Palladium-catalyzed three-component radical-polar crossover carboamination of 1,3-dienes or allenes with diazo esters and amines.

Herein, we report a visible-light-mediated palladium-catalyzed three-component radical-polar crossover carboamination of 1,3-dienes or allenes with diazo esters and amines, affording unsaturated γ- and ε-amino acid derivatives with diverse structures. In this methodology, the diazo compound readily transforms into a hybrid α-ester alkylpalladium radical with the release of dinitrogen. The radical intermediate selectively adds to the double bond of a 1,3-diene or allene, followed by the allylpalladium radical-polar crossover path and selective allylic substitution with the amine substrate, thereby leading to a single unsaturated γ- or ε-amino acid derivative.

Stimuli-responsive rotaxane-branched dendronized polymers with tunable thermal and rheological properties.

Aiming at the creation of polymers with attractive dynamic properties, herein, rotaxane-branched dendronized polymers (DPs) with rotaxane-branched dendrons attached onto the polymer chains are proposed. Starting from macromonomers with both rotaxane-branched dendrons and polymerization site, targeted rotaxane-branched DPs are successfully synthesized through ring-opening metathesis polymerization (ROMP). Interestingly, due to the existence of multiple switchable [2]rotaxane branches within the attached dendrons, anion-induced reversible thickness modulation of the resultant rotaxane-branched DPs is achieved, which further lead to tunable thermal and rheological properties, making them attractive platform for the construction of smart polymeric materials.

Photoredox-Catalyzed Carbonyl Alkylative Amination with Diazo Compounds: A Three-Component Reaction for the Construction of γ-Amino Acid Derivatives.

A photoredox-catalyzed reaction of secondary amines, aldehydes, diazo compounds, and Hantzsch ester is reported, affording biologically active γ-amino acid derivatives in high yields. This one-pot process tolerates a broad range of functional groups and various drug molecules and biologically active compounds. Remarkably, a gram-scale reaction and diverse transformations of γ-amino acid derivatives were successfully performed, and the utility of the products is demonstrated in the synthesis of therapeutic agent pregabalin.

Polymer Topology Reinforced Synergistic Interactions among Nanoscale Molecular Clusters for Impact Resistance with Facile Processability and Recoverability.

The intrinsic conflicts between mechanical performances and processability are main challenges to develop cost-effective impact-resistant materials from polymers and their composites. Herein, polyhedral oligomeric silsesquioxanes (POSSs) are integrated as side chains to the polymer backbones. The one-dimension (1D) rigid topology imposes strong space confinements to realize synergistic interactions among POSS units, reinforcing the correlations among polymer chains.

Unexpected Elasticity in Assemblies of Glassy Supra-Nanoparticle Clusters.

Granular materials, composed of densely packed particles, are known to possess unique mechanical properties that are highly dependent on the surface structure of the particles. A microscopic understanding of the structure-property relationship in these systems remains unclear. Here, supra-nanoparticle clusters (SNPCs) with precise structures are developed as model systems to elucidate the unexpected elastic behaviors.

Radical-Mediated Strategies for the Functionalization of Alkenes with Diazo Compounds.

One of the most common reactions of diazo compounds with alkenes is cyclopropanation, which occurs through metal carbene or free carbene intermediates. Alternative functionalization of alkenes with diazo compounds is limited, and a methodology for the addition of the elements of Z-CHR (with Z = H or heteroatom, and CHR originates from N═CR) across a carbon-carbon double bond has not been reported. Here we report a novel reaction of diazo compounds utilizing a radical-mediated addition strategy to achieve difunctionalization of diverse alkenes.

Lasso Proteins: Modular Design, Cellular Synthesis, and Topological Transformation.

Entangled proteins have attracted significant research interest. Herein, we report the first rationally designed lasso proteins, or protein [1]rotaxanes, by using a p53dim-entwined dimer for intramolecular entanglement and a SpyTag-SpyCatcher reaction for side-chain ring closure. The lasso structures were confirmed by proteolytic digestion, mutation, NMR spectrometry, and controlled ligation.

