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1.
BMC Musculoskelet Disord ; 24(1): 478, 2023 Jun 13.
Artículo en Inglés | MEDLINE | ID: mdl-37312071

RESUMEN

BACKGROUND: Distal radius fracture (DRF) is very common worldwide. In particular, aging countries have numerous patients with DRF, resulting in an urgent need for active preventive measures. As few epidemiological studies have investigated DRF in Japan, we aimed to identify the epidemiological characteristics of patients of all ages with DRF in Japan. METHODS: This descriptive epidemiologic study analyzed data obtained from clinical information of patients diagnosed with DRF from January 1, 2011, to December 31, 2020, at a prefectural hospital in Hokkaido, Japan. We calculated the crude and age-adjusted annual incidences of DRF and described the age-specific incidence, injury characteristics (injury location and cause, seasonal differences, and fracture classification), and 1- and 5-year mortality rates. RESULTS: A total of 258 patients with DRF were identified, of which 190 (73.6%) were female and the mean age (standard deviation) was 67.0 (21.5) years. The crude annual incidence of DRF ranged from 158.0 to 272.6 per 100,000 population/year, and the age-adjusted incidence among female patients demonstrated a significant decreasing trend during 2011-2020 (Poisson regression analysis; p = 0.043). The age-specific incidence differed by sex, with peaks at 10-14 years for males and 75-79 years for females. The most common cause of injury was a simple fall in patients > 15 year of age and sports injuries in patients ≤ 15 years of age. DRFs were most frequently sustained outdoors and were more common in the winter season. In patients > 15 years of age, the proportions of AO/OTA fracture types A, B, and C were 78.7% (184/234), 1.7% (4/234), and 19.6% (46/234), respectively, and 29.1% (68/234) of patients received surgical treatment for DRF. The 1- and 5-year mortality rates were 2.8% and 11.9%, respectively. CONCLUSIONS: Our findings were mostly consistent with previous global studies. Although the crude annual incidence of DRF was relatively high because of recent population aging, the age-adjusted annual incidence among female patients showed a significant decreasing trend during this decade.


Asunto(s)
Fracturas Óseas , Fracturas de la Muñeca , Masculino , Humanos , Femenino , Anciano , Niño , Adolescente , Japón/epidemiología , Envejecimiento , Hospitales
2.
Allergol Int ; 72(1): 128-134, 2023 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-35817698

RESUMEN

BACKGROUND: Fermented soybean (natto)-induced hypersensitivity reactions (natto allergy) are rare and can result in late-onset anaphylaxis. The allergen in natto is considered to be poly-γ-glutamic acid (PGA), and marine sports are a risk factor for natto allergy due to epicutaneous sensitization to PGA from cnidarian stings. However, no research on natto allergy in fishery workers has yet been performed. METHODS: We conducted a chart review of inpatients diagnosed with anaphylaxis due to natto at Hokkaido Prefectural Haboro Hospital between April 1, 2009, and August 31, 2020. We also administered self-report questionnaires about food hypersensitivity reactions to Japanese fishery workers, including members of the Kitarumoi Fishery Cooperative Association and part-time workers in this area, from February 1 to May 31, 2021. RESULTS: We found six inpatients (29 inpatients with food-induced anaphylaxis among approximately 11,000 community-dwelling residents) with late-onset anaphylaxis due to natto; all were involved in scallop aquaculture. The questionnaires revealed that 27 participants had natto allergy. We divided the fishery workers into a scallop aquaculture (Scallop) group (n = 211) and other fishery group (n = 106). The Scallop group was significantly associated with natto allergy after adjustments for confounders (OR: 5.73, 95% CI: 1.46-22.56) by logistic regression analysis. In the Scallop group, older age, experience in repairing nets, and a longer length of work experience were significantly related to participants with natto allergy (n = 23), but not participants without natto allergy (n = 181). CONCLUSIONS: Our results indicated an association between scallop aquaculture and natto allergy.


Asunto(s)
Anafilaxia , Hipersensibilidad a los Alimentos , Alimentos de Soja , Humanos , Anafilaxia/diagnóstico , Anafilaxia/epidemiología , Anafilaxia/etiología , Alimentos de Soja/efectos adversos , Japón/epidemiología , Hipersensibilidad a los Alimentos/diagnóstico , Hipersensibilidad a los Alimentos/epidemiología , Hipersensibilidad a los Alimentos/etiología , Acuicultura
3.
Langmuir ; 36(4): 986-990, 2020 Feb 04.
Artículo en Inglés | MEDLINE | ID: mdl-31941269

