Isolation of the Acetylcholinesterase Inhibitor Ungeremine from Nerine bowdenii by Preparative HPLC Coupled On-Line to a Flow Assay System

Rhee, In Kyung; Appels, Natalie M. G. M.; Hofte, Bertil; Karabatak, Bahadir; Erkelens, C.; Stark, Lucy M.; Flippin, Lee A.; Verpoorte, Robert

doi:10.1248/bpb.27.1804

Cited by 60 publications

(43 citation statements)

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“…It exerts acute toxic effects to pests by irreversible inhibition of the cholinesterase enzyme from breaking down acetylcholine (Rhee et al, 2004). Due to its biodegradability and short residence time in the environment, organophosphate insecticides are being increasingly used, among which dimethoate is one of the important organophosphate insecticide indiscriminately used in India.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of genotoxic and oxidative stress response to dimethoate in freshwater fish Channa punctatus (Bloch)

Ali

Kumar

et al. 2014

Chemical Speciation & Bioavailability

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Dimethoate is one of the organophosphate insecticides widely used in agriculture throughout the world and is an inhibitor of cholinesterase in animals. The objective of the present study was to detect oxidative stress and DNA damage induced by dimethoate in the freshwater fish Channa punctatus (C. punctatus). The LC 50 -96 h value of technical grade dimethoate was estimated at 19.10 µg L -1 in a semi-static system and, on the basis of the LC 50 value, three concentrations were determined. The fish were exposed to these concentrations of dimethoate for 96 h and samplings were done at 24 and 96 h for assessment of oxidative stress and DNA damage. After exposure to dimethoate, the level of superoxide dismutase declined while lipid peroxidation, glutathione, induction of micronucleus and DNA damage were increased in C. punctatus as the concentration and exposure time increased. Thus our results suggest that dimethoate induces genotoxic effects which invariably accompanied and correlated with oxidative stress.

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Section: Introductionmentioning

confidence: 99%

Evaluation of genotoxic and oxidative stress response to dimethoate in freshwater fish Channa punctatus (Bloch)

Ali

Kumar

et al. 2014

Chemical Speciation & Bioavailability

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“…Hence, in the current senario, inhibitors of AChE and BuChE have become a major target for the development of therapeutic strategies for AD. The ChE inhibitors directly block the ACh and BuCh hydrolysis thereby promoting the cholinergic functions, which ultimately results in the improvement of cognitive deficit (Rhee et al, 2004). There are a few synthetic medicines, like tacrine, donepezil and rivastigmine, for treatment of cognitive dysfunction and memory loss associated with AD.…”

Section: Introductionmentioning

confidence: 99%

Antioxidant and anti-cholinesterase activity ofSargassum wightii

Syad

Shunmugiah

Kasi

2013

Pharmaceutical Biology

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Context: Sargassum has been used in traditional Chinese medicine since the eighth century AD to treat goiter. Sargassum wightii Greville (Sargassaceae) is a major source of alginic acid used widely in food and drug industries. Objective: To evaluate the anti-Alzheimer potential of S. wightii through evaluation of antioxidant and cholinesterase inhibitory activities. Materials and methods: Successive extraction was done using solvents of varying polarity. Solvent extracts (100-500 mg/mL) were employed for all the antioxidant assays. Free radical scavenging activity was evaluated by 2,2-diphenyl-1-picrylhydrazyl, OH. , H 2 O 2 radical scavenging assay. The reducing power of the seaweed was evaluated by ferric reducing antioxidant power and reducing power assay. Cholinesterase (ChE) inhibitory activity was evaluated and the Km, Vmax and Ki were calculated. Further, compound characterization was done by GC-MS analysis. Results: The non-polar extracts were found to possess significant antioxidant activity. At 100 mg/mL, petroleum ether, hexane, benzene and dichloromethane extracts showed significant ChE inhibitory activity with IC 50 values of 19.33 AE 0.56, 46.81 AE 1.62, 27.24 AE 0.90, 50.56 AE 0.90 mg/mL, respectively, for AChE, and 17.91 AE 0.65, 32.75 AE 1.00, 12.98 AE 0.31, 36.16 AE 0.64 mg/mL, respectively, for BuChE. GC-MS reveals that 1,2-benzenedicarboxylic acid, diisooctyl ester is the major compound present in dichloromethane extract of S. wightii. The mode of inhibition exhibited by dichloromethane extract against the cholinesterases was found to be competitive type. Discussion and conclusion: The presence of high amount of terpenoids could be the possible reason for its potential antioxidant and ChE inhibitory activity.

