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1.
Harmful Algae ; 129: 102523, 2023 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-37951622

RESUMEN

Floating macroalgae of Sargassum horneri (S. horneri) in the East China Sea (ECS) has increased in recent years, with ocean warming being one of the driving factors. Yet their possible origins, based on a literature review, are unclear. Here, using multi-sensor high-resolution remote sensing data and numerical experiments for the period of 2015-2023, we show two possible origins of the ECS floating S. horneri, one being local near the Zhejiang coast with initiation in January-February and the other being remote (> 800 km from the first) in the Bohai Sea with initiation in June-November. While their drifting pathways are revealed in the sequential remote sensing imagery, numerical experiments suggest that S. horneri from the remote origin (Bohai Sea) can hardly meander through the strong Yangtze River frontal zone, which may serve as a "wall" to prevent trespassing of surface floating seaweed to the south of the frontal zone, where S. horneri has a local origin. PLAIN LANGUAGE SUMMARY: Sargassum horneri (S. horneri) is a brown macroalgae (seaweed) abundant in surface waters of the East China Sea (ECS), which can serve as a moving habitat, but can also cause major beaching events and environmental problems. Knowledge of its origins is important to help implement mitigation strategies and understand possible ecological impacts along its drifting pathways. Using high-resolution remote sensing images and numerical experiments, we track floating S. horneri in space and time between 2015 and 2023. Two possible origins are identified, one being far away from the ECS and the other being local, both of which are known to have benthic S. horneri. The study also reveals how S. horneri are transported from their source regions resulting in large-scale distributions previously observed in medium-resolution satellite imagery.


Asunto(s)
Sargassum , Algas Marinas , Ecosistema , China
2.
ACS Nano ; 17(8): 7475-7486, 2023 04 25.
Artículo en Inglés | MEDLINE | ID: mdl-37057972

RESUMEN

The therapy of solid tumors is always hampered by the intrinsic tumor physical microenvironment (TPME) featured with compact and rigid extracellular matrix (ECM) microstructures. Herein, we introduce nattokinase (NKase), a thrombolytic healthcare drug, to comprehensively regulate the TPME for versatile enhancement of various therapy modalities. Intratumoral injection of NKase not only degrades the major ECM component fibronectin but also inhibits cancer-associated fibroblasts (CAFs) in generating fibrosis, resulting in decreased tumor stiffness, enhanced perfusion, and hypoxia alleviation. The NKase-mediated regulation of the TPME significantly promotes the tumoral accumulation of therapeutic agents, leading to efficient chemotherapy without inducing side effects. Additionally, the enhancement of tumor radiotherapy based on radiosensitizers was also achieved by the pretreatment of intratumorally injected NKase, which could be ascribed to the elevated oxygen saturation level in NKase-treated tumors. Moreover, a xenografted human breast MDB-MA-231 tumor model is established to evaluate the influence of NKase on chimeric antigen receptor (CAR)-T cell therapy, illustrating that the pretreatment of NKase could boost the infiltration of CAR-T cells into tumors and thus be a benefit for tumor inhibition. These findings demonstrate the great promise of the NKase-regulated TPME as a translational strategy for universal enhancement of therapeutic efficacy in solid tumors by various treatments.


Asunto(s)
Neoplasias de la Mama , Neoplasias , Receptores Quiméricos de Antígenos , Animales , Humanos , Femenino , Receptores Quiméricos de Antígenos/metabolismo , Linfocitos T , Neoplasias/terapia , Inmunoterapia Adoptiva/métodos , Neoplasias de la Mama/metabolismo , Modelos Animales de Enfermedad , Microambiente Tumoral
3.
Sensors (Basel) ; 23(8)2023 Apr 19.
Artículo en Inglés | MEDLINE | ID: mdl-37112435

