Palladium-catalyzed decarboxylative α-allylation of thiazolidinones and azlactones with sulfonamido-substituted acyclic allylic carbonates.

A palladium-catalyzed decarboxylative α-allylation of thiazolidinones and azlactones with aza-π-allylpalladium zwitterionic intermediates, in situ generated from sulfonamido-substituted allylic carbonates, is successfully developed. This method allows the formation of a series of structurally diverse 5-alkylated thiazolidinones and 2-piperidones under mild conditions in moderate to high yields (up to 99% yield).

Impact of Oat (Avena sativa L.) on Metabolic Syndrome and Potential Physiological Mechanisms of Action: A Current Review.

Oat (Avena sativa L.), an annual herbaceous plant belonging to the Gramineae family, is widely grown in various regions including EU, Canada, America, Australia, etc. Due to the nutritional and pharmacological values, oats have been developed into various functional food including fermented beverage, noodle, cookie, etc. Meanwhile, numerous studies have demonstrated that oats may effectively improve metabolic syndrome, such as dyslipidemia, hyperglycemia, atherosclerosis, hypertension, and obesity. However, the systematic pharmacological mechanisms of oats on metabolic syndrome have not been fully revealed. Therefore, in order to fully explore the benefits of oat in food industry and clinic, this review aims to provide up-to-date information on oat and its constituents, focusing on the effects on metabolic syndrome.

Intra-articular delivery system of methotrexate for rheumatoid arthritis therapy: An in-suit thermosensitive comprehensive gel of polysaccharide from Aconitum carmichaelii Debx.

The polysaccharides (FP) extracted from the lateral roots of Aconitum carmichaelii Debx. (Fuzi) are natural compounds, which have effective therapy for rheumatoid arthritis (RA). Methotrexate (MTX) is the first-line drug for RA, but its application is greatly limited to the toxicity in liver and kidney and drug resistance. In this study, an attempt is made to apply oxidized FP (OFP) as a polymer carrier based on intra-articular delivery system loaded MTX. The FP could be modified and used as comprehensive gel carriers with biocompatibility and degradability for therapy of RA. Firstly, OFP-chitosan-poloxamer 407 in situ gel (OFP-CS-F407-MTX gel) was prepared by natural non-toxic cross-linking agents. Physicochemical characterization was performed by using 1H NMR and FTIR spectroscopic techniques to assess the successful functionalization of OFP. TGA, SEM and rheological experiment of OFP-CS-F407-MTX gel were investigated. Notably, we loaded MTX into OFP-CS-F407-MTX gel which had remarkable therapeutic efficacy and biosafety for RA. Therefore, OFP-CS-F407-MTX in situ gel delivery system can potentially reduce systemic toxicity and irritation of oral administration of MTX but hold a controlled release of drug for a long period of time.

Reconciling patterns of long-term topographic growth with coseismic uplift by synchronous duplex thrusting.

How long-term changes in surface topography relate to coseismic uplift is key to understanding the creation of high elevations along active mountain fronts, and remains hotly debated. Here we investigate this link by modeling the development of growth strata and the folding of river terraces above the Pishan duplex system in the southern Tarim Basin. We show that synchronous duplex thrusting of two neighboring faults with varying slip rates, associated with in-sequence propagation of the Pishan thrust system, is required to explain the presence of opposite-dipping panels of growth strata on the duplex front, and basinward migration of terrace fold crests. Importantly, this process of synchronous thrusting within the duplex reconciles the discrepancy between the deformation of terrace folds at the 10-1-100 million-year timescale and the maximum coseismic uplift of the 2015 Mw 6.4 Pishan earthquake on the frontal thrust. These results suggest that topography mismatch at different time scales can reflect the long-term kinematic evolution of fault systems. Thus, our study highlights the importance of characterizing complex subsurface fault kinematics for studying topographic growth, and motivates rethinking of the mountain building process in worldwide active fold-and-thrust belts, from short-term to long-term timescales.

South China Sea documents the transition from wide continental rift to continental break up.

During extension, the continental lithosphere thins and breaks up, forming either wide or narrow rifts depending on the thermo-mechanical state of the extending lithosphere. Wide continental rifts, which can reach 1,000 km across, have been extensively studied in the North American Cordillera and in the Aegean domain. Yet, the evolutionary process from wide continental rift to continental breakup remains enigmatic due to the lack of seismically resolvable data on the distal passive margin and an absence of onshore natural exposures. Here, we show that Eocene extension across the northern margin of the South China Sea records the transition between a wide continental rift and highly extended (<15 km) continental margin. On the basis of high-resolution seismic data, we document the presence of dome structures, a corrugated and grooved detachment fault, and subdetachment deformation involving crustal-scale nappe folds and magmatic intrusions, which are coeval with supradetachment basins. The thermal and mechanical weakening of this broad continental domain allowed for the formation of metamorphic core complexes, boudinage of the upper crust and exhumation of middle/lower crust through detachment faulting. The structural architecture of the northern South China Sea continental margin is strikingly similar to the broad continental rifts in the North American Cordillera and in the Aegean domain, and reflects the transition from wide rift to continental breakup.