Uncompetitive nanomolar dimeric indenoindole inhibitors of the human breast cancer resistance pump ABCG2.

Multidrug resistance membrane pumps reduce the efficacy of chemotherapies by exporting a wide panel of structurally-divergent drugs. Here, to take advantage of the polyspecificity of the human Breast Cancer Resistance Protein (BCRP/ABCG2) and the dimeric nature of this pump, new dimeric indenoindole-based inhibitors from the monomeric α,β-unsaturated ketone 4b and phenolic derivative 5a were designed. A library of 18 homo/hetero-dimers was synthesised.

Ninhydrins inhibit carbonic anhydrases directly binding to the metal ion.

Ninhydrins show extensive application in organic chemistry and agriculture whereas they have been poorly investigated as bioactive molecules for medicinal chemistry purposes. A series of ninhydrin derivatives was here investigated for the inhibition of human carbonic anhydrases (CAs, EC 4.2.

Eco-friendly synthesis of self-regenerative low-cost biosorbent by the incorporation of CuO: a photocatalyst sensitive to visible light irradiation for azo dye removal.

Acid pretreated biomass Lemna minor (BM-HPO) was used as support for CuO nanoparticles loading, to investigate the dye biosorption capacity and the photocatalytic performance under artificial visible light. The surface morphology, crystal structure, elemental composition, and the bandgap of modified biomass have been determined using FE-SEM, XRD, EDX, XPS, FTIR, and UV-DR analysis. The results showed that NH and P-O functional groups of (BM-HPO) can attract the copper ions (Cu), which can facilitate the loading of CuO nanoparticles hence, smaller nanoparticles with an average diameter of 21 nm was obtained.

Chemical characterisation, hypoglycaemic and renoprotective effects of aqueous leaf extract of on fructose-induced metabolic syndrome in rats.

In the present study, we chemically characterised the aqueous leaf extract of by HPLC-TOF/MS and evaluated its effects on fructose-induced metabolic syndrome (MetS) in Wistar rats. MetS groups were given (10% w/v) fructose solution to drink for 9 weeks, whereas, normal animals received ordinary water. LG extract was administrated to treated groups by gavage for the last 6 weeks of the experimental period.

Occurrence and characterization of surface sediment microplastics and litter from North African coasts of Mediterranean Sea: Preliminary research and first evidence.

The aim of this research work is to investigate the abundance of macroplastics and microplastics from North African coasts of Mediterranean Sea in the Gulf of Annaba (Algeria). The study areas are well known for the high population and high industrial activities that can contribute to the plastic pollution. In this case, microplastics were sampled from the surface sediments at four different stations representing different local activities.

QSAR Model of Indeno[1,2-]indole Derivatives and Identification of -isopentyl-2-methyl-4,9-dioxo-4,9-Dihydronaphtho[2,3-]furan-3-carboxamide as a Potent CK2 Inhibitor.

Casein kinase II (CK2) is an intensively studied enzyme, involved in different diseases, cancer in particular. Different scaffolds were used to develop inhibitors of this enzyme. Here, we report on the synthesis and biological evaluation of twenty phenolic, ketonic, and -quinonic indeno[1,2-]indole derivatives as CK2 inhibitors.

aqueous extract improves insulin sensitivity and hepatic steatosis in rodent model of fructose-induced metabolic syndrome.

Context: Fructose consumption is associated with the development of obesity and metabolic syndrome (MetS) in human and animal models.

Objective: This study investigates the ability of an aqueous extract of Asso (AH) to ameliorate fructose-induced MetS in Male Wistar rats.

Methods: AH extract at doses of 100, 200 and 400 mg/kg b.

Detection and classification of bearing faults in industrial geared motors using temporal features and adaptive neuro-fuzzy inference system.

This paper concerns the automatic diagnosis of ball bearing defects in industrial geared motor based on statistical indicators and the Adaptive Neuro-Fuzzy Inference System (ANFIS). The approach consists of three essential steps: the first is the extraction of statistical indicators from the root mean square (RMS) of the raw vibration signals measured experimentally for different states of the bearing (healthy and in the presence of defects). The second step consists of the selection of the more relevant indicators, and finally the introduction of these indicators to the ANFIS network in order to classify the various defects in the bearing (inner and outer race faults, and combined fault).

