RESUMEN

Drought is a major environmental stress limiting crop yields worldwide. Upland rice (Oryza sativa) has evolved complex genetic mechanisms to adjust to drought stress. However, few genetic variants have been identified that mediate drought resistance in upland rice, and little is known about the evolution of this trait during domestication. Here, using a genome-wide association study in rice, we identified ROOT LENGTH 1 (RoLe1) controlling root length and drought resistance. We demonstrate that a G-to-T polymorphism in the RoLe1 promoter increases binding of the transcription factor OsNAC41 to activate its transcription. We also show that RoLe1 interacts with and interferes with the function of OsAGAP, an ARF-GTPase activating protein involved in auxin-dependent root development, to modulate root development. Furthermore, RoLe1 enhanced crop yield by increasing the seed setting rate under moderate drought conditions. Genomic evolution analysis showed that a newly arisen favorable allelic variant, proRoLe1-526T, originated from Region I (Midwest Asia) and was retained in upland rice during domestication. Our findings propose a OsNAC41-RoLe1-OsAGAP module, providing promising genetic targets for molecular breeding of drought-resistant varieties in rice.

RESUMEN

In this study, twenty-two novel cholic acid (CA) derivatives were designed and synthesized as potential Takeda G protein-coupled receptor 5 (TGR5) positive allosteric modulators (PAMs) using structure-based drug design (SBDD). GloSensor cAMP accumulation assay was employed to assess the functional activity and allosteric mechanism of final compounds. Biological results showed that all target compounds were able to activate the TGR5 in the cAMP formation assay. Remarkably, compound B1, selective methylation of 7-OH in CA, exhibited 5-fold higher activity for TGR5 compared to that of CA. Moreover, B1 positively modulate the functional activity of chenodeoxycholic acid (CDCA) in TGR5, indicating that B1 is a TGR5 PAM. On the other hand, 12-carbonyl derivative A1 displayed 7-fold higher potency for TGR5 relative to CA. Unexpectedly, compound A1 exhibited the same positive allosteric effect as B1, suggesting that A1 is a TGR5 PAM as well. Molecular modeling study revealed that 12-carbonyl in A1 and 12-OH in B1 formed H-bolds with the key amino acid Thr131, which are significant for TGR5 allosteric property. Taken together, we found two potent TGR5 PAMs A1 and B1 through SBDD, which could be used as lead compounds to further study TGR5 allosteric functionality.

Asunto(s)

Diseño de Fármacos , Receptores Acoplados a Proteínas G , Ácido Cólico/farmacología , Receptores Acoplados a Proteínas G/metabolismo , Modelos Moleculares , Regulación Alostérica

RESUMEN

Drought is a major factor restricting the production of rice (Oryza sativa L.). The identification of natural variants for drought stress-related genes is an important step toward developing genetically improved rice varieties. Here, we characterized a member of the SQUAMOSA PROMOTER BINDING PROTEIN-LIKE (SPL) family, OsSPL10, as a transcription factor involved in the regulation of drought tolerance in rice. OsSPL10 appears to play a vital role in drought tolerance by controlling reactive oxygen species (ROS) production and stomatal movements. Haplotype and allele frequency analyses of OsSPL10 indicated that most upland rice and improved lowland rice varieties harbor the OsSPL10Hap1 allele, whereas the OsSPL10Hap2 allele was mainly present in lowland and landrace rice varieties. Importantly, we demonstrated that the varieties with the OsSPL10Hap1 allele showed low expression levels of OsSPL10 and its downstream gene, OsNAC2, which decreases the expression of OsAP37 and increases the expression of OsCOX11, thus preventing ROS accumulation and programmed cell death (PCD). Furthermore, the knockdown or knockout of OsSPL10 induced fast stomatal closure and prevented water loss, thereby improving drought tolerance in rice. Based on these observations, we propose that OsSPL10 confers drought tolerance by regulating OsNAC2 expression and that OsSPL10Hap1 could be a valuable haplotype for the genetic improvement of drought tolerance in rice.

