l -( -) -Quebrachitol as a Ligand for Selective Copper(0)-Catalyzed N-Arylation of Nitrogen-Containing Heterocycles.

l-(-)-Quebrachitol (QCT) has been found as a ligand of copper powder for selective N-arylation of nitrogen-containing heterocycles with aryl halides. Furthermore, another potential catalytic system (copper powder/QCT/ t-BuOK) was successfully adapted to unactivated aryl chlorides.

Targeting HDAC/OAZ1 axis with a novel inhibitor effectively reverses cisplatin resistance in non-small cell lung cancer.

Cisplatin yields significant efficacy and is generally used as a frontline therapy for non-small cell lung cancer (NSCLC). However, acquired resistance strongly limits its application. Here, we identified that a novel histone deacetylase (HDAC) inhibitor S11, with P-glycoprotein inhibitory activity, could obviously suppress cell growth in cisplatin-resistant NSCLC cell lines.

Targeted delivery of ibrutinib to tumor-associated macrophages by sialic acid-stearic acid conjugate modified nanocomplexes for cancer immunotherapy.

Ibrutinib (IBR), an irreversible Bruton's tyrosine kinase (BTK) inhibitor, is expected to be a potent therapeutic modality, given that BTK is overexpressed in tumor-associated macrophages (TAMs) and participates in promoting tumor progression, angiogenesis, and immunosuppression. However, rapid clearance in vivo and low tumor accumulation have rendered effective uptake of IBR by TAMs challenge. Herein, we designed and synthesized a sialic acid (SA)-stearic acid conjugate modified on the surface of nanocomplexes to encapsulate IBR (SA/IBR/EPG) for targeted immunotherapy.

Design, synthesis and evaluation of N-hydroxypropenamides based on adamantane to overcome resistance in NSCLC.

A series of novel N-hydroxypropenamides containing adamantane moiety were identified and most of them exhibited HDAC inhibitory activity and could reverse the resistance of cisplatin in NSCLC cell lines. In this process, molecular docking was employed to verify the rationality of designing, subsequently, target compounds were synthesized and conducted to enzyme- and cell-based biological evaluation. Most of synthesized compounds could inhibit HDAC activity with the IC values lower than 50 nM and result in the increase of Ac-H4 and p21 in A549 cells.

Synthesis and biological evaluation of 2,2-dimethylbenzopyran derivatives as potent neuroprotection agents.

The development of novel neuroprotection agents is of great significance for the treatment of ischemic stroke. In this study, a series of compounds comprising 2,2-dimethylbenzopyran groups and cinnamic acid groups have been synthesized. Preferential combination principles and bioisostere that improved the neuroprotective effect of the compounds were identified for this series biological activity assay .

[Knockdown of serpin E2 inhibits proliferation, invasion and migration of colon cancer cells].

Objective To investigate the effect of serpin E2 on the proliferation, invasion and migaration of colon cancer cells. Methods The expression of serpin E2 was detected by immunohistochemistry in 30 pairs of colon cancer and adjacent tissues. The expression of serpin E2 in colon cancer SW480 cells was down-regulated by siRNA.

Arylsulfonamide 64B Inhibits Hypoxia/HIF-Induced Expression of c-Met and CXCR4 and Reduces Primary Tumor Growth and Metastasis of Uveal Melanoma.

Purpose: Uveal melanoma (UM) is the most prevalent and lethal intraocular malignancy in adults. Here, we examined the importance of hypoxia in UM growth and tested the antitumor effects of arylsulfonamide 64B, an inhibitor of the hypoxia-induced factor (HIF) pathway in animal models of UM and investigated the related mechanisms.

Experimental Design: UM cells were implanted in the uvea of mice eyes and mice systemically treated with 64B.

Intraspectrum Discrimination and Interspectrum Correlation Analysis Deep Network for Multispectral Face Recognition.

Multispectral images contain rich recognition information since the multispectral camera can reveal information that is not visible to the human eye or to the conventional RGB camera. Due to this characteristic of multispectral images, multispectral face recognition has attracted lots of research interest. Although some multispectral face recognition methods have been presented in the last decade, how to fully and effectively explore the intraspectrum discriminant information and the useful interspectrum correlation information in multispectral face images for recognition has not been well studied.

OAB-14, a bexarotene derivative, improves Alzheimer's disease-related pathologies and cognitive impairments by increasing β-amyloid clearance in APP/PS1 mice.

