• Applied Biological Chemistry
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• v.31 no.3
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• pp.241-248
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• 1988

In order to determine the approptiate usage of insecticides to honeybee(Apis mellifera L.), median effective dose to seven insecticides were studied. $LC_(50)$ value of DDT was the highest as being 58 ppm, and that of EPN was the lowest as being 1.61ppm. Various detoxifying enzymes from the midget cf adult worker bee, including microsomal oxidases, glutathione Stransferases, esterases, and DDT-dehydrochlorinase were assayed. Effects of various insecticides on microsomal enzyme activities were as follows: Aldrin epoxidase activity was inhibited by malathione and permethrin treatment. N-demethylase activity was induced by diazinon and EPN treatment and O-demethlase activity was induced by diazinon treatment. Of the glutathione S-transferases, aryltransferase(DCNB conjugation) activity was significantly induced by diazinon, and moderately induced by permethrin. Of the esterases, ${\alpha}-NA$ esterase activity was moderately inhibited by malatjione and permethrin. Acetylcholinesterase activity was not affected by the sublethal exposure of honeybee to the insecticides. Sublethal exposure of honeybee to the insecticides had no effect on DDT-dehydrochlorinase activity, except carbaryl and permethrin were significantly induced.

• Journal of Physiology & Pathology in Korean Medicine
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• v.16 no.2
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• pp.279-288
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• 2002

This research investigates the effect of the Crataegus pinnatifida BGE. var. major N.E. BR(CPVM) on Alzheimer's disease. The CPVM extract suppressed the expression of IL-1 β, IL-6, APP, AChE mRNA in PC-12 cells treated with CT105. The CPVM extract suppressed the AChE activity, and the production of APP significantly in PC-12 cells treated with CT105. The CPVM extract group showed a significant inhibitory effect on the memory deficit for the mice with Alzheimer's disease induced by CT105 in the Morris water maze experiment. The CPVM extract suppressed the over-expression of IL-1 β, TNF- α and ROS in the mice with Alzheimer's disease induced by CT105. This study suggests that CPVM may be effective for the prevention and treatment of Alzheimer's disease.

• Archives of Pharmacal Research
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• v.28 no.9
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• pp.1092-1096
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• 2005

Huperzine A-loaded microspheres composed of poly(D,L-lactide-co-glycolide) were prepared by an O/w emulsion solvent evaporation method. The characterization of the microspheres such as drug loading, size, shape and release profile was described. The in vitro release in the initial 7 days was nearly linear with $10\%$ released per day. Thereafter drug release rate became slow gradually and about $90\%$ drug released at day 21. The in vitro release rate determined by dialysis bag method had a good correlation with the in vivo release rate. Huperzine A aqueous solution was intramuscularly injected (i.m.) at 0.4mg/kg and microspheres were intra­muscularly injected at 8.4 mg eq huperzine A/kg in rats. The maxium plasma concentration $(C_{max})$ after i.m. microspheres was only $32\%$ of that after i.m. solution. Drug in plasma could be detectd until day 14 and about $5\%$ of administered dose was residued at the injection site at day 14. The relative bioavailability of huperzine A microspheres over a period of 14 days was $94.7\%$. Inhibition of acyecholinesterase activity (AchE) in rat's cortex, hippocampus and striatum could sustain for about 14 days. In conclusion, huperzine A-loaded microspheres possessed a prolonged and complete drug release with significant inhibition of AchE for 2 weeks in rats.

• Korean Journal of Pharmacognosy
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• v.48 no.4
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• pp.304-313
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• 2017

These days, as the average span of population's life increases, the number patients of dementia also increases. But Research on Korean medicine is stilled limited. The research evaluates the effect of the extract from Cornus officinalis S.et Z on cognitive impairment induced by scopolamine in mice. The mice were randomly divided into five groups of ten mice. The normal group was treated with only 0.9% saline. The control group was treated with scopolamine (5 mg/kg, i.p.). The positive control group was treated with tacrin. The C100, 200 group was treated with C. officinalis extracts 100, 200 mg/kg. Memory-related behaviors were evaluated using a morris water maze and a passive avoidance test. Protein levels of BDNF, p-CREB (ser133), immunohistochemistry staining, and cholinergic activities were measured in brain tissue. The effects of C. officinalis extract significantly increased acetylcholine concentration and decreased acetylcholinesterase activity. The C. officinalis extract affected memory formation. Also, to confirm expression of protein BDNF, p-CREB (ser133) in the hippocampus, the researchers observed that immunohistochemistry and western blot increased in C. officinalis extract. These results suggest that C. officinalis provides a significant neuroprotective effect against scopolamine-induced cholinergic system and cognitive impairment.

• 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 Haehwa Medicine
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• v.12 no.1
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• pp.11-26
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• 2003

Alzheimer's disease (AD) is characterized by amyloid deposition and associated loss of neunons in brain regions involved in learning and memory processes. Several causes of evidence support that the congnitive disturbance is closed associated with the deficit of cerebral acetylcholine neurotransmission, and the effect of carboxyl terminal 105 amino acid fragment (CT105) of the amyloid precursor protein (APP) on the gene expression of proinflammatory cytokines. We tested it on the scopolamine-induced amnesia model of the ICR mouse using the Morris water maze with repeated orally administration of 1st Green-Tea extract (200 mg/kg) and 2nd Green-Tea extract (200 mg/kg). The Green-Tea prevents impairment of learning and memory and neuronal loss in mouse models of cognitive disturbance and it demonstrated selectivity for inhibition of acetylcholinesterase (AChE). Furthermore, the repeated administration of Green-Tea, CT105-induced alzheimer's mouse model showed central cholinergic activity by ameliorates learning and memory impairment, and isolation of CD14 microglia showed significantly decreases intracellular release of the proinflammatory cytokines tumor necrosis factor-${\alpha}$, interleukin-$1{\beta}$ and reactive oxygen species (ROS). Because of its composite profile, oral therapeutic index and a prophylactic, Green-Tea is considered the better therapeutic candidate for the treatment of Alzheimer's disease.