Asunto(s)

Oryza , Oryza/metabolismo , Resistencia a la Sequía , Especies Reactivas de Oxígeno/metabolismo , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Factores de Transcripción/metabolismo , Sequías , Regulación de la Expresión Génica de las Plantas , Estrés Fisiológico/genética , Plantas Modificadas Genéticamente/metabolismo

RESUMEN

Probiotics exhibit many health benefits and a great potential for broad applications in pharmaceutical fields, such as prevention and treatment of gastrointestinal tract diseases (irritable bowel syndrome), prevention and therapy of allergies, certain anticancer effects, and immunomodulation. However, their applications are limited by the low viability and metabolic activity of the probiotics during processing, storage, and delivery in the digestive tract. To overcome the mentioned limitations, probiotic delivery systems have attracted much attention. This review focuses on alginate as a preferred polymer and presents recent advances in alginate-based polymers for probiotic delivery systems. We highlight several alginate-based delivery systems containing various types of probiotics and the physical and chemical modifications with chitosan, cellulose, starch, protein, fish gel, and many other materials to enhance their performance, of which the viability and protective mechanisms are discussed. Withal, various challenges in alginate-based polymers for probiotics delivery systems are traced out, and future directions, specifically on the use of nanomaterials as well as prebiotics, are delineated to further facilitate subsequent researchers in selecting more favorable materials and technology for probiotic delivery.

RESUMEN

Student well-being and its relationships with academic achievement in China have not been well-investigated. This study aimed at investigating student well-being and the trade-off of the well-being and academic achievement with a sample of 1,353 Chinese high-school students from four cities in China during coronavirus disease 2019 (COVID-19) pandemic period. The six dimensions of well-being (academic, psychological, self, physical, social, and spiritual) were utilised to test the relationships with three subjects including Mathematics, English, and Chinese using a quantitative analysis. In this study, the relationships between six dimensions of well-being and three academic subject achievements were tested in one statistical model. Results showed that spiritual well-being was ranked the highest, followed by psychological, physical, self, and social well-being. Students gave the lowest ranking to academic well-being. The two significant paths identified were between spiritual well-being and two subjects, namely, Chinese and Mathematics. It is interesting to note that the other five dimensions of well-being were significantly associated with any subjects and English was not significantly related to any dimensions of well-being in this study. Our findings suggested that policymakers and other stakeholders should avoid an "all or nothing" mindset on practice when considering well-being as a multidimensional construct.

RESUMEN

The antioxidant effect of probiotics has been widely recognized across the world, which is of great significance in food, medicine, and aquaculture. There are abundant marine microbial resources in the ocean, which provide a new space for humans to explore new probiotics. Previously, we reported on the anti-infective effects of Planococcus maritimu ML1206, a potential marine probiotic. The antioxidant activity of ML1206 in C. elegans was studied in this paper. The study showed that ML1206 could improve the ability of nematodes to resist oxidative stress and effectively prolong their lifespan. The results confirmed that ML1206 could significantly increase the activities of CAT and GSH-PX, and reduce the accumulation of reactive oxygen species (ROS) in nematodes under oxidative stress conditions. In addition, ML1206 promoted DAF-16 transfer to the nucleus and upregulated the expression of sod-3, hsp-16.2, and ctl-2, which are downstream antioxidant-related genes of DAF-16. Furthermore, the expression of the SOD-3::GFP and HSP-16.2::GFP was significantly higher in the transgenic strains fed with ML1206 than that in the control group fed with OP50, with or without stress. In summary, these findings suggest that ML1206 is a novel marine probiotic with an antioxidant function that stimulates nematodes to improve their defense abilities against oxidative stress and prolong the lifespan by regulating the translocation of FOXO/DAF-16. Therefore, ML1206 may be explored as a potential dietary supplement in aquaculture and for anti-aging and antioxidant purposes.

Asunto(s)

Proteínas de Caenorhabditis elegans , Caenorhabditis elegans , Animales , Humanos , Caenorhabditis elegans/metabolismo , Longevidad , Antioxidantes/farmacología , Antioxidantes/metabolismo , Proteínas de Caenorhabditis elegans/genética , Proteínas de Caenorhabditis elegans/metabolismo , Estrés Oxidativo , Especies Reactivas de Oxígeno/metabolismo , Superóxido Dismutasa/metabolismo , Factores de Transcripción Forkhead/genética , Factores de Transcripción Forkhead/metabolismo

