Search results for "General Pharmacology"

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

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…

Effects of dexamethasone on human synovial fibroblast-like cells, from osteoarthritic joints, in culture.

1990

The effect of Dexamethasone (DEX) on cell division and macromolecular synthesis was investigated in a line (McCoy cells, A 9) of synovial fibroblast-like cells derived from human osteoarthritic joints. DEX markedly reduced the proliferation of McCoy cells in a time and dose-dependent manner. The maximal inhibition (45%) was found at 500 nM DEX 24 h after incubation and was accompanied by the appearance of giant macrophage-like cells. After DEX treatment cells showed increased content of DNA, proteins and RNA together with the reduction of [3H]-thymidine incorporation into the TCA-precipitable fraction.

Variations in the Chemical Composition of the Essential Oil of Lavandula angustifolia Mill., Moldoveanca 4 Romanian Variety

2020

International audience; In this research, the variations in the chemical composition of the Lavandula angustifolia Mill. essential oil, the Romanian variety Moldoveanca 4, obtained from the same culture, in the same harvesting and extraction conditions, during the years 2016-2018, representing the years 2-4 of culture. Lavandula angustifolia Mill. flowers were supplied from an ecological-crops from N-E Romania and the essential oils were obtained by hydro distillation of freshly harvested flowers. To determine the chemical composition, the essential oil was semi-quantitatively analysed by using gas chromatography coupled with mass spectrometry (GC-MS). In all the samples, 30 organic compoun…

Nitric oxide metabolism is impaired by type 1 diabetes and diabetic nephropathy

2020

Diabetes leads to reduced nitric oxide bioavailability, resulting in endothelial dysfunction. However, overproduction of nitric oxide due to hyperglycaemia is associated with oxidative stress and tissue damage. The objective of this study was to characterise nitric oxide production (NO) and added nitrite and nitrate (NO(2)(-)+NO(3)(-)) concentration in the blood and urine of patients with and without diabetic nephropathy. A total of 268 patients with type 1 diabetes and 69 healthy subjects were included. Diabetic nephropathy was defined as macroalbuminuria and/or estimated glomerular filtration rate below 60 ml/min/1.73 cm(2). NO(2)(-)+NO(3)(-) concentration was measured by Griess reaction.…

Receptor-mediated uptake of boron-rich neuropeptide y analogues for boron neutron capture therapy.

2014

Peptidic ligands selectively targeting distinct G protein-coupled receptors that are highly expressed in tumor tissue represent a promising approach in drug delivery. Receptor-preferring analogues of neuropeptide Y (NPY) bind and activate the human Y1 receptor subtype (hY1 receptor), which is found in 90% of breast cancer tissue and in all breast-cancer-derived metastases. Herein, novel highly boron-loaded Y1 -receptor-preferring peptide analogues are described as smart shuttle systems for carbaboranes as (10) B-containing moieties. Various positions in the peptide were screened for their susceptibility to carbaborane modification, and the most promising positions were chosen to create a mu…