• 한국균학회지
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• 제49권2호
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• pp.243-248
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• 2021

본 연구에서는 진균류 유래의 새로운 항치매성 BChE저해물질을 생산할 목적으로 대전광역시 하천에서 분리하여 선별한 비병원성 야생효모들의 무세포추출물들을 제조하여 이들의 BChE 저해활성 측정하였다. 비병원성 야생효모들 중 S. cerevisiae WJSL0113의 무세포추출물이 85.2%의 BChE 저해활성을 보여 최종 선발하였다. 선발 균주의 BChE 저해활성은 시판 주류용 S. cerevisiae과 식용 버섯들의 추출물보다 높은 저해활성을 보였고 선발 균주인 S. cerevisiae WJSL0113을 30℃에서 48시간 배양하였을 때 가장 높은 항치매성 BChE 저해활성을 보였다.

• Fisheries and Aquatic Sciences
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• 제2권2호
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• pp.167-171
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• 1999

This study was designed to develop biomarkers of coastal pollution using biochemical indices of flounder (Paralichthys olivaceus) by changes in lactate dehydrogenase (LDH) activity in the serum and cholinesterase activities in brain membranes. For this purpose acetylcholiesterase (AChE) activity, butyrylcholinesterase (BChE) activity, LDH/AChE ratio and LDH/BChE ratio of cultured flounders at 5 different sites on the southern coast of Korea were compared to those of wild flounders caught in the Pohang, eastern coast of Korea as a control group. Relatively high LDH activities were measured in the serum of flounders cultured on the southern coast of Korea (0.101-0.145 unit) than those in the Pohang control group (0.093 unit). AChE activities were significantly low $(about\;10-20\%)$ in brain membranes of cultured flounders compared to those in the Pohang control group. The ratios of LDH/AChE and LDH/BChE were consistently higher $(136-178\%,\; 155-214\%)$ in cultured flounders than those of Pohang control group. Thus, we propose that the ratios of LDH/AChE and LDH/BChE in flounders could be applicable for the diagnosis of marine pollution.

• Journal of Ginseng Research
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• 제34권4호
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• pp.348-354
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• 2010

Black ginseng and white ginseng were extracted with 80% ethanol and evaluated for relative ginsenoside composition, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, and antioxidant properties. As analyzed by HPLC, black ginseng contained a greater proportion of ginsenoside $Rg_3$ compared to white ginseng. White ginseng was characterized by undetectable ginsenoside $Rg_3$ but it contained more total ginsenosides than black ginseng. Black ginseng extract exhibited higher (p<0.05) free radical-scavenging activity, as well as higher antioxidant activities than white ginseng against 2,2-diphenyl-1-picryl-hydrazyl, superoxide dismutase, and xanthine oxidase, despite the fact that the total saponin content was higher in white ginseng than black ginseng. In addition, the black ginseng extract displayed greater AChE and BChE inhibitory activities. These results suggest that black ginseng has stronger effects on anti-oxidation and AChE and BChE inhibition than white ginseng.

• 생약학회지
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• 제43권2호
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• pp.122-126
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• 2012

The MeOH extract of Evodiae Fructus exhibited a significant inhibition on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), in a dose dependent manner, respectively. The extensive bioactivity-guided fractionation process with the MeOH extract finally isolated four compounds, as rutaecarpine (1), evodiamine (2), limonin (3) and dehydroevodiamine (4). Among them, compound 2 exhibited specific inhibitory activity on BChE with the $IC_{50}$ values 1.7 ${\mu}g/ml$, whereas compound 4 showed the potent inhibition upon both AChE and BChE.