RESUMEN

A novel gram-negative, aerobic, pink, motile, gliding, rod-shaped bacterium, designated P51T, was isolated from saline silt samples in Yantai, China. It was able to grow at 4-42 °C (optimum 33 °C), pH 4.0-9.0 (optimum 7.0), and in 0-11.0% NaCl (optimum 4.0%, w/v). It grew at 4 °C, which was lower than the minimum temperature for related strains. The genome consisted of 4111 genes with a total length of 5 139 782 bp. The 16S rRNA gene sequence analysis indicated that strain P51T was a member of the genus Echinicola and most closely related to 'Echinicola shivajiensis'. A genome analysis identified genes encoding proteins associated with carbon source utilisation, and the carotenoid biosynthesis and ß-lactam resistance pathways. Strain P51T shared an average nucleotide identity value below 84.7%, an average amino acid identity value between 70.8 and 89.3%, and a digital DNA-DNA hybridisation identity of between 17.9-28.2% with closely related type strains within the genus Echinicola. The sole menaquinone was MK-7, and the major fatty acids were iso-C15:0, summed feature 3 (C16:1ω7c and/or C16:1ω6c), summed feature 4 (anteiso-C17:1 B and/or iso-C17:1 I), and summed feature 9 (iso-C17:1ω9c and/or 10-methyl C16:0). The polar lipids included one phosphatidylethanolamine, one unidentified aminophospholipid, one unidentified phospholipid, three unidentified aminolipids, and one unknown lipid. The phenotypic, chemotaxonomic, and phylogenetic analyses suggest that strain P51T is a novel species of the genus Echinicola, for which the name Echinicola salinicaeni sp. nov. is proposed. The type strain was P51T (KCTC 82513T = MCCC 1K04413T).

Asunto(s)

Ácidos Grasos , Fosfolípidos , Técnicas de Tipificación Bacteriana , Bacteroidetes , Composición de Base , ADN Bacteriano/genética , Filogenia , ARN Ribosómico 16S/genética , Análisis de Secuencia de ADN , Vitamina K 2

RESUMEN

Trichomes function in plant defenses against biotic and abiotic stresses; examination of glabrous lines, which lack trichomes, has revealed key aspects of trichome development and function. Tests of allelism in 51 glabrous rice (Oryza sativa) accessions collected worldwide identified OsSPL10 and OsWOX3B as regulators of trichome development in rice. Here, we report that OsSPL10 acts as a transcriptional regulator controlling trichome development. Haplotype and transient expression analyses revealed that variation in the approximately 700-bp OsSPL10 promoter region is the primary cause of the glabrous phenotype in the indica cultivar WD-17993. Disruption of OsSPL10 by genome editing decreased leaf trichome density and length in the NIL-HL6 background. Plants with genotype OsSPL10WD-17993 /HL6 generated by crossing WD-17993 with NIL-HL6 also had fewer trichomes in the glumes. HAIRY LEAF6 (HL6) encodes another transcription factor that regulates trichome initiation and elongation, and OsSPL10 directly binds to the HL6 promoter to regulate its expression. Moreover, the transcript levels of auxin-related genes, such as OsYUCCA5 and OsPIN-FORMED1b, were altered in OsSPL10 overexpression and RNAi transgenic lines. Feeding tests using locusts (Locusta migratoria) demonstrated that non-glandular trichomes affect feeding by this herbivore. Our findings provide a molecular framework for trichome development and an ecological perspective on trichome functions.

Asunto(s)

Regulación de la Expresión Génica de las Plantas , Ácidos Indolacéticos/metabolismo , Oryza/genética , Proteínas de Plantas/genética , Tricomas/crecimiento & desarrollo , Animales , Secuencia de Bases , Sitios Genéticos , Genotipo , Saltamontes/fisiología , Oryza/parasitología , Oryza/ultraestructura , Fenotipo , Proteínas de Plantas/metabolismo , Regiones Promotoras Genéticas/genética , Transducción de Señal , Transactivadores/metabolismo , Tricomas/ultraestructura

