• 대한한의학회지
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• 제25권4호
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• pp.1-7
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• 2004

Objective : This study was designed to examine the effects of orally administered Prunus persica water extract (PPE), which is used as herbal medicine, for treatment of Yu Xue (stasis of blood) and tacrine on the basal concentration of extracellular acetylcholine in the hippocampus of rats. Methods: To investigate the effects of PPE and tacrine on concentration of extracellular acetylcholine in the hippocampus of rats, the microdialysis technique, under the same experimental conditions, was used. And we used male Wistar rats which were 7 weeks of age and 210-290 g. PPE was extracted with boiling water, and the rats were anesthetized with pentobarbital Na. Their skulls were exposed and a hole was drilled for implantation of a microdialysis probe. In order to increase the recovery of acetylcholine, a probe with a long membrane was used. One day after surgery, the microdialysis probe was perfused with Ringer's solution at a flow rate of 1.5 l/min. The acetylcholine concentration in dialysis samples was measured by high-performance liquid chromatography (HPLC) with electrochemical detection. AChE activity was measured using the radiometric method, as described by Sherman. Results : The comparative effects of PPE and tacrine on hippocampal extracellular acetylcholine concentration was that these cholinesterase inhibitors produced dose-dependent increases in the extracellular acetylcholine concentration. And the effect of PPE and tacrine on rat brain AChE activity was that PPE produced maximal inhibition at 1 h after administration, when AChE activity was 44% of the intact level. AChE activity gradually recovered thereafter, and reached 78% of the intact level at 12 h after administration. Conclusion : In this study, PPE has a potent activity and a long-lasting effect on the central cholinergic system, in terms of the basal concentration of extracellular acetylcholine in the hippocampus and the AChE activity in the brain of rats. And oral administration of PPE increased dose-dependently the basal concentration of extracellular acetylcholine in the hippocampus of rats. PPE may be one of the more useful cholinesterase inhibitors for the treatment of Alzheimer's disease.

• 한국어병학회지
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• 제9권1호
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• pp.53-63
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• 1996

경골어류의 혈관평활근에 대한 choline 작동성 조절기작을 규명하기 위한 목적의 일환으로 틸라피아의 배대동맥(dorsal aorta)에 대한 acetylcholine 효과와 이들 효과의 매개에 관여하는 수용체의 subtype에 대한 연구를 수행하였으며 그 결과는 다음과 같다. 1. Acetylcholine은 틸라피아의 배대동맥에 대하여 농도의존적인 혈관수축반응만을 나타내었으며, 이와 같은 반응은 혈관내피세포와 methylene blue에 의해 영향을 받지 않았다. 2. Acetylcholine에 의한 농도의존적인 혈관수축반응곡선은 비선택적인 muscarine 수용체 길항제인 atropine과 선택적인 $M_2$-수용체 길항제인 gallamine의 경우 그 농도가 증가함에 따라 현저하게 오른쪽으로 평행이동되었으나, 선택적인 $M_1$-수용체 길항제인 pirenzepine에 의해서는 고농도($1{\times}10^{-5}$M)에서만 약간 이동되었다. 3. Acetylcholine의 수축효과는 cyclooxygenase 억제제인 indomethacin에 의해 거의 영향을 받지 않았다. 4. Acetylcholine의 혈관수축반응은 calcium제거 생리적 완충용액에서는 거의 소실되었으나, calcium 유입차단제인 verapamil에 의해서는 거의 영향을 받지 않았다. 이상의 실험결과에서 acetylcholine은 틸라피아 배대동맥에 대하여 내피세포와는 무관하게 혈관수축효과를 나타내었다. Acetylcholine에 의한 이 수축은 주로 $M_2$-subtype의 수용체를 매개하며 receptor-linked $Ca^{2+}$ channel을 통하여 유입된 세포질내의 $Ca^{2+}$에 의해 일어난다고 사료된다.

• Journal of Plant Biology
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• 제19권1호
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• pp.14-18
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• 1976

Inhibition of flowering in Lemna perpusilla 6746 by 30 mM sucrose was reversed by the addition of acetylcholine (>$10^{-4}M) supplemented with 10^{-4}M$ ascorbic acid to 1/10-strength Hunter's growth medium. The reversible effect of acetylcholine was found to be greater at early stages of flowering than in the later period. Promotive effects of both acetylcholine ($10^{-3}M) and eserine(10^{-5}M$) on flowering in the short-day plant under various photoperiodic conditions were studied. It was indicated that the application decreased length of the critical dark period for the floral induction, and it was also shown that the endogenous status of acetylcholine was involved in the floral response which had a correlation with phytochrome. Interruption of inductive dark periods by red irradiation (1min) immediately followed by far-red light (1 min) completely inhibited flowering, while the addition of acetylcholine and eserine to the medium under the same condition slightly promoted flowering, indicating possible involvement of phytochrome system in acetylcholine activity for photoperiodic sensitivity of floral response in Lemna perpusilla 6746.