RESUMEN

Deep learning anomaly detection is important in distributed optical fiber acoustic sensing (DAS). However, anomaly detection is more challenging than traditional learning tasks, due to the scarcity of true-positive data and the vast imbalance and irregularity within datasets. Furthermore, it is impossible to catalog all types of anomalies, therefore, the direct application of supervised learning is deficient. To overcome these problems, an unsupervised deep learning method that only learns the normal data features from ordinary events is proposed. First, a convolutional autoencoder is used to extract DAS signal features. A clustering algorithm then locates the feature center of the normal data, and the distance to the new signal is used to determine whether it is an anomaly. The efficacy of the proposed method was evaluated in a real high-speed rail intrusion scenario, and considered all behaviors that may threaten the normal operation of high-speed trains as abnormal. The results show that the threat detection rate of this method reaches 91.5%, which is 5.9% higher than that of the state-of-the-art supervised network and, at 7.2%, the false alarm rate is 0.8% lower than the supervised network. Moreover, using a shallow autoencoder reduces the parameters to 1.34 K, which is significantly lower than the 79.55 K of the state-of-the-art supervised network.

4.
Photochem Photobiol ; 99(3): 1010-1019, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-36094140

RESUMEN

Nonphotochemical quenching (NPQ) is known to depress in vivo fluorescence (IVF) of chlorophyll a (Chla) in aquatic environments, which makes it difficult to interpret the hour-to-hour variations in Chla measured by in situ fluorometers. We hypothesized that ratios between quenched and unquenched IVF are a function of both NPQ and photochemical quenching. In this study, two diatom model species Thalassiosira pseudonana (CCMP1335) and Thalassiosira weissflogii (CCMP1047) incubated under a sinusoidal light:dark cycle were studied; IVF was recorded continuously, and Chla and photo-physiological variables were measured seven times a day. The maximal decline in Chla-specific IVF (IVFB ) attributable to quenching was 50% under the experimental settings. An NPQ and photochemical quenching-based modeling equation exhibited a better match to the measured IVFB than equations representing the sole NPQ effect. Photochemical quenching induced by measuring light beam varied substantially during the day, and the part of the model for this process is excitation intensity-dependent (which is differed between models of in situ fluorometers, implying no straightforward method to correct Chla for all instrument models, instrument-specific parameterization is required). The forms of the IVFB -light relationship are discussed as well. The findings foster a holistic understanding of NPQ effects on in vivo Chla fluorometry.


Asunto(s)
Clorofila , Diatomeas , Clorofila A , Luz , Fluorometría/métodos , Fluorescencia , Complejo de Proteína del Fotosistema II
5.
Water Res ; 166: 115070, 2019 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-31525510

RESUMEN

Predicting changes of phytoplankton communities in response to global warming is one of the challenges of ecological forecasting. One of the constraints is the paucity of general principles applicable to community ecology. Based on a synecological analysis of a decadal-scale database, we created a niche habitat classification scheme relating nine phytoplankton groups to fifteen statistically refined realized niches comprised of three niche dimensions: temperature, irradiance, and nitrate concentrations. The niche scheme assigned the nine phytoplankton groups to three types of niches: a cold type, a warm type, and a type associated with high irradiance and high nitrate concentrations. The fact that phytoplankton groups in cold niches were governed by irradiance and those in warm niches by nitrate is consistent with general ecological theories, but the fact that diatoms were the only dominant group in high-irradiance, high-nitrate niches challenges the idea based on autecological studies that diatoms are generally better adapted to low-irradiance, high-nutrient conditions. When combined with an irradiance model, the niche scheme revealed that photoinhibition of Prochlorococcus, which is predicted from autecological studies, is a function of temperature. We used the niche scheme to predict the responses of phytoplankton communities to environmental changes due to seawater warming and eutrophication. The results of the study suggest that a synecological analysis of large databases from field studies facilitates identification of general principles of community ecology that can be used to forecast responses of biological communities to environmental changes.


