Rosangela Montanaro

Synthesis and biological evaluation of novel fused pyridopyrimidine derivatives as topoisomerase I inhibitors and as potential antitumor agents: promising results in lung, ovary and gastric cancer

Leyre Lopez-Aguileta, Endika Martín-Encinas, Birgitta Ruth Knudsen, Cinzia Tesauro et autres

ABSTRACT. The topoisomerase I (TOP1) enzymatic inhibition was investigated using novel pyrimidine and quinazolinone derivatives. First, the synthesis of these compounds was performed by intramolecular cycloaddition reaction of functionalized aminoalcohols, aminoesters and aldimines, obtained by the condensation of 2-aminopyridine and unsaturated aldehydes, …

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Synthesis and biological evaluation of novel fused pyridopyrimidine derivatives as topoisomerase I inhibitors and as potential antitumor agents: promising results in lung, ovary and gastric cancer

Leyre Lopez-Aguileta, Endika Martín‐Encinas, Birgitta Ruth Knudsen, Cinzia Tesauro et autres

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Harnessing Moringa oleifera Lam's Isothiocyanates for Targeted H 2 S Delivery: A Systematic Review of the Literature

Maria Ponticelli, Rosangela Montanaro, Valentina Vellecco, Eugenia Piragine et autres

ABSTRACT The gasotransmitter hydrogen sulfide (H 2 S) and its natural donor isothiocyanates have been suggested by emerging evidence to play a significant role in the therapeutic management of several conditions like metabolic syndrome, neurodegeneration, inflammation, and so forth. In particular, isothiocyanates …

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CC48 a new CB2R agonist/FAAH inhibitor dual drug blocks gastric cancer progression and overcomes paclitaxel resistance

Annalisa Schirizzi, Giampiero De Leonardis, Rosangela Montanaro, Francesco Mastropasqua et autres

Gastric cancer (GC) has poor survival in advanced stages, with limited treatment options. Paclitaxel (PTX) is commonly used, but resistance often arises, highlighting the need for targeted therapies. Cannabinoid receptor type 2 (CB2R) is overexpressed in several cancers and its activation has …

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The endocrine disruptor vinclozolin causes endothelial injury via eNOS/Nox4/IRE1α signaling

Chiara Indolfi, Ivana Bello, Martina Smimmo, Valentina Vellecco et autres

Vinclozolin (VCZ) is a common dicarboximide fungicide used to protect crops from diseases. It is also an endocrine disruptor, and its effects on various organs have been described but its influence on vasculature has not yet been addressed. This study focuses on …

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Hydrogen sulfide dysfunction in metabolic syndrome-associated vascular complications involves cGMP regulation through soluble guanylyl cyclase persulfidation

Martina Smimmo, V. Casale, Gian Marco Casillo, Emma Mitidieri et autres

Here, by using in vitro and ex vivo approaches, we elucidate the impairment of the hydrogen sulfide (H2S) pathway in vascular complications associated with metabolic syndrome (MetS). In the in vitro model simulating hyperlipidemic/hyperglycemic conditions, we observe significant hallmarks of endothelial dysfunction, …

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Regulatory TR3-56 Cells in the Complex Panorama of Immune Activation and Regulation

Flavia Carriero, Valentina Rubino, Stefania Leone, Rosangela Montanaro et autres

The interplay between immune activation and immune regulation is a fundamental aspect of the functional harmony of the immune system. This delicate balance is essential to triggering correct and effective immune responses against pathogens while preventing excessive inflammation and the immunopathogenic mechanisms …

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Erucin Exerts Cardioprotective Effects on Ischemia/Reperfusion Injury through the Modulation of mitoKATP Channels

Lorenzo Flori, Rosangela Montanaro, Eleonora Pagnotta, Luisa Ugolini et autres

Modulation of mitochondrial K channels represents a pharmacological strategy to promote cardioprotective effects. Isothiocyanates emerge as molecules capable of releasing hydrogen sulfide (H2S), an endogenous pleiotropic gasotransmitter responsible for anti-ischemic cardioprotective effects also through the involvement of mitoK channels. Erucin (ERU) is …

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Persulfidation of mitoKv7.4 channels contributes to the cardioprotective effects of the H2S-donor Erucin against ischemia/reperfusion injury

Lara Testai, Rosangela Montanaro, L. Flori, Eleonora Pagnotta et autres

Hydrogen sulfide (H2S) is a gasotransmitter deeply involved in cardiovascular homeostasis and implicated in the myocardial protection against ischemia/reperfusion. The post-translational persulfidation of cysteine residues has been identified as the mechanism through which H2S regulates a plethora of biological targets. Erucin (ERU) …

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Activity Methods for Cardiovascular System Diseases

Rosangela Montanaro, Emma Mitidieri, Roberta d’ Emmanuele di Villa Bianca, Vincenzo Brancaleone

This chapter provides a collection of methods generally used in experimental pharmacology to test compounds with different activities in the cardiovascular system. There are many models in vitro and in vivo and we have highlighted those used in the field of natural …

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Activity Methods For Animal Pharmacokinetic and Pharmacodynamic Studies

Rosangela Montanaro, Francesco Μaione, Vincenzo Brancaleone

This chapter provides an overview of the main features that need to be assessed with respect to the general pharmacology (pharmacokinetics, PK; pharmacodynamics, PD) of all molecules, including natural compounds. Here, the attention has been focused on bioavailability, the volume of distribution, …

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Adaptive and Innate Cytotoxic Effectors in Chronic Lymphocytic Leukaemia (CLL) Subjects with Stable Disease

Valentina Rubino, Flavia Carriero, Anna Teresa Palatucci, Angela Giovazzino et autres

Chronic lymphocytic leukaemia (CLL) is characterised by the expansion of a neoplastic mature B cell clone. CLL clinical outcome is very heterogeneous, with some subjects never requiring therapy and some showing an aggressive disease. Genetic and epigenetic alterations and pro-inflammatory microenvironment influence …

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