RESUMEN

We studied the phase behavior of a ternary polymerizable gemini surfactant (PC11-6-11)/1-undecanol/water system and stabilized these liquid crystalline structures through the polymerization of surfactants. The addition of 1-undecanol to a PC11-6-11/water system formed bicontinuous cubic (V1) and reversed hexagonal (H2) liquid crystal phases in addition to hexagonal (H1) and lamellar (Lα) phases, which were also formed using the binary system of PC11-6-11/water. These new phases were formed because the fatty alcohol penetrated the palisade layer of the PC11-6-11 micelles. The polymerization of PC11-6-11 with a thermal initiator successfully preserved the Lα and H2 phases. Layered or honeycomb structures of these liquid crystals were clearly observed by transmission electron microscopy. The nanomaterials have potential applications as membranes for nano- or microfiltration and catalyst support materials.

4.
Int J Mol Sci ; 21(15)2020 Jul 30.
Artículo en Inglés | MEDLINE | ID: mdl-32751745

RESUMEN

Cell-penetrating peptide (CPP) can directly penetrate the cytosol (cytolysis) and is expected to be a potent vector for a drug delivery system (DDS). Although there is general agreement that CPP cytolysis is related to dynamic membrane deformation, a distinctive process has yet to be established. Here, we report the key process and factors controlling CPP cytolysis. To elucidate the task, we have introduced trypsin digestion of adsorbed CPP onto giant unilamellar vesicle (GUV) to quantify the adsorption and internalization (cytolysis) separately. Also, the time-course analysis was introduced for the geometric calculation of adsorption and internalization amount per lipid molecule consisting of GUV. As a result, we found that adsorption and internalization assumed to occur successively by CPP molecule come into contact with membrane lipid. Adsorption is quick to saturate within 10 min, while cytolysis of each CPP on the membrane follows successively. After adsorption is saturated, cytolysis proceeds further linearly by time with a different rate constant that is dependent on the osmotic pressure. We also found that temperature and lipid composition influence cytolysis by modulating lipid mobility. The electrolyte in the outer media is also affected as a chemical mediator to control CPP cytolysis by following the Hoffmeister effect for membrane hydration. These results confirmed the mechanism of cytolysis as temporal and local phase transfer of membrane lipid from Lα to Mesh1, which has punctured bilayer morphologies.


Asunto(s)
Permeabilidad de la Membrana Celular/efectos de los fármacos , Péptidos de Penetración Celular/química , Sistemas de Liberación de Medicamentos , Membrana Dobles de Lípidos/química , Animales , Arginina/química , Membrana Celular/efectos de los fármacos , Péptidos de Penetración Celular/farmacología , Pollos , Citosol/química , Citosol/efectos de los fármacos , Yema de Huevo/química , Fluoresceína-5-Isotiocianato/química , Lípidos de la Membrana/química , Tripsina/química , Tripsina/farmacología , Liposomas Unilamelares/química , Liposomas Unilamelares/farmacología
5.
Int J Mol Sci ; 21(19)2020 Oct 07.
Artículo en Inglés | MEDLINE | ID: mdl-33036492

RESUMEN

A specific series of peptides, called a cell-penetrating peptide (CPP), is known to be free to directly permeate through cell membranes into the cytosol (cytolysis); hence, this CPP would be a potent carrier for a drug delivery system (DDS). Previously, we proposed the mechanism of cytolysis as a temporal and local phase transfer of membrane lipid caused by positive membrane curvature generation. Moreover, we showed how to control the CPP cytolysis. Here, we investigate the phospholipid vesicle's size effect on CPP cytolysis because this is the most straightforward way to control membrane curvature. Contrary to our expectation, we found that the smaller the vesicle diameter (meaning a higher membrane curvature), the more cytolysis was suppressed. Such controversial findings led us to seek the reason for the unexpected results, and we ended up finding out that the mobility of membrane lipids as a liquid crystal is the key to cytolysis. As a result, we could explain the cause of cytolysis suppression by reducing the vesicle size (because of the restriction of lipid mobility); osmotic pressure reduction to enhance positive curvature generation works as long as the membrane is mobile enough to modulate the local structure. Taking all the revealed vital factors and their effects as a tool, we will further explore how to control CPP cytolysis for developing a DDS system combined with appropriate cargo selection to be tagged with CPPs.


