RESUMEN

Breast cancer and osteosarcoma are common cancers in women and children, respectively, but ideal drugs for treating patients with breast cancer or osteosarcoma remain to be found. Micafungin is an antifungal drug with antitumor activity on leukemia. Based on the notion of drug repurposing, this study aims to evaluate the antitumor effects of micafungin on breast cancer and osteosarcoma in vitro and in vivo, and to elucidate the underlying mechanisms. Five breast cancer cell lines (MDA-MB-231, BT-549, SK-BR-3, MCF-7, and 4T1) and one osteosarcoma cell line (143B) were chosen for the in vitro studies. Micafungin exerted an inhibitory effect on the viability of all cell lines, and MCF-7 cells were most sensitive to micafungin among the breast cancer cell lines. In addition, micafungin showed an inhibitory effect on the proliferation, clone formation, and migration in MCF7 and 143B cells. The inhibitory effect of micafungin on the growth of breast cancer and osteosarcoma was further confirmed with xenograft tumor mouse models. To explore the underlying mechanisms, the effect of micafungin on epithelial-mesenchymal transition (EMT) was examined. As expected, the levels of matrix metalloproteinase 9 and vimentin in MCF-7 and 143B cells were notably reduced in the presence of micafungin, concomitant with the decreased levels of ubiquitin-specific protease 7 (USP7), p-AKT, and p-GSK-3ß. Based on these observations, we conclude that micafungin exerts antitumor effect on breast cancer and osteosarcoma through preventing EMT in an USP7/AKT/GSK-3ß pathway-dependent manner.

Asunto(s)

Antineoplásicos , Neoplasias Óseas , Neoplasias de la Mama , Transición Epitelial-Mesenquimal , Glucógeno Sintasa Quinasa 3 beta , Micafungina , Osteosarcoma , Proteínas Proto-Oncogénicas c-akt , Transducción de Señal , Osteosarcoma/tratamiento farmacológico , Osteosarcoma/patología , Osteosarcoma/metabolismo , Humanos , Animales , Glucógeno Sintasa Quinasa 3 beta/metabolismo , Micafungina/farmacología , Micafungina/uso terapéutico , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/patología , Neoplasias de la Mama/metabolismo , Femenino , Transición Epitelial-Mesenquimal/efectos de los fármacos , Proteínas Proto-Oncogénicas c-akt/metabolismo , Antineoplásicos/farmacología , Línea Celular Tumoral , Transducción de Señal/efectos de los fármacos , Neoplasias Óseas/tratamiento farmacológico , Neoplasias Óseas/patología , Neoplasias Óseas/metabolismo , Ratones Endogámicos BALB C , Ubiquitina Tiolesterasa/metabolismo , Ratones Desnudos , Proliferación Celular/efectos de los fármacos , Movimiento Celular/efectos de los fármacos , Ensayos Antitumor por Modelo de Xenoinjerto , Ratones , Células MCF-7

RESUMEN

Clothing analysis has garnered significant attention, and within this field, clothing classification plays a vital role as one of the fundamental technologies. Due to the inherent complexity of clothing scenes in real-world environments, the learning of clothing features in such complex scenes often encounters interference. Because clothing classification relies on the contour and texture information of clothing, clothing classification in real scenes may lead to poor classification results. Therefore, this paper proposes a clothing classification network based on frequency-spatial domain conversion. The proposed network combines frequency domain information with spatial information and does not compress channels. It aims to enhance the extraction of clothing features and improve the accuracy of clothing classification. In our work, (1) we combine the frequency domain information and spatial information to establish a clothing feature extraction clothing classification network without compressed feature map channels, (2) we use the frequency domain feature enhancement module to realize the preliminary extraction of clothing features, and (3) we introduce a clothing dataset in complex scenes (Clothing-8). Our network achieves a top-1 model accuracy of 93.4% on the Clothing-8 dataset and 94.62% on the Fashion-MNIST dataset. Additionally, it also achieves the best results in terms of top-3 and top-5 metrics on the DeepFashion dataset.

