• Title/Summary/Keyword: sedative activity

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Chemical Components of Acanthopanax divaricatus and Anticancer Effect in Leaves (개오가피의 성분 및 항암효과)

  • Yook, Chang-Soo;Rho, Young-Soo;Seo, Seong-Hoon;Leem, Jae-Yoon;Han, Dug-Ryong
    • YAKHAK HOEJI
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    • v.40 no.3
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    • pp.251-261
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    • 1996
  • Acanthopanax divaricatus Seem. is a medicinal plant growing widely through out Korea, Japan and China. The plant material of Acanthopanax spp. is used as analgesic , tonic, sedative drug as well as for the treatment of hypertension, rheumatism and diabetes. From the stem barks and root barks of A. divaricatus, diterpenoid compound was isolated and identified as pamaric acid ($C_{20}H_{30}O_2,\;mp\;164^{\circ}C$), lignan compounds were isolated and identified as d-sesamin ($C_{20}H_{18}O_6,\;mp\;123{\sim}124^{\circ}C$), eletheroside E ($C_{34}H_{46}O_{18},\;mp\;257{\sim}259^{\circ}C$), three sterol compounds were identified as ${\beta}$-sitosterol, campesterol, stigmasterol, and six fatty acid compounds were identified as stearic acid, palmitic acid, oleic acid, linolenic acid, arachidonic acid and behenic acid. And also leaves of A. divaricatus, chiisanoside were identified, one of secotriterpenoidal compound(white amorphorous powder crystal, mp $228^{\circ}C$). Anticancer activity and nephrotoxicity were tested by MTT assay. Anticancer effect of chiisanoside was much lower than that of cisplatin.

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Pharmacological Actions of New Woohwangchungsimwon Pill on Cerebral Ischemia and Central Nervous System (신우황청심원의 뇌허혈 및 중추신경계에 대한 약효)

  • Cho, Tai-Soon;Lee, Sun-Mee;Lee, Eun-Bang;Cho, Sung-Ig;Kim, Yong-Kee;Shin, Dae-Hee;Park, Dai-Kyu
    • YAKHAK HOEJI
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    • v.41 no.6
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    • pp.817-828
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    • 1997
  • In order to investigate pharmacological properties of New Woohwangchungsimwon Pill (NWCH) and Woohwangchungsimwon Pill(WCH), effects of NWCH and WCH on cerebral ischemia and central nervous system were compared. Cerebral ischemia insult was performed using unilateral carotid artery occlusion in Mongolian gerbils. The histological observations showed preventive effect of NWCH and WCH treatments with ischemia-induced brain damage. The ATP in brain tissue was decreased in vehicle-treated ischemic gerbils. This decrease was prevented by NWCH and WCH treatment. In contrast to what was seen with ATP, the lactate and lipid peroxide were both elevated in vehicle-treated ischemic gerbils. This elevation was inhibited by NWCH and WCH treatments. In central nervous system, NWCH and WCH had sedative effect in rotarod and spontaneous activity test, but no effects on the hexobarbital-induced sleeping time. And, NWCH and WCH had weak anticonvulsion effects in electric shock- and pentetrazol-induced convulsion test. NWCH and WCH increased the respiration rate, but decreased the respiration depth in rats. Furthermore, NWCH and WCH showed antistress effect. Our findings suggest that the pharmacological profiles of NWCH on cerebral ischemia and central nervous system are similar to that of WCH.