Asunto(s)
Péptidos de Penetración Celular/metabolismo , Vesículas Citoplasmáticas/metabolismo , Algoritmos , Transporte Biológico , Membrana Celular/metabolismo , Permeabilidad de la Membrana Celular , Fenómenos Químicos , Vesículas Citoplasmáticas/química , Vesículas Citoplasmáticas/ultraestructura , Membrana Dobles de Lípidos/química , Modelos Teóricos , Análisis Espectral
6.
J Nanosci Nanotechnol ; 19(4): 1996-2007, 2019 04 01.
Artículo en Inglés | MEDLINE | ID: mdl-30486940

RESUMEN

Liposomes, entrapped with Job's Tears fractions, were prepared by the supercritical carbon dioxide fluid (scCO2) technique with and without sonication. Physical characteristics, which were the particle size, zeta potential, vesicular morphology, microviscosity and bioactivities including anti-proliferative, apoptotic and antioxidative activities of the S1L-S5L liposomal systems, were investigated. The potent anti-proliferative activity with the IC50 value of 4.44±2.31 ug/ml in a colon cancer cell (HT-29) was observed in the S5L. S5L also showed the apoptotic activity of 4.45±0.92% in an HT-29 cell. For antioxidative activities, the S3L showed the highest free radical scavenging activity and lipid peroxidation inhibition, whereas the S4L gave the highest metal chelating activity. This study has demonstrated the potent anti-proliferative activity on an HT-29 cell of the S5L liposomal formulation prepared by the scCO2 technique which can be further developed towards a novel anticancer drug.


Asunto(s)
Antineoplásicos , Coix , Neoplasias del Colon , Antineoplásicos/farmacología , Neoplasias del Colon/tratamiento farmacológico , Células HT29 , Humanos , Liposomas/farmacología
7.
Phys Chem Chem Phys ; 20(13): 8874-8880, 2018 Mar 28.
Artículo en Inglés | MEDLINE | ID: mdl-29546256

RESUMEN

In this study, we synthesize a novel oleic acid-based gemini surfactant with carboxylate headgroups, and study the effect of stereochemistry (anti- vs. syn-) on self-aggregation properties in water. We investigate these properties using phase diagrams, static surface tension, and one-dimensional and two-dimensional nuclear magnetic resonance (NMR) measurements. We find that a phase transition from a hexagonal liquid crystal (H1) phase to a lamellar liquid crystal (Lα) phase occurs at a lower surfactant concentration in the syn form, when compared with the anti form. In addition, the syn form gemini surfactant forms micelles with a close packing of the headgroups via hydrogen bonding. This was supported by static surface tensiometry; the area occupied by surfactant molecules at the air/aqueous solution interface is smaller for the syn form than for the anti form. We propose that, for the syn form gemini surfactant, the closer packing of the headgroups as well as the hydrogen bonding network around the micelle interface prevent water penetration into the hydrophobic part of the micelle.

8.
BMC Pulm Med ; 18(1): 88, 2018 May 23.
Artículo en Inglés | MEDLINE | ID: mdl-29792181

RESUMEN

BACKGROUND: Mortality prediction of pneumonia by severity scores in patients with multiple underlying health conditions has not fully been investigated. This prospective cohort study is to identify mortality-associated underlying health conditions and to analyse their influence on severity-based pneumonia mortality prediction. METHODS: Adult patients with community-acquired pneumonia or healthcare-associated pneumonia (HCAP) who visited four community hospitals between September 2011 and January 2013 were enrolled. Candidate underlying health conditions, including demographic and clinical characteristics, were incorporated into the logistic regression models, along with CURB (confusion, elevated urea nitrogen, tachypnoea, and hypotension) score as a measure of disease severity. The areas under the receiver operating characteristic curves (AUROC) of the predictive index based on significant underlying health conditions was compared to that of CURB65 (CURB and age ≥ 65) score or Pneumonia severity index (PSI). Mortality association between disease severity and the number of underlying health conditions was analysed. RESULTS: In total 1772 patients were eligible for analysis, of which 140 (7.9%) died within 30 days. Six underlying health conditions were independently associated: home care (adjusted odds ratio, 5.84; 95% confidence interval, CI, 2.28-14.99), recent hospitalization (2.21; 1.36-3.60), age ≥ 85 years (2.15; 1.08-4.28), low body mass index (1.99, 1.25-3.16), neoplastic disease (1.82; 1.17-2.85), and male gender (1.78; 1.16-2.75). The predictive index based on these conditions alone had a significantly or marginally higher AUROC than that based on CURB65 score (0.78 vs 0.66, p = 0.02) or PSI (0.78 vs 0.71, p = 0.05), respectively. Compared to this index, the AUROC of the total score consisting of six underlying health conditions and CURB score (range 0-10) did not improve mortality predictions (p = 0.3). In patients with one or less underlying health conditions, the mortality was discretely associated with severe pneumonia (CURB65 ≥ 3) (risk ratio: 7.24, 95%CI: 3.08-25.13), whereas in patients with 2 or more underlying health conditions, the mortality association with severe pneumonia was not detected (risk ratio: 1.53, 95% CI: 0.94-2.50). CONCLUSIONS: Mortality prediction based on pneumonia severity scores is highly influenced by the accumulating number of underlying health conditions in an ageing society. The validation using a different cohort is necessary to generalise the conclusion.


