulating Smad signaling. Moreover, EEB increased the mRNA expression of filaggrin, involucrin, and loricrin in UVB-irradiated human epidermal keratinocytes (HaCaT). EEB decreased UVB-induced reactive oxygen species (ROS) generation by upregulating glutathione peroxidase 1 (GPx1) and heme oxygenase-1 (HO-1) expression via nuclear factor erythroid-2-related factor 2 (Nrf2) activation in Hs68 cells. In a UVB-induced HR-1 hairless mouse model, the oral administration of EEB mitigated photoaging lesions including wrinkle formation, skin thickness, and skin dryness by downregulating MMP-1 production and upregulating the expression of pro-collagen type I alpha 1 chain (pro-COL1A1). Collectively, our findings revealed that EEB prevents UVB-induced skin damage by regulating MMP-1 and pro-collagen type I production through MAPK/AP-1 and Smad pathways.
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Antioxidantes/farmacología , Phaeophyceae , Extractos Vegetales/farmacología , Envejecimiento de la Piel/efectos de los fármacos , Animales , Organismos Acuáticos , Modelos Animales de Enfermedad , Fibroblastos , Humanos , Masculino , Ratones , Ratones Pelados , Rayos UltravioletaRESUMEN
Dear Colleagues, [...].
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Productos Biológicos/historia , Historia del Siglo XX , Metaboloma , MetabolómicaRESUMEN
Autophagy is a lysosome-dependent degradation program to maintain cellular homeostasis in response to a variety of stressful conditions, such as long-lived or non-functional subcellular organelles, protein aggregates, nutrient limitation, and virus/bacteria infection. Accordingly, dysregulation of autophagy is closely associated with many human pathophysiological conditions, such as neurodegenerative diseases, aging, and cancer, and autophagy is highlighted as an important therapeutic target for these human diseases. In autophagy process, PIK3C3/VPS34 complex plays important roles in autophagosome biogenesis. Accumulating evidences that inhibition of PIK3C3/VPS34 complex successfully blocks autophagy make the complex as an attractive target for the development of autophagy-specific inhibitors. However, considering that various forms of PIK3C3/VPS34 complex exist and they are involved in many different cellular functions, the targeting of the pro-autophagy PIK3C3/VPS34 complex is required to specifically inhibit autophagy. To identify autophagy inhibitors targeting the pro-autophagy complex, we have performed the screening of a customized natural product library consisting of 35 herbal extracts which are widely used in the oriental medicine as anti-inflammation and/or anti-tumor reagents. We discovered that an alcoholic extract of Thuja orientalis L. leaves inhibits pro-autophagy complex formation by disrupting the interaction between autophagy-specific factor, ATG14L, and the complex core unit Vps34-Beclin 1 in vitro. Also, it inhibits the nutrient starvation induced autophagy and diminished pro-autophagy PIK3C3/VPS34 complex containing either ATG14L or UVRAG in several cell lines. Our results strongly suggest that Thuja orientalis L. leave extract functions as an autophagy-specific inhibitor not decreasing the complex activity nor the protein level, but preventing protein-protein interaction between autophagy-specific factor (ATG14L and UVRAG) and PIK3C3/VPS34 complex core unit, Vps34-Beclin 1, thereby specifically depleting the pro-autophagy complex to inhibit autophagy.
