• Natural Product Sciences
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• 제26권2호
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• pp.165-170
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• 2020

Carica papaya is a medicinal and fruit plant owing biological activities including antioxidant, antiviral, antibacterial and anticancer. The present study aims to investigate the acetyl (AChE) and butyryl (BChE) cholinesterase inhibitory potentials of C. papaya extracts as well as their chemical compositions. The chemical composition of the active extract was identified using a gas chromatography-mass spectrometry (GC-MS). Ellman enzyme inhibition assay showed that the alkaloid-enriched leaf extract of C. papaya possessed significant anti-BChE activity with an enzyme inhibition of 75.9%. GC-MS analysis showed that the alkaloid extract composed mainly the carpaine (64.9%) - a major papaya alkaloid, and some minor constituents such as aliphatic hydrocarbons, terpenes and phenolics. Molecular docking of carpaine revealed that this molecule formed hydrogen bond and hydrophobic interactions with choline binding site and acyl pocket. This study provides some preliminary findings on the potential use of C. papaya leaf as an herbal supplement for the prevention and treatment of Alzheimer's disease.

• 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 $2.32{\pm}0.15{\mu}M$.

• Advances in pediatric surgery
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• 제7권2호
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• pp.105-111
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• 2001

To investigate the diagnostic accuracy and applicability of barium enema(BE) and rectal suction biopsy with acetyl cholinesterase(AChE) histochemistry in the diagnosis of neonatal Hirschsprung's disease(HD), we retrospectively reviewed the findings of BE and AChE staining in 96 neonates with suspected HD during a 10-year period from January 1991 to December 2000. Sixty-nine cases of HD(58 males and 11 females) and 27 cases of non-HD are included in this study. In regard to BE, HD was based on definite transitional zone, suspicious HD on reversed rectosigmoid index(RSI <1), and non-HD on normal RSI(RSI>1). The histochemical criterion used for the diagnosis of HD was that of Chow et al(1977), i.e., the presence of many coarse discrete cholinergic nerve fibers in the muscularis mucosae and in the immediately subjacent submucosa regardless of infiltration of cholinergic nerve fibers in the lamina propria. Of 66 neonates with HD who underwent BE, transitional zone was identified in 33 cases(50 %) and reversed RSI in 19 cases(21 %), microcolon in 4 cases and normal finding in 10 cases(15 %) while of 27 neonates with non-HD, there was normal finding in 16 cases and reversed RSI in 9 cases(41 %). Thus diagnostic accuracy based on transitional zone was 64 %. The positive predictive value of reversed RSI for the diagnosis of HD was 68 %. Of 42 neonates with HD who underwent AChE histochemistry, there were 41 AChE-positive reactions and one AChE-negative reaction in a neonate with total colonic aganglionosis, while of 27 cases of non-HD, there were one equivocal AChE-positive reaction and 26 AChE-negative reactions. Thus AChE histochemical study showed a 97 % diagnostic accuracy with a 98 % sensitivity and a 96 % specificity. In conclusion, we believe that BE is valuable as a first diagnostic step since about 80 % of neonates with HD show significant radiologic findings such as a transitional zone or reversed RSI. AChE histochemical study was a more reliable diagnos tic tool showing a 97 % diagnostic accuracy, and is part.

• Asian Pacific Journal of Cancer Prevention
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• 제16권7호
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• pp.2763-2769
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• 2015

Background: Cancer is an unnatural type of tissue growth in which the cells exhibit unrestrained division, leading to a progressive increase in the number of dividing cells. It is now the second largest cause of death in the world. The present study concerned antioxidant, anticancer and anticholinesterase activities and protocatechuic, catechin, caffeic acid, syringic acid, p-coumaric acid and o-coumaric concentrations in methanol extracts of flowers, fruits and seeds of Hypericum amblysepalum. Materials and Methods: Antioxidant properties including free radical scavenging activity and reducing power, and amounts of total phenolic compounds were evaluated using different tests. Protocatechuic, catechin, caffeic acid, syringic acid, p-coumaric acid and o-coumaric concentrations in extracts were determined by HPLC. Cytotoxic effects were determined using the MTT test with human cervix cancer (HeLa) and rat kidney epithelium cell (NRK-52E) lines. Acetyl and butyrylcholinesterase inhibitory activities were measured by by Ellman method. Results: Total phenolic content of H. amblysepalum seeds was found to be higher than in fruit and flower extracts. DPPH free radical scavenging activity of the obtained extracts gave satisfactory results versus butylated hydroxyanisole and butylated hydroxytoluene as controls. Reducing power activity was linearly proportional to the studied concentration range: $10-500{\mu}g/mL\;LC_{50}$ values for H. amblysepalum seeds were 11.7 and 2.86 respectively for HeLa and NRK-52E cell lines. Butyryl-cholinesterase inhibitory activity was $76.9{\pm}0.41$ for seed extract and higher than with other extracts. Conclusions: The present results suggested that H. amblysepalum could be a potential candidate anti-cancer drug for the treatment of human cervical cancer, and good source of natural antioxidants.