Asunto(s)
Infecciones Comunitarias Adquiridas/epidemiología , Neumonía Asociada a la Atención Médica/epidemiología , Neumonía , Medición de Riesgo/métodos , Anciano , Anciano de 80 o más Años , Área Bajo la Curva , Femenino , Disparidades en el Estado de Salud , Humanos , Japón/epidemiología , Masculino , Mortalidad , Neumonía/diagnóstico , Neumonía/mortalidad , Neumonía/fisiopatología , Valor Predictivo de las Pruebas , Pronóstico , Curva ROC , Proyectos de Investigación , Factores de Riesgo , Índice de Severidad de la Enfermedad
9.
Chem Biodivers ; 15(2)2018 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-29144597

RESUMEN

A new steroid, 20-hydroxyisofucosterol (stigmasta-5,24(28)-diene-3ß,20ß-diol) (7), along with six known compounds 1 - 6 were isolated from the MeOH extract of the leaves of Sauropus androgynus L. Merr. (Euphorbiaceae). The structure of new steroid was determined by HR-APCI-MS and various NMR techniques in combination with literature data. Subsequently, their anti-inflammatory, cytotoxic activities against five human cell lines, as well as inhibitory activities against the α-MSH induced melanogenesis on the B16 cell line were evaluated. As the results, steroid compounds, 6 and 7 exhibited moderate cytotoxic to HL60, AZ521, SKBR3, and A549 tumor cell lines (IC50 26.9 - 45.1 µm) with high tumor selectivity for A549 relative to WI38 cell lines (SI 2.6 and 3.0, resp.). And, flavonoid compounds, 4 and 5 exhibited superior inhibitory activities against melanogenesis (67.0 - 94.7% melanin content), even with no or low toxicity to the cells (90.1 - 99.6% cell viability) at the concentrations from 10 to 100 µm. Furthermore, Western blot analysis suggested that compound 5 could inhibit melanogenesis by suppressing the protein expressions of MITF, TRP-1, TRP-2, and tyrosinase.


Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Antineoplásicos Fitogénicos/farmacología , Euphorbiaceae/química , Melaninas/antagonistas & inhibidores , Estigmasterol/análogos & derivados , Animales , Antiinflamatorios no Esteroideos/química , Antiinflamatorios no Esteroideos/aislamiento & purificación , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Melaninas/genética , Melaninas/metabolismo , Melanoma Experimental/tratamiento farmacológico , Melanoma Experimental/genética , Melanoma Experimental/metabolismo , Ratones , Estructura Molecular , Hojas de la Planta/química , Estigmasterol/química , Estigmasterol/aislamiento & purificación , Estigmasterol/farmacología , Relación Estructura-Actividad , alfa-MSH/metabolismo
10.
Chem Biodivers ; 15(7): e1800137, 2018 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-29763975

RESUMEN

There is a growing interest in the exploitation of agricultural byproducts. This study explored the potential beneficial health effects from the main biowaste, tea seed pomace of Camellia oleifera Abel (Theaceae), produced when tea seed is processed. Eighteen compounds were isolated from the 70% EtOH extract of the seed cake of C. oleifera. Their structures were determined by ESI-MS, 1 H- and 13 C-NMR together with literature data. All fractions and compounds were evaluated for the antioxidant and melanogenesis inhibitory activities. As the result, AcOEt fraction has the best in vitro antioxidant and antimelanogenesis activities, compounds 7 - 12 and 15 showed remarkable antioxidant activity, compounds 4, 6, 8, and 15 - 17 exhibited superior inhibitory activities against melanogenesis. Furthermore, tyrosinase inhibitory activity assay suggested that compound 8 could suppress melanogenesis by inhibiting the expression of tyrosinase.


