The first successful synthesis of 1,2,3-triazoles using CyreneTM as a biodegradable and non-toxic solvent in click chemistry has been developed. In contrast to previous methods, this sustainable approach allows product isolation by simple precipitation in water, eliminating the need for organic solvent extractions and column chromatography purifications, thus minimizing waste consumption while reducing operational costs. The protocol, performed also at gram scale, has broad applicability and versatility, as shown with complex substrates like biologically active coumarins or triazole-linked bifunctional molecules.
View Article and Find Full Text PDFPurpose: Sarcopenia is a progressive and generalized skeletal muscle disorder, involving the accelerated loss of skeletal muscle mass and function, associated with an increased probability of adverse outcomes including falls. The circadian timing system may be involved in molecular pathways leading to sarcopenia in older adults. We aimed to provide an updated and systematic map of the available evidence on the role of the circadian timing system in sarcopenia, specifically related to the aging process.
View Article and Find Full Text PDFPurpose: Caregivers of people with dementia often face a demanding care burden that may lead to adverse physical and psychological outcomes. Wearable sensors are becoming a valuable tool for preventive care. We aimed to provide the first systematic map of the published evidence on the use of wearable sensors to monitor caregivers of people with dementia.
View Article and Find Full Text PDFPurpose: Choroid plexus tumors (CPT) are rare entities, and even rarer in adulthood.
Methods: A retrospective consecutive series of 24 adult CPT patients was reviewed.
Results: We described 24 adult CPTs.
The use of fotemustine (FTM) has been authorized in certain countries for the treatment of recurrent high-grade gliomas (HGG) after Stupp therapy. However, to the best of our knowledge, no studies have assessed changes in magnetic resonance imaging (MRI) during treatment with FTM monotherapy. The aim of the present study was to assess the neuroradiological findings in a cohort of patients with recurrent HGG treated with FTM monotherapy.
View Article and Find Full Text PDFA library of novel nicotinic acid derivatives, focusing on the modification of position 6 of the pyridine ring with (thio)ether functionalities, was mostly produced through an innovative green synthetic approach (Cyrene-based) and evaluated for their α-amylase and α-glucosidase inhibitory activity. Compounds and demonstrated micromolar inhibition against α-amylase (IC of 20.5 and 58.
View Article and Find Full Text PDFAmide Proton Transfer-weighted (APTw) imaging is a molecular MRI technique used to quantify protein concentrations in gliomas, which have heterogeneous components with varying cellularity and metabolic activity. This study aimed to assess the correlation between the component-specific APT signal of the neoplasm and WHO grade, molecular profile and survival status. Sixty-one patients with adult-type diffuse gliomas were retrospectively analyzed.
View Article and Find Full Text PDFObjective: The COVID-19 pandemic affected neuro-oncological patients and their caregivers regarding tumor care and emotional functioning, including Quality of Life (QoL). This study aimed to understand how COVID-19 affected their psychological state and the relations between patients and health personnel in neuro-oncology.
Methods: A cross-sectional study was conducted on neuro-oncological patients and their caregivers.
CDKL5 deficiency disorder is a rare genetic disease caused by mutations in the CDKL5 gene. Central apneas during wakefulness have been reported in patients with CDKL5 deficiency disorder. Studies on CDKL5-knockout mice, a CDKL5 deficiency disorder model, reported sleep apneas, but it is still unclear whether these events are central (central sleep apnea) or obstructive (obstructive sleep apnea) and may be related to alterations of brain circuits that modulate breathing rhythm.
View Article and Find Full Text PDFNarcolepsy type-1 (NT1) is a lifelong sleep disease, characterised by impairment of the orexinergic system, with a typical onset during adolescence and young adulthood. Since the wake-sleep cycle physiologically changes with ageing, this study aims to compare sleep patterns between orexin-knockout (KO) and wild type (WT) control mice at different ages. Four groups of age-matched female KO and WT mice (16 weeks of age: 8 KO-YO and 9 WT-YO mice; 87 weeks of age: 13 KO-OLD and 12 WT-OLD mice) were implanted with electrodes for discriminating wakefulness, rapid-eye-movement sleep (REMS), and non-REMS (NREMS).
View Article and Find Full Text PDFDown syndrome (DS) is a segmental progeroid genetic disorder associated with multi-systemic precocious aging phenotypes, which are particularly evident in the immune and nervous systems. Accordingly, people with DS show an increased biological age as measured by epigenetic clocks. The Ts65Dn trisomic mouse, which harbors extra-numerary copies of chromosome 21 (Hsa21)-syntenic regions, was shown to recapitulate several progeroid features of DS, but no biomarkers of age have been applied to it so far.