The pathogenesis of Alzheimer's disease (AD) is complex, though the clinical failures of anti-AD candidates targeting Aβ production (such as β- and γ-secretase inhibitors) make people suspect the Aβ hypothesis, in which the neurotoxicity of Aβ is undoubtedly involved. According to studies, >95% of AD patients with sporadic AD are primarily associated with abnormal Aβ clearance. Therefore, drugs that increase Aβ clearance are becoming new prospects for the treatment of AD.

Nomogram prediction of individual prognosis of patients with acute-on-chronic hepatitis B liver failure.

Background: The current definitions and etiologies of acute-on-chronic liver failure (ACLF) are clearly very different between East and West.

Aims: This study aimed to develop an effective prognostic nomogram for acute-on-chronic hepatitis B liver failure (ACHBLF) as defined by the Asia Pacific Association for the Study of the Liver (APASL).

Methods: The nomogram was based on a retrospective study of 573 patients with ACHBLF, defined according to the APASL, at the Beijing Ditan Hospital.

Zinc (II)-Mediated Selective -Benzylation of 2-Oxo-1,2-Dihydropyridines Systems.

The selective -benzylation of 2-oxo-1,2-dihydropyridines plays a critical role in organic synthesis of natural products and biological active molecules. Herein we report a novel ternary system of ZnO, ZnCl₂ and ,-diisopropylethylamine (DIEA), that is highly effective for selective -benzylation of 2-oxo-1,2-dihydropyridines using abundant substituted benzyl halides and related substituted 2-oxo-1,2-dihydropyridines compounds. This process allows access to a variety of -benzyl products under mild reaction conditions, which are important synthetic intermediates in the protection of functional groups, and represents a new method toward the development for the -benzylation of 2-oxo-1,2-dihydropyridines.

Design, synthesis and activity of BBI608 derivatives targeting on stem cells.

STAT3 plays a vital role in maintaining the self-renewal of tumor stem cells. BBI608, a small molecule identified by its ability to inhibit gene transcription driven by STAT3 and cancer stemness properties, can inhibit stemness gene expression and kill stemness-high cancer cells isolated from a variety of cancer types. In order to improve the pharmacokinetic properties of BBI608 and the antitumor activity, a series of BBI608 derivatives were designed and synthesized here.

Conversion between 2 military combat-related injury coding systems.

Deployable medical systems(DEPMEDS) patient conditions (PCs) and Military Combat Injury Scale (MCIS) are 2 important military medical coding systems. However, both of them have defects when applied in military medical planning. Although each PC code contains information about treatment, intensity of care, treatment time, length of stay, and probability of disposition that is relevant to simulation, its description is too comprehensive and ambiguous to code historical military medical records.

Characteristics and mechanisms of cadmium adsorption from aqueous solution using lotus seedpod-derived biochar at two pyrolytic temperatures.

Herein, biochar derived from lotus seedpods, as an effective adsorbent, was prepared by pyrolysis method at 300 and 600 °C. The physicochemical characteristics and cadmium adsorption properties were studied systematically by batch adsorption experiments, FTIR, SEM-EDX, XRD, and XPS. Cd adsorption onto lotus seedpod-derived biochar was better fitted using Freundlich isotherm and pseudo-second-order model.

Surface structure feature matching algorithm for cardiac motion estimation.

Background: Cardiac diseases represent the leading cause of sudden death worldwide. During the development of cardiac diseases, the left ventricle (LV) changes obviously in structure and function. LV motion estimation plays an important role for diagnosis and treatment of cardiac diseases.

Inhibition of histone deacetylases sensitizes EGF receptor-TK inhibitor-resistant non-small-cell lung cancer cells to erlotinib in vitro and in vivo.

Background And Purpose: Intrinsic and/or acquired resistance of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) commonly occurs in patients with non-small-cell lung cancer (NSCLC). Here, we developed a combined therapy of histone deacetylase inhibition by a novel HDAC inhibitor, YF454A, with erlotinib to overcome EGFR-TKI resistance in NSCLC.

Experimental Approach: The sensitization of the effects of erlotinib by YF454A was examined in a panel of EGFR-TKI-resistant NSCLC cell lines in vitro and two different erlotinib-resistant NSCLC xenograft mouse models in vivo.

