Molecular phylogenetic study of flavonoids in medicinal plants: a case study family Apiaceae

Journal of Plant Research - The current study examined the phylogenetic pattern of medicinal species of the family Apiaceae based on flavonoid groups production, as well as the overall mechanism of...     

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.     

Synthesis of New Bis(pyrazolo[1,5-a]pyrimidines) Linked to Different Spacers as Potential MurB Inhibitors

An efficient protocol was adopted to efficiently prepare three new series of bis(pyrazolo[1,5-a]pyrimidines) linked to different spacers. The new bis(pyrazolo[1,5-a]pyrimidines) were prepared in 80–90 % yields by reacting the respective bis(enaminones) and 4-(4-substituted benzyl)-1H-pyrazole-3,5-diamines in pyridine at reflux temperature for 5–7 h. The new products showed a wide spectrum of antibacterial activity against six different bacterial strains. In general, propane- and butane-linked bis(pyrazolo[1,5-a]pyrimidines), which are attached to 3-(4-methyl- or 4-methoxybenzyl) units, had the best antibacterial activity with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values up to 2.5 and 5.1 μM, respectively. Additionally, the previous products demonstrated promising MurB inhibitory activity with IC₅₀ values up to 7.2 μM.     

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.     

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.     

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.     

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.     

Examination through a principal component analysis of the phosphorus exchanges between sediments and water in trophically different reservoirs

Phosphorus exchange at the sediment-water interface coupled with several parameters were assessed in several reservoirs with geologically different catchment basins and different trophic status in Morocco and France.The results showed that these exchanges were regulated by a combination of factors: physical chemical variability of the environment, the geological composition of catchment basins and the trophic status of the lake.In the hypereutrophic Villerest, iron-bound phosphorus is the major form of phosphorus trapped by the sediment whereas, in Moroccan reservoirs, calcium-bound phosphorus prevailed.We suggest that a drastic control of phosphorus inputs into the waters must be done through a large program of dephosphatization of tributaries to avoid Microcystis aeruginosa bloom formation in Villerest (Aleya et al., 1993) and calcium-bound phosphorus dissociation in Moroccan reservoirs with upward release of bioavailable phosphorus.

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Résumé Les échanges de phosphore au niveau de l'interface eau-sédiment couplés á la distribution temporelle de divers éléments chimiques et biologiques ont été étudiés dans divers réservoirs de niveaux trophiques différents, au Maroc et en France.Nos résultats mettent clairement en évidence une influence directe de l'environnement physico-chimique, de la nature géologique des bassins versants et de l'état trophique du lac sur la dynamique du phosphore au sein de cette interface.De plus, il apparait que dans le lac hypereutrophe de Villerest (Roanne, France), le phosphore est majoritairement complexé au fer alors que dans les retenues marocaines, ce sont les complexes phosphore-calcium qui prédominent.Nous préconisons un contrôle drastique des apports en phosphore á travers l'installation et la multiplication d'unités de déphosphatation afin d'éviter d'une part, la prolifération massive de la Cyanobactérie Microcystis aeruginosa á Villetest (Aleya et al., 1994) et d'autre part la dissociation des complexes phhosphore-calcium au sein des retenues marocaines avec libération de phosphore biodisponible.