• Title/Summary/Keyword: AChE활성저해

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Effeds of Malathion on the Development of the Chick Embryo Cerebrum (계배의 대뇌의 발생에 미치는 Malathion의 영향)

  • 김완종;등용건;최임순
    • The Korean Journal of Zoology
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    • v.31 no.3
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    • pp.191-206
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    • 1988
  • Chick embryos which have received a single injection of the organophosphate compound,malathion (0.1 mg, 0.5 mg, 1.0 mg or 2.0 mg in 0.05 ml of corn oil) via the yolk sac at certain times (2 daya, 4 days or 6 days after incubation) have been investigated. After 9 days of incubation, chick embryos were harvested to investigate the effects of malathion on the development of cerebrum morphologically and biochemically. The effects of simultaneous injection of malathion and nicotinamide were also compared. On ultrastructural examination, neurons in cerebral cortex showed to be inhibited in their differentiation by malathion; nuclear irregularity, swelling of endoplasmic reticulum, and cytoplasmic vacuoles were observed. On cytochemical study of acetylcholinesterase(AChE) by electron microscope, the positive reaction products of this enryme were localized at the membrane of nucleus and endoplasmic reticulum of neurons. Inhibition of AChE activty was severe in groups treated with relatively low doses, which was consistent with the results of spectrophotometric analysis. The activity of lactate dehydrogenase(LDH) of cerebrum in groups treated with malathion was higher than that of the control group. The nicotinamide adenine dinucleotide(NAD) content of chick embruo treated with malathioti decreased significantly, and nicotinamide coinjection raised the NAD level as compared with the control group, thus preventing malathion-induced momhological alteration. In conclusion, it is suggested that malathion changes the ultrastructure of differentiating neurons and alters some enzyme activities in chick embryo cerebrum, and the severity of which is consistently dose-or age-dependent.

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Evaluation of the Antioxidant Activity and Physiological Functionality of Baegilju (백일주의 항산화 활성 및 생리기능성 평가)

  • Cho, Young Ho;Byun, Tae Kang;Lee, Jong-Hwa;Lee, Gye Won
    • Journal of Life Science
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    • v.23 no.12
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    • pp.1525-1531
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    • 2013
  • Baegilju is a famous traditional Korean wine made over the course of 100 days. The physiological functionalities of Baegilju were evaluated using different tests. The spectrophotometric method was used to determine the total concentration of polyphenolics and flavonoids and DPPH and ABTS radicals. A nitrite scavenging assay was used to evaluate antioxidant activity. The fibrin plate method was used for fibrinolysis and to evaluate angiotensin I converting enzyme (ACE) inhibitory activity; finally, the colorimetric determination method was used to evaluate acetylcholinesterase (AChE) inhibitory activity. The total polyphenolic content of non-sterilized Baegilju and sterilized Baegilju were 391.59 ${\mu}g$ and 401.33 ${\mu}g$ tannic acid equivalents/ml, respectively; and the flavonoids contents were 284.75 ${\mu}g$ and 308.35 ${\mu}g$ quercetin equivalents/ml, respectively. Baegilju exhibited more excellent antioxidant activities (DPPH and ABTS radicals, nitrite scavenging activity) than did Cheongju. In addition, the fibrinolytic activity and AChE inhibitory activity were found to be higher in Baegilju than they were in Cheongju. The ACE inhibitory activity of non-sterilized Baegilju, sterilized Baegilju, and Cheongju were 23.62%, 19.99%, and 38.91%, respectively. Therefore, these results suggest that Baegilju has potential as an antioxidant agent and anti-thrombosis agent.