Asunto(s)
Diatomeas , Fitoplancton , Ecosistema , Eutrofización , Agua de Mar
6.
Front Microbiol ; 9: 1589, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-30116223

RESUMEN

The various photosynthetic apparatus and light utilization strategies of phytoplankton are among the critical factors that regulate the distribution of phytoplankton and primary productivity in the ocean. Active chlorophyll fluorescence has been a powerful technique for assessing the nutritional status of phytoplankton by studying the dynamics of photosynthesis. Further studies of the energetic stoichiometry between light absorption and carbon fixation have enhanced understanding of the ways phytoplankton adapt to their niches. To explore the ecophysiology of a Prochlorococcus-dominated phytoplankton assemblage, we conducted studies of the diel patterns of variable fluorescence and carbon fixation by phytoplankton in the oligotrophic South China Sea (SCS) basin in June 2017. We found that phytoplankton photosynthetic performance at stations SEATS and SS1 were characterized by a nocturnal decrease, dawn maximum, and midday decrease of the maximum quantum yield of PSII ( Fv(') / Fm(') , which has been denoted as both Fv/Fm and Fv' / Fm' ) in the nutrient-depleted surface layer. That these diel patterns of Fv(') / Fm(') were similar to those in the tropical Pacific Ocean suggests macro-nutrient and potentially micro-nutrient stress. However, the fact that variations were larger in the central basin than at the basin's edge implied variability in the degree of nutrient limitation in the basin. The estimated molar ratio of gross O2 production to net production of carbon (GOP:NPC) of 4.9:1 was similar to ratios reported across the world's oceans. The narrow range of the GOP:NPC ratios is consistent with the assumption that there is a common strategy for photosynthetic energy allocation by phytoplankton. That photo-inactivated photosystems or nonphotochemical quenching rather than GOP accounted for most of the radiation absorbed by phytoplankton explains why the maximum quantum yield of carbon fixation was rather low in the oligotrophic SCS.

7.
Sci Total Environ ; 633: 618-629, 2018 Aug 15.
Artículo en Inglés | MEDLINE | ID: mdl-29597159

RESUMEN

Increases of atmospheric CO2 concentrations due to human activity and associated effects on aquatic ecosystems are recognized as an environmental issue at a global scale. Growing attention is being paid to CO2 enrichment effects under multiple stresses or fluctuating environmental conditions in order to extrapolate from laboratory-scale experiments to natural systems. We carried out a mesocosm experiment in coastal water with an assemblage of three model phytoplankton species and their associated bacteria under the influence of elevated CO2 concentrations. Net community production and the metabolic characteristics of the phytoplankton and bacteria were monitored to elucidate how these organisms responded to CO2 enrichment during the course of the algal bloom. We found that CO2 enrichment (1000µatm) significantly enhanced gross primary production and the ratio of photosynthesis to chlorophyll a by approximately 38% and 39%, respectively, during the early stationary phase of the algal bloom. Although there were few effects on bulk bacterial production, a significant decrease of bulk bacterial respiration (up to 31%) at elevated CO2 resulted in an increase of bacterial growth efficiency. The implication is that an elevation of CO2 concentrations leads to a reduction of bacterial carbon demand and enhances carbon transfer efficiency through the microbial loop, with a greater proportion of fixed carbon being allocated to bacterial biomass and less being lost as CO2. The contemporaneous responses of phytoplankton and bacterial metabolism to CO2 enrichment increased net community production by about 45%, an increase that would have profound implications for the carbon cycle in coastal marine ecosystems.


Asunto(s)
Contaminantes Atmosféricos/toxicidad , Dióxido de Carbono/toxicidad , Ecosistema , Eutrofización/efectos de los fármacos , Fitoplancton/efectos de los fármacos , Agua de Mar/microbiología , Contaminantes Atmosféricos/análisis , Bacterias/efectos de los fármacos , Bacterias/crecimiento & desarrollo , Dióxido de Carbono/análisis , Clorofila/análisis , Clorofila/metabolismo , Clorofila A , Fotosíntesis , Fitoplancton/metabolismo , Agua de Mar/química
8.
Front Microbiol ; 9: 3259, 2018.
Artículo en Inglés | MEDLINE | ID: mdl-30687258

