• 제목/요약/키워드: sedative action

검색결과 65건 처리시간 0.03초

Effects of Hesperidin Are Not Associated with Changes in Basal Synaptic Transmission, Theta-burst LTP, and Membrane Excitability in CA1 Neuron

  • Baek, Jin-Hee;Kim, Jae-Ick;Kaang, Bong-Kiun
    • Animal cells and systems
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    • 제13권4호
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    • pp.357-362
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    • 2009
  • Hesperidin, the most abundant polyphenolic compound found in citrus fruits, has been known to possess neuroprotective, sedative, and anticonvulsive effects on the nervous system. In a recent electrophysiological study, it was reported that hesperidin induced biphasic change in population spike amplitude in hippocampal CA1 neurons in response to both single spike stimuli and theta-burst stimulation depending on its concentration. However, the precise mechanism by which hesperidin acts on neuronal functions has not been fully elucidated. Here, using whole-cell patch-clamp recording, we revealed that hesperidin did not affect excitatory synaptic activities such as basal synaptic transmission and theta-burst LTP. Moreover, in a current injection experiment, spike number, resting membrane potential and action potential threshold also remained unchanged. Taken together, these results indicate that the effects of hesperidin on the neuronal functions such as spiking activity might not be attributable to either modification of excitatory synaptic transmissions or changes in membrane excitability in hippocampal CA1 neuron.

마이크로에멀젼을 이용한 프로포폴 주사제의 개발 및 평가 (Preparation and Evaluation of Propofol Microemulsion for Parenteral Use)

  • 이종화;박선영;김동우;조미현;조인숙;이계원;박목순;지웅길
    • 약학회지
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    • 제46권5호
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    • pp.337-342
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    • 2002
  • Propofol(2,6-diisopropyl phenol) is a phenol derivative that is chemically distinct from other intravenous sedative hypnotics. It has been extensively used as a short term anesthetic agent, because of the rapid onset and short duration of action. Propofol microemulsion system was prepared with different concentrations of ethyl oleate, $Solutol^{(R)}$ HS 15 and $Kollidon^{(R)}$ 17 PF. Propofol microemulsions were studied by transmittance, viscosity, particle size, in vitro release and pharmacokinetics. The range of transmittance of A group with 4% ethyl oleate and that of B group with 5% ethyl oleate were 92.6~95.1 and 91.3~94.2%, respectively. Transmittance 1~2% decreased as concentration of $Kollidon^{(R)}$ 17 PF was increased and increased 0.8~3.3% when 10 times diluted with normal saline. The viscosity of A and B group were in the range of 3.9~4.1 mPaㆍsec and 4.4~5.3 mPaㆍsec, respectively. The particle sizes of A and B group increased as amount of $Kollidon^{(R)}$ 17 PF. Also, release of propofol was slowly increased as the amount of $Kollidon^{(R)}$ 17 PF was increased. Propofol plasma concentration by i.v injection showed 2-compartment model. Pharmacokinetics of A-5 was similar to that of commercial emuision(POFOL).

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.

소아 진정시 Chloral Hydrate, Hydroxyzine복용 후 Midazolam의 점막하 투여 용량에 따른 진정효과에 관한 연구 (Sedative Effect of Sublingual Midazolam after Oral Chloral Hydrate or Hydroxyzine in Children)

  • 이현정;백광우;정상혁
    • 대한치과마취과학회지
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    • 제8권1호
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    • pp.16-21
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    • 2008
  • Recently combining regimen of minimal doses of chloral hydrate, hydroxyzine and midazolam is good in sedation of children. Midazoalm, water soluble benzdiazepine, has rapid onset and relatively short duration of action. And midazolam has prospective amnesic effect. With these advantages midazolam is popular in conscious sedation for children. This study was to reveal the dose-dependency of behavior and physiologic effects of sublingual midazolam. Sedation records were surveyed retrospectively, of which the patients admitted from April, 2005 to July, 2007. we assigned three groups according the dose of midazolam, 0.1 mg/kg, 0.2 mg/kg and 0.3 mg/kg, respectively and the behavioral evaluation was analyzed with Houpt scale statistically. Combined sublingual midazolam increased the success rate in sedation and the vital signs were stable during sedation.