Shot-gun proteome and transcriptome mapping of the jujube floral organ and identification of a pollen-specific S-locus F-box gene.

The flower is a plant reproductive organ that forms part of the fruit produced as the flowering season ends. While the number and identity of proteins expressed in a jujube ( Mill.) flower is currently unknown, integrative proteomic and transcriptomic analyses provide a systematic strategy of characterizing the floral biology of plants.

Influence of Sulfur on the Arsenic Phytoremediation Using Vallisneria natans (Lour.) Hara.

Influences of sulfur (S) on the accumulation and detoxification of arsenic (As) in Vallisneria natans (Lour.) Hara, an arsenic hyperaccumulating submerged aquatic plant, were investigated. At low sulfur levels (<20 mg/L), the thiols and As concentrations in the plant increased significantly with increasing sulfate nutrient supply.

Neurophysiological Evidence of Compensatory Brain Mechanisms Underlying Attentional-Related Processes in Symptomatically Remitted Patients with Schizophrenia.

A recent electrophysiological study suggests existing compensatory brain activity as a mechanism for functional recovery of visual attention detection (the capacity for detecting external cues) in symptomatically remitted schizophrenia patients. Despite such evidence, little is known about other aspects of attentional-related processes in schizophrenia during clinical remission, such as their capacity to concentrate on the task at hands without being interfered by distracting information. To this end, we recorded event-related brain potentials (ERPs) from 20 symptomatically remitted schizophrenia patients and 20 healthy controls while they engaged in a classic Stroop task.

New Avermectin Analogues from a Mutant Streptomyces avermectinius Strain.

Two new avemectin analogues 1 and 2 belonging to 'b' series of components were isolated from a ∆aveCDE mutant Streptomyces avermectinius strain. Their structures were elucidated by detailed analysis of NMR and MS spectroscopic data. Compounds 1 and 2 displayed moderate cytotoxicities against B16, MG-63, and Saos-2 cell lines in an in vitro assay.

[Efficacy of Shangbai ointment in alleviating pain in patients with acute ankle joint lateral collateral ligament injury: a randomized controlled trial].

Objective: To investigate the effect of Shangbai ointment in relieving pain in patients with acute ankle joint lateral collateral ligament injury.

Methods: Fifty patients with unilateral ankle injury were randomized into Shangbai ointment treatment group and control group (n=25). The Visual Analog Scale (VAS) pain scores, ankle joint circumference, Kofoed score and self-rated lower limb function were recorded before and at 3, 7, and 14 days after the treatment.

Anti-tumor activity of SL4 against breast cancer cells: induction of G/M arrest through modulation of the MAPK-dependent p21 signaling pathway.

SL4, a chalcone-based compound, has been shown to retard tumor invasion and angiogenesis by suppressing HIF1 activity and to induce apoptosis by promoting ROS release. Here, we report that SL4 is able to inhibit the proliferation of different types of breast cancer cell in vitro and in vivo by inducing G/M cell cycle arrest. Our results showed that SL4 exhibited strong anti-proliferative activity in several human breast cancer cell lines, with IC values lower than 1.

SYP-5, a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.

Hypoxia-inducible factor-1 (HIF-1) plays an essential role in carcinogenesis. The overexpression of HIF-1 induced by hypoxia is closely associated with metastasis, poor prognosis and high mortality. In this study, a novel HIF-1 inhibitor SYP-5 was first observed by the luciferase reporter assay.

Lung motion estimation by robust point matching and spatiotemporal tracking for 4D CT.

We propose a deformable registration approach to estimate patient-specific lung motion during free breathing for four-dimensional (4D) computed tomography (CT) based on point matching and tracking between images in different phases. First, a robust point matching (RPM) algorithm coarsely aligns the source phase image onto all other target phase images of 4D CT. Scale-invariant feature transform (SIFT) is introduced into the cost function in order to accelerate and stabilize the convergence of the point matching.

The L-type Ca(2+) Channel Blocker Nifedipine Inhibits Mycelial Growth, Sporulation, and Virulence of Phytophthora capsici.

The oomycete vegetable pathogen Phytophthora capsici causes significant losses of important vegetable crops worldwide. Calcium and other plant nutrients have been used in disease management of oomycete pathogens. Calcium homeostasis and signaling is essential for numerous biological processes, and Ca(2+) channel blockers prevent excessive Ca(2+) influx into the fungal cell.