Application of PEG-400 as a green biodegradable polymeric medium for the catalyst-free synthesis of spiro-dihydropyridines and their use as acetyl and butyrylcholinesterase inhibitors.

A simple, efficient and green approach for the synthesis of spiro-dihydropyridines derivatives by one-pot multi-component reaction of isatin or acenaphthoquinone derivatives (1 equiv) with malononitrile (1 equiv) and N,N'-substituted-2-nitroethene-1,1-diamines (1 equiv) in PEG-400 under catalyst-free conditions is described. This method provides several advantages such as environmental friendliness, short reaction time, and simple workup procedure for the synthesis of biologically important compounds. The ability of synthesized compounds in inhibition of acetyl and butyrylcholinesterase were investigated both in vitro and in silico. All compounds showed moderate to high level activity against both acetyl and butyrylcholinesterase. There was a good correlation between in vitro and in silico studies.

Dandelion flower-fabricated Ag nanoparticles versus synthetic ones with characterization and determination of photocatalytic, antioxidant, antibacterial, and α-glucosidase inhibitory activities.

In the present work, Silver nanoparticles (AgNPs) were fabricated through the dandelion flower hydroalcoholic extract, and their properties were characterized by FTIR, XRD, UV visible, SEM, and EDX. The results demonstrated that the average diameter of the green fabricated AgNPs is 45-55 nm (G-AgNPs). The antioxidant, antimicrobial, antidiabetic, and photocatalytic properties of G-AgNPs were compared with two commercially available different diameter sizes (20 and 80-100 nm) of AgNPs (C-AgNPs1- and C-AgNPs2, respectively). The sample's capacity for antioxidants was evaluated by DPPH free radical scavenging method. The consequences showed that G-AgNPs have higher radical scavenging activity (47.8%) than C-AgNPs2 (39.49%) and C-AgNPs1 (33.91%). To investigate the photocatalytic property, methylene blue dye was used. The results displayed that G-AgNPs is an effective photo-catalyst compared to C-AgNPs2 and C-AgNPs1, which respectively have an inhibition potential of 75.22, 51.94, and 56.65%. Also, the antimicrobial capacity of nanoparticles was assayed against, the gram-negative Escherichia coli and gram-positive Staphylococcus aureus bacteria. The results indicated that G-AgNPs could effectively inhibit the growth of both bacteria, compared to C-AgNPs1 and C-AgNPs2. Finally, G-AgNPs exhibited a considerable α-glucosidase enzyme inhibitory effect (88.37%) in comparison with C-AgNPs1 (61.7%) and C-AgNPs2 (50.5%).

Antimicrobial activity of some Salvia species essential oils from Iran.

The aerial parts of Salvia multicaulis, S. sclarea and S. verticillata were collected at full flowering stage. The essential oils were isolated by hydrodistillation and analyzed by combination of capillary GC and GC-MS. The in vitro antimicrobial activity of the essential oils were studied against eight Gram-positive and Gram-negative bacteria (Bacillus subtilis, Bacillus pumulis, Enterococcus faecalis, Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae) and three fungi (Candida albicans, Saccharomyces cerevisiae and Aspergillus niger). The results of antibacterial activity tests of the essential oils according to the disc diffusion method and MIC values indicated that all the samples have moderate to high inhibitory activity against the tested bacteria except for P. aeruginosa which was totally resistant. In contrast to antibacterial activity, the oils exhibited no or slight antifungal property, in which only the oil of S. multicaulis showed weak activity against two tested yeasts, C. albicans and S. cerevisiae.

Design and Synthesis of New Benzimidazole and Pyrimidine Derivatives as α-glucosidase Inhibitor.

