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1.
Front Chem ; 11: 1245071, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-37621851

RESUMEN

Introduction: The root of Cratoxylum cochinchinense has been widely used as Chinese folk medicine to cure fevers, burns, and abdominal complications because it contains various bioactive metabolites such as xanthones, triterpenes, and flavonoids. In this study, we estimated bacterial neuraminidase inhibition with a series of xanthones from C. cochinchinense. BNA has connected to various biological functions such as pathogenic bacteria infection inflammatory process after infection and biofilm formation. Methods: The identification of xanthones (1-6) bearing geranyl and prenyl groups was established by spectroscopic data using UV, IR, NMR, and HREIMS. BNA inhibitory modes of isolated xanthones were investigated by Double-reciprocal plots. Moreover, the competitive inhibitor was evaluated the additional kinetic modes determined by kinetic parameters (k 3, k 4, and K i app). The molecular docking (MD) and molecular dynamics simulations (MDS) studies also provided the critical information regarding the role of the geranyl and prenyl groups against BNA inhibition. Results: A series of xanthones (1-6) appended prenyl and geranyl groups on the A-ring were isolated, and compounds 1-3 were shown to be new xanthones. The analogues within this series were highly inhibited with excellent affinity against bacterial neuraminidase (BNA). A subtle change in the prenyl or geranyl motif affected the inhibitory potency and behavior significantly. For example, the inhibitory potency and binding affinity resulting from the geranyl group on C4: xanthone 1 (IC50 = 0.38 µM, KA = 2.4434 × 105 L·mol-1) were 100-fold different from those of xanthone 3 (IC50 = 35.8 µM, KA = 0.0002 × 105 L·mol-1). The most potent compound 1 was identified as a competitive inhibitor which interacted with BNA under reversible slow-binding inhibition: K i app = 0.1440 µM, k 3 = 0.1410 µM-1s-1, and k 4 = 0.0203 min-1. The inhibitory potencies (IC50) were doubly confirmed by the binding affinities (KA). Discussion: This study suggests the potential of xanthones derived from C. cochinchinense as promising candidates for developing novel BNA inhibitors. Further research and exploration of these xanthones may contribute to the development of effective treatments for bacterial infections and inflammatory processes associated with BNA activity.

2.
J Agric Food Chem ; 71(27): 10393-10402, 2023 Jul 12.
Artículo en Inglés | MEDLINE | ID: mdl-37358831

RESUMEN

The low levels of bioactive metabolites in target plants present a bottleneck for the functional food industry. The major disadvantage of soy leaves is their low phytoestrogen content despite the fact that these leaves are an enriched source of flavonols. Our study demonstrated that simple foliar spraying with 1-aminocyclopropane-1-carboxylic acid (ACC) significantly enhanced the phytoestrogen contents of the whole soy plant, including its leaves (27-fold), stalks (3-fold), and roots (4-fold). In particular, ACC continued to accelerate the biosynthesis pathway of isoflavones in the leaves for up to 3 days after treatment, from 580 to 15,439 µg/g. The detailed changes in the levels of this metabolite in soy leaves are disclosed by quantitative and metabolomic analyses based on HPLC and UPLC-ESI-TOF/MS. The PLS-DA score plot, S-plot, and heatmap provide comprehensive evidence to clearly distinguish the effect of ACC treatment. ACC was also proved to activate a series of structural genes (CHS, CHR, CHI, IFS, HID, IF7GT, and IF7MaT) along the isoflavone biosynthesis pathway time-dependently. In particular, ACC oxidase genes were turned on 12 h after ACC treatment, which was rationalized to start activating the synthetic pathway of isoflavones.


Asunto(s)
Isoflavonas , Isoflavonas/metabolismo , Glycine max/química , Fitoestrógenos , Vías Biosintéticas , Aceleración
3.
Bioorg Chem ; 127: 105978, 2022 10.
Artículo en Inglés | MEDLINE | ID: mdl-35752099

RESUMEN

Artocarpus elasticus is a popular fruit tree in the tropical regions. Primary screenings of methanol extracts of the root bark confirmed its potent inhibition of bacterial neuraminidase (BNA), which plays an essential role in the pathogenesis of many microbial diseases. Assessments of the responsible phytochemicals were conducted by isolating eight compounds (1-8) and two of them (6 and 8) were identified as new compounds. Among the isolates, the dihydrobenzoxanthones attained the highest BNA inhibition with IC50 values of 0.5 âˆ¼ 3.9 µM. Further investigation of the inhibitory mechanism by Lineweaver-Burk plots revealed the phytochemicals to function as reversible noncompetitive inhibitors. Fluorescence quenching showed their binding affinities were highly correlated with their inhibitory potential dose-dependently. Molecular docking experiments suggested the dihydrobenzoxanthones (4 and 6) as noncompetitive inhibitors of BNA with unique interaction with Tyr435 of BNA in comparison with the mother flavonoid (7).


