• 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.

• Archives of Pharmacal Research
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• 제29권3호
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• pp.195-198
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• 2006

Slavins A (1) and B (2), the new amyrin type triterpenes, have been isolated from the chloroform soluble fraction of Salvia santolinifolia and assigned structures on the basis of spectral studies including 2D NMR. Both the compounds displayed inhibitory potential against the enzyme butyrylcholinesterase.

• 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.

• Natural Product Sciences
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• 제18권4호
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• pp.233-238
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• 2012

Nine compounds (1 - 9), ${\alpha}$-linolenic acid (1), cis-5,8,11,14,17-elcosapentaenoic acid (2), phytol (3), loliolide (4), uridine (5), thymidine (6), deoxyadenosine (7), adenine (8), and adenosine (9), were isolated from the n-hexane, methylene chloride, ethyl acetate and n-butanol fractions of Capsosiphon fulvescens. The structures of these compounds were elucidated on the basis of spectroscopic evidence. Compounds 1 - 9 exhibited acetylcholinesterase (AChE) inhibitory activities with $IC_{50}$ values ranging from 114.91 to $252.40{\mu}M$, whereas 2 - 4 showed butyrylcholinesterase (BChE) inhibitory activities with $IC_{50}$ values ranging from 251.18 to $499.16{\mu}M$.

• 생약학회지
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• 제47권2호
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• pp.192-196
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• 2016

The herb of Agastache rugosa (Lamiaceae) called Korean mint as a spice or Agastache Herba as a crude drug is known to contain highly fragrant volatile substances. This research aimed to establish the quantitative gas chromatography (GC) method on the essential oil of A. rugosa using the three standard compounds, estragole, methyleugenol, pulegone, and to find whether the essential oil has anti-Alzheimer's activity. The GC quantification method was established by determining the linearity of calibration curve ($R^2$), linear range, and both limit-of-detection (LOD) and limit-of-quantification (LOQ). The $IC_{50}$ of the essential oil on the activities of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) were determined to be $69.06{\pm}0.26$ and $76.71{\pm}0.58{\mu}g/ml$, respectively.

• 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.

• Natural Product Sciences
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• 제23권3호
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• pp.208-212
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• 2017

A new sesquiterpenoid, 11-hydroxy-valenc-1(10),3(4)-dien-2-one (3), two chemically synthesized but first isolate from nature, $3-oxocedran-8{\beta}-ol$ (1) and valenc-1(10),3(4),11(12)-trien-2-one (2) along with four known compounds, sugiol (4), (+)-nootkatone (5), 11-hydroxy-valenc-1(10)-en-2-one (6), and clovandiol (7), were isolated from the heartwood of Juniperus chinensis. All chemical structures were elucidated using extensive spectroscopic analysis including 1D and 2D NMR spectroscopy. Valenc-1(10),3(4),11(12)-trien-2-one (2) exhibited significant inhibitory activity against butyrylcholinesterase with an $IC_{50}$ value of $68.45{\mu}M$.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.377.1-377.1
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• 2002

Neuroscience and molecular biology studies show that inappropriate butyrylcholinesterase (BuChE) activity as well as acetylcholinesterase (AChE) activity increases the risk and/or progression of Alzheimer's disease. BuChE may also regarded to participate in the transformation of Abeta (${\beta}$-amyloid) from an initially benign form to an eventually malignant form associated with neuritic tissue degeneration and clinical dementia. (omitted)

• 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 $2.32{\pm}0.15{\mu}M$.

• Bulletin of the Korean Chemical Society
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• 제34권4호
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• pp.1025-1029
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• 2013

In the previous paper (Bull. Korean Chem. Soc., 2011, 32, 2997), the hybrid molecules between ${\alpha}$-lipoic acid (ALA) and polyphenols (PPs) connected with neutral 2-(2-aminoethoxy)ethanol linker (linker-1) showed new biological activity such as butyrylcholinesterase (BuChE) inhibition. In order to increase the binding affinity of the hybrid compounds to cholinesterase (ChE), the neutral 2-(2-aminoethoxy)ethanol (linker 1) was switched to the cationic 2-(piperazin-1-yl)ethanol linker (linker 2). The $IC_{50}$ values of the linker-2 hybrid molecules for BuChE inhibition were lower than those of linker-1 hybrid molecules (except 9-2) and they also had the same great selectivity for BuChE over AChE (> 800 fold) as linker-1 hybrid molecules. ALA-acetyl caffeic acid (10-2, ALA-AcCA) was shown as an effective inhibitor of BuChE ($IC_{50}=0.44{\pm}0.24{\mu}M$). A kinetic study using 7-2 showed that it is the same mixed type inhibition as 7-1. Its inhibition constant (Ki) to BuChE is $4.3{\pm}0.09{\mu}M$.