• 제목/요약/키워드: Sedative-hypnotic activity

검색결과 20건 처리시간 0.019초

Ethanol Extract of Polygalae Radix Augments Pentobarbital-Induced Sleeping Behaviors through $GABA_Aergic$ Systems

  • Lee, Chung-Il;Lee, Mi Kyeong;Oh, Ki-Wan
    • Natural Product Sciences
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    • 제19권2호
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    • pp.179-185
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    • 2013
  • Polygalae radix (PR) has traditionally been used as a sedative and anti-stress agent in oriental countries for a long time. PR which contains many ingredients is especially rich in saponins. This study was performed to investigate whether ethanol extract of PR enhances pentobarbital-induced sleep behaviors. In addition, possible mechanisms also were investigated. PR inhibited locomotor activity in mice. PR increased sleep rate and sleep time by concomitant administration with sub-hypnotic dose of pentobarbital (28 mg/kg). PR prolonged total sleeping time, and shortened sleep latency induced by pentobarbital (42 mg/kg). In addition, PR increased intracellular chloride concentration in primary cultured neuronal cells. The expression level of glutamic acid decarboxylase (GAD) were increased, and ${\gamma}$-aminobutyric acid $(GABA)_A$ receptors subunits were modulated by PR, especially increasing ${\gamma}$-subunit expression. In conclusion, PR augments penobarbital-induced sleep behaviors through activation of $GABA_A$ receptors and chloride channel complex.

Some Pharmacological Studies with Tiliacorine, a Diphenylbisbenzylisoquinoline Alkaloid from Tiliacora racemosa

  • Khasnobis, Arnab;Seal, Tapan;Vedasiromoni, J. Rajan;Gupta, Malaya;Mukherjee, Biswapati
    • Natural Product Sciences
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    • 제5권3호
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    • pp.142-147
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    • 1999
  • Tiliacora racemosa Colebr. belonging to the family Menispermaceae is the biggest store-house of diphenyl bisbenzylisoquinoline (DBBI) alkaloids. Exhaustive chemical processing of the root of T. racemosa by the application of modern separation techniques yielded a DBBI alkaloid which was identified as tiliacorine using sophisticated spectroscopic methods (UV, IR, $1^H-NMR$, Mass). Tiliacorine potentiated the sleeping time induced by standard hypnotics viz. chlorpromazine (CPZ), pentobarbitone (PB) and diazepam (DZ) in a dose dependent manner. Tiliacorine potentiated the analgesic action of standard analgesic agents viz., morphine and meperidine. It was also found to possess anti convulsive activity in the strychnine induced convulsion model.

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진간식풍탕가감방(鎭肝熄風湯加減方)이 중추신경계(中樞神經)에 미치는 효능에 관한 연구(硏究) (Effects of Jingansikpungtanggagam-bang on Central Nerve System)

  • 이상택;김경옥;이인;정윤관;김근우;구병수
    • 동의신경정신과학회지
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    • 제17권3호
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    • pp.21-43
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    • 2006
  • This study was designed to assess Effects of jingansikpungtanggagam-bang on Central Nerve System. Method : jingansikpungtanggagam-bang, a Korean traditional prescription, was evaluated for its anticonvulsant effect, hypnotic activity, analgesic action, anxiolytic effect, memory enhancement, and MAO inhibitory activity and detennined the content of neurotransmitter in brain by HPLC method. Result : 1. The extract increased potently anticonvulsant effect at 1g/kg by 5.6-fold extention of onset time against control group. 2. The extract increased hvrmsis at 500mg/kg by over twofold length of sleeping time compared to control. 3. The extract showed a significant analgesic effect with 86.0% inhibition on writhing frequency at 500mg/kg by phenylquinone-induced writhing test. 4. The extract inhibited dose-dependently the activity of monoamine oxidase in vitro. 5. This prescription increased the brain levels of serotonin and 5-hydroxyindoleacetic acid by 3.3% and 1.4%, respectively. 6. the extract exhibited the anxiolytic effect with 21.3% decrease of the immobility duration against control group. 7. the extract enhanced memory recovery on scopolamine-induced impairment of passive avoidance performance at 1g/kg pretreatment with 20.2% increase of latency time. Conclusion : The result sugguest that jiugansikpungtanggagam-bang can be used effectively as a sedative prescription in Korean traditional medicine.

