• Title/Summary/Keyword: ACH

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Toxicological Test Methods and AChE Inhibition of Organophosphorus Acaricides of Twospotted Spider Mite, Tetranychus urticae (점박이응애의 독성 시험방법과 유기인계 살비제 AChE 활성저해에 관한 연구)

  • 김도익;이승찬
    • Korean journal of applied entomology
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    • v.31 no.1
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    • pp.1-6
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    • 1992
  • These studies were carried out to compare toxicological test methods of two spotted spider mite, Tetranychus urticae Koch,; and to investigate relationship between in vivo resistant level of highly acaricide-selected population, and in vitro insensitivity of the AChE in the same population to carbophenothion and ethion. The slide dip method (CV = 8.7%) was of more accuracy and suitability than that of the leaf dip method(CV=12.2%) and leaf disc method (CV= 13.6 %) in determination of the resistant levels of twospotted spider mite to acaricides. The slide dip method also had the advantages of simple treatment with different populations on a slide at the same time, standardization of post-treatement conditions and living plants exclud¬ed from the test. Even though the topical application method(CV =8.1 %) showed high accuracy, it had the demerits of the much time consuming, need of expensive equipment and difficulty of test manipulation. For a limited time, the 22nd successive carbophenothion-selected population of two-spotted spider mite showed 156- and 128-fold resistant levels to carbophenothion and ethion(both alPs), respectively. However, the 24th successive ethion-selected population revealed 64.1- and 65-fold resistant levels to ethion and carbophenothion, respectively. In the inhibition of AChE activity, the carbophenothion-selected population showed 3.3- and 2.7-fold insensitivity in AChE activity to carbophenothion and ethion, respectively. Likewise, the ethion -selected population exhibited 3- and 2.6-fold insensitivity in AChE activity to carbophenothion and ethion, respectively, as compared with that of susceptible population. As a result, a good relation was recognized between in vivo resistance to organophosphorous acaricides and in vitro insensitivity of the AChE to corresponding inhibitors.

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Screening of a Potent Antidementia Acetylcholinesterase Inhibitor-containing Fruits and Optimal Extraction Conditions (항치매성 아세틸콜린에스터라제(Acetylcholinesterase) 저해 물질 함유 과일의 선발 및 저해 물질의 추출 최적 조건)

  • Lee, Eun-Na;Song, Jung-Hwa;Lee, Jong-Soo
    • The Korean Journal of Food And Nutrition
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    • v.23 no.3
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    • pp.318-323
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    • 2010
  • 아세틸콜린에스터라아제(AChE) 저해제에 의한 아세틸콜린 분해 억제는 알츠하이머 질병의 가장 확실한 치료 방법 중의 하나로 알려져 있다. 본 연구는 최근 웰빙 건강 소재로 각광을 받고 있는 과일과 채소로부터 새로운 AChE 저해제를 개발하여 항치매 식품이나 대체 의약품 생산에 응용하기 위해 과일과 채소로부터 AChE 저해 활성이 우수한 시료를 선별하고, AChE 저해 물질의 추출조건을 최적화하였다. AChE 저해 활성은 호두의 메탄올 추출물에서 72.6% ($IC_{50}=14.2\;{\mu}g$)로 가장 높았고, 호두의 AChE 저해 물질은 80% 메탄올로 $40^{\circ}C$에서 12시간 동안 처리하였을 때 가장 많이 추출되었다.

Screening of Potent Anti-dementia Acetylcholinesterase Inhibitor-containing Edible Mushroom Pholiota adiposa and the Optimal Extraction Conditions for the Acetylcholinesterase Inhibitor

  • Kim, Do-Yeon;Bae, Sang-Min;Han, Sang-Min;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.44 no.4
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    • pp.314-317
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    • 2016
  • To develop a new anti-dementia acetylcholinesterase (AChE) inhibitor from edible mushrooms, AChE inhibitory activities were determined on water and ethanol extracts of various edible mushrooms from oriental medicine markets and agriculture markets. As a result, the 70% ethanol extract from Pholiota adiposa fruiting body had the highest AChE inhibitory activity of 30.6, and its water extract also had an AChE inhibitory activity of 23.8%. Therefore, we finally selected P. adiposa as a potent anti-dementia AChE inhibitor-containing mushroom. The AChE inhibitor of P. adiposa was maximally extracted when its fruiting body was treated with water for 3hr at $70^{\circ}C$ and 70% ethanol for 12 hr at $70^{\circ}C$, respectively.

