B(CF)/CPA-Catalyzed Aza-Diels-Alder Reaction of 3,3-Difluoro-2-Aryl-3H-indoles and Unactivated Dienes.

Here we report B(CF)CPA-catalyzed enantioselective aza-Diels-Alder reaction of 3,3-difluoro-2-Aryl-3H-indoles with unactivated dienes to access chiral 10,10-difluoro-tetrahydropyrido[1,2-a]indoles. This protocol allows the formation of pyrazole-based C2-quaternary indolin-3-ones with high enantioselectivities and regioselectivities. Moreover, gram-scale synthesis of the 10,10-difluoro-tetrahydropyrido[1,2-a]indole skeleton was successfully achieved without any reduction in both yield and enantioselectivity.

Highly Enantioselective Synthesis of 3-Fluorofuro[3,2-]indolines via Organocatalytic Aza-Friedel-Crafts Reaction/Selective C-F Bond Activation.

Fluoroalkylated compounds are of high interest in drug discovery and have inspired the evolution of diverse C-F bond activation methodologies. However, the selective activation of polyfluorinated compounds remains challenging. Herein, we describe an unprecedented strategy for synthesizing enantioenriched fluorofuro[3,2-]indolines through the organocatalytic aza-Friedel-Crafts reaction coupled with selective C-F bond activation.

Anti-freezing dual-network hydrogels with high-strength, self-adhesive and strain-sensitive for flexible sensors.

Hydrogels as flexible sensor have attracted significant attention due to its conductivity, stretchability and flexibility. However, it is still a great challenge to prepare hydrogels that simultaneously possess high strength, anti-fatigue, self-adhesion, and anti-freezing. Herein, a multifunctional dual-network hydrogel was prepared by in situ polymerization of acrylic monomer in chitosan chains, and coordinated with aluminum chloride and glycerol.

SOAT1 is a new prognostic factor of colorectal cancer.

Colorectal cancer (CRC) is one of the most common malignant gastrointestinal cancers. Metastasis is the major leading cause of death in patients with CRC, and many patients treated with radical surgery were diagnosed with metastasis during follow-up. However, the underlying molecular mechanisms regulating CRC metastasis are still elusive.

Prediction of Peking duck intramuscle fat content by near-infrared spectroscopy.

Peking duck is the most representative of the meat-type duck breed, and it is also one of the most popular meats in Asia. Few studies were reported on the fast assessment of duck meat quality. This study aimed to develop a fast measuring of duck fat content by using the near-infrared spectroscopy (NIRS) method.

Shaoyao-Gancao Decoction alleviated hyperandrogenism in a letrozole-induced rat model of polycystic ovary syndrome by inhibition of NF-κB activation.

Shaoyao-Gancao Decoction (SGD) has been widely used for the treatment of gynopathy. The present study aimed to evaluate the therapeutic effect and potential mechanism of SGD on hyperandrogenism in polycystic ovary syndrome (PCOS) rats. In the present work, SGD was orally administrated to the PCOS rats at the dose of 12.

Downregulation of S100A4 Alleviates Cardiac Fibrosis via Wnt/β -Catenin Pathway in Mice.

Background/aims: Cardiac fibrosis is a pathological change leading to cardiac remodeling during the progression of myocardial ischemic diseases, and its therapeutic strategy remains to be explored. S100A4, a calcium-binding protein, participates in fibrotic diseases with an unclear mechanism. This study aimed to investigate the role of S100A4 in cardiac fibrosis.

[Effect of Dracocephalum moldavica total flavones on expression of TGF-β1/Smad signaling pathway and matrix metalloproteinase of atherosclerosis ApoE-/- mice].

To investigate the effect and mechanism of Dracocephalum moldovica total flavones (TFDM) on the formation of atherosclerosis ApoE-/- mice induced by high fat diet. A total of 40 SPF 8-week-old male ApoE-/- mice were fed with high fat diet and randomly divided into 5 groups. TFDM high, medium, low-dose group were given 21, 42, 84 mg•kg⁻¹•d⁻¹ by gavage; Simvastatin group was fed with simvastatin 3.

Optimization modeling of single-chain antibody against hepatoma based on similarity algorithm.

The purposes was to establish optimal modeling of single-chain antibody molecules based on similarity algorithm and seek the connecting peptides that had the minimal effect on the structure and bioactivity of the variable region of heavy chain (VH) and that of light chain (VL) in a single-chain antibody against liver cancer. After the Linker with different lengths (n=0~7) had been added into single chain fragment variable (ScFv), modeling of the overall sequences of VH, VL and ScFv were conducted respectively. Meanwhile, the peptide chain structure of (Gly4Ser)n was adopted for the connecting peptide.

Efficacy of Albendazole-Chitosan Microsphere-based Treatment for Alveolar Echinococcosis in Mice.

This study aimed to investigate the pharmacology and anti-parasitic efficacy of albendazole-chitosan microspheres (ABZ-CS-MPs) for established intraperitoneal infections of Echinococcus multilocularis metacestodes in an experimental murine model. Male outbred Kunming mice infected with E. multilocularis Metacestodes were administered with three ABZ formulations, namely, ABZ-CS-MPs, Liposome-Albendazole (L-ABZ), and albendazole tablet (ABZ-T).

Quercetin reversed lipopolysaccharide-induced inhibition of osteoblast differentiation through the mitogen‑activated protein kinase pathway in MC3T3-E1 cells.

