Scorpions of the genus Odontobuthus Vachon, 1950 (Scorpiones: Buthidae) from Iran: Phylogenetic relationships inferred from mitochondrial DNA sequence data

The molecular phylogeny of the genus Odontobuthus Vachon, 1950 (Scorpiones: Buthidae) in Iran was evaluated using two mitochondrial DNA genes, cytochrome c oxidase, subunit I (COI) and 16S ribosomal RNA (16S rRNA). The molecular phylogenetic analyses were performed using Maximum Parsimony, Maximum Likelihood and Bayesian inference methods. The resulting topologies supported two main clades: the clade comprising Odontobuthus doriae, O. bidentatus, and O. tavighiae, and another one which is the O. tirgari clade. The results clearly presented additional support for the taxonomic validity of the recently described species, O. tirgari and O. tavighiae. In addition, the monophyly of two previously described species O. doriae and O. bidentatus was confirmed. According to the data presented here, three taxonomically valid species belonging to the genus Odontobuthus occur in Iran.     

Design and synthesis of new water-soluble tetrazolide derivatives of celecoxib and rofecoxib as selective cyclooxygenase-2 (COX-2) inhibitors

In an attempt to prepare a new water-soluble, parenteral COX-2 inhibitor, rofecoxib (9) and celecoxib (13) analogues were designed and synthesized for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors with in vivo anti-inflammatory activity. In this experiment, respective SO(2)Me and SO(2)NH(2) hydrogen-bonding pharmacophores were replaced by a tetrazole ring. Molecular modeling (docking) studies showed that the tetrazole ring of these two analogues (9 and 13) was inserted deep into the secondary pocket of the human COX-2 binding site where it undergoes electrostatic interaction with Arg(513). The rofecoxib (9) and celecoxib (13) analogues exhibited a high in vitro selectivity (9, COX-1 IC(50) = 3.8 nM; COX-2 IC(50) = 1.8 nM; SI = 2.11; 13, COX-1 IC(50) = 4.1 nM; COX-2 IC(50) = 1.9 nM; SI = 2.16) relative to the reference drug celecoxib (COX-1 IC(50) = 3.7 nM; COX-2 IC(50) = .2 nM; SI=1.68) and also showed high aqueous solubility at pH higher than 7 and good anti-inflammatory activity in a carrageenan-induced rat paw edema assay. However, 9 and 13 had no significant damage on gastric mucosa.     

An expedient synthesis of benzyl 2,3,4-tri-O-benzyl-beta-D-glucopyranoside and benzyl 2,3,4-tri-O-benzyl-beta-D-mannopyranoside

An efficient three-step synthesis of benzyl 2,3,4-tri-O-benzyl-beta-D-glucopyranoside, a widely used building block in carbohydrate chemistry, is described. The key step is the selective debenzylation-acetylation of perbenzylated beta-glucose using ZnCl2-Ac2O-HOAc. This approach was also used to affect an efficient three-step synthesis of benzyl 2,3,4-tri-O-benzyl-beta-D-mannopyranoside.     

The Effect of Winter Sowing,Chemical, and Nano-Fertilizer Sources on Oil Content and Fatty Acids of Dragon’s Head (Lallemantia iberica Fischer & C.A. Meyrefeer)

Journal of Plant Growth Regulation - Dragon’s head is a multifunctional plant with diverse applications so that all its parts, including its leaves and seeds, have nutritional value. For the...     

Design, synthesis, and biological evaluation of substituted 2-alkylthio-1,5-diarylimidazoles as selective COX-2 inhibitors

A new type of 1-aryl-5-(4-methylsulfonylphenyl)imidazoles, possessing C-2 alkylthio (SMe or SEt) substituents, were designed and synthesized for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors with in vivo anti-inflammatory activity. The compound, 1-(4-bromophenyl)-5-(4-methylsulfonylphenyl)-2-methylthioimidazole (11g), was the most potent and selective COX-2 inhibitor (COX-2 IC50=0.43 microM with no inhibition of COX-1 up to 25 microM) relative to the reference drug celecoxib (COX-2 IC50=0.21 microM with no inhibition of COX-1 up to 25 microM) and also showed very good anti-inflammatory activity compared to celecoxib in carrageenan-induced rat paw edema assay.     

