• Title/Summary/Keyword: ACh

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Changes in Esterase Activity and Acetylcholinesterase Sensitivity of Insecticide-selected Strains of the Brown Planthopper(Nilaparvata lugens Stal) (저항성 벼멸구의 효소활성 변화에 관한 연구)

  • 박형만;최승윤
    • Korean journal of applied entomology
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    • v.30 no.2
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    • pp.117-123
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    • 1991
  • Acetylcholinesterase(AChE) and esterase activities as mechanisms of resistance to fenobucarb, carbofuran and diazinon in the insecticide-selected brown planthopper strains were investigated. Although there was no significant difference in AChE activity from suscept tible and resistant strains, AChE insensitivity was highly increased in the carbam없e insecticide-selected strains. On the other hand, esterase activity was moderately increa잃d in all the s selected strains. It is concluded that the cross-resistance and the level of resistance in the b brown planthopper can be explained by the combination of altered AChE and high esterase a activity, although a possible involvement of other factor(s) can not be excluded.

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Incidental Finding of Abnormal Cervical Pathology in Hysterectomy Specimens after Normal Preoperative Papanicolaou Smears in Thammasat University Hospital

  • Chundarat, Pong-Anan;Suwannarurk, Komsun;Bhamarapravatana, Kornkarn;Pattaraarchachai, Junya;Thaweekul, Yuthadej;Mairaing, Karicha;Poomtavorn, Yenrudee
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.14
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    • pp.5811-5814
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    • 2014
  • Background: To investigate abnormal cervical histopathology (ACH) from hysterectomy specimens with normal preoperative Papanicolaou (Pap) smears. Materials and Methods: Medical records from May 2009 to April 2012 were retrospectively reviewed of subjects from whom hysterectomy specimens were taken in Thammasat University Hospital. All had normal preoperative Pap smears. ACH was the primary outcome. A p-value less than 0.05 was considered significant. A total of 483 subjects with an average age of 50.5 years were recruited. Benign cases of enlarged uterus and pelvic mass were present in 94% (430/483). Endometrial and ovarian cancer were found at 6.2 and 4.7%, respectively. In hysterectomy specimens there were 19 (4%) cases of ACH. Silent ACH with benign disease, endometrial and ovarian cancers were 1.2% (5/430), 33.3% (10/30) and 17.4% (4/23), respectively. The negative predictive value (NPV) and false negative rate of Pap smears were 96 and 4%, respectively. ACH in malignant cases were 27.9% (12/43) and 20% (2/10) in adequate (APS) and inadequate (IPS) Pap collection groups, respectively. ACH in benign condition were 0.68% (2/292) and 2.2% (3/138) in APS and IPS, respectively. ACH was more often found in hysterectomy specimens with indication of malignancy than benign conditions with statistical significance. One third of preoperative stage I endometrial cancer cases had cervical involvement. Conclusions: Silent ACH in normal preoperative Pap smear was 4 %. Inadequate Pap smear collection is still the major problem in this study. Reducing inadequate Pap smear collection could reduce the false negative rate.

Inducibility of human atrial fibrillation in an in silico model reflecting local acetylcholine distribution and concentration

  • Hwang, Minki;Lee, Hyun-Seung;Pak, Hui-Nam;Shim, Eun Bo
    • The Korean Journal of Physiology and Pharmacology
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    • v.20 no.1
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    • pp.111-117
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    • 2016
  • Vagal nerve activity has been known to play a crucial role in the induction and maintenance of atrial fibrillation (AF). However, it is unclear how the distribution and concentration of local acetylcholine (ACh) promotes AF. In this study, we investigated the effect of the spatial distribution and concentration of ACh on fibrillation patterns in an in silico human atrial model. A human atrial action potential model with an ACh-dependent $K^+$ current ($I_{KAch}$) was used to examine the effect of vagal activation. A simulation of cardiac wave dynamics was performed in a realistic 3D model of the atrium. A model of the ganglionated plexus (GP) and nerve was developed based on the "octopus hypothesis". The pattern of cardiac wave dynamics was examined by applying vagal activation to the GP areas or randomly. AF inducibility in the octopus hypothesis-based GP and nerve model was tested. The effect of the ACh concentration level was also examined. In the single cell simulation, an increase in the ACh concentration shortened $APD_{90}$ and increased the maximal slope of the restitution curve. In the 3D simulation, a random distribution of vagal activation promoted wavebreaks while ACh secretion limited to the GP areas did not induce a noticeable change in wave dynamics. The octopus hypothesis-based model of the GP and nerve exhibited AF inducibility at higher ACh concentrations. In conclusion, a 3D in silico model of the GP and parasympathetic nerve based on the octopus model exhibited higher AF inducibility with higher ACh concentrations.