Quercetin, a flavonoid found in onions and other vegetables, has potential inhibitory effects on bone resorption in vivo and in vitro. In our previous study it was identified that quercetin triggered the apoptosis of lipopolysaccharide (LPS)‑induced osteoclasts and inhibited bone resorption. Currently, little information is available detailing the effect of quercetin on osteoblast differentiation and bone formation in bacteria‑induced inflammatory diseases.

[Efficacy of albendazole chitosan microspheres against Echinococcus granulosus infection in mice].

Objective: To observe the therapeutic effect of albendazole chitosan microspheres (ABZ-CS-MPs) on cystic echinococcosis in mice.

Methods: Two hundred male kunming mice were each infected by intraperitoneal inoculation of about 5 000 viable protoscoleces of Echinococcus granulosus. Another 20 mice were kept as blank control.

[Study on intestinal absorption of tilianin in rats of single-pass perfusion model].

Objective: To study the intestinal absorption mechanism of tilianin in rats.

Method: The single-pass perfusion model was established in rats. The concentrations of tilianin with in situ intestinal perfusion were determined by HPLC.

Effect of pomegranate peel polyphenol gel on cutaneous wound healing in alloxan-induced diabetic rats.

Background: Pomegranate (punica granatum) belongs to the family Punicaceae, and its peel has been used as a traditional Chinese medicine because of its efficacy in restraining intestine, promoting hemostasis, and killing parasites. Pomegranate peel has been reported to possess wound-healing properties which are mainly attributed to its polyphenol extracts. The purpose of this study was to investigate the effect of pomegranate peel polyphenols (PPP) gel on cutaneous wound healing in diabetic rats.

Changes in plasma angiotensin II and circadian rhythm of blood pressure in hypertensive patients with sleep apnea syndrome before and after treatment.

Objective: To explore the changes in plasma angiotensin II (Ang II) and circadian rhythm of blood pressure among hypertensive patients with sleep apnea syndrome (SAS) before and after continuous positive airway pressure (CPAP) or surgical treatment.

Methods: A total of 180 essential hypertension patients were enrolled in our study. The determination of plasma Ang II concentration, ambulatory blood pressure (ABP), and polysomnography (PSG) monitoring were performed before and 3 months after CPAP or surgical treatment.

[Circadian blood pressure variability and plasma neopterin level before and after surgery for obstructive sleep apnea syndrome].

Objective: To investigate the change of circadian blood pressure variability (BPV) and plasma neopterin before and after surgery (uvulopalatopharyngoplasty) for patients with obstructive sleep apnea syndrome (OSAS).

Methods: A total of 382 OSAS patients underwent uvulopalatopharyngoplasty were divided into three groups based on polysomnography (PSG) results: mild OSAS (n = 206), moderate OSAS (n = 108) and severe OSAS (n = 68). Plasma neopterin, 24-hour ambulatory blood pressure monitoring (ABPM), PSG were measured before and 3 months after surgery.

[Activation of nuclear factor-kappaB and aberrant gene expression of interleukin 6 in middle ear cholesteatoma].

Objective: To establish the activation of NF-kappaB in middle ear cholesteatoma, discuss the relationship of NF-kappaB and the gene expression of IL-6 and explore the pathogenesis of middle ear cholesteatoma.

Methods: Ten cases of cholesteatoma and 6 cases of normal external meatal skin were obtained from middle ear surgery. The NF-kappaB DNA binding activity and the mRNA level of IL-6 in these two kinds of tissues were detected by electrophoretic motility shift assay (EMSA) and Reverse transcription polymerase chain reaction (RT-PCR) respectively.

[Study on drug release in vitro and rat intestinal absorption of resveratrol nanoliposomes].

Objective: To study the release feature of Res-nanoliposomes in vitro and clarify the difference in absorption of Res-nanoliposomes from varied intestinal segments and the absorptive mechanism in vivo.

Method: Dialytic method was used to determine resveratrol release rate of Res-nanoliposomes in vitro. An in situ rat perfusion method was used to investigate the intestinal absorption of Res-nanoliposomes.

[Comparison of two preparation methods applied in tanshinone II(A)-loaded PLGA nanoparticles].

Objective: To optimize formulation of tanshinone II(A)-loaded PLGA nanoparticles and compare the difference of two methods in preparation and quality of nanoparticles.

Method: The two methods were nanoprecipitation method and emulsion-evaporation method. Single factor experiments and central composite design and response surface method were used to optimize the formulation of nanoparticles.

[Effect of endotoxemia on thyrotropin releasing hormone and its receptor in Wistar rat brain].

Objective: To study the dose and location of thyrotropin releasing hormone (TRH) and its receptor in Wistar rat's brain when early endotoxemia happened.

Methods: Twenty-two Wistar rats were selected. In 13 mouse the model was established with endotoxemia and hemorrhagic shock.

Effect of devazepide reversed antagonism of CCK-8 against morphine on electrical and mechanical activities of rat duodenum in vitro.

AIM:To study the antagonism of cholecystokinin octapeptide (CCK-8) against the effect of morphine and its mechanism.METHODS:The method of simultaneously recording the electrical and mechanical activities of rat duodenum in vitro was adopted.RESULTS:Acetylcholine (ACh) could increase the amplitude and the number of the spike potential (SPA and SPN of rat duodenum in vitro, followed by the increase of the duodenal contraction amplitudes (CA), showing a positive correlation.