Alkynol served as an enolizable carbonyl equivalent to react with (thio)urea and aromatic aldehydes, furnishing a variety of spirofuran-hydropyrimidinone compounds in good yields and excellent diastereoselectivities. The one-pot multicomponent reactions were realized with co-catalysis of palladium chloride and trifluoroacetic acid through a Biginelli-like tandem reaction pathway.

The common and frequent disease, ulcerative colitis (UC), causes serious physical and mental distress to patients. M2 macrophages have proven to play a role in anti-inflammation, which is a new potential target for UC therapy. In this study, we designed a safe and macrophages-targeting oral drug delivery system. Natural products, berberine (BBR), and Epigallocatechin Gallate (EGCG) with anti-inflammatory activity were assembled and encapsulated into yeast microcapsule (YM), generating therapeutic system BBR/MPN@YM. BBR and EGCG exhibited synergistic effects against UC through the effect of antioxidation. Through the interaction between β-1,3-d-glucan on the surface of YM and dectin-1 receptors on macrophages, BBR/MPN@YM could be effectively transported to inflammation parts and internalized into macrophages, avoiding gastric degradation. In the in vivo UC mouse model, BBR/MPN@YM could transform M1 macrophages into anti-inflammatory M2 macrophages, thus exerting specific anti-inflammatory effects. Therefore, this BBR/MPN@YM targeted oral drug delivery system provided a new macrophages-targeting strategy for the clinical treatment of UC.

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An efficient and cooperative catalytic one-pot synthetic methodology for 8-hydroxyquinoline compounds has been developed.