Background: ACTION, a 24-week, prospective, randomized, parallel-group, double-blind study in patients with severe Alzheimer’s disease (AD), demonstrated significant efficacy of 13.3 mg/24 h versus 4.6 mg/24 h rivastigmine patch on the Severe Impairment Battery (SIB) and Alzheimer’s Disease Cooperative Study–Activities of Daily Living scale–Severe Impairment Version (ADCS-ADL-SIV). Overall, 61% of the study population received at least 1 dose of concomitant memantine, regardless of dose or duration. This retrospective analysis investigated the effects of concomitant memantine on the efficacy, safety and tolerability of 13.3 mg/24 h versus 4.6 mg/24 h rivastigmine patch. Methods: Patients were stratified according to whether or not they received at least one dose of concomitant memantine during the double-blind phase. Changes from…
Purpose: The aim of the present study was to compare the potential for cartilage repair of fresh amniotic membrane (AM), cryopreserved AM and cryopreserved AM previously cultured with bone marrow mesenchymal stem cells (BM-MSCs) in an in vivo sheep animal model. Methods: A full-thickness cartilage defect was surgically produced in 12 adult sheep, in the bearing region of the lateral femoral condyle. The animals were randomized into 4 groups (n=3): no treatment of the defect (G1); filling with fresh AM (G2); with cryopreserved AM previously cultivated with BM-MSCs (G3); with cryopreserved AM alone (G4). Postoperatively, the full load was possible. At two months, the animals were euthanized. The quality of the new synthesized tissue was evaluated with the macroscopic, by using International Cartilage Repair Society (ICRS) scale, and histological analyses, by using O’Driscoll scale. Results: The control samples showed an ICRS grade III (abnormal); while the samples of Groups 2, 3 and 4 reported a grade II (similar to healthy cartilage)…
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Abstract: Ecto-nucleotidases are nucleotide metabolizing enzymes that are divided into four different families; nucleoside triphosphate diphosphohydrolases (NTPDases), ecto-5′-nucleotidase (ecto-5′-NT), nucleotide pyrophosphatase/phosphodiesterases (NPPs), and alkaline phosphatases (APs). These enzymes are responsible for the hydrolysis of nucleotidases (nucleoside 5′-triphosphates, 5′-diphosphates and 5′-monophosphates). Ecto-nucleotidases modulate P1- and P2-receptor-mediated signaling. Alterations in extracellular nucleotide and adenosine level can increase or decrease P1 and P2 activity. Potent and selective ligands for certain ectonucleotidase are important as pharmacological tools to investigate the (patho)physiological roles of these enzymes. Furthermore, such ligands are required to study their potential as novel drugs, e.g., as immunomodulatory agents, for the treatment of cancer, cardiovascular or central nervous system disorders. Hence, this review aims to provide an overview of ecto-nucleotidases inhibitors developed so far.
Mini-Reviews in Medicinal Chemistry, 2015, 15, 21-33
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Abstract: As an important part of non steroids anti-inflammation drug (NSAIDs), salicylate has developed from natural substance salicylic acid to natrium salicylicum, to aspirin. Now, methyl salicylate glycoside, a new derivative of salicylic acid, is modified with a -COOH group integrated one methyl radical into formic ether, and a -OH linked with a monosaccharide, a disaccharide or a trisaccharide unit by glycosidic linkage. It has the similar pharmacological activities, anti-inflammatory, analgesic, antipyretic and antithrombotic as the previous salicylates’ without resulting in serious side effects, particularly the gastrointestinal toxicity. Owing to the superiority of those significant bioactivities, methyl salicylate glycosides have became a hot research area in NSAIDs for several years. This paper compiles all 9 naturally occurring methyl salicylate glycosides, their distribution of the resource and pharmacological mechanism, which could contribute to the new drug discovery.