• Korean Journal of Pharmacognosy
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• v.48 no.2
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• pp.119-124
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• 2017

Taraxacum platycarpum H. Dahl. (Compositae) has been used as an anti-inflammatory or anti-cancer agent in the clinic. Although its antidepressant effect has been reported, however, its cognitive function is not investigated until yet. In the present study, we investigated whether the water extract of T. platycarpum (WETP) could improve cognitive function in cholinergic blockade-induced amnesia mouse model using the passive avoidance or Y-maze task. WETP (12.5, 25 or 50 mg/kg) significantly ameliorated the scopolamine-induced cognitive impairment both in the passive avoidance test and the Y-maze test. In addition, WETP significantly inhibited acetylcholinesterase (AChE) activity measured by an ex vivo study using the mouse whole brain. These results suggest that WETP alleviates the cognitive dysfunction caused by the cholinergic blockade, in part, via AChE inhibition, and that it may be a useful for treating cognitive dysfunction.

• Journal of the Korean Society of Food Culture
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• v.36 no.6
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• pp.633-639
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• 2021

Raphanus sativus var. hortensis f. raphanistroides Makino (Korean wild radish [WR]) are root vegetables belonging to the Brassicaceae family. These radish species mostly grow in sea areas in Asia, where they have been traditionally used as a medicinal food to treat various diseases. To investigate the effect of WR on neuronal cell death in SH-SY5Y cells, beta-amyloid was used to develop the cell death model. WR attenuated neuronal cell death in SH-SY5Y and regulated the mitogen-activated protein kinase (MAPK) signaling. WR extract also inhibited acetylcholinesterase inhibitor activity. Additionally, the WR treatment group ameliorated the behavior of the memory-impaired mice in a scopolamine-induced mouse model. In the behavior test, WR treated mice showed shorter escape latency and swimming distance and improved the platform-crossing number and the swimming time within the target quadrant. Furthermore, WR prevented histological loss of neurons in hippocampal CA1 regions induced by scopolamine. This study shows that WR can prevent memory impairment which may be a crucial way for the prevention and treatment of memory dysfunction and neuronal cell death.

• Journal of Applied Biological Chemistry
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• v.65 no.1
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• pp.23-31
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• 2022

Oxidative stress and neuroinflammation play important roles in the pathogenesis of Alzheimer's disease (AD). This study investigated the protective effects of paeoniflorin (PF) against neuronal oxidative stress and neuroinflammation in lipopolysaccharide (LPS)-induced mice. The brains of LPS-injected control group showed significantly increased neuroinflammation by activating the nuclear factor kappa B (NF-κB) pathway and increasing inflammatory mediators. However, administration of PF significantly attenuated oxidative stress by inhibiting lipid peroxidation, nitric oxide levels, and reactive oxygen species production in the brain; PF at doses of 5 and 10 mg/kg/day downregulated the expression of NF-κB pathway-related proteins and significantly decreased inflammatory mediators including inducible nitric oxide synthase and cyclooxygenase-2. Moreover, the levels of brain-derived neurotrophic factor and its receptor, tropomycin receptor kinase B, were significantly increased in PF-treated mice. Furthermore, acetylcholinesterase activity and the ration of B-cell lymphoma 2 (Bcl-2)/Bcl-2 associated X were significantly reduced by PF in the brains of LPS-induced mice, resulting in the inhibition of cholinergic dysfunction and neuronal apoptosis. Thus, we can conclude that administration of PF to mice prevents the development of LPS-induced AD pathology through the inhibition of neuronal oxidative stress and neuroinflammation, suggesting that PF has a therapeutic potential for AD.

• Korean Journal of Environmental Agriculture
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• v.8 no.1
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• pp.47-54
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• 1989

This study was conducted to investigate insecticide toxicities to a honeybee, Apis cerana F. being raised in Korea and its detoxifying enzyme activities. In order to determine the appropriate usage of insecticides, median effective dose and detoxifying enzyme activities to seven insecticides were observed. Various detoxifying enzymes, including microsomal oxidases, glutathione S-transferases, esterases, and DDT-dehydrochlorinase were assayed in the midguts of adult worker bees as the enzyme source. Of the insecticides used, $LC_{50}$ value in DDT treatment was the highest as 19ppm, and that in EPN treatment was the lowest as 0.75ppm. Sublethal exposures of honeybees to various insecticides had some effects on microsomal enzyme activities. Aldrin epoxidase activity was inhibited by malathion and demeton S-methyl treatment. N-demethylase activity was induced by carbaryl treatment. Of the glutathione S-transferases, aryltransferase(DCNB conjugation) activity was significantly induced by diazinon, and moderately induced by malathion. Of the esterases, ${\alpha}-NA$ esterase activity was moderately inhibited by malathion and permethrin. Carboxylesterase and acetylcholinesterase activity were not affected by the sublethal exposure of honeybee to the insecticides. Sublethal exposure of honeybee to the insecticides had no effect on DDT- dehydrochlorinase activity, except carbaryl, malathion and demeton S-methyl were inhibited.