RESUMEN

With the widespread occurrence of aquaculture diseases and the broad application of antibiotics, drug-resistant pathogens have increasingly affected aquatic animals' health. Marine probiotics, which live under high pressure in a saltwater environment, show high potential as a substitute for antibiotics in the field of aquatic disease control. In this study, twenty strains of non-hemolytic bacteria were isolated from the intestine of wild oysters and perch, and a model of Caenorhabditis elegans infected by Vibrio anguillarum was established. Based on the model, ML1206, which showed a 99% similarity of 16S rRNA sequence to Planococcus maritimus, was selected as a potential marine probiotic, with strong antibacterial capabilities and great acid and bile salt tolerance, to protect Caenorhabditis elegans from being damaged by Vibrio anguillarum. Combined with plate counting and transmission electron microscopy, it was found that strain ML1206 could significantly inhibit Vibrio anguillarum colonization in the intestinal tract of Caenorhabditis elegans. Acute oral toxicity tests in mice showed that ML1206 was safe and non-toxic. The real-time qPCR results showed a higher expression level of genes related to the antibacterial peptide (ilys-3) and detoxification (ugt-22, cyp-35A3, and cyp-14A3) in the group of Caenorhabditis elegans protected by ML1206 compared to the control group. It is speculated that ML1206, as a potential probiotic, may inhibit the infection caused by Vibrio anguillarum through stimulating Caenorhabditis elegans to secrete antibacterial effectors and detoxification proteins. This paper provides a new direction for screening marine probiotics and an experimental basis to support the potential application of ML1206 as a marine probiotic in aquaculture.

Asunto(s)

Caenorhabditis elegans/microbiología , Planococcaceae , Probióticos/administración & dosificación , Vibriosis/prevención & control , Animales , Acuicultura , Femenino , Intestinos/microbiología , Masculino , Ratones , Ratones Endogámicos ICR , Ostreidae/microbiología , Planococcaceae/genética , Planococcaceae/aislamiento & purificación , Probióticos/toxicidad , ARN Ribosómico 16S , Sobrevida , Vibrio/aislamiento & purificación

RESUMEN

Inhibition of the soluble epoxide hydrolase (sEH) is a promising new therapeutic approach in the treatment of inflammation. Driven by the in-house database product lead 1, a hybridization strategy was utilized for the design of a series of novel benzo [d]thiazol derivatives. To our delight, D016, a byproduct of compound 9, was obtained with an extraordinarily low IC50 value of 0.1 nM but poor physical and chemical properties. After removal of a non-essential urea moiety or replacement of the urea group by an amide group, compounds 15a, 17p, and 18d were identified as promising sEH inhibitors, and their molecular binding modes to sEH were constructed. Furthermore, compounds 15a and 18d exhibited more effective in vivo anti-inflammatory effect than t-AUCB in carrageenan-induced mouse paw edema. Compound 15a also showed moderate metabolic stability with a half-time of 34.7 min. Although 18d was unstable in rat liver microsomes, it might be a "prodrug". In conclusion, this study could provide valuable insights into discovery of new sEH inhibitors, and compounds 15a and 18d were worthy of further development as potential drug candidates to treat inflammation.

Asunto(s)

Antiinflamatorios no Esteroideos/farmacología , Benzotiazoles/farmacología , Edema/tratamiento farmacológico , Inhibidores Enzimáticos/farmacología , Epóxido Hidrolasas/antagonistas & inhibidores , Inflamación/tratamiento farmacológico , Animales , Antiinflamatorios no Esteroideos/síntesis química , Antiinflamatorios no Esteroideos/química , Benzotiazoles/síntesis química , Benzotiazoles/química , Carragenina , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Edema/inducido químicamente , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/química , Epóxido Hidrolasas/metabolismo , Células Hep G2 , Humanos , Inflamación/inducido químicamente , Ligandos , Masculino , Ratones , Ratones Endogámicos BALB C , Microsomas Hepáticos/química , Microsomas Hepáticos/metabolismo , Simulación del Acoplamiento Molecular , Estructura Molecular , Ratas , Ratas Sprague-Dawley , Relación Estructura-Actividad

RESUMEN

Herein, with the help of computer-aided drug design (CADD), we describe the structure-based rational drug design, structure-activity relationships, and synthesis of a series of 2-aminopyrimidine derivatives that inhibit both JAK2 and FLT3 kinases. These screening cascades revealed that compound 14l demonstrated the most inhibitory activity with IC50 values of 1.8 and 0.68 nM against JAK2 and FLT3 respectively. 14l also showed potent anti-proliferative activities against HEL (IC50 = 0.84 µM) and Molm-13 (IC50 = 0.019 µM) cell lines, but relatively weak cytotoxicity against K562 and PC-3 cell lines, which proved that it might have high target specificity. In vitro metabolism assay, 14l exhibited moderate stability in RLM (Rat Liver Microsomes) with a half-life time of 31 min. In the cellular context of Molm-13, 14l induced cell cycle arrest in G1/S phase and enhanced apoptosis in a dose-dependent manner. These results indicate that 14l is a promising dual JAK2/FLT3 inhibitor and worthy of further development.

