Acetylcholinesterase - AChE: A Pharmacological Interesting Enzyme

Araújo, Cleônia Roberta Melo; Santos, Victória Laysna dos Anjos; Gonsalves, Arlan de Assis

doi:10.21577/1984-6835.20160122

Cited by 41 publications

(22 citation statements)

References 17 publications

(21 reference statements)

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“…Cholinesterases are enzymes that hydrolyze the neurotransmitter acetylcholine (ACh) in acetate and choline and are found in various parts of the human body being classified in acetylcholinesterase and burthyrylcholinesterase. Therefore, the improvement of the antioxidant status and inhibition of AChE enzyme are suggested as a beneficial tool with therapeutic potential in the prevention of aging and dementia (Araújo et al, 2016). Some flavonoids act by inhibiting AChE activity, increasing the concentration of this cholinergic neurotransmitter (Khan et al, 2018).…”

Section: Introductionmentioning

confidence: 99%

In vitro and in vivo evaluation of enzymatic and antioxidant activity, cytotoxicity and genotoxicity of curcumin-loaded solid dispersions

Sá

Perón

Leimann

et al. 2019

Food and Chemical Toxicology

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Curcumin, the main bioactive polyphenolic compound in Curcuma longa L. rhizomes has a wide range of bioactive properties. Curcumin presents low solubility in water and thus limited bioavailability, which decreases its applicability. In this study, cytotoxic effects of curcumin solid dispersions (CurSD) were evaluated against tumor (breast adenocarcinoma and lung, cervical and hepatocellular carcinoma) and non-tumor (PLP2) cells, while cytotoxic and genotoxic effects were evaluated in Allium cepa. The effect of the CurSD on the acetylcholinesterase (AChE), butyrylcholinesterase (BChE), glutathione S-transferase (GST), and monoamine oxidase (MAO A-B) enzymes was determined, as well as its capacity to inhibit the oxidative hemolysis (OxHLIA) and the formation of thiobarbituric acid reactive substances (TBARS). CurSD are constituted by nanoparticles that are readily dispersible in water, and inhibited 24% and 64% of the AChE and BChE activity at 100 μM, respectively. GST activity was inhibited at 30 μM while MAO-A and B activity were inhibited at 100 μM. CurSD showed cytotoxicity against all the tested tumor cell lines without toxic effects for non-tumor cells. No cytotoxic and genotoxic potential was detected with the Allium cepa test. CurSD maintained the characteristics of free curcumin on the in vitro modulation of important enzymes without appreciable toxicity.

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Section: Introductionmentioning

confidence: 99%

In vitro and in vivo evaluation of enzymatic and antioxidant activity, cytotoxicity and genotoxicity of curcumin-loaded solid dispersions

Sá

Perón

Leimann

et al. 2019

Food and Chemical Toxicology

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“…Acetylcholinesterase inhibitory drugs are termed anticholinesterases, and these are therapeutically used to reverse the neuromuscular blockade promoted by depolarizing myorelaxants, in the treatment of neurological diseases such as MG and myasthenic syndrome, in smooth muscle atony, in strabismus, and in the treatment of symptoms of Alzheimer's disease, among others. An anticholinesterase drug delays the degradation of ACh, so the neurotransmitter spends more time in the synaptic cleft, thus intensifying cholinergic transmission, as can be observed in Figure 2 [20][21][22].…”

Section: Acetylcholinesterase Inhibitorsmentioning

confidence: 99%

Interaction between Pyridostigmine Bromide and Oxidative Stress

Azzolin¹,

Barbisan²,

Jung³

et al. 2021

Medical Toxicology

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In this chapter the following topics will be addressed: (1) actions of the cholinergic system in the nervous system, commenting on acetylcholine metabolism and acetylcholinesterase metabolism; (2) acetylcholinesterase inhibitors as subtitle in this topic: pharmacological characterization of pyridostigmine bromide, mechanism of action, and therapeutic effect of the drug; (3) use of pyridostigmine bromide in Persian Gulf War; and (4) potential effect of pyridostigmine bromide in oxidative stress, addressing as subtitle the influence of pyridostigmine bromide on the superoxide-hydrogen peroxide imbalance model. Studies indicate that the interaction between pyridostigmine bromide and stressors could trigger genotoxicity, the mechanism associated with the induction of oxidative stress that leads to this side effect of this drug; however, this discussion needs to be better elucidated and may be more discussed as there is interaction between the pyridostigmine bromide and an endogenous oxidative imbalance caused by it or even by the possible interaction of this with genetic variations present in the antioxidant metabolism.

