Search results for "ANALOGS"
showing 10 items of 53 documents
Dynamics of Ca2+ and guanosine 5'-[gamma-thio]triphosphate action on insulin secretion from alpha-toxin-permeabilized HIT-T15 cells.
1994
The time course of Ca2+ and GTP-analogue effects on insulin secretion was investigated in HIT-T15 cells permeabilized with Staphylococcus alpha-toxin. These cells responded to Ca2+ in the range 0.1-10 microM and could be used in a dynamic perifusion system because of the minimal run-down of the secretory response. High Ca2+ (10 microM) elicited a monophasic ATP-dependent stimulation of insulin secretion that reached a peak within 5 min (approximately 20-fold increase) and rapidly decreased during the subsequent 15 min to a plateau remaining above basal rates (0.1 microM Ca2+). The decrease in Ca(2+)-induced insulin secretion with time could not be attributed to decreased capacity to respond…
Retarding Chronic Kidney Disease (CKD) Progression: A Practical Nutritional Approach for Non-Dialysis CKD
2016
This is a case report on a patient with non-dialysis chronic kidney disease (CKD) in whom several nutritional issues are briefly discussed from a practical point of view. The article is accompanied by an editorial published in this Journal in relation to the 2nd International Conference of the European Renal Nutrition working group at ERA-EDTA—“Retarding CKD progression: readily available through comprehensive nutritional management?”— and focuses on several practical topics associated with the nutritional approach for the conservative treatment of non-dialysis CKD. The article is divided into 3 sections—basic nutritional assessment, nutritional targets, and nutritional follow-up in non-di…
On/Off Photoswitching in a Cyanide-Bridged {Fe2Co2} Magnetic Molecular Square
2013
International audience; A repeatable bidirectional paramagnetic ↔ diamagnetic photomagnetic effect has been observed in the cyanide-bridged Fe-Co square complex {[Fe{B(pz)(4)}(CN)(3)](2)[Co(bik)(2)](2)}(ClO(4))(2)*3H(2)O [B(pz)(4) = tetrapyrazolylborate, bik = bis(1-methylimidazol-2-yl)ketone]. Magnetic measurements and low-temperature single-crystal X-ray diffraction experiments have shown that a complete electron transfer from the diamagnetic Fe(II)-Co(III) state to the paramagnetic Fe(III)-Co(II) metastable state is induced by 808 nm laser light irradiation, whereas the diamagnetic state is recovered in an almost quantitative yield under irradiation at 532 nm.
Addressing subphthalocyanines and subnaphthalocyanines features relevant to fluorescence imaging
2018
International audience; A series of new synthetic subphthalocyanines bear structural features aimed at allowing either fluorescence activation or a bathochromic shift of the absorption band towards the near-infrared window, relevant to optical imaging. X-ray diffraction studies of four subphthalocyanines are reported. Spectrofluorimetric studies on subnaphthalocyanines and activatable subphthalocyanine pro-fluorophores are reported.
Opioid epidemic spread from Northern and Eastern Europe to Mediterranean Area.
2021
The addiction to illicit opioid and the misuse of prescription synthetic opioids pain relievers and fentanyl analogs generated an opioid epidemic in North America over the last two decades that affected public health with a constantly rising number of overdoses deaths. This health treat moved to Europe with a significant increase starting from 2015 involving mainly norther and eastern countries and finally also the Mediterranean area. The "lock down" isolation and economic recession caused by COVID-19 pandemic showed a resurgence in opioid use and harms.
Isolation and purification of enniatins A, A1, B, B1, produced by Fusarium tricinctum in solid culture, and cytotoxicity effects on Caco-2 cells
2010
Enniatins (ENs) are antibiotic compounds of hexadepsipeptidic structure produced by several strains of Fusarium spp. The ENs A, A(1), B, B-1 were purified from extracts of Fusarium tricinctum grown on a solid medium of corn, by a low pressure liquid chromatography (LPLC) on reverse phase of Amberlite XAD-7 followed by semipreparative LC. The purity and the structure of the isolated compounds were confirmed by LC-MS/MS. The technique of the purification of the fungal extract enabled complete separation of the ENs A, A(1), B, B-1 with a mean purity of 97% for all the compounds. The cytoxicity of the ENs was tested in the cell lines of human origin (epithelial colorectal adenocarcinoma cells, …
Reproductive effects in German cockroaches by ecdysteroid agonist RH-0345, juvenile hormone analogue methoprene and carbamate benfuracarb
2004
1379-1176 (Print) Journal Article Research Support, Non-U.S. Gov't; Blatta germanica is the more prevalent cockroach species in Algeria. In the present study, we tested the effect on reproduction in B. germanica of two insect growth regulators, RH-0345, a benzoylhydrazine analogue that mimics the action of 20-hydroxyecdysone, and methoprene, one of the most commercially important juvenile hormone analogues, and a novel carbamate insecticide, benfuracarb. The compounds were applied topically (10 and 20 microg/insect for RH-0345, and 1 and 10 microg/insect for methoprene) or orally administrated (at 2% for benfuracarb) on newly emerged females and evaluated on reproductive events during the a…
1,2,4-Oxadiazole topsentin analogs as staphylococcal biofilm inhibitors targeting the bacterial transpeptidase sortase A
2020
The inhibition or prevention of biofilm formation represents an emerging strategy in the war against antibiotic resistance, interfering with key players in bacterial virulence. This approach includes the inhibition of the catalytic activity of transpeptidase sortase A (Srt A), a membrane enzyme responsible for covalently attaching a wide variety of adhesive matrix molecules to the peptidoglycan cell wall in Gram-positive strains. A new series of seventeen 1,2,4-oxadiazole derivatives was efficiently synthesized and screened as potential new anti-virulence agents. The ability of inhibiting biofilm formation was evaluated against both Gram-positive and Gram-negative pathogens. Remarkably, all…
Pt(II) complex @mesoporous silica: preparation, characterization and study of release
2016
Cisplatin analogs, having cytotoxic activity higher than that exerted by cisplatin, have recently triggered considerable interest by the community. The cis-[PtCl2(DMSO)HL]·2DMSO, where HL = 7-amino-2-(methylthio)[1,2,4]triazolo[1,5-a]pyrimidine-6-carboxylic acid, has shown a potent cytotoxic activity on HepG2 hepatocarcinoma cells, while under identical conditions, it did not affect normal immortalized human liver cells (Chang). In this work, the above complex has been incorporated into MCM41 mesoporous silica, pure and functionalized with amino group, which is considered one of the best host for a drug delivery system for carrying high dosages of a variety of drugs in their mesopores. Sinc…
Temporally precise control of single-neuron spiking by juxtacellular nanostimulation
2017
Temporal patterns of action potentials influence a variety of activity-dependent intra- and intercellular processes and play an important role in theories of neural coding. Elucidating the mechanisms underlying these phenomena requires imposing spike trains with precisely defined patterns, but this has been challenging due to the limitations of existing stimulation techniques. Here we present a new nanostimulation method providing control over the action potential output of individual cortical neurons. Spikes are elicited through the juxtacellular application of short-duration fluctuating currents (“kurzpulses”), allowing for the sub-millisecond precise and reproducible induction of arbitr…