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감송향 정유성분의 흡입 및 경구투여시의 중추신켱 억제효과 (Inhibitory Effects of the Essential Oil from Nardostachys intamansi on Central Nervous System after Inhalation and Oral Administration)

  • 구병수;김대근;최정현;이동웅
    • 생명과학회지
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    • 제16권1호
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    • pp.156-161
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    • 2006
  • The essential oil of Nardostachys jatamansi (Valerianaceae), which has been used for a long time in aroma therapy, was investigated after inhalation or oral administration for its analgesic effect, anticonvulsant action, hypnotic effect and in vitro inhibitory activity on monoamine oxidase. This fragrance oil showed a significant analgesic effect in the phenylquinone-induced .writhing test, suppressed the convulsion induced by pentylenetetrazole and lengthened the pentobarbital-induced sleeping time in a time-dependent manner after fragrance inhalation or dose-independently by oral administration. Its inhibitory activity on monoamine oxidase was remarkable, showing $49.4\%$ inhibition at a concentration of 5.0 mg/ml. Six new terpenes with seven known compounds were detected by our GC-MS analytical conditions used. As a result, the essential oil fragrance of Nardostachys jatamansi would be clinically useful for a sedative by either inhalation or oral administration.

중추신경흥분제 및 Adenosine이 마우스의 자발운동에 미치는 영향 (Effects of Adenosine and CNS Stimulants on Motor Activity in Mice)

  • 곽정재;김혜영;김원준
    • 대한약리학회지
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    • 제19권1호
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    • pp.77-84
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    • 1983
  • The behavioral pattern of an animal is influenced by endogenous and endogenous stimuli such as humoral secretion, neurohumoral transmitters, drugs, light and environmental change. It has teen known that adenosine is a normal constituent of brain, and has sedative or hypnotic effects and anticonvulsant effects, inhibiting the spontaneous firing of cells in the brain via membrane adenosine receptors. Recent studies suggest that the excitatory responses to xanthines in the CNS might be related to the competitive antagonism of xanthines to adenosine. This study was undertaken to Investigate the effects of adenosine and the CNS stimulants such as picrotoxin, strychnine and caffeine on the spontaneous activity of mire, and to examine the influence of adenosine on the seizures induced by large doses of CNS stimulants. Subjects were $20{\sim}30\;g$ adult mice, and the spontaneous activity was measured using the Selective Activity Meter after intraperitoneal injection of adenosine (10 mg/kg), caffeine (100 mg/kg), strychnine(0.2 mg/kg) or picrotoxin(0.5 mg/kg) with or without adenosine pretreatment. The seizures were induced with caffeine(200, 250 and 300 mg/kg), strychnine(1.25 and 1.5 mg/kg) or picrotoxin(10 and 15 mg/kg). The results are summarized as follows : 1) The spontaneous activity in mite was significantly inhibited between 10 and 20 minutes after adenosine treatment. 2) Caffeine and picrotoxin increased the motor activity significantly while strychnine had no effect on the activity. 3) The ambulatory activity in the caffeine, strychnine and picrotoxin treated groups was significantly inhibited by adenosine pretreatment. 4) The seizures were observed with caffeine(200, 250 and 300 m9/kg), strychnine(1.25 and 1.5 mg/kg) or picrotoxin(10 and 15 mg/kg). The caffeine induced seizures were inhibited by adenosine pretreatment, but the strychnine or picrotoxin induced seizures were not affected.

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Arousal Inhibitory Effect of Phlorotannins on Caffeine in Pentobarbital-Induced Mice

  • Cho, Suengmok;Yang, Hyejin;Yoon, Minseok;Kim, Jiyoung;Kim, Dongsoo;Kim, Jinkyung;Kim, Seon-Bong
    • Fisheries and Aquatic Sciences
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    • 제17권1호
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    • pp.13-18
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    • 2014
  • Sleep is vital to maintain health and well-being; however, insomnia is currently a widespread health complaint worldwide. In particular, caffeine, a psychoactive component of coffee, tea, and caffeine beverages may lead to sleep disorders such as insomnia. In this study, our primary objective was to investigate the inhibitory effect of high-purity phlorotannin preparation (HP-PRT) on caffeine-induced wakefulness. The sleep test of pentobarbital-induced mice was used as an in vivo animal model. Caffeine (50 and 100 mg/kg) showed significant arousal effects (an increase in sleep latency and a decrease in sleep duration). Co-administration of caffeine (50 mg/kg) and the sedative-hypnotic diazepam (DZP, 1 mg/kg) did not result in similar arousal activity. HP-PRT (500 mg/kg) also inhibited caffeine-induced wakefulness. Our results suggest that HP-PRT would be a useful additive for developing coffee products without the arousal effect.

