• 고려인삼학회:학술대회논문집
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• 고려인삼학회 1990년도 Proceedings of International Symposium on Korean Ginseng, 1990, Seoul, Korea
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• pp.36-44
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• 1990

The analgesic effect of morphine was antagonized and the development of tolerance was suppressed by the modification of the neurologic function in the animals treated with ginseng saponins. The activation of the spinal descending inhibitory systems as well as the supraspinal structures by the administration of morphine was inhibited in the animals treated with ginseng saponins intracerebrally or intrathecally The development of morphine tolerance and dependence, and the abrupt expression of naloxone induced abstinence syndrome were also inhibited by ginsenoside Kbl , Rba, Rgl and Re. These results suggest that ginsenoside Kbl, Rba, Rgl and Re are the bioactive components of panax ginseng on the inhibition of the development of morphine tolerance and dependence, and the inhibition of abrupt abstinence syndrome. In addition, further research on the minor components of Panax ginseng should be investigated. A single or daily treatment with ginseng saponins did not induce any appreciable changes in the brain level of monoamines at the various time intervals and at the various day intervals, respectively The inhibitory or facilitated effects of ginseng saponins on electrically evoked contractions in guinea pig ileum (U-receptor) and mouse was definers (5·receptor) were not mediated through opioid receptors. The antagonism of a x receptor agonist, U-, iO.488H was also not mediated through opioid receptors in the animals treated with ginseng saponins, bolt mediated through serotonergic mechanisms. Ginseng saponins inhibited morphine S-dehydrogenase that catalyzed the production of morphine from morphine, and increased hepatic glutathione contents for the detoxification of morphine. This result suggests that the dual action of the above plays an important role in the inhibition of the development of morphine tolerance and dependence.

• 생약학회지
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• 제30권2호
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• pp.145-150
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• 1999

To explain the theory of KIMI which is the theory of therapeutics in oriental medicine, monoamine oxidase(MAO) activities were measured in the brain and liver of mice which were orally administered oriental medicinal herbs which were classified into cold and hot drugs. Rheum palmatum, Anemarrhena asphodeloides, Gardenia jasminoides, Scutellaria baicalensis and Coptis japonica were considered as the cold drugs and Zingiber officinale, Aconitum carmichaeli, Asiasarum sieboldi, Evodia officinalis and Cinnamomum cassia were included in the hot drugs. The effects of cold and hot drugs on in vitro enzyme activities were measured and compared with the in vivo effects. Serotonin is important neurotransmetter involved in the control of body temperature. The MAO plays a central role in the metabolism of many neurotransmetter monoamines including serotonin. MAO is a flavoprotein found exclusively in the mitochondrial outer membrane, occuring in the MAO-A and MAO-B subtypes. MAO-A deaminates serotonin and noradrenaline, whereas MAO-B prefers phenylethylamine and benzylamine as substrates. Coptis japonica and Aconitum carmichaeli elevated the in vivo MAO activities and especialy, in vivo MAO-B activities were significantly increased. In vitro MAO-A activities were increased by hot drugs, whereas the in vitro MAO-B activities were inhibited. Cold drugs inhibited both enzyme activities in vitro.

• Journal of Applied Biological Chemistry
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• 제61권2호
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• pp.187-190
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• 2018

Two curcumin derivatives, demethoxycurcumin (DMC) and bisdemethoxycurcumin (BDMC), isolated from Curcuma longa were analyzed for their inhibitory activities against two isoforms of monoamine oxidase (MAO), which is involved in the catalysis of neurotransmitting monoamines. In the study, DMC and BDMC potently inhibited human MAO-B, with $IC_{50}$ values of 2.45 and $2.59{\mu}M$, respectively, and both compounds showed effective inhibitory activities against human MAO-A, with $IC_{50}$ values of 3.24 and $3.09{\mu}M$, respectively. The inhibitory activities of the two compounds were higher than those of curcumin. The removal of the methoxy or dimethoxy groups in curcumin might increase the inhibitory activities against human MAO-A and MAO-B. The inhibited activities were recovered to almost the values of the reversible references in the dialysis experiments with DMC and BDMC. DMC and BDMC showed competitive inhibition for MAO-A and MAO-B, respectively, with $K_i$ values of 0.91 and $0.80{\mu}M$, respectively. These results suggest that the two curcumin derivatives may be useful or lead compounds in the treatment of related disorders as potent reversible MAO inhibitors.