Effects of Sowing Time and Chemical,Organic, and Biological Fertilizer Sources on Yield Components and Antioxidant Properties of Dragon’s Head (Lallemantia iberica (M. Bieb.) Fisch. & C. A. Mey)

Journal of Plant Growth Regulation - The effects of winter and spring sowing and chemical, organic, and biological fertilizer sources were studied on yield components and antioxidant properties of...     

Structural and Mechanical Behavior of Tristearin/Triolein-rich Mixtures and the Modification Achieved by Interesterification

The effects of chemical and enzymatic interesterification on the structure and rheological behavior of blends of fully hydrogenated canola oil (FHCO) with high oleic acid sunflower oil in the range of 10–90% was studied. Relationships between chemical composition, crystallization temperature (20–50°C), solid fat content (SFC) of the blends, and their rheological properties, characterized using both small and large deformation mechanical testing, were investigated. The storage modulus (G′) and yield force increased with FHCO concentration in the blends and was affected strongly by interesterification. The SFC in the interesterified samples was lower than in the non-interesterified blends, but they had higher values of G′. This increase in G′ at 30°C upon interesterification was attributed to a decrease in the fractal dimension of the fat crystal network which translates into a decrease in crystal cluster size in the interesterified samples. The higher G′ in the chemically interesterified samples relative to the enzymatic interesterified samples, on the other hand, was due to a higher λ parameter which is directly proportional to the strength of interparticle interactions and inversely proportional to crystal size. Microscopy and nucleation kinetics studies allowed for the independent determination of λ.     

Synthesis, antibacterial activity, and quantitative structure-activity relationships of new (Z)-2-(nitroimidazolylmethylene)-3(2H)-benzofuranone derivatives

A new series of (Z)-2-(1-methyl-5-nitroimidazole-2-ylmethylene)-3(2H)-benzofuranones (11a-p) and (Z)-2-(1-methyl-4-nitroimidazole-5-ylmethylene)-3(2H)-benzofuranones (12a-m) were synthesized and assayed for their antibacterial activity against Gram-positive and Gram-negative bacteria. Most of the 5-nitroimidazole analogues (11a-p) showed a remarkable inhibition of a wide spectrum of Gram-positive bacteria (Staphylococcus aureus, Streptococcus epidermidis, MRSA, and Bacillus subtilis) and Gram-negative Klebsiella pneumoniae, whereas 4-nitroimidazole analogues (12a-m) were not effective against selected bacteria. The quantitative structure-activity relationship investigations were applied to find out the correlation between the experimentally evaluated activities with various parameters of the compounds studied. The QSAR models built in this work had reasonable predictive power and could be explained by the observed trends in activities.     

Biochemical and Biophysical Characterization of Carbonic Anhydrase VI from Human Milk and Saliva

The Protein Journal - Carbonic anhydrases (CA, EC 4.2.1.1) catalyze the hydration of carbon dioxide and take part in many essential physiological processes. In humans, 15 CAs are characterized,...     

Design, synthesis, and biological evaluation of substituted 3-alkylthio-4,5-diaryl-4H-1,2,4-triazoles as selective COX-2 inhibitors

A new type of 4,5-diaryl-4H-1,2,4-triazole, possessing C-3 thio and alkylthio (SH, SMe or SEt) substituents, was designed and synthesized for evaluation as selective cyclooxygenase-2 (COX-2) inhibitors with in vivo anti-inflammatory activity. The compound, 3-ethylthio-5-(4-fluorophenyl)-4-(4-methylsulfonylphenyl)-4H-1,2,4-triazole (10d), exhibited a high in vitro selectivity (COX-1 IC50=20.5 nM; COX-2 IC50=1.8 nM; SI=11.39) relative to the reference drug celecoxib (COX-1 IC50=3.7 nM; COX-2 IC50=2.2 nM; SI=1.68) and also showed good anti-inflammatory activity compared to celecoxib in a carrageenan-induced rat paw edema assay.