AChE Inhibitory Activity Research Articles

Dimeric sesquiterpenoid-4H-chromone derivatives from agarwood of Aquilaria crassna and their cytotoxicity

Six previously undescribed uncommon ester-bonded dimeric compounds (aquilacrassnins A–F) containing a sesquiterpenoid and a 5,6,7,8-tetrahydroxy-2-(2-phenylethyl)-5,6,7,8-tetrahydro -4H-chromone units were isolated from the EtOAc extract of agarwood originating from Aquilaria crassna. Their structures were elucidated by spectroscopic (NMR, UV, IR, MS, and ECD) methods. All the compounds were tested for AChE inhibitory activity and cytotoxicity against K562, BEL-7402, SGC-7901, Hela, and A549 tumor cell lines. The results showed that aquilacrassnin A, B, and E exhibited weak cytotoxicity against the five tested cell lines, whereas all the compounds were inactive against AChE.

The polysaccharide extracts from the fungi Coprinus comatus and Coprinellus truncorum do exhibit AChE inhibitory activity

The polysaccharide (PSH) extracts from the edible mushroom species Coprinus comatus and Coprinellus truncorum were screened in liquid for their acetylcholinesterase inhibitory (AChE) activity. Both extracts were found to display inhibition of the aforementioned enzyme reaching similar IC50 values of 0.62 ± 0.07 and 0.61 ± 0.03 mg/mL, respectively. According to the means of FTIR spectroscopy, these PSH extracts mostly contained β-glucans. However, the presence of some proteins and polyphenolics as minor ingredients were also detected. Compared with existing literature data for anti-AChE activity of the sugar samples, the findings within this study may be treated as a profound bioactivity. Consequently, this study puts some light on the possible use of the screened macrofungi in the palliative treatment of Alzheimer’s disease.

The effects of human drugs in Corbicula fluminea. Assessment of neurotoxicity, inflammation, gametogenic activity, and energy status

The constant release of pharmaceuticals products to aquatic environment even at low concentrations (ng L−1 to µg L−1) could lead to unknown chronic effects to non-target organisms. The aim of this study was to evaluate neurotoxic responses, inflammation, gametogenic activity and energy status on the fresh water clam C. fluminea after exposure to different concentrations of caffeine (CAF), ibuprofen (IBU), carbamazepine (CBZ), novobiocin (NOV) and tamoxifen (TMX) for 21 days under laboratory conditions. During the assay, water was spiked every two days with CAF (0; 0.1; 5; 15; 50µgL−1), IBU (0; 0.1; 5; 10; 50µgL−1), CBZ, NOV, and TMX (0.1, 1, 10, 50µgL−1). After the exposure period, dopamine levels (DOP), monoamine oxidase activity (MAO), arachidonic acid cyclooxygenase activity (COX), vitellogenin-like proteins (VTG), mitochondrial electron transport (MET), total lipids (TLP), and energy expenditure (MET/TLP) were determined in gonad tissues, and acetyl cholinesterase activity (AChE) was determined in digestive gland tissues. Results showed a concentration-dependence response on biomarkers tested, except for MAO. Environmental concentrations of pharmaceuticals induced significant changes (p < 0.05) in the neurotoxic responses analyzed (CAF, CBZ and NOV increased DOP levels and CBZ inhibited AChE activity), inflammation (CAF induced COX), and energy status (MET and TLP increased after exposure to CBZ, NOV and TMX). Responses of clams were related to the mechanism of action (MoA) of pharmaceuticals. Biomarkers applied and the model organism C. fluminea constituted a suitable tool for environmental risk assessment of pharmaceutical in aquatic environment.

