• The Korean Journal of Physiology and Pharmacology
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• 제10권5호
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• pp.273-282
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• 2006

The aim of the present study was to investigate the effects of R-(-)-2,10,11-trihydroxy-N-propylnoraporphine [R-(-)-TNPA], a selective agonist of dopaminergic $D_2$ receptor and S(-)-raclopride, a selective antagonist of dopaminergic $D_2$ receptor, on the secretion of catecholamines (CA) evoked by cholinergic stimulation and membrane-depolarization in the isolated perfused model of the rat adrenal gland, and also to establish its mechanism of action. R-(-)-TNPA $(10{\sim}100\;{\mu}M)$ perfused into an adrenal vein for 60 min produced dose- and time-dependent inhibition in CA secretory responses evoked by ACh (5.32 mM), high $K^+$ (56 mM), DMPP $(100\;{\mu}M)$ and McN-A-343 $(100\;{\mu}M)$. R-(-)-TNPA itself did also fail to affect basal CA output. Also, in adrenal glands loaded with R-(-)-TNPA $(30\;{\mu}M)$, the CA secretory responses evoked by Bay-K-8644 $(10\;{\mu}M)$, an activator of L-type $Ca^2+$ channels and cyclopiazonic acid $(10\;{\mu}M)$, an inhibitor of cytoplasmic $Ca^{2+}-ATPase$ were also inhibited. However, S(-)-raclopride $(1{\sim}10\;{\mu}M)$, given into an adrenal vein for 60 min, enhanced the CA secretory responses evoked by ACh, high $K^+$, DMPP and McN-A-343 only for the first period (4 min), although it alone has weak effect on CA secretion. Moreover, S(-)-raclopride $(3.0\;{\mu}M)$ in to an adrenal vein for 60 min also augmented the CA release evoked by BAY-K-8644 and cyclopiazonic acid only for the first period (4 min). However, after simultaneous perfusion of R-(-)-TNP A $(30\;{\mu}M)$ and S(-)-raclopride $(3.0\;{\mu}M)$, the inhibitory responses of R(-)-TNPA $(30\;{\mu}M)$ on the CA secretion evoked by ACh, high $K^+$, DMPP, McN-A-343, Bay-K-8644, and cyclopiazonic acid were significantly reduced. Taken together, these experimental results suggest that R-(-)-TNPA greatly inhibits the CA secretion from the perfused rat adrenal medulla evoked by cholinergic stimulation (both nicotininc and muscarinic receptors) and membrane depolarization, but S(-)-raclopride rather enhances the CA release by them. It seems that this inhibitory of R-(-)-TNPA may be mediated by stimulation of inhibitory dopaminergic $D_2$ receptors located on the rat adrenomedullary chromaffin cells, while the facilitatory effect of S(-)-raclopride is due to the blockade of dopaminergic $D_2$ receptors, which are relevant to extra- and intracellular calcium mobilization. Therefore, it is thought that dopaminergic $D_2$ receptors may be involved in regulation of CA release in the rat adrenal medulla.

• Korean Journal of Food Science and Technology
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• 제48권1호
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• pp.86-91
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• 2016

Oxidative stress caused by reactive oxygen species is ascribed to many neurodegenerative diseases like Alzheimer's disease. Phenolic antioxidants can reduce the oxidative stress. In this study, ripe fruits of Opuntia ficus-indica var. saboten (OFS) were extracted using 80% (v/v) aqueous ethanol. Total phenolic and flavonoid contents of the OFS fruits (100 g) were 409.9 mg gallic acid equivalents and 72.2 mg catechin equivalents, respectively. The OFS fruits had antioxidant capacity at 381.2, 298.2, and 3,219.9 mg vitamin C equivalents/100 g in ABTS, DPPH, and ORAC assays, respectively. The OFS fruits showed protective effects on PC-12 cells against oxidative stress in a dose-dependent manner, partly due to decrease of intracellular oxidative stress. Furthermore, the OFS fruits inhibited both acetylcholinesterase and butyrylcholinesterase. Consequently, these results suggest that the OFS fruits might be served as a source of functional materials to reduce oxidative stress in neuronal cells and to inhibit cholinesterases.

• Natural Product Sciences
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• 제27권2호
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• pp.86-98
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• 2021

This study was designed to characterize the effect of ginsenoside-Rg2 (Rg2), one of panaxatriol saponins isolated from Korean ginseng root, on the release of catecholamines (CA) in the perfused model of the rat adrenal medulla, and also to establish its mechanism of action. Rg2 (3~30 µM), administered into an adrenal vein for 90 min, depressed acetylcholine (ACh)-induced CA secretion in a dose- and time-dependent manner. Rg2 also time-dependently inhibited the CA secretion induced by 3-(m-chloro-phenyl-carbamoyl-oxy)-2-butynyltrimethyl ammonium chloride (McN-A-343), 1.1-dimethyl-4-phenyl piperazinium iodide (DMPP), and angiotensin II (Ang II). Also, during perfusion of Rg2, the CA secretion induced by high K⁺, veratridine, cyclopiazonic acid, methyl-1,4-dihydro-2,6-dimethyl-3-nitro-4-(2-trifluoro-methyl-phenyl)-pyridine-5-carboxylate (Bay-K-8644) depressed, respectively. In the simultaneous presence of Rg2 and N^ω-nitro-L-arginine methyl ester hydrochloride ʟ-NAME), the CA secretion induced by ACh, Ang II, Bay-K-8644 and veratridine was restored nearly to the extent of their corresponding control level, respectively, compared to those of inhibitory effects of Rg2-treatment alone. Virtually, NO release in adrenal medulla following perfusion of Rg2 was significantly enhanced in comparison to the corresponding spontaneous release. Also, in the coexistence of Rg2 and fimasartan, ACh-induced CA secretion was markedly diminished compared to the inhibitory effect of fimasartan-treated alone. Collectively, these results demonstrated that Rg2 suppressed the CA secretion induced by activation of cholinergic as well as angiotensinergic receptors from the perfused model of the rat adrenal gland. This Rg2-induced inhibitory effect seems to be exerted by reducing both influx of Na⁺ and Ca²⁺ through their ionic channels into the adrenomedullary cells as well as by suppressing Ca²⁺ release from the cytoplasmic calcium store, at least through the elevated NO release by activation of NO synthase, which is associated to the blockade of neuronal cholinergic and AT₁-receptors. Based on these results, the ingestion of Rg2 may be helpful to alleviate or prevent the cardiovascular diseases, via reduction of CA release in adrenal medulla and consequent decreased CA level in circulation.

