• Natural Product Sciences
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• v.25 no.2
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• pp.115-121
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• 2019

Alzheimer's disease is a chronic neurodegenerative disorder with no curative treatment. The commercially available drugs, which target acetylcholinesterase, are not satisfactory. The aim of this study was to investigate the cholinesterase inhibitory activity of Solenostemma argel aerial part. Eight compounds were isolated and identified by NMR: kaempferol-3-O-glucopyranoside (1), kaempferol (2), kaempferol-3-glucopyranosyl($1{\rightarrow}6$)rhamnopyranose (3) p-hydroxybenzoic acid (4), dehydrovomifoliol (5), 14,15-dihydroxypregn-4-ene-3,20-dione (6), 14,15-dihydroxy-pregn-4-ene-3,20-dione-$15{\beta}$-D-glucopyranoside (7) and solargin I (8). Two of them (compounds 2 and 3) could inhibit over 50 % of butyrylcholinesterase activity at $100{\mu}M$. Compound (2) displayed the highest inhibitory effect against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with a slight selectivity towards the latter. Molecular docking studies supported the in vitro results and revealed that (2) had made several hydrogen and ${\pi}-{\pi}$ stacking interactions which could explain the compound potency to inhibit AChE and BChE.

• Dementia and Neurocognitive Disorders
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• v.21 no.4
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• pp.107-116
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• 2022

Attention is being paid to diagnosis and treatment of mild cognitive impairment (MCI) because early diagnosis and preventive management can slow down the progression of Alzheimer's disease. In particular, in the present era, the use of biomarkers for predicting conversion into dementia is permitted in medical practice. Therefore, authors aimed to propose additional considerations when updating guidelines for the management of MCI, including predictable biomarkers, revising treatment option after additional clinical trials for cholinesterase inhibitors, and detailed regimes for lifestyle interventions. After reviewing 3 patients with MCI by detailed evaluation, we realized that cholinesterase inhibitors were not recommended. In addition, regular exercise and cognitive training were only possible recommendations for patients according to current guidelines, although all 3 patients had evidence of β-amyloid accumulation and related neurodegeneration. Furthermore, caregivers for all 3 patients were worried whether patients could keep doing regular exercise and cognitive training by themselves and asked about the economic training system which monitors patients so that they can keep training. Therefore, we propose that guidelines for managing MCI need to be updated in the present era when the use of biomarkers for predicting conversion into dementia is permitted in medical practice.

• Ocean and Polar Research
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• v.39 no.1
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• pp.45-49
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• 2017

During the search for anticholinesterase compounds from marine organisms, we were able to isolate 6,6'-bieckol from a red alga, Grateloupia elliptica. This compound showed moderate acetylcholinesterase (AChE) inhibitory activity in a micromole range ($IC_{50}$ $44.5{\mu}M$). However, for butyrylcholinesterase (BuChE), a new target for the treatment of Alzheimer's disease (AD), it showed particularly potent inhibitory activity ($IC_{50}$ $27.4{\mu}M$), which is more potent compared to AChE. It also inhibits BACE-1, a new target for reducing the generation of ${\beta}-amyloid$.

• Environmental Analysis Health and Toxicology
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• v.8 no.1_2
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• pp.1-10
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• 1993

This study was done to determine the toxic effect of fthalide in rats which have oral administration at levels of 100 mg/kg/day for twelve days. It was examined the hematogram and serological parameters, and also the content of cytochrome P-450, the activity of NADPH-cytochrome c reductase, glucose-6-phosphatase, cholinesterase and carboxylesterase in liver. Any significant alteration of hematogram was not found but the value of AST, LDH and content of glucose in serum were statistically increased. The content of cytochrome P-450, the activty of NADPH-cytochrome c reductase were increased but glucose-6-phosphatase were slightly decreased compare with that of control group. The activity of cholinesterase was decreased slightly and on the contrary the activity of carboxylesterase was found to be the tendeny of increase in both of liver and serum.

• Korean Journal of Pharmacognosy
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• v.47 no.2
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• pp.192-196
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• 2016

The herb of Agastache rugosa (Lamiaceae) called Korean mint as a spice or Agastache Herba as a crude drug is known to contain highly fragrant volatile substances. This research aimed to establish the quantitative gas chromatography (GC) method on the essential oil of A. rugosa using the three standard compounds, estragole, methyleugenol, pulegone, and to find whether the essential oil has anti-Alzheimer's activity. The GC quantification method was established by determining the linearity of calibration curve ($R^2$), linear range, and both limit-of-detection (LOD) and limit-of-quantification (LOQ). The $IC_{50}$ of the essential oil on the activities of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) were determined to be $69.06{\pm}0.26$ and $76.71{\pm}0.58{\mu}g/ml$, respectively.