Evaluation of chemical composition, antioxidant and anti-acetylcholinesterase activities of Hypericum neurocalycinum and Hypericum malatyanum

This study was conducted to evaluate the chemical composition, antioxidant and anti-acetylcholinesterase (anti-AChE) activities of methanolic extracts of H. neurocalycinum and H. malatyanum, two endemic species of the Turkish flora. HPLC-DAD analysis indicated that two naphthodianthrones (pseudohypericin and hypericin) together with chlorogenic acid, rutin, hyperoside, isoquercitrin, kaempferol, quercitrin, quercetin, amentoflavone and hyperforin are the main compounds present in the methanol extracts. The extracts were tested in vitro for their antioxidant activities including, inhibition of lipid peroxidation in liposomes, induced by Fe3+/ascorbate system, scavenging effect on DPPH and superoxide anion radicals, and ferric ion reducing antioxidant power (FRAP). H. neurocalycinum demonstrated stronger antioxidant properties than H. malatyanum due to higher activity on scavenging DPPH (EC50=2.49±0.09mg/mL) and superoxide anion radicals (EC50=0.613±0.05mg mg/mL), and inhibition of lipid peroxidation (EC50=2.49±0.09mg/mL). This difference in activity seems to be due to the presence of higher amounts of the antioxidant compounds (flavonoids) such as rutin, quercetin and kaempferol in H. neurocalycinum extract. The antioxidant activities of the extract may be attributed to their reducing capabilities. At 5mg/mL H. neurocalycinum (FRAP value=2.39±0.039mM Fe2+) and H. malatyanum (FRAP value=2.23±0.013mM Fe2+) showed high ability to reduce Fe3+ to Fe2+. The extracts were tested also for their in vitro AChE inhibitory activities. H. neurocalycinum inhibited 72.24±0.39% of AChE activity at a concentration of 5mg/mL. It was concluded that H. neurocalycinum is more effective AChE inhibitor and antioxidant than H. malatyanum.

Modification of Bischler-Möhlau indole derivatives through palladium catalyzed Suzuki reaction as effective cholinesterase inhibitors, their kinetic and molecular docking studies

Due to the immense importance of aryl indole nucleus, herein we report the palladium-catalyzed arylation of N-substituted 2-aryl indole utilizing Suzuki-Miyaura cross coupling methodology. The biological screening for cholinesterase inhibition of the resulted biaryl indole moieties was carried out to evaluate their pharmacological potential, expecting to involve the development of new therapeutics for various inflammatory, cardiovascular, gastrointestinal and neurological diseases. This research work also involved the use of utilization of microwave-assisted organic synthesis (MAOS) for the synthesis of Bischler-Möhlau indole which is further biarylated via palladium-catalyzed cross coupling reaction. All the synthetic compounds (3a-n) were tested for cholinesterase inhibition and exhibited high level of AChE inhibitory activities. Interestingly, compounds 3m and 3n were found to be dual inhibitors, however, remaining compound exhibited no inhibitory activity against BChE. The biological potential of the resulted compounds was explained on the basis of molecular docking studies, performed against AChE and BChE, exploring the probable binding modes of most potent inhibitors.

Acetylcholinesterase inhibitory activity of chemical constituents isolated from Miliusa thorelii

Two new dihydrooxoprotoberberine alkaloids; miliusathorines A (1) and B (2), a new natural flavone, miliusathorone (3), together with twenty-two known compounds (4–25) were isolated from the combined stem and root extract and the leaf extract of Miliusa thorelii. The structures of all isolated compounds were elucidated by spectroscopic methods and mass spectrometry. All compounds were evaluated for their acetylcholinesterase activities. Miliusathorine A (1) and norushisunine had the best AChE inhibitory activities, however these were weak inhibitors when compared to the standard galantamine.

Bioactive Asarone-Derived Phenylpropanoids from the Rhizome of Acorus tatarinowii Schott.

