An asymmetric cyclization reaction of azadienes and azlactones was investigated by employing a Cinchona squaramide catalyst, which could afford series benzofuran-fused six-membered heterocycles containing α,α-disubstituted amino acid unit in highly diastereoselective (>20:1 dr) enantioselective (up to 99% ee) manner with good excellent yields 92%). A plausible pathway proposed explain the process.

Reported herein is an inverse-electron-demand oxa-Diels-Alder reaction that remotely β,γ-regioselective with β,γ-unsaturated amides and β,γ-unsaturated-α-ketoesters using a bifunctional catalyst. It can provide different kinds of dihydropyrans bearing three subsequent chiral carbon centers in good to high yield (61-99%) complete enantioselectivity (99 >99% ee). Furthermore, larger-scale experiment confirmed the reliability current reaction, further effective transformation product has been realized.

A vinylogous addition–cyclization reaction of cyclic α-amide enones with good yields and excellent regioselectivity catalyzed by cinchona squaramides has been reported. Using 4-aryl-3-butenyl N-acylpyrazoles as nucleophiles led to 1,4-selective γ-addition enones, 1,2-selective took place when 3-aryl-3-butenyl was used the donors. The 1,4- γ-adducts are then formed into corresponding highly stereoselective enantioselective fused bicyclic spirocyclic products intramolecular cyclization....

Microglia hyperactivation is an important cause of neuroinflammation in Alzheimer's disease (AD). Paeoniflorin (PF), ferulic acid (FA), and atractylenolide III (ATL) are potent anti-inflammation neuroprotection. Multiple components can act on different targets simultaneously to exert synergistic therapeutic effects exploring the potential between compounds area research. We investigated PF, FA, ATL, alone or combination, LPS-induced autophagy BV2 microglia cells. found that significantly...

The dried parts of medicinal herbs are susceptible to the infection fungi during pre- or post-harvest procedure. This study aimed investigate presence and their metabolites mycotoxins on surface collected from China. Forty-five retail samples 15 different were 3 regions in Then potential immediately washed off each sample with 0.1% Tween-20 followed by incubation rinse petri-dish potato dextrose agar containing chloramphenicol at 28 °C. obtained isolated as single colonies then characterized...

The construction of cyclobutanes has attracted much attention because its unique four-membered ring skeleton. Herein, we report the highly enantioselective direct vinylogous Michael reaction β,γ-unsaturated pyrazole amides and nitroolefin using a squaramide catalyst. Cyclobutane derivatives were obtained by subsequent cyclization in good yields (up to 85%) with excellent enantioselectivities 99% ee). Importantly, large-scale experiment confirmed reliability reaction. Furthermore, synthetic...

Palmatine (PAL) is an isoquinoline alkaloid derived from Fibraureae caulis Pierre that has been used to relieve inflammatory diseases like ulcerative colitis (UC). The metabolites of PAL were believed contribute significantly its outstanding biological activities. 8-Oxypalmatine (OPAL), a liver-mediated oxidative metabolite PAL, firstly identified in the present work. We aimed comparatively investigate potential effect and mechanism OPAL on dextran sodium sulfate (DSS)-induced Balb/c mice....

Rubia cordifolia L. (Rubiaceae), one of the traditional anti-rheumatic herbal medicines in China, has been used to treat rheumatoid arthritis (RA) since ancient times. Purpurin, an active compound L., identified previous studies and exerts antibacterial, antigenotoxic, anticancer, antioxidant effects. However, efficacy underlying mechanism purpurin alleviate RA are unclear. In this study, effect on inflammation was investigated using macrophage RAW264.7 inflammatory cells, induced by...

Novel construction methods for obtaining 3,4'-pyran spirooxindole heterocyclic skeletons have always been the focus of attention. Herein, we report a highly enantioselective inverse-electron-demand oxa-Diels-Alder cycloaddition reaction β,γ-unsaturated pyrazole amide and

The present work provides a simple and efficient access to chiral pyrano[2,3-<italic>c</italic>]pyrrole<italic>via</italic>an asymmetric [4 + 2] cyclization reaction catalyzed by cinchona-squaramide catalyst.