Asunto(s)
Artocarpus , Artocarpus/química , Bacterias , Flavonoides/química , Simulación del Acoplamiento Molecular , Neuraminidasa , Fitoquímicos , Extractos Vegetales/química
4.
Phytomedicine ; 103: 154209, 2022 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-35689901

RESUMEN

BACKGROUND: Leaky gut symptoms and inflammatory bowel disease (IBD) are associated with damaged intestinal mucosa, intestinal permeability dysfunction by epithelial cell cytoskeleton contraction, disrupted intercellular tight junction (TJ) protein expression, and abnormal immune responses and are intractable diseases. PURPOSE: We evaluated the effects of schisandrin C, a dibenzocyclooctadiene lignan from Schisandra chinensis, on intestinal inflammation and permeability dysfunction in gut mimetic systems: cultured intestinal cells, intestinal organoids, and a Caenorhabditis elegans model. METHODS: Schisandrin C was selected from 9 lignan compounds from S. chinensis based on its anti-inflammatory effects in HT-29 human intestinal cells. IL-1ß and Pseudomonas aeruginosa supernatants were used to disrupt intestinal barrier formation in vitro and in C. elegans, respectively. The effects of schisandrin C on transepithelial electrical resistance (TEER) and intestinal permeability were evaluated in intestinal cell monolayers, and its effect on intestinal permeability dysfunction was tested in mouse intestinal organoids and C. elegans by measuring fluorescein isothiocyanate (FITC)-dextran efflux. The effect of schisandrin C on TJ protein expression was investigated by western blotting and fluorescence microscopy. The signaling pathway underlying these effects was also elucidated. RESULTS: Schisandrin C ameliorated intestinal permeability dysfunction in three IBD model systems and enhanced epithelial barrier formation via upregulation of ZO-1 and occludin in intestinal cell monolayers and intestinal organoids. In Caco-2 cells, schisandrin C restored IL-1ß-mediated increases in MLCK and p-MLC expression, in turn blocking cytoskeletal contraction and subsequent intestinal permeabilization. Schisandrin C inhibited NF-ĸB and p38 MAPK signaling, which regulates MLCK expression and structural reorganization of the TJ complex in Caco-2 cells. Schisandrin C significantly improved abnormal FITC-dextran permeabilization in both intestinal organoids and C. elegans. CONCLUSION: Schisandrin C significantly improves abnormal intestinal permeability and regulates the expression of TJ proteins, long MLCK, p-MLC, and inflammation-related proteins, which are closely related to leaky gut symptoms and IBD development. Therefore, schisandrin C is a candidate to treat leaky gut symptoms and IBDs.


Asunto(s)
Enfermedades Inflamatorias del Intestino , Lignanos , Animales , Células CACO-2 , Caenorhabditis elegans/metabolismo , Ciclooctanos , Humanos , Inflamación/metabolismo , Enfermedades Inflamatorias del Intestino/tratamiento farmacológico , Mucosa Intestinal/metabolismo , Lignanos/farmacología , Ratones , Quinasa de Cadena Ligera de Miosina/metabolismo , Organoides/metabolismo , Permeabilidad , Compuestos Policíclicos , Proteínas de Uniones Estrechas/metabolismo , Uniones Estrechas
5.
Food Funct ; 13(13): 6923-6933, 2022 Jul 04.
Artículo en Inglés | MEDLINE | ID: mdl-35695875

RESUMEN

Ethanol extract of soybean (Glycine max (L.) Merr.) showed good inhibitory activity against bacterial neuraminidase (BNA), which plays a pivotal role in the pathogenesis of a number of microbial diseases. The saponin portion fractionated through preparative HPLC (IC50 = 2.25 µg mL-1) was found to be responsible for the observed BNA inhibition. Estimation of the inhibitory effects by individual compounds showed that the soyasaponins of group B (Ba, Bb, Bb', Bc, and Bd) exhibited extremely high inhibitions (IC50 = 0.25-0.48 µM), whereas group A (Aa, Ab, and Ac) was almost inactive. Kinetic studies determined that group B soyasaponins were noncompetitive inhibitors. Furthermore, molecular docking experiments confirmed that soyasaponin Ba (group B) could undergo binding interactions with various residues in the binding pocket. In contrast, soyasaponin Aa (group A) failed to enter the binding pocket due to its extra scaffold structure of oligosaccharides bonded to the 22-hydroxyl position. The metabolites in the soybean extract were fully characterized using UPLC-ESI-TOF/MS.


Asunto(s)
Fabaceae , Saponinas , Cromatografía Líquida de Alta Presión , Cinética , Simulación del Acoplamiento Molecular , Neuraminidasa , Fitoquímicos , Extractos Vegetales/química , Extractos Vegetales/farmacología , Saponinas/química , Saponinas/farmacología , Glycine max/química
6.
Molecules ; 26(21)2021 Oct 31.
Artículo en Inglés | MEDLINE | ID: mdl-34771010

RESUMEN

The aim of this study is to explore anti-inflammatory phytochemicals from B. chinensis based on the inhibition of pro-inflammatory enzyme, human neutrophil elastase (HNE) and anti-inflammatory activities in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage. Three stereoisomers of iridal-type triterpenoids (1-3) were isolated from the roots of B. chinensis and their stereochemistries were completely identified by NOESY spectra. These compounds were confirmed as reversible noncompetitive inhibitors against HNE with IC50 values of 6.8-27.0 µM. The binding affinity experiment proved that iridal-type triterpenoids had only a single binding site to the HNE enzyme. Among them, isoiridogermanal (1) and iridobelamal A (2) displayed significant anti-inflammatory effects by suppressing the expressions of pro-inflammatory cytokines, such as iNOS, IL-1ß, and TNF-α through the NF-κB pathway in LPS-stimulated RAW264.7 cells. This is the first report that iridal-type triterpenoids are considered responsible phytochemicals for anti-inflammatory effects of B. chinensis.