Asunto(s)

Antineoplásicos/farmacología , Descubrimiento de Drogas , Janus Quinasa 2/antagonistas & inhibidores , Inhibidores de Proteínas Quinasas/farmacología , Pirimidinas/farmacología , Tirosina Quinasa 3 Similar a fms/antagonistas & inhibidores , Antineoplásicos/síntesis química , Antineoplásicos/química , Apoptosis/efectos de los fármacos , Puntos de Control del Ciclo Celular/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Janus Quinasa 2/metabolismo , Simulación del Acoplamiento Molecular , Estructura Molecular , Inhibidores de Proteínas Quinasas/síntesis química , Inhibidores de Proteínas Quinasas/química , Pirimidinas/síntesis química , Pirimidinas/química , Relación Estructura-Actividad , Tirosina Quinasa 3 Similar a fms/metabolismo

RESUMEN

We previously discovered a series of novel biaryloxazolidinone analogues bearing a hydrazone moiety with potent antibacterial activity. However, the most potent compound OB-104 exhibited undesirable chemical and metabolic instability. Herein, novel biaryloxazolidinone analogues were designed and synthesized to improve the chemical and metabolic stability. Compounds 6a-1, 6a-3, 14a-1, 14a-3 and 14a-7 showed significant antibacterial activity against the tested Gram-positive bacteria as compared to radezolid and linezolid. Further studies indicated that most of them exhibited improved water solubility and chemical stability. Compound 14a-7 had MIC values of 0.125-0.25 µg/mL against all tested Gram-positive bacteria, and showed excellent antibacterial activity against clinical isolates of antibiotic-susceptible and antibiotic-resistant bacteria. Moreover, it was stable in human liver microsome. From a safety viewpoint, it showed non-cytotoxic activity against hepatic cell and exhibited lower inhibitory activity against human MAO-A compared to linezolid. The potent antibacterial activity and all these improved drug-likeness properties and safety profile suggested that compound 14a-7 might be a promising drug candidate for further investigation.

Asunto(s)

Antibacterianos/farmacología , Farmacorresistencia Bacteriana/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Inhibidores de la Monoaminooxidasa/farmacología , Oxindoles/farmacología , Antibacterianos/síntesis química , Antibacterianos/química , Supervivencia Celular/efectos de los fármacos , Relación Dosis-Respuesta a Droga , Células Hep G2 , Humanos , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Monoaminooxidasa/metabolismo , Inhibidores de la Monoaminooxidasa/síntesis química , Inhibidores de la Monoaminooxidasa/química , Oxindoles/síntesis química , Oxindoles/química , Relación Estructura-Actividad

RESUMEN

A series of novel 4-phenoxyquinoline derivatives containing 3-oxo-3,4-dihydro-quinoxaline moiety were synthesized and evaluated for their antiproliferative activity against five human cancer cell lines (A549, H460, HT-29, MKN-45 and U87MG) in vitro. Most of the tested compounds exhibited more potent inhibitory activities than the positive control foretinib. Compound 1b, 1s and 1t were further examined for their inhibitory activity against c-Met kinase. The most promising compound 1s (with c-Met IC50 value of 1.42 nM) showed remarkable cytotoxicity against A549, H460, HT-29, MKN45 and U87MG cell lines with IC50 values of 0.39 µM, 0.18 µM, 0.38 µM, 0.81 µM, respectively. Their preliminary structure-activity relationships (SARs) study indicated that the replacement of the aromatic ring with the cyclohexane improved their antiproliferative activity.