RESUMEN

Atomic-scale catalysts leverage the advantages of both heterogeneous catalysts for their stability and reusability and homogeneous catalysts for their isolated active sites. Here, a palladium catalyst supported by Si-thiol, a commercially available mercaptopropyl-modified and TMS-passivated amorphous silica, was synthesized and characterized by SEM,TEM, aberration-corrected STEM-HAADF, XRD, FT-IR and XPS. Statistical analysis revealed that the catalytic Pd species predominantly consisted of intermediate sized nanoparticles (<2 nm), small amounts of essentially isolated atoms (ca. 0.1 nm), and limited amounts of somewhat larger nanoparticles (<5 nm). The nanoscale atomic clusters dominated the reactivity and served as the key active sites for Suzuki coupling. The outcomes of the reaction were greatly affected by the choice of solvents, and Pd/Si-thiol was demonstrated to be reusable for more than three times without a noticeable loss of catalytic activity. [Formula: see text].

RESUMEN

Polychlorinated biphenyl (PCB) and organochlorine pesticide (OCP) were analyzed in surficial sediments from the Haihe River and Haihe Estuary Area, Tianjin, China. The concentrations of [summation operator]PCBs (the sum of 32 PCB concentrations) and [summation operator]OCPs (the sum of eight OCPs concentrations) in the sediments from this area ranged from n.d. (not detected) to 253 ng g(-1) (average value: 66.8 ng g(-1)) and from 0.997 to 2447 ng g(-1) (average value: 738 ng g(-1)), respectively. Among the OCPs, the range of concentrations of hexachlorocyclohexane and its isomers (HCHs), dichlorodiphenyltrichloroethane and its metabolites (DDTs) and hexachlorobenzene (HCB) were 0.997-1620 ng g(-1) (547 ng g(-1)), n.d. - 155 ng g(-1) (18.5 ng g(-1)) and n.d. - 835 ng g(-1) (173 ng g(-1)), respectively. In general, the concentrations of all persistent organic pollutants (POPs) from the Haihe River were higher than those from the Haihe Estuary Area. Compositional analyses of the POPs indicated that tri-PCBs were dominant in sediment from the Haihe River, while tetra-PCBs and penta-PCBs were identified as being prevalent in the Haihe Estuary Area. In addition, beta-HCH and p,p'-DDD were found to be the dominant HCHs and DDTs, respectively. Compared with other areas around the world, the concentrations of POPs in sediments from the Haihe River were higher, but pollution level was comparable with other areas in the Haihe Estuary Area. According to established sediment quality guidelines (SQGs), POPs in this area have potential ecological risk.

Asunto(s)

Sedimentos Geológicos/química , Hidrocarburos Clorados/análisis , Plaguicidas/análisis , Bifenilos Policlorados/análisis , Ríos/química , China , Ambiente , Monitoreo del Ambiente , Medición de Riesgo

RESUMEN

The synthesis of four (+/-)-fluorinated 1-(3-morpholin-4-yl-phenyl)-ethylamines and an enantioselective approach to these amines through reductive amination are described.

Asunto(s)

Antibacterianos/síntesis química , Fenetilaminas/síntesis química , Flúor/química , Estructura Molecular , Morfolinas/química , Estereoisomerismo

RESUMEN

A facile detrifluoromethylation was observed when 4,4-bis(trifluoromethyl)-5-hydroxyimidazoline 5 was treated with a variety of bases to afford the biologically interesting 4-(trifluoromethyl)imidazole analogs (9 and 10). A unique mechanism was proposed for this transformation, supported by isolating and trapping the hypothesized intermediates. Heating of 5 with Et(4)NCN in DMSO provided 19, which was clearly derived from the proposed intermediate 17. Finally, imidazole 9 was converted into the N-[2-phenyl-4-(trifluoromethyl)-1H-imidazol-5-yl]-N-methylbenzamide analogs, which were potential acyl CoA:cholesterol acyltransferase (ACAT) inhibitors.