RIP1 regulates TNF-α-mediated lymphangiogenesis and lymphatic metastasis in gallbladder cancer by modulating the NF-κB-VEGF-C pathway.

Background: Tumor necrosis factor alpha (TNF-α) enhances lymphangiogenesis in gallbladder carcinoma (GBC) via activation of nuclear factor (NF-κB)-dependent vascular endothelial growth factor-C (VEGF-C). Receptor-interacting protein 1 (RIP1) is a multifunctional protein in the TNF-α signaling pathway and is highly expressed in GBC. However, whether RIP1 participates in the signaling pathway of TNF-α-mediated VEGF-C expression that enhances lymphangiogenesis in GBC remains unclear.

[Effectiveness of limbs shortening and re-lengthening in treatment of tibial infectious bone defect and chronic osteomyelitis].

Objective: To evaluate the limbs shortening and re-lengthening in the treatment of tibial infectious bone defect and chronic osteomyelitis.

Methods: Between January 2011 and April 2016, 19 cases of tibial infectious bone defect and chronic osteomyelitis were treated with the limbs shortening and re-lengthening technique. There were 13 males and 6 females, aged from 22 to 62 years (mean, 44 years).

[Posterior short-segment fixation including the fractured vertebra for severe unstable thoracolumbar fractures].

Objective: To discuss the effectiveness of posterior short-segment fixation including the fractured vertebra for severe unstable thoracolumbar fractures using pedicle screw fixation.

Methods: Between May 2008 and July 2013, 52 patients of severe unstable thoracolumbar fractures were treated through posterior short-segment fixation including the fractured vertebra using pedicle screw fixation. There were 33 males and 19 females with an age of 21-56 years (mean, 37.

N-acylanthranilic acid derivatives with anti-Aβ aggregation activity from the leaves of Isatis indigotica fortune.

Seven new N-acylanthranilic acid derivatives (1-3, 4a/4b, 5a/5b) including two pairs of enantiomers (4a/4b and 5a/5b) were isolated from the leaves of Isatis indigotica Fortune. Their chemical structures were elucidated by extensive spectroscopic data analyses. The absolute configurations of compounds 4a/4b and 5a/5b were determined by comparison of the experimental and calculated ECD spectra.

Sheets of human retinal progenitor transplants improve vision in rats with severe retinal degeneration.

Loss of photoreceptors and other retinal cells is a common endpoint in retinal degenerate (RD) diseases that cause blindness. Retinal transplantation is a potential therapy to replace damaged retinal cells and improve vision. In this study, we examined the development of human fetal retinal sheets with or without their retinal pigment epithelium (RPE) transplanted to immunodeficient retinal degenerate rho S334ter-3 rats.

Three new polyketides from sp. ZJ-M-5 by the OSMAC strategy.

Three new compounds, ascotrichols A-B () and ascotrichrone A (), along with two known isocoumarin derivatives (), were isolated from the solid culture of a sea mud-derived fungus, sp. ZJ-M-5 on rice media. The structures were elucidated by extensive spectroscopic analyses, including 1D and 2D NMR data, and the absolute configurations were determined by electronic circular dichroism and biogenetic correlation.

ent-Kaurane Diterpenoids with Neuroprotective Properties from Corn Silk ( Zea mays).

Thirteen new ent-kaurane diterpenoids, stigmaydenes A-M (1-13), together with two known compounds (14, 15), were isolated from the crude extract of corn silk ( Zea mays). The structures of the compounds were confirmed by comprehensive spectroscopic analyses. The absolute configuration of compound 1 was defined by single-crystal X-ray diffraction.

Synthesis, biological evaluation and molecular modeling of 2-amino-2-phenylethanol derivatives as novel β-adrenoceptor agonists.

A novel series of 2-amino-2-phenylethanol derivatives were developed as β-adrenoceptor agonists. Among them, 2-amino-3-fluoro-5-(2-hydroxy-1-(isopropylamino)ethyl)benzonitrile (compound 2f) exhibited the highest activity (EC = 0.25 nM) in stimulating β-adrenoceptor-mediated cellular cAMP production with a 763.

Synthesis and biological evaluation of β-adrenoceptor agonists bearing the 2-amino-2-phenylethanol scaffold.