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오공 약침을 병행한 경추증성 척수증 환자 1례에 대한 임상적 고찰 (Clinical Study on a Case of Cervical Myelopathy with Additional Scolopendrae Corpus Pharmacopuncture)

  • 권호영;김정환
    • Korean Journal of Acupuncture
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    • 제26권4호
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    • pp.225-235
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    • 2009
  • Objective : The purpose of this study was to report a case of a treatment with Scolopendrae Corpus Herbal-Acupuncture for one patient suffering from the Cervical Myelopathy. Scolopendrae Corpus Herbal-Acupuncture has been used as a analgesics and antispasmodics in the oriental medicine and reported to have antiinflammatory effect, sedative action and immunity enhancing activity, on one patient suffering from the Cervical Myelopathy. Methods : TThe patient was treated with Scolopendrae Corpus Herbal-Acupuncture, acupuncture, herbal medication. Scolopendrae Corpus Pharmacopuncture was administered two or three times per week and we injected 0.2~1.0 ml of Scolopendrae Corpus Pharmacopuncture to the patient's neck and both arms. The improvement of the symptoms was evaluated by JOA score(Japanese Orthopedic Association score), Nurick grading, VAS(Visual Analog Scale), reflex testing, Finger escape sign, Grip and Release test. Result : After 5 weeks of treatment, the patient's JOA score, Nurick grading and VAS were improved from 12 to 16, from grade III to grade II and from 10 to 3 respectively. The movement and power of upper and lower limbs were restored to nearly normal range.

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길경 수용액 추출물에 의한 NCI-H460 인체 폐암세포의 p53 및 pRB의 발현에 미치는 영향 (Effects of an Extract from the Roots of Platycodon Grandiflorum on the Levels of p53 and pRB in NCI-H460 Human Lung Carcinoma Cells)

  • 박봉규;감철우;허태율;박동일
    • 동의생리병리학회지
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    • 제20권6호
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    • pp.1530-1537
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    • 2006
  • Platycodi Radix, the root of Platycodon grandiflorum A. DC (Campanulaceae), commonly known as Doraji in Korea (Chinese name, 'Jiegeng', and Japanese name, 'Kikyo') has been used as an expectorant in traditional Oriental medicine. Extracts from the roots of P. grandiflorum have been reported to have wide ranging health benefits. In Korea, Platycodi Radix is also used as a food and employed as a folk remedy for adult diseases, such as bronchitis, asthma and pulmonary tuberculosis, hyperlipidemia, diabetes, and inflammatory diseases, and as a sedative. Several studies on its chemical and immunopharmacological effects including immunostimulation and antitumor activity have been performed. However, the relevant molecular mechanisms are poorly understood. Platycodi Radix, the root of Platycodon grandiflorum A. DC (Campanulaceae), commonly known as Doraji in Korea (Chinese name, 'Jiegeng', and Japanese name, 'Kikyo') has been used as an expectorant in traditional Oriental medicine. Extracts from the roots of P. grandiflorum have been reported to have wide ranging health bensfits. In Korea, Platycodi Radix is also used as a food and employed as a folk remedy for adult diseases, such as bronchitis, asthma and pulmonary tuberculosis, hyperlipidemia, diabetes, and inflammatory diseases, and as a sedative. Several studies on its chemical and immunopharmacological effects including immunostimulation and antitumor activity have been performed. However, the relevant molecular mechanisms are poorly understood. In the present study, we investigated the effects of an aqueous extract from the roots of P. grandiflorum AEPG) on the cell growth of human lung adenocarcinoma NCI-H460 cells in order to understand its anti-proliferative mechanism. AEPG treatment down-regulated the cyclin D1 expression in both transcriptional and translational levels without alteration of cyclin E. In AEPG-treated cells, the levels of cyclin-dependent kinase (C아) 6 mRNA and protein were significantly inhibited, but the levels of Cdk2 and Cdk4 were slightly inhibited by treatment of AEPG. AEPG treatment induced a marked accumulation of Cdk inhibitors, p16 and p27. However, AEPG treatment did not affect not only retinoblastoma protein (pRB) but also tumor suppressor p53 protein expression. The present results indicated that AEPG-induced inhibition of lung cancer cell proliferation is associated with the blockage of G1 phase progression through induction of Cdk inhibitors such as p16 and p27, and inhibition of cyclin D1 and Cdk6. AEPG exposure, as offered by this study, provides cluse for the mechanism of AEPG action. Taken together, these findings suggest that P. grandiflorum has strong potential for development as an agent for prevention and treatiment against human lung cancer.

