• Title/Summary/Keyword: AChE활성저해

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Nutritional Characteristics and Physiological Functionality of Antidementia Acetylcholinesterase Inhibitor-containing Methanol Extract from Sorghum bicolor (항치매성 아세틸콜린에스터레이즈 저해 물질을 함유한 수수(Sorghum bicolor) 메탄올 추출물의 영양학적 특성과 생리 기능성)

  • Song, Jung-Eun;Song, Jung-Hwa;Cho, Soo-Muk;Min, Gyung-Hun;Lee, Jong-Soo
    • The Korean Journal of Food And Nutrition
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    • v.23 no.2
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    • pp.226-232
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    • 2010
  • 새로운 항치매성 건강식품을 개발하기 위해 아세틸콜린에스터레이즈(AChE)를 강력하게 저해하는 추출물을 곡류와 두류의 다양한 추출물로부터 선발한 후 최적 추출 조건을 조사하였다. 추출물 중 수수 메탄올 추출물이 63.4%의 가장 높은 AChE 저해 활성을 보였다. 수수를 80% 메탄올로 $40^{\circ}C$에서 12시간 추출했을 때 최대의 AChE 저해 활성을 나타내었다. AChE를 저해하는 수수 메탄올 추출물의 영양성과 생리 기능성을 조사하였다. 메탄올 추출물은 유리당으로 고형물 100 g당 4.78 g의 포도당과 4.13 g의 자당 및 0.97 g의 과당을 함유하였다. 또한, 수수 메탄올 추출물의 고형물 100 g에 linoleic acid 273.82 mg, oleic acid 215.65 mg, palmitic acid 122.03 mg, stearic acid 4.96 mg을 함유하고 있었고, 주요 유기산으로 주석산 27.45 mg, 말론산 15.43 mg, 사과산 9.94 mg이 메탄올 추출물 1 g에 함유되어 있었다. 수수 메탄올 추출물은 항치매 활성 외에도 콜레스테롤 합성을 저해하는 HMG-CoA reductase 저해 활성이 50.2%이었고, 항산화 활성은 56.1%를 보였다.

AChE Inhibitory Effect and Antioxidative Activity of Submerged Cultured Products from Hericium erinaceum (Hericium erinaceum 액체배양 생성물의 Acetyl-cholinesterase 저해 활성과 항산화 활성)

  • Jung, Jae-Hyun;Lee, Shin-Young
    • KSBB Journal
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    • v.22 no.1
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    • pp.30-36
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    • 2007
  • The water-soluble or ethanol-soluble materials extracted from fruit bodies and cultured products (mycelium and broth) of H. erinaceum were prepared, and their inhibitory effect on acetylcholinesterase (AChE) activity from Electrophorous electricus was investigated. Inhibition of 75-85% for AChE activity at concentration of 10 mg/ml was obtained and the mechanism was due to general non-competitive inhibition. Especially, the supernatant of culture broth by ethanol treatment, exhibited a strong inhibition activity of 94% at 10 mg/ml. The samples from fruit body, mycelium and broth (supernatant and precipitate by ethanol treatment) which were extracted from H. erinaceum, were very effective to inhibit the initial stage oxidation of a linoleic acid at concentration of 0.1 mg/ml. The antioxidative activity of these samples were superior than rutin, vitamin C and tocopherol as antioxidative standards by FTC (ferric thiocyanate) method, and also showed the very strong antioxidative activity of 95% without significant difference of the samples by TBA-RS (thiobarbituric acid-reactive substance) method.

A Comparative Study of GABA, Glutamate Contents, Acetylcholinesterase Inhibition and Antiradical Activity of the Methanolic Extracts from 10 Edible Plants (10가지 식용식물 추출물의 가바, 글루탐산 함량, 아세틸콜린에스테라제 억제 및 라디컬 소거능 비교)

  • Jung, Yeon-Seop;Park, Sung-Jin;Kim, Ji-Eun;Yang, Seun-Ah;Park, Jung-Hyun;Kim, Jung-Hyun;Jhee, Kwang-Hwan;Lee, Sam-Pin;Lee, In-Seon
    • Korean Journal of Food Science and Technology
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    • v.44 no.4
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    • pp.447-451
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    • 2012
  • In order to investigate the efficacies for cognitive function of edible plants, we measured the inhibitory effects of acetylcholinesterase(AChE) activity, radical scavenging activities, and the contents of GABA and glutamate in the plant extracts. Among the plant extracts, Schizandra chinensis contained the highest GABA 14.8 mg/g and the extracts of Cnidium officinale and Polygonum multiflorum also had a relatively high GABA. On the other hand, plant extracts except, Acorus gramineus, showed similar glutamate contents. S. chinensis, Hovenia dulcis, Thuja orientalis, and Eleutherococcus senticosus exhibited high inhibition against AChE activities at about 18-33% at 1 mg/mL. In addition, strong radical scavenging activities were also detected in those extracts which showed high AChE inhibition. Taken together, H. dulcis, T. orientalis, E. senticosus, and S. chinensis could be effective resources for enhancing cognitive function. Further, it was suggested that the AChE inhibitory activities of plant extracts might be related to antioxidative activity.

