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This study evaluated anti-acetylcholinesterase and antioxidant potentials in mice hippocampus treated with essential oils (EO) of Citrus sinensis (L.) Osbeck (orange) in vitro and in vivo. The acetylcholinesterase (AChE) activity was evaluated by using an adapted spectrophotometric method by Ellman after administration (30 consecutive days) in albino mice at doses of 50.00 mg/kg (EO 50), 100.00 mg/kg (EO 100) and 200.00 mg/kg (EO 200). The results showed that there was a significant decrease on enzymatic activity of AChE in mice hippocampus treated with essential oil of C. sinensis at doses of 50.00 mg/kg (vehicle= 9.89±0.19, OE 50= 2.63±0.21) [P <0.05], 100.00 mg/kg (vehicle= 9.89±0.19, EO 100= 1.65±0.15) [P <0.05] and 200.00 mg/kg (vehicle= 9.89±0.19, EO 200= 2.38±0.12) [P <0.05] when compared with vehicle group (0.05% Tween 80 dissolved in saline 0.9%). Concerning antioxidant activity, there was a significant reduction (P <0.05) of 20% on lipid peroxidation level in mice hippocampus treated with a dose of 200.00 mg/kg. The results obtained from the current studies showed that the essential oil of C. sinensis has considerable antioxidant and activity and inhibitory effect on AChE. [ABSTRACT FROM AUTHOR]

A novel pyrrole alkaloid, strychnuxin (1), along with five known compounds (2–6) was isolated from the fruit peels ofStrychnos nux-blanda. The structures of all the isolated compounds (1–6) were fully characterised using spectroscopic data, as well as comparison with the previous literature data. Moreover, all isolated compounds were assessed for theirα-glucosidase and acetylcholinesterase inhibitory activities. [ABSTRACT FROM PUBLISHER]

In the present study, a series of 4(3H)-quinazolinone derivatives (5a-f) were synthesized through the cylization reaction of substituted 1,3,4-thiadiazoles containing an aromatic primary amin and anthranilic acid in the presence of acetic anhydride and acetic acid. The structures of the synthesized compounds were confirmed by elemental analysis, IR, 1H-NMR and mass spectroscopic (5b and 5f) methods. Each derivative was evaluated for its ability to inhibit acetylcholinesterase (AChE) using a modification of Ellman's spectrophotometric method. Compounds 2-methyl-3-{4-[5-(ethylamino)-1,3,4-thiadiazol-2-yl]phenyl}quinazolin-4(3H)-one (5b) and 2-methyl-3-{4-[5-(cyclohexylamino)-1,3,4-thiadiazol-2-yl]phenyl}quinazolin-4(3H)-one (5d) can be identified as promising anticholinesterase agents due to their inhibitory effect when compared with donepezil as a reference drug. [ABSTRACT FROM AUTHOR]

Jacaranda oxyphyllaCham. is popularly known as ‘caroba-de-São-Paulo’ and it is used in traditional medicine for microbial infections. A new phytoquinoid (α/β-glucoside-4-phenylacetate-6-(1-hydroxy-4-oxo-2,5-cyclohexadiene-1-acetate) (1) was isolated fromJ. oxyphyllaleaves, together with three known compounds: quercetin-3-O-β-d-galactoside (2), verbascoside (3) and polystyrene (4). Their chemical structures were elucidated using spectroscopic techniques and by comparison with the related known compounds. In addition, it was found a pronounced acetylcholinesterase inhibitory activity for the quinoid1(100.0 ± 0.8%) and phenolic compounds2and3(99.9 ± 0.7 and 99.3 ± 0.5%, respectively), if compared to the standard eserine (92.7 ± 0.4%), that was analysed by a microplate spectrophotometer. [ABSTRACT FROM PUBLISHER]

The purpose of this work is to assess the radical scavenging activity, acetylcholinesterase inhibition, and proline content of an aqueous extract from wild pistachio ( Pistacia atlantica Desf.) leaves. The effect of aqueous extract on superoxide radical scavenging, hydroxyl radical scavenging, N,N-dimethyl-1,4-phenylendiammoniumdichloride (DMPD) radical scavenging, ABTS radical scavenging, nitric oxide scavenging, and β-carotene bleaching activities was examined. This study found that the aqueous extract possesses considerable amounts of flavonoids (33.52±2.04 μg catechin equivalents/mg of extract). The effect of this extract in scavenging activity of hydroxyl radical and DMPD was significantly better than that of ascorbic acid and butylated hydroxyanisole (BHA). The effect of the extract in superoxide and ABTS was significantly similar than that of tested standard antioxidants. The proline content of the extract was found to be 0.54±0.01 μg proline/mg of extract. Aqueous extract of P. atlantica inhibited acetylcholinesterase activity effectively with IC value of 58.05±0.12 μg/mL. [ABSTRACT FROM AUTHOR]

