• Title/Summary/Keyword: acetylcholinesterase inhibition activity

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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.

Antioxidant, anti-inflammatory and anti-acetylcholinesterase activities of fruiting bodies of Phellinus xeranticus (기와층버섯 자실체의 메탄올 및 열수추출물의 항산화, 항염증 및 아세틸콜린에스테라제 저해 활성)

  • Nguyen, Trung Kien;Shin, Do Bin;Lee, Kyung Rim;Shin, Pyung Gyun;Cheong, Jong Chun;Yoo, Young Bok;Lee, Min Woong;Jin, Ga-Heon;Kim, Hye Young;Im, Kyung Hoan;Lee, Tae Soo
    • Journal of Mushroom
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    • v.11 no.4
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    • pp.278-286
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    • 2013
  • Phellinus xeranticus is an medicinal mushroom belongs to Family Hymenochaetaceae of Polyporales, Basidiomycota. The purpose of this study was to investigate the antioxidant, anti-inflammatory and anti-acetylcholinesterase activities of methanol and hot water extracts prepared from fruiting bodies of Phellinus xeranticus. Besides measuring of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity, a reducing power and a chelating activity on ferrous ions were also measured to evaluate the antioxidant activity of the extracts. To measure the anti-inflammatory activities of the extracts, nitric oxide(NO) production from lipopolysaccharide (LPS) stimulated RAW 264.7 macrophage cells and carrageenan-induced acute hind paw edema of rats were investigated. The results showed that the extracts have excellent DPPH scavenging and chelating activity on the ferrous ions compared with positive controls. The nitric oxide (NO) production in LPS-induced RAW 264.7 macrophage cells were decreased as the concentration of the mushroom extracts increased. Significant reduction of paw edema of rats were observed at 2~6 h after treatment of methanol and hot-water extracts with 50 mg/kg concentration to the rats which are induced acute hind paw edema by carrageenan administration. The anti-acetylcholinesterase activity of the methanol extract of the mushroom showed 83.34% inhibition on AcHE which is lower than that of positive control galanthamine. The experimental results suggested that methanol and hot-water extracts of Phellinus xeranticus fruiting bodies might be used for good sources of antioxidant, anti-inflammatory and anti-acetylcholinesterase agents.

Development of Cholinesterase Inhibitors using 1-Benzyl Piperidin-4-yl (α)-Lipoic Amide Molecules

  • Lee, Seung-Hwan;Kim, Beom-Cheol;Kim, Jae-Kwan;Lee, Hye Sook;Shon, Min Young;Park, Jeong Ho
    • Bulletin of the Korean Chemical Society
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    • v.35 no.6
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    • pp.1681-1686
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    • 2014
  • A series of hybrid molecules between (${\alpha}$)-lipoic acid (ALA) and 4-amino-1-benzyl piperidines were synthesized and their in vitro cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)) inhibitory activities were evaluated. Even though the parent compounds did not exhibit any inhibitory activity against cholinesterase (ChE) with the exception of compound 14 ($IC_{50}=255.26{\pm}4.41$ against BuChE), all hybrid molecules demonstrated BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, compound 17 was shown to be an effective inhibitor against both AChE ($IC_{50}=1.75{\pm}0.30{\mu}M$) and BuChE ($IC_{50}=5.61{\pm}1.25{\mu}M$) comparable to galantamine ($IC_{50}=1.7{\pm}0.9{\mu}M$ against AChE and $IC_{50}=9.4{\pm}2.5{\mu}M$ against BuChE). Inhibition kinetic studies using compound 17 indicated a mixed inhibition type for AChE and a noncompetitive inhibition type for BuChE. Its binding affinity ($K_i$) values to AChE and BuChE were $3.8{\pm}0.005{\mu}M$ and $7.0{\pm}0.04{\mu}M$, respectively.

Effects of white ginseng and red ginseng extract on learning performance and acetylcholinesterase activity inhibition (백삼과 홍삼추출물의 학습수행과 Acetylcholinesterase 억제에 미치는 효과)

