• 제목/요약/키워드: Ach T

검색결과 35건 처리시간 0.034초

INFLUENCE OF PINACIDIL ON CATECHOLAMINE SECRETION EVOKED BY CHOLINERGIC STIMULATION AND MEMBRANE DEPOLARIZATION FROM THE RAT ADRENAL GLAND

  • Lim, Dong-Yoon;Park, Geun-Hong;Choi, Cheol-Hee;Ko, Suk-Tai
    • 한국응용약물학회:학술대회논문집
    • /
    • 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
    • /
    • pp.148-149
    • /
    • 1998
  • It has been known that potassium channel openers are a new class of molecules that have attracted general interest because of their potent antihypertensive activity in vivo and vasorelaxant activity in vitro (Hamilton and Weston, 1989). In the present study, it was attempted to examine the effect of the potassium channel opener on catecholamine (CA) secretion evoked by cholinergic stimulation, membrane depolarization and calcium mobilization from the isolated perfused rat adrenal gland. The perfusion of pinacidil (30-300 uM) into an adrenal vein for 20 min produced relatively dose-dependent inhibition in CA secretion evoked by ACh (5.32 mM), high $K^{+}$ (56 mM), DMPP (100 uM for 2 min), McN-A-343 (100 uM for 2 min), cyclopiazonic acid (10 uM for 4 min) and Bay-K-8644 (10 uM for 4 min). Also, under the presence of minoxidil (100 uM), which is also known to be a potassium channel activator, CA secretory responses evoked by ACh, high potassium, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid were also significantly depressed. However, in adrenal glands preloaded with pinacidil (100 uM) under the presence of glibenclamide (1 uM), an antidiabetic sulfonylurea that has been shown to be a specific blocker of ATP-regulated potassium channels (for 20 min), CA secretory responses evoked by ACh, high potassium, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid were considerably recovered to a considerable extent of the normal release as compared to that of pinacidil only. These results, taken together, suggest that pinacidil cause the marked inhibition of CA secretion evoked by stimulation of cholinergic (both nicotinic and muscarinic) receptors as well as by membrane depolarization, indicating strongly that this effect may be mediated by inhibiting influx of extracellular calcium and release in intracellular calcium in the rat adrenomedullary chromaffin cells. Furthermore, these findings suggest strongly that these potassium channel openers-sensitive membrane potassium channels also play an important role in regulating CA secretion.

  • PDF

사육탕가미방(四六湯加味方)이 흰쥐의 학습(學習) 및 기억(記憶)에 미치는 영향(影響) (An exprimental Study on the Effects of saruktanggamibangbangbang on Memory and Learning of Rats)

  • 장규태;김장현;박보경
    • 대한한방소아과학회지
    • /
    • 제18권1호
    • /
    • pp.207-220
    • /
    • 2004
  • Objective: This study was conducted to find out the effect of saruktanggamibang(SRT) on memory and learning of rats. Methods: The mon·is water maze was used. It was performed Acquisition test, Retention test of water maze. After Behavioral test, it was investigated AChE cell numbers of CAI and CA3 on hippocampus. Results: of water maze revealed that acqusitive abilities of SAP+SRT group significantly improved on 3, 4, 5th day compared with SAP+Saline group. Retention test of water maze didn't reveal that retentive abilities of SAP+SRT group significantly improved comparing with another group. ChAT cell numbers of medial septum of SAP+SRT group significantly increased compared with SAP+Saline group. AChE cell numbers of CAl and CA3 on hippocampus of Sham+SRT group significantly increased compared with Sham group. And AChE cell numbers of CAl and CA3 on hippocampus of SAP+SRT group significantly increased compared with SAP+Saline group. Conclusion: Saruktanggamibang(SRT) has an effect on memory and learning of rats.

  • PDF

A Role for Leu247 Residue within Transmembrane Domain 2 in Ginsenoside-Mediated α7 Nicotinic Acetylcholine Receptor Regulation