Relationship between Tissue Distributions of Modified Wuzi Yanzong Prescription () in Rats and Meridian Tropism Theory.

Objective: To investigate the relationship between tissue distributions of modified Wuzi Yanzong prescription (, MWP) in rats and meridian tropism theory.

Methods: A high-performance liquid chromatography with Fourier transform-mass spectrometry (HPLC-FT) method was used to identify the metabolites of MWP in different tissues of rats after continued oral administration of MWP for 7 days. The relationship between MWP and meridian tropism theory was studied according to the tissue distributions of the metabolites of MWP in rats and the relevant literature.

[Study of effect of Humifuse Euphorbia Herb on alleviating insulin resistance in type 2 diabetic model KK-Ay mice].

[To explore the effect of Humifuse Euphorbia Herb ( HEH) on alleviating insulin resistance in type 2 diabetic KK-Ay mice. Totally 40 KK-Ay mice fed with high-fat diet were divided into four groups: the metformin group, the model group, the HEH low-dose group and the HEH high-dose group, and orally administrated with metformin hydrochloride (250 mg x kg(-1)), distilled water, humifuse euphorbia herb 1 g x kg(-1) and 2 g x kg(-1). Besides, C57BL/6J mice with ordinary feed were taken as the normal control group and orally administrated with equal distilled water.

Schisandrin B exerts anti-neuroinflammatory activity by inhibiting the Toll-like receptor 4-dependent MyD88/IKK/NF-κB signaling pathway in lipopolysaccharide-induced microglia.

Microglial-mediated neuroinflammation is now considered to be central to the pathogenesis of various neurodegenerative processes, including Alzheimer's disease and Parkinson's disease. Therefore, rational modulation of microglia function to obtain neuroprotective effects is important for the development of safe and effective anti-inflammatory and neuroprotective agents. Here, we investigated the anti-inflammatory and neuroprotective effects, and potential molecular mechanism of action of Schisandrin B (Sch B); which is isolated from the Schizandra fruit (Schisandra chinesnesis).

Aluminum maltolate induces primary rat astrocyte apoptosis via overactivation of the class III PI3K/Beclin 1-dependent autophagy signal.

Aluminum-induced neuronal cell apoptosis has been implicated in various neurodegenerative disorders. However, whether autophagy, a vital lysosomal degradation pathway, is involved in this pathogenesis still remains unknown. Our present findings demonstrated that aluminum significantly increased rat astrocyte apoptosis and autophagy levels in a dose-dependent manner.

Modified Wu-Zi-Yan-Zong prescription, a traditional Chinese polyherbal formula, suppresses lipopolysaccharide-induced neuroinflammatory processes in rat astrocytes via NF-κB and JNK/p38 MAPK signaling pathways.

Neuroinflammation plays an important role in several neurodegenerative diseases. In this study, we investigated the anti-inflammatory properties of modified Wu-Zi-Yan-Zong prescription (MWP), a traditional Chinese polyherbal formula, in primary cultured rat astrocytes treated with lipopolysaccharide (LPS). The results showed that MWP significantly inhibited release of nitric oxide (NO) and prostaglandin E (PGE), as well as expressions of inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 in LPS-induced rat astrocytes.

A randomized double-blind placebo-controlled study of Pu'er tea extract on the regulation of metabolic syndrome.

Objective: To explore the regulative efficacy of Pu'er tea () extract on metabolic syndrome.

Methods: Ninety patients with metabolic syndrome were randomly divided into two groups, the intervention group administered with Pu'er tea extract, and the placebo group with placebo capsules. After 3 months' treatment, body mass index, waist hip ratio, blood lipids, blood sugar, immune and inflammatory index, and oxidation index of the patients with metabolic syndrome were tested and analyzed.

Icariin attenuates lipopolysaccharide-induced microglial activation and resultant death of neurons by inhibiting TAK1/IKK/NF-kappaB and JNK/p38 MAPK pathways.

Microglia in the central nervous system (CNS) play an important role in the initiation of neuroinflammatory response. Icariin, a compound from Epimedium brevicornum Maxim, has been reported to have anti-inflammatory effect on the macrophage cell line RAW264.7.

