A supramolecular hydrogel based on D-amino acids, which resists hydrolysis catalyzed by proteinase K and offers long-term biostability, exhibits controlled release in vivo, as proved by the pharmacokinetics of encapsulated 125I tracers and the SPECT imaging of the hydrogel-encapsulated 131I tracers. As the first in vivo imaging investigation of the drug release properties of the supramolecular hydrogel, isotope encapsulation serves as a valid, useful assay for characterizing the controlled release properties of supramolecular hydrogels in vivo. Our results indicate that supramolecular hydrogels promise new biomaterials for controlled drug release.
Pd-Catalyzed denitrogenative functionalizations of benzotriazoles with alkenes and 1,3-dienes have been developed, which enable the rapid access of diverse ortho-amino styrenes and 2-vinylindolines, respectively. This study shows the great potential of benzotriazoles as a [1C]-synthon in cross-coupling reactions and an aza-[3C]-synthon in cycloaddition reactions.
Guided by our biosynthetic
hypothesis, pericoannosins C–F,
four new PKS–NRPS hybrid metabolites, were discovered from
the endophytic fungus Periconia sp. F-31. Their structures
and absolute configurations were elucidated by extensive spectroscopic
data and electronic circular dichroism analyses. Preliminary biological
evaluation revealed that pericoannosins C–D exhibited anti-HIV
activities with IC50 values of 15.5 and 13.5 μM.
Furthermore, the bioinspired syntheses of pericoannosins C–E
have also been completed with high efficiency.
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