Asunto(s)
Antiinflamatorios/farmacología , Iridaceae/química , Elastasa de Leucocito/antagonistas & inhibidores , Extractos Vegetales/farmacología , Triterpenos/farmacología , Animales , Antiinflamatorios/química , Antiinflamatorios/aislamiento & purificación , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Humanos , Elastasa de Leucocito/metabolismo , Lipopolisacáridos/antagonistas & inhibidores , Lipopolisacáridos/farmacología , Ratones , Conformación Molecular , FN-kappa B/antagonistas & inhibidores , FN-kappa B/metabolismo , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Células RAW 264.7 , Triterpenos/química , Triterpenos/aislamiento & purificación
7.
J Ethnopharmacol ; 272: 113935, 2021 May 23.
Artículo en Inglés | MEDLINE | ID: mdl-33609726

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Caragana has a standing history of implementation in Traditional Chinese Medicine (TCM). Most species of this genus have been explored for multi-functional purposes, such as promoting blood circulation and curing neuralgia, fatigue, migraine, arthritis, and vascular hypertension (Meng et al., 2009). Among them, the well-known species C. sinica showed the most promising potential to increase the expression of ADAM10 among 313 tested medicinal plants, which is one of the promising approach for the treatment of Alzheimer's disease (AD). (Schuck et al., 2015). AIM OF THIS STUDY: The aim of this work is to explore ß-secretase inhibitory activity of compounds isolated from the aerial part of endemic Caragana balchaschensis (Kom.) Pojark. We provided a full characterization of their inhibitory mechanisms, binding affinities, and binding modes. MATERIALS AND METHODS: The isolation of quercetin derivatives was accomplished by various chromatographical approaches and their structures were annotated by spectroscopic analysis. The detailed kinetic behavior of ß-secretase inhibitors was determined by estimation of kinetic parameters (Km, Vmax, KI, and KIS). Binding affinities (KSV) and binding modes of inhibitors were elucidated by fluorescence quenching and molecular docking studies, respectively. RESULTS: O-methylated quercetins (2-7) were significantly effective in ß-secretase inhibition with IC50 ranging from 1.2 to 6.5 µM. The most active one (6) was 20-fold effective than the mother skeleton, quercetin. The O-methyl motif was a critical factor in ß-secretase inhibition: tri-O-methylated (1.2 µM) > di-O-methylated (3.5 µM) > mono-O-methylated (6.5 µM) > quercetin (25.2 µM). In the kinetic study, all quercetins (1-7) showed a noncompetitive inhibition, but glucoside ones (8 and 9) were mixed type I inhibitors. The binding affinities (KSV) were agreed with inhibitory potencies. The O-methylated quercetins were annotated as the most natural abundant metabolites in the aerial part by LC-ESI-TOF/MS. Binding modes of inhibitors to enzyme were elucidated by molecular docking experiments. CONCLUSION: This study disclosed that most of the major phenolic metabolites of the aerial part of C. balchaschensis are O-methylated quercetins, which have a significant inhibitory effect on ß-secretase, which is a critical factor for AD.


Asunto(s)
Secretasas de la Proteína Precursora del Amiloide/antagonistas & inhibidores , Caragana/química , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Quercetina/química , Quercetina/farmacología , Secretasas de la Proteína Precursora del Amiloide/química , Cromatografía Líquida de Alta Presión , Inhibidores Enzimáticos/aislamiento & purificación , Cinética , Metilación , Simulación del Acoplamiento Molecular , Componentes Aéreos de las Plantas/química , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Unión Proteica , Quercetina/aislamiento & purificación , Espectrometría de Masa por Ionización de Electrospray , Relación Estructura-Actividad , Espectrometría de Masas en Tándem
8.
Molecules ; 25(17)2020 Aug 25.
Artículo en Inglés | MEDLINE | ID: mdl-32854419

RESUMEN

Soybean sprouts are one of the most inexpensive and nutritious food items that can be easily grown year-round. Several studies have been conducted to increase their yield and nutritional values. This study was carried out to examine the effects of Pu-erh tea extracts on the production and nutrients content of soybean sprouts. Soybean seeds were soaked in 1%, 2%, or 3% (w/v) tea extracts, or tap water, before keeping for sprout cultivation; the sprout samples were named PE-1, PE-2, PE-3, and the control, respectively. The sprout yields were increased by up to 17% in PE-2 and PE-3 than in the control. The vitamin C, total free amino acid, total mineral, total isoflavone, total polyphenol, and flavonoid contents as well as the antioxidant potentials of the tea extract-treated sprouts were higher than those of the control. The results indicated that pre-soaking soybean seeds in 2% Pu-erh tea extracts could offer an easy, inexpensive, and efficient way to improve the yield and nutritional value of soybean sprouts.


