Efficient and Practical Synthesis of Saflufenacil

Efficient and Practical Synthesis of Saflufenaci

A Novel Process for the Key Intermediate of Fluoroquinolones

A Novel Process for the Key Intermediate of Fluoroquinolone

Development of a New Manufacturing Route for Benzoylphenylureas and Their Key Intermediates

A new and efficient manufacturing technology is disclosed in the present work for the preparation of benzoylphenylureas and their key intermediates. This new route significantly reduces the number of reaction steps from six to three, resulting in a streamlined process. Additionally, the overall yield is increased from 56% to over 69%. Compared to the original process route, the new manufacturing route has the advantages of fewer chemical steps, higher overall yield, less process safety hazard and environmental impact. Considering these factors, the new manufacturing route exhibits considerable potential for industrialization.</p

Manipulating High-Valent Cobalt-Oxo Generation on Co/N Codoped Carbon Beads via PMS Activation for Micropollutants Degradation

Manipulating high-valent cobalt-oxo [Co(IV)O] species in a catalytic system is pivotal; however, it is challenging due to the inefficiency and unsustainability of Co(IV)O generation. In this study, we fabricated macroscopic porous Co/N codoped carbon beads (Co–NC) and identified Co(IV)O as the prominent species in peroxymonosulfate (PMS) activation. Specifically, Co(IV)O species on a Co–NC-900/PMS system was regarded as the crucial driver of tetracycline (TC) removal (with a degradation efficiency of 97.3% and an initial concentration of 20 mg L–1) through quenching experiments, methyl phenyl sulfoxide (PMSO) degradation, and methyl phenyl sulfone (PMSO2) generation. Importantly, Co–Nx active sites are responsible for the formation of Co(IV)O species, which contribute as much as 98.33% to TC degradation based on the calculation of the steady-state concentration. In addition, the relative contributions of Co(IV)O toward various micropollutants are substrate-specific and related to their ionization potential (IP). The practical application of Co–NC-900 was further evaluated in the continuous flow mode, and it showed excellent durability and performance. Overall, we have aroused the importance of Co(IV)O on micropollutants removal in heterogeneous systems and provided an alternative macroscopic catalyst that can be potentially exploited in real water decontamination scenarios

DataSheet2_WTAP mediates the anti-inflammatory effect of Astragalus mongholicus polysaccharide on THP-1 macrophages.docx

Background:Astragalus mongholicus polysaccharides (APS) have anti-inflammatory, antioxidant and immunomodulatory effects. Recent studies have demonstrated the epigenetic regulation of N6-methyladenosine (m6A) in the development of inflammation. However, the effect of APS on m6A modification is unclear. Here, for the first time, we investigate the mechanism of m6A modification in APS regulation of THP-1 macrophage inflammation.Methods: We treated LPS-induced THP-1 macrophages with APS at different concentrations and times, and detected IL-6 mRNA and protein levels by quantitative real-time PCR (qRT-PCR) and western blot, respectively. The m6A modification level was detected by m6A quantification kit. The proteins that regulate m6A modification were screened by western blot. Wilms’ tumor 1-associating protein (WTAP) was overexpressed in APS-treated THP-1 macrophages and the m6A modification level and IL-6 expressions were detected.Results: These findings confirmed that APS significantly abolished LPS-induced IL-6 levels in THP-1 macrophages. Meanwhile, APS reduced m6A modification levels and WTAP gene expression in THP-1 macrophages. Further overexpression of WTAP can significantly reverse APS-induced m6A modification level and IL-6 expression. Mechanistically, APS regulates IL-6 expression through WTAP-mediated p65 nuclear translocation.Conclusion: Overall, our study suggested that WTAP mediates the anti-inflammatory effect of APS by regulating m6A modification levels in THP-1 macrophages. This study reveals a new dimension of APS regulation of inflammation at the epigenetic level.</p

DataSheet1_WTAP mediates the anti-inflammatory effect of Astragalus mongholicus polysaccharide on THP-1 macrophages.docx