Neuronal Cell Protective Effect of Dendropanax morbifera Extract against High Glucose-Induced Oxidative Stress (High Glucose로 유도된 산화 스트레스에 대한 황칠나무 잎 추출물의 뇌신경세포 보호 효과)

  • Kim, Jong Min;Park, Seon Kyeong;Guo, Tian Jiao;Kang, Jin Yong;Ha, Jeong Su;Lee, Du Sang;Kwon, O-Jun;Lee, Uk;Heo, Ho Jin
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.45 no.7
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    • pp.938-947
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    • 2016
  • Antioxidant activities and neuroprotective effects of ethyl acetate fraction from Dendropanax morbifera (EFDM) against high glucose-induced oxidative stress and neurotoxicity were investigated to confirm their physiological activities. An 80% ethanolic extract of D. morbifera showed the highest contents of total phenolic compounds as well as 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) and 1,1-diphenyl-2-picrylhydrazyl radical scavenging activities. The extract was fractionated using several solvents, and the ethyl acetate fraction showed the highest activities in ferric reducing/antioxidant power and malondialdehyde inhibitory assays. To evaluate the neuroprotective effect based on antioxidant activities, cell viability was assessed using PC12 and MC-IXC cells in $H_2O_2$- and high glucose-induced cytotoxic assays, respectively. EFDM evidently showed neuroprotective effects in all cells (neuron-like PC12 cells and human brain-originated neuroblastoma MC-IXC cells). Inhibitory effect of the extract on acetylcholinesterase (AChE) as an acetylcholine-hydrolyzing enzyme was performed to examine the effect on cognitive function. EFDM presented an AChE inhibitory effect. Finally, high-performance liquid chromatography analysis showed that the major phenolic compound of EFDM is probably a rutin.

Effect of Insecticide Carbofuran and Phenobarbital Sodium and 3-Methylcholanthrene on Activity of Enzyme in Rat (살충제 Carbofuran과 Phenobarbital Sodium 및 3-Methylcholanthrene이 쥐의 효소활성에 미치는 영향)

  • Rim, Yo-Sup;Han, Seong-Soo
    • The Korean Journal of Pesticide Science
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    • v.3 no.3
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    • pp.27-36
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    • 1999
  • Effect of insecticide carbofuran and phenobarbital sodium(PB) or 3-methylcholanthrene(3-MC), they were orally administered by the chemicals, alone or in combination, on activities of several enzymes in rats were investigated. In in vivo test for the effect of this chemicals on activity of enzyme in rat, activities of acetylcholinesterase(AChE) and butyrylcholinesterase(BuCheE) were inhibited by $20{\sim}70%$ for 48 hrs after the oral administration of carbofuran alone of 3.8mg/kg, whereas those were lowered at the beginning, but recovered to the control level after 24 hrs, in case of the mixed administration of carbofuran+PB or carbofuran+3-MC. The activity of glutathione S-transferase(GST) was inhibited by more than 15 to 35% for an early period of 0.5 to 6 hrs, in the case of the administration of carbofuran alone, whereas that was slightly inhibited at the beginning, recovered almost to the control level after 3 hrs, and raised by mere than 20% above the control after 6 hrs, in case of the mixed administration of carbofuran+PB or carbofuran+3-MC. When carbofuran was administered alorig with PB or 3-MC, the activities of UDP-glucuronosyltransferase(UDPGT) and cytochrome P-450 were more than 2.6 to 2.8 times higher than that in the case of the administration of carbofuran alone for 6 hrs. These results suggest that a simultaneous application of carbofuran and PB or 3-MC is critical for the enhancentment of activity of GST, UDPGT and cytochrome P450 and the protection of rat from carbofuran toxicity.

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Anti-Xanthine Oxidase, Anti-Cholinesterase, and Anti-Inflammatory Activities of Fruiting Bodies of Phellinus gilvus (마른진흙버섯 자실체의 Xanthine Oxidase, Cholinesterase 및 염증 저해 효과)

  • Yoon, Ki Nam;Jang, Hyung Seok
    • 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.

