RESUMEN
Five undescribed lignans, cleiseberharnins A-D (1-4), cleiseberharside A (5) were isolated from the fruits of Cleistanthus eberhartii (Phyllanthaceae), together with six known aryltetralin lignans, cleistantoxin (6), picroburseranin (7), neocleistantoxin (8), 7-hydroxypicropolygamain (9), cleisindoside D (10), and cleisindoside A (11). Their structures and relative configurations were established by analysis of HRESIMS and NMR data, and quantum chemical calculations of JH,H coupling constants. The absolute configurations of 1-5 were determined by analysis of their experimental CD spectra and comparison with calculated electronic circular dichroism (ECD) spectra. All compounds (1-11) were evaluated for their cytotoxicity against KB, MCF-7, HepG-2, and Lu-1 human cancer cell lines. Among the tested compounds, compounds 6 and 7 showed strong activity against KB, MCF7, HepG2 and Lu-1 cell lines with IC50 values in the range of 0.02-0.62 µM. Compound 1 showed activity against three cancer cell lines KB, HepG2, and Lu-1 with IC50 values of 6.98, 7.61 and 11.75 µM, respectively. Compound 2 exhibited a selective inhibition with moderate cytotoxicity against Lu-1 with IC50 value of 15.30 µM. Compounds 4, 5 and 9 showed moderate activity against the three cancer cell lines with IC50 values in the range of 8.73-19.70 µM.
Asunto(s)
Antineoplásicos Fitogénicos , Antineoplásicos , Lignanos , Malpighiales , Humanos , Línea Celular Tumoral , Frutas/química , Antineoplásicos Fitogénicos/farmacología , Antineoplásicos Fitogénicos/química , Estructura Molecular , Lignanos/farmacología , Lignanos/químicaRESUMEN
Aplydactylonins A-C (1-3), three new sesquiterpenes, were isolated from the Vietnamese sea hare Aplysia dactylomela. Their structures and absolute configurations were elucidated based on spectroscopic analysis, X-ray crystallography, and density functional theory (DFT) calculations of NMR and ECD data. Compound 2 exhibited cytotoxicity against HepG2, DU145 and A549 cells with respective IC50 values of 4.08 ± 0.63, 38.64 ± 1.04 and 12.33 ± 0.95 µM. In addition, HepG2 cells treated with 5 µM compound 2 for 48 h showed a significant increase in early apoptotic cells (P < 0.05) and increased caspase 3 activity (P < 0.01). Moreover, compound 2 induced sub-G1 phase arrest in HepG2 cells.
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Liebres , Sesquiterpenos , Animales , Aplysia , Pueblo Asiatico , Humanos , Estructura Molecular , Sesquiterpenos/farmacologíaRESUMEN
Functional food plants are nature's gift to human beings to help them battle against various ailments for thousands of years. With the global pursuit of improving the quality of life, there is an increasing demand for functional plants in the world's diet. There is a long history of using Gyruna bicolor not only as a vegetable but also as a medicinal herb in East and Southeast Asia. It has been found in G. bicolor that there is a broad spectrum of nutrients and plant bioactives. G. bicolor has been acknowledged by local people as a useful source of medicine for several therapeutic treatments. This paper provides a comprehensive review of G. bicolor from updated research literature. Botanical characteristics, cultivation information, traditional uses, phytochemistry, nutrient values, as well as biological activities are discussed. The storage, processes, proposals for product development, and toxic assessment of G. bicolor are also covered. It is expected that the paper will encourage further research thereby contributing to open avenues for scientific applications of G. bicolor as a valuable plant with multiple health benefits.
Asunto(s)
Asteraceae/química , Fitoquímicos/química , Fitoterapia , Plantas Comestibles , Plantas MedicinalesRESUMEN
Childhood obesity prevalence is shooting up at a phenomenal rate worldwide, leading to long-term devastating consequences. A great number of studies have investigated factors contributing to the increase in BMI of children and adolescents. School-based, home-based and clinic-based solutions have been suggested as possible viable strategies, among which school-based interventions is believed to produce a noticeable effect on a massive scale. However, the question of whether school interventions, especially school education exert significant impact on childhood obesity or not, is left with mixing results. This article aims to holistically review the relationship between school education and childhood obesity. Various factors are covered, including health education, nutrition education, school nutrition, physical education, teachers' awareness, teaching practice and school stress, In all, school education is not the answer to childhood obesity but just part of it. More attempts from other stakeholders (parents, community, policy makers, researchers, etc.) should be made in order to solve this complicated puzzle.