View Article and Find Full Text PDFIntroduction: Proprotein convertase subtilisin/kexin 9 (PCSK9) plays a crucial role in breaking down the hepatic low-density lipoprotein receptor (LDLR), thereby influencing the levels of circulating low-density lipoprotein cholesterol (LDL-C). Consequently, inhibiting PCSK9 through suitable ligands has been established as a validated therapeutic strategy for combating hypercholesterolemia and cardiovascular diseases.
Area Covered: Patent literature claiming novel compounds inhibiting PCSK9 disclosed from 2018 to June 2023 available in the espacenet database, which contains more than 150 million patent documents from over 100 patent-granting authorities worldwide.
Background: We previously reported that tumor 3D volume growth rate (3DVGR) classification could help in the assessment of drug activity in patients with meningioma using 3 main classes and a total of 5 subclasses: class 1: decrease; 2: stabilization or severe slowdown; 3: progression. The EORTC-BTG-1320 clinical trial was a randomized phase II trial evaluating the efficacy of trabectedin for recurrent WHO 2 or 3 meningioma. Our objective was to evaluate the discriminative value of 3DVGR classification in the EORTC-BTG-1320.
View Article and Find Full Text PDFFive-year glioblastoma (GBM) survivors (LTS) are the minority of the isocitrate dehydrogenase (IDH)-wild-type GBM patients, and their molecular fingerprint is still largely unexplored. This multicenter retrospective study analyzed a large LTS-GBM cohort from nine Italian institutions and molecularly characterized a subgroup of patients by mutation, DNA methylation (DNAm) and copy number variation (CNV) profiling, comparing it to standard survival GBM. Mutation scan allowed the identification of pathogenic variants in most cases, showing a similar mutational spectrum in both groups, and highlighted TP53 as the most commonly mutated gene in the LTS group.
View Article and Find Full Text PDFA one-pot protocol, consisting of a Pd-catalysed carboamination reaction, followed by -deprotection and oxidative denitrogenation, has been developed for the synthesis of diversely substituted spirocyclopropyloxindoles, in yields up to 73% and with diastereoselectivity close to 1 : 1. Readily accessible starting materials, mild reaction conditions, an easy to operate one-pot procedure and good functional group tolerance make this transformation a versatile tool for the synthesis of substituted spirocyclopropyloxindoles. This protocol successfully works on the gram-scale and allows access to both diastereoisomers separately.
View Article and Find Full Text PDFGlob Reg Health Technol Assess
January 2024
Background: Prolactinoma, the most common pituitary adenoma, is usually treated with dopamine agonist (DA) therapy like cabergoline. Surgery is second-line therapy, and radiotherapy is used if surgical treatment fails or in relapsing macroprolactinoma.
Objective: This study aimed to provide economic evidence for the management of prolactinoma in Italy, using a cost-of-illness and cost-utility analysis that considered various treatment options, including cabergoline, bromocriptine, temozolomide, radiation therapy, and surgical strategies.
Introduction: Drug repurposing is a promising strategy to develop new treatments for glioblastoma. In this phase II clinical trial, we evaluated the addition of chlorpromazine to temozolomide in the adjuvant phase of the standard first-line therapeutic protocol in patients with unmethylated gene promoter.
Methods: This was a multicenter phase II single-arm clinical trial.
Proprotein convertase subtilisin/kexin 9 (PCSK9) is responsible for the degradation of the hepatic low-density lipoprotein receptor (LDLR), which regulates circulating cholesterol levels. Consequently, the PCSK9 inhibition is a valuable therapeutic approach for the treatment of hypercholesterolemia and cardiovascular diseases. In our studies, we discovered , a polyimidazole derivative reducing the protein-protein interaction between PCSK9 and LDLR with an IC of 1.
View Article and Find Full Text PDFEndocr Metab Immune Disord Drug Targets
November 2023
Introduction: This guideline (GL) is aimed at providing a reference for the management of prolactin (PRL)-secreting pituitary adenoma in adults. However, pregnancy is not considered.
Methods: This GL has been developed following the methods described in the Manual of the Italian National Guideline System.
The purpose of this editorial is to consider some of the aspects of the diagnosis and treatment of adult gliomas. These are rare diseases with all their limitations. Innovations in diagnosis and therapy and their constraints are analyzed and compared with the current treatment reality.
View Article and Find Full Text PDFBackground: Altered microRNA profiles have been observed not only in tumour tissues but also in biofluids, where they circulate in a stable form thus representing interesting biomarker candidates. This study aimed to identify a microRNA signature as a non-invasive biomarker and to investigate its impact on glioma biology.
Methods: MicroRNAs were selected using a global expression profile in preoperative serum samples from 37 glioma patients.