Composition and Chemical Variability of the Essential Oil from Aerial Parts of Cladanthus scariosus,an Endemic Species to the Moroccan High Atlas

Cladanthus scariosus (Ball) Oberpr. & Vogt is endemic to Moroccan High Atlas. It is known under the vernacular names Irezghi or Irezgui. Three essential oil samples have been isolated from aerial parts and analyzed by combination of chromatographic and spectroscopic techniques [gas chromatography (GC) in combination with retention indices (RI), gas chromatography-mass spectrometry (GC/MS) and ¹³C-NMR spectroscopy]. The compositions of oil samples were dominated by monoterpenes: α-pinene sabinene, and terpinen-4-ol. Chamazulene and dihydrochamazulene isomers as well as various hemiterpene esters and analogs have been identified. To evidence a chemical variability, statistical analysis performed on 13 oil sample compositions allowed partitioning into three groups, mainly differentiated by their contents of sabinene, camphor, borneol, terpinen-4-ol, and germacrene D.     

Design,in Silico Studies and Biological Evaluation of New Chiral Thiourea and 1,3-Thiazolidine-4,5-dione Derivatives

In this study, new chiral thiourea and 1,3-thiazolidine-4,5-dione derivatives were synthesized, it was aimed to evaluate the various biological activities and molecular docking of these compounds. Firstly, the new thioureas ( 1 – 16 ) were obtained by reacting 1-naphthylisothiocyanate with different chiral amines. Then, the chiral thioureas were cyclized with oxalyl chloride to obtain 1,3-thiazolidine-4,5-dione derivatives ( 17 – 32 ). All compounds were evaluated with several in vitro antioxidant and enzyme inhibition activities. Compound 30 was the most active compound against AChE, with a value of IC₅₀=8.09±0.58 μM. On the other hand, all compounds were tested in silico absorption, distribution, metabolism, and excretion (ADME) assays to better understand their bioavailability. These physicochemical properties, pharmacokinetics, and drug-likeness of all compounds were calculated using SwissADME. Furthermore, according to molecular docking analyses compound 30 exhibited significant binding affinities for all enzymes. Based on our overall observations, compound 30 could be recommended as a potential lead for the therapuetic of Alzheimer's.     

Unveiling the Anthelminthic Potential of Merremia vitifolia Stem through in Vitro and in Silico Approach

This study aimed to assess the anthelmintic activity of methanol extracts from Merremia vitifolia stems using a combination approach encompassing experimental, in vitro, and in silico evaluations. Despite the well-recognized pharmacological properties of M. vitifolia, its potential as an anthelmintic agent remained unexplored. This plant's anthelmintic potential was assessed on adult earthworms (Pheretima posthuma), revealing a dose-dependent reduction in spontaneous motility leading to paralysis and eventual mortality. The most effective dose of M. vitifolia (200 mg/ml) for anthelmintic effects on Pheretima posthuma was identified. Complementary in silico investigations were also conducted, employing Autodock PyRx 0.8 for docking studies of reported M. vitifolia compounds. Notably, quercetin emerged as a promising candidate with superior binding energies against β-tubulin (−8.3 Kcal/mol). Moreover, this comprehensive research underlines the anthelmintic potential of Merremia vitifolia stem extract and highlights quercetin as a noteworthy compound for further investigation in the quest for novel anthelmintic agents.     

Isolation of Two Plasticizers,Bis(2-ethylhexyl) Terephthalate and Bis(2-ethylhexyl) Phthalate,from Capparis spinosa L. Leaves

Many plants have been known to be contaminated and accumulate plasticizers from the environment, including water sources, soil, and atmosphere. Plasticizers are used to confer elasticity and flexibility to various fiber and plastic products. Consumption of plasticizers can lead to many adverse effects on human health, including reproductive and developmental toxicity, endocrine disruption, and cancer. Herein, we report for the first time that two plasticizers, bis(2-ethylhexyl) terephthalate (DEHT) and bis(2-ethylhexyl) phthalate (DEHP), have been isolated from the leaves of Capparis spinosa L. (the caper bush), a plant that is widely used in food seasonings and traditional medicine. 297 mg/kg of DEHT and 48 mg/kg of DEHP were isolated from dried and grounded C. spinosa L. leaves using column chromatography and semi-preparative high-performance liquid chromatography. Our study adds to the increase in the detection of plasticizers in our food and medicinal plants and to the alarming concern about their potential adverse effects on human health.     

First chemical synthesis of a scorpion alpha-toxin affecting sodium channels: the Aah I toxin of Androctonus australis hector.

Aah I is a 63-residue alpha-toxin isolated from the venom of the Buthidae scorpion Androctonus australis hector, which is considered to be the most dangerous species. We report here the first chemical synthesis of Aah I by the solid-phase method, using a Fmoc strategy. The synthetic toxin I (sAah I) was renatured in DMSO-Tris buffer, purified and subjected to thorough analysis and comparison with the natural toxin. The sAah I showed physico-chemical (CD spectrum, molecular mass, HPLC elution), biochemical (amino-acid composition, sequence), immunochemical and pharmacological properties similar to those of the natural toxin. The synthetic toxin was recognized by a conformation-dependent monoclonal anti-Aah I antibody, with an IC50 value close to that for the natural toxin. Following intracerebroventricular injection, the synthetic and the natural toxins were similarly lethal to mice. In voltage-clamp experiments, Na(v) 1.2 sodium channel inactivation was inhibited by the application of sAah I or of the natural toxin in a similar way. This work describes a simple protocol for the chemical synthesis of a scorpion alpha-toxin, making it possible to produce structural analogues in time.     

