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Theonellasterols and conicasterols from Theonella swinhoei. Novel marine natural ligands for human nuclear receptors.
Pharmacological and structure-activity relationship analysis demonstrate that these natural polyhydroxylated steroids are potent ligands of human nuclear pregnane receptor (PXR) and modulator of farnesoid-X-receptor (FXR). Expand
Conicasterol E, a small heterodimer partner sparing farnesoid X receptor modulator endowed with a pregnane X receptor agonistic activity, from the marine sponge Theonella swinhoei.
It is demonstrated that conicasterol E is an FXR modulator endowed with PXR agonistic activity and that this steroid might hold utility in treatment of liver disorders. Expand
Total synthesis and pharmacological characterization of solomonsterol A, a potent marine pregnane-X-receptor agonist endowed with anti-inflammatory activity.
It is found that administration of synthetic solomonsterol A effectively protects against development of clinical signs and symptoms of colitis and reduced the generation of TNFα, a signature cytokine for this disorder. Expand
4-Methylenesterols from Theonella swinhoei sponge are natural pregnane-X-receptor agonists and farnesoid-X-receptor antagonists that modulate innate immunity
It is demonstrated that swinhosterol B counter-regulates induction of pro-inflammatory cytokines in a PXR-dependent manner and pave the way to development of a dual PX R agonist/FXR antagonist with a robust immunomodulatory activity and endowed with the ability to modulate the expression of bile acid-regulated genes in the liver. Expand
Modification in the side chain of solomonsterol A: discovery of cholestan disulfate as a potent pregnane-X-receptor agonist.
In vitro studies on hepatic cells provided evidence that cholestan disulfate has the ability to modulate the immune response triggered by bacterial endotoxin as well as to counter-activate hepatic stellate cell activation induced by thrombin. Expand
The First Total Synthesis of Solomonsterol B, a Marine Pregnane X Receptor Agonist
A concise route to the pregnane X receptor (PXR) agonist solomonsterol B, a natural product isolated from the marine sponge Theonella swinhoei, has been developed starting from commercially availableExpand
Preliminary Structure-Activity Relationship on Theonellasterol, a New Chemotype of FXR Antagonist, from the Marine Sponge Theonella swinhoei
Using theonellasterol as a novel FXR antagonist hit, we prepared a series of semi-synthetic derivatives in order to gain insight into the structural requirements for exhibiting antagonistic activity.Expand
Concise synthesis of AHMHA unit in perthamide C. Structural and stereochemical revision of perthamide C
Abstract Diastereomers of 3-amino-2-hydroxy-6-methylheptanoic acid (AHMHA), a new amino acid unit in perthamides C and D, have been synthesized from commercially available 4-methylpentanol in aExpand
Monoacylglycerides from the Diatom Skeletonema marinoi Induce Selective Cell Death in Cancer Cells
It is shown that monoacylglycerides purified from the marine diatom Skeletonema marinoi have selective cytotoxic activity against the haematological cancer cell line U-937 and colon cancer cell lines HCT-116 compared to normal MePR-2B cells. Expand
Natural ligands of nuclear receptors. Isolation, design, synthesis, biochemical decodification and potential therapeutic applications.
This study disclosed cholestan disulfate (Coldisolf) as a new, simplified agonist of PXR, currently in pharmacological evaluation on animal models of liver fibrosis induced by HIV infection and a wide family of 4-methylene steroids were isolated from the apolar extracts of Theonella swinhoei, endowed with a potent agonistic activity on PxR while antagonize the effects of natural ligands for FXR. Expand