A highly enantioselective 1,4-addition reaction of azadiene with 3-homoacyl coumarin has been accomplished by low amounts bifunctional cinchona alkaloid catalysis under mild conditions. Varieties benzofuran skeletons were obtained in moderate to high yields (up 99%) excellent enantioselectivities 99% ee) and complete diastereoselectivity.

Farnesyl pyrophosphate synthase (FPPS) plays an important role in the synthesis of plant secondary metabolites, but its function and molecular regulation mechanism remain unclear Pogostemon cablin . In this study, full-length cDNA FPP gene from P. ( PcFPPS ) was cloned characterized. The expressions are different among tissues (highly flowers). Subcellular localization analysis protoplasts indicated that located cytoplasm. functionally complemented lethal FPPS deletion mutation yeast CC25....

Abstract A highly enantioselective organocatalytic Michael addition‐acetalation/oxa‐Michael reaction involving aldehydes and dioxopyrrolidines has been discovered. The asymmetric is mediated by modularly designed organocatalysts (MDOs) self‐assembled from cinchona alkaloid derivatives amino acids providing a range of optically active tricyclic hexahydro‐2 H ‐pyrano[3′,2′:5,6]pyrano[2,3‐ c ]pyrrol in high yields (up to 99%) with good excellent enantioselectivities 99% ee) under mild...

The process of radical decarboxylation is crucial in organic synthesis. Nevertheless, dienoic acids presents a greater challenge compared to that aliphatic carboxylic acids. Herein, catalyst- and additive-free visible-light-promoted [4 + 3] annulation lactones diamines was achieved via By means this novel EDA-activated annulation, the 1,5-benzodiazepines, which display wide range biological activities are widely used many fields, can be directly accessed high yields under mild conditions....

Paclitaxel (PTX) is a famous anti-cancer drug with poor aqueous solubility. In clinical practices, Cremophor EL (polyethoxylated castor oil), toxic surfactant, used for dissolution of PTX, which accounts serious side effects. the present study, single glucose-conjugated PTX prodrug (SG-PTX) and double (DG-PTX) were synthesized glycosylated strategy via succinate linkers. Both two prodrugs presented significant solubility improvement drug-like lipophilicities. Compared to DG-PTX, SG-PTX...

Skimmianine is a furoquinoline alkaloid present mainly in the Rutaceae family. It has been reported to have analgesic, antispastic, sedative, anti-inflammatory, and other pharmacologic activities. Despite its critical pharmacological function, metabolite profiling still unclear. In this study, vivo of skimmianine rats was investigated using ultra-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry (UPLC/Q-TOF-MS). The metabolites were predicted...

Zanthoxylum nitidum (Roxb.) DC (Rutaceae), called as "liangmianzhen" in China, is well known for its anti-inflammation and analgesic effect. Alkaloids are main active constituents. However, little has been about the absorption of alkaloids vivo. In this study, an ultra-performance liquid chromatography coupled with quadrupole-time-of-flight mass spectrometry was employed identification absorbed rats after oral administration Z. decoction. By analyzing fragmentation patterns, a total nineteen...

This study aimed to develop a method, followed by gas chromatography-mass spectrometry, for detecting 37 pesticides in Chrysanthemum indicum (C. indicum) and investigating the decrease matrix-induced enhancement effect. The influence of QuEChERS extraction matrix solid-phase dispersion (MSPD) on recovery effect (ME) was compared. compared ME. cleanup sorbents, volume type solvent, treatment time were optimized. accuracy (as recovery), precision relative standard deviation, RSD), linearity,...

Alzheimer's disease (AD) is a neurodegenerative brain disorder that progressively impairs long-term and working memory. The function mechanism of PA(Patchouli alcohol) in improving AD the external treatment encephalopathy remain unclear. This study aimed to investigate therapeutic effect PA on using an Aβ