• Archives of Pharmacal Research
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• v.12 no.1
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• pp.34-38
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• 1989

Papaverine administration produced significant increases in acetylcholinesterase activity in cerebral cortex and striatum of rat brain. Two related compounds, tetrahydropapaverine and tetrahydropapaveroline, also gave similar effects. However, their actions seem to be indirect because papaverine has no in vitro effect on the enzymatic activity.

• The Korean Journal of Physiology
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• v.30 no.2
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• pp.269-278
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• 1996

The mechanism of impaired endothelium-dependent relaxation in the aorta of one-kidney, one clip Goldblatt hypertensive (1K,1C-GBH) rats was investigated. 8 week-old Wistar-Kyoto (WKY) rats were made hypertensive by left renal artery stenosis with contralateral nephrectomy. Endothelium-dependent relaxation was significantly reduced in 1K,1C-GBH rats as compared with WKY rats. However, the relaxation by sodium nitroprusside in 1K,1C-GBH rats was not reduced as compared with WKY rats. The impairment of endothelium-dependent relaxation in 1K,1C-GBH rats was partially restored by the pretreatment of indomethacin or SQ29548. When the nitric oxide production was inhibited by L-nitroarginine methyl ester, acetylcholine (ACh) induced a endothelium-dependent contraction that was greater in 1K,1C-GBH rats than in WKY rats. Endothelium-dependent contraction by ACh was completely abolished by indomethacin or SQ29548. However, imidazole, tranylcypromine and superoxide dismutase did not affect the endothelium-dependent contraction in 1K,1C-GBH rats. These results suggest that impaired endothelium-dependent relaxation in the 1K,1C-GBH rats might be due to the simultaneous release of EDCF, and that prostaglandin B2 may be involved as a mediator of endothelium-dependent contraction.

• Journal of the Korean Chemical Society
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• v.60 no.2
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• pp.125-130
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• 2016

With the goal of developing Alzheimer’s disease therapeutics, we have designed and synthesized new triazole linked decursinol derivatives having potency inhibitory activities against cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)]. Since inhibition of cholinesterase (ChE) is still considered to be one of the most effective targets to treat AD patients, many new classes of ChE inhibitors have been synthesized. In an effort of identifying new type of cholinergic drug, decursinol derivatives 11-17 have been synthesized between decursinol and other biological interesting compounds such as lipoic acid, polyphenols, etc by using the click reaction and then evaluated their biological activities. Compound 12 (IC₅₀ = 5.89 ± 0.31 mM against BuChE) showed more effective inhibitory activity against BuChE than galantamine (IC₅₀ = 9.4 ± 2.5 mM). Decursinol derivatives can be considered a new class inhibitor for BuChE and can be applied to be a novel drug candidate to treat AD patients.

• Bulletin of the Korean Chemical Society
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• v.32 no.spc8
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• pp.2997-3002
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• 2011

A series of hybrid molecules between (R)-lipoic acid (ALA) and the acetylated or methylated polyphenol compounds were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibition activities were checked. The $IC_{50}$ values of all hybrid molecules for a BuChE inhibition were lower than those of the single parent compounds. Specifically, ALA-acetyl protected caffeic acid (11, ALA-AcCA) was shown as an effective inhibitor of BuChE ($IC_{50}=0.5{\pm}0.2\;{\mu}M$) and also had a great selectivity for BuChE over AChE (more than 800 fold). Inhibition kinetic study indicated that 11 is a mixed inhibition type. Its binding affinity ($K_i$) value to BuChE is $1.52{\pm}0.18\;{\mu}M$.

• Environmental Analysis Health and Toxicology
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• v.18 no.2
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• pp.155-163
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• 2003

Fluoranthene, a common polycyclicaromatic hydrocarbon (PAH), exhibits phototoxicity which may affect aquatic organisms. The eventual goal of this study is to develop a biomarker of Japanese medaka (Oryzias latipes) used in monitoring hazardous chemicals in the ecosystem. In this study we investigated neural toxicity of fluoranthene in Japanese medaka (Oryzias latipes) along with comparative analysis of corresponding behavioral response. The untreated individuals shooed normal behavioral characteristics (i. e., smooth and linear movements). The treated fish, however, showed stopping and abrupt change of orientation (100 ppb), and severely reduced locomotive activity and enhanced surfacing activity (1,000 ppb). Treatment of the medaka fish with fluoranthene caused a significant suppresson of acetycholine esterase (AChE) activities in the body portion but not in the head portion. When fish were exposed to 1,000 ppb of fluoranthene for 24 hr, the body AChE activities decreased from 126.${\pm}$31.89 (nmoles substrate hydrolyzed per min per mg protein) to 49.51${\pm}$11.99. Expressions of tyrosine hydroxylase (TH) protein in the different organs from both head and body portions were comparatively analyzed using an immunohistochemical technique. Five organs of the medaka fish showing a strong TH protein expression were the olfactory bulb, hypothalamus, optic lobe, pons and myelencephalon regions. This study provides molecular and neurobehavioral bases of a biomonitoring system for toxic chemicals using fish as a model organism.

