A note on nonnegative normal matrices

AbstractIn this note we characterize nonnegative matrices A for which AT = p(A), where p(A) is a polynomial with nonnegative coefficients and p(0) ≠ 0

Synthesis and antiviral activity of a series of novel N-phenylbenzamide and N-phenylacetophenone compounds as anti-HCV and anti-EV71 agents

AbstractA series of novel N-phenylbenzamide and N-phenylacetophenone compounds were synthesized and evaluated for their antiviral activity against HCV and EV71 (strain SZ-98). The biological results showed that three compounds (23, 25 and 41) exhibited considerable anti-HCV activity (IC50=0.57–7.12μmol/L) and several compounds (23, 28, 29, 30, 31 and 42) displayed potent activity against EV71 with the IC50 values lower than 5.00μmol/L. The potency of compound 23 (IC50=0.57μmol/L) was superior to that of reported compounds IMB-1f (IC50=1.90μmol/L) and IMB-1g (IC50=1.00μmol/L) as anti-HCV agents, and compound 29 possessed the highest anti-EV71 activity, comparable to the comparator drug pirodavir. The efficacy in vivo and antiviral mechanism of these compounds warrant further investigations

N-(4-Chloro­phen­yl)-4-meth­oxy-3-(propanamido)­benzamide cyclo­hexane hemisolvate

The title compound, C17H17ClN2O3·0.5C6H12, was prepared by the condensation reaction of 4-meth­oxy-3-(propanamido)­benzoic acid with 4-chloro­aniline. The Cl atom, the propionyl CH3 group and the cyclo­hexyl CH2 group are disordered over two sets of sites of equal occupancy in both mol­ecules. The cyclo­hexane solvent mol­ecule is disordered over two orientations which were modelled with relative occupancies of 0.484 (4) and 0.516 (4). In the crystal, there are a number of N—H⋯O hydrogen bonds, forming layers perpendicular to (001)

Synthesis and antiviral activities of a novel class of thioflavone and flavonoid analogues

AbstractA novel class of thioflavone and flavonoid derivatives has been prepared and their antiviral activities against enterovirus 71 (EV71) and the coxsackievirus B3 (CVB3) and B6 (CVB6) were evaluated. Compounds 7d and 9b showed potent antiviral activities against EV71 with IC50 values of 8.27 and 5.48μM, respectively. Compound 7f, which has been synthesized for the first time in this work, showed the highest level of inhibitory activity against both CVB3 and CVB6 with an IC50 value of 0.62 and 0.87μM. Compounds 4b, 7a, 9c and 9e also showed strong inhibitory activities against both the CVB3 and CVB6 at low concentrations (IC50=1.42−7.15μM), whereas compounds 4d, 7c, 7e and 7g showed strong activity against CVB6 (IC50=2.91–3.77μM) together with low levels of activity against CVB3. Compound 7d exhibited stronger inhibitory activity against CVB3 (IC50=6.44μM) than CVB6 (IC50>8.29μM). The thioflavone derivatives 7a, 7c, 7d, 7e, 7f and 7g, represent a new class of lead compounds for the development of novel antiviral agents

Synthesis of novel substituted N-aryl benzamides as hA3G stabilizers and their inhibitory activities against hepatitis C virus replication

AbstractA series of novel amino-substituted N-aryl benzamide analogs were synthesized and evaluated for their ability to inhibit hepatitis C virus (HCV) replication in acutely infected Huh7.5 cells. Most of the substituted N-aryl benzamide compounds showed convincing anti-HCV activities. Compounds 1f, 1g and 4c exhibited potent anti-replicative activity at low micromolar levels (IC50=1.0–2.0μM) with selective indices (SI) greater than 40. Mechanistic analysis indicated that the active compounds increased intracellular hA3G protein levels and inhibited HCV replication in a dose-dependent manner. The results demonstrate that this series of substituted N-aryl benzamide compounds warrant further investigation as inhibitors of HCV replication

A cross-subject decoding algorithm for patients with disorder of consciousness based on P300 brain computer interface

BackgroundBrain computer interface (BCI) technology may provide a new way of communication for some patients with disorder of consciousness (DOC), which can directly connect the brain and external devices. However, the DOC patients’ EEG differ significantly from that of the normal person and are difficult to collected, the decoding algorithm currently only is trained based on a small amount of the patient’s own data and performs poorly.MethodsIn this study, a decoding algorithm called WD-ADSTCN based on domain adaptation is proposed to improve the DOC patients’ P300 signal detection. We used the Wasserstein distance to filter the normal population data to increase the training data. Furthermore, an adversarial approach is adopted to resolve the differences between the normal and patient data.ResultsThe results showed that in the cross-subject P300 detection of DOC patients, 7 of 11 patients achieved an average accuracy of over 70%. Furthermore, their clinical diagnosis changed and CRS-R scores improved three months after the experiment.ConclusionThese results demonstrated that the proposed method could be employed in the P300 BCI system for the DOC patients, which has important implications for the clinical diagnosis and prognosis of these patients

Tilianin improves cognition in a vascular dementia rodent model by targeting miR-193b-3p/CaM- and miR-152-3p/CaMKIIα-mediated inflammatory and apoptotic pathways