Using photoactivated acetone for the degradation of Chlorazol Black in aqueous solutions: Impact of mineral and organic additives.

This study examined the effect of different mineral and organic additives on the degradation of Chlorazol Black (CB, 25.5 μM) in aqueous media by UV/acetone process. Initially, it was found that acetone (50 mM)-assisted UV irradiation accelerated the CB removal within 30 min to 98% against 34% for the sole UV, presumably due to the implication of methyl radicals in the degradation process as confirmed by O saturation and nitrite addition (as CH-specific scavengers).

Chirocephalus sanhadjaensis sp. nov., a new chirocephalid species (Branchiopoda: Anostraca) from Numidia (Algeria).

A new species of Chirocephalus collected in temporary freshwater ponds in Northeastern Algeria is described. Chirocephalus sanhadjaensis sp. nov.

Intensification of light green SF yellowish (LGSFY) photodegradion in water by iodate ions: Iodine radicals implication in the degradation process and impacts of water matrix components.

The results of this work showed that UV/IO oxidation process supplies good performance in the degradation of light green SF yellowish (LGSFY) dye in deionized water. This process generated reactive iodine radicals that make the degradation much faster than the sole UV irradiation. The assistance of UV-irradiation by 10 mM of iodate increased the LGSFY removal after 10 min from 36% to 90% for C = 10 mg/L and from 18% to 85% for C = 20 mg/L.

Impact of seawater salinity on the sonochemical removal of emerging organic pollutants.

The results presented in this study illustrate the multiple roles of seawater salinity toward the sonochemical degradation, at variable frequencies (300-1700 kHz), of several hazardous substances, i.e. propylparaben (PPR) endocrine disruptor and several synthetic dyes: naphthol blue black (NBB), malachite green (MG), basic red 29 (BR29), acid orange 7 (AO7), Rhodamine B (RhB) and basic fuchsin (BF).

Colistin- and Carbapenem-Resistant Klebsiella pneumoniae Clinical_Isolates: Algeria.

This study investigates the molecular mechanisms of colistin and carbapenem resistance in Klebsiella pneumoniae ST101 strains. The three K. pneumoniae carried bla, bla, and bla genes and two coharbored bla.

Insecticidal effects of the Olea europaea subsp. laperrinei extracts on the flour Pyralid Ephestia kuehniella.

In the present study, the aerial parts of the Laperrine olive (Olea europaea subsp. Laperrinei) are subjected to acid extraction and the chemical composition of the extracts is determined by HPLC-DAD. The main compounds found in all of extracts are: hydroxytyrosol (30.

Numerical investigation of the effect of dual frequency sonication on stable bubble dynamics.

A computational study aiming to simulate an oxygen single acoustic bubble oscillation under a dual-frequency sonication was presented in this paper. The non-linear response of the bubble to the superposition of two fields of ultrasonic waves was investigated through dynamics parameters, collapse ratios and average velocities. The main goal of this analyze is to link the properties of the wave resulting from the dual-frequency excitation to the dynamics behavior of the bubble.

Conservation of stored food using plant's extracts. Effect of oregano (Origanum vulgaris) essential oils on the reproduction and development of flour moth (Ephestia kuehniella).

In the search for effective methods of biological control of stored products insect-pests, the essential oil of Origanum vulgaris was extracted using Clevenger apparatus and tested on reproduction and mortality of flour moth Ephestia kuehniella. Bio-insecticide works with a double action mechanism; administered by inhalation in pupae, essential oil affects their pupal development. It also disrupts the reproduction of exuviated adults by extending the preoviposition period and reducing the period of egg laying and fecundity because fecundated females cannot live more than four days compared to control group.

Depth effect on the inertial collapse of cavitation bubble under ultrasound: Special emphasis on the role of the wave attenuation.

Acoustic cavitation concentrates and releases a very large amount of energy in localized areas, which can be used for many physical and chemical processes. Even though acoustic cavitation has been studied widely for decades in lab-scale sonoreactors, only few studies have been devoted to characterize this event in big-scale sonoreactors, where the liquid depth may have a critical influence on the bubble collapse. The present computational study furnished numerical data about the effect of depth (z = 0-10 m) on acoustic cavitation with special focus on the role of attenuation of the ultrasound wave on the dramatic conditions developed within bubbles at collapse.

