• YAKHAK HOEJI
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• v.39 no.4
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• pp.450-460
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• 1995

The acute toxicity of fthalide in rat was studied in vivo by the observations of the changes in hematogram, serological parameters, content of cytochrome p-450, activities of NADPH-cytochrom c reductase, glucose-6-phosphatase, and the contents of cholinesterase and carboxylesterase in liver. Fthabde is a practically non-toxic substance(LD50 is 3.86g/kg), but rats were intoxicated with fthabde at a oral dose of 100 mg/kg for 12 days. WBC were significantly decreased and activities of ALT and LDH, on the cotrary, the content of glucose in serum were slightly increased. Cytochrome p-450 and lipid peroxide in liver were significantly increased in the fthalide-intoxicated rats. The longer administration of fthalide showed further increase of carboxylesterase activity in liver and serum, but decrease of activities of glucose-6-phosphatase and cholinesterase in liver and serum. These results show that fthatide can induce the hepatocellular injury and neurotoxicity.

• YAKHAK HOEJI
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• v.46 no.3
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• pp.185-191
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• 2002

Alzheimer's disease (AD) involves neuronal degeneration with impaired cholinergic transmission, particularly in areas of the brain associated with learning and memory. Several cholinesterase inhibitors are widely prescribed to ameliorate the cognitive deficits in AD patients. In an attempt to examine if tacrine and donepezil, two well-known cholinesterase inhibitors, exhibit additional pharmacological actions in primary cultured rat cortical cells, we investigated the effects on neuronal injuries induced by glutamate or N-methyl-D-aspartate (NMDA), $\beta$-amyloid fragment ( $A_{{beta}25-35)}$), and various oxidative insults. Both tacrine and donepezil did not significantly inhibit the excitotoxic neuronal damage induced by glutamate. However, tacrine inhibited the toxicity induced by NMDA in a concentration-dependent fashion. In addition, tacrine significantly inhibited the $A_{{beta}25-35)}$-induced neuronal injury at the concentration of 50 $\mu$M. In contrast, donepezil did not reduce the NMDA- nor $A_{{beta}25-35)}$-induced neuronal injury. Tacrine and donepezil had no effects on oxidative neuronal injuries in cultures nor on lipid peroxidation in vitro. These results suggest that, in addition to its anticholinesterase activity, the neuroprotective effects by tacrine against the NMDA- and $A_{{beta}25-35)$-induced toxicity may be beneficial for the treatment of AD. In contrast, the potent and selective inhibition of central acetylcholinesterase appears to be the major action mechanism of donepezil.

• Journal of Preventive Medicine and Public Health
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• v.57 no.1
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• pp.73-82
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• 2024

Objectives: The unsafe use of pesticides in agriculture represents a major hazard to human health. This study was conducted to investigate the association between pesticide exposure and health symptoms among chili farmers in northeast Thailand. Methods: This cross-sectional analytic study included 141 chili farmers in Sakon Nakhon Province, in northeast Thailand. Data regarding health symptoms were gathered using a self-report questionnaire. A medical technician tested blood cholinesterase activity using an erythrocyte method, and an occupational medicine specialist at Ramathibodi Hospital in Bangkok, Thailand reviewed the results. Associations between personal characteristics, pesticide exposure factors, and health symptoms were analyzed using multiple logistic regression. Results: Of the 141 chili farmers studied, 66.7% experienced pesticide poisoning, as indicated by below-normal cholinesterase levels. Fatigue was the most frequently reported symptom associated with pesticide exposure, affecting 37.6% of participants. This was followed by nausea and vomiting (31.9%), dizziness (14.9%), and dry throat (14.9%). Multivariate logistic regression analysis revealed that several factors were significantly associated with adverse symptoms: amount of work experience, volume of pesticides used, use of chemical pesticides, use of leaking containers during spraying, direct pesticide exposure while working, contact with pesticide-soaked clothing, consumption of food and drinks in the fields, and blood cholinesterase level indicating risk. Conclusions: This study suggests potential health risks for chili farmers stemming from exposure to and contamination by pesticides used in agricultural practices. To mitigate these risks, it is essential to supply personal protective equipment and to implement educational programs aimed at improving protective behaviors among farmers.

• 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.

• 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.