Identification of the Component with Anti-acetylcholinesterase Activity from the Essential Oil of Artemisia iwayomogi (더위지기 정유로부터 아세틸콜린에스테라제 억제활성 성분의 동정)

  • Choi, Jae Sue;Song, Byong-Min;Park, Hee-Juhn
    • Korean Journal of Plant Resources
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    • v.30 no.1
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    • pp.17-21
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    • 2017
  • Since the acetylcholinesterase (AChE) inhibitor is used to treat Alzheimer's disease, the present study aimed to analyze the component with anti-AChE activity from the essential oil of Artemisia iwayomogi (Compositae). The four major components of the essential oil were identified to be camphor (29.8%), borneol (28.0%), eucalyptol (5.81%) and coumarin (5.49%) from a gas chromatography-mass spectrometry (GC-MS). The essential oil and its three components, camphor, borneol, and coumarin, were subjected to anti-AChE assay. The $IC_{50}$ values of the essential oil and coumarin were shown to be $0.298mg/m{\ell}$ and $0.236mg/m{\ell}$, though those of other two components, camphor and borneol, were more than $0.250mg/m{\ell}$. These results suggest that coumarin is an active substance of this essential oil with anti-AChE activity.

Interaction of Forskolin with the Effect of $N^6-Cyclopentyladenosine$ on $[^3H]-Acetylcholine$ Release in Rat Hippocampus (흰쥐 해마에서 Acetylcholine 유리에 미치는 $N^6-Cyclopentyladenosine$ 및 Forskolin의 영향)

  • Choi, Bong-Kyu;Park, Hie-Man;Kang, Yeon-Wook;Kook, Young-Johng
    • The Korean Journal of Pharmacology
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    • v.28 no.2
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    • pp.129-136
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    • 1992
  • As it has been reported that the depolarization-induced acetylcholine (ACh) release is modulated by activation of presynaptic $A_1-adenosine$ heteroreceptor in hippocampus and various lines of evidence indicate the involvement of adenylate cyclase system in $A_1-adenosine$ post-receptor mechanism in hippocampus, it was attempted to delineate the role of adenylate cyclase system in the $A_1-receptor-mediated$ control of ACh release in this study. Slices from rat hippocampus were incubated with $[^3H]-choline$ and the release of the labelled products was evoked by electrical stimulation $(3\;Hz,\;5\;Vcm^{-1},\;2\;ms,\;rectangular\;pulses)$, and the influence of various agents on the evoked tritium-outflow was investigated. $N^6-cyclopentyladenosine$ (CPA), a specific $A_1-adenosine$ receptor agonist, in concentrations ranging from 0.1 to $10\;{\mu}M$, decreased the $[^3H]-ACh$ release in a dose-dependent manner without the changes of basal rate of release. 8-cyclopentyl-1,3-dipropylxanthine $(DPCPX,\;1{\sim}10\;{\mu}M)$, a selective $A_1-receptor$ antagonist, increased the $[^3H]-ACh$ release in a dose-related fashion with slight increase of basal tritium-release. And the CPA effects were significantly inhibited by DPCPX $(2\;{\mu}M)$ pretreatment and the dose-response curve produced by CPA was shifted to the right. The responses to N-ethylmaleimide $(NEM,\;10\;&\;30\;{\mu}M)$, a SH-alkylating agent of G-protein, were characterized by increments of the evoked ACh-release and the basal release, and the CPA effect were completely abolished by NEM pretreatment. Forskolin, a specific adenylate cyclase activator, in concentrations ranging from 0.3 to $10\;{\mu}M$, increased the evoked ACh-release in a dose-dependent manner and the CPA effects were inhibited by forskolin. These results indicate that the $A_1-adenosine$ heteroreceptor plays an important role in ACh-release via nucleotide-binding protein Gi in the rat hippocampus and that the adenylate cyclase system might be participated in this process.

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Production of the Acetylcholinesterase Inhibitor from Yarrowia lipolytica S-3

  • Lee, Dae-Hyung;Lee, Ji-Su;Yi, Sung-Hun;Lee, Jong-Soo
    • Mycobiology
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    • v.36 no.2
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    • pp.102-105
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    • 2008
  • The acetylcholinesterase (AChE) inhibitor of Yarrowia lipolytica S-3 was maximally produced when it was incubated at $30^{\circ}C$ for 36 h in an optimal medium containing 1% yeast extract, 2% peptone and 2% glucose, with an initial pH 6.0. The final AChE inhibitory activity under these conditions was an $IC_{50}$ value of 64mg/ml. After partial purification of the AChE inhibitor by means of systematic solvent extraction, the final $IC_{50}$ value of the partially purified AChE inhibitor was 0.75 mg/ml. We prepared a test product by using the partially purified AChE inhibitor and then determined its stability for the development of a new antidementia commercial product. The test product was stable at room temperature for 15 weeks.