Asunto(s)

Proteínas Proto-Oncogénicas c-met/antagonistas & inhibidores , Quinolinas/síntesis química , Humanos , Estructura Molecular , Quinolinas/química , Relación Estructura-Actividad

RESUMEN

Hybridization strategy is an effective strategy to obtain multi-target inhibitors in drug design. In this study, we assembled the pharmacophores of momelotinib and tandutinib to get a series of 4-piperazinyl-2-aminopyrimidine derivatives. All compounds were tested for the inhibition of JAK2 and FLT3 enzymes, of which, compounds with potent enzyme activities were assayed for antiproliferative activities against three cancer cell lines (HEL, MV4-11, and HL60). The structure-activity relationship studies were conducted through variations in two regions, the "A" phenyl ring and "B" phenyl ring. Compound 14j showed the most balanced in vitro inhibitory activity against JAK2 and FLT3 (JAK2 IC50 = 27 nM, FLT3 IC50 = 30 nM), and it also showed potent inhibition against the above tested cell lines. In the cellular context, 14j strongly induced apoptosis by arresting cell cycle in the G1/S phase, and was selected as a promising JAK2/FLT3 dual inhibitor.

Asunto(s)

Janus Quinasa 2/antagonistas & inhibidores , Inhibidores de Proteínas Quinasas/química , Inhibidores de Proteínas Quinasas/farmacología , Pirimidinas/química , Pirimidinas/farmacología , Tirosina Quinasa 3 Similar a fms/antagonistas & inhibidores , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Diseño de Fármacos , Humanos , Janus Quinasa 2/metabolismo , Simulación del Acoplamiento Molecular , Neoplasias/tratamiento farmacológico , Piperazinas/química , Piperazinas/farmacología , Tirosina Quinasa 3 Similar a fms/metabolismo

RESUMEN

A Gram-stain-negative, non-flagellated, catalase-positive, oxidase-positive bacterial strain, designated YLY08T, was isolated from the gut microflora of sea bass (Dicentrarchus labrax L.) collected from the coast of Yuanyao Wharf, Weihai, PR China, and subjected to a polyphasic taxonomic study. Strain YLY08T grew optimally at 28-30 °C, at pH 7.0-7.5 and in the presence of 2.0-3.0 % (w/v) NaCl. Poly-ß-hydroxybutyrate granules were produced. Neighbour-joining, maximum-likelihood and maximum-parsimony phylogenetic trees based on 16S rRNA gene sequences revealed that strain YLY08T clustered with the type strain of Oceaniglobus indicus, with which it exhibited 95.3 % sequence similarity, while the similarity to other genera was below 95.0 %. Genomic analyses, including average nucleotide identity and the digital DNA-DNA hybridization, clearly separated YLY08T from O. indicus MCCC 1A11863T with values below the thresholds for species delineation. The major cellular fatty acid was summed feature 8 (C18 : 1ω7c and/or C18 : 1ω6c). The sole respiratory quinone detected was Q-10. The polar lipid profile consisted of phosphatidylethanolamine, phosphatidylglycerol, phosphatidylcholine, phosphatidyldimethylethanolamine, diphosphatidylglycerol, one unidentified aminolipid and one unidentified phospholipid. The genome of strain YLY08T, with 38 assembled contigs, was 3.9 Mb long with a G+C content of 59.0 mol%. The results of the phenotypical, phylogenetic and biochemical analyses between the strain YLY08T and the related type strain indicated that this strain represents a novel species in genus Oceaniglobus within the family Rhodobacteraceae, for which the name Oceaniglobus ichthyenteri sp. nov. is proposed. The type strain is YLY08T (=MCCC 1H00318T=KCTC 62182T).

Asunto(s)

Lubina/microbiología , Microbioma Gastrointestinal , Filogenia , Rhodobacteraceae/clasificación , Animales , Técnicas de Tipificación Bacteriana , Composición de Base , China , ADN Bacteriano/genética , Ácidos Grasos/química , Hidroxibutiratos , Hibridación de Ácido Nucleico , Fosfolípidos/química , Poliésteres , ARN Ribosómico 16S/genética , Rhodobacteraceae/aislamiento & purificación , Alimentos Marinos/microbiología , Agua de Mar/microbiología , Análisis de Secuencia de ADN

