• Journal of Microbiology and Biotechnology
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• 제28권1호
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• pp.40-49
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• 2018

We evaluated the antioxidant activity and neuronal cell-protective effect of fucoidan extract from Ecklonia cava (FEC) on hydrogen peroxide ($H_2O_2$)-induced cytotoxicity in PC-12 and MC-IXC cells to assess its protective effect against oxidative stress. Antioxidant activities were examined using the ABTS radical scavenging activity and malondialdehyde-inhibitory effect, and the results showed that FEC had significant antioxidant activity. Intracellular ROS contents and neuronal cell viability were investigated using the DCF-DA assay and MTT reduction assay. FEC also showed remarkable neuronal cell-protective effect compared with vitamin C as a positive control for both $H_2O_2$-treated PC-12 and MC-IXC cells. Based on the neuronal cell-protective effects, mitochondrial function was analyzed in PC-12 cells, and FEC significantly restored mitochondrial damage by increasing the mitochondrial membrane potential (${\Delta}{\Psi}m$) and ATP levels and regulating mitochondrial-mediated proteins (p-AMPK and BAX). Finally, the inhibitory effects against acetylcholinesterase (AChE), which is a critical hydrolyzing enzyme of the neurotransmitter acetylcholine in the cholinergic system, were investigated ($IC_{50}$ value = 1.3 mg/ml) and showed a mixed (competitive and noncompetitive) pattern of inhibition. Our findings suggest that FEC may be used as a potential material for alleviating oxidative stress-induced neuronal damage by regulating mitochondrial function and AChE inhibition.

• 한국식품저장유통학회지
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• 제14권2호
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• pp.213-219
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• 2007

퇴행성 뇌질환의 하나인 알츠하이머는 가벼운 기억력의 장애에서부터 전반적인 인지기능의 장애를 나타내는 질환으로 해마 (hippocampus)를 포함한 신경세포에서 세포사와 관련이 있는 것으로 보고 되어왔다. AP의 자체 독성과 산화 스트레스, $A{\beta}$ plaque에서 나오는 free radical은 세포내 $Ca^{2+}$를 높이고 이로 인해 calpain이 활성화되어 신경 세포사가 촉진되며 microtubule과 같은 cytoskeleton을 파괴시킨다. 이러한 ROS와 $A{\beta}$에 의해 유도되는 세포사멸을 보호하는 물질을 해바라기 씨 추출물을 이용하여 실험을 실시하였다. 우선 추출물이 항산화 효과 (DPPH, FRAP assay), acetylcholinesterase(AChE)의 활성 및 SH-SY5Y cell의 세포사멸에 미치는 영향을 검토하였다. 항산화 활성과 AChE에 대한 억제활성은 해바라기 씨 추출물 처리농도가 높을수록 유의적으로 높게 나타났다. $H_2O_2$와 $A{\beta}$에 의해 유도된 SH-SY5Y에 대한 세포사멸 억제효과 실험(MTT assay)에서 해바라기 씨 추출물이 모두 높은 활성을 나타내었으므로 이의 성분분리는 뇌세포 보호를 위한 좋은 식품재료가 될 수 있다.

• 생명과학회지
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• 제34권9호
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• pp.656-665
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• 2024

효소 억제제는 인체 내 다양한 대사과정을 조절하는 단백질에 속하는 효소의 작용을 억제하여 특정 질병이나 상태를 치료하는 데 도움을 준다. 퀘르세틴은 폴리페놀 계열에 속하는 플라보노이드의 일종으로 식물에서 발견되는 이차 대사산물이다. 이러한 퀘르세틴은 구조적 이점을 바탕으로 효소의 활성부위에 결합하여 α-glucosidase, acetylcholinesterase, bacterial neuraminidase, xanthine oxidase에 대한 억제 활성을 갖는 것으로 보고된다. 또한, 퀘르세틴은 glycosylation, methoxylation, alkylation 등을 통해 특징적인 치환기를 가질 수 있으며 이러한 천연 퀘르세틴 유도체는 효소 활성 부위의 촉매 잔기와 특이적인 결합 패턴을 나타내어 더욱 우수한 효소저해활성을 가질 수 있다. 따라서, 본 논문에서는 퀘르세틴 및 그 유도체의 특징적인 구조에 대해 알아보고 이들의 효소저해활성을 통해 유도체별 다양한 질병을 목표로 하는 효과적인 효소 저해제 개발에 유망한 후보가 될 수 있음을 시사한다.