Flavonoid in Clover Honey Exerts a Hypnotic Effect via Positive Allosteric Modulation of the GABAA-BZD Receptor in Mice

  • Han, Kyoung-Sik;Yang, Hyejin;Yoon, Minseok
    • 한국식품영양학회지
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    • 제30권6호
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    • pp.1364-1369
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    • 2017
  • There is a growing demand for natural sleep aids due to various side effects of long-term administration of pharmacological treatments for insomnia. Honey has been reported to exhibit numerous potential health benefits, and it is hypothesized that honey may favorably affect insomnia treatment. Therefore, this study was performed to investigate the possible hypnotic effect of clover honey (CH) and to determine its in vivo mechanism. The total flavonoid content (TFC) of CH and fractions extracted with ethylacetate (EtOAc) and $H_2O$ was measured. The pentobarbital-induced sleep test using $GABA_A$-benzodiazepine (BZD) agonists and antagonists was conducted to evaluate the potential mechanism of action behind the sedative-hypnotic activity of CH in mice. The results showed that administration of 500 and 1,000 mg/kg of CH significantly (p<0.01) reduced the sleep latency to a level similar to that of diazepam (DZP, 2 mg/kg), and 1,000 mg/kg of CH significantly (p<0.01) prolonged the sleep duration, which was comparable to that of DZP (2 mg/kg). Administration of the EtOAc fraction with a higher TFC significantly reduced the sleep latency at 50 to 200 mg/kg and prolonged the sleep duration at 100 to 200 mg/kg, which were comparable to those after administration of DZP (2 mg/kg). However, co-administration of CH and EtOAc with flumazenil, a specific $GABA_A-BZD$ receptor antagonist, blocked the hypnotic effect. Our findings suggest that the hypnotic activity of CH may be attributed to allosteric modulation of $GABA_A-BZD$ receptors. The TFC of CH is expected to be a key factor that contributes to its hypnotic effect.

오공(蜈蚣)의 항산화효과에 관한 연구 (Antioxidative Effects of Scolopendra subspinipes)

  • 최용건;이동웅;김근우;구병수
    • 동의신경정신과학회지
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    • 제19권3호
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    • pp.129-142
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    • 2008
  • Objective: The purpose of this study was to evaluate the antioxidative effects of the extract of Scolopendra subspinipes which has been used mainly for detoxication in the oriental medicine and reported to have sedative action, antiinflammatory effect, antihypertensive property and immunity enhancing activity. Method: Inhibitory activities on oxygen radical generating enzymes (aldehyde oxidase and xanthine oxidase) and increasing activities on oxygen radical scavenging enzymes (superoxide dismutase, glutathione peroxidase, glutathione-S-transferase) were investigated. Furthermore, the content of glutathione in the mouse brain, DPPH radical scavenging activity and also anti-lipid peroxidative effects in vivo and in vitro were estimated. Results: The extract showed weak inhibitory effects on the activities of aldehyde oxidase and xanthine oxidase which are oxygen radical generating enzymes. The extract inhibited lipid peroxidation with 26.1% against control group at 500 mg/kg in vivo and with 11.2% against control group at 10 mg/kg in vitro in a dose-dependent manner, which means this drug may protect radical-induced cell damages. The extract showed dose-dependently the scavenging effect on DPPH radical with 24.8% activity at 10 mg/ml in vitro. The extract enhanced the activities of superoxide dismutase, glutathione peroxidase and glutathione-S-transferase, which are oxygen radical scavenging enzymes, with 28.9%, 22.3% and 23.1%, respectively at 500mg/kg in vivo. Finally, this extract strongly increased the glutathione content in the mouse barin. Conclusion: Above results indicated that Scolopendra subspinipes can be useful for the protection or treatment of some diseases caused by reactive oxygen species.