RESUMEN

A novel Gram-stain-negative, rod-shaped, ivory-white, facultatively anaerobic and catalase-positive bacterium, designated H1304T, was isolated from the gut of sea catfish from Coast of Weihai, China. Optimal growth occurred at 30-33 °C (range, 4-37 °C) and pH 7.0-7.5 (range, pH 6.5-9.0) with 2.0-3.0 % (w/v) NaCl (range, 0.5-4.0 %). Phylogenetic analysis based on 16S rRNA gene sequences showed that H1304T belonged to the genus Cohaesibacter and was most closely related to Cohaesibactermarisflavi CGMCC 1.9157T (96.7 % 16S rRNA gene sequence similarity), Cohaesibactergelatinilyticus MCCC 1A02698T (96.3 %) and Cohaesibacterhaloalkalitolerans KCTC 32038T (96.0 %). The sole isoprenoid quinone was Q-10, the polar lipid profile consisted of phosphatidylglycerol, diphosphatidylglycerol, phosphatidylethanolamine, phosphatidylmonomethylethanolamine, phosphatidylcholine, glycolipid, an unidentified phospholipid and an unidentified aminolipid. The major fatty acids (>10 %) were C18 : 1ω7c and summed feature 3 (C16 : 1ω7c/C16 : 1ω6c). The DNA G+C content of strain H1304T is 50.8 mol%. Based on the combination of phylogenetic analysis, phenotypic data and chemotaxonomic data, strain H1304T is considered to represent a novel species within the genus Cohaesibacter in the family Cohaesibacteraceae, for which the name Cohaesibacter celericrescens sp. nov. is proposed. The type strain of the new species is H1304T (=KCTC 62075T=MCCC 1H00241T).

Asunto(s)

Alphaproteobacteria/clasificación , Bagres/microbiología , Tracto Gastrointestinal/microbiología , Filogenia , Alphaproteobacteria/aislamiento & purificación , Animales , Técnicas de Tipificación Bacteriana , Composición de Base , China , ADN Bacteriano/genética , Ácidos Grasos/química , Glucolípidos/química , Fosfolípidos/química , ARN Ribosómico 16S/genética , Análisis de Secuencia de ADN , Ubiquinona/análogos & derivados , Ubiquinona/química

RESUMEN

BACKGROUND This study investigated the role and mechanism of alprostadil in acute respiratory distress syndrome (ARDS) induced by oleic acid (OA) in rats. MATERIAL AND METHODS Sprague-Dawley rats were randomly divided into control, OA model, and OA + Alprostadil (2.5, 5, and 10 µg/kg, respectively) groups. The ARDS model was induced by femoral vein injection of OA, and alprostadil was administrated immediately. Lung injury was evaluated by lung wet-dry weight ratio (W/D) and histological analyses. Expressions of ACE, inflammatory mediators, apoptotic-related proteins, and proteins in the MAPKs and NF-κB signaling pathways were determined by Western blot or immunohistochemical staining. RESULTS Compared with the control group, the OA model group had significantly increased W/D, lung injury score, and collagen deposition at 3 h after OA injection. However, alprostadil (10 µg/kg) treatment significantly reduced OA-induced elevation of these indicators. Additionally, OA-induced expression of TNF-α and IL-1ß were suppressed by alprostadil. The OA-induced activation of nuclear factor (NF) κB p65 was also reduced by alprostadil. Furthermore, we found that Alprostadil had an inhibitory effect on the phosphorylation of JNK, ERK1/2, and p38 MAPKs. Alprostadil inhibited Bax but increased Bcl-2, indicating a suppressive role in apoptosis. Remarkably increased expression of ACE in the OA model group was observed, which was decreased by alprostadil. CONCLUSIONS Alprostadil has a protective effect on ARDS induced by OA in rats, possibly through inhibiting apoptosis, suppressing the activation of MAPKs and NF-κB signaling pathways, and decreasing ACE protein expression. Therefore, the use of alprostadil in clinical ARDS treatment is promising.

Asunto(s)

Alprostadil/farmacología , Síndrome de Dificultad Respiratoria/tratamiento farmacológico , Animales , Apoptosis/efectos de los fármacos , Líquido del Lavado Bronquioalveolar/citología , Modelos Animales de Enfermedad , Pulmón/efectos de los fármacos , Pulmón/patología , Masculino , Proteínas Quinasas Activadas por Mitógenos/metabolismo , FN-kappa B/metabolismo , Ácido Oléico/toxicidad , Distribución Aleatoria , Ratas , Ratas Sprague-Dawley , Síndrome de Dificultad Respiratoria/inducido químicamente , Síndrome de Dificultad Respiratoria/metabolismo , Síndrome de Dificultad Respiratoria/patología , Transducción de Señal/efectos de los fármacos

RESUMEN

A metal-free brand-new one-pot multinitrogenation of amides for the chemo- and regioselective synthesis of 1,5-disubstituted tetrazoles has been developed. By means of electrophilic amide activation, and further C-C bond cleavage and rearrangement, a diverse set of functionalized 1,5-DST derivatives were selectively constructed under mild conditions. As showcased in the mechanisms, the chemoselectivity is easily switched by the selection of the starting materials in the reaction.