Effect of Organophosphorus Insecticides on the Inhibition of the Acetylcholinesterase Activities (유기인계(有機燐系) 살충제(殺?劑)가 Acetylcholinesterabe 활성저해(活性沮害)에 미치는 영향(影響))

  • Kim, Jung-Ho
    • Applied Biological Chemistry
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    • v.31 no.1
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    • pp.92-99
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    • 1988
  • The responses of brain acetylcholinesterase and plasma cholinesterase activities were examined in chicken given oral doses of an organophosphorus insecticides. Acute oral $LD_{50}$ of terbufos was 1.82mg/kg, and terbufos sulfone was 2.85mg/kg, terbufos sulfoxide, terbufoso xon, terbufosoxon sulfone and terbufosoxon sulfoxide were about $0.30{\sim}0.79mg/kg$, respectively. Acute oral $LD_{50}$ of phorate was 1.02mg/kg, and phorate sulfone was 1.73mg/kg, phorate sulfoxide, phoratoxon, phoratoxon sulfoxide and phoratoxon sulfone were about $0.36{\sim}0.63mg/kg$, respectively. Dosages of 50% inhibition for brain AChE and plasma ChE activities in chicken at 60 mins after oral administration of organop hosphorus insecticides were $35.3{\pm}6.8%\;and\;17.4{\pm}3.6%$ of acute oral $LD_{50}$, respectively. Activities of brain AChE and plasma ChE in chicken at 60 mins after oral administratration of acute oral $LD_{50}$ of organophosphorus insecticides were inhibited by $83.7{\pm}3.9%\;and\;93.3{\pm}2.2%$, respectively.

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Analysis of Marker Components of Fermented Opuntia ficus-indica var. saboten Stem Extracts (유산균 발효에 의한 손바닥선인장 줄기추출물의 지표물질 함량 변화 분석)

  • Shin, Dong Won;Lee, Sang Ho;Lee, Soyeon;Han, Eun Hye
    • Analytical Science and Technology
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    • v.31 no.6
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    • pp.219-224
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    • 2018
  • The fruit and stem of Opuntia ficus-indica var. aboten (OFS), a native plant of Jeju Island, are considered a safe food source. Moreover, stem extracts have been previously reported to possess a variety of biological effects (e.g. anti-inflammatory and anti-oxidant, including the ability to partially ameliorate cognitive impairment), suggesting that this plant may have utility as a functional food. The present study investigated whether fermentation by lactic acid bacteria enhances the biological effects of OFS extracts. The acetylcholinesterase (AChE) inhibitory activity of fermented or non-fermented OFS extracts was evaluated, and the content of marker components dihydrokaempferol (DHK) and quercetin-3-methyl ether (3-MeQ) was analyzed using high-performance liquid chromatography. Fermented (relative to non-fermented) OFS extracts exhibited improved AChE inhibitory activity ($IC_{50}=28.35 mg/mL$), with AChE inhibitory activity resulting from fermentation by L. plantarum ($IC_{50}=12.56mg/mL$) exceeding that resulting from fermentation by L. fermentum ($IC_{50}=17.71mg/mL$). Furthermore, fermented (relative to non-fermented) OFS extracts exhibited a 16.7 % increase in DHK content, and 3-MeQ content of OFS extracts fermented by L. plantarum and L. fermentum increased by 28.6 % and 21.4 %, respectively. Therefore, OFS stem extract AChE inhibitory activity, as well as DHK and 3-MeQ content, was enhanced by fermentation with Lactobacillus spp. This suggests that fermented OFS extracts may contribute to prevention or improvement of cognitive impairment. These data are anticipated to be useful in the development of enhanced-efficacy OFS products.