  • Lee, Byung-Hwan;Choi, Sun-Hye;Pyo, Mi Kyung;Shin, Tae-Joon;Hwang, Sung-Hee;Kim, Bo-Ra;Lee, Sang-MoK;Lee, Jun-Ho;Lee, Joon-Hee;Lee, Hui Sun;Choe, Han;Han, Kyou-Hoon;Kim, Hyoung-Chun;Rhim, Hyewhon;Yong, Joon-Hwan;Nah, Seung-Yeol
    • Molecules and Cells
    • /
    • 제27권5호
    • /
    • pp.591-599
    • /
    • 2009
  • Nicotinic acetylcholine receptors (nAChRs) play important roles in nervous system functions and are involved in a variety of diseases. We previously demonstrated that ginsenosides, the active ingredients of Panax ginseng, inhibit subsets of nAChR channel currents, but not ${\alpha}7$, expressed in Xenopus laevis oocytes. Mutation of the highly conserved Leu247 to Thr247 in the transmembrane domain 2 (TM2) channel pore region of ${\alpha}7$ nAChR induces alterations in channel gating properties and converts ${\alpha}7$ nAChR antagonists into agonists. In the present study, we assessed how point mutations in the Leu247 residue leading to various amino acids affect 20(S)-ginsenoside $Rg_3$ ($Rg_3$) activity against the ${\alpha}7$ nAChR. Mutation of L247 to L247A, L247D, L247E, L247I, L247S, and L247T, but not L247K, rendered mutant receptors sensitive to $Rg_3$. We further characterized $Rg_3$ regulation of L247T receptors. We found that $Rg_3$ inhibition of mutant ${\alpha}7$ nAChR channel currents was reversible and concentration-dependent. $Rg_3$ inhibition was strongly voltage-dependent and noncompetitive manner. These results indicate that the interaction between $Rg_3$ and mutant receptors might differ from its interaction with the wild-type receptor. To identify differences in $Rg_3$ interactions between wild-type and L247T receptors, we utilized docked modeling. This modeling revealed that $Rg_3$ forms hydrogen bonds with amino acids, such as Ser240 of subunit I and Thr244 of subunit II and V at the channel pore, whereas $Rg_3$ localizes at the interface of the two wild-type receptor subunits. These results indicate that mutation of Leu247 to Thr247 induces conformational changes in the wild-type receptor and provides a binding pocket for $Rg_3$ at the channel pore.

현호소약침액(玄胡索藥鍼液)의 acetylcholinesterase 억제효과와 항산화에 미치는 영향(影響) (Effect of Corydalis tuber Acua-acupuncture Solution on Antiacetylcholinesterase and Antioxidants)

  • 강미경;남상수;이윤호
    • Journal of Acupuncture Research
    • /
    • 제21권3호
    • /
    • pp.235-248
    • /
    • 2004
  • It has been investigated about aging theory. However, aging mechanism still remains to be unknown. Aging and aging related diseases might be due to oxidative damage and these were modifiable by genetic and environmental factors. For designing an optimal medical treatment and countermeasure against aging and aging related disease, it is necessary to understand the aging mechanism. Acetylcholine(Ach) plays an important role in memory. If someone doesn't have enough Ach, he has a tendency to catch a Alzheimer's disease. Corydalis tuber has been clinically used to treat heart disease, gastrointestinal disease and other diseases including endocrine disease in Oriental medicine. The purpose of this article is to investigate the inhibitory effect on Acetylcholinesterase and scavenging effects on NO, DPPH of Corydalis tuber Acua-acupuncture solution(CTAS). The results are summerised as follows; 1. There is a significant inhibitory effect of $0.01mg/m{\ell}$ CTAS group at 20, 30, 60 minutes and $0.1mg/m{\ell}$ CTAS group at 10, 20, 30, 60 minutes on AchE. 2. There is no significant scavenging effect of CTAS on NO. 3. There is a significant scavenging effect of $0.1mg/m{\ell}$ and $0.01mg/m{\ell}$ CTAS group at 10 minutes but there is no significant scavenging effect at 20, 30, 60 minutes on DPPH. There is a significant scavenging effect of $1mg/m{\ell}$ CTAS group at 10, 20, 30, 60 minutes on DPPH.

  • PDF

Acetylcholinesterase(AChE)-Catalyzed Hydrolysis of Long-Chain Thiocholine Esters: Shift to a New Chemical Mechanism