Synthesis, Spectroscopic Characterization, and Antibacterial Evaluation of Novel Functionalized Sulfamidocarbonyloxyphosphonates.

Several new sulfamidocarbonyloxyphosphonates were prepared in two steps, namely carbamoylation and sulfamoylation, by using chlorosulfonyl isocyanate (CSI), α-hydroxyphosphonates, and various amino derivatives and related (primary or secondary amines, β-amino esters, and oxazolidin-2-ones). All structures were confirmed by ¹H, C, and P NMR spectroscopy, IR spectroscopy, and mass spectroscopy, as well as elemental analysis. Eight compounds were evaluated for their antibacterial activity against four reference bacteria including Gram-positive (ATCC 25923), and Gram-negative (ATCC 25922), (ATCC 700603), (ATCC 27853), in addition to three clinical strains of each studied bacterial species.

Modelling environment contamination with heavy metals in flathead grey mullet Mugil cephalus and upper sediments from north African coasts of the Mediterranean Sea.

Heavy metals are a serious hazard for aquatic ecosystems and human health. They negatively affect aquatic life functioning through accumulation resulting physiological/growth disturbances in aquatic lifeforms. This survey focused on the assessment of heavy metal pollution in the Gulf of Annaba (northeastern Algeria), the largest and most diversified industrial hub in Africa, using a multi-compartment approach (water-sediment-biota).

An annotated checklist of the Algerian Cladocera (Crustacea: Branchiopoda).

We present an annotated checklist of the Cladocera (orders Ctenopoda and Anomopoda) from the continental waters of Algeria, based on published records and original data from analysis of samples from 112 water bodies collected in 2012-2016 in humid and semi-arid regions of the country. Thirty six species have been identified in this study. Three taxa (Daphnia obtusa, D.

Dentists' intention to report suspected violence: a cross-sectional study in eight Arab countries.

Objectives: This study assessed dentists' intention in eight Arab countries to report suspected exposure to violence among patients and factors associated with this intention based on the theory of planned behaviour.

Methods: A cross-sectional study was conducted in 2016 including a convenience sample of dentists practising in public, private and academic sectors in Algeria, Egypt, Jordan, Kuwait, Libya, Palestine, Saudi Arabia and Yemen. Respondents answered a self-administered questionnaire collecting information about personal and professional background and perceived ability to identify victims of violence.

Insights into numerical simulation of controlled ultrasonic waveforms driving single cavitation bubble activity.

A computational study treating cavitation phenomenon within a single bubble undergoing various controlled ultrasonic waveforms is presented in this paper. Numerical simulations using sinusoidal, square, triangular and sawtooth waves crossing an aqueous media, saturated with oxygen, are conducted upon various operational conditions of frequency and amplitude. Bubble radius, temperature and pressure were estimated over time for 64 combined cases.

Ultrasonic waveform upshot on mass variation within single cavitation bubble: Investigation of physical and chemical transformations.

The mechanical disturbance created by an ultrasonic wave travelling through a liquid medium induces the formation of cavitation that oscillates due to rarefaction and compression of the wave. The duration and the magnitude of the pressure applied by the ultrasonic wave at each instant would generate a specific impact on the variation of the bubble radius, the temperature, the pressure and the mass inside it. In this paper, a numerical study is conducted to simulate four waveforms (sinusoidal, square, triangular and sawtooth) travelling an aqueous media saturated with oxygen with an amplitude of 1.

Isolation, purification, structural elucidation and antimicrobial activities of kocumarin, a novel antibiotic isolated from actinobacterium Kocuria marina CMG S2 associated with the brown seaweed Pelvetia canaliculata.

Aims: Screening of seaweed-associated bacteria capable of producing antimicrobials.

Methods And Results: Fifteen microbial strains, associated to the brown seaweed Pelvetia canaliculata (Linnaeus) attached to the rocks of Sonmiani Beach (Karachi, Pakistan), were screened. Crude extract filtrates of CMG S2 strain grew on Zobell marine agar (ZMA) had the most remarkable antimicrobial activity.