• Title/Summary/Keyword: Cholinesterase inhibitory activity

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In vitro antioxidant, anti-diabetic, anti-cholinesterase, tyrosinase and nitric oxide inhibitory potential of fruiting bodies of Coprinellus micaceus (갈색먹물버섯 자실체의 메탄올과 열수추출물의 항산화, 항당뇨, 항콜린에스테라아제, 항티로시나아제 및 Nitric oxide의 저해 효과)

  • Nguyen, Trung Kien;Lee, Min Woong;Yoon, Ki Nam;Kim, Hye Young;Jin, Ga-Heon;Choi, Jae-Hyuk;Im, Kyung Hoan;Lee, Tae Soo
    • Journal of Mushroom
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    • v.12 no.4
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    • pp.330-340
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    • 2014
  • Coprinellus micaceus, belongs to family Psathyrellaceae of Agaricales, Basidiomycota, has been used for edible purposes in the world. This study was initiated to evaluate the antioxidant, anti-diabetic, anti-cholinesterase, anti-tyrosinase, and nitric oxide inhibitory activities of fruiting bodies from C. micaceus extracted with methanol and hot water. The HPLC analysis of phenolic compounds from the mushroom extracts identified 4 phenolic compounds including procatechuic acid, chlorogenic acid, (-)-epicatechin, and naringin. In 1,1-diphenyl-2-picrylhydrazyl(DPPH) free radical scavenging assay, the scavenging activities of methanol and hot water extracts were lower than that of positive control, BHT. The chelating effects of methanol and hot water extracts were significantly higher than that of BHT, the positive control at the all concentrations tested. In the reducing power assay, methanol and hot water extracts exhibited the lower activities compared with positive control at the 0.125-0.2 mg/ml. The methanol and hot water extracts of the mushroom inhibited the ${\alpha}$-glucosidase activity by 62.26% and 67.59%, respectively at the 2.0 mg/ml, while acarbose, the positive control, inhibited the ${\alpha}$-glucosidase activity by 81.81% at the same concentration. In the acetylcholinesterase(AChE) inhibitory activity assay, methanol and hot water extracts of the mushroom inhibited the AChE by 94.64% and 74.19%, respectively at 1.0 mg/ml, whereas the galanthamine, standard drug, inhibited the AChE activity by 97.80% at the same concentration. The tyrosinase inhibitory activities of methanol and hot water extracts were 91.33% and 91.99% at 2.0 mg/ml, while the inhibitory activity of kojic acid, the positive control, was 99.61% at the same concentration. Nitric oxide(NO) production in lipopolysaccahride (LPS) activated RAW 264.7 cells were inhibited by the methanol and hot water extracts in a concentration dependent manner. Therefore, it is concluded that fruiting bodies of C. micaceus contained natural antioxidant, anti-acetylcholinesterase and ${\alpha}$-glucosidase inhibitory, anti-inflammatory, anti-tyrosinase substances which might be used for promoting human health.

Antioxidant, Anticancer and Anticholinesterase Activities of Flower, Fruit and Seed Extracts of Hypericum amblysepalum HOCHST

  • Keskin, Cumali
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.7
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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.

Toxicity of Mixtures of Diazinon, Toxaphene and/or Endrin in Mice (Diazinon, Toxaphene, Endrin과 그 혼합물의 독성효과)

  • 김종수;하대식;손성기
    • Toxicological Research
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    • v.12 no.2
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    • pp.231-236
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    • 1996
  • The toxicity of the mixture of diazinon, toxaphene(TOX) and/or endrin was studied in ICR male mice(18-22 g) by oral intubation, in corn oil, daily for up to 14 days. On day 15, the exposure was discontinued and animals were monitored for an additional period of 7 days for the possible reversibility of the toxicity. The body weight gain decreased with the mixtures, as well as with the individual pesticides, during the 14-day period. TOX and TOX containing mixtures significantly increased the liver/body weight ratio. The serum glutamic pyruvic transaminase level increased at 23~374% in diazinon, TOX, and endrin or their mixture group. The cholinesterase(ChE) activity in the serum and brain was inhibited in the animals of the group of diazinon(5, 10 mg/kg) and diazinon(5 mg/kg) containing mixtures. TOX(40, 80 mg/kg) caused initial inhibitory effects on the serum ChE Day 1. but there is little effects on the brain ChE levels. endrin(5,10 mg/kg) results in significantly elevated levels of the serum ChE, with substantial decreases in the brain ChE activity. TOX and TOX containing mixtures decreased the pentobarbital(60 mg /kg, ip., in saline) induced sleep. The effects produced by this pesticides singly, as well as by their mixtures, appeared to be reversible in nature. The toxic effects exhibited by the mixtures of diazinon(5 mf/kg), TOX(40 mg/kg), and /or endrin(5 mg/kg) were found to be the resultant of the effect showed by their components individually.

