• 제목/요약/키워드: Acetylcholinesterase activity

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Chlorantraniliprole 저항성 초파리 계통 확립과 저항성 특성 구명 (Establishment of Chlorantraniliprole-Resistant Drosophila Strains and Identification of Their Resistant Characteristics)

  • 김아영;권덕호;정인홍;특안판;트란비느안;이시혁;고영호
    • 한국응용곤충학회지
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    • 제55권4호
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    • pp.413-419
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    • 2016
  • Chlorantraniliprole은 곤충 근육의 $Ca^{2+}$ 농도를 조절하는 Ryanodine 수용기(RyR)에 작용 하는 diamide계통의 작물보호제이다. 최근에 보고된 chlorantraniliprole 저항성 배추좀나방 계통은 RyR에 돌연변이를 가지고 있다. 본 연구에서는 초파리를 모델 곤충으로 저농도와 고농도의 chlorantraniliprole로 도태된 두 종류의 저항성 계통을 확보하였다. 두 종류의 저항성 계통은 접촉독성과 섭식독성 평가법을 활용하여 저항성 지수를 산출하였다. 접촉 독성 평가에서 두 종류의 저항성 계통은 대조군과 비교하여 95% 신뢰구간에서 저항성 발달에 차이가 없었지만, 섭식 독성 평가의 경우에서는 고농도 저항성 계통과 저농도 저항성 계통에서 대조군 대비 각각 2.1배와 8.1배의 통계적으로 유의한 저항성 증가가 나타났다. 작용점 유전자인 RyR 발현량 비교 결과, 두 종류의 저항성 계통에서 RyR의 발현량이 유의하게 감소하였고, 주요 약제 관련 효소인 Acetylcholinesterase와 Glutathione-S-transferase 활성은 조직 특이적으로 증가하는 것을 확인하였다. 이러한 결과들은 초파리에서 chlorantraniliprole에 대한 섭식독성 저항성의 발달에는 주요 해독 관련 효소의 과활성도 관여할 것 임을 보여주고 있다.

생마늘 추출 숙성물의 항산화 및 아세틸콜린에스터라아제 저해 효과 (Antioxidant and Acetylcholinesterase Inhibitory Effect of Aged Raw Garlic Extracts)

  • 정희록;정지희;조유나;신정혜;강민정;성낙주;허호진
    • 농업생명과학연구
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    • 제45권4호
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    • pp.113-120
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    • 2011
  • 본 연구에서는 생마늘 추출 숙성물의 용매 분획물에 대한 항산화 효과와 acetylcholinesterase (AChE) 저해 효과에 대해서 조사하였다. 생마늘 추출 숙성물의 헥산, 클로포름, 에틸아세테이트 및 물 분획물을 통한 총 페놀성 화합물의 함량은 각각 3.70, 23.63, 31.27, 2.35 mg/g으로 나타났다. 또한, 에틸아세테이트 분획물이 ABTS radical scavenging activity, ferric reducing antioxidant power 및 linoleic acid를 활용한 지질의 자동산화 저해 효과에서 가장 높다는 것을 확인하였다. 추가적으로, PC12 신경 세포에서의 에틸아세테이트 분획물의 처리가 $H_2O_2$가 유발시키는 산화적 스트레스의 수준을 감소시켰다. 결국 생마늘 추출 숙성물의 에틸아세테이트 분획물이 농도 의존적으로 AChE를 저해한다는 것을 확인하였다. 그러므로 본 연구는 생마늘 추출 숙성물의 에틸아세테이트 분획물이 PC12 신경세포에 있어서 산화적 스트레스 수준을 감소시키고, 또한 AChE 저해제로서 활용될 수 있는 가능성을 확인하였다.

생쥐에서 사간 추출물의 기억력 감퇴에 대한 개선 효과 (Belamcandae Rhizoma Extract Improves Memory Impairment in Mice)

  • 정지욱
    • 생약학회지
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    • 제52권1호
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    • pp.55-60
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    • 2021
  • Belamcandae Rhizoma (BR), the rhizome of Belamcanda chinensis (L.) DC., possesses various biological properties such as anti-inflammatory activity, antioxidant activity and antimutagenic activity. However, there have been no studies on the anti-amnesic effect of BR. In this study, we assessed the improvement effect of BR extract on scopolamine-induced amnesia in mice. ICR mice were administrated with BR (50, 100 or 200 mg/kg, p.o.) and were subsequently injected of scopolamine (1 mg/kg, i.p.) 30 min before behavioral tasks (Y-maze, passive avoidance and Morris water maze tasks). To further assess the possible mechanisms of BR, the ex vivo acetylcholinesterase (AChE) activity was also evaluated. BR could ameliorate scopolamine-induced memory impairment and could regulate the cholinergic function by inhibiting the AChE activity. These data demonstrated that BR exert candidate extract against amnesia by restoring the cholinergic activity.