• 대한한방내과학회지
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• 제17권1호
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• pp.193-203
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• 1996

These studies were carried out to investigate the effect of Insameumja water extract on the inhibitory contractile action of acetylcholine in guinea pig. The results of these studies were as follows; 1. Contractile force of acetylcholine from trachea smooth muscle in guinea pig was significantly inhibited by Insameumja. 2. Dose-response of acetylcholine pretreated Insameumja in guinea pig was not significantly changed. 3. Inhibitory contractile action of acetylcholine pretreated propranolol in guinea pig was decreased. 4. Inhibitory contractile action of acetylcholine pretreated indomethacin was significantly changed by Insameumja. 5. Inhibitory contractile action of acetylcholine pretreated methylene blue was not significantly changed by Insameumja.

• 대한한방내과학회지
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• 제16권2호
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• pp.92-100
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• 1995

These studies were carried out to investigate the effect of Mahwangchangchultang water extract on the inhibitory contractile action of acetylcholine in guinea pig. The results of these studies were as follows; 1. Contractile force of acetylcholine from trachea smooth muscle in guinea pig was significantly inhibited by Mahwangchangchultang 2. Dose-response of acetylcholine pretreated Mahwangchangchultang in guinea pig was not significantly changed. 3. Inhibitory contractile action of acetylcholine pretreated propranolol in guinea pig was decreased. 4. Inhibitory contractile action of acetylcholine pretreated indomethacin was not significantly changed by Mahwangchangchultang. 5. Inhibitory contractile action of acetylcholine pretreated methylene blue was not significantly changed by Mahwangchangchultang.

• 대한한방내과학회지
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• 제16권1호
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• pp.146-159
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• 1995

These studies were carried out to investigate the effect of Chunggeumeum water extract on the inhibitory contractile action of acetylcholine in guinea pig. The results of these studies were as follows; 1. Contractile force of acetylcholine from trachea smooth muscle in guinea pig was significantly inhibited by Chunggeumeum. 2. Dose-response of acetylcholine pretreated Chunggeumeum in guina pig was not significantly changed. 3. Inhibitory contractile action of acetylcholine pretreated propranolol in guinea pig was decreased. 4. Inhibitory contractile action of acetylcholine pretreated indomethacin was not significantly changed by Chunggeumeum. 5. Inhibitory contractile action of acetylcholine pretreated methylene blue was not significantly changed by Chunggeumeum.

• 동국한의학연구소논문집
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• 제4권
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• pp.267-311
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• 1995

This study was performed to analyze the effects of WhoaDam-JiHae PyeongChunYak on contracted tracheal smooth muscle in rat. Transverse strips were used for the experiment using organ bath. The test strip was perfused with modified Krebs-Ringer Bicarbonate solution which was aerated with 95% $O_2$-5% $CO_2$ mixed gas and kept at $37^{\circ}C$. WhoaDam-JiHae PyeongChunYak extract and acetylcholine infused tracheal strip that was contracted with acetylcholine. The results were as follows : 1. The contractile force of tracheal strip by acetylcholine was significantly increased by Pinelliae Rhizoma, Arisaematis Rhizoma, Sinapis Semen. Typhonii Rhizoma, Peucedani Radix, Eriobotryae Folium, Platycodi Radix, Bambusae Caulis Taeniam, Benincasae Semen, Armeniacae Amarum Semen, Asteris Radix, Periliae Fructus, Mori cortex and Lepidii Semen. 2. Arisaematis Rhizoma($1{\mu}{\ell}/m{\ell}$, $3{\mu}{\ell}/m{\ell}$, $10{\mu}{\ell}/m{\ell}$) and Asteris Radix($1{\mu}{\ell}/m{\ell}$, $3{\mu}{\ell}/m{\ell}$) slightly relaxed the contracted tracheal strip by acetylcholine. 3. Farfarae Flos significantly relaxed the contracted tracheal strip by acetylcholine. 4. The contractile force of tracheal strip by acetylcholine was significantly increased by Stemonae Radix at $30{\mu}{\ell}/m{\ell}$, on the other hand Stemonae Radix at $100{\mu}{\ell}/m{\ell}$ significantly relaxed the contracted tracheal strip by acetylcholine.