• Journal of Microbiology and Biotechnology
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• 제25권9호
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• pp.1425-1428
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• 2015

Monoamine oxidase (MAO) is found in most cell types and catalyzes the oxidation of monoamines. Three anithiactins (A-C, modified 2-phenylthiazoles) isolated from Streptomyces sp. were tested for inhibitory activity of two isoforms, MAO-A and MAO-B. Anithiactin A was effective and selective for the inhibition of MAO-A, with an IC₅₀ value of 13.0 μM; however, it was not effective for the inhibition of MAO-B. Anithiactins B and C were weaker inhibitors for MAO-A and MAO-B. Anithiactin A was a reversible and competitive inhibitor for MAO-A with a K_i value of 1.84 μM. The hydrophobic methyl substituent in anithiactin A may play an important role in the inhibition of MAO-A. It is suggested that anithiactin A is a selective reversible inhibitor for MAO-A, with moderate potency, and can be considered a new potential lead compound for further development of novel reversible inhibitors for MAO-A.

• The Korean Journal of Physiology and Pharmacology
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• 제4권5호
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• pp.347-353
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• 2000

It has been well documented that a massive release of not only glutamate but also other neurotransmitters may modulate the final responses of nerve cells to the ischemic neuronal injury. But there is no information regarding whether the release of monoamines is directly associated with synaptic vesicular proteins under ischemia. In the present study, it was investigated whether synapsin 1, syntaxin and SNAP-25 are involved in the release of 5-hydroxytryptamine $([^3H]5-HT)$ in glucose/oxygen deprived (GOD) rat hippocampal slices. And, the effect of NMDA receptor using DL-2-amino-5-phosphonovaleric acid (APV) on ischemia- induced release of 5-HT and the changes of the above proteins were also investigated. GOD for 20 minutes enhanced release of $[^3H]5-HT,$ which was in part blocked by the NMDA receptor antagonist, APV. The augmented expression of synapsin 1 during GOD for 20 minutes, which was also in part prevented by APV. In contrast, the expression of syntaxin and SNAP-25 were not altered during GOD. These results suggest that ischemic insult induces release of $[^3H]5-HT$ associated with synapsin 1, synaptic vesicular protein, via activation of NMDA receptor in part.

• 대한한의학방제학회지
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• 제17권2호
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• pp.143-150
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• 2009

The effects of aqueous extract of Schizandrae Fructus (AESC) on lead (Pb)-induced changes of monoamine neurotransmitters in the hippocampus (HIP) of adult rats were investigated. Male Sprague-Dawley rats were received intraperitoneal (i.p.) administration of Pb acetate (5 mg/kg/d) for 28 days and sacrificed 7 days after the last administration. Concentrations of norepinephrine (NE), dopamine (DA), serotonin (5-HT), 5-hydroxyindole acetic acid (5-HIAA) in HIP were measured by HPLC. There were significant decreases of NE, DA, 5-HT and 5-HIAA in Pb treated rats (P < 0.05), while pretreatment with AESC (100 mg/kg/d or 300 mg/kg/d, p.o., 2 h before Pb) greatly inhibited the decrease of monoamine transmitters, respectively (P < 0.05). Also, AESC (300 mg/kg/d) significantly increased the reduction of glutathione contents and superoxide dismutase activities in HIP induced by chronic Pb. These results suggest that AESC ameliorates Pb-induced depletion of monoamine neurotransmitters in HIP through its antioxidant activity.

• 한국발생생물학회지:발생과생식
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• 제5권1호
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• pp.9-16
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• 2001

Biogenic amine 류에는 catecholamine, indoleamine 그리고 histamine이 있으며, 동물의 다양한 생리 현상과 행동양식 조절에 중요한 역할을 담당한다. 이중 indoleamine 류인 세로토닌(serotonin혹은 5-hydroxytryptamine, 5-HT)의 경우 최근 들어 그 수용체 아형의 유전자 규명과 발현 조절, 중추신경계 및 표적 기관에서의 역할, 특히 항우울 효과와 같이 행동 및 심리적인 영향 등에 대해 광범위하게 연구되고 있다. 본 논문은 5-HT의 합성 경로, 수용체 아형, 생식과 관련된 기능에 대해 서술하였다. 특히 생식과 관련된 5-HT의 신경내분비학적인 역할로 GnRH-LH-sex steroids 축 조절 기능과 이에 관여하는 수용체 아형들, 생식 조절에 있어서 5-HT 효과의 성적 이형 양상, 중추신경계 이외 기관에서의 역할, 성행동의 조절에 대한 연구 결과들을 요약하였다. 5-HT의 기능에 대한 연구는 특히 현재 주목 받고 있는 '삶의 질' 고양과 밀접하게 연관되어있는 유망한 주제 가운데 하나로 판단된다.