• Fisheries and Aquatic Sciences
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• 제25권2호
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• pp.49-63
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• 2022

Anti-cholinesterase (ChE)s are commonly prescribed as the symptomatic treatment of Alzheimer's disease. They are applied to prevent the breakdown of neurotransmitter acetylcholine (ACh) that bind to muscarinic and nicotinic receptors in the synaptic cleft. Seaweeds are one of the richest sources of bioactive compounds for both nutraceuticals and pharmacognosy applications. This study aimed to determine the anti-ChEs activity of Gracilaria manilaensis, one of the red seaweeds notables for its economic importance as food and raw materials for agar production. Methanol extracts (GMM) of G. manilaensis were prepared through maceration, and further purified with column chromatography into a semi-pure fraction. Ellman assay was carried out to determine the anti-acetylcholinesterase (AChE) and anti-butyrylcholinesterase (BuChE) activities of extracts and fractions. Lineweaver-Burk plot analysis was carried out to determine the inhibition kinetic of potent extract and fraction. Major compound(s) from the most potent fraction was determined by liquid chromatography-mass spectrometry (LCMS). GMM and fraction G (GMMG) showed significant inhibitory activity AChE with EC₅₀ of 2.6 mg/mL and 2.3 mg/mL respectively. GMM and GMMG exhibit mixed-inhibition and uncompetitive inhibition respectively against AChE. GMMG possesses neuroprotective compounds such as cynerine A, graveolinine, militarinone A, eplerenone and curumenol. These findings showed a promising insight of G. manilaensis to be served as a nutraceutical for neuronal health care in the future.

• 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.

• 한국수산과학회지
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• 제47권3호
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• pp.195-203
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• 2014

We investigated the effect low salt (2 or 4% salt) concentrations jeotgal made from Todarodes pacificus on the learning and memory impairments in scopolamine-induced (2 mg/kg, i.p.) dementia rats. Rats treated with oral BF-7 (200 mg/kg, p.o.) as a positive control and Todarodes pacificus jeotgal had significantly reduced scopolamine-induced memory deficits in the passive avoidance test. The Morris water maze test or treatment with 2% salt jeotgal made from Todarodes pacificus significantly ameliorated the scopolamine-induced memory deficits in the formation of long- and short-term memory. The acetylcholine content and acetylcholinesterase acitivity paralleled the results of the behavior experiment. There were no significant differences in the brain acetylcholine contents of the experimental groups, while the brain acetylcholine content of the group treated with 2% salt Todarodes pacificus jeotgal was higher than that of the control group. The inhibitory effect of 2% salt jeotgal made from Todarodes pacificus on the acetylcholinesterase activity in the brain was lower than that of the control group. These trends were similar to those of the gamma-aminobutyric acid content. We suggest that Todarodes pacificus jeotgal enhances learning memory and cognitive function by regulating cholinergic enzymes.

• 대한본초학회지
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• 제36권2호
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• pp.1-9
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• 2021

Objectives : Gossypium arboreum (cotton) is traditionally used to treat various health disorders. However, anti-amnesic effect of G. arboreum has not been reported. The objective of this study was to investigate in-vivo the anti-amnesic effects along with in vitro antioxidant and acetylcholinesterase (AChE) inhibition potential in G. arboreum seed essential oil. Methods : The essential oil of G. arboreum obtained by solid phase microextraction (SPME) techniques were identified by gas chromatography-mass spectroscopy (GC-MS). 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay were performed to determine the antioxidant activity at various concentrations (312.5, 625, 1250, 2500, 5000, 10000 ㎍/㎖. Y-maze, passive avoidance and Morris water maze tests were carried out to evaluate improved effect on scopolamine (1 mg/kg)-induced memory dysfunction at the dose level of 50, 100 and 200 mg/kg. Donepezil (5 mg/kg) was used as a positive drug control. We performed acetylcholinesterase (AChE) activity assay in ex vivo. Results : Five volatile compounds were identified in G. arboreum. The assays of DPPH and ABTS revealed that G. arboreum increased antioxidant activity in a dose-dependent manner. G. arboreum ameliorated the percent of spontaneous alternation in the Y-maze test, shortened step-through latency in the passive avoidance test, and increased swimming time in the target zone in the Morris water maze test. In addition, G. arboreum inhibited the AChE activity. Conclusions : Based on these findings, G. arboreum may aid in the prevention and treatment of learning and memory-deficit disorders through antioxidant and AChE inhibitory activities.

• KSBB Journal
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• 제22권1호
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• pp.30-36
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• 2007