Nitrogen Compounds of Korea Ginseng and their Physiological Significance

  • Park, Hoon;Cho, Byung-Goo;Lee, Mee-Kyoung
    • 고려인삼학회:학술대회논문집
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    • 고려인삼학회 1990년도 Proceedings of International Symposium on Korean Ginseng, 1990, Seoul, Korea
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    • pp.175-189
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    • 1990
  • Nitrogen compounds of Panax ginseng and their biological activities in plant and animal were reviewed. Major nitrogen compounds found in P. ginseng are free amino acids. Water solilble proteins, indouble proteins and peptides. Minor nitrogen compounds are dencichine. Glycolyroteins, amines, alkaloides, methoxy or alkyl pyrazine derivatives, free nucleosides and nucleic acid bases. 4-methyl-i-thiazoltethanol and pyroglutamic acid the contents of total nitrogen and protein in root Increased until 13 years old which was the highest age tinder investigation. Soluble protein content increased with the root weight and was higher in xylem pith than cortex-epidermis indicating the close relation with root growth. Arginine, which covered 58% of total free amino acids, may serve as storage nitrogen. Arginine seems to be changed into proline in rhizome. threonine in stem and again threonine and arginine in leaf. The greater the root weight the higher the polyamine stimulated Polyamine stimlllated the growth of root callus. Physiological roles of other minor nitrogen compounds are unknown although content is relatively high ((1.if) 6.w). Biochemical and pharmacological activities of some nitrogen compounds for animal were more investigated than physiological role there plant itself. Radiation and U.V protective function (heat stable protein). insulin-like activity in lipogenesis and livolysis (adenosine and pyroglutamic acid), depression of blood sugar content (glycopevtide). htmostatic and nellrotoxic activity (dencichine) and, sedative and hypnotic activity (4-methyl-i-thiazoleethanol) are reported. Heat stable protein increased with root age. The traditional quality criteria appear to be well in accordance with biological activities of nitrogen compounds. Chemical studies of nitrogen compounds seem relatively rare, probably due to difficulty of isolation, subsequently the investigations of biological activities are little.

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고려인삼의 함질소 화합물과 생리학적 중요성 (Nitrogen Compounds of Korea ginseng and Their Physiological Significance)

  • Park, Hoon;Cho, Byung-Goo;Lee, Mee-Kyoung
    • Journal of Ginseng Research
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    • 제14권2호
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    • pp.317-331
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    • 1990
  • Nitrogen compounds of Panax ginseng and their biological activities in plant and animal were reviewed. Major nitrogen combounds found in P. ginseng are free amino acids, Water soluble teins, insoluble proteins and peptides. Minor nitrogen compounds are dencichine. glycol)roteins. amines, alkaloides, methoxy or alkyl pyrazine derivatives. free nucleosides and nllrleir arid bases. 4-me- thymi-5-thiazoleethanol and pyroglutamic acid. The contents of total nitrogen and protein in root increased until 13 years old rvhich was the highest age tinder investigation. Soluble protein content increased With the root weight and was higher in xylem pith than cortex-epidermis indicating the rlosc relation with root growth. Arginine which covered 58% of total free amino aroids may serve as a storage nitrogen. Arginine seems to be changed into proline in rhizome, threonine in stem and again threoning and arginine in leaf. The greater the root weight the higher the polyaminc content. Polyamine stimulated the growth of root callus. Physiological roles of other minor nitrogen compounds are unknown although dencichine content is relatively high (0.5% d.w.). biochemical and pharmatological activities of some nitrogen compounds for animal were more investigated than physiological roll iota plant itself. Radiation and U.V. protective function (heat stable protein), insulin-like activity in lipogenesis and lipolysis (adenosine and pyroglutamic acid), depression of blood sugar content (glycopeptide). hemostatir and nellrotoxic activity (denrichine) and. sedative and hypnotic activity (4-methyl-5-thiazoleethilnol) are reported. Heat stable protein increased with root age. The traditional quality critsria appear to be well in accordance with biological activities of nitrogen compounds. Chemical stlldies of nitrogen compounds seem relatively rare, probably dole to difficulty of isolation, subsequently the investigations of biological activities are little.

