Anticholinesterase and acaricidal activities of steroids isolated from Trianthema portulacastrum L. against Rhipicephalus annulatus tick

The anticholinesterase and acaricidal activities of two plants of family Aizoaceae; Trianthema portulacastrum L.and Aizoon canariensis L. against Rhipicephalus annulatus tick were performed. Acaricidal activity was evaluatedusing adult and larval immersion tests of different concentrations (12.5, 25, 50, 100, and 150 mg/ml). Antiacetylcholinesterase activity of plant extracts and isolated compounds were performed spectrophotometrically usingdifferent concentrations (0.25, 0.5, and 1 mg/ml). Trianthema portulacastrum crude hydroalcoholic (CH) extractshowed 100% adult and larval mortality, while A. canariensis L. showed only 20% and 25%, respectively (p ≥ 0.05).The bioassay-guided fractionation of T. portulacastrum hydroalcoholic extract was performed for the acaricidalactivity and both n-hexane fraction and the unsaponifiable matter (USM) retained a significant activity in immersiontests. Its column chromatography (CC) led to the isolation of a β-sitosterol (1)-stigmasterol (2) mixture (1:1). Ethylacetate (EA) fraction showed 70% adult mortality and the compound 20-hydroxyecdysone (3) was isolated as a majorcompound. The hydroalcoholic extract of T. portulacastrum, hexane fraction, and 20-hydroxyecdysone (3) producedthe most potent inhibitory effect on acetylcholinesterase (AChE). In conclusion, T. portulacastrum L. containssecondary metabolites with acaricidal activities that provide promising natural products for controlling bovine tick.These acaricidal effects may be mediated, at least in part, via AChE inhibitory activities.

In vitro evaluation of anti-acetylcholinesterase and free radical scavenging potential of leaf extracts of some selected medicinal plants

Objective: To evaluate the phytochemical present in various solvent extracts from leaves of Ocimum sanctum (L.), Swertia chirayita (L.), Butea monosperma (Lam.) and Stevia rebaudiana (Bert.) as well as antioxidant and anticholinergic activities employing different in vitro models. Methods: Total phenol content of diethyl ether, chloroform and methanolic extracts obtained from leaves of different medicinal plants was determined by Folin-Ciocalteau's spectrophotometric method. Moreover, antioxidant and anticholinergic studies were conducted by four different in vitro methods which included diphenyl picrylhydrazyl radical scavenging, 2,2-azinobis (3-ethylbezoline-6-sulphonic acid), reducing activity by ferrous reduced antioxidant power and anti-acetylcholinesterase assay, in order to ensure pharmacological potential of the plants. Results: The methanolic leaf extract of Ocimum sanctum showed the highest total phenol content which was (21.13±1.04) GAE/g DW and antioxidant activities compared to other plants with the IC50 value of 40.43 μg/mL in diphenyl picrylhydrazyl radical scavenging assay and 53.5 μg/mL in 2,2-azinobis (3-ethylbezoline-6-sulphonic acid) assay as well as metal ion reduced by (78.22±0.38) TE/g DW in ferrous reduced antioxidant power assay. The inhibition percentage of the anti-acetylcholinesterase assay was (94.22±0.26)％. Conclusions: The results of our current study show that Ocimum sanctum leaf is the most significant source of phytochemicals that possesses antioxidant and anticholinergic properties. However, further investigation on isolation and characterization of active compound which is responsible for the pharmacological potential is needed.

In vitro evaluation of anti-acetylcholinesterase and free radical scavenging potential of leaf extracts of some selected medicinal plants

Objective: To evaluate the phytochemical present in various solvent extracts from leaves of Ocimum sanctum (L.), Swertia chirayita (L.), Butea monosperma (Lam.) and Stevia rebaudiana (Bert.) as well as antioxidant and anticholinergic activities employing different in vitro models. Methods: Total phenol content of diethyl ether, chloroform and methanolic extracts obtained from leaves of different medicinal plants was determined by Folin-Ciocalteau's spectrophotometric method. Moreover, antioxidant and anticholinergic studies were conducted by four different in vitro methods which included diphenyl picrylhydrazyl radical scavenging, 2,2-azinobis (3-ethylbezoline-6-sulphonic acid), reducing activity by ferrous reduced antioxidant power and anti-acetylcholinesterase assay, in order to ensure pharmacological potential of the plants. Results: The methanolic leaf extract of Ocimum sanctum showed the highest total phenol content which was (21.13±1.04) GAE/g DW and antioxidant activities compared to other plants with the IC

