• Radiation Oncology Journal
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• 제11권2호
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• pp.205-217
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• 1993

In order to evalute the effects of radiation on mammalian neuronal system, we have examined the effect of gamma-ray radiation on the monoamine oxidase (MAO) activity in monoaminergic neurons. Following the whole body irradiation, MAO activity in the rat brain was measured as well as in the liver for the comparative studies between the neuronal and nonneuronal system. The effects of some radiation protectors and sensitizers were also examined in addition to the $O_2$ effect. The results can be summarized as follows. 1) The MAO activity of rat brain was minimally affected by the radiation dose up to 1,700 cGy Radiation dose above 2,500 cGy inhibited the brain MAO activity by no less than $l0\%.$ MAO-A form was found to be particularly sensitive to radiation. The liver MAO was somewhat inhibited (by about $5\%$) but hardly dependent on the dose of radiation. 2) The inhibitory effect on the brain was initiated immediately by the radiation dose of 2,500 cGy. On the contrary, for the liver, the inhibitory effect became apparent only 2 days after irradiation. 3) Two days after a dose of 2,500 cGy, Vmax and Km of the brain mitochondrial MAO decreased. For liver, Vmax decreased while Km increased, which indicates the kinetic patterns for the neuronal and nonneruronal systems are not affected similarly by radiation. 4) The effect of several known radiation protectors and sensitizers on MAO activity was tested ut no definite results were obtained. The level of -SH group increased in some degree upon radiation but not by the compounds. 5) MAO activity was not affected by $O_2$ concentration, while an elevated level of lipid peroxidase was found under the same condition. The results described here indicate that characteristics of MAO, one of the most important central nervous system enzymes, are liable to radiation, which is partially differentiated from the liver MAO. Also indicated are that the -SH groups are hardly related to the effect of radiation but the production of the lipid peroxide seems to be somewhat correlated to the effect of radiation.

• 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.256.1-256.1
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• 2003

As a part of our ongoing research to discover novel monamine oxidase (MAO) inhibitors of plant origin, we found that a MeOH extract from the whole plant of Cayratia japonica (Vitaceae) strongly inhibited the MAO activity in mouse brain. The EtOAc-soluble fraction was. therefore, subjected to the bioactivity-guided fractionations to isolate the active compounds. (omitted)

• Natural Product Sciences
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• 제6권1호
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• pp.16-19
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• 2000

Four compounds were isolated from the dichloromethane fraction of Cinnamomi Cortex through bioassay-guided isolation. Their structures were identified as coumarin (1), 3,3-dimethoxy-1-propenyl benzene (2), cinnamic acid (3) and o-methoxy cinnamaldehyde (4) on the basis of spectroscopic data. All four compounds showed inhibitory activities in vitro against monoamine oxidase (MAO) prepared by mouse brain. The $IC_{50}$ values were $41.4\;{\mu}M\;(1),\;110.6\;{\mu}M\;(2),\;252.5\;{\mu}M\;(3)\;and\;83.1\;{\mu}M$ (4), respectively.

• Archives of Pharmacal Research
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• 제10권2호
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• pp.142-147
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• 1987

Fourteen kinds of medicinal plants were screened for determining inhibitory activities on monoamine oxidase B. The extracts of Artemisia Messer-Schmidtiana (herba), Chrysanthemum indicum(flos), Ericibe obtusifolia (radix et rhizoma) and Sophora japonica (flos) strongly inhibited the enzyme. Among them, Chrysanthemi flos was chosen for elucidating its active principles, and some flavonoids were isolated and identified as acasetin (I), 5, 7-dihydroxy chromone (II), diosmetin (III), apigenin (IV), eriodictyol (V) and luteolin (VI).$IC_{50} were determined as following: 1, 2.46;II, 0.19; III, 2. 11mM, and the others showed weak inhibition.

• 생약학회지
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• 제33권4호통권131호
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• pp.285-290
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• 2002

From the fruits of Crataegus pinnatifide BUNGE ursolic acid (1), $quercetin-3-O-{\alpha}-L-rhamnopyranosyl(1{\rightarrow}6)-{\beta}-D-glucopyranoside$ (2), (-)-epicatechin (3), $quercetin-3-O-{\beta}-D-galactopyranoside$ (4) and quercetin (5) have been isolated and identified on the basis of their physicochemical properties and spectroscopic evidences in comparison with authentic samples. Among isolated compounds, quercetin showed significant inhibitory effect against MAO.

• Natural Product Sciences
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• 제8권1호
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• pp.30-33
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• 2002

From the bioassay-directed fractionation and isolation of dichloromethane fraction of Aquilaria agallocha, four compounds having MAO inhibitory effect were isolated by repeated silica gel column chromatography. Their chemical structures were established as psoralen (1), bergapten (2), ${\alpha}-amyrin\;acetate$ (3) and 5-hydroxymethylfurfural (4) on the basis of their physicochemical and spectral data. Among these compounds, psoralen and bergapten showed high inhibitory activities in vitro against mouse brain MAO with $IC_{50}$ values $21.3\;{\mu}M\;and\;13.8\;{\mu}M$, respectively.