Development of Multi-Residue Methods for Carbamate Pesticides by the Enzyme Inhibition Test (효소 저해법을 이용한 Carbamate계 농약의 다성분 잔류분석법 개발)

  • Kim, Jung-Ho
    • Journal of Environmental Science International
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    • v.17 no.12
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    • pp.1325-1330
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    • 2008
  • This study was carried out with the detection for multiresidue of the carbamate pesticide such as carbaryl and cabofuran by enzyme-inhibition method. The check time for determination of acetylcholinesterase(AChE) activity was selected at 60 sec. The AChE activity in chicken brain determined by the Ellman's method was $162{\mu}$mol/min/g protein. $I_{50}$ for AChE by carbamate pesticide with wet kit was 0.169mg/L of carbaryl and 0.089mg/L of cabofuran, respectively. The incubation time for enzyme kit with substrate kit was 30min for determination of AChE activity. Enzyme kit with substrate kit was stable at $4^{\circ}C\;and\;25^{\circ}C$ for 5 days. Limit detection concentration of carbaryl with dry kit for AChE was 0.05mg/L. The dry kit such as wet kit applied Enzyme-Inhibition(EI) method with AChE was confirmed the multi residue method to detect the carbamate pesticides.

Extraction of Acetylcholinestrase from the Housefly and Three Other Insect Species for In Vitro Anticholinesterase Screening (In Vitro Anticholinesterase 스크리닝을 위한 집파리 및 3종 곤충으로부터의 Acetylcholinesterase의 추출)

  • 이시혁;이준호;조광연
    • Korean journal of applied entomology
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    • v.30 no.1
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    • pp.18-28
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    • 1991
  • The optimal pH of the extraction buffer was 7.5 considiering AChE stability and its buffer capacity when AChE was isolated and extracted from the housefly(Musca domesitca L.)and three other insect species with 0.01 M sodium phosphate buffer. Also, the optimal pH of the reaction buffer was 7.5 considering enzyme activity and its buffer capacity when AChE activity was measured with the substrate in 0.1 M sodium phosphate buffer. The Potter Elvehjem type homogenizer with Teflon pestle was used to homgenize the tissues. When preparing a AChE suspension by centrifuging the homogenate, 700 g supernatant of adult head for the housefly, 700 g supernatnat of 5th instar nymphal whole body for the brown planthopper, lipid-eliminated 10,000 g supernatant of 5th instar larval whole body for the diamondback moth, and 700 g supernatant of 4th instar larval head for the tobacco cutworm were considered satisfactory as enzyme sources in view of mass preparation, extraction efficiency and stability of enzyme activity during evaluation. When AChE suspensions of 4 insect species were stored at $-18^{\circ}C$, more than 90% of activity was maintained up to 3 weeks. Km values of AChEs of the housefly, the brown planthopper, and the diamondback moth were 0.042, 0.037 and 0.043 mM, respectively and AChE-specific substrate inhibition was observed at high concentration. Km value of the tobacco cutworm ChE was 1.15 mM and BuChE characteristics was observed, though further study is needed. The optimal substrate concentration for the AChE inhibition tests was 0.5 mM for the housfly, the brown planthopper, and the diamondback moth and 12 mM for the tobacco cutworm.

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Molecular characterization and inhibition analysis of the acetylcholinesterase gene from the silkworm maggot, Exorista sorbillans

  • Lang, Guo-Jun;Zhang, Ming-Yan;Li, Bao-Ling;Yu, Lin-Lin;Lu, Xing-Meng;Zhang, Chuan-Xi
    • BMB Reports
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    • v.43 no.8
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    • pp.573-578
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    • 2010
  • Several organophosphorus (OP) insecticides can selectively kill the silkworm maggot, Exorista sorbillans (Es) (Diptera: Tachinidae), while not obviously affecting the host (Bombyx mori) larvae, but the mechanism is not yet clear. In this study, the cDNA encoding an acetylcholinesterase (AChE) from the field Es was isolated. One point mutation (Gly353Ala) was identified. The Es-353G AChE and Es-353A AChE were expressed in baculovirus-insect cell system, respectively. The inhibition results showed that for eserine and Chlorpyrifos, Es-353A AChE was significantly less sensitive than Es-353G AChE. Meanwhile, comparison of the I50 values of eserine, dichlorvos, Chlorpyrifos and omethoate of recombinant Es AChEs with its host (Bombyx mori) AChEs indicated that, both Es AChEs are more sensitive than B. mori AChEs. The results give an insight of the mechanism that some OP insecticides can selectively kills Es while without distinct effect on its host, B. mori.