Potency of Several Structurally Different Acetylcholinesterase Reactivators to Reactivate House Fly and Bovine Acetylcholinesterases Inhibited by Paraoxon and DFP

  • Park, No-Jung;Jung, Young-Sik;Musilek, Kamil;Jun, Daniel;Kuca, Kamil
    • Bulletin of the Korean Chemical Society
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    • v.27 no.9
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    • pp.1401-1404
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    • 2006
  • Eight structurally different acetylcholinesterase reactivators derived from currently commercially available oximes were tested for their potency to reactivate acetylcholinesterase inhibited by pesticide paraoxon (P) and DFP (D). Housefly AChE (F) and bovine red blood cell AChE (B) were used as the source of the cholinesterases. Ellman's method was taken to examine cholinesterases activity. The results show that four AChE reactivators are potent AChE reactivators, able to reach reactivation potency of more than 30% in all cases - PF, PB, DF and DB. Their reactivation potency was comparable with that of pralidoxime and even higher compared with that of HI-6, standard AChE reactivators currently available on the market.

Effects of Phenanthrene Exposure on the Acetylcholinesterase Activity of Olive Flounder (Paralichthys olivaceus)

  • Jee Jung-Hoon;Kang Ju-Chan
    • Fisheries and Aquatic Sciences
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    • v.6 no.4
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    • pp.225-227
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    • 2003
  • Acetylcholinesterase (AChE) activity is a potential biomarker for phenanthrene exposure in aquatic organisms. Olive flounder (Paralichthys olivaceus) were exposed to three different concentrations (0.5, 1.0 and 2.0, uM) of phenanthrene for four weeks. AChE activities in the brain, heart and eyes were documented. Inhibition of AChE activity was found significant in flounder treated with a concentration greater than $1.0 {\mu}M$ of phenanthrene. This indicates that a chronic exposure to phenanthrene induces damage in various organs (brain, heart and eyes) and changes of AChE activities might be a useful biomarker to assess the impacts induced by polycyclic aromatic hydrocarbon (PAH). Evidence from this study confirms that the measurement of AChE in the brain and eyes of flounder is a valuable tool that along with other biomarkers can maximize an ecotoxicologists' confidence in assessing the impacts of oil and PAH pollution in the aquatic environment.

Effects of Diethyl Phthalate on Acetylcholinesterase Activity in Olive Flounder (Paralichthys olivaceus) Following Short-term Exposure

  • Jee Jung-Hoon;Keum Yoo-Hwa;Kang Ju-Chan
    • Fisheries and Aquatic Sciences
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    • v.7 no.3
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    • pp.171-173
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    • 2004
  • Activity of acetylcholinesterase (AChE) is well known as a biomarker of exposure to organophosphate compounds in aquatic organisms. However, the effect of diethyl phthalate (DEP), a widely used plasticizer, on the chance of AChE activity is not yet known. Olive flounder (Paralichthys olivaceus) were exposed to DEP 300 and 1,000 mg DEP/kg b.w. through three times of intraperitoneal injection and effects were assessed in AChE activity of brain, muscle, heart and eyes of the exposed fish. AChE activity in various tissues of flounder was inhibited after exposure to DEP as a concentration-dependent manner, especially in brain, muscle and heart. Among tissues examined, heart is supposed to be a major part of body which is seriously damaged by DEP exposure. It indicates that DEP induces toxic effects in various organs (brain, muscle and heart), and changes of AChE activities. Such changed activities of AChE might be a useful biomarker to assess the impacts induced by phthalate esters including DEP.

Comparative Study of Korean White, Red, and Black Ginseng Extract on Cholinesterase Inhibitory Activity and Cholinergic Function

  • Lee, Mi-Ra;Yun, Beom-Sik;In, Oh-Hyun;Sung, Chang-Keun
    • Journal of Ginseng Research
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    • v.35 no.4
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    • pp.421-428
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    • 2011
  • This study evaluated cholineresterase inhibitory activity of Korean white ginseng extract (WGE), red ginseng extract (RGE), and black ginseng extract (BGE) and the cholinergic effect on scopolamine (SCOP)-induced amnesic mice. WGE, RGE, and BGE inhibited acetylcholineserase (AChE), as well as butyrylcholineserase (BuChE) in a concentration-dependent manner. BGE presented strong inhibition of AChE with an $IC_{50}$ value of 1.72 mg/mL, followed by WGE (5.89 mg/mL), RGE (6.30 mg/mL), respectively. The inhibitory activity of the three ginseng extracts on BuChE showed similar values among the groups. To better understand the mechanisms of the possible effect of ginseng extract on the cholinergic function, this study assessed the expression of the cholinergic markers of choline acetyltransferase (ChAT) and AChE using western blot and RT-PCR analysis in the brains of amnesic mice. Treatment with ginseng extracts led to inhibition of AChE expression and, the activation of ChAT expression in the hippocampus and the cerebral cortex of amnesic mice as induced by SCOP. The results suggest that ginseng extracts including BGE, appear to modulate the metabolism of acetylchoine (ACh), which would greatly increase synaptic ACh levels and most potently revert SCOP-induced amnesia.