Asunto(s)
Antineoplásicos Fitogénicos/farmacología , Antioxidantes/farmacología , Camellia/química , Inhibidores Enzimáticos/farmacología , Melaninas/antagonistas & inhibidores , Monofenol Monooxigenasa/antagonistas & inhibidores , Extractos Vegetales/farmacología , Animales , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/aislamiento & purificación , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/aislamiento & purificación , Melaninas/metabolismo , Ratones , Estructura Molecular , Monofenol Monooxigenasa/metabolismo , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Semillas/química , Relación Estructura-Actividad
11.
BMC Infect Dis ; 17(1): 755, 2017 12 06.
Artículo en Inglés | MEDLINE | ID: mdl-29212450

RESUMEN

BACKGROUND: Various viruses are known to be associated with pneumonia. However, the impact of viral infections on adult pneumonia mortality remains unclear. This study aimed to clarify the effect of virus infection on pneumonia mortality among adults stratified by virus type and patient comorbidities. METHODS: This multicentre prospective study enrolled pneumonia patients aged ≥15 years from September 2011 to August 2014. Sputum samples were tested by in-house multiplex polymerase chain reaction assays to identify 13 respiratory viruses. Viral infection status and its effect on in-hospital mortality were examined by age group and comorbidity status. RESULTS: A total of 2617 patients were enrolled in the study and 77.8% was aged ≥65 years. 574 (21.9%) did not have comorbidities, 790 (30.2%) had chronic respiratory disease, and 1253 (47.9%) had other comorbidities. Viruses were detected in 605 (23.1%) patients. Human rhinovirus (9.8%) was the most frequently identified virus, followed by influenza A (3.9%) and respiratory syncytial virus (3.9%). Respiratory syncytial virus was more frequently identified in patients with chronic respiratory disease (4.7%) than those with other comorbidities (4.2%) and without comorbidities (2.1%) (p = 0.037). The frequencies of other viruses were almost identical between the three groups. Virus detection overall was not associated with increased mortality (adjusted risk ratio (ARR) 0.76, 95% CI 0.53-1.09). However, influenza virus A and B were associated with three-fold higher mortality in patients with chronic respiratory disease but not with other comorbidities (ARR 3.38, 95% CI 1.54-7.42). Intriguingly, paramyxoviruses were associated with dramatically lower mortality in patients with other comorbidities (ARR 0.10, 95% CI 0.01-0.70) but not with chronic respiratory disease. These effects were not affected by age group. CONCLUSIONS: The impact of virus infections on pneumonia mortality varies by virus type and comorbidity status in adults.


Asunto(s)
Neumonía/diagnóstico , Virosis/diagnóstico , Adolescente , Adulto , Anciano , Anciano de 80 o más Años , Comorbilidad , Femenino , Mortalidad Hospitalaria , Humanos , Virus de la Influenza A/genética , Virus de la Influenza A/aislamiento & purificación , Masculino , Persona de Mediana Edad , Reacción en Cadena de la Polimerasa Multiplex , Neumonía/epidemiología , Neumonía/mortalidad , Neumonía/virología , Estudios Prospectivos , ARN Viral/aislamiento & purificación , ARN Viral/metabolismo , Virus Sincitial Respiratorio Humano/genética , Virus Sincitial Respiratorio Humano/aislamiento & purificación , Infecciones del Sistema Respiratorio/diagnóstico , Infecciones del Sistema Respiratorio/epidemiología , Infecciones del Sistema Respiratorio/mortalidad , Infecciones del Sistema Respiratorio/virología , Rhinovirus/genética , Rhinovirus/aislamiento & purificación , Riesgo , Virosis/epidemiología , Virosis/mortalidad , Virosis/virología , Adulto Joven
12.
Chem Biodivers ; 14(6)2017 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-28145090

RESUMEN

Seventy-three limonoids isolated from three Meliaceae plants, Azadirachta indica, A. indica var. siamensis, and Melia azedarach, or semi-synthesized from the Meliaceae limonoids, were evaluated for their inhibitory activity against nitric oxide (NO) production in mouse macrophage RAW 264.7 cells induced by lipopolysaccharide (LPS), as a primary screening test for anti-inflammatory agents. Of the compounds tested, 21 compounds exhibited inhibitory activity (IC50 4.6 - 58.6 µm) without any significant toxicity (IC50 > 100 µm) which were more potent than l-NMMA (NO-production inhibitory activity, IC50 65.6 µm; cytotoxicity, IC50 > 100 µm), and among which, nine compounds, i.e., 17-hydroxy-15-methoxynimbocinol (6), ohchinin (20), 1-cis-cinnamoyl-1-decinnamoylohchinin (24), salannin (27), methyl nimbidate (32), isosalannin (55), nimbolinin D (58), mesendanin E (69), and 7-deacetylgedunin (73) exhibited potent inhibitory activity (IC50 4.6 - 29.3 µm). In particular, compounds 6 (IC50 7.3 µm), an azadirone-type limonoid, and 73 (IC50 4.6 µm), a gedunin-type limonoid, exhibited remarkable activity. Western blot analysis revealed that 27 and 73 reduced the expression levels of the inducible NO synthase and cyclooxygenase-2 proteins in a concentration-dependent manner. These findings suggest that limonoids of A. indica, A. indica var. siamensis, and M. azedarach, and their semi-synthetic derivatives may be effective against inflammation.


