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Juniperus formosana Hayata (J. formosana) is a commom needlebush cultivar growing in China. Six new compounds (1–6), including four cadinene sesquiterpenoids (1 – 4), one abietane diterpenoid (5), and one β-naphthol derivative (6), along with 18 known compounds (7 – 24) were isolated and identified through phytochemical investigation on the heartwood of J. formosana. The structures of these compounds were fully elucidated by their 1D and 2D NMR, HR-ESI-MS, UV, and IR spectral data analyses. The absolute configurations of compounds 1 , 3 , and 5 were confirmed by experimental and calculated electronic circular dichroism (ECD) data. Moreover, X-ray crystallographic analysis was carried out to characterize the structure of compound 4. The inhibitory effects on the nitric oxide (NO) production of all the isolated compounds were initially examined in RAW264.7 macrophages induced by lipopolysaccharide (LPS). The results showed that compounds 3 and 12 possessed significant inhibitory potency on NO generation with IC 50 values of 3.41 μM and 6.15 μM among the new and known compounds, respectively. The expressions of IL-1β, IL-6, and TNF-α were measured in LPS-stimulated RAW264.7 cells to evaluate the anti-inflammatory effects of compounds 1 – 24. Compounds 1–6 and 9–12 exhibited potent anti-inflammatory effects. Additionally, the expressions of p38, Erk, and IκBα proteins were further determined to explore the anti-inflammatory mechanism of the most potent compounds 3 and 12. Overall, our findings indicate the potential of J. formosana for developing medicine candidates as the treatments of inflammation. [Display omitted] • Chemical investigation of J. formosana yielded six new compounds. • The absolute configuration of compounds has been established by ECD data. • The isolated compounds showed moderate to potent anti-inflammatory activity. • The anti-inflammatory mechanisms of 3 and 12 were discussed. [ABSTRACT FROM AUTHOR]

Rationale: Conventional 18 F-labeling methods that demand substrate pre-modification or lengthy radiosynthesis procedures have impeded the visualization and translation of numerous biomolecules, as biomarkers or ligands, using modern positron emission tomography techniques in vivo . Moreover, 18 F-labeled biomolecules in high molar activity (A m ) that are indispensable for sensitive imaging could be only achieved under strict labeling conditions. Methods: Herein, 18 F-labeled fluorothiophosphate (FTP) synthons in high A m have been generated rapidly in situ in reaction solutions with < 5% water via nucleophilic substitution by wet [ 18 F]F - , which required minimal processing from cyclotron target water. Results: Various 18 F-labeled FTP synthons have been prepared in 30 sec at room temperature with high radiochemical yields > 75% (isolated, non-decay-corrected). FTP synthons with unsaturated hydrocarbon or activated ester group can conjugate with typical small molecules, peptides, proteins, and metallic nanoparticles. 337-517 GBq μmol -1 A m has been achieved for 18 F-labeled c(RGDyK) peptide using an automatic module with 37-74 GBq initial activity. Conclusion: The combination of high 18 F-fluorination efficiency of FTP synthons and following mild conjugation condition provides a universal simplified one-pot 18 F-labeling method for broad unmodified biomolecular substrates., Competing Interests: Competing Interests: The authors have declared that no competing interest exists., (© The author(s).)