In an endeavor to find a novel series of antihyperglycemic agents, new benzimidazole and pyrimidine derivatives were successfully synthesized efficiently in high yield with high purity, starting from amino acids in the presence of phosphorus oxychloride (POCl3). The synthesized compounds were identified by (1)H-NMR, (13)C-NMR, FT-IR spectroscopic techniques and elemental analysis. All products were assayed for their inhibitory effects on yeast and rat intestinal α-glucosidases. The results revealed that compounds with aromatic amino acids moiety showed significant inhibition activity on the tested enzymes. Among the benzimidazole derivatives 4c and 4d exhibited the best activity against both of the tested enzymes. Also, among the pyrimidine derivatives 5c and 5d possessed significant inhibition action on the enzymes. The IC50 values for the most potent benzimidazole yeast and intestinal α-glucosidases inhibitor (4d) were found to be 9.1 and 36.7 µM, respectively. The IC50 values for the inhibition of yeast and intestinal α-glucosidases by the most active pyrimidine compound (5d) were calculated to be 8.3 and 21.8 µM, respectively. Overall, this study proved that benzimidazole and pyrimidine derivatives with aromatic amino acids moieties can represent novel promising α-glucosidase inhibitors.

Flavonoids from Salvia chloroleuca with α-Amylsae and α-Glucosidase Inhibitory Effect.

It is believed that the inhibition of carbohydrate hydrolyzing enzymes including α-amylase and α-glucosidase is one of the therapeutic approaches to decrease the postprandial glucose level after a meal, especially in the people with type 2 diabetes. Medicinal plants and their extracts are one of the main sources to find new inhibitors to the enzymes. In our study four flavonoids, namely luteolin 7-O-glucoside (1), luteolin 7-O-glucuronide (2), diosmetin 7-O-glucuronide (3) and salvigenin (4) were isolated from aerial parts of Salvia chloroleuca. The inhibitory activity of these compounds against α-amylase and α-glucosidase were evaluated. Compounds 1, 2 and 3 showed potent α-glucosidase inhibitory effect with IC50 values of 18.3, 14.7, and 17.1 µM, respectively. Also these compounds exhibited moderate α-amylase activity with IC50 values 81.7, 61.5, and 76.3 µM, respectively.

Composition and in vitro antibacterial activity of essential oils from four Satureja species growing in Iran.

The composition and in vitro antibacterial activity of essential oils from four Satureja species (S. bachtiarica, S. khuzistanica, S. mutica and S. rechingeri) growing in Iran were determined. According to the results of GC-FID and GC-MS analysis, all oil samples were principally composed of phenolic constituents (carvacrol and/or thymol) with the percentages ranging from 41.2% (S. bachtiarica) to 77.7% (S. rechingeri). Determining antibacterial activities by the disc diffusion method against two Gram-positive and two Gram-negative bacteria revealed the maximum activity against Bacillus cereus with a range of minimum inhibitory concentration values from 0.25 to 1 mg mL(-1) and minimum bactericidal concentration values from 0.5 to 1 mg mL(-1). The oils of S. khuzistanica and S. rechingeri appeared to be more active in general than those of other species. In conclusion, the essential oils of studied Satureja species have the potential to be considered as alternatives for synthetic food preservatives.

Multivariate optimization of hydrodistillation-headspace solvent microextraction of thymol and carvacrol from Thymus transcaspicus.

In this paper multivariate response surface methodology (RSM) has been used for the optimization of hydrodistillation-headspace solvent microextraction (HD-HSME) of thymol and carvacrol in Thymus transcaspicus. Quantitative determination of compounds of interest was performed simultaneously using gas chromatography coupled with flame ionization detector (GC-FID). Parameters affecting the extraction efficiency were assessed and the optimized values were 5 min, 2 microL and 3 min for the extraction time, micro-drop volume and cooling time after extraction, respectively. The amounts of analyte extracted increased with plant weight. The calibration curves were linear in the ranges of 6.25-81.25 and 1.25-87.50 mg L(-1) for thymol and carvacrol, respectively. Limit of detection (LOD) for thymol and carvacrol was 1.87 and 0.23 mg L(-1), respectively. Within-day and between-day precisions for both analytes were calculated in three different concentrations and recoveries obtained were in the range of 89-101% and 95-116% for thymol and carvacrol, respectively.