Evaluation of a Positron Emission Tomography Tracer Targeting Colony-Stimulating Factor 1 Receptor for Detecting Pulmonary Inflammation.

Colony-stimulating factor 1 receptor (CSF1R) is a type III receptor tyrosine kinase that is crucial for immune cell activation, survival, proliferation, and differentiation. Its expression significantly increases in macrophages during inflammation, playing a crucial role in regulating inflammation resolution and termination. Consequently, CSF1R has emerged as a critical target for both therapeutic intervention and imaging of inflammatory diseases. Herein, we have developed a radiotracer, 1-[4-((7-(dimethylamino)quinazolin-4-yl)oxy)phenyl]-3-(4-[18F]fluorophenyl)urea ([18F]17), for in vivo positron emission tomography (PET) imaging of CSF1R. Compound 17 exhibits a comparable inhibitory potency against CSF1R as the well-known CSF1R inhibitor PLX647. The radiosynthesis of [18F]17 was successfully performed by radiofluorination of aryltrimethyltin precursor with a yield of approximately 12% at the end of synthesis, maintaining a purity exceeding 98%. In vivo stability and biodistribution studies demonstrate that [18F]17 remains >90% intact at 30 min postinjection, with no defluorination observed even at 60 min postinjection. The PET/CT imaging study in lipopolysaccharide-induced pulmonary inflammation mice indicates that [18F]17 offers a more sensitive characterization of pulmonary inflammation compared to traditional [18F]FDG. Notably, [18F]17 shows a higher discrepancy in uptake ratio between mice with pulmonary inflammation and the sham group. Furthermore, the variations in [18F]17 uptake ratio observed on day 7 and day 14 correspond to lung density changes observed in CT imaging. Moreover, the expression levels of CSF1R on day 7 and day 14 follow a trend similar to the uptake pattern of [18F]17, indicating its potential for accurately characterizing CSF1R expression levels and effectively monitoring the pulmonary inflammation progression. These results strongly suggest that [18F]17 has promising prospects as a CSF1R PET tracer, providing diagnostic opportunities for pulmonary inflammatory diseases.

Haplotype-based phylogenetic analysis and population genomics uncover the origin and domestication of sweetpotato.

The hexaploid sweetpotato (Ipomoea batatas) is one of the most important root crops worldwide. However, its genetic origin remains controversial, and its domestication history remains unknown. In this study, we used a range of genetic evidence and a newly developed haplotype-based phylogenetic analysis to identify two probable progenitors of sweetpotato. The diploid progenitor was likely closely related to Ipomoea aequatoriensis and contributed the B1 subgenome, IbT-DNA2, and the lineage 1 type of chloroplast genome to sweetpotato. The tetraploid progenitor of sweetpotato was most likely I. batatas 4x, which donated the B2 subgenome, IbT-DNA1, and the lineage 2 type of chloroplast genome. Sweetpotato most likely originated from reciprocal crosses between the diploid and tetraploid progenitors, followed by a subsequent whole-genome duplication. In addition, we detected biased gene exchanges between the subgenomes; the rate of B1 to B2 subgenome conversions was nearly three times higher than that of B2 to B1 subgenome conversions. Our analyses revealed that genes involved in storage root formation, maintenance of genome stability, biotic resistance, sugar transport, and potassium uptake were selected during the speciation and domestication of sweetpotato. This study sheds light on the evolution of sweetpotato and paves the way for improvement of this crop.

Effects of profenofos on the growth, reproduction, behavior, and gene transcription of Daphnia magna.

Profenofos (PFF) is an organophosphorus pesticide frequently detected in surface waters, soil habitats, and even biota. Some studies have demonstrated the potential risks of PFF to aquatic organisms. However, most of these studies were focused on its acute rather than chronic impacts, and the subjects are usually large vertebrates. Here, we treated D. magna (< 24 h) with PFF at doses of 0, 0.07, 0.28, and 1.12 mg/L for 21 days to study its long-term toxic impacts. Exposure to PFF largely decreased the survival rate and inhibited the growth and reproduction of D. magna. Then, PCR arrays were used to evaluate the changes in the expression of 13 genes related to growth, reproduction, and swimming behavior. The results revealed that the expression of several genes was dramatically changed by exposure to each dose of PFF, which might be responsible for the observed toxic effects of PFF. In summary, our findings imply that long-term PFF exposure can be highly hazardous to the growth, development, and reproduction of D. magna.

Fluorine-18: Radiochemistry and Target-Specific PET Molecular Probes Design.

The positron emission tomography (PET) molecular imaging technology has gained universal value as a critical tool for assessing biological and biochemical processes in living subjects. The favorable chemical, physical, and nuclear characteristics of fluorine-18 (97% ß+ decay, 109.8 min half-life, 635 keV positron energy) make it an attractive nuclide for labeling and molecular imaging. It stands that 2-[18F]fluoro-2-deoxy-D-glucose ([18F]FDG) is the most popular PET tracer. Besides that, a significantly abundant proportion of PET probes in clinical use or under development contain a fluorine or fluoroalkyl substituent group. For the reasons given above, 18F-labeled radiotracer design has become a hot topic in radiochemistry and radiopharmaceutics. Over the past decades, we have witnessed a rapid growth in 18F-labeling methods owing to the development of new reagents and catalysts. This review aims to provide an overview of strategies in radiosynthesis of [18F]fluorine-containing moieties with nucleophilic [18F]fluorides since 2015.