Background:Astragalus mongholicus polysaccharides (APS) have anti-inflammatory, antioxidant and immunomodulatory effects. Recent studies have demonstrated the epigenetic regulation of N6-methyladenosine (m6A) in the development of inflammation. However, the effect of APS on m6A modification is unclear. Here, for the first time, we investigate the mechanism of m6A modification in APS regulation of THP-1 macrophage inflammation.Methods: We treated LPS-induced THP-1 macrophages with APS at different concentrations and times, and detected IL-6 mRNA and protein levels by quantitative real-time PCR (qRT-PCR) and western blot, respectively. The m6A modification level was detected by m6A quantification kit. The proteins that regulate m6A modification were screened by western blot. Wilms’ tumor 1-associating protein (WTAP) was overexpressed in APS-treated THP-1 macrophages and the m6A modification level and IL-6 expressions were detected.Results: These findings confirmed that APS significantly abolished LPS-induced IL-6 levels in THP-1 macrophages. Meanwhile, APS reduced m6A modification levels and WTAP gene expression in THP-1 macrophages. Further overexpression of WTAP can significantly reverse APS-induced m6A modification level and IL-6 expression. Mechanistically, APS regulates IL-6 expression through WTAP-mediated p65 nuclear translocation.Conclusion: Overall, our study suggested that WTAP mediates the anti-inflammatory effect of APS by regulating m6A modification levels in THP-1 macrophages. This study reveals a new dimension of APS regulation of inflammation at the epigenetic level.</p

Rapid Analysis of Bisphenol A and Its Analogues in Food Packaging Products by Paper Spray Ionization Mass Spectrometry

In this study, a paper spray ionization mass spectrometric (PS-MS) method was developed for the rapid in situ screening and simultaneous quantitative analysis of bisphenol A and its analogues, i.e., bisphenol S, bisphenol F, and bisphenol AF, in food packaging products. At the optimal PS-MS conditions, the calibration curves of bisphenols in the range of 1–100 μg/mL were linear. The correlation coefficients were higher than 0.998, and the LODs of the target compounds were 0.1–0.3 μg/mL. After a simple treatment by dichloromethane on the surface, the samples were analyzed by PS-MS in situ for rapid screening without a traditional sample pretreatment procedure, such as powdering, extraction, and enrichment steps. The analytical time of the PS-MS method was less than 1 min. In comparison with conventional HPLC-MS/MS, it was demonstrated that PS-MS was a more effective high-throughput screening and quantitative analysis method

Digital transformation: information system governance

Effects of MEG2 and miR-181a-5p on the growth of gastric cancer xenografted tumours in vivo. a Quantitative analysis of western blot analysis of MEG2 protein expression levels in xenografted tumours. b H&E and immunohistochemical staining for Ki-67 in xenografted tumours. ** P < 0.01. (TIFF 1211 kb

Antagonism of Betulinic Acid on LPS-Mediated Inhibition of ABCA1 and Cholesterol Efflux through Inhibiting Nuclear Factor-kappaB Signaling Pathway and miR-33 Expression

<div><p>ATP-binding cassette transporter A1 (ABCA1) is critical in exporting cholesterol from macrophages and plays a protective role in the development of atherosclerosis. The purpose of this study was to investigate the effects of betulinic acid (BA), a pentacyclic triterpenoid, on ABCA1 expression and cholesterol efflux, and to further determine the underlying mechanism. BA promoted ABCA1 expression and cholesterol efflux, decreased cellular cholesterol and cholesterol ester content in LPS-treated macrophages. Furthermore, we found that BA promoted ABCA1 expression via down-regulation of miR-33s. The inhibition of LPS-induced NF-κB activation further decreased miR-33s expression and enhanced ABCA1 expression and cholesterol efflux when compared with BA only treatment. In addition, BA suppressed IκB phosphorylation, p65 phosphorylation and nuclear translocation, and the transcription of NF-κB-dependent related gene. Moreover, BA reduced atherosclerotic lesion size, miR-33s levels and NF-κB activation, and promoted ABCA1 expression in apoE^−/− mice. Taken together, these results reveal a novel mechanism for the BA-mediated ABCA1 expression, which may provide new insights for developing strategies for modulating vascular inflammation and atherosclerosis.</p></div

The effect of betulinic acid on miR-33a/ABCA1 expression and NF-κB activation in apoE^−/− mice.

<p>8-week-old male apoE^−/− mice were randomly divided into three groups as described in materials and methods. (A) Expression of miR-33a mRNA in the aorta was confirmed by RT-PCR. (B and C) Western blot of aorta ABCA1 protein (B) and aorta NF-κB p65 protein (C). (D, E and F) Plasma levels of TNF-α, IL-6 and IL-1β. All the results are expressed as mean ± SD. *, P<0.05 vs LPS group.</p