Bioorg Chem 2021 Mar 12;108:104642. Epub 2021 Jan 12.
Department of Chemistry and Chemical Engineering, Faculty of Engineering, Niigata University, Ikarashi, 2-8050, Niigata 950-2181, Japan. Electronic address:
Tuberiferin, 6-epi-tuberifelin, dehydrobrachylaenolide and two series of eudesmanolides, eudesmane-12,6 α-lactones and eudesmane-12,6β-lactones, were synthesized for the studies of the structure-activity relationships to explore novel anti-inflammatory, anti-cancer and crop disease prevention agents. The anti-inflammatory activities were tested by the inhibitory on the induction of inter-cellular adhesion molecule (ICAM-1), the permeation of leucocyte into inflammatory air pouch of murine, the killing function of cytotoxic T-lymphocytes (CTL), production of IL-1; The anti-cancer activities were established on the cytotoxic activities to six kinds of cell lines (P388, CCRF-CEM, VA-13, HepG2, QG-56, and WI-38). Results showed that Dehydrobrachylaenolide (an exo-endo cross conjugated dienone and α-methylene γ-lactone) was the most effective compound inhibiting ICAM-1 (IC 3. Read More