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Educación en Salud/métodos , Obesidad Infantil/prevención & control , Obesidad Infantil/psicología , Instituciones Académicas/estadística & datos numéricos , Niño , HumanosRESUMEN
Two new guaiane derivatives (1 and 2) along with six known sesquiterpenoids (3-8) were isolated from the gorgonian Menella woodin. Their structures -were elucidated by ID and 2D NMR and HRESIMS data as well as by comparison of their spectra with those in the literature. Relative configurations of asymmetric centers in 1 and 2 were suggested on the basis of NOESY and ID NOE correlations, absolute stereochemistry of these compounds was proposed in result of comparison of calculated (for both enatiomers) and experimental ECD. Some suggestions were made regarding a biosynthesis of guaiane sesquiterpenoids in this species. All the compounds were firstly isolated from M woodin.
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Antozoos/química , Sesquiterpenos/química , Animales , Estructura MolecularRESUMEN
PURPOSE: High-dose-rate (HDR) brachytherapy was originally used with external beam radiation therapy (EBRT) to increase the dose to the prostate without injuring the bladder or rectum. Numerous studies have reported HDR brachytherapy is safe and effective. We adapted it for use without EBRT for cases not requiring lymph node treatment. PATIENTS AND METHODS: We entered the patient demographics, disease characteristics, and treatment parameters into a prospective registry and serially added follow-up data for 448 men with low-risk (n=288) and intermediate-risk (n=160) prostate cancer treated from 1996 to 2009. Their median age was 64 years (range 42-90). The median prostate-specific antigen (PSA) level was 6.0 ng/mL (range 0.2-18.2). The Gleason score was ≤6 in 76% and 7 in 24%. The median dose was 43.5 Gy in 6 fractions. The clinical and biochemical disease control and survival rates were calculated. Adverse events were graded according to the Common Toxicity Criteria of Adverse Events. RESULTS: The median follow-up period was 6.5 years (range 0.3-15.3). The actuarial 6- and 10-year PSA progression-free survival was 98.6% (95% confidence interval [CI] 96.9%-99.4%) and 97.8% (95% CI 95.5%-98.9%). Overall survival at 10 years was 76.7% (95% CI 69.9%-82.2%). The local control, distant metastasis-free survival, and cause-specific survival were 99.7% (95% CI 97.9%-99.9%), 98.9% (95% CI 96.3%-99.7%), and 99.1% (95% CI 95.8%-99.8%). T stage, initial PSA level, Gleason score, National Comprehensive Cancer Network risk group, patient age, and androgen deprivation therapy did not significantly correlate with disease control or survival. No late grade 3 to 4 rectal toxicities developed. Late grade 3 to 4 genitourinary toxicity occurred in 4.9% (grade 3 in 4.7%). CONCLUSIONS: HDR monotherapy is a safe and highly effective treatment of low- and intermediate-risk prostate cancer.
