BRIEF COMMUNICATION
Anticholinesterase activity of selected phenolic acids and flavonoids – interaction testing in model solutions
1
Department of Biotechnology, Human Nutrition and Food Commodity Science, University of Life Sciences, Lublin, Poland
Corresponding author
Dominik Szwajgier
Department of Biotechnology, Human Nutrition and Food Commodity Science, University of Life Sciences, Lublin, Poland
Department of Biotechnology, Human Nutrition and Food Commodity Science, University of Life Sciences, Lublin, Poland
Ann Agric Environ Med. 2015;22(4):690-694
KEYWORDS
ABSTRACT
Introduction:
Alzheimer’s disease is a progressively developing neurodegenerative disorder of the central nervous system. The only present treatment of this disease is the use of acetyl- and butyrylcholinesterase inhibitors. Previously, the neuroprotection of phenolic acids and flavonoids in the brain has been indicated.
Material and Methods:
This study measured anticholinesterase activities of 9 phenolic acids and 6 flavonoids, singly or in combination. The synergy/antagonism/zero interaction between compounds was evaluated taking into consideration the statistical significance. Ellman’s modified spectrophotometric method was used with the simultaneous measurement of the false-positive effect of compounds.
Results:
The anti-acetylcholinesterase activity of phenolic acids was as follows: homogentisic acid > 4-hydroxyphenylpyruvic acid > nordihydroguaiaretic acid > rosmarinic acid > caffeic acid > gallic acid = chlorogenic acid > homovanillic acid > sinapic acid. p-Hydroxyphenylpyruvic, caffeic, chlorogenic, gentisic, homogentisic, nordihydroguaiaretic and rosmarinic acids in pairs exhibited, in most cases, a lower inhibitory activity (at p>0.05), than the sum of the activities of single compounds. Also, phenolic acids in pairs with flavonoids (cyanidin, delphinidin, kaempferol, myricetin, phloridzin, pelargonidin or quercetin) presented, in most cases, a lower inhibitory activity than could be calculated for both compounds singly (at p>0.05). Only in the case of a few samples was the inhibitory activity of two compounds higher than the sum of inhibitions exerted by the same compounds tested singly (either at p>0.05 or p<0.05). The lack of synergy of pairs of inhibitors suggests one small binding site, making impossible to accommodate both inhibitors adjacent to one another.
Abbreviations:
AD, Alzheimer’s disease; AChE, acetylcholinesterase; BChE, butyrylcholinesterase; 4-OH-PP, 4-hydroxyphenylpyruvic acid; CA, caffeic acid; CHA, chlorogenic acid; GA, gentisic acid; HGA, homogentisic acid; HVA, homovanillic acid; NDGA, nordihydroguaiaretic acid; RA, rosmarinic acid; SA, salicylic acid; KAE, kaempferol; PEL, pelargonidin; QUE, quercetin; PHL, phloridzin; DEL, delphinidin; CYA, cyanidin; MYR, myricetin; ATChI, acetylthiocholine iodide; BTCh, S-butyrylthiocholine chloride; DTNB, 5,5’-dithiobis-2-nitrobenzoic acid.
Alzheimer’s disease is a progressively developing neurodegenerative disorder of the central nervous system. The only present treatment of this disease is the use of acetyl- and butyrylcholinesterase inhibitors. Previously, the neuroprotection of phenolic acids and flavonoids in the brain has been indicated.
Material and Methods:
This study measured anticholinesterase activities of 9 phenolic acids and 6 flavonoids, singly or in combination. The synergy/antagonism/zero interaction between compounds was evaluated taking into consideration the statistical significance. Ellman’s modified spectrophotometric method was used with the simultaneous measurement of the false-positive effect of compounds.
Results:
The anti-acetylcholinesterase activity of phenolic acids was as follows: homogentisic acid > 4-hydroxyphenylpyruvic acid > nordihydroguaiaretic acid > rosmarinic acid > caffeic acid > gallic acid = chlorogenic acid > homovanillic acid > sinapic acid. p-Hydroxyphenylpyruvic, caffeic, chlorogenic, gentisic, homogentisic, nordihydroguaiaretic and rosmarinic acids in pairs exhibited, in most cases, a lower inhibitory activity (at p>0.05), than the sum of the activities of single compounds. Also, phenolic acids in pairs with flavonoids (cyanidin, delphinidin, kaempferol, myricetin, phloridzin, pelargonidin or quercetin) presented, in most cases, a lower inhibitory activity than could be calculated for both compounds singly (at p>0.05). Only in the case of a few samples was the inhibitory activity of two compounds higher than the sum of inhibitions exerted by the same compounds tested singly (either at p>0.05 or p<0.05). The lack of synergy of pairs of inhibitors suggests one small binding site, making impossible to accommodate both inhibitors adjacent to one another.
Abbreviations:
AD, Alzheimer’s disease; AChE, acetylcholinesterase; BChE, butyrylcholinesterase; 4-OH-PP, 4-hydroxyphenylpyruvic acid; CA, caffeic acid; CHA, chlorogenic acid; GA, gentisic acid; HGA, homogentisic acid; HVA, homovanillic acid; NDGA, nordihydroguaiaretic acid; RA, rosmarinic acid; SA, salicylic acid; KAE, kaempferol; PEL, pelargonidin; QUE, quercetin; PHL, phloridzin; DEL, delphinidin; CYA, cyanidin; MYR, myricetin; ATChI, acetylthiocholine iodide; BTCh, S-butyrylthiocholine chloride; DTNB, 5,5’-dithiobis-2-nitrobenzoic acid.
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