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Autofagia/efectos de los fármacos , Fosfatidilinositol 3-Quinasas Clase III/metabolismo , Extractos Vegetales/farmacología , Transducción de Señal/efectos de los fármacos , Thuja , Animales , Beclina-1/metabolismo , Línea Celular , Células HEK293 , Humanos , Ratones , Hojas de la PlantaRESUMEN
The present study introduces a systematic approach using analytical quality by design (AQbD) methodology for the development of a qualified liquid chromatographic analytical method, which is a challenge in herbal medicinal products due to the intrinsic complex components of botanical sources. The ultra-high-performance liquid chromatography-photodiode array-mass spectrometry (UHPLC-PDA-MS) technique for 11 flavonoids in Genkwa Flos was utilized through the entire analytical processes, from the risk assessment study to the factor screening test, and finally in method optimization employing central composite design (CCD). In this approach, column temperature and mobile solvent slope were found to be critical method parameters (CMPs) and each of the eleven flavonoid peaks' resolution values were used as critical method attributes (CMAs) through data mining conversion formulas. An optimum chromatographic method in the design space was calculated by mathematical and response surface methodology (RSM). The established chromatographic condition is as follows: acetonitrile and 0.1% formic acid gradient elution (0-13 min, 10-45%; 13-13.5 min, 45-100%; 13.5-14 min, 100-10%; 14-15 min, 10% acetonitrile), column temperature 28â, detection wavelength 335 nm, and flow rate 0.35 mL/min using C18 (50 × 2.1 mm, 1.7 µm) column. A validation study was also performed successfully for apigenin 7-O-glucuronide, apigenin, and genkwanin. A few important validation results were as follows: linearity over 0.999 coefficient of correlation, detection limit of 2.87-22.41, quantitation limit of 8.70-67.92, relative standard deviation of precision less than 0.22%, and accuracy between 100.13 and 102.49% for apigenin, genkwanin, and apigenin 7-O-glucuronide. In conclusion, the present design-based approach provide a systematic platform that can be effectively applied to ensure pharmaceutically qualified analytical data from complex natural products based botanical drug.
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Cromatografía Líquida de Alta Presión/métodos , Flavonoides/análisis , Flores/química , Espectrometría de Masas/métodos , Plantas Medicinales/química , Cromatografía Líquida de Alta Presión/normas , Flavonoides/química , Espectrometría de Masas/normas , Estructura Molecular , Control de Calidad , Reproducibilidad de los ResultadosRESUMEN
Based on the hypothesis that the variation of the metabolomes of latex is a response to selective pressure and should thus be affected differently from other organs, their variation could provide an insight into the defensive chemical selection of plants. Metabolic profiling was used to compare tissues of three Euphorbia species collected in diverse regions. The metabolic variation of latexes was much more limited than that of other organs. In all the species, the levels of polyisoprenes and terpenes were found to be much higher in latexes than in leaves and roots of the corresponding plants. Polyisoprenes were observed to physically delay the contact of pathogens with plant tissues and their growth. A secondary barrier composed of terpenes in latex and in particular, 24-methylenecycloartanol, exhibited antifungal activity. These results added to the well-known role of enzymes also present in latexes, show that these are part of a cooperative defense system comprising biochemical and physical elements.
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Euphorbia/metabolismo , Euphorbia/microbiología , Geografía , Herbivoria , Látex/metabolismo , Metabolómica , Euphorbia/fisiología , Especificidad de la EspecieRESUMEN
The Wnt/ß-catenin signaling pathway is involved in breast cancer and Myxococcus fulvus KYC4048 is a myxobacterial strain that can produce a variety of bioactive secondary metabolites. Although a previous study revealed that KYC4048 metabolites exhibit anti-proliferative effects on breast cancer, the biochemical mechanism involved in their effects remains unclear. In the present study, KYC4048 metabolites were separated into polar and non-polar (ethyl acetate and n-hexane) fractions via liquid-liquid extraction. The effects of these polar and non-polar KYC4048 metabolites on the viability of breast cancer cells were then determined by MTT assay. Expression levels of Wnt/ß-catenin pathway proteins were determined by Western blot analysis. Cell cycle and apoptosis were measured via fluorescence-activated cell sorting (FACS). The results revealed that non-polar KYC4048 metabolites induced cell death of breast cancer cells and decreased expression levels of WNT2B, ß-catenin, and Wnt target genes (c-Myc and cyclin D1). Moreover, the n-hexane fraction of non-polar KYC4048 metabolites was found most effective in inducing apoptosis, necrosis, and cell cycle arrest, leading us to conclude that it can induce apoptosis of breast cancer cells through the Wnt/ß-catenin pathway. These findings provide evidence that the n-hexane fraction of non-polar KYC4048 metabolites can be developed as a potential therapeutic agent for breast cancer via inhibition of the Wnt/ß-catenin pathway.