Bacteria Associated with Cysts of the Soybean Cyst Nematode (Heterodera glycines)

The soybean cyst nematode (SCN), Heterodera glycines, causes economically significant damage to soybeans (Glycine max) in many parts of the world. The cysts of this nematode can remain quiescent in soils for many years as a reservoir of infection for future crops. To investigate bacterial communities associated with SCN cysts, cysts were obtained from eight SCN-infested farms in southern Ontario, Canada, and analyzed by culture-dependent and -independent means. Confocal laser scanning microscopy observations of cyst contents revealed a microbial flora located on the cyst exterior, within a polymer plug region and within the cyst. Microscopic counts using 5-(4,6-dichlorotriazine-2-yl)aminofluorescein staining and in situ hybridization (EUB 338) indicated that the cysts contained (2.6 ± 0.5) × 10⁵ bacteria (mean ± standard deviation) with various cellular morphologies. Filamentous fungi were also observed. Live-dead staining indicated that the majority of cyst bacteria were viable. The probe Nile red also bound to the interior polymer, indicating that it is lipid rich in nature. Bacterial community profiles determined by denaturing gradient gel electrophoresis analysis were simple in composition. Bands shared by all eight samples included the actinobacterium genera Actinomadura and Streptomyces. A collection of 290 bacteria were obtained by plating macerated surface-sterilized cysts onto nutrient broth yeast extract agar or on actinomycete medium. These were clustered into groups of siblings by repetitive extragenic palindromic PCR fingerprinting, and representative isolates were tentatively identified on the basis of 16S rRNA gene sequence. Thirty phylotypes were detected, with the collection dominated by Lysobacter and Variovorax spp. This study has revealed the cysts of this important plant pathogen to be rich in a variety of bacteria, some of which could presumably play a role in the ecology of SCN or have potential as biocontrol agents.     

Biological Parameters for Four Coccinellid Species in Central Saudi Arabia

Developmental and reproductive rates ofAdonia variegataGoeze,Coccinella novemnotataHerbst,C. septempunctataL., andC. undecimpunctataL. were studied in wheat and barley in Central Saudi Arabia. Beetles were reared in the laboratory at 25 ± 2°C onBrevicoryne brassicae(L.) andRhopalosiphum padiL.A. variegataandC. undecimpunctatahad significantly higher egg hatching (X = 81.8 and 74.5%), adult longevity (X = 71.8 and 70.0 days), and survival (X = 61.8 and 61.5%), respectively.Coccinella undecimpunctatahad the highest fecundity (X = 370.5 eggs/female) and longest oviposition period (X = 29.8 days).C. septempunctataexhibited the lowest values for these biological parameters. No differences were evident in the total developmental time or egg and pupal duration, although species differences occurred in the larval duration. Larvae ofA. variegatadeveloped faster (X = 11.8 days) than Larvae ofC. septempunctata(X = 12.0 days),C. undecimpunctata(X = 12.2 days), orC. novemnotata(X = 13.1 days). The intrinsic rate of increase (r_m) and predicted population density were higher forC. undecimpunctata(X = 0.093 and 98553) after 60 days than forC. novemnotata(X = 0.088 and 59405),C. septempunctata(X = 0.086 and 35033), orA. variegata(X = 0.082 and 37991), respectively.     

Effect of amino acid substitutions on calmodulin binding and cytolytic properties of the LLP-1 peptide segment of human immunodeficiency virus type 1 transmembrane protein.

Previous studies have identified two highly basic amphipathic helical regions in the human immunodeficiency virus type 1 transmembrane protein that, in vitro, display both cytolytic and calmodulin-binding and -inhibitory properties that could contribute to cellular dysfunctions and cytopathogenesis during a persistent viral infection. In the current study, the structural specificity of the cytolytic and calmodulin-binding activities of the human immunodeficiency virus type 1 lentivirus lytic peptide (LLP-1) are examined with synthetic peptide homologs and analogs. The results of these studies demonstrate that even minor changes in LLP-1 amino acid content can markedly affect these properties, suggesting that sequence variation in these highly conserved LLP sequences may correlate with alterations in viral cytopathic properties.     

Immunocytochemical identification and localization of lipase in cells of the mycelium of Penicillium cyclopium variety

The localization of lipase in cells of the fungus Penicillium cyclopium was investigated. It was shown by differential centrifugation of a homogenate of mycelial cells that the activity of the enzyme is associated with the cell wall. A study of ultrathin sections of mycelium fixed using the method of Zvyagintseva in an electron microscope showed that the final products of lipolytic activity of the enzyme is localized on the cell wall. Antibodies were raised against the purified A and B lipases from P. cyclopium and their specificity was assessed by enzyme-linked immunosorbent assay. The antibody preparation was used in cytochemical investigation by immunogold labelling. This study permits the localization of cell-bound lipase mainly in the cell wall and in the periplasmic space. The identity of the cell-bound lipase with one of the two extracellular lipases is also demonstrated.     

Precedence of the first male sperm in successive matings in the HymenopteraDiadromus pulchellus

In most insect species where double matings occur, sperm from the second male preferentially fertilize subsequent eggs. However, we demonstrate here that, as already shown for some other hymenopteran species, this is not the case in the ichneumonid waspDiadromus pulchellus (Wesmeal): sperm from the first male usually father all the female progeny. This precedence of the first male sperm is also observed in double matings involving an haploid male and a diploid sterile male, whichever is the first mating male. We discuss the consequences of this phenomenon from an evolutionary point of view.