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Braquiterapia , Neoplasias de la Próstata/radioterapia , Adulto , Anciano , Anciano de 80 o más Años , Antagonistas de Andrógenos/uso terapéutico , Braquiterapia/efectos adversos , Braquiterapia/métodos , Coito , Supervivencia sin Enfermedad , Disfunción Eréctil/etiología , Estudios de Seguimiento , Humanos , Masculino , Persona de Mediana Edad , Clasificación del Tumor , Antígeno Prostático Específico/sangre , Neoplasias de la Próstata/sangre , Neoplasias de la Próstata/mortalidad , Neoplasias de la Próstata/patología , Traumatismos por Radiación/patología , Dosificación Radioterapéutica , Recto/efectos de la radiación , Riesgo , Factores de Tiempo , Resultado del TratamientoRESUMEN
UNLABELLED: The aim of this study was to investigate the effect of iron (Fe) availability on butyrate production in the complex bacterial ecosystem of the human gut. Hence, different Fe availabilities were mimicked in an in vitro colonic fermentation model (the polyfermenter intestinal model called PolyFermS) inoculated with immobilized gut microbiota from a child and in batch cultures of the butyrate producer Roseburia intestinalis. Shifts in the microbial community (16S rRNA sequencing and quantitative PCR), metabolic activity (high-performance liquid chromatography), and expression of genes involved in butyrate production were assessed. In the PolyFermS, moderate Fe deficiency resulted in a 1.4-fold increase in butyrate production and a 5-fold increase in butyryl-coenzyme A (CoA):acetate CoA-transferase gene expression, while very strong Fe deficiency significantly decreased butyrate concentrations and butyrate-producing bacteria compared with the results under normal Fe conditions. Batch cultures of R. intestinalis grown in a low-Fe environment preferentially produced lactate and had reduced butyrate and hydrogen production, in parallel with upregulation of the lactate dehydrogenase gene and downregulation of the pyruvate:ferredoxin-oxidoreductase gene. In contrast, under high-Fe conditions, R. intestinalis cultures showed enhanced butyrate and hydrogen production, along with increased expression of the corresponding genes, compared with the results under normal-Fe conditions. Our data reveal the strong regulatory effect of Fe on gut microbiota butyrate producers and on the concentrations of butyrate, which contributes to the maintenance of host gut health. IMPORTANCE: Fe deficiency is one of the most common nutritional deficiencies worldwide and can be corrected by Fe supplementation. In this in vitro study, we show that environmental Fe concentrations in a continuous gut fermentation model closely mimicking a child's gut microbiota strongly affect the composition of the gut microbiome and its metabolic activity, particularly butyrate production. The differential expression of genes involved in the butyrate production pathway under different Fe conditions and the enzyme cofactor role of Fe explain the observed modulation of butyrate production. Our data reveal that the level of dietary Fe reaching the colon affects the microbiome, and its essential function of providing the host with beneficial butyrate.
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Butiratos/metabolismo , Microbioma Gastrointestinal/fisiología , Hierro/metabolismo , Butiratos/química , Niño , Cromatografía Líquida de Alta Presión , Coenzima A Transferasas/genética , Coenzima A Transferasas/metabolismo , Fermentación , Microbioma Gastrointestinal/genética , Bacterias Grampositivas/metabolismo , Humanos , Hidrógeno/metabolismo , Hierro/química , L-Lactato Deshidrogenasa/genética , Piruvato-Sintasa/genética , ARN Ribosómico 16S/genéticaRESUMEN
Influenza virus H7N9 foremost emerged in China in 2013 and killed hundreds of people in Asia since they possessed all mutations that enable them to resist to all existing influenza drugs, resulting in high mortality to human. In the effort to identify novel inhibitors combat resistant strains of influenza virus H7N9; we performed virtual screening targeting the Neuraminidase (NA) protein against natural compounds of traditional Chinese medicine database (TCM) and ZINC natural products. Compounds expressed high binding affinity to the target protein was then evaluated for molecular properties to determine drug-like molecules. 4 compounds showed their binding energy less than -11 Kcal/mol were selected for molecular dynamics (MD) simulation to capture intermolecular interactions of ligand-protein complexes. The molecular mechanics/Poisson-Boltzmann surface area (MM/PBSA) method was utilized to estimate binding free energy of the complex. In term of stability, NA-7181 (IUPAC namely {9-Hydroxy-10-[3-(trifluoromrthyl) cyclohexyl]-4.8-diazatricyclo [6.4.0.02,6]dodec-4-yl}(perhydro-1H-inden-5-yl)formaldehyde) achieved stable conformation after 20 ns and 27 ns for ligand and protein root mean square deviation, respectively. In term of binding free energy, 7181 gave the negative value of -30.031 (KJ/mol) indicating the compound obtained a favourable state in the active site of the protein.