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Extracellular Signal-regulated Kinase (ERK) is Required for Water Extract of Nardostachys chinersis-Induced Differentiation in HL-60 Cells

  • Yoon, Sang-Hak;Ju, Sung-Min;Kim, Nam-Su;Park, Sung-Cheol;Park, Jin-Young;Kim, Sung-Hoon;Song, Yung-Sun;Jeon, Byung-Hun
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.20 no.5
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    • pp.1315-1320
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    • 2006
  • The root and rhizomes of Nardostachys chinensis belonging to the family Valerianaceae has been used for medicinal therapy in Korean traditional medicine. The parts have been especially used to elicit stomachic and sedative effects. Our previous studies reported that the water extract of N. chinensis has induced granulocytic differentiation inhuman promyelocytic leukemia (HL-60) cells. The Mitogen-activated protein kinases (MAPKs) are serine/threonine kinases involved in the regulation of various cellular responses, such as cell proliferation, differentiation and apoptosis. In this study, we investigated the signaling pathways on the HL-60 cell differentiation induced by N. chinensis. Activation of extracellular signal-regulated kinase (ERK) increased time-dependently in differentiation of HL-60 cells induced by N. chinersis. Activation of p38 increased slightly at 24 h after N. chinensis treatment, but activation of c-jun N-terminal kinase (JNK) was unaffected. Inhibitor of ERK (PD98059) significantly reduced NBT reduction activity induced by N. chinensis in HL-60 cells. In contrast, p38 inhibitor (SB203580) did not inhibit the cell differentiation. These results indicated that activaiton of ERK may De involved in HL-60 cell differentiation induced by N. chinensis.

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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    • v.25 no.2
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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.

Nypa fruticans wurmb Inhibits Melanogenesis via cAMP/PKA/CREB Signaling Pathway in B16 F10 Cells

  • So-Yeon Han;Hye-Jeong Park;Jeong-Yong Park;Seo-Hyun Yun;Mi-Ji Noh;Soo-Yeon Kim;Tae-Won Jang;Jae-Ho Park
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2021.04a
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    • pp.54-54
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    • 2021
  • The Melanoma Research Coalition reported melanoma affects humans of various races. This study was conducted to confirm the inhibitory effect of melanogenesis in B16 F10 cells of Nypa fruticans Wurmb of ethyl acetate fraction (NEF). Nypa fruticans Wurmb is an important component of the East Asian mangrove vegetation. It belongs to Araceae family. Traditionally, N. fruticans was used to treat various diseases such as asthma, sore throat, liver disease, a pain reliever, and can also be used as sedative and carminative. The present study, the inhibitory effect on melanogenesis was determined by Western blotting and RT-qPCR. The level of expression of tyrosinase, TRP-1, and TRP-2 is regulated by microphthalmia-associated transcription factor (MITF) and cAMP, and cAMP affects the activity of protein kinase A (PKA). Activated PKA stimulates the phosphorylation of cAMP-reactive element-binding protein (CREB) in the nucleus, thereby increasing the amount of MITF expression and enhancing melanogenesis. Western blotting and RT-qPCR analysis showed that NEF treatment decreased the expression of tyrosinase. Similarly, TRP-1 and TRP-2 levels were decreased, which were decreased significantly at compared with the untreated control. Also, NEF attenuated the IBMX mediated increase in the intracellular cAMP level and the phosphorylation of PKA. In conclusion, NEF significantly inhibited the expressions of melanogenesis through cAMP/PKA/CREB signaling pathways.

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Quercetin Inhibits the 5-Hydroxytryptamine Type 3 Receptor-mediated Ion Current by Interacting with Pre-Transmembrane Domain I