Protective effects of Wu-Zi-Yan-Zong-Fang on amyloid beta-induced damage in vivo and in vitro.

This study was designed to determine the effects of Wu-Zi-Yan-Zong-Fang on amyloid-beta(25-35)-induced cognitive deficits in rats and neurotoxicity in pheochromocytoma cells and the possible mechanism of action. In vivo studies showed that Wu-Zi-Yan-Zong-Fang significantly ameliorated the spatial memory and retention deficits, decreased acetylcholinesterase activity, and increased acetylcholine content caused by intracerebroventricular injection of amyloid-beta(25-35). In vitro results showed that Wu-Zi-Yan-Zong-Fang increased cell viability and the activity of superoxide dismutase and catalase and decreased the release of lactate dehydrogenase and the level of malondialdehyde.

Effect of modified wuzi yanzong granule on patients with mild cognitive impairment from oxidative damage aspect.

Objective: To observe the effects of modified Wuzi Yanzong Granule (WYG) on memory function and the activity of serum superoxide dismutase (SOD), malondialdehyde (MDA) levels, leukocyte mitochondrial DNA (mtDNA) deletion rate and beta-amyloid protein(1-28) (A beta(1-28)) in patients with mild cognitive impairment (MCI).

Methods: Thirty-six patients with MCI were selected based on the internationally recognized Petersen's criteria, and equally and randomly assigned to two groups. The treated group was treated with WYG and the control group was treated with placebo for 3 months.

[Study on anti-tumor effect of dry and fresh Gekko swinhonis freeze-dried powders on mice sarcoma S180 and acute toxicity testing of two powders].

Objective: To investigate the anti-tumor activity of dry Gekko swinhonis freeze-dried powder (DGFP) and fresh G. swinhonis freeze-dried powder (FGFP) on mice sarcoma S180 and acute toxicity testing of the two powders.

Method: Mice xenotransplant model of sarcoma S180 was established.

[Effects of modified Wuzi Yanzong Granule on memory ability and volume of hippocampus measured by MRI in patients with mild cognitive impairment].

Objective: To observe the effect of modified Wuzi Yanzong Granule (WYG) on memory ability and volume of hippocampus measured by magnetic resonance imaging (MRI) in patients with mild cognitive impairment (MCI).

Methods: According to the international accepted diagnostic criteria, 36 MCI patients were selected and randomly assigned to two groups equally, the treated group treated with WYG and the control group with placebo, with a course of 3 months for both groups. Besides, 20 healthy subjects were selected as the normal group.

[Clinical study on treatment of mild cognitive impairment by modified wuzi yanzong granule].

Objective: To observe the clinical efficacy and safety of modified Wuzi Yanzong Granule (MWYG) in treating mild cognitive impairment (MCI), and to explore its mechanism.

Methods: Forty-four MCI patients were selected referring to the international recognized Peterson's criteria and randomly divided into two groups, the treated group treated with MWYG and the control group treated with Ginkgo leaf extraction, with the course of 3 months for both groups. Changes of memorial quotient (MQ), superoxide dismutase (SOD) activity, malondialdehyde (MDA) content, mitochondrial DNA (mtDNA) deletion rate and acetylcholinesterase (AchE) before and after treatment were observed.

[Effect of wuzi yanzong Pill on mitochondrial DNA deletion and respiratory chain enzyme complex activity in peripheral leukocyte of aged male with kidney deficiency syndrome].

Objective: To investigate the effect of Wuzi Yanzong Pill (WZYZP) on mitochondrial DNA (mtDNA) deletion and respiratory chain enzyme complex (RCZC) in peripheral blood leukocyte of aged male with Kidney Deficiency Syndrome (KDS).

Methods: Single-blinded study was conducted in 38 aged male with KDS, who were randomly divided into 2 groups treated with WZYZP and placebo respectively for 3 months. Levels of mtDNA deletion and RCZC were determined by polymerase chain reaction (PCR) and enzyme kinetics technique respectively.