• Title/Summary/Keyword: monoamine oxidase-A

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A New Synthetic Approach to 3-Amino-2-phenylthietanes as Potential Monoamine Oxidase Inhibitors

  • Kang, Gun-Il;Frank S. Abbott
    • Archives of Pharmacal Research
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    • v.2 no.1
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    • pp.9-16
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    • 1979
  • 3-Amino-2-phenylthietane derivatives were considered as a useful tool to elusidate the mechanism of inhibiton of MAO by tranylcypromine-type inhitors. The synthesis of 3-benzoylamino-2-phenylthieetane, 3-amino-2-phenylthietane, and 3-N, N-dimentylamino-2-p-nitrophenythietane was attempted using the reaction between 1, 3 dihalogeno alkanes with alkali sulfide. When 1-pheny1-1, 3-dihalo-2-benzolaminopropane was treated with sodium sulfide, 2-pheny 1-4 benzylidene-2-oxazoline was isolated, indicating the case of elimination reaction compared to ring formation. The reaction of 1-p-nitropheny1-1, 3-dichloro-2-N, N-dimethylaminopropane with sodium sulfide gave bis (1-p-nitropheny1-2-N, N-dimethylamino-3-chloropropane)sulfide. The mechanism of reaction was discussed.

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Novel Pharmacological Treatment for Depression (새로운 우울증 치료 약물)

  • Jeong, Hee Jeong;Moon, Eunsoo
    • Korean Journal of Biological Psychiatry
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    • v.23 no.1
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    • pp.1-11
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    • 2016
  • Development of various antidepressants such as monoamine oxidase inhibitors, tricyclic antidepressants, selective serotonin reuptake inhibitors, serotonin norepinephrine reuptake inhibitors, and noradrenergic and specific serotonergic antidepressant has led to a tremendous progression of pharmaceutical treatment for depression, but still there are some limitations of current antidepressants, such as treatment-resistant depression and delayed onset of antidepressants. The pathogenesis of depression is unclear because depression is a heterogeneous disease state, and the mechanisms of antidepressants remain uncertain as well. Nevertheless, in an attempt to develop novel antidepressants, some trials have been conducted based on the potential biological mechanism discovered in the numerous research results. This review will provide information about the potential novel antidepressants and the current states of clinical studies using them. In particular, some potential novel antidepressants anti-inflammatory agents, antioxidants, anticholinergics, modulators of Hypothalamic Pituitary Adrenal Axis, glutamate, and opioid systems, as well as some neuropeptides such as susbstance P, neuropeptide Y, and galanin will be discussed.

Effects of Silkworm(Bombyx mori L..) Powder on Lipofuscin, Acetylcholine and Its Related Enzyme Activities in Brain of Rats (뇌조직의 리포푸신, 아세틸콜린 및 그 관련효소 활성에 미치는 누에분말의 영향)

  • 최진호;김대익;박수현;김정민;조원기;이희삼;류강선
    • Journal of Life Science
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    • v.10 no.6
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    • pp.564-569
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    • 2000
  • This study was designed to investigate the effect of silkworm (Bombyx mori L.) powder on lipofuscin, acetylcholine (ACh) and its related enzyme activities in brain of rats. Sprague-Dawley (SD) male rats ($160{\pm}10g$) were fed basic diet (control group), and experimental diets (SWP-200 and SWP-400 groups) added 200 and 400 mg/kg BW/day for 6 weeks. In case of liver membranes, lipofuscin (LF) levels resulted in a slight decreases (4.6% and 11.5%, respectively) in SWP-200 and SWP-400 groups compared with control group. But in case of barin as the most sensitive organ, LF levels were remarkably inhibited about 16.7% and 20.0% in SWP-200 and SWP-400 groups compared with control group. There were no significant differences in acetylcholine (ACh) syntheses as a very important neurotransmitter, and choline acetyltransferase (ChAT) activities as a synthesis enzyme of ACh, and acetylcholinesterase (AChE) activities as a hydrolysis enzyme, which were concerned in transmission of neuron through synapses in brain of SWP-200 and SWP-400 groups compared with control group. Monoamine oxidase-B (MAO-B) activities were significantly inhibited (about 10.2%) in brain of SWP-400 groups compared with control group. These results suggest that inhibiting effects of LF accumulation and MAO-B activity of silkworm powder (SWP) may play a pivotal role in attenuating a various age-related changes for improvement of brain function.

