• Natural Product Sciences
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• v.22 no.4
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• pp.225-230
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• 2016

Phytochemical investigation from the stem bark of Beilschmiedia pulverulenta resulted in the isolation of five lignans, (+)-yangambin (1), (+)-sesartemin (2), (+)-excelsin (3), (+)-sesamin (4), and (+)-syringaresinol (5), together with lupeol (6), lupenone (7), ${\beta}-sitosterol$ (8), and ${\beta}-sitostenone$ (9). Their structures were established by the analysis of their spectroscopic (1D and 2D NMR) and spectrometric (MS) data, as well as by comparison with those reported in the literature. The isolated lignans were tested for their anticholinesterase (AChE: acetylcholine esterase and BChE: butyryl cholineesterase) and anti-inflammatory (COX-2: cyclooxygenase-2 and LOX: lipoxygenase) activities. All the isolated lignans (1 - 5) exhibited significant inhibition activities in AChE/BChE and COX-2/LOX assays with $IC_{50}$ values ranging from $168.8-504.2{\mu}M$ and $21.0-59.4{\mu}M$, respectively.

• Korean Journal of Pharmacognosy
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• v.48 no.3
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• pp.243-247
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• 2017

To find the anti-Alzheimer's activity of Cacalia hastata var. orientalis (Compositae), caffeoylquinic acids were analyzed in this plant by HPLC and the inhibitory activities of the extract on cholinesterases including acetylcholinesterase (AChE) and butyrylcholinesterse (BChE) and peroxynitrite ($ONOO^-$) were assayed. Sum of caffeoylquinic acids in the 80% MeOH extract was quantitatively higher in leaves (35.8% of the extract) than in stems (3.7%). The compound, 3,5-dicaffeoylquinic acid, was contained in the highest amount in the leaf (44.32 mg/g dry weight). The $IC_{50}s$ of the 80% MeOH extract were shown to be $67.45{\mu}g/ml$ for AChE, and $8.59{\mu}g/ml$ (for $ONOO^-$), respectively, suggesting that the leaves would have the anti-Alzheimer's activity due to the high content of caffeoylquinic acids.

• Environmental Analysis Health and Toxicology
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• v.29
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• pp.1.1-1.7
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• 2014

Objectives The present subacute study was designed to evaluate the effect of coenzyme Q 10 (CoQ10) in the 28 days aroclor 1254 exposure induced oxidative stress in mice brain. Methods Biochemical estimations of brain lipid peroxidation (LPO), reduced glutathione (GSH), and activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx) and acetyl cholinesterase (AChE), and histopathological investigations of brain tissue were carried out. Results Oral exposure of aroclor 1254 (5 mg/kg) led to significant decrease in levels of GSH, and activities of SOD, CAT, GPx, and AChE, and increase in LPO. These aberrations were restored by CoQ10 (10 mg/kg, intraperitoneal injection [IP]). This protection offered was comparable to that of L-deprenyl (1 mg/kg, IP) which served as a reference standard. Conclusions Aroclor 1254 exposure hampers the activities of various antioxidant enzymes and induces oxidative stress in the brains of Swiss albino mice. Supplementation of CoQ10 abrogates these deleterious effects of aroclor 1254. CoQ10 also apparently enhanced acetyl cholinesterase activity which reflects its influence on the cholinergic system.

• The Korean Journal of Physiology and Pharmacology
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• v.15 no.1
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• pp.37-41
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• 2011

Interstitial cells of Cajal (ICC) evoke pacemaker activities in many tissues. The purpose of this study was to investigate the relationship between interstitial cell and pacemaker activity in the human ureter through the recording of spontaneous contractions. Spontaneous contractions of eight circular and longitudinal smooth muscle strips of the human ureter to acetylcholine (ACh) and/or norepinephrine (NE) were observed. Human ureteral strips were divided into proximal and distal groups, and each group was subdivided into circular and longitudinal groups. The proximal group showed spontaneous activities of 3~4 times within 5 minutes in the longitudinal group. ACh ($10^{-4}\;M$) augmented the frequency of the spontaneous contractions. The cumulative application of NE also augmented the frequency in a dose-dependent manner. The effects of NE application were inhibited by concomitant application of $10^{-5}\;M$ glibenclamide. Receptor tyrosine kinase (c-kit) staining revealed abundant ICCs only in proximal tissues. Therefore, spontaneous contractions of the human ureter might be modulated by ICC in the proximal region, and the actions might be related with the activation of cholinergic and/or adrenergic system mediated by a glibenclamide-sensitive pathway.