A new series of β-adrenoceptor agonists bearing the 2-amino-2-phenylethanol scaffold was synthesized. Evaluation of the compounds using cell assays and an in vitro guinea pig trachea relaxation assay showed that 8-hydroxy-5-(2-hydroxy-1-((4-hydroxyphenethyl)amino)ethyl)quinolin-2(1H)-one (compound 5j) has the best pharmacological profile among all the evaluated compounds. The (S)-isomer of 5j was subsequently found to be the active enantiomer with a promising EC value of 1.

Heronamides G-L, polyene macrolactams from .

Six new polyene macrolactams, heronamides G-L (1-6), one new polyenoic acid derivative, niveamide B (10), together with four known compounds, BE-14106-6 (7), BE-14106 (8), GT32-B (9), and niveamide (11), were isolated from the fermentation broth of . Their planar structures were elucidated by detailed analysis of spectroscopic data. The absolute configurations of compounds 1-6 were determined by calculated ECD spectra and analysis of the possible biosynthetic pathways.

c‑Jun suppresses the expression of WNT inhibitory factor 1 through transcriptional regulation and interaction with DNA methyltransferase 1 in gallbladder cancer.

WNT inhibitory factor 1 (WIF‑1) is involved in the tumorigenicity and progression of several types of tumor, which has been attributed to aberrant hypermethylation of its promoter. However, the role of WIF‑1 in the pathogenesis of gallbladder cancer (GBC) remains to be fully elucidated, and the data available are insufficient to identify the upstream molecular mechanisms involved. In the present study, the methylation status of the WIF‑1 promoter was investigated using methylation‑specific polymerase chain reaction (PCR) and bisulfate sequencing PCR in GBC cells.

DUSP14 knockout accelerates cardiac ischemia reperfusion (IR) injury through activating NF-κB and MAPKs signaling pathways modulated by ROS generation.

Inflammation and oxidative stress are significantly involved in the progression of a variety of diseases, including myocardial ischemia/reperfusion (IR). In the present study, we hypothesized a protective role of dual-specificity phosphatase 14 (DUSP14) in myocardial IR, as well as the underlying molecular mechanism. The results indicated that DUSP14 was down-regulated following cardiac IR injury.

Synthetic Approaches to Tetracyclic Indolines as Versatile Building Blocks of Diverse Indole Alkaloids.

Indole alkaloids bearing the tetracyclic indoline scaffolds of 1H-pyrrolo[2,3-d]carbazole have shown fascinating chemical diversity and significant biological activities. The development of efficient synthetic methodologies for such a tetracyclic scaffold remains highly desirable in both synthetic chemistry and medicinal chemistry. This review outlines key strategies for the construction of the tetracyclic indoline scaffolds in total syntheses of many indole alkaloids.

Sparse Reconstruction Based Robust Near-Field Source Localization Algorithm.

Non-Gaussian impulsive noise widely exists in the real world, this paper takes the α-stable distribution as the mathematical model of non-Gaussian impulsive noise and works on the joint direction-of-arrival (DOA) and range estimation problem of near-field signals in impulsive noise environment. Since the conventional algorithms based on the classical second order correlation statistics degenerate severely in the impulsive noise environment, this paper adopts two robust correlations, the fractional lower order correlation (FLOC) and the nonlinear transform correlation (NTC), and presents two related near-field localization algorithms. In our proposed algorithms, by exploring the symmetrical characteristic of the array, we construct the robust far-field approximate correlation vector in relation with the DOA only, which allows for bearing estimation based on the sparse reconstruction.

P_UNSAT approach of attractor calculation for Boolean gene regulatory networks.

Boolean network models provide an efficient way for studying gene regulatory networks. The main dynamics of a Boolean network is determined by its attractors. Attractor calculation plays a key role for analyzing Boolean gene regulatory networks.

Neuroprotective effect of dexmedetomidine in a murine model of traumatic brain injury.

No FDA approved pharmacological therapy is available that would reduce cell death following traumatic brain injury (TBI). Dexmedetomidine (Dex) is a highly selective agonist of alpha-2 adrenergic receptors and has demonstrated neuroprotective effects in hippocampal slice cultures undergoing direct impact. However, no one has tested whether Dex, in addition to its sedative action, has neuroprotective effects in an animal model of TBI.

