Anti-cholinesterase activity of the standardized extract of Syzygium aromaticum L.

Dalai, Manoj Kumar; Bhadra, Santanu; Chaudhary, Sushil Kumar; Bandyopadhyay, Arun; Mukherjee, Pulok K.

doi:10.4103/0973-1296.133275

Cited by 32 publications

(7 citation statements)

References 19 publications

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“…The increase in the brain AChE activity following aluminium exposure of rats was attributed to an allosteric interaction between Al with the peripheral anionic site of the enzyme molecule (50). The ability of eugenol to directly suppress the enhanced AChE activity following Al intoxication in the current study could be explained with the finding of an in vitro study that demonstrated a potential anti-cholinesterase property of eugenol (51). Similarly, eugenol was found to normalise the cortical AChE level in acrylamide-induced brain neuropathy in rats (21).…”

Section: Figure 3 Effect Of Eugenol And/or Aluminium On Brain Acetylcsupporting

confidence: 58%

Neuroprotective effects of eugenol against aluminiuminduced toxicity in the rat brain

Said

Rabo

2017

Archives of Industrial Hygiene and Toxicology

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Aluminium (Al) is a neurotoxic metal that contributes to the progression of several neurodegenerative diseases. The aim of the present study was to evaluate the protective effect of dietary eugenol supplementation against aluminium (Al)- induced cerebral damage in rats. Male Wistar rats were divided into four groups: normal controls, rats fed a diet containing 6,000 μg g-1 eugenol, rats intoxicated daily with aluminium chloride (84 mg kg-1 body weight) p. o. and fed either a basal diet or a eugenol-containing diet. Daily oral administration of Al for four consecutive weeks to rats significantly reduced brain total antioxidant status (TAS) (11.42±0.31 μmol g-1 tissue, p<0.001) with a subsequent significant enhancement of lipid peroxidation (MDA) (32.55±1.68 nmol g-1 tissue, p<0.002). In addition, Al enhanced brain acetylcholinesterase activity (AChE) (46.22±4.90 U mg-1 protein, p<0.001), tumour necrosis factor alpha (TNF-α) (118.72±11.32 pg mg-1 protein, p<0.001), and caspase 3 (Casp-3) (8.77±1.26 ng mg-1 protein, p<0.001) levels, and in contrast significantly suppressed brain-derived neurotrophic factor (BDNF) (82.74±14.53 pg mg-1 protein, p<0.002) and serotonin (5-HT) (1.54±0.12 ng mg-1 tissue, p<0.01) levels. Furthermore, decreased glial fibrillary acidic protein (GFAP) immunostaining was noticed in the striatum of Al-intoxicated rats, compared with untreated controls. On the other hand, co-administration of dietary eugenol with Al intoxication restored brain BDNF (108.76±2.64 pg mg-1 protein) and 5-HT (2.13±0.27 ng mg-1 tissue) to normal levels, enhanced brain TAS (13.43±0.24 μmol g-1 tissue, p<0.05), with a concomitant significant reduction in TNF-α (69.98±4.74 pg mg-1 protein) and Casp-3 (3.80±0.37 ng mg-1 protein) levels (p<0.001), as well as AChE activity (24.50±3.25 U mg-1 protein, p<0.001), and increased striatal GFAP immunoreactivity, compared with Al-treated rats. Histological findings of brain tissues verified biochemical data. In conclusion, eugenol holds potential as a neuroprotective agent through its hydrophobic, antioxidant, and anti-apoptotic properties, as well as its neurotrophic ability against Al-induced brain toxicity in rats.

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Section: Figure 3 Effect Of Eugenol And/or Aluminium On Brain Acetylcsupporting

confidence: 58%

Neuroprotective effects of eugenol against aluminiuminduced toxicity in the rat brain

Said

Rabo

2017

Archives of Industrial Hygiene and Toxicology

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“…Analgesia produced by EOEC in the acute corneal pain appears to depend on its cholinergic activity, since EOEC effect was completely antagonized by the muscarinic cholinergic receptor antagonist atropine. In vitro studies of clove oil and eugenol have shown potent anti-acetylcholinesterase property ( 29 30 ). Since cholinergic system activation by muscarinic agonist or cholinesterase inhibitors have shown to produce analgesic effects, anti-acetylcholinesterase activity of EOEC and eugenol might also be in agreement with its mechanisms of their antinociception ( 31 32 ).…”

Section: Discussionmentioning

confidence: 99%

Effects of topical and systemic administration of Eugenia caryophyllata buds essential oil on corneal anesthesia and analgesia