Asunto(s)
Antiinflamatorios/aislamiento & purificación , Azadirachta/química , Limoninas/farmacología , Melia azedarach/química , Óxido Nítrico/biosíntesis , Animales , Antiinflamatorios/farmacología , Inhibidores de la Ciclooxigenasa 2 , Concentración 50 Inhibidora , Ratones , Óxido Nítrico/antagonistas & inhibidores , Óxido Nítrico Sintasa de Tipo II/antagonistas & inhibidores , Células RAW 264.7
13.
Chem Biodivers ; 14(7)2017 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-28425165

RESUMEN

Four limonoids, 1 - 4, five alkaloids, 5 - 9, and four phenolic compounds, 10 - 13, were isolated from a MeOH extract of the bark of Phellodendron amurense (Rutaceae). Among these, compound 13 was new, and its structure was established as rel-(1R,2R,3R)-5-hydroxy-3-(4-hydroxy-3-methoxyphenyl)-6-methoxy-1-(methoxycarbonylmethyl)indane-2-carboxylic acid methyl ester (γ-di(methyl ferulate)) based on the spectrometric analysis. Upon evaluation of compounds 1 - 13 against the melanogenesis in the B16 melanoma cells induced with α-melanocyte-stimulating hormone (α-MSH), four compounds, limonin (1), noroxyhydrastinine (6), haplopine (7), and 4-methoxy-1-methylquinolin-2(1H)-one (8), exhibited potent melanogenesis-inhibitory activities with almost no toxicity to the cells. Western blot analysis revealed that compound 6 inhibited melanogenesis, at least in part, by inhibiting the expression of protein levels of tyrosinase, TRP-1, and TRP-2 in α-MSH-stimulated B16 melanoma cells. In addition, when compounds 1 - 13 were evaluated for their cytotoxic activities against leukemia (HL60), lung (A549), duodenum (AZ521), and breast (SK-BR-3) cancer cell lines, five compounds, berberine (5), 8, canthin-6-one (9), α-di-(methyl ferulate) (12), and 13, exhibited cytotoxicities against one or more cancer cell lines with IC50 values in the range of 2.6 - 90.0 µm. In particular, compound 5 exhibited strong cytotoxicity against AZ521 (IC50 2.6 µm) which was superior to that of the reference cisplatin (IC50 9.5 µm).


Asunto(s)
Antineoplásicos Fitogénicos/aislamiento & purificación , Phellodendron/química , Alcaloides/aislamiento & purificación , Alcaloides/farmacología , Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Carcinogénesis , Línea Celular Tumoral , Humanos , Concentración 50 Inhibidora , Limoninas/aislamiento & purificación , Limoninas/farmacología , Melanoma Experimental/patología , Metanol , Fenoles/aislamiento & purificación , Fenoles/farmacología , Corteza de la Planta/química , Extractos Vegetales
14.
Chem Biodivers ; 14(12)2017 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-28960771

RESUMEN

Seven phenolic compounds, 1 - 7, including a new organic acid gallate, mucic acid 1-ethyl 6-methyl ester 2-O-gallate (7), were isolated from the MeOH extract of the fruits of Phyllanthus emblica L. (Euphorbiaceae). The structures were elucidated on the basis of extensive spectroscopic analysis and comparison with literature data. Upon evaluated for their antioxidant abilities by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS), and ferric reducing antioxidant power (FRAP) assays. The inhibitory activities against melanogenesis in B16 melanoma cells induced by α-MSH, as well as cytotoxic activities against four human cancer cell lines were also evaluated. All phenolic compounds, 1 - 7, exhibited potent antioxidant abilities (DPPH: IC50 5.6 - 12.9 µm; ABTS: 0.87 - 8.43 µm Trolox/µm; FRAP: 1.01 - 5.79 µm Fe2+ /µm, respectively). Besides, 5 - 7, also exhibited moderate inhibitory activities against melanogenesis (80.7 - 86.8% melanin content), even with no or low toxicity to the cells (93.5 - 101.6% cell viability) at a high concentration of 100 µm. Compounds 1 - 3 exhibited cytotoxic activity against one or more cell lines (IC50 13.9 - 68.4%), and compound 1 with high tumor selectivity for A549 (SI 3.2).