Exploring and exploiting genetics and genomics for sweetpotato improvement: Status and perspectives.

Sweetpotato (Ipomoea batatas (L.) Lam.) is one of the most important root crops cultivated worldwide. Because of its adaptability, high yield potential, and nutritional value, sweetpotato has become an important food crop, particularly in developing countries. To ensure adequate crop yields to meet increasing demand, it is essential to enhance the tolerance of sweetpotato to environmental stresses and other yield-limiting factors. The highly heterozygous hexaploid genome of I. batatas complicates genetic studies and limits improvement of sweetpotato through traditional breeding. However, application of next-generation sequencing and high-throughput genotyping and phenotyping technologies to sweetpotato genetics and genomics research has provided new tools and resources for crop improvement. In this review, we discuss the genomics resources that are available for sweetpotato, including the current reference genome, databases, and available bioinformatics tools. We systematically review the current state of knowledge on the polyploid genetics of sweetpotato, including studies of its origin and germplasm diversity and the associated mapping of important agricultural traits. We then outline the conventional and molecular breeding approaches that have been applied to sweetpotato. Finally, we discuss future goals for genetic studies of sweetpotato and crop improvement via breeding in combination with state-of-the-art multi-omics approaches such as genomic selection and gene editing. These approaches will advance and accelerate genetic improvement of this important root crop and facilitate its sustainable global production.

Relative Contribution of Metal Content and Soil Particle Mass to Health Risk of Chromium-Contaminated Soil.

Three soil samples from a chromium (Cr)-contaminated field were classified into five particle fractions (i.e., 0-50 µm, 50-100 µm, 100-250 µm, 250-500 µm, and 500-1000 µm) and were further characterized to study their physicochemical properties and Cr bioaccessibility. The results indicated that the gastrointestinal bioaccessibility estimated by the Solubility Bioaccessibility Research Consortium (SBRC) method was on average 15.9% higher than that by the physiologically based extraction test (PBET) method. The health risk of all samples was within the safe range, and the health risk based on total Cr content may be overestimated by an average of 13.2 times compared to the bioaccessibility-based health risk. The health risk investigated from metal content was mainly contributed by the 50-250 µm fraction, which was 47.5, 50.2, and 43.5% for low-, medium-, and high-level polluted soils, respectively. As for the combined effect, the fractions of 100-250 µm and 500-1000 µm contributed the highest proportion to health risk, which was 57.1, 62.1, and 64.4% for low-level, medium-level, and high-level polluted soils, respectively. These results may further deepen the understanding of health risk assessment and quantify the contribution of the soil particle mass to health risk.

Triculata A, a novel compound from Tricyrtis maculata (D. Don) J. F. Macbr. with biological properties.

A novel compound, triculata A (1), and seven known compounds were obtained from the Tricyrtis maculata (D. Don) J. F. Macbr.. The structure of the new compound was determined by extensive spectroscopic methods, and its absolute configuration was assigned by single-crystal X-ray diffraction analysis. Compound 1 features a rare naphtho[b,c]pyran carbon skeleton that was found in nature for the first time. Compounds 2-4, 6 and 7 showed potential vasodilatory effects with EC50 values ranging from 7.3 to 111.3 µM. Compounds 1, 3-5 and 7 possessed remarkable antioxidant capacity evaluated by DPPH and ABTS assays.

The curative effect of Reduning injection combined with Xuanfeibaidu formula on COVID-19: A protocol for systematic review and meta-analysis.

BACKGROUND: Since December 2019, COVID-19, caused by the new coronavirus (SARS-CoV-2), posed a serious threat to human health. On March 11, 2020, the World Health Organization announced that COVID-2019 has become a global pandemic. In China, Reduning injection (REDI) and Xuanfeibaidu formula (XFF) is widely used in treating COVID-19. However, there is no evidence-based medical evaluation that XFF combine with REDI is effective for COVID-19. METHODS: The following databases will be searched: China National Knowledge Infrastructure (CNKI), Wanfang database, Chinese Science and Technology Periodical Database, Medline/PubMed, and Cochrane from October 1, 2019 to September 1, 2020. The suitable articles will be comprehensively and systematically searched without limitations of regions or language about REDI with XFF for COVID-19. The meta-analysis was performed by RevMan 5.3 and STATA 14.2 software. RESULTS: This meta-analysis may help provide clarify on the effect of REDI combined with XFF to treat COVID-19. The result will be published at a peer-reviewed journal. CONCLUSIONS: This systematic review aims to provide new evidence of XFF combined with REDI for the treatment of COVID-19 in terms of its efficacy and safety. INPLASY REGISTRATION NUMBER: INPLASY202090039.

Correction: APTES assisted surface heparinization of polylactide porous membranes for improved hemocompatibility.

[This corrects the article DOI: 10.1039/C6RA04525A.].

Copper-Mediated Aromatic 1,1-Difluoroethylation with (1,1-Difluoroethyl)trimethylsilane (TMSCF2 CH3 ).

A new method for the formation of 1,1-difluoroethyl copper species ("CuCF2 CH3 ") with 1,1-difluoroethylsilane (TMSCF2 CH3 ) has been developed. The "CuCF2 CH3 " species can be applied to the efficient 1,1-difluoroethylation of diaryliodonium salts under mild conditions, affording (1,1-difluoroethyl)arenes in good to excellent yields. This convenient procedure tolerates a wide range of functional groups and thus serves as a practical synthetic tool for the introduction of CF2 CH3 group(s) into complex molecules.