• 한국식품과학회지
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• 제37권1호
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• pp.95-102
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• 2005

상심자 추출물이 운동에 의한 체내 monoamine oxidase (MAO) 활성 변화에 미치는 영향을 연구하여. 상심자 추출물을 경구투여(0.3g/kg body weight) 한 흰쥐의 뇌와 간에서 MAO-A와 MAO-B의 활성에 중요한 영향을 미치는 사실을 확인하였다. 각 효소활성은 serotonin과 benzylamine을 기질로 이용하여 측정하였다. 운동 전 후 운동의 유형에 따라 효소활성의 변화경향이 서로 다른 경향을 나타내었다. 뇌에서 측정한 MAO-A 활성은 운동에 의해 효소활성이 현저히 감소하였으며 반면, 간에서 측정한 MAO-B의 활성은 운동이 끝나고 60분이 경과할 때까지 증가된 상태를 유지하고 있었다. 운동 시 체내 변화의 지표효소인 혈중 LDH의 활성 변화와 혈중 lactate의 농도변화를 함께 관찰함으로서 MAO 활성과의 상관관계를 비교하였다. 상심자 추출물을 경구투여 하고 운동을 한 동물의 MAO-A 활성은 증가하였고 MAO-B, LDH 활성과 lactate level은 감소하는 것을 확인하였다. 결과적으로 모은 지표들이 운동 전의 정상상태로 회복되는 것으로 확인되었다. 이 연구의 결과들로부터 상심자 추출물이 운동 전후의 MAO 활성을 조절함으로써 운동능력을 향상시키고 피로를 회복하는 효능을 갖는 것으로 추정되며 이러한 기능성을 갖는 건강기능식품의 소재로 활용이 가능할 것으로 생각한다.

• 생약학회지
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• 제38권2호통권149호
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• pp.108-112
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• 2007

We examined the inhibitory activities against monoamine oxidase (MAO) of Gardenia jasminoides in vitro and in vivo methods. Methanolic extract and ethylacetate fraction of Gardenia jasminoides fruit showed a significant inhibitory activity on MAO-A and MAO-B in vitro. The IC$_{50}$ values of each fraction on MAO-A and MAO-B are as fo11owed; total methanol extracts 1.23 and 1.34 mg/ml, EtOAc fraction 0.72 and 0.77 mg/ml. Water-soluble fraction also showed IC$_{50}$ values of 0.81 mg/ml on MAO-B. MAO-A activity was increased by the oral administration of ethanolic extract of G. jasminoides, while MAO-B activity was decreased. The concentration of serotonin of brain tissue administrated of ethanolic extract of G. jasminoides is slightly increased in rat. This tendency is not different from the activity of deprenyl which is a well known MAO inhibitor was used as a positive control. Consequently, we suggest that G. jasminoides may have the effects on the inhibitory activity against MAO This activity of G. jasminoides is considerable for development of functional materials for treatment and control of depression, dementia, Parkinson' disease, stress and promoting exercise, etc.

• 대한약리학회지
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• 제25권1호
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• pp.87-91
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• 1989

본 실험에서는 ethanol 및 acetaldehyde가 유도하는 MAO 활성변동에 인삼 butanol 분획이 미치는 영향을 검토하였다. Ethanol(1 g/kg)을 mouse 복강내로 투여하였을 때 간장 중 MAO 활성이 현저히 증가하였으며 이러한 작용은 인삼butanol 분획 전처리로 개선되었다. 또한 pyrazole(200mg/kg)을 전처리하였을 때 ethanol에 의해 증가된 간장중 MAO활성이 정상수준으로 감소되었다. 만성적으로 ethanol을 투여한 경우에 있어서도 MAO활성이 증가되었으며 인삼 butaonl분획 전처리로 MAO 활성이 감소됨이 관찰되었다. Ethanol의 대사산물인 acetaldehyde(100mg/kg)을 복강내로 투여하고 관찰한 실험에서도 간장중 MAO활성이 현저하게 증가되었으며 인삼 butanol분획을 전처리함으로써 정상수준 가깝게 MAO활성이 감소되었다. 이 연구결과로 ethanol에 의한 간장중 MAO활성증가는 ethanol의 대사산물인 acetaldehyde에 기인된 것으로 생각되어지며 인삼 butanol분획이 acetaldehyde에 의해 유도되는 간장중 MAO활성 변동을 조절하고 있을 것으로 사료된다.