H. erinaceum은 현재 산업적으로 매우 주목되고 있는 기능성 소재들 중의 하나이다. 본 연구에서는 식용은 물론 각종 약리효과를 나타내는 H. erinaeum의 기능성 식품의 제품화 연구 일환으로, 지금까지 체계적으로 연구된 바 없는 H. erinaceum의 액체배양을 시도하고, 이 버섯의 액체배양 생성물의 acetylcholinestrase (AChE) 저해활성과 항산활성의 효과를 자실체와 비교하면서 평가, 규명하고자 하였다. Electrophorous electricus 유래 AChE에 대한 저해 활성을 조사한 결과, 자실체 및 배양 생성물 (균사체와 배양여액)은 10 mg/ml 농도에서 75$\sim$85%의 저해활성을 보였고, 저해기작은 모두 일반적 비경쟁적 저해 (general non-competitive inhibition)에 의하였다. 특히, 배양여액의 ethanol 침전 상징액은 10 mg/ml의 농도에서 약 94%의 매우 높은 저해활성을 보였다. 한편, linoleic acid를 기질로 한 지질과산화에 대한 노루궁뎅이 버섯 유래 시료들 (자실체와 균사체 추출물, 균사체 추출물의 ethanol 침전물 및 배양여액)의 억제능을 Rhodan-Fe (FTC)법으로 조사한 결과, 균사체와 자실체 추출물은 0.1 mg/ml의 농도에서 지질의 초기 과산화를 완전히 억제하였다. 또 TBA-RS로 조사한 경우도 항산화 표준품으로 사용한 tocopherol, vitamin C 및 rutin보다 우수하였고, 시료들 간의 큰 차이 없이 약 95%의 매우 우수한 지질과산화 억제율을 나타내었다.

• 한국식품영양과학회지
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• 제45권1호
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• pp.1-11
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• 2016

본 연구는 한국인이 일상생활에서 주로 상용하는 미나리에 대해 기억력 관련 효과와 항산화 효과, 미나리 추출물의 flavonoid 중 isorhamnetin을 분석하여 기능성식품 개발 및 이용에 기여하고자 실시하였다. Acetylcholinesterase의 활성 억제를 측정한 결과 화순미나리 추출물이 28.59%로 가장 높게 나타났으며, 나주미나리 추출물 25.11%와 유의적인 차이가 없었다. SH-SY5Y 세포사멸에 미치는 영향을 측정한 결과 DMSO와 비교하여 화순미나리 추출물 37.23%와 나주미나리 추출물 36.68%로 세포사멸이 유의적으로 감소하였다. 수동회피실험 결과 scopolamine 처리에 의해 기억력이 손상된 동물모델에서 미나리 추출물을 투여하였을 때 vehicle control보다 latency time이 높게 나타났다. DPPH 및 ABTS 라디칼 소거능 측정 결과 화순, 나주, 의령 미나리 추출물 모두 미나리 처리 그룹군 간에도 유의적 차이가 있었고(P<0.05), 화순미나리 추출물이 총 폴리페놀 함량 117 mg/g, 총 플라보노이드 함량 30 mg GAE/g으로 가장 높게 측정되었다. TBARS 측정 결과 미나리 추출물 $440{\mu}g/mL$의 농도에서 화순미나리 추출물이 50.7%의 억제력으로 가장 높았으며, 나주와 의령미나리 추출물보다 유의하게 높았다. 미나리 추출물의 플라보노이드 중 isorhamnetin을 분석한 결과 표준용액과 미나리 추출물의 머무름 시간이 14분대로 피크 유지시간이 일치하였으며, 동일한 spectrum을 나타내어 정확한 isorhamnetin의 분리를 확인하였다. 또한 LC/MS/MS를 통한 분석 결과 표준용액과 미나리 추출물에서 동일 시간대에 TIC를 확인하였고 precursor ion은 317 $[M-H]^+$ m/z, product ion은 302 $[M-H]^+$ m/z로 확인할 수 있었다. 이러한 연구 결과에 기초하여 미나리 추출물은 천연 항산화제와 기억력 개선제로써의 활용 가치를 시사한다고 사료된다. 또한 건강기능성 소재로서 식품산업 분야의 이용률 향상에 도움이 될 것으로 판단된다.

• Journal of Ginseng Research
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• 제36권1호
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• pp.93-101
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• 2012

This study evaluated the anti-cholinesterases (ChEs) and antioxidant activities of white ginseng (WG) and black ginseng (BG) roots of Panax ginseng (PG), P. quinquefolium (PQ), and P. notoginseng (PN). Ginsenosides $Rg_1$, Re, Rf, $Rb_1$, Rc, $Rb_2$, and Rd were found in white PG, whereas Rf was not found in white PQ and Rf, Rc, and $Rb_2$ were not detected in white PN. The major ginsenoside content in steamed BG including $RK_3$, $Rh_4$, and 20(S)/(R)-$Rg_3$ was equivalent to approximately 70% of the total ginsenoside content. The WG and BG inhibited acetylcholinesteras (AChE) and butyrylcholinesterase (BChE) in a dose dependent manner. The efficacy of BG roots of PG, PQ, and PN on AChE and BChE inhibition was greater than that of the respective WG roots. The total phenolic contents and 2, 2-diphenyl-1-picryl-hydrazyl (DPPH) scavenging activity were increased by heat treatment. Among the three WG and BG, white PG and steamed black PQ have significantly higher contents of phenolic compounds. The best results for the DPPH scavenging activity were obtained with the WG and BG from PG. These results demonstrate that the steamed BG roots of the three studied ginseng species have both high ChEs inhibition capacity and antioxidant activity.