Asunto(s)
Antioxidantes , Glycine max/crecimiento & desarrollo , Valor Nutritivo , Extractos Vegetales , Plantones/crecimiento & desarrollo , Té/química , Antioxidantes/química , Antioxidantes/farmacología , Extractos Vegetales/química , Extractos Vegetales/farmacología
9.
Nutrients ; 12(5)2020 Apr 25.
Artículo en Inglés | MEDLINE | ID: mdl-32344799

RESUMEN

Nowadays, new types of vinegar have been developed using various raw materials and biotechnological processes. The fruit of Prunus mume has been extensively distributed in East Asia and used as a folk medication for fatigue. In this study, the Prunus mume vinegar (PV) was produced by a two-step fermentation and was evaluated for its anti-fatigue activity by C2C12 myoblasts and high-intensity exercised rats. The administration of PV significantly improved running endurance and glycogen accumulation in the liver and muscle of PV supplemented rats compared to sedentary and exercised control groups. In addition, PV supplementation elicited lower fatigue-related serum biomarkers, for instance, ammonia, inorganic phosphate, and lactate. PV administered rats exhibited higher lactate dehydrogenase activity and glutathione peroxidase activity, and lower creatine kinase activity and malondialdehyde levels. Furthermore, phenolic compounds in PV were identified using HPLC analysis. The phenolic acids analyzed in PV were protocatechuic acid, syringic acid, chlorogenic acid, and its derivates. These results indicate that the administration of PV with antioxidative property contributes to the improvement of fatigue recovery in exhausted rats. The findings of this study suggest that the PV containing various bioactive constituents can be used as a functional material against fatigue caused by high-intensity exercise.


Asunto(s)
Ácido Acético/farmacología , Condicionamiento Físico Animal , Prunus/química , Ácido Acético/química , Aminoácidos/química , Animales , Biomarcadores , Proliferación Celular/efectos de los fármacos , Fenómenos Químicos , Cromatografía Líquida de Alta Presión , Suplementos Dietéticos , Fatiga/tratamiento farmacológico , Fermentación , Glucógeno/metabolismo , Hidroxibenzoatos/química , Hidroxibenzoatos/farmacología , Masculino , Malondialdehído/metabolismo , Ratones , Mioblastos , Fenoles/análisis , Fenoles/química , Fenoles/farmacología , Ratas
10.
J Ethnopharmacol ; 256: 112664, 2020 Jun 28.
Artículo en Inglés | MEDLINE | ID: mdl-32045685

RESUMEN

ETHNOPHARMACOLOGICAL RELEVANCE: Orostachys japonicus A. Berger (O. japonicus), so-called Wa-song in Korea, a traditional food and medicine that grows on mountain rocks and roof tiles. Wa-song containing various phenolic compounds have been reported as a medicinal plant for prevention of fibrosis, cancer, inflammation, and oxidative damage. AIM OF THE STUDY: The present study was designed to examine the anti-angiogenic effects of cultivated Orostachys japonicus 70% ethanol extract (CE) in vascular endothelial growth factor (VEGF)-stimulated human umbilical vein endothelial cells (HUVECs). MATERIALS AND METHODS: CE was prepared with 70% ethanol. HUVECs, rat aortic rings, and matrigel plug in mice were treated with CE (10-20 µg/mL) and VEGF (20-50 ng/mL), and the anti-angiogenic activities of CE were analyzed by SRB, wound healing, trans-well invasion, capillary-like tubule formation, rat aortas, Western blot, and matrigel plug assay. Phenolic compounds in CE were analyzed using a high-performance liquid chromatography (HPLC)-PDA system. RESULTS: Treatment of CE (10-20 µg/mL) markedly suppressed proliferation of HUVECs in the presence (from 136.5% to 112.2%) or absence of VEGF (from 100.0% to 92.1%). The proliferation inhibitory effect of CE was caused by G0/G1 cell cycle arrest, and the decrease of CDK-2, CDK-4, Cyclin D1 and Cyclin E1. Furthermore, CE treatment showed significant angiogenesis inhibitory effects on motility, invasion and micro-vessel formation of HUVECs, rat aortic rings and subcutaneous matrigels under VEGF-stimulation condition. In HUVECs, CE-induced anti-angiogenic effect was regulated by inhibition of the PI3K/AKT/mTOR, MAPK/p38, MAPK/ERK, FAK-Src, and VEGF-VEGFR2 signaling pathways. CONCLUSION: This study demonstrated that CE might be used as a potential natural substance, multi-targeted angiogenesis inhibitor, functional food material.