Eight new (1a/1b, 2a, 3a, 4a/4b, and 5a/5b) and seven known (2b, 3b, and 6-10) asarone-derived phenylpropanoids, a known asarone-derived lignan (12), and four known lignan analogues (11 and 13-15) were isolated from the rhizome of Acorus tatarinowii Schott. The structures were elucidated via comprehensive spectroscopic analyses, modified Mosher's method, and quantum chemical calculations. Compounds 1-8 were present as enantiomers, and 1-5 were successfully resolved via chiral-phase HPLC. Compounds 1a/1b were the first cases of asarone-derived phenylpropanoids with an isopropyl C-3 side-chain tethered to a benzene core from nature. Hypoglycemic, antioxidant, and AChE inhibitory activities of 1-15 were assessed by the α-glucosidase inhibitory, ORAC, DPPH radical scavenging, and AChE inhibitory assays, respectively. All compounds except 3a showed α-glucosidase inhibitory activity. Compound 3b has the highest α-glucosidase inhibitory effect with an IC50 of 80.6 μM (positive drug acarbose IC50 of 442.4 μM). In the antioxidant assays, compounds 13-15 exhibited ORAC and DPPH radical scavenging activities. The results of the AChE inhibitory assay indicated that all compounds exhibited weak AChE inhibitory activities.

Lippia origanoides essential oil: An efficient alternative to control Aedes aegypti, Tetranychus urticae and Cerataphis lataniae

The main objective of the present study is to find an alternative controlling agent for some devastating greenhouse pests, and the yellow fever mosquito larvae. More specifically, the potential bioactivity of Lippia origanoides Kunth. (“erva-de-Marajó”) has been evaluated here against three most common pests found in tropical and subtropical countries: Tetranychus urticae Koch. mites, Cerataphis lataniae Boisd. aphids and Aedes aegypti Linn. larvae. The essential oil extracted from leaves of Lippia origanoides Kunth. has been analyzed by GC-FID and GC–MS and 32 compounds have been identified, representing 97.63% of the raw essential oil. The major compounds are carvacrol (48.31%), p-cymene (9.11%) and thymol (8.78%). The essential oil has been tested for AChE inhibition, obtaining IC50=16.93μg/mL, as well as for its potential antioxidant activities by different methods [DPPH: IC50=8.4±0.1μg/mL, ABTS: 691.8±44.3μM TEs/g (Trolox Equivalents) and FRAP: 933.1±8.1μM Eq Fe(II)/g]. Our results have shown acaricidal and insecticidal activities of this oil against T. urticae Koch. and C. lataniae Boisd. Volatile phase effects have been evaluated for T. urticae (LD50=25.1±1.1μg/mL for 24h) and for C. lataniae (LD50=6.6±0.5μg/mL for 24h, and LD50=2.7±0.6μg/mL for 48h), whose values are in the same order of magnitude as the enzymatic activity. These results show the susceptibility of T. urticae and C. lataniae species to the AChE inhibitory activity. Thus, the mortality of these species may be due to the neurotoxic mode of action, which affect the transport of ions and AChE. Furthermore, L. origanoides essential oil has shown a moderate larvicidal potential with LD50=187.3±0.9μg/mL after 24h. The occurrence of the larvicidal activity at very large concentration indicates that the larval mortality may occurs by ingestion or contact. The present study clearly illustrates the efficacy of the investigated essential oil as a natural pest controlling agent.

Acetylcholinesterase Inhibitory Alkaloids from the Whole Plants of Zephyranthes carinata.

Eleven new alkaloids (1-11), classified as the 12-acetylplicamine (1), N-deformyl-seco-plicamine (2), plicamine (3-6), 4a-epi-plicamine (7), seco-plicamine (8), and lycorine (9-11) framework types, along with 15 known alkaloids (12-26) were isolated from the whole plants of Zephyranthes carinata. The structures of the new alkaloids 1-11 were established by extensive spectroscopic data interpretation. The absolute configurations of 9 and 10 were defined by single-crystal X-ray diffraction analysis. Zephycarinatines A (1), B (2), and G (7) represent the first examples of 12-acetylplicamine, N-deformyl-seco-plicamine, and 4a-epi-plicamine alkaloids, respectively. Alkaloids 6, 11, 17, and 20-23 exhibited AChE inhibitory activities with IC50 values ranging from 1.21 to 184.05 μM, and a preliminary structure-activity relationship is discussed.