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“…Molecules capable of inhibiting or reactivating the AChE enzyme are potential substitutes for organophosphates. Success in developing products of these classes depends on the efficiency and practicality of the tests employed to evaluate AchE activity (Araújo et al 2016).…”

Section: Anticholinesterase Activity Of the Essential Oil (Eo)mentioning

confidence: 99%

Biocidal potential of Eugenia pyriformis essential oil in the control of Rhipicephalus (Boophilus) microplus in the free-living cycle

et al. 2019

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Brazil has one of the largest commercial cattle herds in the world, which naturally coexist with an enormous number of parasitic species. Southern cattle tick, Rhipicephalus (Boophilus) microplus, is among these species, interfering with animal productivity and causing losses to the beef and dairy cattle sector. The use of chemical acaricides in the control of this mite has resulted in the emergence of resistant populations. In this sense, alternative control measures using plants as sources of botanical acaricides have shown to be effective. Eugenia pyriformis Cambess is a Brazilian plant with antioxidant and antimicrobial activity; however, there are no reports on its acaricidal activity in the literature. The present study aimed to evaluate the acaricidal and larvicidal potential of E. pyriformis leaf essential oil (EO) on southern cattle tick at different stages of the reproductive cycle. E. pyriformis leaves were collected and dried, and had their EO extracted by hydrodistillation (3h) using a modified Clevenger apparatus. Chemical analysis was performed by gas chromatography coupled with mass spectrometry (GC/MS), and 32 compounds belonging to the sesquiterpene class were identified: hydrocarbons (17.98%) and oxygenated forms (81.96%), with spathulenol (43.65%) and caryophyllene oxide (12.17%) as the most common. The EO was evaluated by the Adult Immersion Test at the concentrations (500.00 to 3.12mg/mL) in which the following parameters were measured: mortality of females (%), hatchability of eggs (%), and product efficiency (%). Larvae were assessed by the Larval Packet Test at concentrations ranging from 25.00 to 0.00004mg/mL. Lethal concentrations (LC) required for killing 50 and 99.9% of adult females and larvae were determined using Probit analysis. LC50 and LC99.9 of EO were 0.06 and 24.60mg/mL and 1,208.80 and 2,538mg/mL for larvae and adult females, respectively. Action of the EO in the free-living cycle of R. (B.) microplus larvae was another parameter assessed. To this end, the larvae were deposited in pots containing Brachiaria decumbens and, after migration to the leaf apex, a solution containing LC99.9 (24.60mg/mL) of the EO was sprayed. After 24h, 72.25% of the larvae had died, indicating stability of the EO when subjected to uncontrolled temperature and humidity conditions. The mechanism of action through which the EO killed the larvae and adult females was investigated by the Bioautographic Method, which showed inhibition of 3.15mg/mL of the EO on the acetylcholinesterase (AChE) enzyme. The results found in the present experiment indicate that E. pyriformis essential oil is an alternative in the control of southern cattle tick in the larval (parasitic) and free-living cycle (non-parasitic) stages under field conditions.

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Acetylcholinesterase - AChE: A Pharmacological Interesting Enzyme

Cited by 41 publications

References 17 publications

In vitro and in vivo evaluation of enzymatic and antioxidant activity, cytotoxicity and genotoxicity of curcumin-loaded solid dispersions

In vitro and in vivo evaluation of enzymatic and antioxidant activity, cytotoxicity and genotoxicity of curcumin-loaded solid dispersions

Interaction between Pyridostigmine Bromide and Oxidative Stress

Biocidal potential of Eugenia pyriformis essential oil in the control of Rhipicephalus (Boophilus) microplus in the free-living cycle

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