• Proceedings of the Korean Society of Fisheries Technology Conference
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• 1998.06a
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• pp.239-240
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• 1998

• Korean Journal of Clinical Laboratory Science
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• v.50 no.3
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• pp.225-235
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• 2018

Phellinus gilvus is a medicinal mushroom used that has been used in folk medicine in Asian countries for centuries. The aim of this study was to investigate the anti-xanthine oxidase, anti-cholinesterase, and anti-inflammatory activities of methanol (ME) and hot water (HW) extracts prepared from fruiting bodies of Ph. gilvus. ME and HW had good anti-xanthine oxidase (XO) activities compared to allopurinol, an inhibitor of xanthine oxidase. ME showed comparable and slightly lower inhibitory activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), respectively, than galanthamine, a standard AChE and BChE inhibitor. ME also showed a protective effect against glutamate-induced cytotoxicity at 40 mg/mL and 100 mg/mL in PC-12 cells. ME (0.5~2.0 mg/mL) significantly inhibited nitric oxide (NO) production in RAW 264.7 murine macrophage cells stimulated with lipopolysaccharide (LPS). Carrageenan-induced hind-paw edema in rats was significantly reduced 2~6 hr after treatment with 50 mg/kg of ME, which was comparable to administration of 5 mg/kg of indomethacin, the positive control. These results demonstrate that ME and HW of Ph. gilvus fruiting bodies possess good anti-xanthine oxidase, anti-cholinesterase, and anti-inflammatory activities.

• Journal of Preventive Medicine and Public Health
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• v.25 no.2 s.38
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• pp.180-188
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• 1992

The effects of multiple exposures to pesticides on plasma cholinesterase(ChE) activities and urinary p-nitrophenol excretion were evaluated in rats. Rats were received single dose i.p. with $LD_{50}/100(mg/kg)$ of organophosphorous(OP), organophosphorous-organochroline(OP-OC), organophosphorous-carbamate(OP-CAB), organophosphorous-organoarsenate(OP-OA) pesticides for 4 consecutive days. In repeated administration of pesticides, plasma ChE activities were decreased, but urinary p-nitrophenol were increased after the first injection and then decreased gradually The recovery rates of ChE activities and p-nitrophenol excretion at 48 hours after the fourth Injection were delayed in comparision with the baseline value of 24 hours before the first injection. Statistical significances were found between OP and other groups except OP-OA group after the second injection in plasma ChE activities, but in urinary p-nitrophenol excretion there was statistical significance only between OP and OP-CAB.

• Natural Product Sciences
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• v.24 no.4
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• pp.259-265
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• 2018

The three flavone glycosides, 4'-O-methylisoscutellarein 7-O-(6'''-O-acetyl)-${\beta}$-D-allopyranosyl(1${\rightarrow}$2)-${\beta}$-D-glucopyranoside (1), isoscutellarein 7-O-(6'''-O-acetyl)-${\beta}$-D-allopyranosyl(1${\rightarrow}$2)-${\beta}$-D-glucopyranoside (3), and isoscutellarein 7-O-${\beta}$-D-allopyranosyl(1${\rightarrow}$2)-${\beta}$-D-glucopyranoside (4) in addition to a flavonol glycoside, kaempferol 3-O-${\beta}$-D-glucopyranoside (astragalin, 2), were isolated from Stachys japonica (Lamiaceae). In cholinesterase inhibition assay, compound 1 significantly inhibited aceylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities ($IC_{50}s$, $39.94{\mu}g/ml$ for AChE and $86.98{\mu}g/ml$ for BChE). The content of isolated compounds were evaluated in this plant extract by HPLC analysis. Our experimental results suggest that the flavonoid glycosides of S. japonica could prevent the memory impairment of Alzheimer's disease.

• Journal of Mushroom
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• v.18 no.3
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• pp.260-267
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• 2020

Phellinus baumii, a white-rot fungus, has been used for centuries as folk medicine in China, Japan, and Korea. This study aimed to evaluate the in vitro anti-diabetic, and anti-cholinesterase, and in vivo anti-inflammatory effects of the fruiting bodies of P. baumii. The methanol (ME) and hot water (HE) extracts (2.0 mg/mL) of P. baumii fruiting bodies suppressed α-amylase activity, exactly 61.33%, and 65.00%, respectively; of note, acarbose, the positive control, inhibited 93.33% of the α-amylase activity. Moreover, the ME and HE (2.0 mg/mL) inhibited 89.67% and 91.00%, respectively, of the activity of α-glucosidase activity, whereas the same concentration of acarbose suppressed 84.67% of the α-glucosidase activity. The ME and HE (1.0 mg/mL) also inhibited 96.05% and 94.58%, respectively, of the acetylcholinesterase (AChE) activity; galanthamine, the positive control, led to an inhibition of 81.12%. The butyrylcholinesterase (BChE) activity was also inhibited by ME and HE (1.0 mg/mL; 91.05% and 82.27%, respectively); of note, the same concentration of galanthamine suppressed 81.12% of the BChE activity. The production of NO in LPS-induced RAW 264.7 macrophages was significantly suppressed by both ME and HE treatments. Importantly, the carrageenan-activated rat hind-paw edema was significantly reduced 2-6 h after ME administration (50 mg/mL). Taken together, the results suggest that the fruiting bodies of P. baumii have α-amylase, α-glucosidase, α-cholinesterase, and anti-inflammatory activities, and, therefore, may be good natural sources for the promotion of human health.