Search results for " Pharmaceutic"

The Quest for Mononuclear Gold(II) and Its Potential Role in Photocatalysis and Drug Action.

2017

The chemistry of gold strongly focuses on the ubiquitous oxidation states +I and +III. The intermediate oxidation state +II is generally avoided in mononuclear gold species. In recent years, gold(II) has been increasingly suggested as a key intermediate in artificial photosynthesis systems, with gold(III) moieties acting as electron acceptors, as well as in gold-catalyzed photoredox catalysis and radical chemistry. This Minireview provides a concise summary of confirmed and characterized mononuclear open-shell gold(II) complexes. Recent findings on structural motifs and reactivity patterns will be discussed. Exciting developments in the fields of photosynthesis, photocatalysis, and potentia…

Synthesis of dehydrodipeptide esters and their evaluation as inhibitors of cathepsin C

2015

The procedures for the synthesis of esters of dehydropeptides containing C-terminal (Z)-dehydrophenylalanine and dehydroalanine have been elaborated. These esters appeared to be moderate or weak inhibitors of cathepsin C, with some of them exhibiting slow-binding behavior. As shown by molecular modeling, they are rather bound at the surface of the enzyme and are not submersed in its binding cavities. Electronic supplementary material The online version of this article (doi:10.1007/s00044-015-1366-0) contains supplementary material, which is available to authorized users.

Cavernolide

2000

Abstract The inhibitory effect of cavernolide, a novel C 21 terpene lactone isolated from the sponge Fasciospongia cavernosa , on PLA 2 and other enzyme activities involved in the inflammatory process was studied. Cavernolide inhibited human synovial sPLA 2 in a concentration-dependent manner with an IC 50 value of 8.8 μM. Besides, this compound decreased in the nanomolar range the myeloperoxidase degranulation process using different stimuli. Cavernolide also inhibited TNFα, NO and PGE 2 production in intact cell experiments. NO and PGE 2 reduction was the consequence of the inhibition on iNOS and COX-2 expression because it did not affect inducible nitric oxide synthase and cyclooxygenase…

In vivo anti-inflammatory activity of saponins from Bupleurum rotundifolium

2001

Seven oleanane-type triterpene saponins were isolated from the methanolic extract of the aerial parts of Bupleurum rotundifolium. They were identified on the basis of their spectral data as 3-O-[alpha-L-rhamnopyranosyl (1--2)-beta-D-glucopyranosyl (1--2)-beta-D-glucopyranosyl]-28-O-[beta-D-glucopyranosyl (1--2)-beta-D-glucopyranosyl] echinocystic acid (saponin 1), 3-O-[alpha-L-rhamnopyranosyl (1--2)-beta-D-glucopyranosyl (1--2)-beta-D-fucopyranosyl] 11-methoxy-primulagenin A (saponin 2), rotundioside E (saponin 3), rotundioside F (saponin 4), 3beta-sulfate, 28-O-[beta-D-glucopyranosyl (1--6)-beta-D-glucopyranosyl (1--2)-beta-D-glucopyranosyl (1--2)-beta-D-glucopyranosyl] ester of primulagen…

Characterization of intestinal absorption of C -glycoside flavonoid vicenin-2 from Lychnophora ericoides leafs in rats by nonlinear mixed effects mod…

2015

Vicenin-2 (apigenin-6,8-di-C-β-d-glucopyranoside) is present in hydroalcoholic extracts of the Brazilian species Lychnophora ericoides Mart., Asteraceae, leaves, and the biological effects of this compound have been demonstrated including anti-inflammatory, antioxidant and anti-tumor effects in rat models. Given the potential of this compound as a pharmacological agent, the aims of this investigation were to evaluate the extent of intestinal absorption of vicenin-2, and to determine the intestinal permeation profile using an in situ single-pass intestinal perfusion technique. A validated HPLC–UV method was applied to measure the amount of unabsorbed vicenin-2 in the gut after an oral admini…

Corrigendum to “Effects of Oleuropein on tumor cell growth and bone remodeling: Potential clinical implications for the prevention and treatment of m…

2021

Enzyme replacement and gene therapy for mucopolysaccharidoses: current progress and future directions

2015

Introduction: Mucopolysaccharidoses (MPS) are lysosomal storage disorders caused by the deficiency of enzymes that are responsible for the stepwise degradation of complex carbohydrates, the glycosaminoglycans. Whereas in the past the treatment of MPS consisted mainly of palliative care, enzyme replacement therapy (ERT) is now possible for some MPS disorders, and in the future many other therapeutic options will become available.Areas covered: This review, based on personal experience and the currently available literature, will give an overview on the efficacy and limitations of ERT and will discuss new therapeutic approaches, such as anti-inflammatory drugs, substrate reduction therapy, ch…

Lonoctocog alfa (rVIII-SingleChain) for the treatment of haemophilia A

2017

Introduction: The administration of factor VIII (FVIII) concentrates on-demand or on long-term prophylaxis is the effective and safe standard of care of patients with hemophilia A (HA). Development of neutralizing antibodies against exogenous FVIII and the short half-life of the current available products remain major challenges. There is currently a great interest towards newer FVIII products with the goal of reducing the inhibitor risk and increasing the half-life. Area covered: In this review, the authors describe the efficacy and safety of rVIII-SingleChain (Lonoctocog alfa), the first and only single chain recombinant FVIII (rFVIII) molecule developed for the prevention and treatment o…

Contractile Reserve in Heart Failure with Preserved Ejection Fraction.

2022

Background: Diastolic stress echocardiography (SE) is useful for confirming the diagnosis of heart failure with preserved left ventricular ejection fraction (HFpEF) when it is uncertain. The aim of this study was to assess the value of new echocardiographic parameters during diastolic SE in patients with dyspnea and suspected HFpEF. Methods: Sixty-two patients with exertional dyspnea and inconclusive rest echocardiography for a diagnosis of HFpEF were enrolled. Exercise SE was performed in all patients. Contractile reserve (LVCR) was assessed by measuring: 1. changes in the left ventricular ejection fraction (LVEF) between rest and peak stress; 2. stress-to-rest ratio of force (force was de…

Towards Translational ImmunoPET/MR Imaging of Invasive Pulmonary Aspergillosis: The Humanised Monoclonal Antibody JF5 Detects Aspergillus Lung Infect…

2017

Invasive pulmonary aspergillosis (IPA) is a life-threatening lung disease of hematological malignancy or bone marrow transplant patients caused by the ubiquitous environmental fungus Aspergillus fumigatus. Current diagnostic tests for the disease lack sensitivity as well as specificity, and culture of the fungus from invasive lung biopsy, considered the gold standard for IPA detection, is slow and often not possible in critically ill patients. In a previous study, we reported the development of a novel non-invasive procedure for IPA diagnosis based on antibody-guided positron emission tomography and magnetic resonance imaging (immunoPET/MRI) using a [64Cu] DOTA-labeled mouse monoclonal anti…