Terbufos가 병아리 중(中) Acetylcholinesterase에 미치는 영향(影響) (Effect of Terbufos on the Activity of Acetylcholinesterase in the Chicken)

  • 홍종욱;김정호;김장억
    • Applied Biological Chemistry
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    • 제29권3호
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    • pp.324-330
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    • 1986
  • Terbufos가 병아리 중(中) brain Ach-E 및 plasma Ch-E 활성(活性)에 미치는 영향(影響)을 조사한 결과(結果)는 다음과 같았다. Terbufos의 병아리에 대(對)한 급성경구(急性經口) $LD_{50}$은 1.82mg/kg이었다. Brain Ach-E와 plasma Ch-E에 대(對)한 $pI_{50}$과 Ki는 Terbufos$LD_{50}$에서는 Brain Ach-E 활성(活性)이 83%, plasma Ch-E 활성(活性)이 94%가 저해(沮害)되었다.

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Effects of Takju intake and moderate exercise training on brain acetylcholinesterase activity and learning ability in rats

  • Kim, Bo-Ram;Yang, Hyun-Jung;Chang, Moon-Jeong;Kim, Sun-Hee
    • Nutrition Research and Practice
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    • 제5권4호
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    • pp.294-300
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    • 2011
  • Takju is a Korean alcoholic beverage made from rice, and is brewed with the yeast Saccharomyces cerevisiae. This study was conducted to evaluate the effects of exercise training and moderate Takju consumption on learning ability in 6-week old Sprague-Dawley male rats. The rats were treated with exercise and alcohol for 4 weeks in six separate groups as follows: non-exercised control (CC), exercised control (EC), non-exercised consuming ethanol (CA), exercised consuming ethanol (EA), non-exercised consuming Takju (CT), and exercised consuming Takju (ET). An AIN-93M diet was provided ad libitum. Exercise training was performed at a speed of 10 m/min for 15 minutes per day. Ethanol and Takju were administered daily for 6-7 hours to achieve an intake of about 10 ml after 12 hours of deprivation, and, thereafter, the animals were allowed free access to deionized water. A Y-shaped water maze was used from the third week to understand the effects of exercise and alcohol consumption on learning and memory. After sacrifice, brain acetylcholinesterase (AChE) activity was analyzed. Total caloric intake and body weight changes during the experiment were not significantly different among the groups. AChE activity was not significantly different among the groups. The number of errors for position reversal training in the maze was significantly smaller in the EA group than that in the CA and ET groups, and latency times were shorter in the EA group than those in the CC, EC, CT, and ET groups. The latency difference from the first to the fifth day was shortest in the ET group. The exercised groups showed more errors and latency than those of the non-exercised groups on the first day, but the data became equivalent from the second day. The results indicate that moderate exercise can increase memory and learning and that the combination of exercise and Takju ingestion may enhance learning ability.

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

  • 윤군애
    • Journal of Nutrition and Health
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    • 제28권8호
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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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Selective Butyrylcholinesterase Inhibitors Using Polyphenol-polyphenol Hybrid Molecules

  • Woo, Yeun-Ji;Lee, Bo-Hyun;Yeun, Go-Heum;Kim, Hyun-Ju;Won, Moo-Ho;Kim, Sang-Hern;Lee, Bong-Ho;Park, Jeong-Ho
    • Bulletin of the Korean Chemical Society
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    • 제32권8호
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    • pp.2593-2598
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    • 2011
  • Polyphenols (PPs) are known as antioxidant compounds having benign biological activities. In this paper, a series of hybrid molecules between the free or acetyl protected polyphenol compounds were synthesized and their in vitro antioxidant activity (DPPH assay) and cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were evaluated. As expected, free phenolic hybrid compounds (6 and 8) showed better antioxidant activity than acetyl protected hybrid compounds (5 and 7) from DPPH assay. But the contrast result was obtained from BuChE inhibition assay. Acetyl protected hybrid compounds (5 and 7) showed better inhibition activity for BuChE than free phenolic hybrid compounds (6 and 8). Specifically, 10 (AcFA-AcFA) were shown as an effective inhibitor of BuChE ($IC_{50}=2.3{\pm}0.3{\mu}M$) and also had a great selectivity for BuChE over AChE (more than 170 fold). Inhibition kinetic studies with acetyl protected compounds (5, 7, 9, and 10) indicated that 5, 7 and 10 are a hyperbolic mixed-type inhibition and 10 is a competitive inhibition type. The binding affinity (Ki) value of 10 to BuChE is $2.32{\pm}0.15{\mu}M$.

