Acetylcholinesterase inhibitors as Alzheimer therapy: From nerve toxins to neuroprotection

Singh, Manjinder; Kaur, Maninder; Kukreja, Hitesh; Chugh, Rajan; Silakari, Om; Singh, Devinder

doi:10.1016/j.ejmech.2013.09.050

Cited by 305 publications

(183 citation statements)

References 178 publications

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“…It is composed of aglycone tomatidine and a tetrasaccharide residue containing d-galactose, two molecules of d-glucose, and d-xylose. Steroidal alkaloids from tomato have several biological activities, including antiviral, anti-fungal, antibacterial, anti-inflammatory, cholesterol lowering, and immunopotentiating properties (Friedman 2002;Khalid et al 2004;Milner et al 2011;Friedman 2013;Singh et al 2013).…”

Section: Introductionmentioning

confidence: 99%

Chemical Constitutions and Antioxidant Activities of Tomato Leaf Extracts

Lee¹,

Lee²,

Ma³

et al. 2016

Plant Breed. Biotech.

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This is an Open-Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/4.0) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited. ABSTRACT The present study aimed to determine the contents of five flavonols and two glycoalkaloids as well as the antioxidant activities of leaf ethanol extracts of 50 tomato accessions. The antioxidant activity was assessed using different tests: 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), 2,2-diphenyl-1-picryl hydrazyl (DPPH), nitric oxide (NO), and total polyphenol content (TPC). Flavonols and glycoalkaloids contents were determined using a high performance liquid chromatography-diode array detector system. Among five flavonols and two glycoalkaloids, naringenin and tomatine were detected in tomato leaves at high concentrations. Of the 50 tomato accessions, IT 229711, IT2365203, and IT 207224 were found to have the highest contents of quercetin, kaempferol, and tomatine, respectively. Leaf extract of IT189949 exhibited the highest relative antioxidant capacity index (RACI). Among the five flavonols, myricetin showed positive correlations with DPPH, ABTS, and NO, while isorhamnetin had positive correlation with DPPH. These results will expand the chemical constitution database and provide information on tomato leaves. They are valuable for the development of functional foods or feed-additives.

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Section: Introductionmentioning

confidence: 99%

Chemical Constitutions and Antioxidant Activities of Tomato Leaf Extracts

Lee¹,

Lee²,

Ma³

et al. 2016

Plant Breed. Biotech.

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“…Recently, research on AChE inhibitor has been rapidly developed due to the availability of supporting facilities for designing AChE inhibitor compounds in the treatment of AD (Singh et al, 2013). Promising compounds to be developed as AChE inhibitor were chalcone derivatives (Sukumaran et al, 2016;Tran et al, 2016).…”

Section: Introductionmentioning

confidence: 99%

Computer-aided Design of Chalcone Derivatives as Lead Compounds Targeting Acetylcholinesterase

Riswanto

Hariono

Yuliani

et al. 2017

Indonesian J. Pharm.

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One of well-established biological activities for chalcone derivatives is as acetylcholinesterase inhibitors, which can be developed for the therapy of Alzheimer's disease. Assisted by retrospectively validated structure-based virtual screening (SBVS) protocol to identify potent acetylcholinesterase inhibitors, 80 chalcone derivatives were designed and virtually screened. The F-measure value as the parameter of the predictive ability of the SBVS protocol developed in the research presented in this article was 0.413, which was considerably better than the original SBVS protocol (Fmeasure=0.226). Among the screened chalcone derivatives two were selected as potential lead compounds to design potent inhibitors for acetylcholinesterase: 3-[4-(benzyloxy)-3-methoxyphenyl]-1-(4-hydroxy-3-methoxy-phenyl)prop-2-en-1-one(3k) and 3-[4-(benzyloxy)-3-methoxyphenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one (4k).

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“…Among these, acetylcholinesterase inhibitors (AChEI) have lately become a very active research topic because they increase the level of acetylcholine (ACh), which is abnormally low in disorders associated with cognitive processes, memory and neuromuscular activity [4]. Due to this fact, AChEIs have application in the treatment of Alzheimer's disease [5], to combat myasthenia gravis, glaucoma, and as antidotes to toxins [6]. Many natural compounds from plants, with a wide diversity of structural features, are AChEIs [7].…”

Section: Introductionmentioning

confidence: 99%

Anti-acetylcholinesterasic, antioxidant and antibacterial activities of Juniperus brevifolia extracts

Oliveira¹,

Medeiros²,

Rosa³

et al. 2015

Integr Pharm Toxicol Gentoxicol

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Juniperus brevifolia (Seub.) Antoine (Cupressaceae) is an endemic conifer of the Azores, a habitat isolated from the continental masses which may significantly influence the biosynthesis of bioactive compounds with unique features. In this context, the toxicity, antibacterial, antioxidant (DPPH) and anti-acetylcholinesterasic (anti-AChE) activities of the methanol and acetone extracts of J. brevifolia wood and bark were evaluated for the first time. In the brine-shrimp assay all the extracts showed low toxicity, with the concentration causing 50% mortality (LC 50 ) higher than 2.03 mg/mL. The acetone extract of the bark proved to be the most active against Bacillus cereus, B. subtilis and Micrococcus luteus, while the wood acetone extract showed activity only against B. cereus. No activity was observed against Gram (-) bacteria Escherichia coli and Enterobacter cloacae. The acetone extract of bark was the most active showing the higher antioxidant (EC 50 =7.0 µg/mL) and antiAChE activities (IC 50 =193 µg/mL), near to the reference compounds, quercetin (EC 50 =3.2 µg/mL) and ursolic acid (IC 50 =190 µg/mL), respectively. The present study demonstrates the great potential of the acetone bark extract of J. brevifolia as a source of new non-toxic natural bioactive compounds as antioxidant and antiacetylcholinesterasic drugs.

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Acetylcholinesterase inhibitors as Alzheimer therapy: From nerve toxins to neuroprotection

Cited by 305 publications

References 178 publications

Chemical Constitutions and Antioxidant Activities of Tomato Leaf Extracts

Chemical Constitutions and Antioxidant Activities of Tomato Leaf Extracts

Computer-aided Design of Chalcone Derivatives as Lead Compounds Targeting Acetylcholinesterase

Anti-acetylcholinesterasic, antioxidant and antibacterial activities of Juniperus brevifolia extracts

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