Nucleophilic Catalysis of <i>MeON</i>-Neoglycoside Formation by Aniline Derivatives

Neoglycosylations are increasingly being employed in the synthesis of natural products, drug candidates, glycopeptide mimics, oligosaccharide analogues, and other applications, but the efficiency of these reactions is usually limited by slow reaction times. Here, we show that aniline derivatives such as 2-amino-5-methoxybenzoic acid enhance the rate of acid-catalyzed neoglycosylation for a range of sugar substrates up to a factor of 32 relative to the uncatalyzed reaction

Additional file 4: of M1-like tumor-associated macrophages activated by exosome-transferred THBS1 promote malignant migration in oral squamous cell carcinoma

Control images for the Chromogenic double staining with CD80 (pink)/CD68 (brown) in primary OSCC samples. Sections stained for hematoxylin were used as negative control. Sections stained with CD68 were used as single-positive control. (DOCX 557 kb

Additional file 1: of M1-like tumor-associated macrophages activated by exosome-transferred THBS1 promote malignant migration in oral squamous cell carcinoma

Heat-map indication of the densitometry values detected using the PathScan Immune Cell Signaling Antibody Array Kit. Colors illustrate fold changes (see color scale). Red: up-regulation; green: down-regulation. (DOCX 276 kb

Additional file 3: of M1-like tumor-associated macrophages activated by exosome-transferred THBS1 promote malignant migration in oral squamous cell carcinoma

Negative control for tracing exosome uptake by macrophages. Cultured macrophages were fixed, permeabilized, and stained with Acti-stain™ 488-Phalloidin and DAPI. Then, these macrophages were examined under confocal microscope. No red signals were captured in macrophages with an excitation at 460 nm without the incubation of labelled exosomes. (DOCX 240 kb

Additional file 2: of M1-like tumor-associated macrophages activated by exosome-transferred THBS1 promote malignant migration in oral squamous cell carcinoma

Validation of THBS1 knockdown in SCC25 and Cal27 cells. A. Relative mRNA expression of THBS1 in SCC25 and Cal27 after THBS1 knockdown (Scrambled as control), as determined by quantitative real-time PCR. Data are represented as the mean ± SD of three independent experiments, **p < 0.01. B. Relative protein expression of THBS1 in SCC25 and Cal27 after knockdown of THBS1 (Scrambled as control), as determined by Western blotting. Data are represented as the mean ± SD of three independent experiments, **p < 0.01. C. Expression level of THBS1 in CM of SCC25 and Cal27 after THBS1 knockdown (Scrambled as control), as determined by ELISA assays, **p < 0.01. D. Expression level of THBS1 in exosome supernatants of SCC25 and Cal27 cells after THBS1 knockdown (Scrambled as control), as determined by ELISA assays, **p < 0.01. (DOCX 199 kb

Anticonvulsant effects of B2 on strychnine-induced seizures in mice.

<p>(A) The latency of seizure onset was measured. Each column represents the mean ± S.E.M. (n = 7–8). ^*<i>P</i><0.05, ^**<i>P</i><0.01 and ^***<i>P</i><0.001, compared with the control group (one-way ANOVA followed by Newman Keuls post-test). (B) The mortality rate in each treatment group is shown as a percentage. ^*<i>P</i><0.05 compared with the control group (Fisher’s exact test).</p

Coamorphous Lurasidone Hydrochloride–Saccharin with Charge-Assisted Hydrogen Bonding Interaction Shows Improved Physical Stability and Enhanced Dissolution with pH-Independent Solubility Behavior

Recently, coamorphous systems, composed of a drug and a guest molecule, have gained increasing interest, due to their ability to overcome limitations associated with amorphous drug alone. In this study, a single-phase coamorphous form of lurasidone hydrochloride (LH) (a water-insoluble atypical antipsychotic agent with pH-dependent solubility) with saccharin (SAC) in a 1:1 molar ratio was obtained and characterized by differential scanning calorimetry and powder X-ray diffraction. Peak shifts in the Fourier transform infrared spectra indicated the formation of charge-assisted hydrogen bonds between the N⁺-H group of LH and the CO group of SAC. In comparison to crystalline LH, amorphous LH showed similar solubility and temporary improvement in the intrinsic dissolution rate and supersaturated dissolution, while coamorphous LH-SAC exhibited greatly improved solubility with pH-independent solubility behavior in a pH range of 2–5.5, as well as a persistent enhanced intrinsic dissolution rate and supersaturated dissolution. In addition, coamorphous LH-SAC showed superior physical stability compared to amorphous LH under the long-term storage condition. The coamorphization effect and charge-assisted hydrogen bond in coamorphous LH-SAC were speculated to be responsible for the above phenomena by prohibiting the recrystallization of LH

Anticonvulsant effects of B2 on KA-induced seizures in mice.

<p>The seizure score was recorded for each treatment group.</p

SCH58261 pretreatment had no effect on the anticonvulsant activity of B2.

<p>Each column represents the mean ± S.E.M. (n = 8–9). ^*<i>P</i><0.05 compared with the control group (Student’s <i>t</i>-test), ^#<i>P</i><0.05 compared with the B2 group (Newman Keuls post-test).</p

Antagonistic effects of DPCPX on the anticonvulsant activity of B2.

<p>Each column represents the mean ± S.E.M. (n = 9). ^*<i>P</i><0.05 compared with the control group (Student’s <i>t</i>-test), ^#<i>P</i><0.05 compared with the B2 group (Newman Keuls post-test).</p