Sesquiterpenoids of agarwood from Aquilaria crassna / 中草药

Objective To study the chemical constituents of sesquiterpenoids of agarwood from Aquilaria crassna. Methods Seven squiterpenoids were isolated and purified by various column chromatographic techniques and HPLC method. The structures of the compounds were identified through the combined analysis of physicochemical properties and spectral data. The acetylcholinesterase and α-glucosidase inhibitory activity of compounds were evaluated by Ellman colorimetric method and pNPG method, respectively. Results Seven compounds were isolated from the ethyl acetate extract obtained from 95% aq. ethanol extract of agarwood from Aquilaria crassna and were identified as 2-[(2β,8β,8aα)-8,8a-dimethyl-1,2,3,4,6,7,8,8a-octahydro naphthalen-2-yl]-3- hydroxy-2-methoxpropanoic acid (1), 2-[(2β,8α,8aα)-8,8a-dimethyl-1,2,3,4,6,7,8,8a-octahydronaphthalen-2-yl] propane-1,2-diol (2), (1β,3α,4aβ,5β,8aα)-4,4a-dimethyl-6 (prop-1-en-2-yl) octahydronaphtha-lene-1,8a(1H)-diol (3), eremophila-9-en-8β,11-diol (4), eudesma-4-en-8,11-diol (5), eudesma-4-en-11,15-diol (6), and methyl-15-oxo-eudesmane-4,11 (13)-dien-12-oate (7). Moreover, compounds 1, 4 and 5 showed acetylcholinesterase inhibitory activity, and compound 5 exhibited α-glucosidase inhibitory activity.Conclusion Compound 1 is a new compound named as crasscid A, and compounds 1-3 and 7 are obtained from agarwood for the first time.

Phytochemical study ofand its biological activities

Sixteen compounds, including two new natural products (and), were obtained from the twigs of. The structures were elucidated based on NMR, MS, IR data and optical rotation values. Compounds,,anddisplayed moderate antibacterial activities against clinical isolates; compounds,,,andprotected neural cells against oxidative stress; and compoundsandexhibited anti-acetylcholinesterase activity.

Active anti-acetylcholinesterase component of secondary metabolites produced by the endophytic fungi of Huperzia serrata

Background An endophytic fungus lives within a healthy plant during certain stages of, or throughout, its life cycle. Endophytic fungi do not always cause plant disease, and they include fungi that yield different effects, including mutual benefit, and neutral and pathogenic effects. Endophytic fungi promote plant growth, improve the host plant's resistance to biotic and abiotic stresses, and can produce the same or similar biologically active substances as the host. Thus, endophytic fungal products have important implications in drug development. Result Among the numerous endophytic fungi, we identified two strains, L10Q37 and LQ2F02, that have anti-acetylcholinesterase activity, but the active compound was not huperzine A. The aim of this study was to investigate the anti-acetylcholinesterase activity of secondary metabolites isolated from the endophytic fungi of Huperzia serrata. Microbial cultivation and fermentation were used to obtain secondary metabolites. Active components were then extracted from the secondary metabolites, and their activities were tracked. Two compounds that were isolated from endophytic fungi of H. serrata were identified and had acetylcholine inhibitory activities. In conclusion, endophytic fungal strains were found in H. serrata that had the same anti-acetylcholinesterase activity. Conclusion We isolated 4 compounds from the endophytic fungus L10Q37, among them S1 and S3 are new compounds. 6 compounds were isolated from LQ2F02, all 6 compounds are new compounds. After tested anti acetylcholinesterase activity, S5 has the best activity. Other compounds' anti acetylcholinesterase activity was not better compared with huperzine A.

Antioxidant and anti-acetylcholinesterase activities of extracts and secondary metabolites from Acacia cyanophylla