  • Lee, Mi-Ra;Sun, Bai-Shen;Gu, Li-Juan;Wang, Chun-Yan;Mo, Eun-Kyoung;Yang, Sun-Ah;Ly, Sun-Young;Sung, Chang-Keun
    • Journal of Ginseng Research
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    • v.32 no.4
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    • pp.341-346
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    • 2008
  • In the present study, we assessed the effects of white ginseng and red ginseng extract on the learning and memory impairments induced by scopolamine. The cognition-enhancing effect of ginseng extracts was investigated using the Morris water maze and Y-maze test. Drug-induced amnesia was induced by treating animals with scopolamine (2 mg/kg, i.p.), an antagonist of muscarinic acetylcholine (ACh) receptor. Tacrine was used a positive control. Ginseng extract (200 mg/kg, p.o.), tacrine (10 mg/kg, p.o.) administration significantly reduced the escape latency during training in the Morris water maze (p<0.05). At the probe trial session, scopolamine significantly increased the escape latency on day 5 in comparison with control (p<0.01). The effect of ginseng extracts on spontaneous alternation in Y-maze was similar to that of scopolamine treated group. In addition, numbers of arm entries were similar in all experimental groups. Moreover, red ginseng extract significantly inhibited acetylcholinesterase activity in the cortex and serum (p<0.05). Brain ACh contents of ginseng extract treated groups increased more than that of scopolamine group, which did not show statistically significant. These results suggest that ginseng extract may be useful for the treatment of cognitive impairment.

Change of Ginsenoside Rg3 and Acetylcholinesterase Inhibition of Black Ginseng Manufactured by Grape Juice Soaking (포도주스 침지 제조 흑삼의 Ginsenoside Rg3 함량 변화와 Acetylcholinesterase 억제효과)

  • Lee, Mi-Ra;Yun, Beom-Sik;Sun, Bai-Shen;Liu, Lei;Zhang, Dong-Liang;Wang, Chun-Yan;Wang, Zhen;Ly, Sun-Young;Mo, Eun-Kyung;Sung, Chang-Keun
    • Journal of Ginseng Research
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    • v.33 no.4
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    • pp.349-354
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    • 2009
  • This study was conducted to develop a new method for enhancing ginsenoside $Rg_3$, which is abundant in black ginseng. The cognition-enhancing effect of black ginseng extract was investigated via the assay of acetylcholinesterase (AChE) activity. Black ginseng I was prepared through the traditional method (by steaming and drying nine times repetitions). Black ginseng II, on the other hand, was prepared by steaming the ginseng three times at $120^{\circ}C$ for 30 min after soaking it in grape juice for 24 h. The ginsenosides of white, red, and black ginseng I, and II were investigated using the HPLC method, respectively. In black ginseng II, the ginsenoside $Rg_3$ contents, which cannot be found in white ginseng, amounted to 10.91 mg/g, approximately 18 times more than that in red ginseng. In the in-vivo study, black ginseng extract (200 mg/kg, p.o.) inhibited the AChE activity after 24 h by a single administration in the brain. Thus, the new manufacturing method for black ginseng was found to more effective in the conversion of ginsenoside $Rg_3$ compared to the traditional method. Black ginseng may also have the effect of preventing the cognitive impairment induced by cholinergic dysfunction.

Antioxidant and Acetylcholinesterase Inhibitory Effect of Aged Raw Garlic Extracts (생마늘 추출 숙성물의 항산화 및 아세틸콜린에스터라아제 저해 효과)

  • Jeong, Hee-Rok;Jeong, Ji-Hee;Jo, Yu-Na;Shin, Jung-Hye;Kang, Min-Jung;Sung, Nak-Ju;Heo, Ho-Jin
    • Journal of agriculture & life science
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    • v.45 no.4
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    • pp.113-120
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    • 2011
  • In vitro antioxidant activities and acetylcholinesterase (AChE) inhibitory effects of solvent fractions from aged raw garlic extracts were investigated. Total phenolics fractioned by hexane, chloroform, ethyl acetate and water from Aged raw garlic extracts were 3.70, 23.63, 31.27 and 2.35 mg/g, respectively. We found that ethyl acetate fractions had the highest in ABTS radical scavenging activities, ferric reducing antioxidant power and inhibitory effect on auto-oxidation of linoleic acid. Intracellular ROS accumulation resulting from $H_2O_2$ treatment of PC12 cells was significantly reduced when ethyl acetate fractions were present in the medium compared to PC12 cells treated with $H_2O_2$ only. In addition, we found that ethyl acetate fractions from aged raw garlic extracts resulted in a dose-dependent manner on AChE inhibition. Consequently, our results suggest that ethyl acetate fractions from aged raw garlic extracts may be useful as decreasing agents of oxidative stress and AChE inhibitors.