Influence of Dietary Linolenic Acid/linoleic Acid Ratio on Brain Lipid Composition and Acetylcholinestease Activity in Different Aged Rats (Linolenic acid/linoleic acid 비율이 다른 식이가 연령이 다른 흰쥐의 뇌구조지방 조성과 Acetylcholinesterase 활성에 미치는 영향)

  • 윤군애
    • Journal of Nutrition and Health
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    • v.28 no.8
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    • pp.706-716
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    • 1995
  • This study was undertaken to investigate the influence of age and dietary linolenic acid content and the linolenic acid/linoleic acid (LAN/LA) ratio on the brain lipid composition and membrane-bound enzyme, acetylcholinesterase(AchE) activities. AchE was selected as a test case for the relationship between cell lipid composition and cell membrane function. The male rats were fed diets with 0.2, 0.4, 0.6 of LNA/LA ratio within 8% LNA(H-LNA) or 4% LNA(L-LAN) of total fatty acid content for different feeding period(1, 4, 12 month). The fats used s source were sesame oil, perilla oil, soybean oil and beef tallow. The AchE activity of brain crude synaptosomal fraction was reduced with advancing age, showing 20-30% reduction in 12M compared with 1 M, and the P/C ratio was reduced in old rats. In 1 and 4 monthed rats, AchE activites was higher in H-LAN-0.2 and L-LNA-0.2 and 0.4 group. In accordance with rising of AchE activities was higher in H-LNA-0.2 and L-LNA-0.2 and 0.4 group. In accordance with rising of AchE activities, the PC/PE ratio increasedin those groups. Paricularly in L-LNA, the PC/PE ratio increased as the AchE activites for decline of membrane fluidity with increasing cholesterol and decreasing P/C ratio when rats were old. Also, AchE activity increaed with increasing PC/PE ratio which depended on the dietary LNA/LA ratio within each LNA content. Therefore, it is concluded that the lipid composition of cell membrane influenced the AchE activiteis, which was mediated by aging and the modification of dietary LNA/LA ratio.

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Analysis of Clip-induced Ischemic Complication of Anterior Choroidal Artery Aneurysms

  • Cho, Min-Soo;Kim, Min-Su;Chang, Chul-Hoon;Kim, Sang-Woo;Kim, Seong-Ho;Choi, Byung-Yon
    • Journal of Korean Neurosurgical Society
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    • v.43 no.3
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    • pp.131-134
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    • 2008
  • Objective: The surgical approach for anterior choroidal artery (AChA) aneurysm is typically similar to those used for other supraclinoid internal carotid artery (ICA) lesions. However, the surgical clipping of this aneurysm is complicated and as a result. can result in postoperative ischemic complications. The purpose of this study was to clarify the risk of clip-induced ischemic complication in AChA aneurysm and to get the benefits for helping decision making. Methods: We retrospectively investigated 53 cases (4.0%) of AchA aneurysm treated surgically. We divided the AChA aneurysm to 3 subtype according to the origin of aneurysmal neck; A type originating from the AChA itself. J type from junction of AChA and ICA and I type from the ICA itself. We evaluated brain CT about 1 week post-operative day to confirm the low density in AChA territory. Results: Ruptured aneurysm was 26 cases and unruptured aneurysm 27 cases. The aneurysmal subtype of A, J, and I was 13, 17, and 23 cases. Of the 53 cases who performed surgical neck clipping, twelve (22.6%) had postoperative AChA distribution infarcts. Increased infarct after neck clipping had statistic significance in non-I subtype (r=0.005) Conclusion: AChA aneurysm surgery carries a significant risk of postoperative stroke. Don't always stick to clipping only, especially in non-I type of incidental small aneurysm, which has high risk of post-clip ischemic complications.