• Biomolecules & Therapeutics
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• 제19권2호
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• pp.224-230
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• 2011

In order to develop silk peptide (SP) preparations possessing cognition-enhancing effect, several candidates were screened through in vitro assays, and their effectiveness was investigated in facilitated brain aging model rats. Incubation of brain acetyl-cholinesterase with SP-PN (1-1,000 ${\mu}g/ml$) led to inhibition of the enzyme activity up to 35%, in contrast to a negligible effect of SP-NN. The expression of choline acetyltransferase (ChAT) mRNA of neural stem cells expressing ChAT gene (F3.ChAT) was increased by 24-hour treatment with 10 and 100 ${\mu}g/ml$ SP-NN (1.35 and 2.20 folds) and SP-PN (2.40 and 1.34 folds). Four-week subcutaneous injections with D-galactose (150 mg/kg) increased activated hippocampal astrocytes to 1.7 folds (a marker of brain injury and aging), decreased acetylcholine concentration in cerebrospinal fluid by 45-50%, and thereby impaired learning and memory function in passive avoidance and water-maze performances. Oral treatment with SP preparations (50 or 300 mg/kg) for 5 weeks from 1 week prior to D-galactose injection exerted recovering activities on acetylcholine depletion and brain injury/aging as well as cognitive deficit induced by D-galactose. The results indicate that SP preparations restore cognitive functions of facilitated brain aging model rats by increasing the release of acetylcholine, in addition to neuroprotective activity.

• 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 $4.3{\pm}0.09{\mu}M$.

• 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.

• Journal of Nutrition and Health
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• 제21권1호
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• pp.1-11
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• 1988

어미쥐에 있어서 임신기와 수유 기간동안의 저단백 식이와 단백질 회복이 새끼쥐의 성장과 발달 즉, 세포 크기와 세포수, 뇌의 지질 함량과 신경 전달 물질에 미치는 영향을 검토하기 위하여 임신 2주째부터 정상식이(20% casein diet)와 저단백식이(11.7% casein diet)를 급여한 어미쥐에 의해 사육된 새끼쥐를 비교하였는데 그 결과는 다음과 같다. 1) 각군을 생후 21일째 희생시켰을때 체중 및 각 기관의 무게는 저단백식이군이 정상군에 비하여 유의하게 낮았으며(p<0.01), 임신기의 저단백식이군을 수유기에 정상식이를 급여하였을때 정상군 수준으로 회복되었다. 한편 체중에 대한 각 장기의 무게비를 나타내었을 때는 저단백식이군이 정상군에 비하여 높은 경향을 나타내었다. 2) 간의 DNA, RNA 함량 및 단백질 함량은 임신, 수유기의 저단백식이군이 정상군에 비하여 유의하게 낮았다(p<0.01). 한편, 임신기의 식이부족군(L-L군, L-L군)의 간의 체중에 대한 무게비가 임신기의 정상식이군(C-C군, C-L군)에 비해 증가하였으며 liver weight/DNA는 R-R군이 높았으며(p<0.01), C-C군, C-L군, L-C군은 비슷한 경향을 보였다. 3) 근육의 DNA, RNA 함량 역시 임신, 수유기의 저단백식이군이 정상군에 비하여 유의하게 낮았다(p<0.01). 한편 뇌의 체중에 대한 무게비와 brain weight/DNA는 저단백식이군이 정상군에 비하여 증가하였다. 5) 뇌의 총지질 함량은 정상 식이군보다 저단백 식이군이 낮았으며(p<0.01) 수유기 저단백식이에 의한 영향이 컸다. 한편 뇌의 콜레스테롤 함량은 임신기의 저단백식이군이 낮은 경향을 보였다(p<0.01). 한편 뇌의 acetylcholinesterase activity는 암컷의 경우에는 임신기 또는 수유기 또는 임신기와 수유기의 저단백식이에 의하여 영향을 받아 정상식이군(C-C군)에 비하여 낮았다(p<0.01). 본 실험의 결과는 어미쥐에 있어 임신, 수유기의 저단백식이는 새끼쥐의 성장 발달 즉 세포의 수, 세포크기, 단백질 함량, 뇌의 지질 함량 및 acetylcholinesterase activity에 영향을 미침을 나타낸다.