Search results for "DISCOVERY"

Fluorescent Probes for Ecto-5′-nucleotidase (CD73)

2020

[Image: see text] Ecto-5′-nucleotidase (CD73) catalyzes the hydrolysis of AMP to anti-inflammatory, immunosuppressive adenosine. It is expressed on vascular endothelial, epithelial, and also numerous cancer cells where it strongly contributes to an immunosuppressive microenvironment. In the present study we designed and synthesized fluorescent-labeled CD73 inhibitors with low nanomolar affinity and high selectivity based on N(6)-benzyl-α,β-methylene-ADP (PSB-12379) as a lead structure. Fluorescein was attached to the benzyl residue via different linkers resulting in PSB-19416 (14b, K(i) 12.6 nM) and PSB-18332 (14a, K(i) 2.98 nM) as fluorescent high-affinity probes for CD73. These compounds …

Current dental adhesives systems. A narrative review.

2012

Adhesive dentistry is based on the development of materials which establish an effective bond with the tooth tissues. In this context, adhesive systems have attracted considerable research interest in recent years. Successful adhesive bonding depends on the chemistry of the adhesive, on appropriate clinical handling of the material as well as on the knowledge of the morphological changes caused on dental tissue by different bonding procedures. This paper outlines the status of contemporary adhesive systems, with particular emphasis on chemical characteristics and mode of interaction of the adhesives with enamel and dentinal tissues. Dental adhesives are used for several clinical application…

Effect of the basidiomycete Poria cocos on experimental dermatitis and other inflammatory conditions.

1997

The hydroalcoholic extract from P. cocos was examined for oral and topical anti-inflammatory activities. It proved to be active against carrageenan, arachidonic acid, tetradecanoyl phorbol acetate (TPA) acute edemas, TPA chronic inflammation and oxazolone delayed hypersensitivity in mice. Two lanostane-type triterpenes were isolated and identified by spectroscopic methods as dehydrotumulosic and pachymic acids. Their ID50 on acute TPA edema was 4.7 x 10(-3) and 6.8 x 10(-4) mumol/ear, respectively.

Topical anti-inflammatory activity of some Asian medicinal plants used in dermatological disorders.

2001

The topical anti-inflammatory activity of extracts from Cassia angustifolia, Rheum palmatum, Coptis chinensis, Phellodendron amurense and Scutellaria baicalensis, plants used in traditional East Asian medicine against different skin disorders, was studied. Though in different degree, all the extracts significantly inhibited the edema induced by 12-O-tetradecanoylphorbol-13-acetate (TPA), in both single or multiple application, oxazolone, and arachidonic acid (AA). None of the extracts inhibited in vitro the activity of phospholipase A(2) (PLA(2)) from Naja naja.

Pharmacological Interventions on Asymmetric Dimethylarginine, a Clinical Marker of Vascular Disease

2011

The aim of this paper is to review the latest data on the pharmacological modulation of asymmetric dimethylarginine in human disease. When the terminal nitrogens of the guanidine portion of an arginine become methylated through the action of N-methyl transferases, two chemically close, but physiologically different amino acids are synthesized: symmetric and asymmetric dimethylarginine. The vascular origin of asymmetric dimethylarginine and its inhibitory activity on endothelial nitric oxide synthase give it an important role in certain diseases in which microcirculation is compromised: hypertension, atherosclerosis, inflammatory bowel disease, and diabetes. This review discusses the role th…

Triple negative breast cancer: shedding light onto the role of pi3k/akt/mtor pathway

2016

// Daniela Massihnia 1,* , Antonio Galvano 1,* , Daniele Fanale 1 , Alessandro Perez 1 , Marta Castiglia 1 , Lorena Incorvaia 1 , Angela Listi 1 , Sergio Rizzo 1 , Giuseppe Cicero 1 , Viviana Bazan 1 , Sergio Castorina 2,3,** and Antonio Russo 1,** 1 Department of Surgical, Oncological and Oral Sciences, Section of Medical Oncology, University of Palermo, Palermo, Italy 2 Fondazione Mediterranea “G.B. Morgagni”, Catania, Italy 3 Department of Biomedical and Biotechnological Sciences, University of Catania, Catania, Italy * These authors have contributed equally to this work ** Both the authors are last name Correspondence to: Antonio Russo, email: // Keywords : ER, HER2, PI3K/AKT/mTOR inhib…

Application of 1H NMR-based serum metabolomic studies for monitoring female patients with rheumatoid arthritis

2015

AbstractRheumatoid arthritis is a chronic autoimmune-based inflammatory disease that leads to progressive joint degeneration, disability, and an increased risk of cardiovascular complications, which is the main cause of mortality in this population of patients. Although several biomarkers are routinely used in the management of rheumatoid arthritis, there is a high demand for novel biomarkers to further improve the early diagnosis of rheumatoid arthritis, stratification of patients, and the prediction of a better response to a specific therapy.In this study, the metabolomics approach was used to provide relevant biomarkers to improve diagnostic accuracy, define prognosis and predict and mon…

Human immunodeficiency virus infection mimics autoimmune hepatitis--a case report.

1988

Influence of digoxin on sinus node function after pharmacologic autonomic blockade.

1983

The effect of iv digoxin on normal sinus node function was studied after pharmacologic autonomic blockade (AB) in ten patients. Sinus cycle length (SCL), sinus node recovery time (SNRT) and sinoatrial conduction time (SACT) were determined before and after AB with propranolol (0.2 mg/kg body weight) and atropine sulfate (0.04 mg/kg body weight) iv, and 15 min, 30 min, and 45 min after 1 mg iv digoxin. AB resulted in a significant decrease (P less than 0.01) in SCL (916 +/- 158 to 716 +/- 120 ms), in SNRT (1,229 +/- 221 to 871 +/- 190 ms), and in SACT (79 +/- 34 to 44 +/- 10 ms). Fifteen minutes after iv digoxin there was no significant change observed in SCL (716 +/- 120 to 708 +/- 92 ms), …

Comparison of glycemic response and insulin requirements after mixed meals of equal carbohydrate content in healthy, type-1, and type-2 diabetic man

1989

The postprandial insulin requirements after three mixed meals of equal carbohydrate and energy content were assessed in 10 type-1 and 12 type-2 diabetics by a glucose-controlled insulin infusion system. These were compared with the glycemic response to the same meals of 10 healthy individuals (glycemic index). In type-1 diabetics, we found the highest insulin requirements after consumption of a continental breakfast (low fibre, low protein, high fat). Ten percent less insulin was infused after milk (low fat, high protein) and 30% less after an English breakfast (high fibre, high protein). Type-2 diabetics showed no significant differences in insulin requirements between the three test meals…