Asunto(s)
Inhibidores de la Angiogénesis/farmacología , Crassulaceae/química , Neovascularización Patológica/tratamiento farmacológico , Extractos Vegetales/farmacología , Transducción de Señal/efectos de los fármacos , Factor A de Crecimiento Endotelial Vascular/metabolismo , Receptor 2 de Factores de Crecimiento Endotelial Vascular/metabolismo , Inductores de la Angiogénesis/farmacología , Animales , Puntos de Control del Ciclo Celular/efectos de los fármacos , Línea Celular , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Colágeno/efectos de los fármacos , Colágeno/metabolismo , Combinación de Medicamentos , Fase G1/efectos de los fármacos , Células Endoteliales de la Vena Umbilical Humana , Humanos , Laminina/efectos de los fármacos , Laminina/metabolismo , Masculino , Ratones , Ratones Endogámicos C57BL , Neovascularización Patológica/metabolismo , Proteoglicanos/efectos de los fármacos , Proteoglicanos/metabolismo , Ratas , Ratas Sprague-Dawley , Fase de Descanso del Ciclo Celular/efectos de los fármacos
11.
Foods ; 10(1)2020 Dec 29.
Artículo en Inglés | MEDLINE | ID: mdl-33383792

RESUMEN

The fruit of Prunus mume (PM) is widely cultivated in East Asia, and it has been used as a folk medication for gastrointestinal disorders, e.g., diarrhea, stomach ache and ulceration. In this study, the pectinase-treated PM juice (PJ) was fermented with Lactobacillus strains containing fundamental organic acids and free amino acids. The PJ fermented with Lactobacillus plantarum and L. casei (FP) was investigated for its protective effect in dextran sodium sulfate (DSS)-induced colitis mice model. The administration of FP reduced lipid peroxidation and histopathological colitis symptoms, e.g., shortening of the colon length, depletion of mucin, epithelial injury and ulceration, in colonic tissues. The FP-supplemented group showed the alleviation of pro-inflammatory cytokines. Compared with the DSS control group, the supplementation of FP significantly reduced the levels of serum interferon-γ (IFN-γ), interleukin (IL)-1ß, IL-6, IL-12 and IL-17 as well as colonic tumor necrosis factor-α, IFN-γ, IL-12 and IL-17. Furthermore, the DSS-induced TUNEL-positive area was significantly reduced by the FP supplementation. These results show that the supplementation of FP fermented with mixed lactic acid bacteria, L. plantarum and L. casei, elucidated the protective effect in DSS-induced colitis mice. Hence, this study suggests that FP can be utilized as a natural therapeutic agent for colitis and intestinal inflammation.

12.
Pharm Biol ; 57(1): 684-693, 2019 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-31608754

RESUMEN

Context: Kochia scoparia (L.) Schrad (Amaranthaceae), known as a traditional medicine in China, Japan and Korea, is reported to have various biological activities. However, K. scoparia seed extract (KSE) functional roles on angiogenesis and prostate cancer inhibition have not been elucidated. Objective: This study elucidates the effects of KSE on vascular endothelial growth factor (VEGF)-induced angiogenesis in human umbilical vein endothelial cells (HUVECs) and inhibition of proliferation in prostate cancer cells. Materials and methods: HUVECs were treated with 10-20 µg/mL of KSE and 20-50 ng/mL of VEGF for 12-72 h. Anti-angiogenesis properties of KSE were determined by wound healing, trans-well, tube formation, rat aortic ring assay and western blotting. Prostate cancer and normal cells were incubated with 10-250 µg/mL of KSE for 24 h, and cell viability was measured by SRB assay. Phenolic compounds in KSE were analyzed using a HPLC-PDA system. Results: IC50 for cell viability of HUVECs, LNCaP, PC-3, RC-58T and RWPE-1 by KSE were 30.64, 89.25, 123.41, 141.62 and >250 µg/mL, respectively. Treatment with KSE (20 µg/mL) significantly suppressed VEGF-induced migration, invasion and capillary-like structure formation of HUVECs and microvessel sprouting from rat aortic rings. In addition, KSE down-regulated PI3K/AKT/mTOR levels and phosphorylation of VEGF receptor 2 in HUVECs. 3-OH-tyrosol (1.63 mg/g) and morin hydrate (0.17 mg/g) were identified in KSE. Conclusions: KSE inhibits angiogenesis in HUVECs as well as proliferation in human prostate cancer cells, suggesting KSE may be useful herbal medicine for preventing progression of prostate cancer and angiogenesis.


Asunto(s)
Inhibidores de la Angiogénesis/farmacología , Bassia scoparia/química , Extractos Vegetales/farmacología , Neoplasias de la Próstata/tratamiento farmacológico , Inhibidores de la Angiogénesis/aislamiento & purificación , Animales , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Células Endoteliales de la Vena Umbilical Humana , Humanos , Masculino , Neovascularización Patológica/tratamiento farmacológico , Fosfatidilinositol 3-Quinasa/metabolismo , Neoplasias de la Próstata/patología , Proteínas Proto-Oncogénicas c-akt/metabolismo , Ratas , Ratas Sprague-Dawley , Semillas , Serina-Treonina Quinasas TOR/metabolismo , Factor A de Crecimiento Endotelial Vascular/metabolismo , Receptor 2 de Factores de Crecimiento Endotelial Vascular/metabolismo
13.
J Food Sci ; 84(11): 3284-3295, 2019 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-31618463