Identification and Toxic effects of Impurities present in the Technical grade of Phosalone (유기인계 살충제 Phosalone 원제 중의 불순물 동정 및 독성효과)

  • Lim, Geum-Choon;Hur, Jang-Hyun;Han, Dae-Sung
    • Korean Journal of Environmental Agriculture
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    • v.14 no.2
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    • pp.171-178
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    • 1995
  • The purpose of this study was to investigate the identification and the toxicological effects of some impurities present in the technical grade phosalone (94.4%). In instrumental analyses of the technical phosalone, the five impurities such as phosalone oxon, 6-chloro-3-methylthio-2-oxobenzoxazole, 6-chloro-2-oxobenzoxazole, O,O,S-triethyl phosphorodithioate (OOSTEPDT) and dichlorophosalone were identified. The bimolecular inhibition rate constants ($k_i$) indicated that the technical phosalone inhibited both AChE and BuChE about ten times faster than the purified phosalone did. From in vivo studies the technical phosalone showed greater inhibition for mouse brain AChE, rat blood ChE's and mouse cytosolic non-specific esterases. It was presumed that some impurities present in the technical phosalone such as phosalone oxon cause such inhibition patterns of the technical phosalone observed in this study.

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Effects of Ethanol Extracts from Zingiber officinale Rosc., Curcuma longa L., and Curcuma aromatica Salisb. on Acetylcholinesterase and Antioxidant Activities as well as GABA Contents (생강, 울금, 강황 추출물의 항산화 효과, AChE 억제활성 및 GABA 함량)

  • Jung, Yeon-Seop;Park, Sung-Jin;Park, Jung-Hyun;Jhee, Kwang-Hwan;Lee, In-Seon;Yang, Seun-Ah
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.10
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    • pp.1395-1401
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    • 2012
  • This study investigated the cognition-related effects on antioxidant activities, ${\gamma}$-aminobutyric acid (GABA) contents, and AChE inhibitory activities in ethanol extracts from Zingiber officinale Rosc. (Korea), Curcuma longa L. (Korea), Curcuma longa L. (Myanmar), and Curcuma aromatica Salisb. (India). These extracts were investigated to determine the relationships among total polyphenols as well as DPPH and ABTS radical scavenging activities, GABA contents, and acetylcholinestrase (AChE) inhibitory activity. For the results, C. longa L. from Myanmar exhibited the highest contents of curcumin (97.1 ${\mu}g/mg$), total polyphenols (98.4 ${\mu}g/mg$), and GABA (1.31 ${\mu}g/mg$), as well as the strongest radical scavenging activities and AChE inhibitory activity. In addition, C. aromatica Salisb from India, which had the highest total polyphenol content (98.4 ${\mu}g/mg$) and strongest radical scavenging activities, exhibited relatively high AChE inhibitory activity similar to that of C. longa L. from Myanmar. On the other hand, Z. officinale Rosc. and C. longa L. from Korea showed low contents of curcumin (12.2 ${\mu}g/mg$) and polyphenols (85.7 ${\mu}g/mg$), as well as low AChE inhibitory activities. However, we could detect 1.11 ${\mu}g/mg$ of GABA in these extracts, which was similar to that of C. longa L. from Myanmar. Therefore, GABA content was not correlated with AChE inhibitory activity. Based on the results, AChE inhibitory activity is highly correlated with polyphenol contents in Zingibearceae family. Overall, among the Zingiberaceae tested, C. longa L. from Myanmar might be a strong candidate as a cognitive-enhancing ingredient.

Screening of Plant Extracts with Cholinesterase Inhibition Activity (콜린 에스테라제 저해효과 보유 식물 추출물 탐색)