<p><b>OBJECTIVE</b>To investigate the antioxidant potential and anti-acetycholinesterase activity of compounds and extracts from Acacia cyanophylla (A. cyanophylla).</p><p><b>METHODS</b>Three polyphenolic compounds were isolated from ethyl acetate extract of A. cyanophylla flowers. They have been identified as isosalipurposide 1, quercetin 2 and naringenin 3. Their structures were elucidated by extensive spectroscopic methods including 1D and 2D NMR experiments as well as ES-MS. The prepared extracts and the isolated compounds 1-3 were tested for their antioxidant activity using 1'-1'-diphenylpicrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) scavenging assays and reducing power. They have been also investigated for inhibitory effect against acetylcholinesterase using the microplate assay.</p><p><b>RESULTS</b>In the DPPH test, the EtOAc extract of flowers exhibited the highest antioxidant effect (67.26 µg/mL). Isosalipurposide 1 showed a significant antiradical power against DPPH (81.9 µg/mL). All extracts showed a dose-dependent acetylcholinesterase inhibition. In terms of the IC50 value, the butanolic extract (16.03 µg/mL) was the most potent sample. Isosalipurposide 1 was found to be active against AChE with an IC50 value of 52.04 µg/mL.</p><p><b>CONCLUSIONS</b>The results demonstrated the important antioxidant and anti-acetylcholinesterase activity of pure compounds and extracts from A. cyanophylla.</p>

Antioxidant and anti-acetylcholinesterase activities of extracts and secondary metabolites from Acacia cyanophylla

Objective: To investigate the antioxidant potential and anti-acetycholinesterase activity of compounds and extracts from Acacia cyanophylla (A. cyanophylla). Methods: Three polyphenolic compounds were isolated from ethyl acetate extract of A.cyanophylla flowers. They have been identified as isosalipurposide 1, quercetin 2 and naringenin 3. Their structures were elucidated by extensive spectroscopic methods including 1D and 2D NMR experiments as well as ES-MS. The prepared extracts and the isolated compounds 1-3 were tested for their antioxidant activity using 1’-1’-diphenylpicrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) scavenging assays and reducing power. They have been also investigated for inhibitory effect against acetylcholinesterase using the microplate assay.Results:(67.26 μg/mL). Isosalipurposide 1 showed a significant antiradical power against DPPH (81.9 μg/mL). All extracts showed a dose-dependent acetylcholinesterase inhibition. In terms of the IC50 value, the butanolic extract (16.03 μg/mL) was the most potent sample. Isosalipurposide 1 was found to be active against AChE with an IC50 value of 52.04 μg/mL. In the DPPH test, the EtOAc extract of flowers exhibited the highest antioxidant effect Conclusions: The results demonstrated the important antioxidant and anti-acetylcholinesterase activity of pure compounds and extracts from A. cyanophylla.

Acetylcholinesterase Inhibitory Activity After in vitro Gastrointestinal Digestion of Infusions of Mentha Species.

Aims: To study the acetylcholinesterase inhibitory activity of Mentha infusions before and after the gastrointestinal digestion and to correlate this activity with the chemical compounds present in these infusions. Place and Duration of Study: Fresh Mentha x piperita, M. spicata, M. pulegium were bought in a local supermarket. These plants were composed of leaves, stems and flowers for the identification, which was carried out in Plant Biotechnology Centre, Faculty of Sciences, University of Lisbon. The chemical identification of the infusions and the enzymatic tests were carried out in the Center of Chemistry & Biochemistry, Faculty of Science University of Lisbon from September 2010 till June 2011. Methodology: The compounds present in the infusions were identified by LC-MS. The enzyme activity assay was carried out using a spectrophotometric method. The digestive simulation was accomplished using enzymatic juices prepared in the laboratory and Caco-2 cells lines simulating the intestine barrier. Results: All the Mentha infusions contained rosmarinic acid. M. spicata infusion contained also eriocitrin and eriodictyol. The IC50 values for acetylcholinesterase inhibitory activity of the infusions, before digestion, stayed between 0.72 and 1.9 mg/mL. These activities are statistically different at p<.05. These activities can be explained by the presence of the phenolic compounds mentioned. Rosmarinic acid has an IC50 equal to 0.439 mg/mL (1.22 mM), eriocitrin and eriodictyol have IC50 equal to 0.439 mg/mL (0.29 mM) and 0.256 mg/mL (0.89 mM) respectively. The presence of these two flavonoids, eriocitrin and eriodictyol, can account for the higher activity detected for M. spicata. The gastric juice or the pancreatic juices used to simulate the gastrointestinal digestion did not originate any difference in the chemical composition of the infusions (analysed by HPLCDAD). This was also corroborated by the enzymatic tests. The Caco-2 cells did not originate any modification in the enzymatic activity of the infusions. The analysis of the cell homogenate revealed the presence of rosmarinic acid and the phenolic compounds, although in minor amount. Conclusion: Mentha infusions have the capacity to inhibit acetylcholinesterase, due to the presence of rosmarinic acid, eriocitrin and eriodictyol The composition of the Mentha herbal teas was not modified by the gastro-intestinal juices, or by the intestinal cell line.