  • Lee, Byung-Hwan;Jung, Sang-Min;Lee, Jun-Ho;Kim, Jong-Hoon;Yoon, In-Soo;Lee, Joon-Hee;Choi, Sun-Hye;Lee, Sang-Mok;Chang, Choon-Gon;Kim, Hyung-Chun;Han, YeSun;Paik, Hyun-Dong;Kim, Yangmee;Nah, Seung-Yeol
    • Molecules and Cells
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    • v.20 no.1
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    • pp.69-73
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    • 2005
  • The flavonoid, quercetin, is a low molecular weight substance found in apple, tomato and other fruit. Besides its antioxidative effect, quercetin, like other flavonoids, has a wide range of neuropharmacological actions including analgesia, and motility, sleep, anticonvulsant, sedative and anxiolytic effects. In the present study, we investigated its effect on mouse 5-hydroxytryptamine type 3 ($5-HT_{3A}$) receptor channel activity, which is involved in pain transmission, analgesia, vomiting, and mood disorders. The $5-HT_{3A}$ receptor was expressed in Xenopus oocytes, and the current was measured with the two-electrode voltage clamp technique. In oocytes injected with $5-HT_{3A}$ receptor cRNA, quercetin inhibited the 5-HT-induced inward peak current ($I_{5-HT}$) with an $IC_{50}$ of $64.7{\pm}2.2{\mu}M$. Inhibition was competitive and voltage-independent. Point mutations of pre-transmembrane domain 1 (pre-TM1) such as R222T and R222A, but not R222D, R222E and R222K, abolished inhibition, indicating that quercetin interacts with the pre-TM1 of the $5-HT_{3A}$ receptor.

Manufacture of Functional Koumiss supplemented with Cichorium intybus L. (chicory) Extract - Preliminary Study

  • Kim, Dong-Hyeon;Jeong, Dana;Oh, Yong-Taek;Kim, Hong-Seok;Kim, Yun-Gyeong;Song, Kwang-Young;Kang, Il-Byung;Kim, Young-Ji;Park, Jin-Hyeong;Chang, Ho-Seok;Lim, Hyon-Woo;Chon, Jung-Whan;Kim, Hyunsook;Jeong, Dong-Kwan;Seo, Kun-Ho
    • Journal of Dairy Science and Biotechnology
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    • v.35 no.1
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    • pp.1-7
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    • 2017
  • Made using a natural mixed starter of lactic acid bacteria and yeast, Koumiss is a slightly alcoholic fermented mare's milk beverage, and a traditional drink of the nomadic populations of Central Asia. Cichorium intybus L. (chicory) is a sedative with potential cardioactive properties, and its oligosaccharides are beneficial in maintaining healthy gastrointestinal flora. Hence, in this study, we have generated a functional Koumiss containing two different concentrations of chicory. After fermentation of the Koumiss premix, the TA increased to 0.85~0.88%, and the pH decreased to ~4.3. The addition of either concentration of chicory had no significant effect on pH and TA. However, the taste, flavor, color, texture, and overall acceptability decreased in proportion to the added amount of chicory. This study has provided the first data on Koumiss supplemented with chicory. The results could be useful in developing high-quality Koumiss with functional activity using chicory, and allowing large-scale industrial production. Further studies are needed to determine if chicory root extract is beneficial for lifestyle-related diseases.

Pharmacological Studies on Human Vas Deferens -Coexistence of Adrenergic and Cholinergic Receptors, and Effect of Diazepam- (인체 정관의 약리학적 검색 -아드레날린성 및 콜린성 수용체의 공존과 Diazepam의 작용-)

  • Kim, Won-Joon;Lee, Kwang-Youn;Ha, Jeoung-Hee;Park, Tong-Choon
    • The Korean Journal of Pharmacology
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    • v.24 no.2
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    • pp.189-195
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    • 1988
  • This study aimed to investigate the autonomic innervations of human vas deferens and the effect of diazepam, a benzodiazepine sedative antianxiety drug, on the smooth muscle contractility of vas deferens. The specimens were obtained from healthy volunteers undergoing elective vasectomy with local anesthesia. The muscle preparation did not show any spontaneous contraction, but showed a good contraction induced by norepinephrine exerting the strongest response at $33^{\circ}C$. Phentolamine inhibited the norepinephrine-induced contraction concentration-dependently. Isoproterenol, a beta-adrenergic agonist evoked a considerable extent of contraction, and this contractile activity was antagonized by propranolol, a beta-adrenergic blocking agent. Acetylcholine induced a dashing contraction of the human vas deferens, and atropine, a muscarinic receptor blocking agent abolished the acetylcholine-induced contraction. Diazepam inhibited the norepinephrine-induced contraction in a concentration dependent manner. These results suggest that the smooth muscle of human vas deferens has cholinergic muscarinic and beta adrenergic receptors as well as the predominant alpha adrepergic receptor. Diazepam inhibits the motility, especially norepinephrine-induced contraction of human vas deferens.

