• 보험의학회지
• /
• 제1권1호
• /
• pp.84-87
• /
• 1984

1. 전신가토(全身家兎) 및 척수가토(脊髓家兎)에서 MAO 억제하(抑制下)에서의 brethylium의 tyramine 승압효과(昇壓效果)에 미치는 영향(影響)을 관찰(觀察)하였다. 2. 전신가토(全身家兎) 및 척수가토(脊髓家兎)에서 bretylium 정주(靜注) 후(後)에는 tyramine의 승압효과(昇壓效果)는 강화(强化)되었으나 MAO 억제제(抑制劑)인 catron을 정주(靜注)하고 bretylium을 추가(追加) 주입(注入)한 후(後)에는 tyramine의 승압효과(昇壓效果)는 catron 투여전(投與前)의 그것보다 감약(減弱)되었다. 3. Bretylium에 의한 tyramine 승압효과(昇壓效果)의 강화(强化)는 MAO 억제작용(抑制作用)으로 설명(說明)되고, tyramine 승압효과(昇壓效果)의 감약(減弱)은 교감신경말단(交感神經末端)의 차단작용(遮斷作用)으로 설명(說明)된다.

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

• 약학회지
• /
• 제27권4호
• /
• pp.321-329
• /
• 1983

The review characterized active site(s) of MAO with respect to metal ions, hydrophobic and polar region, sulfhydryl group and flavin moiety. The mechanism of inhibition was dealt with three representative types of inhibitors; phenylcyclopropylamines, acetylenic amines, and hydrazines. Multiple forms of MAO was shortly described in relation to their selective inhibition. 84 reference were cited.

• Natural Product Sciences
• /
• 제6권2호
• /
• pp.70-72
• /
• 2000

The effects of coptisine on monoamine oxidase (EC 1.4.3.4; MAO) activity in mouse brain were investigated. Coptisine showed an inhibitory effect on MAO activity with a concentration-dependent manner. Coptisine exhibited 51.0% inhibition of MAO activity at $9\;{\mu}M$. The $IC_{50}$ value of coptisine was $8.7\;{\mu}M$. Coptisine inhibited MAO activity competitively with kynuramine as a substrate. The $K_i$ value of coptisine was $4.1\;{\mu}M$. These results indicate that coptisine functions to regulate the catecholamine content at biologically active sites.

• Natural Product Sciences
• /
• 제5권4호
• /
• pp.159-161
• /
• 1999

The effects of bioactive fractions containing protoberberine alkaloids from Coptis japonica on monoamine oxidase (MAO) activity were investigated. The MAO was obtained from the mitochondrial fraction of mouse brain. The butanol fraction from Coptis japonica was fractionated into separate bioactive fraction (Fr I-IV) by silica gel column chromatography. MAO activity was strongly inhibited by Fr III and IV, which mainly contain protoberberine alkaloids such as berberine, palmatine and coptisine. These results indicated that the protoberberine alkaloids from Coptis japonica had an inhibitory effect on MAO activity.

• Environmental Analysis Health and Toxicology
• /
• 제18권1호
• /
• pp.21-25
• /
• 2003

카바메이트계 농약인 카보푸란은 어류에 대한 독성이 매우 높으며, 낮은 농도에서 어류의 척추기형이나 행동이상을 유발한다. 이러한 카보푸란의 독성기전을 밝히기 위한 일환으로 신경물질대사와 관련이 깊은 acetylcholine esterase(AChE)와 monoamine oxidase(MAO)에 미치는 농약의 효과를 송사리(Oryzias latipes; Medaka fish)를 이용하여 평가하였다. Medaka fish에 대한 카보푸란의 반수치사농도(LC$_{50}$)는 2.5 ppm이었으며, 1 ppb 카보푸란에 24시간 노출된 경우, AChE 효소활성이 머리와 몸통부위에서 각각 30, 20%씩 감소되었다. 한편, MAO 효소활성은 카보푸란의 농도가 증가함에 따라 머리부위에서는 감소한 반면, 몸통부위에서는 증가하는 경향을 보였다. 특히 카보푸란의 농도가 1 ppb에서도 송사리의 MAO 효소활성이 영향을 받는 것으로 나타나, 카보푸란에 의한 송사리의 행동이상은 AChE 활성 뿐 아니라 MAO활성의 변화에 의한 복합적인 효과일 가능성이 높다.

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

• 대한의생명과학회지
• /
• 제12권2호
• /
• pp.91-97
• /
• 2006

The effects of intravenous administration of high concentration of taurocholic acid (TCA) on monoamine oxidase (MAO) A and B activities in rat liver mitochondria and microsomes were studied. These liver subcellular organelles and serum MAO activities were determined from the experimental rats with choledocho-caval shunt (CCS). The Michaelis-Menten constants in these hepatic enzymes were also measured. The activities of mitochondrial MAO A and B, and microsomal MAO B as well as their $V_{max}$ values were found to be decreased significantly in CCS plus TCA injected group then in the control group, such as CCS alone groups. However their $K_m$ values in the experimental groups did not vary. MAO of serum appeared in the CCS plus TCA injected groups only. The above results suggest that TCA represses biosynthesis of the MAO in the liver. The MAO of serum is believed to be caused by the increment of membrane permeability of hepatocytes upon TCA mediated liver cell necrosis.

• Journal of Microbiology and Biotechnology
• /
• 제27권4호
• /
• pp.785-790
• /
• 2017

Two piloquinone derivatives isolated from Streptomyces sp. CNQ-027 were tested for the inhibitory activities of two isoforms of monoamine oxidase (MAO), which catalyzes monoamine neurotransmitters. The piloquinone 4,7-dihydroxy-3-methyl-2-(4-methyl-1-oxopentyl)-6H-dibenzo[b,d]pyran-6-one (1) was found to be a highly potent inhibitor of human MAO-B, with an $IC_{50}$ value of $1.21{\mu}M$; in addition, it was found to be highly effective against MAO-A, with an $IC_{50}$ value of $6.47{\mu}M$. Compound 1 was selective, but not extremely so, for MAO-B compared with MAO-A, with a selectivity index value of 5.35. Compound 1,8-dihydroxy-2-methyl-3-(4-methyl-1-oxopentyl)-9,10-phenanthrenedione (2) was moderately effective for the inhibition of MAO-B ($IC_{50}=14.50{\mu}M$) but not for MAO-A ($IC_{50}$ > $80{\mu}M$). There was no time-dependency in inhibition of MAO-A or -B by compound 1, and the MAO-A and -B activities were almost completely recovered in the dilution experiments with an excess amount of compound 1. Compound 1 showed competitive inhibition for MAO-A and -B, with $K_i$ values of 0.573 and $0.248{\mu}M$, respectively. These results suggest that piloquinones from a microbial source could be potent reversible MAO inhibitors and may be useful lead compounds for developing MAO enzyme inhibitors to treat related disorders, such as depression, Parkinson's disease, and Alzheimer's disease.

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