RESUMEN

Picoeukaryotes play an important role in the biogenic element cycle and energy flow in oligotrophic ecosystems. However, their biodiversity and activity are poorly studied in open ocean systems, such as the northwestern Pacific Ocean, which is characterized by a complex hydrological setting. Here, we investigated the diversity and activity of picoeukaryotes in the northwestern Pacific Ocean using high-throughput sequencing targeting the V9 region of 18S rDNA and rRNA. Our results showed that the DNA picoeukaryotic communities were mainly represented by Mamiellophyceae, MAST, MALV-II, Spirotrichea, Prymnesiophyceae, and MALV-I (69.33% of the total DNA reads), and the RNA communities were dominated by Spirotrichea, Mamiellophyceae, MAST, Pelagophyceae, and MALV-II (67.46% of the total RNA reads). The number of operational taxonomic units (OTUs) was significantly affected by temperature and salinity, and was decreased with the increasing nutrient concentration both in the DNA and RNA surveys. Significant differences were observed in the community composition between DNA-based and RNA-based molecular approaches, and these differences were mainly attributed to Mamiellophyceae, Spirotrichea, and Pelagophyceae. The RNA: DNA ratio was used as a proxy for relative metabolic activity of the individual OTUs. We found that the relative metabolic activities of Mamiellophyceae, Spirotrichea, and Pelagophyceae species in the northwestern Pacific Ocean were highly affected by the nutrient concentration, i.e., the NO3 + NO2 and SiO3 concentration. Overall, our study shed light on picoeukaryotic diversity and distribution in the northwestern Pacific Ocean and revealed the correlation between the diversity, relative metabolic activities of marine picoeukaryotes, and the environmental factors.

9.
PLoS One ; 11(4): e0153735, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-27088991

RESUMEN

It is widely recognized that the mesoscale eddies play an important part in the biogeochemical cycle in ocean ecosystem, especially in the oligotrophic tropical zones. So here a heterogeneous cyclonic eddy in its flourishing stage was detected using remote sensing and in situ biogeochemical observation in the western South China Sea (SCS) in early September, 2007. The high-performance liquid chromatography method was used to identify the photosynthetic pigments. And the CHEMical TAXonomy (CHEMTAX) was applied to calculate the contribution of nine phytoplankton groups to the total chlorophyll a (TChl a) biomass. The deep chlorophyll a maximum layer (DCML) was raised to form a dome structure in the eddy center while there was no distinct enhancement for TChl a biomass. The integrated TChl a concentration in the upper 100 m water column was also constant from the eddy center to the surrounding water outside the eddy. However the TChl a biomass in the surface layer (at 5 m) in the eddy center was promoted 2.6-fold compared to the biomass outside the eddy (p < 0.001). Thus, the slight enhancement of TChl a biomass of euphotic zone integration within the eddy was mainly from the phytoplankton in the upper mixed zone rather than the DCML. The phytoplankton community was primarily contributed by diatoms, prasinophytes, and Synechococcus at the DCML within the eddy, while less was contributed by haptophytes_8 and Prochlorococcus. The TChl a biomass for most of the phytoplankton groups increased at the surface layer in the eddy center under the effect of nutrient pumping. The doming isopycnal within the eddy supplied nutrients gently into the upper mixing layer, and there was remarkable enhancement in phytoplankton biomass at the surface layer with 10.5% TChl a biomass of water column in eddy center and 3.7% at reference stations. So the slight increasing in the water column integrated phytoplankton biomass might be attributed to the stimulated phytoplankton biomass at the surface layer.


Asunto(s)
Tormentas Ciclónicas , Ecosistema , Modelos Teóricos , Fotosíntesis/fisiología , Fitoplancton/fisiología , China , Frío , Alimentos , Océanos y Mares
10.
Chem Commun (Camb) ; 50(30): 3996-9, 2014 Apr 18.
Artículo en Inglés | MEDLINE | ID: mdl-24615183

RESUMEN

A concise palladium-catalyzed method for oxidative C-H/C-H cross-coupling between benzothiazoles and thiophenes/thiazoles has been developed. This CDC reaction is insensitive to air and moisture with high functional group tolerance.


Asunto(s)
Benzotiazoles/química , Paladio/química , Tiazoles/química , Tiofenos/química , Catálisis , Estructura Molecular , Oxidación-Reducción
11.
Org Biomol Chem ; 11(16): 2582-5, 2013 Apr 28.
Artículo en Inglés | MEDLINE | ID: mdl-23503621

RESUMEN

A one-pot two-step synthesis of versatile indenones has been developed. This palladium(II)-catalyzed transformation involves generation and condensation of ortho-functionalized 1,2-benzils from 2-(2-arylethynylphenyl)acetonitriles using Ph2SO as the oxidant. The resulting 3-cyanoindenones can be converted to various valuable molecules.


