• Journal of Yeungnam Medical Science
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• 제16권2호
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• pp.318-325
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• 1999

항콜린에스테라제 약물은 AChE를 억제하여 ACh을 콜린성 수용체에 축적시켜 지속적인 ACh 자극을 유도하는 약물이다. 이러한 특성이 적출한 위장의 운동성에 미치는 영향과 콜린에스테라제 활성화 약물의 영향을 조사하고, 에탄올이 AChE의 활성도를 감소시키는 보고를 바탕으로 항콜린에스테라제와 에탄올의 동시 투여시 나타나는 위장관의 수축운동의 변화를 규명하고자 다음과 같은 실험을 수행하였다. 흰쥐의 위장을 적출하여 $2{\times}10mm$ 환상근 절편을 만들어 적출근편 실험조에 고정하고 등척성 장력측정기를 이용하여 약물 처치에 따른 위장 절편의 수축 변화를 측정하였다. 비가역성 항콜린에스테라제인 fenthion은 ACh 유발 위장 절편의 수축을 증가시켰으며 콜린에스테라제 활성화 약물인 PAM은 이 작용을 길항하였다. 가역성 항콜린에스테라제인 physostigmine은 그 자체로 인해 위장 절편의 수축이 증가하였는데, 이는 비극성을 나타내어 위장 절편 조직으로의 흡수가 빠르기 때문이라고 생각되고, ACh에 의한 반응성 또한 현저히 증가하였다. PAM에 의한 반응성 감소효과도 대조군과 통계적으로 유의한 차이를 보였다. 최근 평활근 이완을 유도한다고 알려진 에탄올은 fenthion 처치에 의한 수축운동 증가를 억제하였고 이러한 결과로 볼 때 항콜린에스테라제와 에탄올의 동시 투여시에는 콜린에스테라제 활성도 감소보다 에탄올에 의한 위장관 운동성 감소가 많이 작용함을 의미하였다. 이상의 결론은 가역성 및 비가역성 항콜린에스테라제에 의해서 위장관 운동성 항진이 나타나고 이는 콜린에스테라제의 활성화 약물로서 길항되었다. 그리고 에탄올과 항콜린에스테라제에 동시에 노출된 경우는 에탄올의 평활근 이완 효과에 의해 위장관 운동성 감소가 나타남을 알 수 있었다.

• 셀메드
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• 제4권2호
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• pp.11.1-11.6
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• 2014

Cinnamomum zeylanicum (C. zeylanicum) is a tropical evergreen tree of Lauraceae family. It is one of the oldest culinary spices known and used traditionally in many cultures for centuries. In addition to its culinary uses, cinnamon also possesses as a folk remedy of many health disease condition including analgesic, antiseptic, antispasmodic, aphrodisiac, astringent, carminative, haemostatic, insecticidal, and parasiticide and memory enhancing property. This study was aimed to assess the acetylcholinesterase and butyrylcholinesterase inhibitory activity of standardized methanol extract of the C. zeylanicum. Gas chromatography - mass spectrometry (GC-MS) and high performance liquid chromatography (HPLC) analysis were done to identify the presence of eugenol as chemical component and support the neuroprotective activity in the extract. Anticholinesterase inhibitory activity of crude methanol extract of C. zeylanicum leaves and cinnamon oil were evaluated by 96-well microtiter plate assay and thin layer chromatography bioassay detection methods. This study revealed that cinnamon oil ($IC_{50}:45.88{\pm}1.94{\mu}g/ml$) has better anticholinesterase activity than methanol extract ($IC_{50}:77.78{\pm}0.03{\mu}g/ml$). In HPLC analysis, retention time of eugenol in cinnamon oil was found to be 15.81 min which was comparable with the retention time (15.99 min) of the reference standard, eugenol. Seven chemical compounds were identified by GC-MS analysis, in which eugenol as an important phytoconstituents. Thus the phytochemicals from C. zeylanicum methanol leaves extract could be developed as potential source of anticholinesterase activity, with particular benefit in the symptomatic treatment of Alzheimer's disease.

• Natural Product Sciences
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• 제22권4호
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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.