Asunto(s)
Antineoplásicos Fitogénicos/química , Fenoles/química , Phyllanthus emblica/química , Células A549 , Animales , Antineoplásicos Fitogénicos/aislamiento & purificación , Antineoplásicos Fitogénicos/toxicidad , Antioxidantes/química , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Frutas/química , Frutas/metabolismo , Células HL-60 , Humanos , Espectroscopía de Resonancia Magnética , Melaninas/metabolismo , Ratones , Conformación Molecular , Fenoles/aislamiento & purificación , Fenoles/farmacología , Phyllanthus emblica/metabolismo , Extractos Vegetales/química
15.
Mol Pharm ; 13(12): 4034-4042, 2016 12 05.
Artículo en Inglés | MEDLINE | ID: mdl-27749081

RESUMEN

The effect of carrier morphology on the intestinal absorption of insulin was investigated using a morphology-tunable polymeric carrier, ß-cyclodextrin-grafted chitosan (BCC). The insulin-BCC complexes were prepared in either acetate or citrate buffer solutions, followed by dilution with phosphate buffer for the administration. The complex had a molecular network structure in the acetate buffer, whereas nanoparticles formed in the citrate buffer. The network structure in the acetate buffer was maintained even after dilution with a phosphate buffer, but the nanoparticles in the citrate buffer caused aggregation after dilution. Both complexes enhanced the intestinal absorption of insulin. Interestingly, their absorption profiles were totally different; prompt absorption was observed for the complex prepared in acetate buffer, whereas sustained absorption was observed for the complex prepared in citrate buffer. The difference in the absorption patterns was attributed to the difference in the complex morphology. Next, penetratin, a cell-penetrating peptide, was grafted to BCC to find further improvement in the absorption behavior. A simple mixture of penetratin and BCC was also effective. An oral administration study was also conducted in mice to observe effective suppression of glucose levels, which was further enhanced by coadministration of penetratin. Thus, BCC was proven to be an effective carrier for enhancing oral absorption of peptide drugs, and it is suggested that the carrier morphology is also an important factor that influences the absorption profile.


Asunto(s)
Proteínas Portadoras/administración & dosificación , Péptidos de Penetración Celular/administración & dosificación , Quitosano/química , Portadores de Fármacos/química , Hipoglucemiantes/administración & dosificación , Insulina/administración & dosificación , Absorción Intestinal/efectos de los fármacos , beta-Ciclodextrinas/química , Administración Oral , Animales , Disponibilidad Biológica , Proteínas Portadoras/química , Péptidos de Penetración Celular/química , Sistemas de Liberación de Medicamentos , Hipoglucemiantes/química , Insulina/química , Masculino , Ratones , Nanopartículas/química , Ratas , Ratas Sprague-Dawley
16.
Planta ; 241(1): 83-93, 2015 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-25218793

RESUMEN

MAIN CONCLUSION: Enzymatic activities of Oryza sativa expansins, which were heterologously overexpressed in Escherichia coli , were analyzed. Results suggested that expansins promote degradation of cellulose by cellulase in a synergistic manner. Sustainable production of future biofuels is dependent on efficient saccharification of lignocelluloses. Expansins have received a lot of attention as proteins promoting biological degradation of cellulose using cellulase. The expansins are a class of plant cell wall proteins that induce cell wall loosening without hydrolysis. In this study, the expansins from Oryza sativa were classified using phylogenetic analysis and five proteins were selected for functional evaluation. At low cellulose loading, the cellulase in expansin mixtures was up to 2.4 times more active than in mixtures containing only cellulase, but at high cellulose loading the activity of cellulase in expansin mixtures and cellulase only mixtures did not differ. Furthermore, expansin activity was greater in cellulase mixtures compared with cellulase-deficient mixtures. Therefore, the expansins showed significant synergistic activity with cellulase. Expansin may play an important role in efficient saccharification of cellulose.


Asunto(s)
Celulasa/metabolismo , Celulosa/metabolismo , Oryza/metabolismo , Proteínas de Plantas/metabolismo , Pared Celular/metabolismo , Celulosa/química , Cristalización , Electroforesis en Gel de Poliacrilamida , Hidrólisis , Modelos Biológicos , Oryza/genética , Filogenia , Proteínas de Plantas/clasificación , Proteínas de Plantas/genética , Unión Proteica , Difracción de Rayos X
17.
Langmuir ; 31(22): 6085-91, 2015 Jun 09.
Artículo en Inglés | MEDLINE | ID: mdl-25996798