• The Korean Journal of Physiology and Pharmacology
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• v.18 no.3
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• pp.201-209
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• 2014

The present study was designed to investigate the efficacy of selective $ET_A$ receptor antagonist, ambrisentan on hyperhomocysteinemia-induced experimental vascular dementia. L-methionine was administered for 8 weeks to induce hyperhomocysteinemia and associated vascular dementia in male rats. Ambrisentan was administered to L-methionine-treated effect rats for 4 weeks (starting from $5^{th}$ to $8^{th}$ week of L-methionine treatment). On $52^{nd}$ day onward, the animals were exposed to the Morris water maze (MWM) for testing their learning and memory abilities. Vascular endothelial function, serum nitrite/nitrate levels, brain thiobarbituric acid reactive species (TBARS), brain reduced glutathione (GSH) levels, and brain acetylcholinesterase (AChE) activity were also measured. L-methionine-treated animals showed significant learning and memory impairment, endothelial dysfunction, decrease in/serum nitrite/nitrate and brain GSH levels along with an increase in brain TBARS levels and AChE activity. Ambrisentan significantly improved hyperhomocysteinemia-induced impairment of learning, memory, endothelial dysfunction, and changes in various biochemical parameters. These effects were comparable to that of donepezil serving as positive control. It is concluded that ambrisentan, a selective $ET_A$ receptor antagonist may be considered as a potential pharmacological agent for the management of hyperhomocysteinemia-induced vascular dementia.

• Environmental Analysis Health and Toxicology
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• v.23 no.3
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• pp.171-178
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• 2008

수백여 종의 개별물질이 불완전 연소 혹은 유기물의 열분해로 인해 발생되는 다환방향족 탄화수소(PAHs)는 환경에서 중요한 오염원이 되고 있다. 본 연구는 다양한 바이오마커를 이용하여 수서생태계에 벤조피렌(benzo[a]pyrene)과 같은 다환방향족 탄화수소의 영향을 분석하였고, 이에 대한 통합적 결과 모델을 도출하였다. 즉, 잉어(Cyprinus carpio)를 이용하여 여러 농도의 벤조피렌(3, 12, $34{\mu}g/L$, 측정농도 기준)에 10일간 노출시킨 다음, DNA single-strand break, ethoxyresorufin-O-deethylase (EROD), acetylcholine esterase (AChE)와 vitellogenin (VTG)의 농도를 측정하였다. 벤조피렌은 잉어의 DNA 손상을 유도하였고, 낮은 농도에서 EROD와 VTC의 유의적인 활성을 보였으나, 신경전달물질과 관련이 깊은 AChE 효소활성에는 영향을 미치지 않았다. 이 결과를 star plot를 이용하여 통합 및 분석하였으며, 노출농도에 따른 통합 반응지수(integrated biomarker response value: IBR)로 나타내었다. 이런 다양한 바이오마커의 결과들은 벤조피렌에 대한 어류의 영향과 수생태 모니터링 자료로 이용 가능할 것으로 여겨지며, 통합반응지수는 생태위해성평가에서 유용한 도구로 쓰일 가치가 있는 것으로 평가된다.

• Journal of the Korean Wood Science and Technology
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• v.45 no.6
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• pp.828-835
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• 2017

Airtightness of buildings is one of critical aspects of its energy performance. To build up references of airtightness of wooden houses built in Korea, blower door tests have been carried out in 42 houses since 2006. Causes of air leakage were investigated recently. The average value of air change rate was $3.7h^{-1}$ for light frame house and $5.5h^{-1}$ for post-beam construction at ACH50 (air change per hour at 50 Pa air pressure difference). Foam type insulation was more advantageous in ensuring building airtightness than glass fiber batt. Airtightness of wooden houses which were constructed after 2010 was improved to have less than $1.5h^{-1}$ of ACH50, threshold for application of artificial air change. The average air change rate of CLT (cross laminated timber) houses showed the lowest value, $1.1h^{-1}$, among the tested structures.