• Journal of Environmental Health Sciences
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• v.22 no.3
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• pp.8-16
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• 1996

Effects of water extract of aloe vera on lead-induced neurotoxicity were investigated in sciatic nerve isolated from rat. The mechanism on toxicity reduction by measuring activities of axonal enzymes, metabolism of myo-inositol in nerve, lead concentration in several organs and so on were further examimed. In the lead-treated rats, the transport rate of axonal enzyme, such as acetyl cholinesterase and choline acetyltransferase, was reduced by from 50% to 30% respectively. Reduction in myo-inositol concentration and $Na^+/K^+$ ATPase activity were also observed in sciatic nerve from lead-treated rat. However, the aloe extract administration significantly eliminated the impairment and maintained myo-inositol concentration to about 85% of normal level. Also aloe extract promoted the excretion rate of lead which is accumulated in blood, sciatic nerve and kidney. These results suggest that lead-induced neurotoxicity was significantly reduced by administration of aloe extract and the mechanism might be partly increase in kidney excretion rate of lead and parity normalization of $Na^+/K^+$ ATPase activity which is critical factor in order to keep nerve maintaining normal myo-inositol level.

• Korean Journal of Pharmacognosy
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• v.43 no.2
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• pp.122-126
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• 2012

The MeOH extract of Evodiae Fructus exhibited a significant inhibition on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), in a dose dependent manner, respectively. The extensive bioactivity-guided fractionation process with the MeOH extract finally isolated four compounds, as rutaecarpine (1), evodiamine (2), limonin (3) and dehydroevodiamine (4). Among them, compound 2 exhibited specific inhibitory activity on BChE with the $IC_{50}$ values 1.7 ${\mu}g/ml$, whereas compound 4 showed the potent inhibition upon both AChE and BChE.

• Journal of Pharmaceutical Investigation
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• v.9 no.2
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• pp.22-30
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• 1979

Effects of Akebiae Lignum, whose scientific name is Akebia quinata Decaisne, on the blood pressure were investigated with EtOH extract in whole and spinal rabbits. Akebia Lignum EtOH extract (AEE), when given intravenously, produced a fall in blood pressure not only in whole rabbit but also in spinal rabbit and AEE administered into a lateral cerebral ventricle of whole rabbit did not elicit a fall in blood pressure. The depressor responses of the whole rabbit to intravenous AEE were weakened by treatment of the animals with atropine and chlorisondamine but not by vagotominijation, phentolamine avil, and then the depressor action causing by AEE in the whole rabbit was not affected by pretreatment of physostigmine which is cholinesterase inhibitor and of hemicholinium which blocks acetylcholine synthesis by interfering with choline uptake in nerves. These observations suggest that the hypotensive action of AEE of which component is not affected by cholinesterase is due to direct action at parasympathetic receptor.

• Archives of Pharmacal Research
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• v.26 no.10
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• pp.796-799
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• 2003

Two known farnesylacetone derivatives (1 and 2) were isolated from the Korean brown alga Sargassum sagamianum off Jeju Island, Korea. Compounds 1 and 2 were identified as (5E,10Z)-6, 10, 14-trimethylpentadeca-5, 10-dien-2, 12-dione and (5E,9E,13E)-6, 10,4-trimethylpentadeca-5,9,13-trien-2,12-dione, respectively, by comparison with the literature data. Compounds 1 and 2 showed moderate acetylcholinesterase and butyrylcholinesterase inhibitory activities with $IC_{50}$ values of 65.0∼48.0 and 34.0∼23.0 $\muM$, respectively.

• Bulletin of the Korean Chemical Society
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• v.28 no.2
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• pp.225-228
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• 2007

Lipoic acid (LA) is a multifunctional antioxidant against a variety of ROS. Nitrone acts as free radical spin trap and exhibits neuroprotective activity. Thus, LA-nitrone derivatives (6, 7, 8, and 9) were synthesized and screened as an antioxidant and inhibitors for cholinesterases. Even though the antioxidant effect of LA-nitrone derivatives was not improved, they turned out to be effective inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) in μM range.