Non-target effects of antifouling agents on mortality, hatching success, and acetylcholinesterase activity in the brine shrimp Artemia salina

Many commercial shipping, leisure crafts, and aquaculture facilities employ antifouling agents to control biofouling/biocorrosion by keeping their metallic hulls clear, but most agents have been known to cause negative effects such as pollution in coastal marine ecosystem. In this study, we measured the deleterious effects of three antifouling agents (i.e. tributyltin; TBT, diuron, irgarol 1051) on nauplii mortality, acetylcholinesterase (AChE, EC3.1.1.7) activity, and hatching success of cysts in the brine shrimp Artemia salina. Lethal concentration 50 (LC50) was measured using A. salina nauplii in time-course (i.e. 24, 48, and 72 h) to select proper concentrations for the suite of AChE assays. The 24 h-LC50 toxicities of three antifouling agents ranged for mortality were as follows: TBT 0.208 μg/L, diuron 10261 μg/L, and irgarol 1051 982 μg/L. Selected doses within the LC50 value of each antifouling agent significantly inhibited AChE activity for 24 h, and newly hatched nauplii were more sensitive than 48 h old nauplii. Furthermore, the exposure conditions dose-dependently reduced the hatching rate of A. salina cysts. We conclude that three antifouling agents tested in this study may have a toxic cholinergic effect on nauplii through AChE inhibition, in addition to ecotoxicity on cyst hatching.

Effect of the Cymbopogon citratus Infusion on the Activity of Acetylcholinesterase Enzyme and on the Redox Profile in Farmers’ Erythrocytes

Agrochemicals were more prominent in 1960, marked due to the agricultural modernization process. As a result of this widespread use for food production, there was also an increase in cases of intoxication caused by these agents which made it necessary to search for alternative therapies for agricultural workers. Thus, considering that phytochemical characterization revealed the presence of antioxidants in Cymbopogon citratus extract, the objective of this study was to evaluate the effect of this plant infusion on the enzyme acetylcholinesterase activity (AChE) and on the redox response in farmers’ erythrocytes. These erytrocytes were processed and subjected to treatment with the Cymbopogon citratus infusion (5, 10, 25 and 50 g/L). In these samples the following were determined: the AChE enzyme activity, the levels of thiobarbituric acid reactive substances (TBARS), protein carbonyls (CPs) and reduced glutathione (GSH). In general, it was discovered that the inhibition of AChE activity is negative regarding to the increase of protein carbonyl levels and positive regarding the GSH levels. In addition, Cymbopogon citratus infusions could not even reverse this inhibition or the high levels of TBARS and CPs. On the other hand, levels of GSH were increased by infusions demonstrating the increased antioxidant activity in rural workers’ erythrocytes.

Two new alkaloids from the twigs of Trigonostemon filipes

A phytochemical investigation of the alkaloid constituents from Trigonostemon filipes Y. T. Chang et S. L. Mo led to the isolation of two new indole alkaloids, trigonostemine G (1) and trigonostemone J (2), together with two known ones, trigonostemine A (3) and trigonostemine B (4). Their structures were determined by extensive spectroscopic methods. Compounds 1–4 exhibited moderate AChE inhibitory activity with inhibition ratio of 31.6, 31.7, 41.7, and 42.4%, respectively. In addition, compounds 1–2 showed weak cytotoxicity against K562 and BEL-7402 human cancer cell lines.

