Activity

Furthermore, 9i could effectively inhibit the proliferation and metastasis of MCF-7 cells in vitro and in zebrafish xenograft. The satisfactory physicochemical property and metabolic stability of 9i further indicated that it can act as a promising and potent anti-angiogenesis, inhibiting proliferation and metastasis of breast cancer agent via targeting tubulin colchicine binding site.Inconsistent results have been reported for the effects of the mitogen-activating extracellular kinase (MEK) inhibitor α-[amino(4-aminophenyl)thio]methylene-2-(trifluoromethyl)benzeneacetonitrile (SL 327) on ethanol-induced conditioned place preference (EtOH-CPP). Since such inconsistencies may be due to the configurational composition of administered SL 327, the interconvertibility of the geometric isomers of this class of compounds has been investigated. This study provides conditions for determination of configurational composition of this class of compounds by HPLC and by 1H NMR and reports details of configurational equilibria as a function of medium and time in solution along with solubility data for SL 327 in aqueous DMSO. The results suggest that the apparently inconsistent results reported for CPP-EtOH may be due to the administration of suspension vs. solutions, as well as to different configurational compositions of SL 327.A series of novel 3-(1-benzotriazole)-nor-β-lapachones 5a-5l were synthesized as the NQO1-targeted anticancer agents. Most of these compounds displayed good antiproliferative activity against the breast cancer MCF-7, lung cancer A549 and hepatocellular carcinoma HepG2 cells in agreements with their NQO1 activity. Among them, compound 5k was identified as a favorable NQO1 substrate. It could activate the ROS production in a NQO1-dependent manner, arrest tumor cell cycle at G0/G1 phase, promote tumor cell apoptosis, and decrease the mitochondrial membrane potential. In HepG2 xenograft models, 5k significantly suppressed the tumor growth with no influences on animal body weights. Therefore, 5k could be a good lead for further anticancer drug developments.Disorders of sex development (DSD) caused by chromosome abnormalities are rarely diagnosed in dogs. In this report, there is a focus on five DSD cases in which the dogs had abnormal karyotypes. All animals were recognized by owners as females, however, these dogs had a large number of reproductive defects. Among these were abnormal external genitalia such as an enlarged clitoris, abnormal development of the labia, abnormal location of the vulva and urethral orifice, and other abnormalities were observed in four dogs. Gonadal histology assessments were conducted on three dogs and there were diagnoses of the presence of an ovary, inactive testes, and ovotestis with calcification in ovarian follicles. Results from cytogenetic analysis indicated there were the following karyotypes (a) X trisomy in a mosaic form (79,XXX/78,XX); (b) Robertsonian translocation in a mosaic form (77,XX,rob/78,XX); (c) nonmosaic X/autosome translocation (78,X,t(X;A)); (d) X/autosome translocation in a mosaic form (78,X,t(X;A)/78,XX); and (e) leukocyte chimerism (78,XX/78,XY). The findings in the present study, emphasize that cytogenetic analysis is essential for elucidating the pathogenesis of DSD in dogs.A new hymenostomatid ciliate, Anteglaucoma orientalis n. sp., isolated from a freshwater pond in Harbin, northeastern China, was investigated using live observation and silver staining methods. Anteglaucoma orientalis is characterized as follows size in vivo about 50-60 × 30-35 μm; oval body shape; buccal area occupies about 25% of body length; 28-36 somatic kineties; membranelle 1 having six or seven basal body rows, membranelle 2 five to seven rows, and membranelle 3 three rows; single macronucleus with one micronucleus attached. selleckchem Morphogenesis of the genus Anteglaucoma is revealed for the first time. The main events during binary fission are as follows morphogenesis begins with proliferation of kinetosomes in the middle part of postoral kinety 1, and kinetosomes of this primordial field multiply and organize to finally form the paroral membrane and membranelles 1-3 of the opisthe; the parental apparatus in the proter does not take part in the stomatogenetic process. Phylogenetic analyses based on SSU rRNA gene sequences show that Anteglaucoma orientalis n. sp. clusters with the type species, A. harbinensis Pan et al., 2017, with full support.An extended activated sludge model (E-ASM2d) was established by including the metabolic processes of double-layer extracellular polymeric substances (EPS) and glycogen-accumulating organisms (GAOs) into the existing ASM2d model for describing and predicting the metabolic processes of the side-stream phosphorus (P) recovery reactor. A sensitivity analysis of model parameters on SPO4(soluble phosphate), XLEPS (loosely-bound EPS), XTEPS (tightly-bound EPS), COD, and SNH4 (soluble ammonia nitrogen) outputs was conducted for identifying influential parameters. The predicted effluent values of COD, ammonia nitrogen (NH4), and P corresponded well with actual measured values and all the model performance coefficient values for COD, NH4, and P were higher than 0.65, implying the E-ASM2d model could accurately simulate the metabolic processes of the side-stream P recovery process under different CODP ratio conditions. The variations in the mainstream biological P metabolic pathway under different CODP conditions were investigated by the E-ASM2d model. At CODP ratios of 30, 20, and 10, the values of fPP,TEPS (fraction of XTEPS in polyphosphate metabolic process) increased from 0.092, 0.094, and 0.096 in the initial phase to 0.107, 0.124, and 0.187 in the side-stream phase, respectively, demonstrating that the fraction of P removal by tightly-bound EPS was improved by the side-stream operation.Heavy metal adsorption onto biochar is an effective method for the treatment of the heavy metal contamination of water and wastewater. This study aims to evaluate the heavy metals sorption efficiency of different biochar characteristics and propose a novel intelligence method for predicting the sorption efficiency of heavy metal onto biochar with high accuracy based on the back-propagation neural network (BPNN) and fuzzy C-means clustering algorithm (FCM), named as FCM-BPNN. Accordingly, the FCM algorithm was used to simulate the properties of metal adsorption data and divide them into clusters with similar features. The clustering results showed that the FCM algorithm simulated metal adsorption data’s properties very well and classified them based on biochar characteristics and adsorption conditions. Afterward, BPNN models were well-developed based on these clusters, and their outcomes were then combined (i.e., FCM-BPNN). The results indicated that the FCM-BPNN model could predict heavy metal’s sorption efficiency onto biochar with a promising result (i.