• 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.255.2-255.2
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• 2003

Monoamine oxidase (MAO) is flavin-containing enzyme that catalyzes the oxidation of variety of amine-containing neurotransmitters such as catecholamines and serotonin to yield the corresponding aldehyde. Thus, MAO activity might play important roles in some pathological states of central nervous system diseases such as depression, alcoholism, and schizophrenia. (omitted)

• Journal of Microbiology and Biotechnology
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• 제31권7호
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• pp.1022-1027
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• 2021

Three compounds were isolated from marine-derived Streptomyces sp. CNQ-031, and their inhibitory activities against monoamine oxidases (MAOs), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-secretase (BACE-1) were evaluated. Compound 1 (5,7-dihydroxy-2-isopropyl-4H-chromen-4-one) was a potent and selective inhibitor of MAO-A, with a 50% inhibitory concentration (IC₅₀) of 2.70 µM and a selectivity index (SI) of 10.0 versus MAO-B. Compound 2 [5,7-dihydroxy-2-(1-methylpropyl)-4H-chromen-4-one] was a potent and low-selective inhibitor of MAO-B, with an IC₅₀ of 3.42 µM and an SI value of 2.02 versus MAO-A. Compound 3 (1-methoxyphenazine) did not inhibit MAO-A or MAO-B. All three compounds showed little inhibitory activity against AChE, BChE, and BACE-1. The K_i value of compound 1 for MAO-A was 0.94 ± 0.28 µM, and the K_i values of compound 2 for MAO-A and MAO-B were 3.57 ± 0.60 and 1.89 ± 0.014 µM, respectively, with competitive inhibition. The 1-methylpropyl group in compound 2 increased the MAO-B inhibitory activity compared with the isopropyl group in compound 1. Inhibition of MAO-A and MAO-B by compounds 1 and 2 was recovered by dialysis experiments. These results suggest that compounds 1 and 2 are reversible, competitive inhibitors of MAOs and can be considered potential therapies for neurological disorders such as depression and Alzheimer's disease.

• Archives of Pharmacal Research
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• 제10권1호
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• pp.50-59
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• 1987

(E)-2-Phenylcyclopropylamine ((E)-TCP), (Z)-2-Phenylacyclopropylamine ((Z)-TCP), (E)-1-methyl-2-phenylcyclopropylamine ((E)-MTCP), and (Z)-1-methyl-2-phenylcyclopropylamine ((Z)-MTCP) were synthesized and used to determine to what extent 1-methylsubstitution and stereochemistry of 2-phenycyclopropylamines affect inhibition of monoamine oxidase (MAO). Inhibition of rat brain mitochondrial MAO-A and B by the compounds were measured using serotonin and benzylamine as the substrate, respectively and $IC_{50}$ values obtianed with 95% confidence limits by the method of computation. For the inhibition of MAO-A, (E)-MTPC ($IC_{50}$ = 6.2 * $10^{-8}$M) was found to be 37 times more potent than (Z)-MTCP ($IC_{50}$ = 7.8 * $10^{-8}$M), was 7 times more potent than (Z)-MTCP($IC_{50}$= 4.7 * $10^{-7}$M) and (E)-TCP($IC_{50}$ =7.8 * $10^{-8}$M),0.6 times as potent as (Z)- TCP ($IC_{50}$ = 4.4 * $10^{-8}$M). The results suggested that while without 1-methyl group, potency of a (Z)-isomer was comparable to that of (E)-isomer, the methyl group in its (Z)-position was very unfavorable to the inhibition of MAO and that in its (E)-position, the methyl group contributed positively to the potency as found by the fact that (E)-MTCP was 1-5 times more potent than (E)-TCP. In view of the selective inhibition of MAO-A- or B over MAO-A and 1-methyl substitution as well as the stereochemical factors did not significantly influence the selectivity.

• 한국산업보건학회지
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• 제21권2호
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• pp.116-122
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• 2011

Human occupational exposure to n-hexane has been associated with neurobehavioral symptoms such as depression, irritablity, acute irritation symptom, concentration disturbance and fatigue. Effects of monoamine oxidase (MAO) B and serotonin transporter receptor (5-HTTR) polymorphisms on the neurobehavioral symptoms were investigated in 70 male workers from TV and computer monitor manufacturing plants exposed to n-hexane. Neurobehavioral symptoms were assessed through a self-reported questionnaire and ambient level of n-hexane was measured by NIOSH method. Blood and urine were collected from each workers to determine the MAO(B), 5-HTTR and urinary 2,5-hexanedione(2,5-HD). The mean concentration of volatile n-hexane was $18.8{\pm}28.8ppm$ and that of urinary 2,5-HD was $1.07{\pm}1.47mg/g$ creatinine. Statistically significant associations with sexual disturbance were age and smoking. The frequencies of MAO(B) AA, AG and GG were 18.6%, 45.7% and 35.7%, respectively, and the frequencies of 5-HTTR ll, ls and ss genotype were 82.9%, 15.7% and 1.4%, respectively. MAO (B) gene polymorphisms had susceptibility to the neurobehavioral symptoms such as fatigue, concentration disturbance, irritability and acute irritation symptom and 5-HTTR gene polymorphism had susceptibility to the sleep disturbance and acute irritation symptom. On multiple logistic regression analysis for the neurobehavioral symptoms, memory disturbance was significantly associated with smoking(OR=6.752, 95% CI=37.46) and drinking(OR=4.033, 95% CI=1.252-12.98), emotional lability was MAO(B) genotype(OR=0.412, 95% CI=0.170-0.996), fatigue (OR=1.011, 95% CI=1.000-1.021) and acute irritation(OR=0.990, 95% CI=0.981-1.000) were working duration and sexual disturbance were significantly associated with age(OR=1.208, 95% CI=1.042-1.399), ambient n-hexane(OR=1.077, 95% CI=1.005-1.154) and 2,5-HD(OR=0.186, 95% CI=0.041-0.841). This finding implies that the MAO (B) and 5-HTTR polymorphisms may affect susceptibility for specific neurobehavioral symptoms associated with n-hexane exposure in workers.