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Dual inhibition of acetylcholinesterase and butyrylcholinesterase enzymes by allicin.

Kumar S - Indian J Pharmacol (2015 Jul-Aug)

Bottom Line: For allicin, the IC₅₀ concentration was 0.01 mg/mL (61.62 μM) for AChE and 0.05 ± 0.018 mg/mL (308.12 μM) for BuChE enzymes.Allicin shows a potential to ameliorate the decline of cognitive function and memory loss associated with AD by inhibiting cholinesterase enzymes and upregulate the levels of acetylcholine (ACh) in the brain.It can be used as a new lead to target AChE and BuChE to upregulate the level of ACh which will be useful in alleviating the symptoms associated with AD.

View Article: PubMed Central - PubMed

Affiliation: University School of Biotechnology, GGS Indraprastha University, Dwarka, New Delhi, India.

ABSTRACT

Objectives: The brain of mammals contains two major form of cholinesterase enzymes, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The dual inhibition of these enzymes is considered as a promising strategy for the treatment of neurological disorder such as Alzheimer's disease (AD), senile dementia, ataxia, and myasthenia gravis. The present study was undertaken to explore the anticholinesterase inhibition property of allicin.

Materials and methods: An assessment of cholinesterase inhibition was carried out by Ellman's assay.

Results: The present study demonstrates allicin, a major ingredient of crushed garlic (Allium sativum L.) inhibited both AChE and BuChE enzymes in a concentration-dependent manner. For allicin, the IC₅₀ concentration was 0.01 mg/mL (61.62 μM) for AChE and 0.05 ± 0.018 mg/mL (308.12 μM) for BuChE enzymes.

Conclusions: Allicin shows a potential to ameliorate the decline of cognitive function and memory loss associated with AD by inhibiting cholinesterase enzymes and upregulate the levels of acetylcholine (ACh) in the brain. It can be used as a new lead to target AChE and BuChE to upregulate the level of ACh which will be useful in alleviating the symptoms associated with AD.

No MeSH data available.


Related in: MedlinePlus

Inhibition of bovine butyrylcholinesterase by different concentration of allicin. Values are expressed as ± standard error of the mean (n = 6). The equation of the line is y = 18.949x2 + 86.651x + 114.59; R2 = 0.9872
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Figure 2: Inhibition of bovine butyrylcholinesterase by different concentration of allicin. Values are expressed as ± standard error of the mean (n = 6). The equation of the line is y = 18.949x2 + 86.651x + 114.59; R2 = 0.9872

Mentions: The result showed that allicin inhibited the AChE in a concentration-dependent manner at different concentrations tested (0.003 mg/mL to 0.1 mg/mL) [Figure 1], a concentration of 0.1 mg/mL showed maximum inhibition which was 95%. The IC50 value was 0.01 ± 0.009 mg/mL (61.62 μM) derived from equation of Figure 1. This result demonstrated that allicin was a potent AChE inhibitor. In contrast to AChE inhibition, allicin also inhibited BuChE enzyme, but the inhibition was not as strong compared with AChE. The concentration of allicin tested in the range of 0.003–0.1mg/mL, showed percentage inhibition ranging from 16% to 56%, respectively. The maximum inhibition was observed at the concentration of 0.1 mg/mL (56%) [Figure 2]. The IC50 concentration calculated was 0.05 ± 0.018 mg/mL (308.12 μM) from the equation of Figure 2. The results showed that allicin was a weak BuChE inhibitor.


Dual inhibition of acetylcholinesterase and butyrylcholinesterase enzymes by allicin.

Kumar S - Indian J Pharmacol (2015 Jul-Aug)

Inhibition of bovine butyrylcholinesterase by different concentration of allicin. Values are expressed as ± standard error of the mean (n = 6). The equation of the line is y = 18.949x2 + 86.651x + 114.59; R2 = 0.9872
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4527070&req=5

Figure 2: Inhibition of bovine butyrylcholinesterase by different concentration of allicin. Values are expressed as ± standard error of the mean (n = 6). The equation of the line is y = 18.949x2 + 86.651x + 114.59; R2 = 0.9872
Mentions: The result showed that allicin inhibited the AChE in a concentration-dependent manner at different concentrations tested (0.003 mg/mL to 0.1 mg/mL) [Figure 1], a concentration of 0.1 mg/mL showed maximum inhibition which was 95%. The IC50 value was 0.01 ± 0.009 mg/mL (61.62 μM) derived from equation of Figure 1. This result demonstrated that allicin was a potent AChE inhibitor. In contrast to AChE inhibition, allicin also inhibited BuChE enzyme, but the inhibition was not as strong compared with AChE. The concentration of allicin tested in the range of 0.003–0.1mg/mL, showed percentage inhibition ranging from 16% to 56%, respectively. The maximum inhibition was observed at the concentration of 0.1 mg/mL (56%) [Figure 2]. The IC50 concentration calculated was 0.05 ± 0.018 mg/mL (308.12 μM) from the equation of Figure 2. The results showed that allicin was a weak BuChE inhibitor.

Bottom Line: For allicin, the IC₅₀ concentration was 0.01 mg/mL (61.62 μM) for AChE and 0.05 ± 0.018 mg/mL (308.12 μM) for BuChE enzymes.Allicin shows a potential to ameliorate the decline of cognitive function and memory loss associated with AD by inhibiting cholinesterase enzymes and upregulate the levels of acetylcholine (ACh) in the brain.It can be used as a new lead to target AChE and BuChE to upregulate the level of ACh which will be useful in alleviating the symptoms associated with AD.

View Article: PubMed Central - PubMed

Affiliation: University School of Biotechnology, GGS Indraprastha University, Dwarka, New Delhi, India.

ABSTRACT

Objectives: The brain of mammals contains two major form of cholinesterase enzymes, acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The dual inhibition of these enzymes is considered as a promising strategy for the treatment of neurological disorder such as Alzheimer's disease (AD), senile dementia, ataxia, and myasthenia gravis. The present study was undertaken to explore the anticholinesterase inhibition property of allicin.

Materials and methods: An assessment of cholinesterase inhibition was carried out by Ellman's assay.

Results: The present study demonstrates allicin, a major ingredient of crushed garlic (Allium sativum L.) inhibited both AChE and BuChE enzymes in a concentration-dependent manner. For allicin, the IC₅₀ concentration was 0.01 mg/mL (61.62 μM) for AChE and 0.05 ± 0.018 mg/mL (308.12 μM) for BuChE enzymes.

Conclusions: Allicin shows a potential to ameliorate the decline of cognitive function and memory loss associated with AD by inhibiting cholinesterase enzymes and upregulate the levels of acetylcholine (ACh) in the brain. It can be used as a new lead to target AChE and BuChE to upregulate the level of ACh which will be useful in alleviating the symptoms associated with AD.

No MeSH data available.


Related in: MedlinePlus