Neuroprotective effect of fermented ginger extracts by Bacillus subtilis in SH-SY5Y cells (고초균에 의한 생강 발효 추출물의 신경세포 보호 효과)

  • Yang, Hee Sun;Kim, Mi Jin;Kim, Mina;Choe, Jeong-sook
    • Journal of Nutrition and Health
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    • v.54 no.6
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    • pp.618-630
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    • 2021
  • Purpose: The ginger rhizome (Zingiber officinale) is widely cultivated as a spice for its aromatic and pungent components. One of its constituents, 6-hydroxydopamine (6-OHDA) is usually thought to cross the cell membrane through dopamine uptake transporters, and induce inhibition of mitochondrial respiration and the generation of intracellular reactive oxygen species (ROS). This study examines the neuroprotective effect and acetylcholinesterase (AChE) inhibitory activity of fermented ginger extracts (FGEs) on 6-OHDA induced toxicity in SH-SY5Y human neuroblastoma cells. Methods: Ginger was fermented using 2 species of Bacillus subtilis, with or without enzyme pretreatment. Each sample was extracted with 70% ethanol. Neurotoxicity was assessed by applying the EZ-Cytox cell viability assay and by measuring lactic dehydrogenase (LDH) release. Morphological changes of apoptotic cell nuclei were observed by Hoechst staining. Cell growth and apoptosis of SH-SY5Y cells were determined by Western blotting and enzyme activity analysis of caspase-3, and AChE enzymatic activity was determined by the colorimetric assay. Results: In terms of cell viability and LDH release, exposure to FGE showed neuroprotective activities against 6-OHDA stimulated stress in SH-SY5Y cells. Furthermore, FGE reduced the 6-OHDA-induced apoptosis, as determined by Hoechst staining. The occurrence of apoptosis in 6-OHDA treated cells was confirmed by determining the caspase-3 activity. Exposure to 6-OHDA resulted in increased caspase-3 activity of SH-SY5Y cells, as compared to the unexposed group. However, pre-treatment with FGE inhibited the activity of caspase-3. The neuroprotective effects of FGE were also found to be caspase-dependent, based on reduction of caspase-3 activity. Exposure to FGE also inhibited the activity of AChE induced by 6-OHDA, in a dose-dependent manner. Conclusion: Taken together, our results show that FGE exhibits a neuroprotective effect in 6-OHDA treated SH-SY5Y cells, thereby making it a potential novel agent for the prevention or treatment of neurodegenerative disease.

Resistance Mechanisms of Green Peach Aphid, Myzus persicae (Homoptera: Aphididae), to Imidacloprid (복숭아혹진딧물(Myzus persicae)의 imidacloprid에 대한 저항성 기작)

  • 최병렬;이시우;유재기
    • Korean journal of applied entomology
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    • v.40 no.3
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    • pp.265-271
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    • 2001
  • Resistance mechanisms in the green peach aphid (Myzus persicae) resistant to imidacloprid were investigated. Imidacloprid residues on the aphid integuments decreased slowly as time passed with no significant difference between the susceptible and resistant strains. Residue in the aphid body increased in both strains with time elapse, and was slightly more in the susceptible strain. A higher metabolic rate of imidacloprid in the resistant strain can be expected by the fact that more amount of imidacloprid were excreted in the resistant strain than in the susceptible one. The activity of AChE was higher 1.4 times in the resistant strain than in the susceptible one, and imidacloprid did not inhibit AChE at all in both strains. Piperonyl butoxide (PBO) and iprobenfos (IBP) synergized imidacloprid activity. The mixtures of imidacloprid and PBO (1 : 1 and 1 : 5) caused 69.4- and 250-fold increase of imidacloprid toxicity against the aphid. Insecticide toxicity of the mixtures of IBP and imidacloprid (1 : 1 and 1 : 5) was also increased 227 and 80.6 times. Esterase activity when $\alpha$-naphtyl butyrate and $\beta$-naphtyl acetate were used as substrates was higher in the resistance strain than in the susceptible one. This means that P450 monooxygenase and esterase are responsible for the resistance to imidacloprid in this aphid strain.

