• Korean Journal of Pharmacognosy
• /
• v.43 no.2
• /
• pp.122-126
• /
• 2012

The MeOH extract of Evodiae Fructus exhibited a significant inhibition on the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), in a dose dependent manner, respectively. The extensive bioactivity-guided fractionation process with the MeOH extract finally isolated four compounds, as rutaecarpine (1), evodiamine (2), limonin (3) and dehydroevodiamine (4). Among them, compound 2 exhibited specific inhibitory activity on BChE with the $IC_{50}$ values 1.7 ${\mu}g/ml$, whereas compound 4 showed the potent inhibition upon both AChE and BChE.

• Natural Product Sciences
• /
• v.28 no.3
• /
• pp.138-142
• /
• 2022

Alzheimer's disease (AD) is the most common age-related neurodegenerative disease in industrialized countries. It is estimated that about 47 million people living with dementia and the number of cases will be tripled by 2050. However, the exact mechanism of AD is not known, and full therapy has still not been found. Various tryptophan-derived alkaloids have been reported as promising agents for the treatment of AD. In the present study, a series of tryptophan-derived alkaloids were isolated and characterized from the methanol extract of Hedera rhombea fruit. Based on the analysis of their observed and reported spectroscopic data, their structures were identified as N-[4'-hydroxy-(E)-cinnamoyl]-L-tryptophan (1), N-[3',4'-dihydroxy-(E)-cinnamoyl]-L-tryptophan (2), N-[4'-hydroxy-(E)-cinnamoyl]-L-tryptophan methyl ester (3), and N-[3',4'-dihydroxy-(E)-cinnamoyl]-L-tryptophan methyl ester (4). These compounds were screened for anti-Alzheimer activity via their inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes in vitro. As a result, compounds 3 and 4 showed moderate BChE inhibition with IC₅₀ values of 86.9 and 78.4 μM, respectively, compared to those of the positive control [berberine (IC₅₀ = 11.5 μM)]. However, all four compounds did not show significant inhibition of the AChE enzyme. This is the first time, the AChE and BChE inhibitory activities of these tryptophan-derived alkaloids were investigated and reported.

• Parasites, Hosts and Diseases
• /
• v.51 no.4
• /
• pp.421-426
• /
• 2013

Several studies have shown the mechanisms and importance of immune responses against Toxoplasma gondii infection and the notable role of cholinesterases in inflammatory reactions. However, the association between those factors has not yet been investigated. Therefore, the aim of this study was to evaluate the acetylcholinesterase (AChE) activity in blood and lymphocytes and the activity of butyrylcholinesterase (BChE) in serum of rats experimentally infected with T. gondii during the acute phase of infection. For that, an in vivo study was performed with evaluations of AChE and BChE activities on days 5 and 10 post-infection (PI). The activity of AChE in blood was increased on day 5 PI, while in lymphocytes its activity was enhanced on days 5 and 10 PI (P<0.05). No significant difference was observed between groups regarding to the activity of BChE in serum. A positive (P<0.01) correlation was observed between AChE activity and number of lymphocytes. The role of AChE as an inflammatory marker is well known in different pathologies; thus, our results lead to the hypothesis that AChE has an important role in modulation of early immune responses against T. gondii infection.

• Proceedings of the PSK Conference
• /
• 2002.10a
• /
• pp.375.3-375.3
• /
• 2002

In continuing search for BChE-inhibitory compounds from Korean marine algae. we found a highly potent inhibitory activity in the methanolic extract of Sargassum species. After partition of the MeOH extract between $CHCl_3$ and 30% MeOH. the former layer was subjected to a series of ODS flash chromatography. silica column chromatography. and preparative TLC to afford three compounds (1-3). Detailed structural elucidation of them is in progress. Compound 1 showed potent BChE-inhibitory activity with $IC_{50}$ values of 11 ng/mL. (omitted)

• Journal of Ginseng Research
• /
• v.34 no.4
• /
• pp.348-354
• /
• 2010

Black ginseng and white ginseng were extracted with 80% ethanol and evaluated for relative ginsenoside composition, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, and antioxidant properties. As analyzed by HPLC, black ginseng contained a greater proportion of ginsenoside $Rg_3$ compared to white ginseng. White ginseng was characterized by undetectable ginsenoside $Rg_3$ but it contained more total ginsenosides than black ginseng. Black ginseng extract exhibited higher (p<0.05) free radical-scavenging activity, as well as higher antioxidant activities than white ginseng against 2,2-diphenyl-1-picryl-hydrazyl, superoxide dismutase, and xanthine oxidase, despite the fact that the total saponin content was higher in white ginseng than black ginseng. In addition, the black ginseng extract displayed greater AChE and BChE inhibitory activities. These results suggest that black ginseng has stronger effects on anti-oxidation and AChE and BChE inhibition than white ginseng.

