Cardiotonic Pills Plus Recombinant Human Prourokinase Ameliorates Atherosclerotic Lesions in LDLR Mice.

Aim: This study was to explore the protective effects of cardiotonic pills (CP) or/and recombinant human prourokinase (proUK)on the atherosclerosis and the potential underlying mechanism.

Methods And Results: Atherosclerosis was induced in LDLR/ mice by high fat diet contained 20% lard and 0.5% cholesterol.

Organocatalytic Reaction of Chromone-Oxindole Synthon: Access to Chromanone-Based Spirocyclohexaneoxindoles with Five Adjacent Stereocenters.

An efficient strategy for stereo-controlled synthesis of potential biological and structurally complex chromanone-based spirocyclohexaneoxindoles via an organocatalytic domino formal double Michael cycloaddition of bifunctional chromone-oxindole synthons and nitroolefins is reported. These products possessing five adjacent stereocenters including one spiro quaternary carbon center, were smoothly afforded in up to 85% yield, >99% ee, and >20:1 dr. This strategy benefits from the intramolecular nature of the second Michael reaction step, through counterbalancing the lower electrophilicity of these unactivated chromones to facilitate the reaction.

[Heiguteng Zhuifenghuoluo capsule inhibits the expression of NF-κB in synovial tissues of rats with collagen-induced arthritis and alleviates joint inflammation].

Objective To investigate the effect of Heiguteng Zhuifenghuoluo Capsule (HZC) on nuclear factor kappa B (NF-κB)-related protein in rheumatoid arthritis rats, and to analyze the expression of IκBα, NF-κBp65, phospho-nuclear factor kappa B p65 (p-NF-κBp65), receptor activator of nuclear factor κB ligand (RANKL), transforming growth factor activated kinase 1(TAK1), transforming growth factor β activated kinase binding protein 1(TAB1), monocyte chemoattractant protein 1 (MCP-1), C-X-C motif chemokine ligand 1 (CXCL1), macrophage inflammatory protein-1 (MIP-1) of plasma in rheumatoid arthritis rats. Methods Male SD rats were randomly divided into control group, model group, HZC (0.315 g/kg) group, and HZC (0.

Stereocontrolled Synthesis of Bispirooxindole-Based Hexahydroxanthones with Five Contiguous Stereocenters.

A bifunctional oxindole-chromone synthon 1 directed tandem reaction is developed, serving as a fruitful strategy for facile access to optically active hexahydroxanthones 3 bearing two spirooxindoles with five contiguous stereocenters. All of the bispirooxindole-based hexahydroxanthones 3 are smoothly obtained with up to 91% yield, >20:1 dr, and >99% ee. Biological evaluation of selected compounds 3 revealed that they exerted good cytotoxic effects on human K562, A549, and PC-3 cells.

Genomic Characterization of a New HIV-1 CRF01_AE/CRF07_BC Recombinant Virus Form in Guizhou in Southwest China.

A novel HIV-1 second-generation recombinant form (CRF01_AE/CRF07_BC) was isolated from an HIV-positive subject among men who have sex with men (MSM) in Guizhou province in Southwest China. Recombinant analyses of the near full-length genome suggested that the strain was composed of CRF01_AE and CRF07_BC with one region of CRF07-BC inserted into a CRF01-AE backbone. Further analysis indicated that the CRF01_AE regions of the recombinant were highly clustered together with a subcluster 4 lineage of CRF01_AE, which is exclusively circulating among MSM in China.

Chemical composition, antioxidant, antimicrobial and anticancer activities of the essential oil from the rhizomes of Diels.

The chemical composition and biological activities of the essential oil (EO) from the rhizomes of Diels were reported for the first time. Forty-five compounds were identified, and represented 95.7% of the total composition of the EO.

Palladium-Catalyzed Highly Enantioselective Cycloaddition of Vinyl Cyclopropanes with Imines.

Palladium-catalyzed asymmetric formal [3 + 2] cycloaddition of vinyl cyclopropanes and aldimines or isatin-derived ketimines proceeded smoothly in the presence of chiral phosphoramidite ligands. The corresponding highly functionalized and optically enriched pyrrolidine or spiro[pyrrolidin-3,2'-oxindole] derivatives are obtained in up to 94% yield and with up to 96% ee and 7:1 dr.

Mechanisms of Zuogui Pill in Treating Osteoporosis: Perspective from Bone Marrow Mesenchymal Stem Cells.

The current treatment strategies for osteoporosis (OP) involve promoting osteogenic differentiation and inhibiting adipogenic differentiation of bone marrow mesenchymal stem cells (BMSCs). According to a theory of traditional Chinese medicine (TCM), the kidneys contain an "essence" that regulate bone metabolism and generate marrow. Kidney disorders are therefore considered to be a major cause of OP as per the principles of TCM, which recommends kidney-tonifying treatments for OP.

Sanggenon C Stimulates Osteoblastic Proliferation and Differentiation, Inhibits Osteoclastic Resorption, and Ameliorates Prednisone-Induced Osteoporosis in Zebrafish Model.

Sanggenon C (SC), which is a natural flavonoid found in the stem bark of Cortex Mori, has been discovered to have the antioxidant, anti-inflammatory, and antitumor properties. However, its effect in osteoporosis has not yet been reported. In this research, the effect of SC on the proliferation of MC3T3-E1 cells was evaluated by using the MTT assay.

Design, Synthesis, and Biological Evaluation of Pyrimido[4,5- d]pyrimidine-2,4(1 H,3 H)-diones as Potent and Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors against L858R/T790M Resistance Mutation.

First-generation epidermal growth factor receptor (EGFR) inhibitors, gefitinib and erlotinib, have achieved initially marked clinical efficacy for nonsmall cell lung cancer (NSCLC) patients with EGFR activating mutations. However, their clinical benefit was limited by the emergence of acquired resistance mutations. In most cases (approximately 60%), the resistance was caused by the secondary EGFR T790M gatekeeper mutation.