RESUMEN

A novel Gram-stain-negative, whitish-yellow, rod-shaped, non-pigmented, aerobic, oxidase-positive and catalase-positive bacterium, designated PX7T, was isolated from coastal sediment of Xiaoshi Island, Weihai, China (37° 31' 36″ N, 122° 00' 58″ E). Strain PX7T grew optimally at 30 °C, at pH 7.0-7.5 and in the presence of 3.0 % (w/v) NaCl. Phylogenetic analysis based on 16S rRNA gene sequences revealed that strain PX7T formed a robust clade with members of the genus Primorskyibacter and was closely related to Primorskyibacter sedentarius, Primorskyibacter aestuariivivens and Primorskyibacter insulae with 96.5, 96.2 and 95.1 % sequence similarities, respectively. The sole respiratory quinone of strain PX7T was ubiquinone-10, and the dominant fatty acid was C18 : 1ω7c (80.2 %). The major polar lipids were phosphatidylglycerol, phosphatidylcholine, phosphatidylethanolamine, one unidentified aminolipid, one unidentified phospholipid and one unidentified lipid. The DNA G+C content of strain PX7T was 60.2 mol%. Based on the combination of phylogenetic analyses, phenotypic and chemotaxonomic data, strain PX7T is considered to represent a novel species within the genus Primorskyibacter in the family Rhodobacteraceae, for which the name Primorskyibacter marinus sp. nov. is proposed. The type strain of the new species is PX7T (=KCTC 42952T=MCCC 1H00196T).

Asunto(s)

Sedimentos Geológicos/microbiología , Filogenia , Rhodobacteraceae/clasificación , Agua de Mar/microbiología , Técnicas de Tipificación Bacteriana , Composición de Base , China , ADN Bacteriano/genética , Ácidos Grasos/química , Fosfolípidos/química , ARN Ribosómico 16S/genética , Rhodobacteraceae/genética , Rhodobacteraceae/aislamiento & purificación , Análisis de Secuencia de ADN , Ubiquinona/química

RESUMEN

A strictly aerobic, Gram-stain negative, long rod-shaped, motile by gliding and yellow pigmented bacterium, designated strain w01T, was isolated from marine sediment. The strain was characterised to determine its taxonomic position by using a polyphasic approach. Strain w01T was observed to grow optimally in the presence of 3.0% (w/v) NaCl, at 30 °C and to hydrolyse Tweens 20, 40 and 80, starch, casein and alginate. Carotenoid pigments were found to be produced but not flexirubin-type pigments. On the basis of 16S rRNA gene sequence similarities, strain w01T is phylogenetically affiliated with the genus Aquimarina and is closely related to Aquimarina macrocephali JCM 15542T (97.4% sequence similarity) and Aquimarina muelleri KCTC 12285T (97.0%). Lower sequence similarities (< 97.0%) were found with the other currently recognised members of the genus Aquimarina. The predominant fatty acids were identified as iso-C15:0 (33.7%), C18:0 3-OH (16.8%) and C17:1ω7c (10.6%). The polar lipid profile was found to contain phosphatidylethanolamine, an unidentified aminolipid and two unidentified polar lipids. MK-6 was identified as the sole respiratory quinone. The G + C content of the genomic DNA was determined to be 33.3 mol%. Strain w01T can be differentiated genotypically and phenotypically from recognised species of the genus Aquimarina. The isolate is therefore concluded to represent a novel species, for which the name Aquimarina sediminis sp. nov. is proposed, with the type strain w01T (= KCTC 62350T = MCCC 1H00287T).

Asunto(s)

Flavobacteriaceae/aislamiento & purificación , Sedimentos Geológicos/microbiología , Composición de Base , ADN Bacteriano/genética , Ácidos Grasos/química , Ácidos Grasos/metabolismo , Flavobacteriaceae/clasificación , Flavobacteriaceae/genética , Flavobacteriaceae/metabolismo , Filogenia , ARN Ribosómico 16S/genética , Agua de Mar/microbiología