Abstract: Plants have been used for many years as a source of traditional medicine to treat various diseases and conditions. Many of these medicinal plants are also excellent sources for phytochemicals, many of which contain potent antioxidant and antiacetylcholinesterase activities. Chard (Beta vulgaris L. var. cicla) is widely spread in Turkey and used as an antidiabetic in traditional medicine. In the present study, the antioxidant activity and acetylcholinesterase inhibitor capacity of chard were examined. In addition, proline level of chard was determined. The antioxidant activity of water extract of chard was evaluated using different antioxidant tests. The results were compared with natural and synthetic antioxidants. The results suggest that chard may provide a natural source of antioxidant and antiacetylcholinesterase activities and proline content. [Copyright &y& Elsevier]

The ent kaurene diterpenoid, melissoidesin was isolated from the acetone extract of the leaves of Isodon wightii and the structure was designated as 3β, 11β, 15β-trihydroxy-6α-acetoxy-ent-kaur-16-ene based on spectral data and previous reports. Melissoidesin isolated from the acetone extract of leaves showed potent antiacetylcholinesterase activity and the IC50 value was observed as 215 µg mL-1. DPPH (1, 1-diphenyl-2-picrylhydrazyl) free radical scavenging activity of melissoidesin was significant and the IC50 value was 138 µg mL-1. The significant reducing property of the melissoidesin was stronger in high concentration. IC50 value of melissoidesin on hydroxyl radicals and metal chelation was observed as 99 and 143 µg mL-1, respectively. The 50% inhibitory concentration of melissoidesin on lipid peroxidation was calculated as 133 µg mL-1. These findings indicate that ent kaurene diterpenoid, melissoidesin was promising antiacetylcholinesterase and antioxidant which can be used as food and drug preparations. [ABSTRACT FROM AUTHOR]

Abstract: The synthesis of a new series of imidazo[2,1-b]thiazole derivatives is described. They were tested as potential acetylcholinesterase and butyrylcholinesterase inhibitors by means of a chemiluminescent microassay. Although most of the new compounds did not show significant cholinesterase inhibition potency, three of them displayed selective antiacetylcholinesterase activity in the micromolar range. [Copyright &y& Elsevier]

Abstract: In the present work, we report the results of a study aimed at evaluating the antiradical activity, the antioxidant activity and the acetylcholinesterase (E.C. 3.1.1.7.) inhibitory capacity of essential oils, ethanol and boiling water extracts from five aromatic herbs growing wild in Portugal and used in traditional food preparations: fennel (Foeniculum vulgare), mint (Mentha spicata), pennyroyal (Mentha pulegium), rosemary (Rosmarinus officinalis) and wild thyme (Thymus serpyllum). The water extracts of M. spicata and M. pulegium showed the highest radical-scavenging activity (DPPH test) values (IC50 =5.7±0.4 and 8.9±0.2μgml−1 respectively). This activity was higher than that found with the standard antioxidant BHT. The ethanol extracts of M. spicata, T. serpyllum and F. vulgare showed the highest antioxidant activities measured by the β-carotene/linoleic acid assay, IC50 =36.9±0.1, 41.2±0.1 and 68.7±0.1μgml−1, respectively. The inhibition of AChE was higher in the essential oil fraction. The highest activity was found for R. officinalis with an IC50 =69.8±0.1μgml−1. [Copyright &y& Elsevier]

Abstract: The synthesis of a new series of imidazo[2,1-b]thiazole derivatives is described. They were tested as acetylcholinesterase inhibitors by means of a chemiluminescent method suitable for high throughput screening. The compounds without quaternization had no appreciable inhibitory potency probably because they are poorly soluble in water. The corresponding quaternized compounds were good inhibitors with activity related to the spacer employed. [Copyright &y& Elsevier]

A series of sulfonamides were synthesized from dopamine derivatives. The reactions of amines with methanesulfonyl chloride followed by O-demethylation with BBr3 afforded phenolic sulfonamides. The antioxidant activities of the synthesized phenolic sulfonamides were investigated by thiocyanate method, 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS(•+)), 1,1-diphenyl-2-picryl-hydrazyl (DPPH(•)), N,N-dimethyl-p-phenylenediamine (DMPD(•+)), and superoxide anion (O2(•-)) radical scavenging, reducing power, and ferrous ion (Fe(2+)) chelating assays. Sulfonamides 13-16 showed around 75-85% inhibition on linoleic acid peroxidation. On the other hand, butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT), α-tocopherol, and trolox indicated an inhibition of 90.0%, 85.73%, 73.33%, and 85.73% on peroxidation, respectively, in the same system at the same concentration (10 µg/mL). Also, the inhibition effects of the synthesized compounds on acetylcholinesterase (AChE) activity were evaluated. AChE was effectively inhibited by sulfanomides 13-16, with K(i) values in the range of 33.04 ± 4.3 to 131.68 ± 8.8 nM., (© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)