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Effect of Phorate, an Organophosphorus Insecticide on the Activity of Acetylcholinesterase (유기인계(有機燐系) 살충제 Phorate 가 Acetylcholinesterase 활성(活性)에 미치는 영향(影響))

  • Jung-Ho, Kim;Hong, Jong-Uck
    • Korean Journal of Environmental Agriculture
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    • v.6 no.2
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    • pp.77-83
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    • 1987
  • Present study was carried out to elucidate the effect of phorate (0,0-dietyl S-ethylthiomethyl phosphorodithioate), an organophosphorus insecticide on the acetylcholinesterase(AChE) and cholinesterase(ChE) activity in the chicken brain and plasma. The inhibitory effect of phorate and its metabolites on AChE and ChE activity was also increased in the order of phorate (p=S,S)$(p=S,SO_2)<phoratoxon$ (p=O,S)$(P=O,SO_2)$. Acute oral $LD_{50}$ of phorate was 1.02mg/kg. After oral administration of phorate, the activity of plasma ChE was inhibited more rapidly then that of brain AChE, whereas recovery of plasma ChE activity was more rapid than that of brain AChE activity.

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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.

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.

Inhibitory Effect of Chaenomeles sinensis Fruit on Amyloid β Protein (25-35)-Induced Neurotoxicity in Cultured Neurons and Memory Impairment in Mice (Amyloid β protein (25-35)-유도 배양신경 세포독성 및 마우스기억손상에 대한 목과의 억제효과)

  • Jung, Myung-Hwan;Song, Kyung-Sik;Seong, Yeon-Hee
    • Korean Journal of Medicinal Crop Science
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    • v.20 no.1
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    • pp.8-15
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    • 2012
  • The present study investigated an ethanol extract of Chaenomeles sinensis fruit (CSF) for possible neuroprotective effects on neurotoxicity induced by amyloid ${\beta}$ protein ($A{\beta}$) (25-35) in cultured rat cortical neurons and also for antidementia activity in mice. Exposure of cultured cortical neurons to $10{\mu}M\;A{\beta}$ (25-35) for 36 h induced neuronal apoptotic death. At $0.1-10{\mu}g/m{\ell}$, CSF inhibited neuronal death, elevation of intracellular calcium concentration ($[Ca^{2+}]_i$), and generation of reactive oxygen species (ROS) induced by $A{\beta}$ (25-35) in primary cultures of rat cortical neurons. Memory loss induced by intracerebroventricular injection of mice with 15 nmol $A{\beta}$ (25-35) was inhibited by chronic treatment with CSF (10, 25 and 50 mg/kg, p.o. for 7 days) as measured by a passive avoidance test. CSF (50 mg/kg) inhibited the increase of cholinesterase activity in $A{\beta}$ (25-35)-injected mice brain. From these results, we suggest that the antidementia effect of CSF is due to its neuroprotective effect against $A{\beta}$ (25-35)-induced neurotoxicity and that CSF may have a therapeutic role for preventing the progression of Alzheimer's disease.

Antioxidant, Anti-diabetic, Anti-cholinesterase, and Nitric Oxide Inhibitory Activities of Fruiting Bodies of Agaricus brasiliensis (신령버섯 자실체 메탄올 추출물의 항산화, 항당뇨 및 Nitric Oxide의 저해 효과)

  • Yoon, Ki Nam;Jang, Hyung Seok;Jin, Ga-Heon
    • Korean Journal of Clinical Laboratory Science
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    • v.47 no.4
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    • pp.194-202
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    • 2015
  • Agaricus brasiliensis, belonging to the family Agaricaceae of Agaricales, Basidiomycota, has been used for edible and medicinal purposes. This study was initiated to evaluate the antioxidant, anti-diabetic, and nitric oxide inhibitory activities of fruiting bodies of A. brasiliensis extracted with methanol. The HPLC analysis of phenolic compounds from the mushroom extracts identified 10 phenolic compounds including gallic acid, procatechuic acid, chlorogenic acid, (-)-epicatechin, vanillin, rutin hydrate, naringin, quercetin, formononetin, and biochanin-A. The free radical scavenging activities of methanol extract were lower than that of positive control, BHT. The chelating effects of methanol extract were significantly higher than those of the positive control, BHT at the all concentrations tested. The methanol extract exhibited the lower reducing power activities compared with the positive control at the 0.5~6.0 mg/mL concentration. The mushroom extract inhibited the ${\alpha}$-glucosidase activity by 54.48% and 78.43% at the 1.0 and 2.0 mg/mL while acarbose, the positive control, inhibited the ${\alpha}$-glucosidase activity by 51.77% and 81.81% at the same concentrations, respectively. Nitric oxide (NO) production in lipopolysaccahride (LPS) induced RAW 264.7 cells were inhibited by the methanol extracts in a concentration dependent manner. Therefore, it is concluded that fruiting bodies of A. brasiliensis contained natural antioxidant, anti-diabetic, and anti-inflammatory substances which can be useful for human health.

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.