Phytochemical and In Silico ADME/Tox Analysis of Eruca sativa Extract with Antioxidant,Antibacterial and Anticancer Potential against Caco-2 and HCT-116 Colorectal Carcinoma Cell Lines

Eruca sativa Mill. (E. sativa) leaves recently grabbed the attention of scientific communities around the world due to its potent bioactivity. Therefore, the present study investigates the metabolite profiling of the ethanolic crude extract of E. sativa leaves using high resolution-liquid chromatography-mass spectrometry (HR-LC/MS), including antibacterial, antioxidant and anticancer potential against human colorectal carcinoma cell lines. In addition, computer-aided analysis was performed for determining the pharmacokinetic properties and toxicity prediction of the identified compounds. Our results show that E. sativa contains several bioactive compounds, such as vitamins, fatty acids, alkaloids, flavonoids, terpenoids and phenols. Furthermore, the antibacterial assay of E. sativa extract showed inhibitory effects of the tested pathogenic bacterial strains. Moreover, the antioxidant activity of 2,2-diphenyl-1-picrylhydrazyl (DPPH) and hydrogen peroxide (H₂O₂) were found to be IC₅₀ = 66.16 μg/mL and 76.05 μg/mL, respectively. E. sativa also showed promising anticancer activity against both the colorectal cancer cells HCT-116 (IC₅₀ = 64.91 μg/mL) and Caco-2 (IC₅₀ = 83.98 μg/mL) in a dose/time dependent manner. The phytoconstituents identified showed promising pharmacokinetics properties, representing a valuable source for drug or nutraceutical development. These investigations will lead to the further exploration as well as development of E. sativa-based nutraceutical products.     

Novel Synthesis of Pyrazolyloxothiazolidine Derivatives

1‐Substituted 3‐[3‐(methyl/phenyl)‐1H‐pyrazol‐5‐yl]thioureas react with the triple bond of dimethyl acetylenedicarboxylate forming (Z)‐methyl 2‐[(Z)‐3‐substituted‐2‐(3‐(methyl/phenyl‐1H‐pyrazol‐5‐ylimino)‐4‐oxothiazolidin‐5‐ylidene)acetates. Rational for these conversations are presented.     

Facile synthesis of new imidazoles from direct reaction of 2,3‐diamino‐1,4‐naphthoquinone with aldehydes

New imidazoles were easily prepared from 2,3‐diamino‐1,4‐naphthoquinone and stoichiometric quantities of the appropriate aldehydes in dimethyl sulfoxide as a solvent. The reaction proceeded for few hours. The procedure can be generalized to different classes of aldehydes. 2‐Methyl‐1H‐naphtho[2,3‐d]imidazole‐4,9‐dione was also obtained in good yield during refluxing of 2,3‐diaminonaphthoquinone in acetic acid. The structure of the newly synthesized imidazoles was extensively investigated using NMR experiments. J. Heterocyclic Chem., (2011).     

Micro and semi-micro determination of organic nitrogen by use of potassium bromate

After Kjeldahl digestion of an organic compound, nitrogen is determined by oxidation of the resultant ammonium sulphate with hypobromite produced in situ by the addition of an excess of potassium bromate and bromide in a special flask. The unreacted potassium bromate is determined iodometrically.     

Prototype reflectivity analyses of hydrogen storage levels in single-walled carbon nanotubes

A prototype case study is presented that examines the level of hydrogen content in H-SWNTs using the Surface Plasmon Resonance technique. The damping effect and the angular shift in the resonance minimum of an SWNT-gold interface due to the presence of hydrogen is analyzed using a parametric model, which is based on the concept of an effective permittivity. The new approach provides for a non-invasive analysis of the level of hydrogen content in H-SWNTs and is potentially extendable to other carbon-based hydrogen storage materials.     

Stability and bioequivalence studies of two marketed formulations of coenzyme Q10 in beagle dogs.

Coenzyme Q10 (CoQ10), a highly lipophilic compound present in the inner mitochondrial membrane, is essential for production of cellular energy in the form of ATP. CoQ10 is used as an antioxidant and also in the treatment of various cardiovascular disorders. The relative bioavailabilities of powder filled capsule (I) and oil-based formulation (II) of CoQ10 were compared in beagle dogs in an open, randomized, multiple dose, cross-over design. Poor and slow absorption characteristics were observed for both the formulations. The AUC, Cmax, and Tmax for formulation I and II are comparable (p < 0.05) where the values for formulation I are 22.84 +/- 6.3 micrograms ml-1 h, 0.51 +/- 0.11 microgram/ml, and 6.1 +/- 2.0 h whereas the values for formulation II are 24.32 +/- 5.6 micrograms ml-1 h, 0.55 +/- 0.16 microgram/ml, and 6.6 +/- 2.3 h, respectively. Stability of CoQ10 at various temperature and humidity conditions and its photostability were studied. Various antioxidants were evaluated to determine the type and amount of antioxidant(s) required to improve the stability of CoQ10. Large extent of degradation was observed at 45 degrees C and 55 degrees C. The effect of humidity conditions on degradation was insignificant. Among the various antioxidants studied, mixture of ascorbic acid (5%) and EDTA (0.1%) offered better protection than phenolic antioxidants such as butylated hydroxy anisole (BHA), butylated hydroxy toluene (BHT), or propyl gallate (PG). Further, increasing concentrations of phenolic antioxidants (from 0.1 to 0.3%) accelerated the degradation.     

Simultaneous analysis of furosemide and bumetanide in horse plasma using high performance liquid chromatography

A high performance liquid chromatographic method is described for the simultaneous determination of furosemide and bumetanide in horse plasma. The C8 (3 microns) reversed phase column (4.8 x 150 mm) provided clear separation of furosemide and bumetanide with other components present in the horse plasma. The detection limit for both the drugs was 10 ng/mL. Both drugs were stable in plasma (at natural or acidic pH) for up to 24 h. The method is sufficiently sensitive to detect furosemide levels in plasma obtained from horses receiving a therapeutic dose of furosemide.     

Unravelling the anticancer potency of 1,2,4-triazole-N-arylamide hybrids through inhibition of STAT3: synthesis and in silico mechanistic studies

Molecular Diversity - The discovery of potent STAT3 inhibitors has gained noteworthy impetus in the last decade. In line with this trend, considering the proven biological importance of...