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“…Among the plant families that have been examined for their AChE inhibitory activity are: Amaryllidaceae (Houghton et al 2004, Rhee et al 2004, Boraginaceae (Ahmad et al 2003b), Chenopodiaceae (Ferheen et al 2005), Lamiaceae (Ahmad et al 2005), Liliaceae (Atta-urRahman et al 2002), and Solanaceae (Roddick 1989.…”

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In vitro inhibition of acetylcholinesterase by crude plant extracts from Colombian flora

Niño

Hernández

Correa

et al. 2006

Mem. Inst. Oswaldo Cruz

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The methanol extracts from five different plant families (Asteraceae, Euphorbiaceae, Melastomataceae, Rubiaceae, and Solanaceae) collected at Regional Natural Park Ucumarí (Colombia), were screened for their acetylcholinesterase inhibitory activity through the modified Ellman's spectrophotometric method. The best inhibitory activities on this study were shown by the extracts of Solanum leucocarpum Dunal (IC 50 = 204.59 mg/l) and Witheringia coccoloboides (Damm) (IC 50 = 220.68 mg/l), both plants belonging to the Solanaceae family.Key words: acetylcholinesterase (AChE) inhibitors -Asteraceae -Euphorbiaceae -Melastomataceae -Rubiaceae -SolanaceaeThe acetylcholinesterase enzyme (AChE) is an attractive target for the rational drug design and for the discovery of mechanism based inhibitors because of its role in the hydrolysis of the neurotransmitter acetylcholine (ACh). AChE inhibitors are the most effective approach to treat the cognitive symptoms of Alzheimer disease (AD) (Kalauni et al. 2002) and other possible therapeutic applications in the treatment of Parkinson's disease, senile dementia, and ataxia, among others (Ahmad et al. 2003a). AChE inhibitors as eserine, tacrine, donepezil, rivastigmine, and galanthamine are the only drugs currently approved for the treatment of AD; however, these drugs are known to have limitations for clinical use due to their short-half-lives and/or unfavorable side-effects (Sung et al. 2002).Because the search of plant extracts that selectively inhibit AChE is of paramount importance to find novel and more potent AChE inhibitors, many of them have been screened and as consequence there have been found extracts and isolated pure compounds with AChE and/or butyrylcholinesterase (BChE) inhibitory properties. Among the plant families that have been examined for their AChE inhibitory activity are: Amaryllidaceae Continuing with the study of the flora from Regional Natural Park Ucumarí (RNPU, Risaralda, Colombia) as a source of new secondary metabolites with diverse grade of biological activities (Niño et al. 2003, 2006, Mosquera et al. 2004a) and the fact that there still is great interest in finding novel and better AChE inhibitors, prompted us to screen 27 crude methanol extracts belonging to the Asteraceae, Euphorbiaceae, Melastomataceae, Rubiaceae, and Solananceae families for their AChE inhibitory activities. MATERIALS AND METHODSIn this study, the solvent hexanes, dichloromethane, and methanol (analytical-reagent grade) were purchased from Mallinckrodt (Phillipsburg, NJ, US). Silica gel plates (Silica gel 60 F 254 0.2 mm layer thickness) were purchased from Merck (Darmstadt, Germany). The electric eel acetylcholinesterase Sigma (St Louis, MO, US) was used. Acetylthiocholine iodide and 5,5-dithiobis (2-nitro benzoic acid) (DTNB) were purchased from Aldrich (St Louis, MO, US). A Spectronic Genesys 5 spectrophotometer Milton Roy (Rochester, NY, US) was used for all measurements of acetylcholinesterase inhibitory activity.Plant material -Twenty seven plants from the selected famili...

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Isolation of the Acetylcholinesterase Inhibitor Ungeremine from Nerine bowdenii by Preparative HPLC Coupled On-Line to a Flow Assay System

Cited by 60 publications

References 21 publications

Evaluation of genotoxic and oxidative stress response to dimethoate in freshwater fish Channa punctatus (Bloch)

Evaluation of genotoxic and oxidative stress response to dimethoate in freshwater fish Channa punctatus (Bloch)

Antioxidant and anti-cholinesterase activity ofSargassum wightii

In vitro inhibition of acetylcholinesterase by crude plant extracts from Colombian flora

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