• Proceedings of the Korean Environmental Sciences Society Conference
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• 2003.05a
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• pp.155-160
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• 2003

Indoor air quality can be affected by indoor sources, ventilation, decay and outdoor levels. Although technologies exist to measure these factors, direct measurements are often difficult. The purpose of this study was to develop an alternative method to characterize indoor environmental factors by multiple indoor and outdoor measurements. Daily indoor and outdoor $NO_2$ concentrations were measured for 30 consecutive days in 28 houses in Brisbane, Australia, and for 21 consecutive days in 37 houses in Seoul, Korea. Using a mass balance model and regression analysis, penetration factor (ventilation rate divided by the sum of ventilation rate and deposition constant) and source strength factor (source strength divided by the sum of ventilation rate and deposition constant) were calculated using multiple indoor and outdoor measurements. Subsequently, the ventilation rate and $NO_2$ source strength were estimated. Geometric means of ventilation rate were 1.44 ACH in Brisbane, assuming a residential $NO_2$ deposition constant of 1.05 $hr^{-1}$, and 1.36 ACH in Seoul, with the measured residential $NO_2$ deposition constant of 0.94 $hr^{-1}$. Source strengths of $NO_2$ were 15.8 $\pm$ 18.2 ${\mu}g$/$m^3$.hr and 44.7 $\pm$ 38.1${\mu}g$/$m^3$.hr in Brisbane and Seoul, respectively. In conclusion, indoor environmental factors were effectively characterized by this method using multiple indoor and outdoor measurements.

• The Journal of Internal Korean Medicine
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• v.27 no.1
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• pp.92-101
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• 2006

Objectives : This study was done with intend to investigate whether two oriental medical prescriptions, daecheongryong-tang (DCRT) and prescription A (P-A) significantly affect mucin release from cultured hamster tracheal surface epithelial (HTSE) cells. Methods : Confluent HTSE cells were metabolically radiolabeled with $^3H$-glucosamine for 24 hrs and chased for 30 min in the presence of DCRT or P-A to assess the effect of each agent on $^3H$-mucin release. Possible cytotoxicities of each agent were assessed by measuring lactate dehydrogenase (LDH) release. Also, the effects of DCRT and P-A on contractility of isolated tracheal smooth muscle were investigated. Results were as follows : 1. DCRT significantly inhibited mucin release from cultured HTSE cells, with significant cytotoxicity. 2. P-A significantly increased mucin release from cultured HTSE cells, with significant cytotoxicity. 3. DCRT inhibited Ach-induced contraction of isolated tracheal smooth muscle. 4. P-A also inhibited Ach-induced contraction of isolated tracheal smooth muscle. Conclusion: Results suggest that DCRT and P-A have regulating effects on mucin secretion from goblet cells. Further investigation is needed, because of the value in finding novel agents to this purpose, and these oriental medical prescriptions have potential for this role.

• Journal of Physiology & Pathology in Korean Medicine
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• v.16 no.2
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• pp.279-288
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• 2002

This research investigates the effect of the Crataegus pinnatifida BGE. var. major N.E. BR(CPVM) on Alzheimer's disease. The CPVM extract suppressed the expression of IL-1 β, IL-6, APP, AChE mRNA in PC-12 cells treated with CT105. The CPVM extract suppressed the AChE activity, and the production of APP significantly in PC-12 cells treated with CT105. The CPVM extract group showed a significant inhibitory effect on the memory deficit for the mice with Alzheimer's disease induced by CT105 in the Morris water maze experiment. The CPVM extract suppressed the over-expression of IL-1 β, TNF- α and ROS in the mice with Alzheimer's disease induced by CT105. This study suggests that CPVM may be effective for the prevention and treatment of Alzheimer's disease.

• Journal of Nutrition and Health
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• v.29 no.1
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• pp.32-40
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• 1996

To investigate the effect of dietary docosahexaenoic acid(DHA) and environmental enrichment on brain fatty acid composition and acetylcholinesterase(AChE) activity, two groups of was fed isocaloric diets containing 10 or 12% dietary lipids for 7 weeks. A third group was fed 10% (w/w) dietary lipids with supplemented 2% DHA-rich fish oil. Each diet group was housed either in a stainless steel cage individually or in a large enriched cage with toys where 7 rats were kept together. The fatty acid composition of plasma and brain was significantly affected by dietary lipid composition but not by environmental enrichment. Fish oil supplementation significanlty decreased plasma levels of monounsaturated fatty acids(MUFA) and increased polyunsaturated fatty acids(PUFA). Fish oil supplemented groups also maintained lower plasma n-6 fatty acids and higher n-3 fatty acids levels than unsupplemented groups. The fish oil supplementation significantly decreased arachidonic acid and increased eicosapentaenic, docosapentaenoic acids, and DHA in brain fatty acid composition. In addition, brain DHA level in supplemented groups tended higher than the unsupplemented. Brain, AChE activity significantly increased by the environmental enrichment but not by the fish oil supplementation. These finding suggest that the 2% fish oil (0.57% DHA & 0.31% EPA, per diet weigth) supplementation is enough to accumulate n-3 fatty acids and to change the n-6 n-3 ratio in brain and environmental enrichment might promote the learning ability.

• Biomolecules & Therapeutics
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• v.11 no.1
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• pp.33-40
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• 2003

The present study was designed to investigate the effects of green tea extract (CUMC6335) and epigallocatechin gallate (EGCG) on secretion of catecholamines (CA) in the isolated perfused rat adrenal gland. ill the presence of CUMC6335 (100 $\mu\textrm{g}$/mL) 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. However, EGCG (8 $\mu\textrm{g}$/mL) did not affect CA release evoked by ACh, high $K^+$ and Bay-K-8644. CUMC6335 itself did fail to affect basal catecholamine output. Taken together, these results demonstrate that CUMC6335 inhibits greatly CA secretion evoked by stimulation of cholinergic nicotinic receptors as well as by the direct membrane deplarization from the isolated perfused rat adrenal gland. It is felt that this inhibitory effect of CUMC6335 may be due to blocking action of the L-type dihydropyridine calcium channels in the rat adrenal medullary chromaffin cells, which is relevant to the cholinergic nicotinic blockade. It seems that there is a big difference in mode of action between CUMC6335 and EGCG.