• 한국임상수의학회지
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• 제29권1호
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• pp.107-111
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• 2012

Three dogs (An 8 years-old intact female Poodle, a 7 years-old intact male Schunauzer, and an 8 yearsold Golden Retriever) were presented due to acute vomiting, dyspnea, and generalized weakness. Megaesophagus was confirmed through radiographic examination in all 3 dogs. Relative oesophageal diameter (ROD) was measured and results of ROD measurements showed the possibility of megaesophagus secondary to myasthenia gravis in three dogs. Thus we performed anticholinesterase test as screening test for myasthenia gravis. In all three dogs, esophageal diameter was reduced after neostigmine methylsulfate administration. For definite diagnosis of acquired myasthenia gravis, serum acetylcholine receptor antibody titer was measured, but definite diagnosis was confirmed only in one case. However, based on history, radiographic findings, anticholinesterase test, ROD measurement, other two cases were still suspected as megaesophagus secondary to myasthenia gravis. Treatment with pyridostigmine bromide was initiated in all dogs, and improvement of esophageal diameter was shown in all dogs. One dog was successfully managed for 15 months after initial treatment and, is still alive, but other two dogs were died shortly after initial treatment, because of severe aspiration pneumonia.

• 대한임상독성학회지
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• 제15권1호
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• pp.56-59
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• 2017

Pneumatosis cystoides intestinalis and portomesenteric venous gas are uncommon radiological findings, but are found commonly in cases of bowel ischemia, or as a result of various non-ischemic conditions. A 72-year-old man visited an emergency center with altered mental status 2 hours after ingestion of an unknown pesticide. On physical examination, he showed the characteristic hydrocarbon or garlic-like odor, miotic pupils with no response to light, rhinorrhea, shallow respiration, bronchorrhea, and sweating over his face, chest and abdomen. Laboratory results revealed decreased serum cholinesterase, as well as elevated amylase and lipase level. We made the clinical diagnosis of organophosphate poisoning in this patient based on the clinical features, duration of symptoms and signs, and level of serum cholinesterase. Activated charcoal, fluid, and antidotes were administered after gastric lavage. A computerized tomography scan of the abdomen with intravenous contrast showed acute pancreatitis, poor enhancement of the small bowel, pneumatosis cystoides intestinalis, portomesenteric venous gas and ascites. Emergent laparotomy could not be performed because of his poor physical condition and refusal of treatment by his family. The possible mechanisms were believed to be direct intestinal mucosal damage by pancreatic enzymes and secondary mucosal disruption due to bowel ischemia caused by shock and the use of inotropics. Physicians should be warned about the possibility of pneumatosis cystoides intestinalis and portomesenteric venous gas as a complication of pancreatitis following anticholinesterase poisoning.

• Asian Pacific Journal of Cancer Prevention
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• 제16권7호
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• pp.2763-2769
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• 2015

Background: Cancer is an unnatural type of tissue growth in which the cells exhibit unrestrained division, leading to a progressive increase in the number of dividing cells. It is now the second largest cause of death in the world. The present study concerned antioxidant, anticancer and anticholinesterase activities and protocatechuic, catechin, caffeic acid, syringic acid, p-coumaric acid and o-coumaric concentrations in methanol extracts of flowers, fruits and seeds of Hypericum amblysepalum. Materials and Methods: Antioxidant properties including free radical scavenging activity and reducing power, and amounts of total phenolic compounds were evaluated using different tests. Protocatechuic, catechin, caffeic acid, syringic acid, p-coumaric acid and o-coumaric concentrations in extracts were determined by HPLC. Cytotoxic effects were determined using the MTT test with human cervix cancer (HeLa) and rat kidney epithelium cell (NRK-52E) lines. Acetyl and butyrylcholinesterase inhibitory activities were measured by by Ellman method. Results: Total phenolic content of H. amblysepalum seeds was found to be higher than in fruit and flower extracts. DPPH free radical scavenging activity of the obtained extracts gave satisfactory results versus butylated hydroxyanisole and butylated hydroxytoluene as controls. Reducing power activity was linearly proportional to the studied concentration range: $10-500{\mu}g/mL\;LC_{50}$ values for H. amblysepalum seeds were 11.7 and 2.86 respectively for HeLa and NRK-52E cell lines. Butyryl-cholinesterase inhibitory activity was $76.9{\pm}0.41$ for seed extract and higher than with other extracts. Conclusions: The present results suggested that H. amblysepalum could be a potential candidate anti-cancer drug for the treatment of human cervical cancer, and good source of natural antioxidants.

• Preventive Nutrition and Food Science
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• 제22권2호
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• pp.107-117
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• 2017