Khalilzadeh¹,

Hazrati²,

Saiah³

2016

Res Pharma Sci

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Clinical studies suggest that essential oil of Eugenia caryophyllata (Clove) buds (EOEC) is efficacious in the treatment of dental pain. In the present study, we investigated the analgesic and local anesthetic effects of EOEC and its possible mechanisms of action in acute corneal pain in rats. EOEC was extracted by hydro-distillation in a Clevenger type apparatus from clove buds. The acute corneal pain was induced by applying a drop (40 µl) of 5 M NaCl solution on the corneal surface, and the numbers of eye wipes were counted during the first 30 s. The mechanical sensation of the cornea was evaluated by calibrated Von Frey filaments. Systemic administration of EOEC (100 and 200 mg/kg, SC) and morphine (2.5 and 5 mg/kg, IP) produced a significant antinociceptive effect in acute corneal pain. Pretreatment with naloxone or atropine prevented the EOEC-induced analgesia. However, L-arginine and methylene blue did not change the suppressive effect of EOEC on corneal pain response. Topical application of EOEC, eugenol and lidocaine significantly decreased corneal sensitivity. Combination treatments of eugenol (25 µg) with lidocaine (0.5%) and EOEC (50 µg) with lidocaine (0.5%) also significantly suppressed corneal sensitivity. Systemic administration of EOEC produced analgesia in the acute corneal pain through mechanisms that involved both opioidergic and cholinergic systems. In addition, topical instillation of EOEC, eugenol, and lidocaine produced local anesthesia in the rat cornea. Sub-anesthetic doses of EOEC or eugenol produced a significant local anesthetic effect when concurrently used with the sub-anesthetic dose of lidocaine.

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“…While in MFA eugenol, methyl eugenol, myristic acid, galbacin and β-sitosterol were identified as an AChE inhibiting compounds. These identified compounds showed potent AChE inhibitory activity (Cuong et al, 2014;Mukherjee et al, 2014;Ayaz et al, 2017;Vargas-Méndez et al, 2019). TLC-MS-bioautography is a simple and fast method to identify bioactive compounds showing AChE activity.…”

Section: Discussionmentioning

confidence: 99%

Development of Synergy-Based Combination for Learning and Memory Using in vitro, in vivo and TLC-MS-Bioautographic Studies

et al. 2021

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The present study is aimed at developing a synergistic combination to enhance learning and memory in Alzheimer’s patients with the help of eight common medicinal plants used in the AYUSH system. Aqueous and hydroalcoholic extracts of eight medicinal plants from the AYUSH system of medicine were prepared. These were subjected to in vitro anticholinesterase activity, to find out the combination index of synergistic combination. The synergistic combination and their individual extracts were subjected to total phenol, flavonoid and antioxidant activity estimation. Further, in vivo neurobehavioral studies in rats were carried out followed by TLC-MS-bioautographic identification of bioactive metabolites. Out of the sixteen extracts, aqueous extracts of Withania somnifera (L.) Dunal (WSA) and Myristica fragrans (L.) Dunal (MFA) were selected for the development of synergistic combination based on their IC50 value in vitro anticholinesterase assay. The synergistic combination inhibited the anticholinesterase activity significantly as compared to the individual extracts of WSA and MFA. The synergistic combination also showed more phenolic and flavonoid contents with potential antioxidant activity. The TLC-bioautography showed four white spots in WSA, signifying sitoindosides VII, VIII, quercetin, isopelletierine and Withanolide S as AChE inhibitory compounds while showing five white spots of anti-cholinesterase active metabolites identified as eugenol, methyl eugenol, myristic acid, galbacin and β-sitosterol in MFA. The observation of neurocognitive behavior in amnesia induced subjects manifested that both the synergistic combinations showed comparable results to that of standard piracetam, though the synergistic combination containing a higher concentration of WSA showed more appreciable results in ameliorating dementia in rats. The study suggests that the synergy based combination successfully enhanced memory and learning by abating free radical and acetylcholine levels, and increased learning and memory in rats, providing a strong rationale for its use in the treatment of dementia and Alzheimer’s disease.

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Anti-cholinesterase activity of the standardized extract of Syzygium aromaticum L.

Cited by 32 publications

References 19 publications

Neuroprotective effects of eugenol against aluminiuminduced toxicity in the rat brain

Neuroprotective effects of eugenol against aluminiuminduced toxicity in the rat brain

Effects of topical and systemic administration of Eugenia caryophyllata buds essential oil on corneal anesthesia and analgesia

Development of Synergy-Based Combination for Learning and Memory Using in vitro, in vivo and TLC-MS-Bioautographic Studies

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