General Synthesis of <i>meso</i>-1,4-Dialdehydes and Their Application in Ir-Catalyzed Asymmetric Tishchenko Reactions

A practical synthesis of meso-1,4-dialdehydes based on the oxidative cleavage of cyclobutanediol derivatives using polymer-supported periodate was developed. The meso-1,4-dialdehydes were obtained in up to >99% yield and subsequently employed in Ir-catalyzed asymmetric Tishchenko reactions to give the corresponding chiral lactones, which are versatile synthetic intermediates, in good yield with moderate enantiomeric excess. The catalytically active species was identified by means of cold-spray ionization mass spectrometry and 1H NMR spectroscopy

General Synthesis of <i>meso</i>-1,4-Dialdehydes and Their Application in Ir-Catalyzed Asymmetric Tishchenko Reactions

A practical synthesis of meso-1,4-dialdehydes based on the oxidative cleavage of cyclobutanediol derivatives using polymer-supported periodate was developed. The meso-1,4-dialdehydes were obtained in up to >99% yield and subsequently employed in Ir-catalyzed asymmetric Tishchenko reactions to give the corresponding chiral lactones, which are versatile synthetic intermediates, in good yield with moderate enantiomeric excess. The catalytically active species was identified by means of cold-spray ionization mass spectrometry and 1H NMR spectroscopy

General Synthesis of <i>meso</i>-1,4-Dialdehydes and Their Application in Ir-Catalyzed Asymmetric Tishchenko Reactions

A practical synthesis of meso-1,4-dialdehydes based on the oxidative cleavage of cyclobutanediol derivatives using polymer-supported periodate was developed. The meso-1,4-dialdehydes were obtained in up to >99% yield and subsequently employed in Ir-catalyzed asymmetric Tishchenko reactions to give the corresponding chiral lactones, which are versatile synthetic intermediates, in good yield with moderate enantiomeric excess. The catalytically active species was identified by means of cold-spray ionization mass spectrometry and 1H NMR spectroscopy

General Synthesis of <i>meso</i>-1,4-Dialdehydes and Their Application in Ir-Catalyzed Asymmetric Tishchenko Reactions

A practical synthesis of meso-1,4-dialdehydes based on the oxidative cleavage of cyclobutanediol derivatives using polymer-supported periodate was developed. The meso-1,4-dialdehydes were obtained in up to >99% yield and subsequently employed in Ir-catalyzed asymmetric Tishchenko reactions to give the corresponding chiral lactones, which are versatile synthetic intermediates, in good yield with moderate enantiomeric excess. The catalytically active species was identified by means of cold-spray ionization mass spectrometry and 1H NMR spectroscopy

General Synthesis of <i>meso</i>-1,4-Dialdehydes and Their Application in Ir-Catalyzed Asymmetric Tishchenko Reactions

A practical synthesis of meso-1,4-dialdehydes based on the oxidative cleavage of cyclobutanediol derivatives using polymer-supported periodate was developed. The meso-1,4-dialdehydes were obtained in up to >99% yield and subsequently employed in Ir-catalyzed asymmetric Tishchenko reactions to give the corresponding chiral lactones, which are versatile synthetic intermediates, in good yield with moderate enantiomeric excess. The catalytically active species was identified by means of cold-spray ionization mass spectrometry and 1H NMR spectroscopy

Additional file 1: Figure S1. of Glutaminase-containing microvesicles from HIV-1-infected macrophages and immune-activated microglia induce neurotoxicity

MVs from HIV-1-infected MDM contain vesicular glutamate transporter. At 7 days post-infection, mock-infected and HIV-1 infected MDM were treated with GW4869 for 24 h in serum-free media. MVs were isolated from the supernatants and MV protein lysates were prepared. The levels of vesicular glutamate transporter were determined by Western blot. (TIFF 41 kb

A ROS-Responsive Simvastatin Nano-Prodrug and its Fibronectin-Targeted Co-Delivery System for Atherosclerosis Treatment

Nanoprodrugs with responsive release properties integrate the advantages of stimuli-responsive prodrugs and nanotechnology. They would provide ultimate opportunity in fighting atherosclerosis. In this study, we synthesized a redox-responsive nanoprodrug of simvastatin (TPTS) by conjugating α-tocopherol polyethylene glycol derivative to the pharmacophore of simvastatin with a thioketal linker. TPTS formed nanoparticles and released parent simvastatin in the presence of hydrogen peroxide. Moreover, by taking advantage of the self-assembly behavior of TPTS, we developed a fibronectin-targeted delivery system (TPTS/C/T) to codelivery simvastatin prodrug and ticagrelor. In vitro and in vivo experiments indicated that TPTS and TPTS/C/T had good stability, which could reduce off-target leakage of drugs. They greatly inhibited the M1-type polarization of macrophages; reduced intracellular reactive oxygen species level and inflammatory cytokine; and TNF-α, MCP-1, and IL-1β were secreted by macrophage cells, thus providing enhanced anti-inflammatory and antioxidant effects compared with free simvastatin. TPTS/C/T realized targeted drug release to plaques and synergistic therapeutic effects of simvastatin and ticagrelor on atherosclerosis treatment in an ApoE–/– mouse model, resulting in excellent atherosclerosis therapeutic efficacy and a promising biosafety profile. Therefore, this study provides a new method for manufacturing statin nanodrugs and a new design idea for related responsive drug release nanosystems for atherosclerosis

Additional file 2: Figure S2. of Glutaminase-containing microvesicles from HIV-1-infected macrophages and immune-activated microglia induce neurotoxicity

HIV-1-infected macrophages induce neurotoxicity through GLS1-containing MVs. (A-F) At 7 days post-infection, mock-infected and HIV-1 infected macrophages were treated with GW4869 at different dosages for 24 h. Cell-free supernatants were collected and added to RCN cultures for neurotoxicity. DMSO was used as solvent control for GW4869. Neurotoxic potentials of the supernatants were determined by MAP2 fluorescent staining. Results are representative of 20 fluorescent images from three independent experiments. (TIFF 523 kb

Additional file 1: of Glutaminase 1 regulates the release of extracellular vesicles during neuroinflammation through key metabolic intermediate alpha-ketoglutarate

Figures S1. Both KGA and GAC are successfully overexpressed by adenovirus in vitro. S2: EV release in HIV-1-infected macrophages is dependent on glutamine. S3: LPS, BPTES, and CB839 do not affect BV2 cell viability. (DOCX 6796 kb