• 생약학회지
• /
• 제47권3호
• /
• pp.287-294
• /
• 2016

Acetylcholinesterase (AChE) activation and amyloid-${\beta}$ ($A{\beta}$) aggregation are major biological markers of Alzheimer's disease. In the present study, we evaluated the inhibitory effects of 50 kinds of herbal formulas on AChE activity and $A{\beta}$ aggregation. Among them, Hwanglyeonhaedok-tang, Cheonwangbosim-dan, Makmundong-tang, and Gamisoyo-san had a potent effects on the inhbition of AChE activity. Sosiho-tang, Samsoeum, Cheonsimyeunjaeum, and Bunsimgieum exerted to have the inhibitory activity on $A{\beta}$ aggregation. In addition, these 8 herbal formulas showed the 3-ethyl-benzothiazoline-6-sulfonic acid (ABTS) radical scavenging activity, indicating their antioxidant activities.

• Food Science and Biotechnology
• /
• 제18권6호
• /
• pp.1532-1536
• /
• 2009

The objective of this study was to evaluate the antioxidant effects and acetylcholinesterase (AChE) inhibition activity of mulberry fruit extracts prepared by hot water (MFH) and 80% ethanol (MFE). Total polyphenolic contents of MFH and MFE were $195{\pm}3.4\;mg$ gallic acid equivalents/g MFH and $185{\pm}2.8\;mg$ gallic acid equivalents/g MFE. MFH and MFE significantly quenched 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydrogen peroxide dose-dependently, and showed high chelating ability and reducing power in non-cellular systems. MFH and MFE also inhibited the formation of intracellular reactive oxygen species and lipid peroxidation, and elevated intracellular glutathione (GSH) levels in RAW264.7 cells. In addition, MFH and MFE also dose-dependently suppressed AChE activity.

• Bulletin of the Korean Chemical Society
• /
• 제31권6호
• /
• pp.1609-1614
• /
• 2010

Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Standard in vitro test was chosen using a rat brain homogenate as the source of AChE. Screening of reactivation potency was performed with two concentration of reactivator (1000 ${\mu}M$ and 10 ${\mu}M$). Results were compared to established reactivators pralidoxime, methoxime, HI-6, trimedoxime and obidoxime. More than 30 novel reactivators performed equal or better reactivation ability of POX-inhibited AChE compared to currently used reactivators. The structure-activity relationship for reactivators of paraoxon-inhibited AChE was developed.

• Archives of Pharmacal Research
• /
• 제27권1호
• /
• pp.53-56
• /
• 2004

In the course of finding Korean natural products with acetylcholinesterase (AChE) inhibitory activity, we found that a methanolic extract of the twigs of Vaccinium oldhami significantly inhibited AChE. Bioassay-guided fractionation of the methanolic extract resulted in the isolation of two compounds, taraxerol (1) and scopoletin (2), as active constituents. These compounds inhibited AChE activity in a dose-dependent manner, and the $IC_{50}$/ values of compounds 1 and 2 were 33.6 (79 $\muM$) and 10.0 (52 $\muM$) $\mu$g/mL, respectively.

• Journal of Microbiology and Biotechnology
• /
• 제23권2호
• /
• pp.161-166
• /
• 2013

At present, acetylcholinesterase (AChE) inhibitors are the first group of drugs to treat mild to moderate Alzheimer's disease (AD). Although beneficial in improving cognitive and behavioral symptoms, the effectiveness of AChE inhibitors has been questioned since they do not delay or prevent neurodegeneration in AD patients. Therefore, in the present study, in order to develop new and effective anti-AD agents from lichen products, both the AChE inhibitory and the neuroprotective effects were evaluated. The AChE inhibitory assay was performed based on Ellman's reaction, and the neuroprotective effect was evaluated by using the MTT method on injured PC12 cells. One AChE inhibitor ($IC_{50}$ = 27.1 ${\mu}g/ml$) was isolated by means of bioactivity-guided isolation from the extract of lichen-forming fungus Cladonia macilenta, which showed the most potent AChE inhibitory activity in previous screening experiment. It was then identified as biruloquinone by MS, and $^1H$- and $^{13}C$-NMR analyses. The inhibitory kinetic assay suggested that biruloquinone is a mixed-II inhibitor on AChE. Meanwhile, biruloquinone improved the viability of the $H_2O_2$- and ${\beta}$-amyloid-injured PC12 cells at 1 to 25 ${\mu}g/ml$. The protective effects are proposed to be related to the potent antioxidant activities of biruloquinone. These results imply that biruloquinone has the potential to be developed as a multifunctional anti- AD agent.

• BMB Reports
• /
• 제31권3호
• /
• pp.296-302
• /
• 1998

A potentiometric flow injection biosensor for the analysis of anti-cholinesterases (anti-ChEs), based on inhibition of enzyme activity, was developed. The sensor system consists of a reactor with acetylcholinesterase (AChE) immobilized on controlled pore glass and a detector with an $H^{+}-selective$ PVC-based membrane electrode. The principle of the analysis is based on the fact that the degree of inhibition of AChE by an anti-ChE is dependent on the concentration of the anti-ChE in contact with AChE. The sensor system was optimized by changing systematically the operating parameters of the sensor to evaluate the effect of the changes on sensor response to ACh. The optimized biosensor was applied to the analysis of paraoxon, an organophosphorus pesticide. Treatment of the inhibited enzyme with pyridine-2-aldoxime fully restored the enzyme activity allowing repeated use of the sensor.