Anti-amnesic and Antioxidant Effect of Yeongkyekamjotanggayonggolmoryo Aqueous Extracts on Scopolamine-induced Memory Impairment in Mice (Scopolamine 유발 기억력손상 흰 쥐에서 영계감조탕가용골모려(笭桂甘棗湯加龍骨牡蠣)의 인지기능개선과 항산화 효과)

  • Kim, Dae-eok;Han, Da-young;Kim, Sang-ho;Chung, Dae-kyoo
    • Journal of Oriental Neuropsychiatry
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    • v.29 no.3
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    • pp.121-134
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    • 2018
  • Objectives: The purpose of this in vivo study is to observe anti-amnesic effects of Yeongkyekamjotanggayonggolmoryo (YGYM), a novel mixed herbal prescription, Ossis Mastodi and Ostreae Testa added Yeongkyekamjo-tang, on scopolamine induced amnesia in C57BL/6 mice through acetylcholine (ACh) and acetylcholinesterase (AChE) activity, Choline acetyltransferase (ChAT) mRNA expression, and antioxidant effects. Methods: Six groups, total 20 intact or 100 Sco treated mice were used in this study after one week of acclimatization period. Half the animals were used for passive avoidance task tests and hippocampus ACh content, AChE activity, and ChAT mRNA expression were measured. The other half was subjected to an underwater maze test and then the cerebral cortex antioxidant defense system was measured. Results: In the passive avoidance experiment, there was significant decrease in residence time in the bright room and in the underwater maze test, escape latency to escape from the esophagus significantly increased compared with the normal control group. At the final sacrifice, ACh content and ChAT mRNA expression decreased, AChE activity increased, and cerebral cortical MDA increased GSH content, SOD and CAT activity in Sco control mice, as compared to intact vehicle control mice. However, these Sco treatment-related memory loss through AChE activation destroyed the cerebral cortex antioxidant defense system, and was inhibited dose-dependently by 28 days consecutive oral pretreatments of YGYM extracts 500, 250, 125 mg/kg. Conclusions: In the above results, YGYM extract that oral administration of YGYM extracts alleviates the antioxidant defense system, through preservation of ACh mediated by upregulation of ChAT mRNA expression, and increase of AChE inhibition and brain antioxidant defense systems.

Lysophosphatidylcholine Attenuates Endothelium-dependent Relaxation Responses through Inhibition of ACh-induced Endothelial $[Ca^{2+}]_i$ Increase

  • Kwon, Seong-Chun;Lee, Yong-Ho;Nam, Taick-Sang;Ahn, Duck-Sun
    • The Korean Journal of Physiology and Pharmacology
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    • v.10 no.1
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    • pp.25-30
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    • 2006
  • Lysophosphatidylcholine (LPC), which accumulates in atherosclerotic arteries, has been reported to inhibit endothelium-dependent relaxation (EDR) in many different species. However, the underlying mechanism of LPC-induced inhibition of EDR is still uncertain. In the present study, we measured simultaneously both isometric tension and cytosolic free $Ca^{2+}$ ($[Ca^{2+}]_i$) in rabbit carotid strips, and examined the effect of LPC on tension and $[Ca^{2+}]_i$. In carotid strips with intact-endothelium, high $K^+$ (70 mM) increased both tension and $[Ca^{2+}]_i$, and cumulative addition of acetylcholine (ACh) from 0.1 to $10{\mu}M$ induced dose dependent increase of $[Ca^{2+}]_i$ with concomitant relaxation. In the presence of L-NAME (0.1 mM), ACh increased $[Ca^{2+}]_i$ without affecting the amplitude of high $K^+-induced$ tension. These ACh-induced change of $[Ca^{2+}]_i$ and tension was abolished by removal of endothelium or 10 nM 4-DAMP (muscarinic receptor antagonist) pretreatment. Pretreatment of LPC ($10{\mu}M$) inhibited ACh ($10{\mu}M$)-induced change of tension and $[Ca^{2+}]_i$ in endothelium-intact carotid artery. On the other hand, LPC had no effect on ACh-induced change of tension and $[Ca^{2+}]_i$ in endothelium denuded artery. In $Ca^{2+}$-free external solution, ACh transiently increased $[Ca^{2+}]_i$, and pretreatment of LPC significantly inhibited ACh-induced transient $[Ca^{2+}]_i$ change. Based on the above results, it may be concluded that LPC inhibits the ACh-induced $[Ca^{2+}]_i$ change through inhibition of $Ca^{2+}$ mobilization in vascular endothelial cells, resulting in decreased production of NO and concomitant inhibition of endotheliumdependent vascular relaxation.