• 생약학회지
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• 제34권2호통권133호
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• pp.185-189
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• 2003

We examined the inhibitory activities against monoamine oxidase (MAO) of Morus alba in vitro and in vivo methods. Methanolic extract of M. alba showed significantly inhibitory activities on MAO-A and MAO-B that were prepared from rat brain and liver in vitro. The inhibitory activities were measured by serotonin and benzylamine as substrates, respectively. MAO-A and MAO-B activities were potently inhibited by ethylacetate extracts of M. alba in vitro tests. Those activities in vivo tests have different tendency each other. MAO-A activity was increased by the oral administration of methanolic extract of M. Alba, while, MAO-B activity was decreased. Consequently, we can suggest that M. alba may have the effects on the inhibitory activities against MAO both in vitro and in vivo.

• 생약학회지
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• 제37권3호
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• pp.157-161
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• 2006

We examined the inhibitory activities against monoamine oxidase (MAO) of Prunella vulgaris in vitro and in vivo methods. Methanolic extract of P. vulgaris showed significantly Inhibitorγ activities on MAO-A and MAO-B that were prepared from rat brain and liver in vitro. The inhibitory activities were measured by serotonin and benzylamine as substrates, respectively. MAO-A and MAO-B activities were potently inhibited by ethylacetate extracts of P. vulgaris in vitro tests. It was observed that those activities in vivo tests have different tendency each other. MAO-A activity was increased by the oral administration of methanolic extract of P. vulgaris while MAO-B activity was decreased. Consequently, we suggest that P. vulgaris may have the effects on the inhibitory activities against MAO both in vitro and in vivo.

• Natural Product Sciences
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• 제19권1호
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• pp.8-14
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• 2013

The inhibitory effect and the structure-activity relationships of luteolin and its related derivatives isolated from Taraxacum mongolicum against MAO activities were investigated. The activity-guided isolation of extract from Taraxacum mongolicum led to the isolation of three flavonoids, luteolin, diosmetin, and luteolin-7-glucoside, a polyphenol, chlorogenic acid, a tyrosine and a uridine. The inhibitory activities of luteolin and its related derivatives against MAOs activities are dependent on their molecular structures. The presence of the phenolic hydroxy group at para-position is the active site for MAO-A inhibition as well as of MAO-B. The methoxy group has no potential on MAO-A inhibition. An additional phenolic hydroxy group at the ortho-position alleviates about 4-fold MAO-A inhibitory activity of phenolic hydroxy group at para-position. A carboxylic group seems to be critical for DBH inhibition and has no effects on MAO.

• 생약학회지
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• 제37권4호
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• pp.229-234
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• 2006

We examined the inhibitory activities against monoamine oxidase (MAO) of Taraxacum mongolicum in vitro and in vivo methods. Methanol extract of T. mongolicum showed significantly inhibitory activities on MAO-A and MAOB that were prepared from rat brain and liver in vitro. MAO-A and MAO-B activities were potently inhibited by chloroform fraction of T. mongolicum in vitro tests. The $IC_{50}$ values of each fraction on MAO-A are as followed; methanol extracts (0.90 mg/ml), $CHCl_3$ fraction (0.10 mg/ml), EtOAc fraction (0.36 mg/ml). and those on MAO-B are methanol extracts $(0.39{\mu}g/ml)$, $CHCl_3$ fraction $(0.18{\mu}g/ml)$, BuOH fraction $(0.22{\mu}g/ml)$. Those MAO-A and MAO-B activities in vivo tests have different tendency each other. MAO-A activity was increased by the oral administration of ethanol extract of T mon golicum, while MAO-B activity was decreased. The concentration of serotonin of brain tissue after oral administration of ethanolic extract of T. mongolicum is slightly increased in rat. This tendency is not different from the activity of deprenyl which is the well known MAO inhibitor used as a positive control. Based on these results, we can suggest that T. mongolicum may have the effects on the inhibitory activities against MAO. Thess activities of T. mongolicum is considerable for development of functional materials for the purpose of treatment and control of depressant, dementia, Parkinson' disease, stress and promoting exercise.

• Biomolecules & Therapeutics
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• 제20권2호
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• pp.214-219
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• 2012