Effects of Lead and Selenium Interaction on Acetylcholinesterase Activity in Brain and Accumulation of Metal in Tissues of Oreochromis niloticus (L., 1758)

The potential accumulation of lead in different tissues of Oreochromis niloticus and the effects of selenium in AChE inhibition caused by lead in brain were investigated. Juvenile O. niloticus samples were exposed to combination of 1 mg L-1 and 2 mg L-1 lead and 1mg L-1 lead+2mg L-1 selenium and 2mg L-1 lead+4mg L-1 selenium for 1, 7 and 15 days respectively. The accumulation of lead in gill, brain, liver and muscle tissues was analyzed by Inductively Coupled Plasma Mass Spectrometry (ICP-MS) as well as brain acetylcholinesterase (AChE, E.C.3.1.1.7) enzyme activity was also analyzed by spectrophotometric method. No mortality was observed during lead exposure in relation to time period and exposed concentrations. Lead accumulation was occurred in all tissues in relation to time. Maximum lead accumulation occurred in brain tissue, followed by the liver, gills and muscle tissues in relation to time period. Selenium caused a decrease on accumulation of lead in tissues (all selenium mixtures in muscle tissue on the first day, 1mg L-1 Pb+2mg L-1 selenium in gill tissue on the seventh day, in liver tissue on the seventh day except 2mg L-1 Pb+4mg L-1 selenium mixtures) at the end of each of all three test periods. Inhibition of AChE activity was caused by the highest concentration and by the short-term effect of lead. Such effect of lead was eliminated by selenium mixture. Lead and selenium mixture were resulted an increase in activity on 15th day at the highest concentration. Selenium led to decrease in the accumulation of lead in the tissues and caused to improvement in the loss of AChE activity.

Phytochemical and pharmacological evaluation of organic and non-organic cultivated nutritional Centella asiatica collected after different time intervals of harvesting

The aim of the present study was to perform a comparative phytochemical and pharmacological evaluation of organically and non-organically cultivated nutritional Centella asiatica collected at different time intervals of harvesting. The fertilizers and pesticides applied in case of organic cultivation included combination of medicinal plants along with other natural products and the harvesting was carried out after 1st, 2nd and 3rd month of cultivation. From all the physicochemical parameters evaluated, the leaves collected after third month of harvesting showed higher ash values suggesting higher contents of sand or earthy matter along with higher moister content. The results from the phytochemical evaluations revealed that, the samples collected from first harvesting showed higher quantities of phytoconstituents. This was also confirmed through chromatographic studies using HPTLC showing higher content of Asiatic acid in samples collected after first month of harvesting, which was more pronounced in case of organic cultivation. The pharmacological evaluation included comparative nootropic activity of different samples of organic and nonorganic C. asiatica. The results depicted a significant (p<0.05) reduction in escape latency of mice treated with 100mg/kg, p.o. of organic and nonorganic cultivated C. asiatica collected after first month of harvesting and also showed a significant increase in the spatial working memory, which included acquisition and retrieval trials. Further, the two samples also revealed significant inhibition in AChE activity as observed in different brain region i.e. hippocampus, prefrontal cortex and amygdale, where organically cultivated C. asiatica was found to be more effective. Thus, from the overall observation, it may be concluded that, the organically cultivated C. asiatica, if collected after first month of cultivation shows the best memory enhancing activity as compared to other time interval of harvesting.

The effects of different solvents on bioactive metabolites and “in vitro” antioxidant and anti-acetylcholinesterase activity of Ganoderma lucidum fruiting body and primordia extracts

