Theoretical and Experimental Study of Molecular Interactions of Fluralaner with Lipid Membranes.

Fluralaner is a relatively new insecticide belonging to the isoxazoline group, whose action mechanism involves the blocking of GABA-receptors in the insect nervous system. Because of its high hydrophobicity, fluralaner could bioaccumulate and reach toxic local concentrations. Since there are no data available about the penetration and persistence of isoxazolines in biological membranes, we intend to evaluate fluralaner permanence as a pollutant by using model membranes.

The insecticide fipronil affects the physical properties of model membranes: A combined experimental and molecular dynamics simulations study in Langmuir monolayers.

Fipronil is a widely used commercial insecticide whose action mechanism consists in blocking the influx of chloride ions through the γ-aminobutyric acid type A receptor (GABA-R), an integral membrane protein. The present study investigates the interaction of fipronil with phospholipid Langmuir monolayers, in order to characterize the effects that its partition could exert on the physical properties of these model membranes. A combined experimental and molecular dynamics (MD) simulations approach was performed.

Promising Chitosan-Coated Alginate-Tween 80 Nanoparticles as Rifampicin Coadministered Ascorbic Acid Delivery Carrier Against Mycobacterium tuberculosis.

The aim of this study was to design a nanocarrier system for inhalation delivery of rifampicin (RIF) in combination with ascorbic acid (ASC), namely constituted of sodium alginate coated with chitosan and Tween 80 (RIF/ASC NPs) as a platform for the treatment of pulmonary tuberculosis infection. A Box-Behnken experimental design and response surface methodology (RSM) were applied to elucidate and evaluate the effects of several factors on the nanoparticle properties. On the other hand, it was found that RIF/ASC NPs were less cytotoxic than the free RIF, showing a significantly improved activity against nine clinical strains of Mycobacterium tuberculosis (M.

Interaction of gabaergic ketones with model membranes: A molecular dynamics and experimental approach.

γ-Aminobutyric-acid receptor (GABA-R), a membrane intrinsic protein, is activated by GABA and modulated by a wide variety of recognized drugs. GABA-R is also target for several insecticides which act by recognition of a non-competitive blocking site. Mentha oil is rich in several ketones with established activity against various insects/pests.

Effects of Insecticidal Ketones Present in Mint Plants on GABA Receptor from Mammalian Neurons.

Background: The genus , an important member of the family, is represented by many species commonly known as mint. The insecticidal activity of oil and its main components has been tested and established against various insects/pests. Among these, the ketone monoterpenes that are most common in different species demonstrated insect toxicity, with pulegone being the most active, followed by carvone and menthone.

Membrane effects of dihydropyrimidine analogues with larvicidal activity.

Two recently synthesized dihydropyrimidines (DHPMs) analogues have demonstrated larvicide and repellent activity against Anopheles arabiensis. DHPMs high lipophilicity suggests that these compounds may interact directly with the membrane and modify their biophysical properties. The purpose of the present study was to characterize the interaction of both compounds with artificial membranes.

Effects of bioactive monoterpenic ketones on membrane organization. A langmuir film study.

The cyclic ketones, thujone and dihydrocarvone, are lipophilic components of essential oils extracted from different plants, which have proven insecticidal activity. The GABAA receptor is activated by the neurotransmitter GABA and is the action site of widely used neurotoxic pesticides. Many compounds that regulate GABAA receptor function interact with membrane lipids, causing changes in their physical properties and consequently, in the membrane dynamic characteristics that modulate receptor macromolecules.

Synthesis, Polymorphism, and Insecticidal Activity of Methyl 4-(4-chlorophenyl)-8-iodo-2-methyl-6-oxo-1,6-dihydro-4H-pyrimido[2,1-b]quinazoline-3-Carboxylate Against Anopheles arabiensis Mosquito.

Mosquitoes are the major vectors of pathogens and parasites including those causing malaria, the most deadly vector-borne disease. The negative environmental effects of most synthetic compounds combined with widespread development of insecticide resistance encourage an interest in finding and developing alternative products against mosquitoes. In this study, pyrimido[2,1-b]quinazoline derivative DHPM3 has been synthesized by three-step chemical reaction and screened for larvicide, adulticide, and repellent properties against Anopheles arabiensis, one of the dominant vectors of malaria in Africa.

Effect of beta-adrenoceptors on the behaviour induced by the neuropeptide glutamic acid isoleucine amide.

Excessive grooming behaviour is induced by intracerebroventricular injections of the neuropeptide glutamic acid isoleucine amide (neuropeptide-EI), via the activation of A-10 dopaminergic neurons and the noradrenergic system. Our object was to study the latter system involved in these behaviours, using male Wistar rats weighing 250-300 g with i.c.