Asunto(s)
Acetonitrilos/química , Hidrocarburos Aromáticos/síntesis química , Nitrilos/síntesis química , Paladio/química , Acetonitrilos/síntesis química , Catálisis , Ciclización , Hidrocarburos Aromáticos/química , Nitrilos/química , Oxidación-Reducción
12.
Org Biomol Chem ; 11(16): 2574-7, 2013 Apr 28.
Artículo en Inglés | MEDLINE | ID: mdl-23487245

RESUMEN

A novel Pd/Cu catalyzed domino reaction for the synthesis of functionalized pyrrolo[1,2-b]pyridazines from readily accessible (hetero)aryl propargyl alcohols and 1-amino-2-bromopyrroles was developed. This cascade process involves a Sonogashira cross-coupling reaction, an isomerization and an intramolecular condensation.


Asunto(s)
Piridazinas/síntesis química , Pirroles/síntesis química , Alquinos/síntesis química , Alquinos/química , Catálisis , Cobre/química , Halogenación , Isomerismo , Paladio/química , Propanoles/síntesis química , Propanoles/química , Piridazinas/química , Pirroles/química
13.
Org Biomol Chem ; 10(38): 7730-8, 2012 Oct 14.
Artículo en Inglés | MEDLINE | ID: mdl-22903499

RESUMEN

An efficient general synthetic approach has been developed to synthesize pyrazole-containing bisphosphonate (N-BPs) esters from chromenone derivatives via a sequential two-step reaction in one pot at ambient temperature in good to excellent yields. This protocol provides a new convenient method to prepare lipophilic bisphosphonate precursors with potential activities.


Asunto(s)
Difosfonatos/síntesis química , Ésteres/síntesis química , Pirazoles/química , Temperatura , Difosfonatos/química , Ésteres/química , Estructura Molecular
14.
Bioorg Med Chem Lett ; 22(1): 339-42, 2012 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-22130133

RESUMEN

PI3K is a promising therapeutic target for cancer. With PI-103 as the lead compound, we designed and synthesized 4-(2-arylpyrido[3',2':3,4]pyrrolo[1,2-f][1,2,4]triazin-4-yl)morpholine derivatives. 9, 10a, 10d, 10e had the IC(50) against PI3Kα comparable with PI-103. All of the compounds showed selectivity over 15 tested protein kinases and anti-proliferative activity at micromolar concentration against several cancer cell lines.


Asunto(s)
Antineoplásicos/farmacología , Inhibidores Enzimáticos/farmacología , Furanos/farmacología , Morfolinas/farmacología , Inhibidores de las Quinasa Fosfoinosítidos-3 , Piridinas/farmacología , Pirimidinas/farmacología , Ciclo Celular , Línea Celular Tumoral , Proliferación Celular , Diseño de Fármacos , Ensayos de Selección de Medicamentos Antitumorales , Furanos/química , Humanos , Concentración 50 Inhibidora , Morfolinas/química , Fosfatidilinositol 3-Quinasas/química , Piridinas/química , Pirimidinas/química
15.
Eur J Med Chem ; 46(12): 5878-84, 2011 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-22000922

RESUMEN

A series of novel 11H-benzo[a]carbazole-5-carboxamide derivatives were designed, synthesized and evaluated for their antitumor activity against human cancer A549 and HCT-116 cell lines. Most of the compounds showed potent antitumor activities, and compound 8 displayed remarkable in vitro and in vivo anticancer activity comparable to that of amonafide.