• Archives of Pharmacal Research
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• v.28 no.9
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• pp.1092-1096
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• 2005

Huperzine A-loaded microspheres composed of poly(D,L-lactide-co-glycolide) were prepared by an O/w emulsion solvent evaporation method. The characterization of the microspheres such as drug loading, size, shape and release profile was described. The in vitro release in the initial 7 days was nearly linear with $10\%$ released per day. Thereafter drug release rate became slow gradually and about $90\%$ drug released at day 21. The in vitro release rate determined by dialysis bag method had a good correlation with the in vivo release rate. Huperzine A aqueous solution was intramuscularly injected (i.m.) at 0.4mg/kg and microspheres were intra­muscularly injected at 8.4 mg eq huperzine A/kg in rats. The maxium plasma concentration $(C_{max})$ after i.m. microspheres was only $32\%$ of that after i.m. solution. Drug in plasma could be detectd until day 14 and about $5\%$ of administered dose was residued at the injection site at day 14. The relative bioavailability of huperzine A microspheres over a period of 14 days was $94.7\%$. Inhibition of acyecholinesterase activity (AchE) in rat's cortex, hippocampus and striatum could sustain for about 14 days. In conclusion, huperzine A-loaded microspheres possessed a prolonged and complete drug release with significant inhibition of AchE for 2 weeks in rats.

• Proceedings of the Ginseng society Conference
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• 1993.09a
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• pp.36-39
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• 1993

We reported earlier (Br. J. Pharmac. 82. 485 - 491. 1984) that ginsenosides from Panax ginseng CA. Meyer antagonized noradrenaline or prostaglandin $F_{2\alpha}-induced$ contractions of pulmonary and intrapulmonary arterial rings of rabbits. Because this effect resembled that of acetylcholine (ACh). we questioned whether these acitons were due to release of nitric oxide from vaseular endothelium. We therefore determined whether ginsenosides could vasodilate preconstricted lungs and also protect against free radical injury. which normally eliminates the vasodilator response to ACh(J. Appl. Physiol. 71. 821 - 825. 1991 J. We found that ginsenoside $Rg_1$ or a mixture of saponins could ,a) vasodilate perfused. $U_{46619}-preconstricted$ lungs. b) promote increased synthesis of nitric oxide by endothelial cells in culture and c) prevent the pulmonary edema often associated with free radical injury (Biochem. Biophys. Res. Comm. 189. 670 - 676. 1992). Thus, vasodilator and protective effects of ginsenosides against free radical injury may reflect enhanced synthesis and release of nitric oxide. These data suggest that ginsenosides may be useful in treatment of pulmonary and systemic hypertension. Aided by grants from the National Institutes of Health. Bethesda.

• Journal of Physiology & Pathology in Korean Medicine
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• v.30 no.1
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• pp.33-39
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• 2016

Alzheimer's disease(AD), one of the most common forms of dementia, is characterized pathologically by the presence of intracellular neurofibrillary tangles and deposition of β-amyloid(Aβ) peptides of 40-42 residues. Aβ has been believed to be neurotoxic and now is also considered to have a role on the mechanism of memory dysfunction. Only a few acetylcholinesterase(AChE) inhibitors have been developed for treatment of AD, although the numbers of patients are rapidly increasing within aging society. Here, we show that ethanol extract of Rosae Rugosae Flos(RR) or its butanol fraction reduce the enzyme activity of AChE and BACE1(β-site APP cleaving enzyme 1). Furthermore, We found that RR inhibits Aβ aggregation and removes Aβ aggregates by Transmission electron microscopy(TEM). In addition, RR reduces the free radical of 2, 2-diphenyl-1-picrylhydrazyl(DPPH). We suggest that Rosae Rugosae Flos may be useful as a herbal medicine to treat AD.