Chiral Aldehyde-Palladium Catalysis Enables Asymmetric Synthesis of α-Alkyl Tryptophans via Cascade Heck-Alkylation Reaction.

The first catalytic asymmetric cascade Heck-alkylation reaction of NH-unprotected amino acid esters with -(2-iodophenyl)allenamides is reported in this work. Under the promotion of a combining catalytic system comprising a chiral aldehyde, a chiral palladium complex, and the Lewis acid ZnCl, the title reaction takes place smoothly, giving optically active α-alkyl tryptophan derivatives in moderate to good yields and excellent enantioselectivities. The target products can be converted into other structurally complex chiral indoles without the loss of enantioselectivities.

Risk factors of lymph node metastasis or lymphovascular invasion for superficial esophageal squamous cell carcinoma: A practical and effective predictive nomogram based on a cancer hospital data.

Background: Lymphovascular invasion (LVI) is mostly used as a preoperative predictor to establish lymph node metastasis (LNM) prediction models for superficial esophageal squamous cell carcinoma (SESCC). However, LVI still needs to be confirmed by postoperative pathology. In this study, we combined LNM and LVI as a unified outcome and named it LNM/LVI, and aimed to develop an LNM/LVI prediction model in SESCC using preoperative factors.

A Novelly Developed Bipolar Needle Knife Can Be an Alternative Device Choice for Endoscopic Submucosal Dissection (With Video).

Background: Endoscopic submucosal dissection (ESD) is technically difficult with high rates of complications, such as perforation and bleeding. We aimed to explore the safety and cutting efficiency of a novelly devised bipolar knife for ESD procedure.

Methods: Taking a traditional monopolar knife as a reference, the safety and feasibility of the novel bipolar knife were evaluated by an animal experiment and a human study.

Catalytic asymmetric Tsuji-Trost α-benzylation reaction of N-unprotected amino acids and benzyl alcohol derivatives.

Catalytic asymmetric Tsuji-Trost benzylation is a promising strategy for the preparation of chiral benzylic compounds. However, only a few such transformations with both good yields and enantioselectivities have been achieved since this reaction was first reported in 1992, and its use in current organic synthesis is restricted. In this work, we use N-unprotected amino acid esters as nucleophiles in reactions with benzyl alcohol derivatives.

Epiregulin as an Alternative Ligand for Leptin Receptor Alleviates Glucose Intolerance without Change in Obesity.

The leptin receptor (LepR) acts as a signaling nexus for the regulation of glucose uptake and obesity, among other metabolic responses. The functional role of LepR under leptin-deficient conditions remains unclear. This study reports that epiregulin (EREG) governed glucose uptake in vitro and in vivo in mice by activating LepR under leptin-deficient conditions.

"Pink Pattern" Visualized in Magnifying Endoscopy With Narrow-Band Imaging Is a Novel Feature of Early Differentiated Gastric Cancer: A Bridge Between Endoscopic Images and Histopathological Changes.

A pink color change occasionally found by us under magnifying endoscopy with narrow-band imaging (ME-NBI) may be a special feature of early gastric cancer (EGC), and was designated the "pink pattern". The purposes of this study were to determine the relationship between the pink pattern and the cytopathological changes in gastric cancer cells and whether the pink pattern is useful for the diagnosis of EGC. The color features of ME-NBI images and pathological images of cancerous gastric mucosal surfaces were extracted and quantified.

Retrospective analysis of predictive factors for lymph node metastasis in superficial esophageal squamous cell carcinoma.

This study aimed to identify the risk factors of lymph node metastasis (LNM) in superficial esophageal squamous cell carcinoma and use these factors to establish a prediction model. We retrospectively analyzed the data from training set (n = 280) and validation set (n = 240) underwent radical esophagectomy between March 2005 and April 2018. Our results of univariate and multivariate analyses showed that tumor size, tumor invasion depth, tumor differentiation and lymphovascular invasion were significantly correlated with LNM.

A Nomogram for Predicting Lymphovascular Invasion in Superficial Esophageal Squamous Cell Carcinoma.

The lymphovascular invasion (LVI) status facilitates the determination of the optimal therapeutic strategy for superficial esophageal squamous cell carcinoma (SESCC), but in clinical practice, LVI must be confirmed by postoperative pathology. However, studies of the risk factors for LVI in SESCC are limited. Consequently, this study aimed to identify the risk factors for LVI and use these factors to establish a prediction model.

Direct Catalytic Asymmetric α-Allylic Alkylation of Aza-aryl Methylamines by Chiral-Aldehyde-Involved Ternary Catalysis System.

A ternary catalytic system comprising a chiral aldehyde, a transition metal, and a Lewis acid is rationally designed for the asymmetric α-allylic alkylation reaction of aza-aryl methylamines and π-allylmetal electrophiles. Structural diversity chiral amines bearing carbon-carbon double bonds and aza-heterocycles are produced in moderate to good yields with good to excellent enantioselectivities. These products can be readily converted into other chiral amines without the loss of enantioselectivity.

