排序方式： 共有5条查询结果，搜索用时 15 毫秒
1
1.
Quentin Coquerel Claire Legendre Jacinthe Frangieh Stephan De Waard Jrme Montnach Leos Cmarko Joseph Khoury Charifat Said Hassane Dimitri Brard Benjamin Siegler Ziad Fajloun Harold De Pomyers Kamel Mabrouk Norbert Weiss Daniel Henrion Pascal Richomme Csar Mattei Michel De Waard Anne-Marie Le Ray Christian Legros 《Molecules (Basel, Switzerland)》2022,27(13)
Voltage-gated Na+ (NaV) channels are significant therapeutic targets for the treatment of cardiac and neurological disorders, thus promoting the search for novel NaV channel ligands. With the objective of discovering new blockers of NaV channel ligands, we screened an In-House vegetal alkaloid library using fluorescence cell-based assays. We screened 62 isoquinoline alkaloids (IA) for their ability to decrease the FRET signal of voltage sensor probes (VSP), which were induced by the activation of NaV channels with batrachotoxin (BTX) in GH3b6 cells. This led to the selection of five IA: liriodenine, oxostephanine, thalmiculine, protopine, and bebeerine, inhibiting the BTX-induced VSP signal with micromolar IC50. These five alkaloids were then assayed using the Na+ fluorescent probe ANG-2 and the patch-clamp technique. Only oxostephanine and liriodenine were able to inhibit the BTX-induced ANG-2 signal in HEK293-hNaV1.3 cells. Indeed, liriodenine and oxostephanine decreased the effects of BTX on Na+ currents elicited by the hNaV1.3 channel, suggesting that conformation change induced by BTX binding could induce a bias in fluorescent assays. However, among the five IA selected in the VSP assay, only bebeerine exhibited strong inhibitory effects against Na+ currents elicited by the hNav1.2 and hNav1.6 channels, with IC50 values below 10 µM. So far, bebeerine is the first BBIQ to have been reported to block NaV channels, with promising therapeutical applications. 相似文献
2.
Jacinthe Frangieh Mohamad Rima Ziad Fajloun Daniel Henrion Jean-Marc Sabatier Christian Legros Csar Mattei 《Molecules (Basel, Switzerland)》2021,26(8)
Cardiovascular diseases (CVDs) are considered as a major cause of death worldwide. Therefore, identifying and developing therapeutic strategies to treat and reduce the prevalence of CVDs is a major medical challenge. Several drugs used for the treatment of CVDs, such as captopril, emerged from natural products, namely snake venoms. These venoms are complex mixtures of bioactive molecules, which, among other physiological networks, target the cardiovascular system, leading to them being considered in the development and design of new drugs. In this review, we describe some snake venom molecules targeting the cardiovascular system such as phospholipase A2 (PLA2), natriuretic peptides (NPs), bradykinin-potentiating peptides (BPPs), cysteine-rich secretory proteins (CRISPs), disintegrins, fibrinolytic enzymes, and three-finger toxins (3FTXs). In addition, their molecular targets, and mechanisms of action—vasorelaxation, inhibition of platelet aggregation, cardioprotective activities—are discussed. The dissection of their biological effects at the molecular scale give insights for the development of future snake venom-derived drugs. 相似文献
3.
A. Dhenain M. R. Frangieh A. J. Bougrine H. Delalu 《Journal of Thermal Analysis and Calorimetry》2013,113(2):947-954
This work involves the study of the solid/liquid equilibrium in the NaCl–NaOH–H2O ternary system. The aim is to optimize the operating conditions of an evaporator–crystallizer used in a hydrazine extraction process. The latter is conducted at industrial scale using the Raschig method, a general method for preparing hydrazines for aerospace and pharmaceutical applications. The extraction process includes the use of a Kestner type evaporator–crystallizer to first isolate hydrazine and water by evaporation and then separate two salts: sodium hydroxide, recovered as an aqueous solution, and sodium chloride which crystallizes. However, problems related to the co-precipitation of NaCl–NaOH may be encountered in industry, leading to the clogging of installations. Therefore, it is necessary to ensure that only NaCl crystallizes while maintaining NaOH in liquid state. Knowledge of the equilibrium phases of the NaCl–NaOH–H2O ternary system is thus required, particularly the liquid/solid phase. Phase equilibrium experiments were performed by isoplethic thermal analysis (ITA) and chemical titrations over the temperature range of 313 to 353 K at atmospheric pressure. ITA is an isobaric and isothermal method developed in our laboratory and based on the measurement of the thermal effects associated with transformations in a system (appearance or disappearance of a phase) when its composition is changed. The NaCl crystallization domain was fully determined and the operating parameters of the device were defined precisely as a function of temperature and composition of the Kestner loop. 相似文献
4.
G. Frangieh M.‐A. Pinault J. Barjon T. Tillocher F. Jomard J. Chevallier 《physica status solidi (a)》2010,207(8):2003-2003
5.
Bougrine Anne-Julie Renault Anne Frangieh Marie-Rose Darwich Chaza 《Journal of Thermal Analysis and Calorimetry》2022,147(12):6869-6881
Journal of Thermal Analysis and Calorimetry - The present study was carried out in the frame of the optimization of the synthesis process of 1,1,4,4-tetramethyl-2-tetrazene (TMTZ), a prospective... 相似文献
1