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Antineoplásicos/farmacología , Proliferación Celular/efectos de los fármacos , Myxococcus/química , Vía de Señalización Wnt/efectos de los fármacos , Apoptosis/efectos de los fármacos , Puntos de Control del Ciclo Celular/efectos de los fármacos , Ciclina D1 , Glicoproteínas , Humanos , Células MCF-7 , Proteínas Proto-Oncogénicas c-myc , Proteínas Wnt , beta CateninaRESUMEN
Mass spectrometry-based molecular imaging has been utilized to map the spatial distribution of target metabolites in various matrixes. Among the diverse mass spectrometry techniques, matrix-assisted laser desorption/ionization-mass spectrometry (MALDI-MS) is the most popular for molecular imaging due to its powerful spatial resolution. This unparalleled high resolution, however, can paradoxically act as a bottleneck when the bio-imaging of large areas, such as a whole plant, is required. To address this issue and provide a more versatile tool for large scale bio-imaging, direct analysis in real-time-time of flight-mass spectrometry (DART-TOF-MS), an ambient ionization MS, was applied to whole plant bio-imaging of a medicinal plant, Ephedrae Herba. The whole aerial part of the plant was cut into 10-20 cm long pieces, and each part was further cut longitudinally to compare the contents of major ephedra alkaloids between the outer surface and inner part of the stem. Using optimized DART-TOF-MS conditions, molecular imaging of major ephedra alkaloids of the whole aerial part of a single plant was successfully achieved. The concentration of alkaloids analyzed in this study was found to be higher on the inner section than the outer surface of stems. Moreover, side branches, which are used in traditional medicine, represented a far higher concentration of alkaloids than the main stem. In terms of the spatial metabolic distribution, the contents of alkaloids gradually decreased towards the end of branch tips. In this study, a fast and simple macro-scale MS imaging of the whole plant was successfully developed using DART-TOF-MS. This application on the localization of secondary metabolites in whole plants can provide an area of new research using ambient ionization mass spectroscopy and an unprecedented macro-scale view of the biosynthesis and distribution of active components in medicinal plants.
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Alcaloides/metabolismo , Ephedra/metabolismo , Espectrometría de Masas/métodos , Plantas Medicinales/metabolismo , Efedrina/análogos & derivados , Efedrina/metabolismo , Espectrometría de Masas/instrumentación , Imagen Molecular/instrumentación , Imagen Molecular/métodos , Componentes Aéreos de las Plantas/metabolismo , Espectrometría de Masa por Láser de Matriz Asistida de Ionización DesorciónRESUMEN
The purpose of this research was to identify metabolite change during barley (Hordeum vulgare) germination and reveal active principles for the anti-wrinkle activity. Barley was germinated with deionized water (DW) and mineral-rich water (MRW) for the comparison of the effect of mineral contents on the metabolites changes during germination. The effects of germinated barley extracts (GBEs) on collagen production and collagenase inhibition were evaluated in vitro using human dermal fibroblasts (HDFs). A pronounced anti-wrinkle activity was observed in the test group treated with the MRW-GBEs. In order to find out the active components related to the anti-wrinkle activity, an orthogonal projection to latent structure-discriminant analysis (OPLS-DA) was performed, using the data from secondary metabolites profiling conducted by UPLC-PDA-ESI-MS. The anti-wrinkle activity of MRW-GBEs was revealed to be associated with the increase of oligomeric compounds of procyanidin and prodelphinidin, indicating that it can be used as an active ingredient for anti-wrinkle agents.