Antioxidants and Acetyl-cholinesterase Inhibitory Activity of Solvent Fractions Extracts from Dendropanax morbiferus (황칠나무의 용매 분획별 추출물의 항산화 활성 및 Acetyl-cholinesterase 저해 활성비교)

  • Yu, Ji Min;Moon, Hyung In
    • Korean Journal of Plant Resources
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    • v.31 no.1
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    • pp.10-15
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    • 2018
  • The leaves and stems of Dendropanax morbiferus were separated from organic solvents with methanol. The organic solvent fractions were fractionated with dichloromethane, ethyl acetate and butanol according to the systematic fractionation method. Oxidation in the body induces aging, and antioxidant activity has attracted the attention of many people as a preventive component to suppress negative reactions in the body. To investigate the antioxidant activity of Dendropanax morbiferus were subjected to DPPH free radical assay. In addition, acetyl cholinesterase inhibitions were performed for Alzheimer's disease as an aging neurological disease. As a result, it was confirmed that the antioxidant effect of DPPH was generally good in the antioxidant test. The ethyl acetate fractions of Dendropanax morbiferus stems and leaves were $IC_{50}=30{\mu}g/m{\ell}$. Acetyl cholinesterase inhibition experiments were carried out at a concentration of $250{\mu}g/m{\ell}$. Dendropanax morbiferus stems fractions showed dichloromethane fraction of 57.68%, which significantly inhibited the activity of acetyl cholinesterase.

Screening of the Biologoical Activity from Water Extracts of the Medicinal Plants and the Protective Effect of R. palmatum on MTPT-induced Neurotoxicity (한약재 물 추출물의 생리활성 검색 및 MPTP-유도 신경독성에 대한 대황의 보호효과)

  • Kim Tae Eun;Yoon Yeo Min;Park Yong In;Kim Youn Seok;Jeon Byung Hun;Kim Myung Dong
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.18 no.6
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    • pp.1666-1685
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    • 2004
  • This present study was designed to screen medicinal plants for the treatment of brain diseases such as Parkinson's disease or aging. We tested the effects of the water extracts from 38 species medicinal plants on antioxidant capacity, monoamine oxidase B (MAO-B) inhibitory activity, acetylcholinesterase (AChE) inhibition and antiperoxidation activity in vitro. The water extracts from 38 species were tested on their antioxidant activity using radical scavenging effects against ABTS+. The water extract of C. sappan was showed the highest antioxidant capacity, the antioxidant activity at 1 Jig of herbal extract being 0.38mM TE. Lipid peroxidation in brain homogenates induced by NADPH and ADP-Fe/sup 2+/ was strong inhibited by C. sappan and R. palmatum extracts. Among the 38 medicinal plants investigated, R. palmatum showed significant biological activity (antioxidant capacity, MAO-B inhibiory activity, and AChE inhibitory activity). The protective efficacy of R. palmatum water extract on 1-methyl-4­phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced parkinsonism and its possible mechanism were studied in C57BL/6 mice. Treatment of R. palmatum water extract protected biomacromolecules such as lipids from oxidative damage induced by MPTP. The content of MDA in brain tissue was decreased significantly by R. palmatum extract. These results suggest that R. palmatum water extract plays on effective role in attenuating MPTP-induced neurotoxicity in mice. This protective effect of R. palmatum might be estimated the result from the inhibitory activity on monoamine oxidase B and the enhancement of antioxidant activity.

Effect of Leonurus japonicus Houtt. on Scopolamine-induced Memory Impairment in Mice (Scopolamine 유발 기억 손상 마우스에서 익모초의 효과)

  • Lee, Jihye;Kim, Hye-Jeong;Jang, Gwi Yeong;Seo, Kyung Hye;Kim, Mi Ryeo;Choi, Yun Hee;Jung, Ji Wook
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.34 no.2
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    • pp.81-87
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    • 2020
  • Cognitive impairment is symptoms of dementia, a degenerative brain disease that is drawing attention in a rapidly aging society. This study was conducted to investigate the improvement of cognitive function of Leonurus japonicus on scopolamine-induced memory impairment in mice and the effect and mechanism of memory recovery. In vivo studies were conducted on mice orally pretreated with L. japonicus in doses of 50, 100 and 200 mg/kg (p.o.) and scopolamine (1 mg/kg, i.p.) were injected 30 min before the behavioral task. Antioxidant activity was assessed by 2,2-diphenyl-1-picryl hydrazyl (DPPH) assay and 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay, and acetylcholinesterase (AChE) inhibition activity evaluated by Ellman's method. In behavior studies showed that L. japonicus has an improved the memory of scopolamine-treated mice in Y-maze, passive avoidance and Morris water maze test. In addition, L. japonicus was also exerted free radical scavenging activity and inhibited acetyl cholinesterase activity. These results suggest that L. japonicus improves short-term and long-term memory in scopolamine-induced memory decline model and prevents scopolamine-induced memory impairments through in reduced oxidative stress and acetyl cholinesterase inhibition effect. Thus, L. japonicus is related to functional medicinal materials for prevention and treatment of human dementia patients.

Comparative Study of White and Steamed Black Panax ginseng, P. quinquefolium, and P. notoginseng on Cholinesterase Inhibitory and Antioxidative Activity

  • Lee, Mi-Ra;Yun, Beom-Sik;Sung, Chang-Keun
    • Journal of Ginseng Research
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    • v.36 no.1
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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.