• Journal of Applied Biological Chemistry
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• 제66권
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• pp.165-170
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• 2023

Isolation of the culture broth of a marine-derived Acremonium sp. CNQ-049 guided by HPLC-UV yielded compound 1 (3-phenethyl-2-phenylquinazolin-4(3H)-one), and its inhibitory activities against monoamine oxidases (MAOs), cholinesterases (ChEs), and β-secretase 1 (BACE1) were evaluated. Compound 1 was an effective selective MAO-B inhibitor with an IC₅₀ value of 9.39 µM and a selectivity index (SI) value of 4.26 versus MAO-A. In addition, compound 1 showed a potent selective butyrylcholinesterase (BChE) inhibition with an IC₅₀ value of 7.99 µM and an SI value of 5.01 versus acetylcholinesterase (AChE). However, compound 1 showed weak inhibitions against MAO-A, AChE, and BACE1. The Ki value of compound 1 for MAO-B was 5.22±1.73 µM with competitive inhibition, and the Ki value of compound 1 for BChE was 3.00±1.81 µM with mixed-type inhibition. Inhibitions of MAO-B and BChE by compound 1 were recovered by dialysis experiments. These results suggest that compound 1 is a dual-functional reversible inhibitor of MAO-B and BChE, that can be used as a treatment agent for neurological disorders.

• Natural Product Sciences
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• 제24권2호
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• pp.88-92
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• 2018

The present study was undertaken to investigate the isolated compounds from the stem bark of Garcinia atroviridis as potential cholinesterase inhibitors and the ligand-enzyme interactions of selected bioactive compounds in silico. The in vitro cholinesterase results showed that quercetin (3) was the most active AChE inhibitor ($12.65{\pm}1.57{\mu}g/ml$) while garcinexanthone G (6) was the most active BChE inhibitor ($18.86{\pm}2.41{\mu}g/ml$). It is noteworthy to note that compound 6 was a selective inhibitor with the selectivity index of 11.82. Molecular insight from docking interaction further substantiate that orientation of compound 6 in the catalytic site which enhanced its binding affinity as compared to other xanthones. The nature of protein-ligand interactions of compound 6 is mainly hydrogen bonding, and the hydroxyl group of compound 6 at C-10 is vital in BChE inhibition activity. Therefore, compound 6 is a notable lead for further drug design and development of BChE selective inhibitor.

• Natural Product Sciences
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• 제28권3호
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• pp.138-142
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• 2022

Alzheimer's disease (AD) is the most common age-related neurodegenerative disease in industrialized countries. It is estimated that about 47 million people living with dementia and the number of cases will be tripled by 2050. However, the exact mechanism of AD is not known, and full therapy has still not been found. Various tryptophan-derived alkaloids have been reported as promising agents for the treatment of AD. In the present study, a series of tryptophan-derived alkaloids were isolated and characterized from the methanol extract of Hedera rhombea fruit. Based on the analysis of their observed and reported spectroscopic data, their structures were identified as N-[4'-hydroxy-(E)-cinnamoyl]-L-tryptophan (1), N-[3',4'-dihydroxy-(E)-cinnamoyl]-L-tryptophan (2), N-[4'-hydroxy-(E)-cinnamoyl]-L-tryptophan methyl ester (3), and N-[3',4'-dihydroxy-(E)-cinnamoyl]-L-tryptophan methyl ester (4). These compounds were screened for anti-Alzheimer activity via their inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes in vitro. As a result, compounds 3 and 4 showed moderate BChE inhibition with IC₅₀ values of 86.9 and 78.4 μM, respectively, compared to those of the positive control [berberine (IC₅₀ = 11.5 μM)]. However, all four compounds did not show significant inhibition of the AChE enzyme. This is the first time, the AChE and BChE inhibitory activities of these tryptophan-derived alkaloids were investigated and reported.