Asunto(s)
Evaluación Preclínica de Medicamentos/métodos , Subtipo H7N9 del Virus de la Influenza A/genética , Neuraminidasa/química , Neuraminidasa/genética , Antivirales/farmacología , Humanos , Subtipo H7N9 del Virus de la Influenza A/efectos de los fármacos , Subtipo H7N9 del Virus de la Influenza A/enzimología , Gripe Humana , Simulación de Dinámica Molecular , Proteínas Virales/química , Proteínas Virales/genéticaRESUMEN
This study performed phytochemical and bioactive assessments of the mangrove Lumnitzera racemosa Willd. leaves. Bioassay-guided fractionation of the methanolic extracts led to the identification of thirty-six compounds (1-36), their structures were elucidated using detailed NMR spectroscopic and MS analysis. The extracts, fractions, and the isolated compounds were screened for potential antioxidant and cytotoxic activities. Antioxidant assays were performed using peroxyl radical-scavenging and reducing assays, whereas cytotoxicity was measured using MTT assays in HL-60 and Hel-299 cell lines. The methanolic extract, CH2Cl2 and n-BuOH fractions (10.0 µg/mL) exhibited potent antioxidant activity, with Trolox equivalent (TE) values of 24.94 ± 0.59, 28.34 ± 0.20, and 27.09 ± 0.37 (µM), respectively. In addition, the isolated compounds exerted cytotoxic effects in a dose-dependent manner; compounds 1 and 14 exhibited the most potent cytotoxicity in HL-60 cells, with IC50 values of 0.15 ± 0.29 and 0.60 ± 0.16 µM, respectively. To clarify the mechanism(s) behind these cytotoxic effects, we measured the time-dependent changes in apoptotic markers including the condensation and fragmentation of nuclear chromatin, and the downregulation of p-ERK1/2, p-AKT, and c-Myc levels.
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Antioxidantes/farmacología , Combretaceae , Citotoxinas/farmacología , Extractos Vegetales/farmacología , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Apoptosis/efectos de los fármacos , Apoptosis/fisiología , Citotoxinas/química , Citotoxinas/aislamiento & purificación , Evaluación Preclínica de Medicamentos/métodos , Células HL-60 , Humanos , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Hojas de la PlantaRESUMEN
BACKGROUND: Vietnam is a country blessed with many medicinal plants widely used as food and for medicinal purposes, and they contain a host of active substances that contribute to health. However, the analysis of chemical constituents of these plant species has not been subject of literature discussion. RESULTS: In this study, the chemical compositions of essential oils of four Hedychium species, obtained by hydrodistillation, were determined by means of gas chromatography-flame ionization detector (GC-FID) and gas chromatography-mass spectrometry (GC-MS) techniques. Individually, α-pinene (52.5%) and ß-pinene (31.8%) were present in the leaf oil of Hedychium stenopetalum Lodd., while linalool (45.2%), (E)-nerolidol (8.7%) and α-pinene (5.0%) were identified in the root. The leaf of Hedychium coronarium J. König was characterized by ß-pinene (20.0%), linalool (15.8%), 1,8-cineole (10.7%), α-pinene (10.1%) and α-terpineol (8.6%); while ß-pinene (23.6%), α-humulene (17.1%) and ß-caryophyllene (13.0%) were identified in the root. Hedychium flavum Roxb., gave oil whose major compounds were ß-pinene (22.5%), α-humulene (15.7%) and ß-caryophyllene (10.4%) in the leaf; α-humulene (18.9%), ß-caryophyllene (11.8%) and ß-pinene (11.2%) in the stem, as well as ß-pinene (21.8%), linalool (17.5%) and 1,8-cineole (13.5%) in the root. The main constituents of Hedychium ellipticum Buch.-Ham. ex Smith were (E)-nerolidol (15.9%), ß-pinene (11.8%) and bornyl acetate (9.2%) in the leaf with 1,8-cineole (40.8%), α-pinene (18.3%) and ß-pinene (11.0%) occurring in the root. CONCLUSIONS: Ubiquitous monoterpenes and sesquiterpenes were identified as characteristic markers for Hedychium species. This work is of great importance for the evaluation of Hedychium essential oils grown in Vietnam.
RESUMEN
From January 2000 to July 2002, in Tuyen Quang Hospital of Traditional Medicine, 52 patients (32 male, 20 female) aged 30-37, with the syndrome of hyperlipidemia, having clinical signs of pain and weary limbs, dim sight, deteriorated memory, high blood presure and headache… A 30 days course of LP4 formula in combining with proper diet (a decoction daily). Good results reported on 27 patients, satisfied on 21, medium 2 and bad on 2. No side effect is notified