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By modifying the structures of targeted A 2A R antagonists and tracers, novel compounds 3 , 7a , 9 , 12c , and BIBD-399 were designed and synthesized. In vitro inhibition experiments demonstrated that 3 , 12c , and BIBD-399 have high affinity for A 2A R. [ 18 F]3 and [ 18 F]BIBD-399 were successfully synthesized. In terms of biological distribution, the brain uptake of [ 18 F]MNI-444 exhibits greater than that of [ 18 F]3 and [ 18 F]BIBD-399. PET imaging shows that [ 18 F]3 is off-target in the brain, while [ 18 F]BIBD-399 and [ 18 F]MNI-444 can be specifically imaged in regions with high A 2A R expression. Differently, [ 18 F]BIBD-399 could quickly reach equilibrium in the targeted region within 10 min after administration, while [ 18 F]MNI-444 shows a slowly increasing trend within 2 h of administration. [ 18 F]BIBD-399 is mainly metabolized by the liver and kidney, and there is no obvious defluorination in vivo. Additional in vitro autoradiography showed that the striatal signals of [ 18 F]BIBD-399 and [ 18 F]MNI-444 were inhibited by the A 2A R antagonist SCH442416 but not by the A 1 R antagonist DPCPX, demonstrating the high A 2A R binding specificity of [ 18 F]BIBD-399. Molecular docking further confirms the high affinity of MNI-444 and BIBD-399 for A 2A R. Further tMCAo imaging showed that [ 18 F]BIBD-399 can sensitively distinguish between infarcted and noninfarcted sides, a capability not observed with [ 18 F]MNI-444. Given its pharmacokinetic properties and the ability to identify lesion regions, [ 18 F]BIBD-399 has potential advantages in monitoring A 2A R changes, meriting further clinical investigation.

[ 18 F]Gln-OSO 2 F, [ 18 F]Arg-OSO 2 F, and [ 18 F]FSY-OSO 2 F were designed by introducing sulfonyl 18 F-fluoride onto glutamine, arginine, and tyrosine, respectively. [ 18 F]FSY-OSO 2 F can be prepared directly by sulfur 18 F-fluoride exchange, while [ 18 F]Gln-OSO 2 F and [ 18 F]Arg-OSO 2 F require a two-step labeling method. Those tracers retain their typical transport characteristics for unmodified amino acids. Both PET imaging and biodistribution confirmed that [ 18 F]FSY-OSO 2 F visualized MCF-7 and 22Rv1 subcutaneous tumors with high contrast, and its tumor-to-muscle ratio was better than that of [ 18 F]FET. However, [ 18 F]Gln-OSO 2 F and [ 18 F]Arg-OSO 2 F poorly image MCF-7 subcutaneous tumors, possibly due to differences in the types and amounts of transporters expressed in tumors. All three tracers can visualize the U87MG glioma. According to our biological evaluation, none of the tracers evaluated in this study exhibited obvious defluorination, and subtle structural changes led to different imaging characteristics, indicating that the application of sulfur 18 F-fluoride exchange click chemistry in the design of radioactive sulfonyl fluoride amino acids is feasible and offers significant advantages., Competing Interests: The authors declare no competing financial interest., (© 2024 American Chemical Society.)

Objective: To explore the therapeutic effect and inflammatory mechanism of fire needles on gouty arthritis., Methods: Sixty male Sprague-Dawley rats were divided into four groups, that is, control group, the model group, the colchicine group, and the fire needle treatment group. Acute gouty arthritis was prepared by injection of monosodium urate in the ankle joint. The inflammation-related protein [toll-like receptor 4 (TLR4), pyrin domain-containing protein 3 (NLRP3), interleukin (IL)-1β, myeloid differentiation factor 88 (MyD88), nuclear factorkappa B (NF-κB), phosphorylated NF-κB (p-NF-κB), caspase-1, and p-caspase-1] in swollen tissues, the inflammation-related mRNAs indicators (TLR4, NLRP3, NF-κB, and caspase-1) and the inflammatory factors [IL-1β, IL-6, IL-8, tumor necrosis factor-α (TNF-α), and C-reactive protein (CRP)] in the serum were detected by Western blot, real-time quantitative polymerase chain reaction, and enzyme-linked immunosorbent assay, respectively., Results: The fire needle treatment could reduce joint swelling, increase mechanical pain threshold and decrease the inflammation index score in the fire needle treatment group. It could also significantly decreased the protein expression of IL-1β, TLR4, MyD88, p-NF-κB and NLRP3 in joint tissue, markedly downregulated the mRNA levels of TLR4 and NLRP3 in joint tissue, and significantly reduce serum levels of IL-1β, IL-6, IL-8, TNF-α, and CRP., Conclusion: The fire needle treatment had positive effect of treating gouty arthritis, and its under- lying mechanism might be associated with NF-κB activation and related inflammatory response.