• Parasites, Hosts and Diseases
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• 제51권4호
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• pp.421-426
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• 2013

Several studies have shown the mechanisms and importance of immune responses against Toxoplasma gondii infection and the notable role of cholinesterases in inflammatory reactions. However, the association between those factors has not yet been investigated. Therefore, the aim of this study was to evaluate the acetylcholinesterase (AChE) activity in blood and lymphocytes and the activity of butyrylcholinesterase (BChE) in serum of rats experimentally infected with T. gondii during the acute phase of infection. For that, an in vivo study was performed with evaluations of AChE and BChE activities on days 5 and 10 post-infection (PI). The activity of AChE in blood was increased on day 5 PI, while in lymphocytes its activity was enhanced on days 5 and 10 PI (P<0.05). No significant difference was observed between groups regarding to the activity of BChE in serum. A positive (P<0.01) correlation was observed between AChE activity and number of lymphocytes. The role of AChE as an inflammatory marker is well known in different pathologies; thus, our results lead to the hypothesis that AChE has an important role in modulation of early immune responses against T. gondii infection.

• 생명과학회지
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• 제7권1호
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• pp.17-23
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• 1997

해양오염의 진단을 위한 생화학적 오염지표 설정의 기초 연구의 일환으로, 오염이 심각한 서해(또는 황해)산 넙치(Paralchthys olvaceus)의 노 및 근육중의 아세틸콜린에스테라아제(AChE) 및 무털릴콜린에스테라아제(butyrylcho-linesterase:BChE)의 활성, 그리고 전산탈수소효소(lactate dehydrogenase:LDH)의 활성을 분석${\cdot}$평가하였다. 서해안의 양식산의 넙치의 뇌 및 근육증의 AChE의 활성은 동해안의 포항의 자연산 넙치의 노 및 근육의 AChE의 활성 대비 각각 40-50% 미 40-55% 정도나 유의적으로 저하되었을 뿐만 아니라 서해안의 자연산 넙치의 뇌 및 근욱중의 AChE의 활성 대비 각각 15-40% 및 25-35% 정도나 유의적으로 저하되었다. 또 서해안의 양식산 넙치의 뇌 및 근육중의 BChE의 활성은 동해안 포항의 자연산 넙치의 뇌 및 근육중의 BChE의 활성 대비 각각 70-75% 및 65-75% 정도나 유의적으로 저하되었ㅇ르 뿐만아니라 서해안의 자연산 넙치의 뇌 및 근육중의 BChE의 활성 대비 각각 50-75% 및 45-50% 정도나 유의적으로 저하되었다. 한편 서해안의 양식산 넙치의 혈약중의 LDH의 활성은 동해안 포항의 자연산 넙치의 혈액중의 LDH의 활성 대비 10-50%정도나 유의적으로 증가하였을 뿐만 아니라 서해안의 자연산 넙치의 혈액중의 LDH의 활성 대비 20-25% 정도나 유의적으로 증가하였다. 따라서 서해안의 양식산 넙치의 오염 뿐만 아니라 자연산 넙치의 오염 가능성도 있다는 사실을 알 수 있다.

• Natural Product Sciences
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• 제25권2호
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• pp.115-121
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• 2019

Alzheimer's disease is a chronic neurodegenerative disorder with no curative treatment. The commercially available drugs, which target acetylcholinesterase, are not satisfactory. The aim of this study was to investigate the cholinesterase inhibitory activity of Solenostemma argel aerial part. Eight compounds were isolated and identified by NMR: kaempferol-3-O-glucopyranoside (1), kaempferol (2), kaempferol-3-glucopyranosyl($1{\rightarrow}6$)rhamnopyranose (3) p-hydroxybenzoic acid (4), dehydrovomifoliol (5), 14,15-dihydroxypregn-4-ene-3,20-dione (6), 14,15-dihydroxy-pregn-4-ene-3,20-dione-$15{\beta}$-D-glucopyranoside (7) and solargin I (8). Two of them (compounds 2 and 3) could inhibit over 50 % of butyrylcholinesterase activity at $100{\mu}M$. Compound (2) displayed the highest inhibitory effect against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with a slight selectivity towards the latter. Molecular docking studies supported the in vitro results and revealed that (2) had made several hydrogen and ${\pi}-{\pi}$ stacking interactions which could explain the compound potency to inhibit AChE and BChE.