RESUMEN

Pectinase is a well-known enzyme used in the food processing industry to produce fruit juice and concentrate. This study evaluated the anticancer and antiangiogenesis activities of pectinase-treated Prunus mume fruit concentrate (PC) and its phenolic components. PC treatment (250 to 1,000 µg/mL) resulted in decreased proliferation of SW480 human colorectal cancer cells through S-phase cell cycle arrest; however, equivalent concentrations of PC did not show toxicity toward CRL-1539 colon normal cells. Furthermore, PC-induced caspase-dependent apoptosis in SW480 cells, which was characterized by accumulation of apoptotic cell population, cell shrinkage, formation of apoptotic bodies, upregulation of proapoptotic Bax, cleaved PARP, caspase-3, caspase-8, and caspase-9, and downregulation of antiapoptotic Bcl-2. Antiangiogenesis effects of PC were assessed using human umbilical vein endothelial cells (HUVECs). We found that PC did not inhibit HUVECs proliferation at concentrations of 500 to 1,500 µg/mL. In addition, treatment with PC at nontoxic concentrations (500 to 1,000 µg/mL) blocked vascular endothelial growth factor induced cell migration, invasion, capillary-like tube formation, and angiogenesis from rat aortic rings. HPLC-PDA analysis showed that there were at least four different phenolics including 5-HMF, neochlorogenic acid, protocatechuic acid, and syringic acid. Taken together, these results indicated that PC could be used as a good source of phenolic compounds with selective anticancer and antiangiogenesis activities. PRACTICAL APPLICATION: Pectinases are one of the well-known enzyme used in the part of food processing. Treatment of pectinase is a useful strategy to reduce viscosity, turbidity, and pulp particles in the production of fruit juice, extract, and concentrate. In the present study, we found that pectinase-treated P. mume fruit concentrate significantly suppresses colorectal cancer proliferation and angiogenesis of human umbilical vein endothelial cells. The significance of our findings is that pectinase-treated P. mume concentrate may be used as a commercial functional food material to inhibit colorectal cancer and angiogenesis.


Asunto(s)
Inhibidores de la Angiogénesis/química , Inhibidores de la Angiogénesis/farmacología , Neoplasias Colorrectales/fisiopatología , Extractos Vegetales/química , Extractos Vegetales/farmacología , Poligalacturonasa/química , Prunus/química , Animales , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Movimiento Celular/efectos de los fármacos , Proliferación Celular/efectos de los fármacos , Neoplasias Colorrectales/genética , Neoplasias Colorrectales/metabolismo , Frutas/química , Células Endoteliales de la Vena Umbilical Humana/citología , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Células Endoteliales de la Vena Umbilical Humana/metabolismo , Humanos , Hidroxibenzoatos/química , Hidroxibenzoatos/farmacología , Fenoles/química , Fenoles/farmacología , Proteínas Proto-Oncogénicas c-bcl-2/genética , Proteínas Proto-Oncogénicas c-bcl-2/metabolismo , Ratas , Factor A de Crecimiento Endotelial Vascular/genética , Factor A de Crecimiento Endotelial Vascular/metabolismo
14.
Clin Endosc ; 50(5): 479-485, 2017 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-28669148

RESUMEN

BACKGROUND/AIMS: Few studies have evaluated the use of a smartphone application (app) for educating people undergoing colonoscopy and optimizing bowel preparation. Therefore, this study was designed to develop a smartphone app for people to use as a preparation guide and to evaluate the efficacy of this app when used prior to colonoscopy. METHODS: In total, 142 patients (male:female=84:58, mean age=43.5±9.3 years), who were scheduled to undergo a colonoscopy at Myongji Hospital, were enrolled in this study. Seventy-one patients were asked to use a smartphone app that we had recently developed to prepare for the colonoscopy, while the 71 patients of the sex and age-matched control group were educated via written and verbal instructions. RESULTS: The quality of bowel cleansing, evaluated using the Boston Bowel Preparation Scale, was significantly higher in the smartphone app group than in the control group (7.70±1.1 vs. 7.24±0.8, respectively, p=0.007 by t-test). No significant differences were found between the two groups regarding work-up time and the number of patients with polyps. CONCLUSIONS: In this study, targeting young adults (≤50 years), the bowel preparation achieved by patients using the smartphone app showed significantly better quality than that of the control group.