• Applied Biological Chemistry
• /
• 제29권3호
• /
• pp.324-330
• /
• 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.

• 대한임상독성학회지
• /
• 제6권1호
• /
• pp.25-31
• /
• 2008

Purpose: Acute organophosphate (OP) poisoning may be monitored by measuring the acetylcholinesterase (AChE). It is important to assess severity and establish prognostic tests in the early stage of OP poisoning. The aim of this study was to look at the relationship between various clinical aspects of the OP poisoning, prognostic indicators of OP poisoning including Simplified Acute Physiology Score (SAPS) 3, and the associated changes in AChE levels. Methods: Clinical data and initial AChE levels from thirty-seven patients with OP poisoning were prospectively reviewed from 12 teaching hospitals in South Korea from August 2005 to July 2006. Clinical manifestations at the time of arrival such as miosis, respiratory abnormality, salivation, urinary incontinence, GCS score, AVPU scale, need for intubation, and mechanical ventilation requirements were recorded. SAPS 3 was calculated using clinical data and laboratory results. Results: The median level of AChE was 9.8 (1.3-53.6) U/gHb. There was no significant difference in AChE levels between the groups with and without cholinergic symptoms. The median level of AChE of the patients who required intubation and those who did not were 3.5 U/gHb and it 19.7 U/gHb respectively (Mann-Whitney test; p<0.001). The AChE levels were also significantly different (p=0.007) in patients who needed mechanical ventilation compared to those who did not with AChE levels found to be 3.1 U/gHb and it was 14.8 U/gHb, respectively. Level of consciousness assessed using the AVPU scale was correlated with AChE levels (Kruskal-Wallis test; p=0.013). GCS score were correlated with AChE levels (p=0.007, Spearman's rho = 0.454). In addition, the lower the level of initial AChE, the longer the ICU stay (p=0.029, Spearman's rho=-0.380). SAPS 3 was inversely correlated with the initial AChE (p<0.001, Spearman's rho=-0.633). Conclusion: In the acute OP poisoning, low AChE levels appear to help indicate the severity of poisoning. The initial AChE level may be a useful prognostic parameter for acute OP poisoning.

• 한국자원식물학회지
• /
• 제32권4호
• /
• pp.270-274
• /
• 2019

국화과에 속하는 단풍취의 추출물이 가지는 알츠하이머에 대한 효과를 알기 위하여 AChE에 대한 억제효과와 peroxynitrite 소거효과를 연구하였다. 단풍취 추출물은 AChE에 대한 억제효과로서 그 $IC_{50}$가 $73.4{\mu}g/ml$이었으며 peroxynitrite 소거효과에 관한 $IC_{50}$는 $8.60{\mu}g/mL$이었으므로 알츠하이머 질환에 유익할 것으로 판단된다. 단풍취에 가장 많이 함유된 성분인 3,5-dicaffeoylquinic acid 성분의 활성도 이와 유사한 활성을 보였으므로 단풍취 추출물의 효과는 주로 이 화합물의 활성에 따른 것으로 예상된다. Caffeoylquinic acid가 알츠하이머 질환에 효과있다는 보고가 있으므로 이 식물의 잎과 줄기 추출물에서 6종의 지표물질을 이용하여 정량법을 확립한 후 정량하였다. 그 결과 잎에서는 성분 함량이 25.1%를 차지하여 줄기의 함량보다 훨씬 높았다. 특히 잎 추출물 중 3,5-dicaffeoylquinic acid의 함량이 145.6 mg/g에 달하여 알츠하이머 질환 치료에 유익할 것으로 예상된다.

• 한국식품과학회지
• /
• 제41권4호
• /
• pp.435-440
• /
• 2009

잎녹차 추출물 보다는 분말녹차 추출물의 경우가 그리고 저장된 sample보다는 fresh sample의 AChE 저해활성이 상대적으로 높았고 이는 생리활성 물질의 추출효율성과 생리활성 물질의 특성 변화 측면에서 기인되는 것으로 판단된다. 또한 본 연구팀에서 구성한 저장 조건에서, 4주간의 짧은 저장기간이 3개월 저장조건보다는 우수한 효소 저해활성도를 나타냈다. 수분활성도 측면에서는 수분활성도 0.81의 조건을 갖는 sample에서의 효과가 비교적 우수했고, 3개월 저장하는 동안의 저장온도 조건은 효소 저해 활성도에 큰 차이를 보이는 요소로 작용하지 못했다. 다만 상온이나 냉장조건 보다는 냉동상태의 저장조건이 다소 우수한 것으로 판단된다. 결국 생리활성물질을 보다 효율적으로 추출할 수 있는 녹차의 상태와 처리 또는 섭취 농도가 더욱 중요한 것으로 사료되고, 추출 효율을 증가시키기 위해서는 잎 보다는 분말의 상태가 더 우수한 것으로 판단된다. 따라서 녹차 추출물은 acetylcholine성 신경세포의 기능을 강화시켜줄 수 있는 AChE 저해제로서 활용가치가 높을 것이다.