It is known that the lingzhi mushroom Ganoderma lucidum (Fr.) Karst produces various, bioactive metabolites. The objective of this study was to evaluate the antioxidant activity and acetylcholinesterase inhibitory activity of various extracts obtained from G. lucidum fruiting body and primordium, which is the initial stage of the mushroom’s fruiting body. Classical extraction of G. lucidum fruiting bodies and primordia using different solvents (water, methanol, acetone, ethanol and hexane) at two temperatures (at 25 °C and at the boiling point of the solvent) was performed.The influence of a solvent on the extraction yields and afterwards on the activity of the extract was observed. The extracts are rich in phenols, polysaccharides and proteins. The highest yield of 23.30% was obtained after water extraction. The total phenolic content was between 9 mgGA/g and 74.36 mgGA/g for G. lucidum fruiting bodies extracts and from 11.16 mgGA/g to 103.32 mgGA/g for G. lucidum primordia extracts. The antioxidant activity using the DPPH* free radical scavenging method was from 0.48% to 23.66% and from 5.32% to 54.57% for fruiting bodies and primordia extracts, respectively.Assessment of acetylcholinesterase enzyme inhibition was carried out using a colorimetric method based on Ellman’s reaction. Acetylcholinesterase enzyme inhibition (AChE inhibition) by G. lucidum fruiting bodies extracts was between 18.1% and 32.5%. The highest AChE inhibitory activity of primordia extracts was 29.48%. This is the first report of G. lucidum primordia extracts and their biological activity.

Antioxidant activity, acetylcholinesterase inhibitory potential and phytochemical analysis of Sarcocephalus latifolius Sm. bark used in traditional medicine in Sudan

BackgroundSarcocephalus latifolius is used as a traditional medicine for curing many diseases in Sudan. The main objective of the current study was to determine the antioxidant activity and acetylcholinesterase inhibition (AChEI) of S. latifolius, and to estimate its total phenolic and flavonoid contents.MethodsAntioxidant activity of the tested plant extracts was carried out by determining their ability to scavenge the 2,2-diphenyl-1-picryl hydrazyl (DPPH) free radical. On the other hand, AChE inhibitory activity was determined spectrophotometrically using the Ellman’s colorimetric method. The levels of total phenols and flavonoids were determined quantitatively using spectrophotometric methods. MTT assay was consumed to assess the cytotoxic effect of the most active fractions. These fractions were subjected to phytochemical analysis using GC-MS techniques to determine thier chemical composition.ResultsHexane and chloroform fractions exhibited the highest antioxidant activity with IC50 values of (0.098 ± 0.08 and 0.099 ± 0.029 mg/ml) respectively. Standard propyl gallate had the lowest IC50 value of 0.0414 ± 0.11 mg/ml. The ethanolic crude extract showed low AChEI activity with 40.2 ± 0.10%. High concentrations of phenolic and flavonoid contents were observed. GCMS revealed the presence of well-known antioxidants compounds e.g. Vitamin E and caffeic acid.ConclusionThe ethanolic extract of bark of S. latifolius showed potent antioxidant effects and low AChEI activity, high phenolic and flavonoid contents and presence of pharmacologically active compounds. These findings explain its wide usages in traditional medicine.

One-pot microwave assisted stereoselective synthesis of novel dihydro-2′H-spiro[indene-2,1′-pyrrolo-[3,4-c]pyrrole]-tetraones and evaluation of their antimycobacterial activity and inhibition of AChE

An efficient one-pot microwave assisted stereoselective synthesis of novel dihydro-2′H-spiro[indene-2,1′-pyrrolo[3,4-c]pyrrole]-tetraone derivatives through three-component 1,3-dipolar cycloaddition of azomethine ylides generated in situ from ninhydrin and sarcosine with a series of 1-aryl-1H-pyrrole-2,5-diones is described. The synthesised compounds were screened for their antimycobacterial and AChE inhibition activities. Compound 4b (IC50 1.30µM) has been found to display twelve fold antimycobacterial activity compared to cycloserine and it is thirty seven times more active than pyrimethamine. Compound 4h displays maximum AchE inhibitory activity with IC50 value of 0.78±0.01µmol/L.