The purpose of this study was to evaluate the antioxidant and anticholinesterase activities of yellow and white bitter yams from South Western Nigeria using methanolic extraction and simulated gastrointestinal digestion models. The phenolic compounds in the bitter yam varieties were evaluated by high performance liquid chromatography with a diode array detector (HPLC-DAD). The total phenolic content of the bitter yams was measured by the Folin-Ciocalteu method, reductive potential by assessing the ability of the bitter yam to reduce $FeCl_3$ solution, and the antioxidant activities were determined by the 2,2-diphenyl-1-picrylhydrazyl radical ($DPPH^{\cdot}$) scavenging activity, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical cation ($ABTS^{{\cdot}+}$) scavenging activity, nitric oxide radical ($NO^{\cdot}$) scavenging ability, hydroxyl radical scavenging ability, and ability to inhibit $Fe^{2+}$-induced lipid oxidation. The HPLC-DAD analysis revealed the presence of some phenolic compounds in the studied bitter yam varieties, with varying degree of quantitative changes after cooking. The antioxidant indices (total phenolic content, total flavonoid content, reducing power, $DPPH^{\cdot}$ scavenging activity, $ABTS^{{\cdot}+}$ scavenging activity, and $NO^{\cdot}$ scavenging activity) were higher in the simulated gastrointestinal digestion model compared to the methanolic extract, with the in vitro digested cooked white bitter yam ranking higher. Similarly, the in vitro digested yams had a higher inhibitory action against lipid oxidation compared to the methanolic extracts, with the cooked white bitter yam ranking high. The methanolic extracts and in vitro enzyme digests showed no acetylcholinesterase inhibitory abilities, while methanolic extracts and the in vitro enzyme digest displayed some level of butyrylcholinesterase inhibitory activities. Therefore the studied bitter yams could be considered as possible health supplements.

• Journal of Yeungnam Medical Science
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• 제16권2호
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• pp.326-332
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• 1999

이 연구에서는 유기인제 농약으로 인한 acetylcholinesterase와 pseudolcholinesterase의 활성도 변화와 알콜과 유기인제 농약의 상호 작용시 효소 활성도 변화를 비교하고, 임상적으로 쓰이고 있는 가역성 항콜린에스터라제 약물과도 비교하여 여러 항콜린에스터라제 약물의 효능과 알콜 섭취가 콜린에스터라제 활성도에 미치는 영향을 파악하는 것에 이 실험의 목적을 두었다. 남자 대학생 15명을 무작위 추출하여 상박부 정맥에서 채혈하여 혈액중 적혈구내에 존재하는 acetylcholinesterase와 혈장에 존재하는 acetylcholinesterase를 분리하였고 cholinesterase가 acetylcholine을 acetic acid와 choline으로 가수분해한다는 점을 이용하여 각 효소에 acetylcholine을 기질로서 주입한 후 1시간 후 생성된 acetic acid에 의해 변화된 pH를 pH meter로 측정하여 간접적으로 활성도를 알아내는 electrometric method를 이용하여 활성도 변화를 측정하였다. 위 실험 조건에서 가역성 항콜린에스터라제 약물이 유기인제 농약보다 콜린에스터라제 활성도를 감소시켰고, 유기인제로 인한 acetylcholinesterase와 pseudocholinesterase의 활성도 변화는 에탄올 처치시 더욱 현저하게 감소되는 것으로 나타났으며, 콜린에스터라제 활성제인 oxime은 acetylcholinesterase에 대해서는 효소 활성도를 높이지만 pseudocholinesterase의 효소 활성도에는 영향을 미치지 않는 것으로 나타났다.

• 셀메드
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• 제2권2호
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• pp.19.1-19.6
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• 2012

$Capparis$ $zeylanica$ Linn. a 'Rasayana' drug is used for its memory enhancing effects in the traditional Ayurvedic system of medicine. The aim of this study was to evaluate acetylcholinesterase (AChE) inhibitory and memory enhancing activities of $Capparis$ $zeylanica$ Linn. The$in-vitro$ and $ex-vivo$ models of AChE inhibitory activity were used along with Morris water maze test to study the effect on memory in rats. The anticholinesterase effect of methanolic and aqueous extracts of $Capparis$ $zeylanica$ was measured by spectrophotometric Ellman method at 0.1, 0.3, 1.0, 3.0, 10 and 30 mg/ml and brain monoamine oxidase (MAO-A and MAO-B) activity was assessed by Naoi's method. The results $in-vitro$ and $ex-vivo$ AChE assay revealed that methanolic and aqueous extracts of $Capparis$ $zeylanica$ inhibit AChE activity, whereas these extracts did not alter MAO activity at any concentration tested as compared to moclobemide and L-deprenyl. The results indicate that $Capparis$ $zeylanica$ improves scopolamine-induced memory deficits through inhibition of AChE activity, and not by direct MAO inhibition.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.248.3-249
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• 2003

A series of tetrahydroaminoacridine and their analogues were synthesized. Tetrahydroaminoacridine(tacrine) is an anticholinesterase agent used in the treatment of Alzheimer's disease. Introduction of piperidine group at the para position enhanced anti-inflamatory activity for Alzheimer's disease. We investigated their ability to inhibit cyclooxygenase-1 and 2 isoforms. (omitted)