• 약학회지
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• 제56권4호
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• pp.222-229
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• 2012

In order to determine acetylcholine and choline in the biological samples, the specific enzymes of acetylcholinesterase (AChE) and choline oxidase (ChO), which utilize acetylcholine and choline as substrates, were employed to convert substrates to $H_2O_2$. The produced $H_2O_2$ was coupled to 4-aminoantipyrine/phenol with peroxidase (PO) yielding quinoneimine dye which was measured at 508 nm. In the present enzymatic spectrophotometric analysis the product at the equilibrium state was measured considering accuracy, precision, time and cost of the analysis. The developed analytical method yielded good linearity (calibration curve; $A_{508}$=9534[acetylcholine]+0.009, correlation coefficient ($R^2$); 0.999) with detection limit of $1.11{\times}10^{-7}M$, reasonable precision (relative standard deviation; 0.10~1.62% at $2.5{\times}10^{-6}M{\sim}1.25{\times}10^{-4}M$) and accuracy (relative error; -0.24~0.97% at $4.13{\times}10^{-6}M{\sim}1.01{\times}10^{-4}M$) for acetylcholine chloride standard solution. The concentrations of acetylcholine and choline in human serum were found as $3.20{\times}10^{-5}M$ and $1.14{\times}10^{-4}M$, respectively. The brain tissues of Sprague-Dawley strain rat contained 9.82${\mu}g/g$ of acetylcholine and 6.53 ${\mu}g/g$ of choline in the cerebrum, while 7.37 ${\mu}g/g$ of acetylcholine and 5.34 ${\mu}g/g$ of choline in the cerebellum.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1996년도 춘계학술대회
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• pp.179-179
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• 1996

The involvement of the cyclic AMP (cAMP) effector system in the release of endogenous dopamine and acetylcholine from the rat neostriatum was assessed. Forskolin, an activator of adenylate cyclase, was used to enhance CAMP production, and the consequence of this enhancement on the spontaneous and potassium stimulated release of dopamine and acetylcholine was evaluated. Neostriatal slices were prepared from Fischer 344 rats and after a preincubation period the release of each endogenous neurotransmitter was measured from the same slice preparation. To measure acetylcholine release the slice acetylcholinesterase (AChE) activity was inhibited with physostigmine, but the release from slices with intact AChE activity was also determined (choline, instead of acetylcholine was detected in the medium). Under both conditions forskolin induced a significant dose-dependent increase in the potassium-evoked release of dopamine. In the same tissue preparations the release of neither acetylcholine (AChE inhibited) nor choline (AChE intact) was affected by forskolin. The results indicate that the cAMP second messenger system is involved ill neuronal mechanisms that enhance neuronal dopamine release, but stimulation of this second messenger by forskolin does not further enhance neostriatal acetylcholine release.

• The Korean Journal of Physiology and Pharmacology
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• 제15권4호
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• pp.195-201
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• 2011

The flavonoid quercetin is a low molecular weight compound generally found in apple, gingko, tomato, onion and other red-colored fruits and vegetables. Like other flavonoids, quercetin has diverse pharmacological actions. However, relatively little is known about the influence of quercetin effects in the regulation of ligand-gated ion channels. Previously, we reported that quercetin regulates subsets of nicotinic acetylcholine receptors such as ${\alpha}3{\beta}4$, ${\alpha}7$ and ${\alpha}9{\alpha}10$. Presently, we investigated the effects of quercetin on muscle-type of nicotinic acetylcholine receptor channel activity expressed in Xenopus oocytes after injection of cRNA encoding human fetal or adult muscle-type of nicotinic acetylcholine receptor subunits. Acetylcholine treatment elicited an inward peak current ($I_{ACh}$) in oocytes expressing both muscle-type of nicotinic acetylcholine receptors and co-treatment of quercetin with acetylcholine inhibited $I_{ACh}$. Pre-treatment of quercetin further inhibited $I_{ACh}$ in oocytes expressing adult and fetal muscle-type nicotinic acetylcholine receptors. The inhibition of $I_{ACh}$ by quercetin was reversible and concentration-dependent. The $IC_{50}$ of quercetin was $18.9{\pm}1.2{\mu}M$ in oocytes expressing adult muscle-type nicotinic acetylcholine receptor. The inhibition of $I_{ACh}$ by quercetin was voltage-independent and non-competitive. These results indicate that quercetin might regulate human muscle-type nicotinic acetylcholine receptor channel activity and that quercetin-mediated regulation of muscle-type nicotinic acetylcholine receptor might be coupled to regulation of neuromuscular junction activity.