RESUMEN

Effects of the addition of water on solvation layers of imidazolium-type room temperature ionic liquids (RT-ILs) have been studied through force curve measurements of atomic force microscopy (AFM). Two kinds of RT-ILs were employed in this study; one is a hydrophilic RT-IL (1-butyl-3-methylimidazolium tetrafluoroborate, BmimBF4), and the other is a hydrophobic one (1-ethyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide, EmimTFSI). These RT-ILs form solvation layers on hydrophilic solid substances (i.e., silica and mica) in the absence of added water. The addition of water into BmimBF4 resulted in the disruption of the solvation layers and then the formation of an interfacial water phase on silica. In contrast, the formation of the interfacial water phase was not evidenced on mica because of the absence of hydrogen-bonding sites on the mica surface. Interestingly, the addition of water into EmimTFSI induced the formation of the interfacial water phase on the two solid surfaces. In the EmimTFSI system, importantly, significantly greater adhesion forces were observed on silica than on mica. This reflects the different formation mechanisms of the interfacial water phase on the two solid surfaces. We conclude that the hydrogen bonding is a key factor in determining whether water molecules can be adsorbed on the solid surfaces, but it is also necessary to take into account the hydrophilic/hydrophobic nature of the RT-ILs.

18.
Phys Chem Chem Phys ; 17(29): 19474-83, 2015 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-26145125

RESUMEN

A new series of ester functionalized cationic gemini surfactants having different cationic headgroups (i.e. piperidinium, pyrrolidinium, morpholinium and quaternary ammonium) have been synthesized and characterized using NMR and Mass spectroscopy. These new gemini surfactants were investigated for their micellization and viscosity properties using surface tension, conductivity, fluorescence and rheology thechniques. The physicochemical properties of the aqueous surfactant system were influenced by polarity, size and the nature of cationic headgroups as the surface, thermodynamic and viscosity properties of these gemini surfactants were found to be dependent on the type of cationic headgroup. The current research finding establishes the structure-property relationship of the surfactant molecule specifically taking into account the dominant role displayed by the nature of the cationic headgroup.

19.
Appl Microbiol Biotechnol ; 99(14): 5833-41, 2015 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-25957491

RESUMEN

To develop a structural homolog of mannosylerythritol lipids (MELs), Pseudozyma tsukubaensis JCM16987 (known to be a specific producer of the diastereomer type of mono-acetylated MEL (MEL-B)) was cultivated in medium containing 4 % (w/v) olive oil as the primary carbon source and 4 % L-arabitol as the supplemental sugar alcohol. Based on thin-layer chromatography (TLC), the glycolipid extract showed two major spots corresponding to MEL-B and an unknown glycolipid (GL1). Based on high-performance liquid chromatography after acid hydrolysis, GL1 from the L-arabitol culture showed two primary peaks identical to mannose and arabitol using the sugar analysis column, and one peak identical to L-arabitol was detected using the chiral resolution column. Based on NMR analysis, GL1 was identified as mono-acetylated mannosyl-L-arabitol lipid (MLAL-B) consisting of mannose, with L-arabitol as the sugar moiety. The observed critical micelle concentration (CMC) and surface tension at the CMC (γCMC) of MLAL-B were 1.2 × 10(-5) M and 32.8 mN/m, which were significantly higher than MEL-B (CMC = 3.1 × 10(-6) M and γcmc = 26.1 mN/m). Furthermore, based on a water-penetration scan, MLAL-B efficiently formed lamellar phase (Lα) and myelins at a broad concentration range. Thus, the present glycolipid showed higher hydrophilicity and/or water solubility and increased our understanding of environmentally advanced biosurfactants.


Asunto(s)
Glucolípidos/metabolismo , Ustilaginales/metabolismo , Carbono/metabolismo , Cromatografía Líquida de Alta Presión , Cromatografía en Capa Delgada , Medios de Cultivo/química , Interacciones Hidrofóbicas e Hidrofílicas , Espectroscopía de Resonancia Magnética , Aceite de Oliva/metabolismo , Alcoholes del Azúcar/metabolismo , Ustilaginales/crecimiento & desarrollo
20.
Chemistry ; 20(49): 16293-300, 2014 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-25297535

RESUMEN

Memory operations based on variation of a molecule's properties are important because they may lead to device miniaturization to the molecular scale or increasingly complex information processing protocols beyond the binary level. Molecular memory also introduces possibilities related to information-storage security where chemical information (or reagents) might be used as an encryption key, in this case, acidic/basic reagents. Chemical memory that possesses both volatile and non-volatile functionality requires reversible conversion between at least two chemically different stable or quasi-stable states. Here we have developed the phenol-phenoxide equilibrium of phenol fluorophores as a data storage element, which can be used to write or modulate data using chemical reagents. The properties of this system allow data to be stored and erased either in non-volatile or volatile modes. We also demonstrate non-binary switching of states made possible by preparation of  a composite containing the molecular memory elements.

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