  • Jung, Dai-Il;Shin, Young-Ju;Lee, Eun-Seok;Moon, Tae-sung;Yoon, Chang-No;Lee, Bong-Ho
    • Bulletin of the Korean Chemical Society
    • /
    • 제24권1호
    • /
    • pp.65-69
    • /
    • 2003
  • The kinetic and chemical mechanisms of AChE-catalyzed hydrolysis of short-chain thiocholine esters are relatively well documented. Up to propanoylthiocholine (PrTCh) the chemical mechanism is general acid-base catalysis by the active site catalytic triad. The chemical mechanism for the enzyme-catalyzed butyrylthiocholine(BuTCh) hydrolysis shifts to a parallel mechanism in which general base catalysis by E199 of direct water attack to the carbonyl carbon of the substrate. [Selwood, T., et al. J. Am. Chem. Soc. 1993, 115, 10477- 10482] The long chain thiocholine esters such as hexanoylthiocholine (HexTCh), heptanoylthiocholine (HepTCh), and octanoylthiocholine (OcTCh) are hydrolyzed by electric eel acetylcholinesterase (AChE). The kinetic parameters are determined to show that these compounds have a lower Michaelis constant than BuTCh and the pH-rate profile showed that the mechanism is similar to that of BuTCh hydrolysis. The solvent isotope effect and proton inventory of AChE-catalyzed hydrolysis of HexTCh showed that one proton transfer is involved in the transition state of the acylation stage. The relationship between the dipole moment and the Michaelis constant of the long chain thiocholine esters showed that the dipole moment is the most important factor for the binding of a substrate to the enzyme active site.

실내공기질을 고려한 유치원 보육실의 적정 환기량 검토 (Minimum Ventilation Rate of Kindergarten in the respect of IAQ)

  • 정창헌;이윤규;김태연;이승복
    • 대한설비공학회:학술대회논문집
    • /
    • 대한설비공학회 2006년도 하계학술발표대회 논문집
    • /
    • pp.283-288
    • /
    • 2006
  • Indoor Air Quality Guideline of Kindergarten in korea didn't consider the vulnerable properties of children to indoor air pollutants. For this reason, Suggestion for the IAQ guideline of formaldehyde and minimum ventilation rate was made in this study. Suggested IAQ guidelines for formaldehyde in the respect of children's vulnerable immune system is $30{\mu}g/m^3$ and $50{\mu}g/m^3$, and for the ventilation rate 11.9 ACH, 5.8 ACH, respectively. This value is based only formaldehyde and CO2 concentrations in child-care room of Kindergarten and needed to be verified by further investigations and studies. However it is discovered that lower formaldehyde concentration can do mal-effects to children's health by literature review.

  • PDF

침자극에 대한 반응과 비반응군 흰쥐의 특이 유전자 발현 연구 (Gene Expression Profile of the Responder vs. the Non-Responder to the Acupuncture Mediated Analgesic Effects)

  • 서영찬;노삼웅;이기석;고은정;홍무창;신민규;민병일;배현수
    • 동의생리병리학회지
    • /
    • 제17권3호
    • /
    • pp.633-642
    • /
    • 2003
  • A pain is the symptom which defends against noxious stimulus about a human body, it is known that if the periphery of perceptive nerve were stimulated by a physical or chemical factors, the stimulation is induced by transmission to pain center in the cerebral cortex according to pain conduction tract. The treatment of pain is to decrease a stimulus that causes a pain or block off a nerve transmitting a stimulus or puts on a way to calm down pain center, but It is for adjustment of a pain to be the most representative in acupuncture among various ways to cure a pain in Oriental medicine. However, the analgesic effect of an individual response to acupuncture stimulation shows marked individual variations, so these days genetic a few approach is attempted. On this the author determined that the responding group was appointed those whose tail flick latency (TFL) responding time delayed the minimum of 30 % comparing with basal reaction time. For those whose TFL time had shorter than 30 % was grouped as a non-responding group. And then the hypothalamus of each group was dissected and RNA was further purified. After synthesizing cDNA using oligo dT primer, products were finally applied to the PCR. The results were as follows; The ratio of responding group to non-responding group was 6:4. Ach T (acetylcholinesterase T subunit), BF-I (Brain factor-I), DBH (Dopamine β-hydroxylase) and PNM (Phosphotidylethanolamine N-Methyltransferase) were revealed significantly in the responding group. Cathepsin B and Tau were revealed significantly in the non-responding group. The PCR results show that Ach T, BF-I, DBH and PNM are expressed abundantly in the responding group, where as cathepsin B and tau are abundant in the non-responding group. These results suggest that the analgesic effect on acupuncture stimulation is related to regulation of neurotransmitter as well as neurodegeration of cerebrum.