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원지(遠志)가 NMDA로 유발된 선경세포 손상에 미치는 효과 (A Study on the Protective Effects of Polygalae Radix on Neurotoxicity Induced by N-methyl-D-aspartic acid(NMDA))

  • 이수배;성낙술;이영종
    • 대한본초학회지
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    • 제20권2호
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    • pp.115-125
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    • 2005
  • Objectives : Polygalae Radix (PR) from Polygalae tenuifolia (Polygalaceae) has been clinically used as a sedative, anti-inflammatory, and anti-bacterial agent. To extend pharmacological effects of PR in the central nervous system (CNS) on the basis of its CNS protective effect, the present study was conducted to identify the effect of PR, whether it shows the neuroprotective action against excitatory neurotoxicity. Methods : To identify the protective effect of PR to excitatory neuro-toxic agent, the present study was focused on the PR effect on cell death, that was caused by applying NMDA to nerve cell, elevation of $(Ca^{2+})_i$, releasement of glutamate, and ROS generation. Result : 1. PR methanol extract, at the concentration range of 0.05 to 5 g/ml, significantly inhibited NMDA (1 mM)-induced neuronal cell death as well as MK-801 (non competitive NMDA antagonist). 2. PR methanol extract $(0.5\;{\mu}g/ml)$ inhibited NMDA (1 mM)-induced elevation of cytosolic calcium concentration $[Ca^{2+}]_i$. NMDA application in the presence of MK-801 $(10\;{\mu}M)$ failed to produce the increase of $[Ca^{2+}]_i$ through all the measurement time. 3. PR methanol extract $(0.5\;{\mu}g/ml)$ inhibited the NMDA-induced elevation of glutamate release. Also, MK-801 showed similar protective effects. 4. PR methanol extract $(0.5\;{\mu}g/ml)$ inhibited the NMDA-induced elevation of ROS generation. Also, MK-801 showed similar protective effects. Conclusion : The present study provides the availability of PR to exert its protective effect on the neuronal cell death in various neurodegenerative pathophysiological conditions.

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Protection Against Electroshock- and Pentylenetetrazol-induced Seizures by the Water Extract of Rehmannia glutinous can be Mediated through GABA Receptor-chloride Channel Complexes

  • Kim, Mikyung;Kim, Hee Jin;Kim, Sung Mok;de la Pena, June Bryan;dela Pena, Irene Joy;Botanas, Chrislean Jun;Woo, Taeseon;Lee, Yong Soo;Ryu, Jong Hoon;Cheong, Jae Hoon
    • Natural Product Sciences
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    • 제23권1호
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    • pp.40-45
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    • 2017
  • Epilepsy is a brain disorder that affects millions of people worldwide. It is characterized by recurrent and unpredictable seizures that are usually controlled with antiepileptic/anticonvulsive drugs. However, most antiepileptic drugs produce various side effects such as tolerance and sedation. Thus, there is a growing interest for alternative anticonvulsive drugs, preferably from natural or herbal sources. In this study, we evaluated the anticonvulsive effects of Rehmannia glutinosa (RG). The anticonvulsive effect of RG extract was evaluated using electroshock- and chemical-induced seizure tests in mice. To identify its probable mechanism of action, the effects of RG extract on $Cl^-$ influx was measured in vitro. We found that RG extract has anticonvulsive effects against electroshock-induced seizures, as indicated by an increased seizure threshold in mice. The RG extract also decreased the percentage of seizure responses induced by the GABAergic antagonist, pentylenetetrazole. These results suggest that the anticonvulsive effects of RG extract are mediated through a GABAergic mechanism. In support of this mechanism, our in vitro test showed that RG extract increases intracellular $Cl^-$ influx. Furthermore, RG extract did not show sedative and/or muscle relaxant effects in the open-field and rota-rod tests. Altogether, these results confirm that RG extract could be a herbal anticonvulsant and a potential alternative for clinical use.