Asunto(s)
Antineoplásicos/química , Antineoplásicos/uso terapéutico , Carbazoles/química , Carbazoles/uso terapéutico , Amidas/síntesis química , Amidas/química , Amidas/farmacología , Amidas/uso terapéutico , Animales , Antineoplásicos/síntesis química , Antineoplásicos/farmacología , Carbazoles/síntesis química , Carbazoles/farmacología , Puntos de Control del Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Ratones , Ratones Desnudos , Neoplasias/tratamiento farmacológico , Relación Estructura-Actividad
16.
Eur J Pharmacol ; 654(1): 17-25, 2011 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-21184754

RESUMEN

PTD4-apoptin protein enters cells and harbors tumor-selective cell death activity. Dacarbazine is the mainstay of treatment for malignant melanoma. In this study, we investigated the cytotoxic effect of PTD4-apoptin protein and/or dacarbazine in mouse B16-F1 and human A875 and SK-MEL-5 melanoma cells in vitro and by means of a mouse B16-F1 melanoma model in vivo. PTD4-apoptin protein inhibits the growth of B16-F1, A875 and SK-MEL-5 melanoma cells in a dose-dependent manner, but not in normal human cell lines WI-38 and L-02. PTD4-apoptin combined with dacarbazine revealed a synergistic cytotoxic effect (coefficient of drug interaction<1) in all three different tumor cell lines. In vivo, PTD4-apoptin protein and dacarbazine alone effectively inhibited the growth of B16-F1 melanoma in C57BL/6 mice. Strikingly, combined PTD4-apoptin/dacarbazine treatment significantly increased the antitumor effect in comparison to the single treatments. As important, a combined PTD4-apoptin/dacarbazine treatment with a 50% reduction of dacarbazine revealed similar antitumor activities, without detectable hematologic side effects. A combined PTD4-apoptin/dacarbazine treatment represents a promising novel efficient and safe anticancer strategy.


Asunto(s)
Proteínas de la Cápside/farmacología , Dacarbazina/farmacología , Melanoma/tratamiento farmacológico , Proteínas Recombinantes de Fusión/química , Animales , Antineoplásicos Alquilantes/farmacología , Proteínas de la Cápside/administración & dosificación , Proteínas de la Cápside/química , Línea Celular , Línea Celular Tumoral , Sinergismo Farmacológico , Femenino , Humanos , Melanoma/patología , Melanoma Experimental/tratamiento farmacológico , Melanoma Experimental/patología , Ratones , Ratones Endogámicos C57BL
17.
J Comb Chem ; 11(5): 806-8, 2009.
Artículo en Inglés | MEDLINE | ID: mdl-19645499

RESUMEN

C-5 arylated 2/9-substituted pyrimido[5,4-b]indolizines were synthesized via palladium-catalyzed direct arylation. A variety of substituents on both pyrimido[5,4-b]indolizines and aryl/heteroaryl bromides are tolerated, providing rapid access to substituted pyrimido[5,4-b]indolizines in good to excellent yields.


Asunto(s)
Bromuros/química , Indolizinas/química , Paladio/química , Catálisis , Espectroscopía de Resonancia Magnética , Espectrometría de Masas
18.
Health Phys ; 96(4): 483-92, 2009 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-19276709

RESUMEN

We examined the acute toxicity of depleted uranium (DU) after subcutaneous injection as a simulated wound model (experiment I), and the effects of a chelating agent, catechol-3,6-bis(methyleiminodiacetic acid) (CBMIDA), on the removal and damages caused by uranium by local treatment for wounds in rats (experiment II). Experiment I: To examine the initial behavior and toxicity of uranium of different chemical forms, male Wistar rats were subcutaneously injected with 4 and 16 mg kg-1 DU in a solution of pH 1 and 7. The rats were killed 1, 3, 6, and 24 h after DU injection. The DU (pH 1) injection site on the skin was altered markedly by acid burn, and the chemical action of uranium compared with that of DU (pH 7). After the injection of 4 mg kg-1 DU (pH 1), about 60% of the uranium was retained 1-3 h at the injected sites and then decreased to 16% at 24 h. However, the concentration of uranium in the injected site after 16 mg kg-1 DU (pH 1) injection did not change significantly. Urinary excretion rates of uranium (pH 1) increased in a time-independent manner after the injection. Depositions of uranium in the liver, kidneys and femur were found at 1 h after DU injection, and the results of serum and urinary examinations indicated that severe damage in the organs, including the kidney, was induced. The results of the DU (pH 7) were useful for estimating the chemical toxicity of uranium. Experiment II: The effects of CBMIDA by local treatment for wounds with DU were examined. CBMIDA (480 mg kg-1) was infused into the DU-injected site 0, 10, 30, 60, 120 min, and 24 h after the subcutaneous injection of 4 mg kg-1 DU (pH 1 and 7). The uranium at the injected sites decreased to 4-17% of that at 24 h in the DU (pH 1) group without CBMIDA treatment in experiment I, when it was administered within 120 min after DU injection. In addition, CBMIDA had excellent efficacy in excreting the uranium in urine and feces and decreasing the concentrations of uranium in the kidneys and femur. However, there were no distinct effects of CBMIDA for DU (pH 7). In conclusion, the results indicated that the subcutaneous injected uranium acutely induced severe damage in the DU-injected sites and organs by chemical toxicity within a very short time after DU intake, despite the chemical forms of uranium used, and the local treatment of CBMIDA for wounds contaminated with DU was effective in decreasing the acute toxicity of uranium if carried out within 120 min after DU administration.