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Fibroblastos/efectos de los fármacos , Germinación , Hordeum/metabolismo , Metaboloma , Extractos Vegetales/farmacología , Envejecimiento de la Piel/efectos de los fármacos , Células Cultivadas , Colágeno Tipo I/metabolismo , Dermis/citología , Dermis/efectos de los fármacos , Dermis/metabolismo , Fibroblastos/citología , Fibroblastos/metabolismo , Hordeum/crecimiento & desarrollo , Humanos , Metaloproteinasa 1 de la Matriz/químicaRESUMEN
Skin, the organ protecting the human body from external factors, maintains structural and tensile strength by containing many collagen fibrils, particularly type I procollagen. However, oxidative stress by ultraviolet (UV) exposure causes skin photoaging by activating collagen degradation and inhibiting collagen synthesis. Acer tataricum subsp. ginnala extract (AGE) is a herbal medicine with anti-inflammatory and anti-oxidative effects, but there is no report on the protective effect against skin photoaging. Therefore, we conducted research concentrating on the anti-photoaging effect of Acer tataricum subsp. ginnala (AG) in UVB (20 mJ/cm2)-irradiated human dermal fibroblasts (HDF). Then, various concentrations (7.5, 15, 30 µg/mL) of AGE were treated in HDF for 24 h following UVB irradiation. After we performed AGE treatment, the matrix metalloproteinase1 (MMP1) expression was downregulated, and the type I procollagen level was recovered. Then, we investigated the mitogen-activated protein kinases/activator protein 1 (MAPK/AP-1) and nuclear factor-κB (NF-κB) pathway, which induce collagen breakdown by promoting the MMP1 level and pro-inflammatory cytokines. The results indicated that AGE downregulates the expression of the MAPK/AP-1 pathway, leading to MMP1 reduction. AGE inhibits nuclear translocation of NF-κB and inhibitor of nuclear factor-κB (IκB) degradation. Therefore, it downregulates the expression of MMP1 and pro-inflammatory cytokines such as TNF-α, IL-1ß, and IL-6 increased by UVB. Besides, the TGFß/Smad pathway, which is mainly responsible for the collagen synthesis in the skin, was also analyzed. AGE decreases the expression of Smad7 and increases TGFßRII expression and Smad3 phosphorylation. This means that AGE stimulates the TGFß/Smad pathway that plays a critical role in promoting collagen synthesis. Thus, this study suggests that AGE can be a functional material with anti-photoaging properties.
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Acer/química , Fibroblastos/efectos de los fármacos , Extractos Vegetales/farmacología , Transducción de Señal/efectos de los fármacos , Envejecimiento de la Piel/efectos de los fármacos , Piel/efectos de los fármacos , Antiinflamatorios/farmacología , Células Cultivadas , Colágeno Tipo I/metabolismo , Regulación hacia Abajo/efectos de los fármacos , Fibroblastos/metabolismo , Humanos , Metaloproteinasa 1 de la Matriz/metabolismo , Proteínas Quinasas Activadas por Mitógenos/metabolismo , FN-kappa B/metabolismo , Piel/metabolismo , Proteínas Smad/metabolismo , Factor de Transcripción AP-1/metabolismo , Factor de Crecimiento Transformador beta/metabolismoRESUMEN
BACKGROUND: Periodontitis is a common oral disease characterized as inflammation on gingival tissue and alveolar bone resorption. Spirulina maxima has been reported to have anti-oxidative and anti-inflammatory effects on gastric ulcers. However, its effects on gingival inflammation and alveolar bone resorption of periodontitis have not been studied. PURPOSE: This study was designed to investigate the effects of S. maxima on the P. gingivalis-induced periodontitis and to elucidate its mechanism. METHODS: The phycocyanin contents in S. maxima were identified by high-performance liquid chromatography. 8-week old SD rats were induced periodontitis by inoculation with P. gingivalis for 14 days. The rats were then orally treated with S. maxima 100, 200, 400 mg/kg, or indomethacin (IND, positive control) 5 mg/kg for an additional 14 days. Inflammatory responses, expressions of collagenases in gingival tissue, osteoclast formation and activation, alveolar bone resorption, osteogenesis-related markers, and BMP2/Smad signaling in alveolar bone were measured. RESULTS: Pro-inflammatory cytokines such as TNF-α, IL-1ß, IL-6, and inflammatory transcription factor NF-κB were decreased in gingival tissue by S. maxima administration. Also, myeloperoxidase (MPO) activity and matrix metalloproteinase (MMPs) expression were decreased by S. maxima administration. Conversely, S. maxima increased IL-4, anti-inflammatory cytokine from Th2 cells. The osteoprotegerin (OPG) / receptor activator of NF-κB ligand (RANKL) expression ratio, which represents osteoclast-osteoblast balance, was increased in S. maxima-treated groups. The alveolar bone loss and the number of TRAP-positive osteoclast cells were also declined in S. maxima-treated groups while the osteoblasts count was increased. Besides, in S. maxima-treated groups, the osteogenesis-related factors were promoted and BMP-2/Smad pathway was up-regulated in a periodontitis condition. CONCLUSION: S. maxima reduces periodontitis induced by P. gingivalis through anti-inflammatory effect and resultant reduction in bone loss, suggesting that S. maxima might be a potential agent for treating periodontitis.