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Pharmacological actions of H2O and MeOH extract of Opuntia ficus-indica Semen

  • Suh, My-Hyun;Lee, Ji-Yun;Jang, Yong-Un;Sim, Sang-Soo;Kim, Chang-Jong
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.299.3-300
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    • 2002
  • Both of Semen (OF-Se) or stem (OF-Sf) of Opuntia ficus-indica Semen have been used as a healthful food or folk medicine in korea for the treatment of asthma. diabetes mellitus. aging, osteoporosis, rheumatic arthritis. constipation, cancer. gastric ulcer. constipation. toxic state, edema, etc, There are many reports that OF have the anti-gastric damage, wound healing, diabetes mellitus, monoamine oxidase B inhibitor etc. (omitted)

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Anti-obesity and Anti-hyperlipidemic Effects of Taeyeumjowee-tang and its modified prescription (태음조위탕(太陰調胃湯)과 그 가감방(加減方)의 항비만 및 항고지혈증 효과에 관한 연구)

  • Kim, Kil-Soo;Lee, Dong-Ung;Kim, Yong-Lae;Hwang, Moon-Je;Kim, Geun-Woo;Koo, Byung-Soo
    • Journal of Oriental Neuropsychiatry
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    • v.18 no.2
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    • pp.57-74
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    • 2007
  • Objective : The purpose of this study was to investigate the anti-obesity and anti-hyperlipidemic Effects of Taeyeumjowee-tang and its modified prescription on the animal model of obesity and hyperlipidemia induced high-fat diet. Method : 1) The extracts of Taeyeumjowee-tang (TJT) and its modified prescription, Taeyeumjoweetang gagam-bang (TJGB) were evaluated for its inhibitory effects on obesity. 2) The body weight and feed weight were determined in the pre-treated and post-treated mice and the lipid profiles in the serum were analyzed in order to evaluate the anti-hyperlipidemia action of the extracts. 3) The effect of each extract was investigated for the influences on monoamine oxidase activity and HMG-CoA reductase activity. Results 1. TJT and TJGB extracts dose-dependently reduced the body weight and feed intake in normal mice. The effect of TJGB extract was better than that of TJT extract. 2. TJGB extract diminished the body weight increase and reduced the feed intake in the pre-treatment or post-treatment of the extract 3. TJGB extract decreased the amount of total cholesterol slightly and triglyceride potently after the pre-treatment or post-treatment, but HDL cholesterol exhibited no remarkable change compared with control. 4. TJGB extract weakly potentiated the monoamine oxidase activity, but its effect was better than that of TJT extract. 5. TJGB extract weakly inhibited the HMG-CoA reductase activity, but its effect was better than that of TJT extract. Conclusion : Taeyeumjowee-tang and its modified prescription can clinically be useful as anti-obesity drug and also for the improvement of hyperlipidemia.

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Effects of Bupleuri Radix on Rat Hepatic MAO by Common Bile Duct Ligation and Taurocholate Load after Common Bile Duct Ligation (시호(柴胡)가 총담관결찰 및 taurocholate 부하(負荷) 흰쥐 간의 MAO 활성에 미치는 영향)

  • Kim, Seong-Mo;Wang, Wu-Hao;Park, Jae-Hyun
    • The Journal of Internal Korean Medicine
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    • v.21 no.2
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    • pp.275-281
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    • 2000
  • Object : This study was carried out to examine the effect of Bupleuri Radix on experimental cholestasis, and make clear apart of this mechanism. Methods : Two models of common bile duct ligation group and taurocholate load group after common bile duct ligation were induced, and Bupleuri Radix extract was taken orally for 14 days. In the 1, 2, 4, 7 and 14 days after treatment, the mitochondrial and microsomal monoamine oxidase(MAO) A and B activities in liver were measured. Results : The mitochondrial MAO A and B activities increased in both Blupleuri Radix treated group after common bile duct ligation and Blupleuri Radix treated group after taurocholate load and common bile duct ligation. MAO A increased in Blupleuri Radix treated group after taurocholate load and common bile duct ligation, and MAO B increased in Blupleuri Radix treated group after common bile duct ligation. The microsomal MAO A activities increased in both Blupleuri Radix treated group after common bile duct ligation and Blupleuri Radix treated group after taurocholate load and common bile duct ligation. Conclusion : According to the result, it is consider that Blupleuri Radix not only improves cholestatis in liver, but also decreases a genetic synthesis of taurocholic acid.

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Inhibitory effect of Capparis zeylanica Linn. on acetylcholinesterase activity and attenuation of scopolamine-induced amnesia

  • Chaudhary, Amrendra Kumar;Solanki, Ruchi;Singh, Vandana;Singh, Umesh Kumar
    • CELLMED
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    • v.2 no.2
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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.