• 대한한의학회지
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• 제24권3호
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• pp.23-34
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• 2003

Objective : In 2001, the rate of obesity in Korea reached 30.6%. There are many therapeutic ways to reduce body weight, such as low and very low calorie diet, exercise therapy, behavior modification therapy, etc. However, in many cases the patients feel stress under obesity treatment because of starvation. This study was aimed to evaluate the anti-starvation stress effect of Coicis Semen on mice. Methods : First, the mice were divided into 6 groups : Normal (group with no starvation), Control (administrated normal saline 6 times before starting 36 hours starvation), and Samples A, B, C, and D (administrated 0.25, 0.5, 1.0, 3.0 g/kg Coicis Semen respectively 6 times before starting 36 hours starvation). Then the plasma corticosterone level and rectal temperature were measured. The norepinephrine, dopamine, DOPAC (dihydroxy-phenylacetic acid), 5-HT (5-hydroxytryptamine) and 5- HIAA (5-hydroxy-indole-acetic acid) in the hypothalamus were measured by the HPLC method. Result : I. The rectal temperature in Sample group D showed a significant difference (P<0.05) compared with the Control group. 2. The DOPAC in Sample groups A, C and D showed the significant difference (P<0.05) compared with the Control group. Conclusion : It might be recognized that Coicis Semen has an anti-starvation stress effect.

• 대한화학회지
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• 제44권5호
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• pp.448-452
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• 2000

포스포리파제 D(PLD)는 인지질의 말단염기를 가수분해하여 phosphatidic acid(PA)와 염기로 분리시키는 효소이다. 본 연구는 쥐의 뇌에서 분리한 미토콘드리아 분획에서 PLD를 활성에 미치는 spermine의 영향을 조사하였다. 올레산 존재하에서 spermine이 PLD를 활성화시켰으며 $Ca^{2+}$, $Mg^{2+}$ 그리고 $Ba^{2+}$는 spermine의 영향을 더욱 강화시켜주는 것으로 나타났다. 다른 아민들은 별 효과가 없었으나 histamine경우 높은 농도에서 PLD를 활성화시켰다. Polylysine들도 PLD를 활성화시켰으며 그 길이가 길수옥 더욱 효과적으로 작용하였다. 기질 특이성에 있어서는 phosphatidylcholine(PC)과 phosphatidylethanolamine(PE) 사이에 큰 차이를 보이지는 않았다. 이 기질 특이성은 쥐 소장 미토콘드리아 PLD의 PE 특이성과 상이한 것으로 나타났다.

• Journal of Microbiology and Biotechnology
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• 제27권2호
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• pp.316-320
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• 2017

Alternariol monomethyl ether (AME), a dibenzopyrone derivative, was isolated from Alternaria brassicae along with altertoxin II (ATX-II). The compounds were tested for the inhibitory activity of monoamine oxidase (MAO), which catalyzes neurotransmitting monoamines. AME was found to be a highly potent and selective inhibitor of human MAO-A with an $IC_{50}$ value of $1.71{\mu}M$; however, it was found to be ineffective for MAO-B inhibition. ATX-II was not effective for the inhibition of either MAO-A or MAO-B. The inhibition of MAO-A using AME was apparently instantaneous. MAO-A activity was almost completely recovered after the dilution of the inhibited enzyme with an excess amount of AME, suggesting AME is a reversible inhibitor. AME showed mixed inhibition for MAO-A in Lineweaver-Burk plots with a $K_i$ value of $0.34{\mu}M$. The findings of this study suggest that microbial metabolites and dibenzopyrone could be potent MAO inhibitors. In addition, AME could be a useful lead compound for developing reversible MAO-A inhibitors to treat depression, Parkinson's disease, and Alzheimer's disease.