15.
Ann Occup Environ Med ; 29: 23, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-28652920

RESUMEN

BACKGROUND: Occupational physicians (OPs) have complex relationships with employees, employers, and the general public. OPs may have simultaneous obligations towards third parties, which can lead to variable conflicts of interests. Among the various studies of ethical issues related to OPs, few have focused on the Korean OPs. The aim of the present survey was to investigate the ethical contexts, the practical resolutions, and the ethical principles for the Korean OPs. METHODS: An email with a self-administered questionnaire was sent to members of the Korean Society of Occupational and Environmental Medicine, comprising 150 specialists and 130 residents. The questionnaire was also distributed to 52 specialists and 46 residents who attended the annual meeting of the Korean Association of Occupational and Environmental Clinics in October 2015, and to 240 specialists by uploading the questionnaire to the online community 'oem-doctors' in February 2016. The responses to each question (perception of general ethical conflicts, recognition of various ethical codes for OPs, core professional values in ethics of occupational medicine, and a mock case study) were compared between specialists and residents by the chi-squared test and Fisher's exact test. RESULTS: Responses were received from 80 specialists and 71 residents. Most participants had experienced ethical conflicts at work and felt the need for systematic education and training. OPs suffered the most ethical conflicts in decisions regarding occupational health examination and evaluation for work relatedness. Over 60% of total participants were unaware of the ethical codes of other countries. Participants thought 'consideration of worker's health and safety' (26.0%) and 'neutrality' (24.7%) as the prominent ethical values in professionality ofoccupational medicine. In mock cases, participants chose beneficence and justice for fitness for work and confidential information acquired while on duty, and beneficence and respect for autonomy in pre-placement examinations. CONCLUSIONS: This study evaluated the current perception of and attitude toward ethical issues among the Korean OPs. These findings will facilitate the development of a code of ethics and the ethical decision-making program forthe Korean OPs.

16.
Sci Rep ; 7(1): 2804, 2017 06 05.
Artículo en Inglés | MEDLINE | ID: mdl-28584248

RESUMEN

There has been controversy regarding the clinical utility of fecal occult blood test (FOBT) as a screening tool for colorectal cancer (CRC) in the general population. The purpose of this study was to examine the results of Korea national CRC screening using FOBT from 2006 to 2013 and to evaluate the implementation of the program. We analyzed the results of FOBT, colonoscopy, and the side effects during colonoscopy for the subjects (n = 20,609,909) from the Korea National Health Insurance Cancer Screening database. For evaluation of Korea national CRC screening program implementation over the 8-year period, we calculated uptake rate, FOBT positivity rate, and subsequent test compliance rate. The overall uptake rate was 30.1%, with an increasing pattern from 2006 to 2011. A relatively higher FOBT positivity rate (6.4%) and lower subsequent test compliance rate (46.6%) were observed in comparison to the results previously reported in Western countries. Side effects reported within 3 months period after colonoscopy accounted for 0.17% of all procedures, with bleeding being the most prevalent type. Although the implementation of CRC screening program using FOBT in Korea seems successful, trends in key indicators for Korea national CRC screening program should be monitored continuously.


Asunto(s)
Neoplasias Colorrectales/epidemiología , Detección Precoz del Cáncer , Sangre Oculta , Anciano , Anciano de 80 o más Años , Neoplasias Colorrectales/diagnóstico , Detección Precoz del Cáncer/métodos , Femenino , Humanos , Masculino , Tamizaje Masivo , Persona de Mediana Edad , Programas Nacionales de Salud , Vigilancia de la Población , Reproducibilidad de los Resultados , República de Corea/epidemiología
17.
J Agric Food Chem ; 65(2): 358-363, 2017 Jan 18.
Artículo en Inglés | MEDLINE | ID: mdl-28001066

RESUMEN

S-Allylcysteine (SAC), produced in large amounts during the aging process of garlic via enzymatic hydrolysis, is known as a key compound responsible for the multiple pharmacological activities of aged black garlic. This study investigated the effects of enzyme- and high hydrostatic pressure (HHP)-assisted extraction on the content of the bioactive compounds, including SAC, in black garlic juice (BGJ) and evaluated the antidiabetic effects of SAC-enriched BGJ in streptozotocin (STZ)-treated mice. The aging process increased the contents of SAC, total polyphenols, and total flavonoids in garlic juice. More importantly, pretreatment of pectinase cocktail with HHP resulted in a greater increase in those compounds during aging. Enzyme-treated BGJ reduced hyperglycemia and improved islet architecture and ß-cell function in STZ-treated mice. Moreover, these effects were more potent than those of BGJ prepared by the conventional aging process. These findings provide useful information for the production of black garlic with improved bioactivities.


Asunto(s)
Cisteína/análogos & derivados , Diabetes Mellitus Experimental/dietoterapia , Jugos de Frutas y Vegetales , Ajo/química , Hipoglucemiantes/farmacología , Animales , Apoptosis/efectos de los fármacos , Cisteína/análisis , Cisteína/farmacología , Flavonoides/análisis , Manipulación de Alimentos/métodos , Jugos de Frutas y Vegetales/análisis , Hipoglucemiantes/química , Células Secretoras de Insulina/efectos de los fármacos , Células Secretoras de Insulina/patología , Masculino , Ratones Endogámicos C57BL , Poligalacturonasa/química , Polifenoles/análisis , Estreptozocina
19.
Int J Hyg Environ Health ; 217(8): 871-7, 2014 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-25043456