Determination of Peripheral Catechol O-methyltransferase (COMT) Activity in vivo using $[2-^{14}C]-3',4'-Dihydroxyacetophenone$

  • Kim, Eun-Joo;Ahn, Jong-Woong;Lee, Hye-Suk;Christ, Wolfram
    • Archives of Pharmacal Research
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    • v.14 no.4
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    • pp.290-294
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    • 1991
  • For the determination of peripheral COMT activity, we synthesized $[2-^{14}C]-3',4'-dihydroxyacetophenone([^{14}C]-DHAP)$, a model substrate closely related to catecholamines, which cannot be attacked by monoamine oxidase. After i.v.-injection of $[^{14}C]-DHAP$ in living animals, only 3',4'-dihydroxy-acetophenone (3',4'-DHAP) and 3'-methoxy-4'-hydroxyacetophenone (3'-MHAP) were detected in blood by thin layer radio chromatography. It could be speculated that 3',4'-DHAP was primarily O-methylated by COMT, followed by subsequent conjugations. The concentration of 3',4'-DHAP, a substrate for COMT, in blood at 5 min after injection of $[^{14}C]-DHAP$, were similar in all animals. The rate of 3'-MHAP formation can be therefore used as an indicator for peripheral COMT activity. The velocity of methylation in 15 min after i.v.-administration of $[^{14}C]-DHAP$ was $0.28\;{\mu}g/ml{\cdot}min$. From these results, 3',4'-DHAP was shown to be used as an appropriate substrate to determine the COMT activity in vivo.

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Influences of Hydrocortisone, DHEA, Estradiol and Testosterone on the Hepatic and Intestinal Polyamine Metabolism of Castrated Mice (Hydrocortisone, DHEA, Estradiol 및 Testosterone에 의하여 나타나는 마우스-간 및 소장 Polyamine 대사의 변동에 관한 연구)

  • Choi, Sang-Hyun;Chun, Boe-Gwun;Kim, Nam-Hun;Chun, Yeon-Sook
    • The Korean Journal of Pharmacology
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    • v.26 no.1
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    • pp.67-76
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    • 1990
  • Hydrocortisone 50 mg/kg (HC), dehydroepiandrosterone 250 mg/kg (DHEA), ${\beta}-estradiol$ 5 mg/kg (E2), and testosterone 20 mg/kg (TS) were subcutaneously injected into the castrated ICR mice at noon for four days, and the animals were sacrificed at 10-12 A.M. of the fifth day. The intestinal DAO activity was significantly decreased by HC, but it was rather increased by E2 and TS, respectively. And DHEA did not change the DAO activity. But the hepatic MAO activity was not affected by anyone of HC, DHEA, E2, and TS. Aminoguanidine 25 mg/kg produced the marked decrease of the intestinal DAO activity and the significant increases of the intestinal PT and SD contents, but it did not change the hepatic polyamine contents. HC and DHEA induced the significant increase of the intestinal PT content. E2 induced the marked increase of the hepatic PT content and the moderate increase of the intestinal PT content. TS little affected the polyamine contents of the liver and intestine. These results suggest that the E2-induced increase of the hepatic PT content is rather ascribed to the greater enhancement of PT synthesis than the inhibition of polyamine catabolism, and that the HC-induced increase of the intestinal PT content is due partly to the inhibition of polyamine catabolism via DAO.

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Positive effects of anthocyanin-rich mulberry milk on mental health problems in the working population: an open-label study

  • Poonsri Rangseekajee;Nawanant Piyavhatkul;Jintanaporn Wattanathorn;Wipawee Thukham-mee;Pongsatorn Paholpak
    • Nutrition Research and Practice
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    • v.18 no.1
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    • pp.110-118
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    • 2024
  • BACKGROUND/OBJECTIVES: Depression and anxiety are common mental health problems. Anthocyanins from berries might have an inhibitory effect on monoamine oxidase (MAO) enzymes and alleviate various mood and anxiety symptoms. This study examined the effects of a daily supplement of an anthocyanin-rich product on mental health problems. SUBJECTS/METHODS: This study was a secondary analysis from a randomized, 6-week, open-label trial in 300 healthy participants aged 18-60 years who consumed 1 or 2 servings of anthocyanin-rich mulberry milk daily. The General Health Questionnaire-28 (GHQ-28) and Hospital Anxiety and Depression Scale (HADS) were used to monitor mental health problems. In addition, the saliva activity levels of MAO-A, MAO-B, and cortisol were examined at the baseline and after 6 weeks. RESULTS: The total scores of the GHQ-28 and HADS and all their subscales decreased in both groups (all P < 0.05). The cortisol, MAO-A, and MAO-B activities decreased significantly (all P < 0.05), but there were no significant differences between the groups (all P > 0.05). Significant correlations were noted between the decreased activity level of MAO-A enzyme and decreased scores from the GHQ-28 somatic subscale and the HADS depression subscale (all P < 0.05). CONCLUSIONS: Daily consumption of anthocyanin-rich mulberry milk possibly improves mental health problems by reducing depressive and anxiety symptoms in the working population. The suppression of MAO-A activity is a possible underlying mechanism.