Epiregulin induces leptin secretion and energy expenditure in high-fat diet-fed mice.

Adipokine leptin regulates neuroendocrine circuits that control energy expenditure, thermogenesis and weight loss. However, canonic regulators of leptin secretion, such as insulin and malonyl CoA, do not support these processes. We hypothesize that epiregulin (EREG), a growth factor that is secreted from fibroblasts under thermogenic and cachexia conditions, induces leptin secretion associated with energy dissipation.

Induction of innervation by encapsulated adipocytes with engineered vitamin A metabolism.

Innervation is a fundamental basis for function and survival of tissues. In the peripheral tissues, degenerative diseases create a neurotoxic metabolic milieu that either causes neurodegeneration or fails to sustain regenerative growth and reinnervation of injured/diseased tissues. Encapsulation of cells producing neurotrophic factors can augment axon growth and neuron survival; however, sustained innervation in vivo requires a combination of factors promoting axon growth and guidance pathway that are released in a tissue-specific context.

A Novel Saccadic Strategy Revealed by Suppression Head Impulse Testing of Patients with Bilateral Vestibular Loss.

Objective: We examined the eye movement response patterns of a group of patients with bilateral vestibular loss (BVL) during suppression head impulse testing. Some showed a new saccadic strategy that may have potential for explaining how patients use saccades to recover from vestibular loss.

Methods: Eight patients with severe BVL [vestibulo-ocular reflex (VOR) gains less than 0.

Aldehyde dehydrogenase 1 a1 regulates energy metabolism in adipocytes from different species.

Background: Survival and longevity of xenotransplants depend on immune function and ability to integrate energy metabolism between cells from different species. However, mechanisms for interspecies cross talk in energy metabolism are not well understood. White adipose tissue stores energy and is capable of mobilization and dissipation of energy as heat (thermogenesis) by adipocytes expressing uncoupling protein 1 (Ucp1).

Saccadic Velocity in the New Suppression Head Impulse Test: A New Indicator of Horizontal Vestibular Canal Paresis and of Vestibular Compensation.

Objective: To determine whether saccadic velocity in the suppression head impulse paradigm (SHIMP) test is a reliable indicator of vestibular loss at the acute and at the chronic stage in patients suffering from different vestibular pathologies.

Methods: Thirty-five normal subjects and 57 patients suffering from different vestibular pathologies associated with unilateral vestibular loss (UVL) or bilateral vestibular loss (BVL) were tested in the SHIMPs paradigm. SHIMPs were performed by turning the head 10 times at high velocities to the left or right side, respectively.

[Research progress of TRPV4 and cerebral ischemic reperfusion injury].

Transient receptor potential vanilloid 4 (TRPV4) channel is a member of transient receptor potential superfamily. TRPV4 is selectively permeable to calcium. Activation of the TRPV4 channel induces an increase in intracellular calcium concentration and plays an important role under physiological and pathological conditions.

Encapsulation Thermogenic Preadipocytes for Transplantation into Adipose Tissue Depots.

Cell encapsulation was developed to entrap viable cells within semi-permeable membranes. The engrafted encapsulated cells can exchange low molecular weight metabolites in tissues of the treated host to achieve long-term survival. The semipermeable membrane allows engrafted encapsulated cells to avoid rejection by the immune system.

Egg yolks inhibit activation of NF-κB and expression of its target genes in adipocytes after partial delipidation.

How composition of egg yolk (EY) influences NF-κB, a key transcription pathway in inflammation, remains unclear. We performed partial delipidation of EY that removed 20-30% of cholesterol and triglycerides. The resulting polar and nonpolar fractions were termed EY-P and EY-NP.

Adipocyte reporter assays: application for identification of anti-inflammatory and antioxidant properties of mangosteen xanthones.

Scope: Three fluorescence biosensors were developed based on a 3T3-L1 preadipocyte line that stably expressed Nfkb-RE/GFP, Fabp4-P/CFP, and Nrf2-P/YFP fluorescent reporters. We hypothesized that nutraceuticals' inflammatory, adipogenic, and antioxidant status will be identified based on the change in fluorescence in reporter adipocytes. We validated these assays with activators of NFκB, FABP4-regulating peroxisome proliferator activated receptor gamma, NFR2 and, thereafter, tested known and unknown properties of mangostines (MGs), the xanthone metabolites in mangosteen fruit.

Zinc deficiency augments leptin production and exacerbates macrophage infiltration into adipose tissue in mice fed a high-fat diet.

Zinc (Zn) deficiency and obesity are global public health problems. Zn deficiency is associated with obesity and comorbid conditions that include insulin resistance and type 2 diabetes. However, the function of Zn in obesity remains unclear.