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Sinomenine, an Alkaloid Derived from Sinomenium acutum Potentiates Pentobarbital-Induced Sleep Behaviors and Non-Rapid Eye Movement (NREM) Sleep in Rodents

  • Yoo, Jae Hyeon;Ha, Tae-Woo;Hong, Jin Tae;Oh, Ki-Wan
    • Biomolecules & Therapeutics
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    • 제25권6호
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    • pp.586-592
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    • 2017
  • Sinomenium acutum has been long used in the preparations of traditional medicine in Japan, China and Korea for the treatment of various disorders including rheumatism, fever, pulmonary diseases and mood disorders. Recently, it was reported that Sinomenium acutum, has sedative and anxiolytic effects mediated by GABA-ergic systems. These experiments were performed to investigate whether sinomenine (SIN), an alkaloid derived from Sinomenium acutum enhances pentobarbital-induced sleep via ${\gamma}$-aminobutyric acid (GABA)-ergic systems, and modulates sleep architecture in mice. Oral administration of SIN (40 mg/kg) markedly reduced spontaneous locomotor activity, similar to diazepam (a benzodiazepine agonist) in mice. SIN shortened sleep latency, and increased total sleep time in a dose-dependent manner when co-administrated with pentobarbital (42 mg/kg, i.p.). SIN also increased the number of sleeping mice and total sleep time by concomitant administration with the sub-hypnotic dosage of pentobarbital (28 mg/kg, i.p.). SIN reduced the number of sleep-wake cycles, and increased total sleep time and non-rapid eye movement (NREM) sleep. In addition, SIN also increased chloride influx in the primary cultured hypothalamic neuronal cells. Furthermore, protein overexpression of glutamic acid decarboxylase ($GAD_{65/67}$) and $GABA_A$ receptor subunits by western blot were found, being activated by SIN. In conclusion, SIN augments pentobarbital-induced sleeping behaviors through $GABA_A$-ergic systems, and increased NREM sleep. It could be a candidate for the treatment of insomnia.

Rosmarinic Acid Potentiates Pentobarbital-Induced Sleep Behaviors and Non-Rapid Eye Movement (NREM) Sleep through the Activation of GABAA-ergic Systems

  • Kwon, Yeong Ok;Hong, Jin Tae;Oh, Ki-Wan
    • Biomolecules & Therapeutics
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    • 제25권2호
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    • pp.105-111
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    • 2017
  • It has been known that RA, one of major constituents of Perilla frutescens which has been used as a traditional folk remedy for sedation in oriental countries, shows the anxiolytic-like and sedative effects. This study was performed to know whether RA may enhance pentobarbital-induced sleep through ${\gamma}-aminobutyric$ acid $(GABA)_A-ergic$ systems in rodents. RA (0.5, 1.0 and 2.0 mg/kg, p.o.) reduced the locomotor activity in mice. RA decreased sleep latency and increased the total sleep time in pentobarbital (42 mg/kg, i.p.)-induced sleeping mice. RA also increased sleeping time and number of falling sleep mice after treatment with sub-hypnotic pentobarbital (28 mg/kg, i.p.). In electroencephalogram (EEG) recording, RA (2.0 mg/kg) not only decreased the counts of sleep/wake cycles and REM sleep, but also increased the total and NREM sleep in rats. The power density of NREM sleep showed the increase in ${\delta}-waves$ and the decrease in ${\alpha}-waves$. On the other hand, RA (0.1, 1.0 and $10{\mu}g/ml$) increased intracellular $Cl^-$ influx in the primary cultured hypothalamic cells of rats. RA (p.o.) increased the protein expression of glutamic acid decarboxylase ($GAD_{65/67}$) and $GABA_A$ receptors subunits except ${\beta}1$ subunit. In conclusion, RA augmented pentobarbital-induced sleeping behaviors through $GABA_A-ergic$ transmission. Thus, it is suggested that RA may be useful for the treatment of insomnia.