• Journal of Applied Biological Chemistry
• /
• v.66
• /
• pp.165-170
• /
• 2023

Isolation of the culture broth of a marine-derived Acremonium sp. CNQ-049 guided by HPLC-UV yielded compound 1 (3-phenethyl-2-phenylquinazolin-4(3H)-one), and its inhibitory activities against monoamine oxidases (MAOs), cholinesterases (ChEs), and β-secretase 1 (BACE1) were evaluated. Compound 1 was an effective selective MAO-B inhibitor with an IC₅₀ value of 9.39 µM and a selectivity index (SI) value of 4.26 versus MAO-A. In addition, compound 1 showed a potent selective butyrylcholinesterase (BChE) inhibition with an IC₅₀ value of 7.99 µM and an SI value of 5.01 versus acetylcholinesterase (AChE). However, compound 1 showed weak inhibitions against MAO-A, AChE, and BACE1. The Ki value of compound 1 for MAO-B was 5.22±1.73 µM with competitive inhibition, and the Ki value of compound 1 for BChE was 3.00±1.81 µM with mixed-type inhibition. Inhibitions of MAO-B and BChE by compound 1 were recovered by dialysis experiments. These results suggest that compound 1 is a dual-functional reversible inhibitor of MAO-B and BChE, that can be used as a treatment agent for neurological disorders.

• Journal of applied mathematics & informatics
• /
• v.5 no.1
• /
• pp.99-110
• /
• 1998

In this paper we study cyclic codes in $Z_m$. i.e., ideals in $Z_mG$, G afinite abelian group and we give a classification of such codes. We also sgtudy the minimum Hamming distance and the generalized Hamming weight of BCH codes over $Z_m$.

• Natural Product Sciences
• /
• v.24 no.2
• /
• pp.88-92
• /
• 2018

The present study was undertaken to investigate the isolated compounds from the stem bark of Garcinia atroviridis as potential cholinesterase inhibitors and the ligand-enzyme interactions of selected bioactive compounds in silico. The in vitro cholinesterase results showed that quercetin (3) was the most active AChE inhibitor ($12.65{\pm}1.57{\mu}g/ml$) while garcinexanthone G (6) was the most active BChE inhibitor ($18.86{\pm}2.41{\mu}g/ml$). It is noteworthy to note that compound 6 was a selective inhibitor with the selectivity index of 11.82. Molecular insight from docking interaction further substantiate that orientation of compound 6 in the catalytic site which enhanced its binding affinity as compared to other xanthones. The nature of protein-ligand interactions of compound 6 is mainly hydrogen bonding, and the hydroxyl group of compound 6 at C-10 is vital in BChE inhibition activity. Therefore, compound 6 is a notable lead for further drug design and development of BChE selective inhibitor.

• Journal of Life Science
• /
• v.12 no.1
• /
• pp.32-42
• /
• 2002

It was researched to react horse serum-BChE with hefanoylthiocholine chosen among choline esters. According as number of carbon of acyl group in choline esters was increased, reactivity was decreased but strength of ES complex was increased (Km=0,140mM). The pH-V/K profile for BChE-catalyzed hydrolysis of hexanoylthiocholine yields a p $K_{a}$ =4.974$\pm$0.028. This value is equal to recent literature that shows systematic shift from dependence of activity on the basic form fo a residue that huts a p $K_{a}$ =6.2~6.4 to catalysis by a residue or residues that has a p $K_{a}$ =4.7~5.0. The resulting kinetic solvent isotope effect of hexanoylthiocholine is $^{D/V}$K=1.18. The magnitude of the isotope effect suggests that proton transfer is not an element of transition-state stabilization.n.

• Proceedings of the Korean Institute of Information and Commucation Sciences Conference
• /
• 2002.05a
• /
• pp.559-562
• /
• 2002

본 논문에서는 최근 제한적으로 사용이 승인된 UWB(초광대역： Ultra-Wideband) 통신을 AWGN 하에서 다중 접속을 고려하지 않은 단일 사용사일 경우로 가정시, M진 값이 변화함에 따른 에러율과 성능 개선 기법으로 BCH를 채용시의 에러율을 비교 분석하였다. 기존에 연구되어 오던 변조로 PAM(Pulse Amplitude Modulation)과 PPM(Pulse Position Modulation)방식을 비교하였으며 에러율 $10^{-6}$을 기준으로 M=2, 4일 경우 PAM이 PPM보다 약 E$_{b}$/N$_{o}$ =3~4［dB］, M=8 이상의 경우 PPM이 약 E$_{b}$/N$_{o}$ =9［dB］, M=16일 경우 약 E$_{b}$/N$_{o}$ =15［dB］정도 성능이 우수하였다. AWGN 채널 하에서 에러 정정 부호인 BCH(15,7)를 도입하였을 경우 에러율 $10^{-6}$을 기준으로 PAM방식은 약 E$_{b}$/N$_{o}$ 가 약 1［dB］, PPM 방식은 M=2, 4일 경우 약 E$_{b}$/N$_{o}$ =1~1.5［dB］정도 개선되었다.