Phenylpropanoids from the fruit of Crataegus pinnatifida exhibit cytotoxicity on hepatic carcinoma cells through apoptosis induction.

Eight new phenylpropanoids (1a/1b, 2-4, 5a/5b and 6) including two pairs of enantiomers (1a/1b and 5a/5b), along with a known analogue (7) were isolated from the fruit of Crataegus pinnatifida. Their structures were elucidated using comprehensive spectroscopic methods. Compounds 1a/1b and 5a/5b were separated successfully by chiral chromatographic column.

Alkaloids with neuroprotective effects from the leaves of Isatis indigotica collected in the Anhui Province, China.

Six undescribed alkaloids, indiforine A-F, together with four known ones, were isolated from the leaves of Isatis indigotica Fortune. Their structures were elucidated on the basis of extensive spectroscopic analyses. The absolute configurations of indiforine A and B were determined by comparison of the experimental and calculated electronic circular dichroism spectra, as well as experimental and calculated optical rotations.

Enantiomeric lignans with anti-β-amyloid aggregation activity from the twigs and leaves of Pithecellobium clypearia Benth.

To develop potential agents for slowing the progression of Alzheimer's disease, two pairs of new enantiomeric lignans, including a couple of rarely 8',9'-dinor-3',7-epoxy-8,4'-oxyneolignanes named (7S, 8S)- and (7R, 8R)-pithecellobiumin A (1a/1b) and a pair of 2',9'-epoxy-arylnaphthalenes named (7R, 8R, 8'R)- and (7S, 8S, 8'S)-pithecellobiumin B (2a/2b) were separated by chiral high performance liquid chromatography (HPLC). Their planar structures were elucidated by spectroscopic data analyses. The absolute configurations were determined by comparing of experimental and calculated electronic circular dichroism (ECD).

Intestinal absorption and activation of decitabine amino acid ester prodrugs mediated by peptide transporter PEPT1 and enterocyte enzymes.

Decitabine (DAC), a potent DNA methyltransferase (DNMT) inhibitor, has a limited oral bioavailability. Its 5'-amino acid ester prodrugs could improve its oral delivery but the specific absorption mechanism is not yet fully understood. The aim of this present study was to investigate the in vivo absorption and activation mechanism of these prodrugs using in situ intestinal perfusion and pharmacokinetics studies in rats.

[Comparision of clinical effects between one-stage anterior and posterior approach in treating thoracolumbar tuberculosis with debridement and internal fixation].

Objective: To compare the outcomes of surgical operation by posterior or anterior approach only for thoracolumbar tuberculosis.

Methods: The clinical data of 97 patients with thoracolumbar tuberculosis underwent debridement and internal fixation from January 2005 to December 2014 were retrospectively analyzed. The study included 59 males and 38 females, with a mean age of 53.

Tetrahydrocurcumin‑induced autophagy via suppression of PI3K/Akt/mTOR in non‑small cell lung carcinoma cells.

Lung carcinoma is the leading cause of mortality due to cancer worldwide. Autophagy has a significant role in the development and progression of non‑small cell lung carcinoma (NSCLC). A previous study has revealed that tetrahydrocurcumin (THC), a traditional Chinese medicine isolated from Curcuma wenyujin (Chen & Ling, 1981), induces autophagy in human A549 NSCLC cells.

Risk factors for non-fusion segment disease after anterior cervical spondylosis surgery: a retrospective study with long-term follow-up of 171 patients.

Background: The purpose of this study was to investigate the incidence and causes of non-fusion segment disease (NFSD), both adjacent and non-adjacent to a fused segment, after anterior cervical arthrodesis.

Methods: This is a single-center study. Between January 1998 and January 2011, two surgeons' 171 patients who had an anterior cervical decompression and fusion were followed clinically for more than 5 years.

Chiral resolution and bioactivity of enantiomeric benzofuran neolignans from the fruit of Rubus ideaus L.

Rubus ideaus L., a member of the Rosaceae family, is popular for its distinctive flavor and attractive red color. In order to explore the functional factors possibly presented in the fruit, seven new benzofuran neolignans (1a/1b-3a/3b and 4b), together with one known neolignan 4a, were isolated from the fruit of R.