IntroductionAlthough vascular dementia (VaD) is the second most prevalent form of dementia, there is currently a lack of effective treatments. Tilianin, isolated from the traditional drug Dracocephalum moldavica L., may protect against ischemic injury by inhibiting oxidative stress and inflammation via the CaMKII-related pathways but with weak affinity with the CaMKII molecule. microRNAs (miRNAs), functioning in post-transcriptional regulation of gene expression, may play a role in the pathological process of VaD via cognitive impairment, neuroinflammatory response, and neuronal dysfunction. This study aimed to investigate the role of tilianin in VaD therapy and the underlying mechanism through which tilianin regulates CaMKII signaling pathways based on miRNA-associated transcriptional action.MethodsRats with 2-vessel occlusion (2VO), a standard model of VaD, were treated with tilianin, vehicle control, and target overexpression or downregulation. High-throughput sequencing, qRT-PCR, and western blot analyses were utilized to identify the downstream target genes and signaling pathways of tilianin involved in VaD.ResultsOur results showed that tilianin ameliorated cognitive deficits, neurodegeneration, and microglial and astrocytic activation in rats with 2VO. Subsequent high-throughput sequencing and qRT-PCR analyses revealed that tilianin increased the downregulated miR-193b-3p and miR-152-3p levels in the cortex and hippocampus of 2VO rats. Mechanistically, miR-193b-3p targeting CaM and miR-152-3p targeting CaMKIIα were identified to play a role in VaD-associated pathology, inhibiting the p38 MAPK/NF--κB p65 pathway and decreasing TNF-α and IL-6 levels. Further gain- and loss-of-function experiments for these key genes showed that tilianin-exerted cognitive improvement by activating the p38 MAPK/NF--κB p65 and Bcl-2/Bax/caspase-3/PARP pathways in the brain of 2VO rats was abolished by miR-193b-3p and miR-152-3p inhibition. Moreover, CaM and CaMKIIα overexpression eliminated the elevated effects of miR-193b-3p and miR-152-3p on tilianin’s protection against ischemic injury through increased inflammatory reactions and apoptotic signaling.DiscussionTogether, these findings indicate that tilianin improves cognition by regulating the miR-193b-3p/CaM- and miR-152-3p/CaMKIIα-mediated inflammatory and apoptotic pathways, suggesting a potential small-molecule regulator of miRNA associated with inflammatory signaling for VaD treatment

7-Pyrrolidinethoxy-4′-Methoxyisoflavone Prevents Amyloid β–Induced Injury by Regulating Histamine H3 Receptor-Mediated cAMP/CREB and AKT/GSK3β Pathways

In studies on the treatment of Alzheimer’s disease (AD), in which cognition is enhanced even modestly or selectively, it has been considered that the histamine H3 receptor (H3R) may be a potential target. In this study, we aimed at evaluating the ability of 7-pyrrolidinethoxy-4′-methoxyisoflavone (indicated as LC1405), a novel potential H3R antagonist identified from our H3R antagonist screening system, to ameliorate amyloid β (Aβ)-induced cognitive deficits, and to explore the underlying mechanisms that are related to H3R-modulated signaling. Our results demonstrated that LC1405 effectively reduced the progression of Aβ-associated disorders, such as improved learning and memory capabilities, preserved tissues from suffering neurodegeneration and ultrastructural abnormalities, and ameliorated cholinergic dysfunction in an APP/PS1 double transgenic mouse model of AD. In an in vitro model, LC1405 protected neuronal cells against copper-induced Aβ toxicity, as demonstrated by the improvement in cell viability and decrease in neuronal apoptotic ratio. In addition, treatment with LC1405 resulted in the up-regulation of acetylcholine (ACh) or histamine release and provided neuroprotection through cellular signaling cascades involving H3R-mediated cAMP/CREB and AKT/GSK3β pathways. Furthermore, the beneficial effects of LC1405 on Aβ-mediated toxicity and H3R-mediated cAMP/CREB and AKT/GSK3β axes were reversed after pharmacological activation of H3R. In conclusion, our results demonstrated that LC1405 blocked Aβ-induced toxicity through H3R-modulated signaling transduction both in vitro and in vivo. The results also suggested that LC1405 might have translational potential as a complementary therapy to control disease progression in AD patients who developed cognitive deficits with H3R-related ACh neurotransmission abnormality

Image Translation by Domain-Adversarial Training

Image translation, where the input image is mapped to its synthetic counterpart, is attractive in terms of wide applications in fields of computer graphics and computer vision. Despite significant progress on this problem, largely due to a surge of interest in conditional generative adversarial networks (cGANs), most of the cGAN-based approaches require supervised data, which are rarely available and expensive to provide. Instead we elaborate a common framework that is also applicable to the unsupervised cases, learning the image prior by conditioning the discriminator on unaligned targets to reduce the mapping space and improve the generation quality. Besides, domain-adversarial training inspired by domain adaptation is proposed to capture discriminative and expressive features, for the purpose of improving fidelity. Effectiveness of our method is demonstrated by compelling experimental results of our method and comparisons with several baselines. As for the generality, it could be analyzed from two perspectives: adaptation to both supervised and unsupervised setting and the diversity of tasks

(E)-2-Hydroxy-4-methoxy-3-(3-methylbut-2-enyl)-6-styrylbenzoic acid

The title compound, C21H22O4, also known as cajanine, features an intramolecular O—H...O hydrogen bond between the adjacent carboxy and hydroxy groups. The benzene rings make an interplanar angle of 175.4 (2)°. In the crystal, molecules are linked by pairs of O—H...O hydrogen bonds, forming inversion dimers