• The Korean Journal of Physiology and Pharmacology
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• 제26권5호
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• pp.313-323
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• 2022

Atrial fibrillation (AF) is the most common supraventricular arrhythmia, and it corresponds highly with exercise intensity. Here, we induced AF in mice using acetylcholine (ACh)-CaCl₂ for 7 days and aimed to determine the appropriate exercise intensity (no, low, moderate, high) to protect against AF by running the mice at different intensities for 4 weeks before the AF induction by ACh-CaCl₂. We examined the AF-induced atrial remodeling using electrocardiogram, patch-clamp, and immunohistochemistry. After the AF induction, heart rate, % increase of heart rate, and heart weight/body weight ratio were significantly higher in all the four AF groups than in the normal control; highest in the high-ex AF and lowest in the low-ex (lower than the no-ex AF), which indicates that low-ex treated the AF. Consistent with these changes, G protein-gated inwardly rectifying K⁺ currents, which were induced by ACh, increased in an exercise intensity-dependent manner and were lower in the low-ex AF than the no-ex AF. The peak level of Ca²⁺ current (at 0 mV) increased also in an exercise intensity-dependent manner and the inactivation time constants were shorter in all AF groups except for the low-ex AF group, in which the time constant was similar to that of the control. Finally, action potential duration was shorter in all the four AF groups than in the normal control; shortest in the high-ex AF and longest in the low-ex AF. Taken together, we conclude that low-intensity exercise protects the heart from AF, whereas high-intensity exercise might exacerbate AF.

• Journal of Advanced Marine Engineering and Technology
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• 제29권7호
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• pp.736-743
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• 2005

In this study, three different types of mechanical ventilation systems are compared based on their ventilation characteristics: tracer gas concentration decay characteristics, and ventilation effectiveness by calculating actual ventilation air flow rate. The experiments are performed by using a step-down method for measuring tracer gas. $CO_{2}$ gas, concentration in the model chamber. Application of a mixing factor, k, was used and measured values ranged from 0.68 to 0.77. The Type 2 ventilation system was found to have the highest ventilation effectiveness rather than the Types 1 and 3.

• Proceedings of the PSK Conference
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.295.2-296
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• 2002

An organophosphate pesticide terbufos (S-t-butylthiomethyl-O.O-diethyl phosphorodithioate; TBF) has been extensively used as an insecticide. A sexual dimorphism in TBF toxicity was not reported and remains unclear. Objective of the work is to investigate the influence of TBF on sexual dimorphism in rats by using acethlcholinesterase (AchE). (omitted)

• Proceedings of the PSK Conference
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.186.2-187
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• 2003

A sexual dimorphism in terbufos (S-t-butylthiomethyl-O,O-diethyl phosphorodithioate: TBF) toxicity was not reported and remains unclear. Previously. we reported that TBF treatment showed sexual dimorphic effects on acetylcholinesterase (AchE) activity. We further investigated that sexual dimorphism of TBF was affected to age and brain-regional selectivity, and whether ovary plays an important role in the effect. (omitted)

• Proceedings of the PSK Conference
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• 대한약학회 2001년도 Proceedings of the Pharmaceutical Society of Korea
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• pp.206.3-207
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• 2001

• Proceedings of the Korean Society of Toxicology Conference
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• 한국독성학회 2002년도 Current Trends in Toxicological Sciences
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• pp.123-123
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• 2002

Abstract The protective effects of physostigmine against the toxicity of parathion (diethyl-4-nitrophenyl phosphorothionate) were examined in male Sprague-Dawley rats. Physostigmine (100 or 1,000 ㎎/㎏, ip) injected 30 min before decreased the inhibition of acetylcholinesterase (AChE) activities in brain, lung and blood induced by parathion (2 ㎎/㎏, ip).(omitted)

• Proceedings of the PSK Conference
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.255.2-255.2
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• 2002

The present study was designed to investigate the effects of green tea extract (GTE) and epigallocatechin gallate (EGCG) on secretion of catecholamines (CA) in the isolated perfused rat adrenal gland. In the presence of GTE (100 ${\mu}$g/$m\ell$) into an adrenal vein for 60 min. CA secretory responses evoked by ACh (5.32 mM), high K＋ (56 mM) and Bay-K-8644 (10 ${\mu}$M for 4 min) from the isolated perfused rat adrenal glands were greatly inhibited in a time-dependent fashion. (omitted)