Study of Effects of Electroacupuncture on the Hippocampal Cholinergic Neuronal Activity

  • Lee Kwang Ro;Kang Sei Young;Yoon Ji Won;Cho Chang Hyun;Sung Kang Keyng
    • 동의생리병리학회지
    • /
    • 제18권6호
    • /
    • pp.1850-1855
    • /
    • 2004
  • The purpose of this report is to investigate the electroacupuncture effect on the cholinergic neuronal activation in the hippocampal CA1 section. The electroacupuncture was performed on S36 of white rats and its consequencies were investigated by immunohistochemical method. Hippocampal CA1 sections of Sprague Dawley white male rats electroacupunctured on S36 at 20㎐ and 100㎐ are stained by cresyl violet to show that the values of 100㎐ and 20㎐ group increased significantly compared to sham group's one. Especially, 100㎐ group shows stronger neuronal activation compared to 20㎐ group. Induction of AChE, a neurotransmitter, in hippocampal CA1 is increased significantly in 100㎐ and 20㎐ group compared to sham group. Especially 20㎐ group shows higher AChE immunoreaction than 100㎐ does, although it wasn't significant enough. Induction of NGF(Nerve Growth Factor) in hippocampal CA1 sections was observed higher in 20㎐ and 100㎐ group than in sham group. Especially, 20㎐ group shows higher NGF immunoreaction compared to 100㎐. The facts above indicate that the eletroacupucture is effect to the cholinergic neuronal activation of hippocampus induced by focal ischemia.

가상 검색 및 시험관 시험을 이용한 총명탕 중 주성분들에 대한 약물작용 및 대사 예측 (In silico Prediction and In vitro Screening of Biological Activities and Pharmacokinetics for the Major Compounds in Chong Myung Tang)

  • 권영이
    • 약학회지
    • /
    • 제51권6호
    • /
    • pp.463-468
    • /
    • 2007
  • Chong Myung Tang is consisted of three medicinal herbs (Acori Graminei Rhizoma, Polygalae Radix and Hoelen cum Radix). It has been used as a medicine for the purpose of learning and memory improvement. In this paper, Chong Myung Tang was screened the biological activities for Alzheimer's disease. The extract (70% ethanol) of Acari Graminei Rhizoma (1 mg/ml) showed that acetylcholinesterase (AChE) and amyloid beta ($A{\beta}$) peptide aggregation inhibitory potency are 43.1% and 76.5%, respectively. The extract of Polygalae Radix showed inhibitory activity against $A{\beta}_{1-42}$ peptide aggregation (51.5%). To predict the drug-likeness, oral absorption ability; blood-brain barrier (BBB) penetraion rate, mutagenecity and carcinogenicity; in silico screening was performed against 16 compounds in the three medicinal herbs. According to the results, all compounds have appropriate chemical structures as medicines. The six compounds in Acori Graminei Rhizoma and the five compounds in Hoelen cum Radix showed excellent oral absorption rate and BBB penetration rate. The four compounds in Polygalae Radix showed excellent oral absorption rate, but their BBB penetration was presented low rate. And, the extract of Hoelen cum Radix didn't show AChE and $A{\beta}_{1-42}$ peptide aggregation inhibitory activities in vitro. Therefore, their activity in brain may be other mechanism. According to all of the results, in silico prediction technology is convenient and effective to determine biological active compounds in medicinal herbs.

Indoor radon and thoron from building materials: Analysis of humidity, air exchange rate, and dose assessment

  • Syuryavin, Ahmad Ciptadi;Park, Seongjin;Nirwono, Muttaqin Margo;Lee, Sang Hoon
    • Nuclear Engineering and Technology
    • /
    • 제52권10호
    • /
    • pp.2370-2378
    • /
    • 2020
  • Building materials contribute significantly to the indoor radon and thoron levels. Therefore, parameters that influence the exhalation rates of radon and thoron from building material need to be analyzed closely. As a preliminary study, the effects of humidity on exhalation rates were measured using a system with an accumulation chamber and RAD7 detector for Korean brick, Korean soil, and Indonesian brick. Resulting doses to a person who resides in a room constructed from the building materials were assessed by UNSCEAR method for different air exchange rates. The measurements have revealed that Korean brick exhaled the highest radon and thoron while Indonesian brick exhaled the lowest thoron. Results showed that for a typical low dense material, radon and thoron exhalation rate will increase until reached its maximum at a certain value of humidity and will remain saturated above it. Analysis on concentration and effective dose showed that radon is strongly affected by air exchange rate (ACH). This is showed by about 66 times decrease of radon dose from 0.00 h-1 to those of 0.50 h-1 ACH and decrease by a factor of 2 from 0.50 h-1 to those of 0.80 h-1. In case of thoron, the ACH doesn't have significant effects on effective dose.