RESUMEN

This study evaluated blood lead concentrations in the Korean general population and the correlation between various exposure sources using data from the 2008 Korea National Survey for Environmental Pollutants in the Human Body (National Institute of Environmental Research, Korea). The general and occupational characteristics were gathered from 5136 participants who were 20 years of age and older using a structured questionnaire. Blood lead concentrations were analyzed using an atomic absorption spectrophotometer. Statistical analysis was performed using multiple linear regressions of the log lead concentrations to the independent variables such as age, gender, smoke, herbal medication and drug consumption, drinking water, and living area. Geometric mean (GM) blood lead concentrations in Korean adults were 19.7 µg/l. The blood lead concentrations increased with age; the highest concentrations were found in the 50-69-year age group (p<0.001). Males were higher than in females (p<0.001). Current smokers and drinkers had higher concentrations than nonsmokers (p<0.001) and nondrinkers (p<0.001), respectively. People who took herbal medication and drug consumption were higher than those who did not (p<0.001). Education level was negatively associated with blood lead concentration (p<0.001). People living in or around industrial areas had elevated blood lead concentration (p<0.001). Family income was also negatively associated with lead concentration, but not significantly. For drinking water, the underground water (spring or well water) drinking group had higher concentrations than other types of water drinking groups, but not significantly (p=0.063). The blood lead concentrations by occupation were significant (p<0.034): the highest was in laborer and Agricultural-Fishery-Forestry and the lowest in office workers. In women, blood lead concentrations tended to decrease with increasing delivery times, but not significantly. The blood lead concentration (GM) of the general adult population in Korea has decreased over time from 45.8 µg/l (1999) to 19.7 µg/l (2008). Although it is still higher than in other countries such as the United States and Canada, it is rapidly decreasing. Gender, age, smoking and alcohol drinking status, herbal medication and drug consumption, education level, living area and occupation were significantly related to the blood lead concentrations in Korea.


Asunto(s)
Exposición a Riesgos Ambientales/análisis , Contaminantes Ambientales/sangre , Plomo/sangre , Adulto , Factores de Edad , Anciano , Consumo de Bebidas Alcohólicas , Agua Potable , Escolaridad , Femenino , Humanos , Modelos Lineales , Masculino , Persona de Mediana Edad , Ocupaciones , Preparaciones Farmacéuticas/administración & dosificación , Extractos Vegetales/administración & dosificación , República de Corea , Características de la Residencia , Factores Sexuales , Fumar , Espectrofotometría Atómica , Encuestas y Cuestionarios , Adulto Joven
20.
J Am Heart Assoc ; 3(1): e000650, 2014 Feb 26.
Artículo en Inglés | MEDLINE | ID: mdl-24572249

RESUMEN

BACKGROUND: The mortality rate from cardiovascular disease (CVD) among young adults has declined less than that in the older population, raising concerns about the increasing prevalence of obesity-related conditions including hypercholesterolemia in the younger population. We investigated the age-standardized mean levels of serum cholesterols and the prevalence, awareness, treatment and control rates of hyper-low-density lipoprotein (LDL)-cholesterolemia based on age. METHODS AND RESULTS: Nationally representative samples of 19 489 subjects aged ≥20 years were analyzed from the Korea National Health and Nutrition Examination Surveys 2008-2010. Hyper-LDL-cholesterolemia was individually evaluated by the 2004 National Cholesterol Education Program Adult Treatment Panel III guidelines. Age-standardized mean levels of total cholesterol, high-density lipoprotein-cholesterol, LDL-cholesterol, and triglycerides were 186.8, 48.0, 112.9, and 136.0 mg/dL, respectively. Age-standardized prevalence of hyper-LDL-cholesterolemia was 23.2% (men, 25.5%; women, 21.8%). Among subjects with hyper-LDL-cholesterolemia, awareness and treatment rates were significantly lower in younger adults (<50 years) compared to older adults ≥50 years (awareness, 8.0% versus 21.5%; treatment, 5.1% versus 18.5%, all Ps<0.001), indicating significant discrepancies in awareness and treatment rates of hypercholesterolemia between younger and older adults. Among subjects aware of their hyper-LDL-cholesterolemia, younger adults were more likely to have controlled LDL-cholesterol than the elderly (82.1% versus 67.5%, P<0.001). CONCLUSIONS: Compared to the elderly, significant proportions of young and middle-aged adults are unaware of their hypercholesterolemia and are not treated with proper lipid-lowering medications. Early screening, education, and proper management should be stressed in national public healthcare policies to reduce the increasing burden of CVD in the younger population with undiagnosed hypercholesterolemia.


Asunto(s)
Anticolesterolemiantes/uso terapéutico , Concienciación , LDL-Colesterol/sangre , Conocimientos, Actitudes y Práctica en Salud , Hipercolesterolemia , Adulto , Distribución por Edad , Factores de Edad , Anciano , Biomarcadores/sangre , Estudios Transversales , Femenino , Conductas Relacionadas con la Salud , Encuestas Epidemiológicas , Humanos , Hipercolesterolemia/sangre , Hipercolesterolemia/diagnóstico , Hipercolesterolemia/tratamiento farmacológico , Hipercolesterolemia/epidemiología , Masculino , Persona de Mediana Edad , Encuestas Nutricionales , Prevalencia , República de Corea/epidemiología , Factores de Riesgo , Factores de Tiempo , Resultado del Tratamiento , Triglicéridos/sangre , Adulto Joven
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