Krill-Derived Phosphatidylserine Improves TMT-Induced Memory Impairment in the Rat

  • Shim, Hyun-Soo;Park, Hyun-Jung;Ahn, Yong-Ho;Her, Song;Han, Jeong-Jun;Hahm, Dae-Hyun;Lee, Hye-Jung;Shim, In-Sop
    • Biomolecules & Therapeutics
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    • 제20권2호
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    • pp.207-213
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    • 2012
  • The present study examined the effects of krill-derived phosphatidylserine (Krill-PS) on the learning and memory function and the neural activity in rats with trimethyltin (TMT)-induced memory deficits. The rats were administered vehicle (medium-chain triglyceride: MCT) or Krill-PS (50, 100 mg/kg, p.o.) daily for 21 days. The cognitive improving efficacy of Krill-PS in TMT-induced amnesic rats was investigated by assessing the Morris water maze test and by performing choline acetyltransferase (ChAT), acetylcholinesterase (AChE) and cAMP responsive element binding protein (CREB) immunohistochemistry. The rats with TMT injection showed impaired learning and memory of the tasks and treatment with Krill-PS produced a significant improvement of the escape latency to find the platform in the Morris water maze at the $2^{nd}$ and $4^{th}$ day compared to that of the MCT group (p<0.05). In the retention test, the Krill-PS+MCT groups showed increased time spent around the platform compared to that of the MCT group. Consistent with the behavioral data, Krill-PS 50+MCT group significantly alleviated the loss of acetylcholinergic neurons in the hippocampus and medial septum compared to that of the MCT group. Treatment with Krill-PS significantly increased the CREB positive neurons in the hippocampal CA1 area as compared to that of the MCT group. These results suggest that Krill-PS may be useful for improving the cognitive function via regulation of cholinergic marker enzyme activity and neural activity.

Extraction and Characteristics of Anti-obesity Lipase Inhibitor from Phellinus linteus

  • Lee, Jong-Kug;Jang, Jeong-Hoon;Lee, Jong-Tae;Lee, Jong-Soo
    • Mycobiology
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    • 제38권1호
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    • pp.52-57
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    • 2010
  • To develop a potent anti-obesity lipase inhibitor from mushroom, the lipase inhibitory activities of various mushroom extracts were determined. Methanol extracts from Phellinus linteus fruiting body exhibited the highest lipase inhibitory activity (72.8%). The inhibitor was maximally extracted by treatment of a P. linteus fruiting body with 80% methanol at $40^{\circ}C$ for 24 hr. After partial purification by systematic solvent extraction, the inhibitor was stable in the range of $40\sim80^{\circ}C$ and pH 2.0~9.0. In addition to lipase inhibitory activity, the inhibitor showed 59.4% of superoxide dismutase-like activity and 56.3% of acetylcholinesterase inhibitory activity.

Cholinergic Activity Related to Cardiovascular Regulation in Rostral Ventrolateral Medulla of Spontaneously Hypertensive Rats

  • Lee, Seok-Yong;Lee, Sang-Bok
    • The Korean Journal of Physiology and Pharmacology
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    • 제3권1호
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    • pp.29-34
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    • 1999
  • The hyperactivity of cholinergic system in the RVLM of spontaneously hypertensive rats (SHR) may contribute to the sustained elevation of blood pressure. However, the hyperactivity mechanisms of cholinergic system are controversial. Thus, to clarify the mechanisms of cholinergic hyperactivity in RVLM of the SHR, we studied the activities of enzymes that participate in the biosynthesis and degradation of acetylcholine (ACh) and the density of muscarinic receptors in RVLM of the 14- to 18-week-old SHR and age-marched Wistar Kyoto rats (WKY). Choline acetyltransferase activity was far greater in RVLM of SHR than that of WKY. $[^3H]ACh$ release from RVLM was also greater in SHR than in WKY. Acetylcholinesterase activity and $[^3H]NMS$ binding of RVLM slice of SHR were not significantly different from that of WKY. These results suggest that the enhanced cholinergic mechanisms in the RVLM of SHR is due to the enhanced presynaptic cholinergic tone rather than the altered postsynaptic mechanisms.

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