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Tolaasins A--E, five new lipodepsipeptides produced by Pseudomonas tolaasii.
Among the target microorganisms used (fungi, yeast, and bacteria) the Gram-positive bacteria were the most sensitive, although the antimicrobial activity appeared to be correlated to the structural modification in the different analogues. Expand
Polycyclic guanidine alkaloids from the marine sponge Crambe crambe and Ca++ channel blocker activity of crambescidin 816.
Four pentacyclic guanidine derivatives related to ptilomycalin A have been isolated from the Mediterranean sponge Crambe crambe and were found to have a potent Ca++ antagonist effect and to inhibit the acetylcholine-induced contraction of guinea pig ileum at very low concentrations. Expand
Anti-inflammatory and analgesic activity of a novel inhibitor of microsomal prostaglandin E synthase-1 expression.
The data suggest that inhibition of mPGES-1 protein expression in acute and chronic inflammatory models by BTH, could provide a potential therapeutic target and a pharmacological tool to discern the role of the inducible enzymes COX-2 and mPGes-1 in inflammatory pathologies. Expand
Synthesis and pharmacological evaluation of a selected library of new potential anti-inflammatory agents bearing the gamma-hydroxybutenolide scaffold: a new class of inhibitors of prostanoid
A promising inhibitor of prostanoid production acting by in vitro and in vivo selective modulation of microsomal prostaglandin E synthase 1 expression is discovered. Expand
Isolation and structure elucidation of four new triterpenoid estersaponins from fruits of Pittosporum tobira ait.
Abstract Four new triterpenoid estersaponins, tentatively designated as IIIA2 ( 1 ), IIIA3 ( 2 ), IIIB2 ( 3 ), and IIIC4 ( 4 ) have been isolated from fruits of Pittosporum tobira ait . and theirExpand
New bisindole alkaloids of the topsentin and hamacanthin classes from the Mediterranean marine sponge Rhaphisia lacazei.
The major compounds 1-3 were tested in vitro for antitumor activity; compounds 2 and 3 showed antiproliferative activity against human bronchopulmonary cancer cells (NSCLC-N6) with an IC(50) of 12 and 6.3 microg/mL, respectively. Expand
Chemical proteomics-driven discovery of oleocanthal as an Hsp90 inhibitor.
Hsp90, a key target in cancer therapy, has been identified as the main partner of oleocanthal, an olive oil bioactive compound and its mechanism of action at the molecular level was disclosed. Expand