  • Park, Saet-Byul;Lee, Jeong-Hoon;Kim, Hyung-Don;Soe, Kyung-Hae;Jeong, Hyeon-Soo;Kim, Dong-Hwi;Lee, Seung-Eun
    • Korean Journal of Plant Resources
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    • v.31 no.5
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    • pp.433-452
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    • 2018
  • This study was conducted to select candidates from plant resources for the purpose of improving or treating Alzheimer's disease, a type of dementia. One hundred and eighty-four plant extracts at a final concentration of $100{\mu}g/ml$ were screened to determine their capacity to inhibit acetylcholinesterase (AChE) by in vitro assay. From this AChE assay, seven plant extracts - including methanol ext. and water ext. of Phellaodendron amurense Rupr. (bark), methanol ext. of Nelumbo nucifera Gaertn (stamen/ovary), methanol ext. of Persicaria tinctoria H. GROSS (flower), methanol ext. of Coptis chinensis (rhizome), ethanol ext. of Cinnamomum cassia Blume(bark) and ethanol ext. of Carthamus tinctorius L. (fruit) - showed effective inhibition activity ranging from 18.7% to 63.1%. The selected extracts were testified their inhibition activities on AChE and BuChE (butyrylcholinesterase) at concentrations of 25, 50, 100, $200{\mu}g/ml$. In the AChE assay, five extracts including methanol ext. of Nelumbo nucifera Gaertn. (stamen/ovary), methanol ext. of Persicaria tinctoria H. GROSS (flower), methanol ext. of Coptis chinensis (rhizome), methanol ext. and water ext. of Phellaodendron amurense Rupr. (bark) showed inhibition activity of 15.0%~73.5%, 19.5%~63.5%, 81.6%~58.5%, 69.9%~80.5%, and 54.8%~78.3%, respectively, at concentrations of 25, 50, 100, $200{\mu}g/ml$. In the BuChE assay, the extracts of Nelumbo nucifera Gaertn. (stamen/ovary), Persicaria tinctoria H. GROSS (flower), and Coptis chinensis (rhizome) showed inhibitory capacities of 58.9~81.6%, 45.8%~72.4%, and 33.1%~55.4% at concentrations of 25, 50, 100, $200{\mu}g/ml$, respectively. In conclusion, it is suggested that Nelumbo nucifera Gaertn. (stamen/ovary), Persicaria tinctoria H. GROSS, Coptis chinensis (rhizome) and Phellaodendron amurense Rupr. (bark) could be selected as candidate materials for improving or treating Alzheimer's disease on the basis of further study.

Physicochemical Characteristics of Antidementia Acetylcholinesterase Inhibitor-containing Methanol Extract from Sorghum bicolor and Industrial Application (항치매성 Acetylcholinesterase저해물질을 함유하고 있는 수수 메탄올 추출물의 특성 및 산업적 응용)

  • Song, Jung-Eun;Lee, Jong-Soo
    • The Journal of Natural Sciences
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    • v.19 no.1
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    • pp.45-55
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    • 2008
  • Alzheimer's disease is charaterized by the acetylcholine depletion, amyloid b-protein aggregation and neurofibrillary tangles. The prevention of the breakdown of acetylcholine by acetylcholinesterase (AChE) inhibitor has the best clinically therapeutic efficacy for Alzheimer's disease patients. To develop new antidementia alternative drugs or nutraceuticals, methanol extracts of Sorghum bicolor was screened from various extracts of cereals and legumes as a potent AChE inhibitor-containing extract in previous paper. In this paper, physicochemical properties of the methanol extracts was investigated. The methanol extracts was soluble by water, methanol and DMSO and had 215 nm and 282nm of maximum absorption spectra. It was also stable at 20-$100^{\circ}C$ and pH 2.0-10.0 for 1 hr. Test product was prepared by using methanol extracts from Sorghum bicolor and changes of its quality during storge at $20^{\circ}C$ and $40^{\circ}C$ were investigated. It was very stable for 8 weeks at $40^{\circ}C$.

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Biological Compounds Extracted from Codium fragile by Enzymatic Hydrolysis and Their Biological Activities (효소적 가수분해를 이용한 청각으로부터 생리활성 물질의 추출 및 가수분해물의 생리활성)

  • Lee, Ka-Hwa;Senevirathne, Mahinda;Ahn, Chang-Bum;Je, Jae-Young
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.39 no.7
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    • pp.953-959
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    • 2010
  • We extracted bioactive materials from Codium fragile by enzymatic hydrolysis using four different proteases (Alcalase, Flavourzyme, Neutrase, and Protamex) and seven different carbohydrases (amyloglucosidase (AMG), Celluclast, Dextrozyme, Maltogenase, Promozyme, Termamyl, and Viscozyme), and evaluated their biological activities such as antioxidant, anti-acetylcholinesterase (AChE), and anti-inflammatory effects. All enzymatic hydrolysates showed good DPPH radical scavenging capacities, in particular, Flavourzyme and Promozyme hydrolysates possessed the highest activity. The two hydrolysates also exhibited strong hydrogen peroxide scavenging activity, $Fe^{2+}$ chelating activity, and reducing power in a dose-dependent manner. Furthermore, the two hydrolysates effectively protected DNA damage induced by hydroxyl radical by measuring the conversion of supercoiled DNA to the open circular DNA. All enzymatic hydrolysates also showed high anti-AChE inhibitory activities in a dose-dependent manner, and did not showed any significant cytotoxicity on RAW264.7 cells (p<0.05). In addition, the enzymatic hydrolysates significantly (p<0.05) inhibited lipopolysaccharide induced-nitric oxide production on RAW264.7 cells. These results suggest that the enzymatic extracts from Codium fragile would be good source as an ingredient of functional foods.