Asunto(s)
Catecoles/farmacología , Quelantes/farmacología , Uranio/toxicidad , Heridas y Lesiones/patología , Animales , Concentración de Iones de Hidrógeno , Inyecciones Subcutáneas , Riñón/patología , Riñón/efectos de la radiación , Hígado/efectos de la radiación , Masculino , Ratas , Ratas Wistar , Uranio/farmacocinética
19.
Hemoglobin ; 32(1-2): 191-8, 2008.
Artículo en Inglés | MEDLINE | ID: mdl-18274996

RESUMEN

The effects of bicarbonate and its combination with the chelating agents, deferiprone (L1), 4,6-dimethyl-1-hydroxypyrimidin-2(1H)-one (AK-4), catechol-3,6-bis(methyleneimino-diacetic-acid) (CBMIDA), and ethane-1-hydroxy-1,1-bisphoshonate (EHBP) in removing depleted uranium (DU) for radiation emergency medicine were examined. After the intramuscular injection of DU in rats, various time schedules of bicarbonate and chelating agent administration were tested. The results indicate that the bicarbonate helps increase significantly the effects of LI and AK-4, while there were no effects of using bicarbonate alone. The effects of bicarbonate on CBMIDA were unclear, and the effects of EHBP were negative. Further studies are necessary to obtain distinctly synergic effects by the combination of chelating agents with bicarbonate.


Asunto(s)
Bicarbonatos/uso terapéutico , Quelantes/uso terapéutico , Traumatismos por Radiación/tratamiento farmacológico , Uranio/metabolismo , Alanina Transaminasa/sangre , Alanina Transaminasa/orina , Fosfatasa Alcalina/sangre , Fosfatasa Alcalina/orina , Animales , Aspartato Aminotransferasas/sangre , Aspartato Aminotransferasas/orina , Bicarbonatos/metabolismo , Quelantes/metabolismo , Terapia por Quelación , Creatinina/sangre , Creatinina/orina , Masculino , Nitrógeno/sangre , Nitrógeno/orina , Protectores contra Radiación/metabolismo , Protectores contra Radiación/uso terapéutico , Ratas , Ratas Wistar
20.
Bioorg Med Chem ; 15(17): 5828-36, 2007 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-17574424

RESUMEN

3-Aryl-tetrahydroquinolines, aza analogues of equol, are synthesized and evaluated for their binding properties to the estrogen receptors ERalpha and ERbeta. Several of these compounds exhibited binding selectivity for ER similar to that of genistein. Compounds 8c and 8d were found to have dual actions: antagonists for ERalpha and agonists for ERbeta in a yeast two-hybrid assay. These compounds have no estrogenic effects on the uterus and bone in vivo.


Asunto(s)
Compuestos Aza/síntesis química , Compuestos Aza/farmacología , Receptor beta de Estrógeno/metabolismo , Isoflavonas/química , Isoflavonas/farmacología , Animales , Compuestos Aza/química , Densidad Ósea , Equol , Receptor alfa de Estrógeno/metabolismo , Femenino , Humanos , Isoflavonas/síntesis química , Ligandos , Estructura Molecular , Ratas , Relación Estructura-Actividad , Útero/efectos de los fármacos
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