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MANAGEMENT OF ORAL MUCOSITIS OWING TO CHEMICAL BURN BY INTOXICATION OF AGRICULTURAL CHEMICALS(GRAMOXON) : REPORT OF CASES (농약(Gramoxon)중독에 의한 화상으로 발생된 구강점막염 치험)

  • Yoo, Jae-Ha;Kang, Sang-Hoon;Kim, Hyun-Sil;Baek, Sang-Hum;You, Tae-Min;Lee, Ji-Woong;Chung, Won-Gyun;Kim, Jong-Bae
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • v.29 no.2
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    • pp.123-127
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    • 2003
  • Chemical burns onto oral mucosa which are infrequent, may result from contact with a wide variety of chemical agents. The degree of injury depends on the chemical, its concentration, duration of contact, and the natural penetrability and resistance of the tissues involved. Chemicals do not usually "burn" in that they do not cause destruction by hyperthermic activity. Rather, they damage tissue by causing coagulation of protein by one of several processes, reduction, oxidation, desiccation, corrosion, or vesication. Paraquat(Gramoxon) is the most frequently agricultural chemicals that induce the severe toxic reactions onto the organs of human body in Korea. The toxic reaction are composed of pulmonary edema and fibrosis, formation of hyaline membrane, inflammatory reaction and bleeding tendency, owing to the cell damage by the production of superoxide radicals. The contents of essential treatment in paraquat intoxication are commonly airway and breathing maintenance, gastric lavage, much hydration and diuresis, hemoperfusion and medications for the removal of the chemicals and the prevention of various complications. The sedative oral dressings, such as, orabase ointment application, warm saline gargling, lidocaine viscous gargling and oral gargling by the mixed solutions(tetracycline, prednisolone and 10% dextrose water) are important for the improvement of chemical oral mucositis and the comfortable feeding of diet. The authors managed properly two cases of oral chemical mucositis that were occurred by the incorrect use of agricultural chemicals(paraquat) and report the cases with the review of literatures about care of the chemical intoxication and oral mucositis.

Profiling of Metabolites and Proteins from Eschscholtzia californica induced by Yeast Extract (Yeast Extract로 처리된 Eschscholtzia californica의 Metabolite와 Protein의 변화)

  • Cho Hwa-Young;Park Jeong-Jin;Yoon Sung-Yong;Part Jong Moon
    • KSBB Journal
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    • v.20 no.4
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    • pp.285-290
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    • 2005
  • Benzophenanthridine alkaloids - sanguinarine, chelirubine, macarpine, and chelerythrine are produced from Eschscholtzia californica (Californica Poppy, used as a sedative by Native Americans) and most of them are derived from dihydrosanguinarine. The properties of sanguinarine are the basis of its antimicrobial activity and its use in chemosurgery and skin cancer excision. For overproduction of sanguinarine from E. californica, yeast extract was used as elicitor and the elicited cell's metabolites were checked. Sanguinarine production was increased intracelluarly about 8 times in the cell and 5 times extracelluarly. We have peformed proteomic analysis of proteins sequentially extracted from E. califormica suspended cells which were cultured with elicitor, an increase of spot intensity was seen at 24 hours following elicitation. These proteins were separated by two-dimensional electrophoresis (2-DE). We found several spots that were expected to be related to benzophenanthridine alkaloids production by comparing the production profiles of metabolites such as sanguinarine. These results demonstrate the use of metabolite analysis as a tool for detecting target proteins related to metabolites production pathway.