Tebuconazole alters morphological, behavioral and neurochemical parameters in larvae and adult zebrafish (Danio rerio)

In this study, we evaluated the effects of tebuconazole on morphology and exploratory larvae behavior and adult locomotion. Furthermore, we analyzed the effects of this fungicide on AChE activity and gene expression in zebrafish larvae and in the adult zebrafish brain. Tebuconazole (4 mg/L) increased the ocular distance in larvae and reduced the distance travelled, absolute turn angle, line crossing and time outside area in exposed larvae. Moreover, adult zebrafish that were exposed to this fungicide (4 and 6 mg/L) showed a decrease in distance travelled and mean speed when compared to the control group. However, tebuconazole did not alter the number of line crossings or time spent in the upper zone. Tebuconazole inhibited AChE activity at concentrations of 4 mg/L for larvae and 4 and 6 mg/L in the adult zebrafish brain. However, this fungicide did not alter AChE gene expression in the adult zebrafish brain but increased AChE mRNA transcript levels in larvae. These findings demonstrated that tebuconazole could modulate the cholinergic system by altering AChE activity and that this change may be associated with the reduced locomotion of these animals.

Polyphenol-rich fraction of Parquetina nigrescens mitigates dichlorvos-induced neurotoxicity and apoptosis

BackgroundParquetina nigrescens (Afzel.) Bullock of the family Asclepiadaceae is known for its antioxidant effects with wide range of uses in Southwestern Nigeria especially in traditional medicine. This study was undertaken to explore if polyphenol-rich fraction (prf) from P. nigrescens will ameliorate dichlorvos-induced neurotoxicity and apoptosis. The exploration utilized evaluation of markers of oxidative stress, apoptosis and serum acetylcholinesterase (AchE) levels. MethodsForty Wistar rats randomly placed in four groups were utilized for the study. Animals in Group A received corn oil, group B- dichlorvos (16 mg/kg), groups C and D- dichlorvos + 100 and 200 mg/kg prf of P. nigrescens respectively. Markers of oxidative stress, antioxidants and apoptosis were assessed in the serum and brain tissues using biochemical assay and immunohistochemistry. ResultsExposure to dichlorvos caused significant decreases in AchE, catalase, superoxide dismutase, glutathione peroxidase (GPx) and increases in hydrogen peroxide (H2O2) generation and malondialdehyde levels. Histopathology and immunohistochemistry of the cerebellum and cerebrum of rats exposed to dichlorvos revealed greater neurotoxic effects in the cerebellum as well as decreased expressions of AchE with a concomitant increase in Bax (proapototic) compared to prf of P. nigrescens treated rats. ConclusionThis study showed that dichlorvos caused cellular and tissue neurotoxicity by inhibiting AchE activity, induced oxidative stress and apoptosis in rats with prominent effects on the cerebellum than cerebrum. The prf of P. nigrescens showed amelioration of neurotoxicity by its antioxidative and antiapoptotic properties in rats exposed to dichlorvos.

The anti-AChE and anti-proliferative Activities of Glaucium acutidentatum and Glaucium corniculatum Alkaloid Extracts

In this study, methanol and water extracts of Glaucium acutidentatum and Glaucium corniculatum were analysed for anti-AChE activity on neuronal PC12 cell and anti-proliferative activity on HT-29 and HeLa cancer cells. In this study, total alkaloid, phenol and flavonoid content were analyzed for the determination of active compounds of Glaucium acutidentatum and Glaucium corniculatum. Indeed, methanol and water alkaloid extracts of these plants were evaluated for their anti-AChE activities on NGF-differentiated PC12 cells (dPC12) and anti-proliferative activities on HT-29 and HeLa cancer cells. Our data showed that alkaloid was major compound, the different concentrations of plant extracts had 35-90% in vitro AChE inhibitory activity and 26-54% cellular AChE inhibitory activity and it is dose dependent manner. Furthermore, G. acutidentatum methanolic extracts showed the highest anti-proliferative activity in HT-29 cells (45±5%) Both 1000 μg/ml methanolic extracts showed the maximum anti-proliferative effect in HeLa cells (64±3%). In conclusion, this study has shown that the anti-AChE and anti-proliferative effects of these two plants and the presence of a new AChEi may be effective in AD and cancer.