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Mass-Production of Acetylcholinesterase Sensitive to Organophosphosphates and Carbamates Insecticides (유기인계 및 카바메이트계 농약의 고감수성 아세틸콜린에스테라이즈의 대량생산)

  • Kim, Young-Mee;K., Cho;Cho, Moon-Jae
    • Applied Biological Chemistry
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    • v.46 no.4
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    • pp.353-360
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    • 2003
  • For the simple rapid bioassay of organophosphorus and carbamate pesticide residues, a mass-production system of acetycholinesterase (AChE, EC 3.1.1.7, MAChE) using baculovirus and insect cell culture was constructed. The cDNA for AChE was synthesized from Drosophila melanogaster in Halla Mountain, the lipid anchor tail was removed by PCR and was used for the site-directed mutagenesis of three amino acid residues (E107Y, F368L, L408F). The mutated cDNA was inserted into the baculovirus vector and expressed in insect cells. Maximum cell growth and enzyme activity were reached when the cells $(2{\times}10^6\;cell/ml)$ were infected four times at four-day-intervals. His-tag containing MAChE was purified using Ni-NTA column and used for characterization. The activity was maintained under various pHs (3-10) and temperatures $(20-50^{\circ}C)$ under experimental conditions. As an extraction solution for pesticides, methanol is more effective than ethanol. Against major organophosphate and carbamate pesticides, the MAChE showed better sensitivity than AChE and AChE from housefly (Taiwan).

Inhibitory Effects of Some Herbal Extracts on the Acetylcholinesterase (AChE) In Vitro (생약추출물들의 acetylcholinesterase (AChE) 저해활성 검색)

  • Kim, Jeoung-Seob;Kim, Young-Sup;Kim, Seong-Kie;Heor, Jung-Hee;Lee, Bong-Ho;Choi, Byoung-Wook;Ryu, Geon-Seek;Park, Eun-Kyung;Zee, Ok-Pyo;Ryu, Shi-Yong
    • Korean Journal of Pharmacognosy
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    • v.33 no.3 s.130
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    • pp.211-218
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    • 2002
  • The methanol extracts of 340 kinds of Korean medicinal herbs were examined in vitro for the inhibitory effect on the acetylcholinesterase (AChE, E.C. 3.1.1.7) from electric eel using acetylthiocholine as a substrate. Among tested, the extracts of Coptidis Rhizoma, Phellodendri Cortex, Evodiae Fructus, Myrrha, Arecae Semen and Piperis nigri Fructus were found to exhibit a significant inhibition upon the acetylcholinesterase in a dose dependent manner, respectively.

Effects of Acorn (Quercus acutissima CARR.) Supplementation on the Level of Acetylcholine and Its Related Enzyme Activities in the Brain of Dementia Mouse Model (도토리 급여가 치매모델 마우스 뇌조직의 아세틸콜린 및 관련효소 활성에 미치는 영향)

  • Lee, Sung-Hyeon;Kim, Dae-Ik;Cho, So-Yong;Jung, Hyun-Jin;Cho, Soo-Muk;Park, Hong-Ju;Lillehoj Hyun S.
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.34 no.5
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    • pp.738-742
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    • 2005
  • This study was designed to investigate the anti-dementia effects of acorn (Quercus acutissima CARR.) in brain of the mouse. Dementia model was induced by administration of scopolamin (30 mg/kg BW) Male ICR mouse $(30{\pm}2g\;BW)$ were fed basal diet (control group), and experimental diets (AP-5 and AP-10 groups) added $5\%\;and\;10\%$ of dried acorn powder to basal diet for 8 months. Acetylcholine content significantly increase in AP-5 and AP-10 groups ($4.2\%\;and\;11.3\%$, respectively) compared with control group. Acetylcholinesterase activities were significantly inhibited ($13.5\%\;and\;17.6\%$, respectively) in brain of AP-5 and AP-10 groups. Monoamine oxidase-B (MAO-B) activities were significantly inhibited ($10.0\%\;and\;12.7\%$, respectively) in brain of AP-S and AP-10 groups. These results suggest that acorn (Q. acutissima CARR.) may play an effective role in an attenuating various age-related changes such as dementia including learning and memory impairments in brain.