This research was designed to determine what components of Gardenia jasminoides play a major role in inhibiting the enzymes related antidepressant activity of this plant. In our previous research, the ethyl acetate fraction of G. jasminosides fruits inhibited the activities of both monoamine oxidase-A (MAO-A) and monoamine oxidase-B (MAO-B), and oral administration of the ethanolic extract slightly increased serotonin concentrations in the brain tissues of rats and decreased MAO-B activity. In addition, we found through in vitro screening test that the ethyl acetate fraction showed modest inhibitory activity on dopamine-${\beta}$ hydroxylase (DBH). The bioassay-guided fractionation led to the isolation of five bio-active compounds, protocatechuic acid (1), geniposide (2), 6'-O-trans-p-coumaroylgeniposide (3), 3,5-dihydroxy-1,7-bis(4-hydroxyphenyl) heptanes (4), and ursolic acid (5), from the ethyl acetate fraction of G. jasminoides fruits. The isolated compounds showed different inhibitory potentials against MAO-A, -B, and DBH. Protocatechuic acid showed potent inhibition against MAO-B ($IC_{50}$ $300{\mu}mol/L$) and DBH ($334{\mu}mol/L$), exhibiting weak MAO-A inhibition (2.41 mmol/L). Two iridoid glycosides, geniposide ($223{\mu}mol/L$) and 6'-O-trans-p-coumaroylgeniposide ($127{\mu}mol/L$), were selective MAO-B inhibitor. Especially, 6'-O-trans-p-coumaroylgeniposide exhibited more selective MAO-B inhibition than deprenyl, well-known MAO-B inhibitor for the treatment of early-stage Parkinson's disease. The inhibitory activity of 3,5-dihydroxy-1,7-bis (4-hydroxyphenyl) heptane was strong for MAO-B ($196{\mu}mol/L$), modest for MAO-A ($400{\mu}mol/L$), and weak for DBH ($941{\mu}mol/L$). Ursolic acid exhibited significant inhibition of DBH ($214{\mu}mol/L$), weak inhibition of MAO-B ($780{\mu}mol/L$), and no inhibition against MAO-A. Consequently, G. jasminoides fruits are considerable for development of biofunctional food materials for the combination treatment of depression and neurodegenerative disorders.

• 약학회지
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• 제28권6호
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• pp.305-311
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• 1984

Relationship between hypertension and monoamine oxidase (MAO) activity in rat brain and the change of this relationship by presynaptic ${\alpha}-receptor$ agonist were studied. Animals were divided into three groups. Group I was composed of normotensive Sprague-Dawley rats (NR), group II of spontaneously hypertensive rats (SHR) and group III of acquired hypertensive rats induced by deoxycorticosterone acetate (DOCA) and NaCl treatment. Clonidine, a presynaptic ${\alpha}-receptor$ agonist, was administered to groups II and III. Blood pressures and MAO activities were measured in each group. MAO activities in the brain of SHR were lower than those of NR. Animals in group II received clonidine which lowered blood pressures but did not change MAO activities in the brain. DOCA and NaCl induced hypertension 21 days after these treatments in group III and did not cause any changes in brain MAO activity. Clonidine lowered blood pressures of group III but did not change MAO activities. The data from the present study suggest that abnormaly low MAO activities in SHR brain may be one of the underlying factors for the susceptibility to hypertension and that the decrease in noradrenergic neuronal activities through presynaptic ${\alpha}-receptor$ activation by clonidine may not be related to the changes of brain MAO activities.

• Archives of Pharmacal Research
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• 제11권1호
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• pp.33-40
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• 1988

Two new nitro analogs of tranylcypromine, (E)-2-(p-nitrophenyl)cyclopropylamine ((E)-p-NTCP) and (E)-2-(m-nitrophenyl)cyclopropylamine ((E)-m-NTCP) were synthesized in order to examine the effect of aromatic nitro substitution on the MAO-inhibitory activity of 2-phenylcyclopropylamines. The compounds were obtained by treating t-butyl (E)-2-(p-nitrophenyl) cyclopropanecarbamate and t-butyl (E)-2-(m-nitrophenyl)cyclopropanecarbamate with p-toluenesulfonic acid in $CH_3$CN. Inhibitions of rat brain mitochondrial MAO-A and B by the compounds were examined using serotonin and benzylamine as the substrate at both in vitro and ex vivo levels. It was found from in vitro measurements that (E)-p-NTCP at $6.0{\times}10^{-5}M$ elicited merely 22.5% inhibition against MAO-B without any effect on MAO-A. In contrast, (E)-m-NTCP showed fair degrees of inhibitions of MAO-A and B with $IC_{50}$ values, $2.5{\times}10^{-7}M\;and\;1.4{\times}10^{-6}M$, respectively. It was also noted from (E)-m-NTCP that m-nitro substitution caused a shift of selectivity of the inhibition toward MAO-A. According to ex vivo measurements at 1.5, 3, 6, and 12 hr following the administration of a dose of 0.015 mmol/kg, i.p. to the rats, the inhibition percents of MAO-A by (E)-m-NTCP were 58.6, 63.7 63.6, and 46.6%, slightly lower than those observed by tranylcypromine. Whereas, (E)-m-NTCP at the same dose level did not show significant inhibitions against both MAO-A and MAO-B. Possible reasons for the difference in potencies between (E)-m-NTCP and (E)-p-NTCP were sought in relation to differing electron withdrawing effects of m- and p-substituents which will influence electron density of the side chain amino functions and the partitions.