Purpose: This observational study aimed to compare the outcome and health-related quality of life (HRQOL) amongst breast cancer patients using Chinese herbal medicine (CHM) and those not using CHM during chemotherapy., Methods: A prospective, non-randomised longitudinal study was conducted in two government integrated hospitals over an 8-month period. Early-stage breast cancer patients who were (1) either already using complementary and alternative medicine (CAM) or not and (2) who were on a regime of 5-fluorouracil, epirubicin, and cyclophosphamide were included in the study. Patients who agreed to receive CHM were assigned to receive individualised CHM prescriptions deemed suitable for the individual at a particular time. Those who were not willing to take Chinese herbal medicines (CHM) were assigned to the non-CHM control group. Blood profile and chemotherapy-induced AE were recorded whilst HRQOL assessment was done using the EORTC QLQ-C30 questionnaire on first, third, and sixth cycles., Results: Forty-seven patients [32 female vs. 1 male, p = 0.31; mean year of age: 52.2(SD = 7.6), p = 0.28)}] were recruited during the study period. Demographics of both groups were comparable. Fifty percent of respondents reported using some kind of CAM before chemotherapy. Diet supplements (40.6%) were the most common CAM used by the respondents. The study showed that patients using CHM had significantly less fatigue (p = 0.012), nausea (p = 0.04), and anorexia (p = 0.005) during chemotherapy. There were no significant differences in patients' HRQOL (p = 0.79). There were no AEs reported during the study., Conclusion: The use of CHM as an adjunct treatment with conventional chemotherapy have been shown to reduce fatigue, nausea, and anorexia in breast cancer patients but did not reduce chemotherapy-associated hematologic toxicity. The sample size of this study was not powered to assess the significance of HRQOL between two groups of patients.

Mechanically mixed γ-Al 2 O 3 and HZSM-5 (Si/Al = 50) with different mass ratio were utilized as support for Cu-Co higher alcohol synthesis catalysts prepared through incipient wetness impregnation. The textural and structural properties were studied using Ar low temperature adsorption and desorption, H 2 -temperature programmed reduction (H 2 -TPR), X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), transmission electron microscope (TEM) and catalytic performance measurements. The results indicated that the mechanically mixed HZSM-5 and γ-Al 2 O 3 supported copper-cobalt catalysts were superior to either γ-Al 2 O 3 or HZSM-5 supported ones with the same metal loading. The results revealed that using HZSM-5 and γ-Al 2 O 3 mechanically mixed benefited the dispersion of metallic phases and stronger synergetic functions between smaller nanoparticles containing copper and/or cobalt, which is essential for HAS from CO hydrogenation. Under working conditions of P = 5.0 MPa, T = 300 °C, V (H 2 ) :  V (CO) :  V (N 2 ) = 4 : 2 : 1 and GHSV = 7200 mL g -1 h -1 , mechanically mixed HZSM-5 and γ-Al 2 O 3 supported catalysts showed higher catalytic activity than those over single support. For CuCo catalysts upon support containing 50.0 wt% HZSM-5 and 50.0 wt% γ-Al 2 O 3 , the CO conversion was 21.3% and the C 2+ alcohol selectivity was 41.8%., Competing Interests: There are no conflicts to declare., (This journal is © The Royal Society of Chemistry.)