Background: There are two fundamental forms of cell death: apoptosis and necrosis. Molecular studies of cell death thus far favor a model in which apoptosis and necrosis share very few molecular regulators. It appears that apoptotic processes triggered by a variety of stimuli converge on the activation of a member of the caspase family, such as caspase 3, which leads to the execution of apoptos...

1 Department of Dermatology, University of Luebeck, D-23538 Luebeck, Germany; 2 Department of Dermatology, Hadassah Hebrew University Medical Centre, Jerusalem, Israel; 3 Laboratory of Cutaneous Physiopathology and Integrated Centre of Metabolomics Research, San Gallicano Dermatologic Institute (IRCCS), Rome, Italy; 4 DE-MTA “Lendület” Cellular Physiology Research Group, Department of Physiolog...

Although osteoarthritis (OA), a degenerative joint disease characterized by the degradation of joint articular cartilage and subchondral bones, is generally regarded as a degenerative rather than inflammatory disease, recent studies have indicated the involvement of inflammation in OA pathogenesis. Tabebuia avellanedae has long been used to treat various diseases; however, its role in inflammat...

A phytochemical investigation of the inner bark of Tabebuia avellanedae Lorentz ex Griseb was carried out by various chromatographic techniques, resulting in the isolation and characterization of eight new iridoid esters, namely Avelladoids A-H (1-8). Their chemical structures were elucidated on the basis of extensive spectroscopic analyses, especially 2D NMR experiments and HRMS data. The anti...

Numerous therapeutic strategies have been developed for osteoarthritis (OA) management, including intra-articular (IA) injections. The ideal IA formulation should control cartilage degradation and restore synovial fluid viscosity. To this end, we propose to combine thermo-sensitive polymers (poloxamers) with hyaluronic acid (HA) develop suitable beta-lapachone (βLap) loaded formulations. develo...

Agents, such as β-lapachone, that target the redox enzyme, NAD(P)H:quinone oxidoreductase 1 (NQO1), to induce programmed necrosis in solid tumors have shown great promise, but more potent tumor-selective compounds are needed. Here, we report that deoxynyboquinone kills a wide spectrum of cancer cells in an NQO1-dependent manner with greater potency than β-lapachone. Deoxynyboquinone lethality r...

β-lapachone is a naturally occurring 1,2-naphthoquinone-based compound that has been advanced into clinical trials based on its tumor-selective cytotoxic properties. Previously, we focused on the related 1,4-naphthoquinone pharmacophore as a basic core structure for developing a series of potent indoleamine 2,3-dioxygenase 1 (IDO1) enzyme inhibitors. In this study, we identified IDO1 inhibitory...

Agents, such as b-lapachone, that target the redox enzyme, NAD(P)H:quinone oxidoreductase 1 (NQO1), to induce programmed necrosis in solid tumors have shown great promise, but more potent tumor-selective compounds are needed. Here, we report that deoxynyboquinone kills a wide spectrumof cancer cells in anNQO1dependent manner with greater potency than b-lapachone. Deoxynyboquinone lethality reli...

The in vivo antifungal activity of the naphthoquinone beta-lapachone against disseminated infection by Cryptococcus neoformans was investigated. Swiss mice were immunosuppressed daily with dexamethasone (0.5 mg per mouse) intraperitoneally for 3 days, the procedure was repeated 4 days later, and the animals were then challenged intravenously with C. neoformans (10(6) CFU/mL) 1 week later. Seven...