• Archives of Pharmacal Research
• /
• v.12 no.3
• /
• pp.196-200
• /
• 1989

The methanolic extract of the Rhizome of Curcuma zedoaria exhibited a significant prolongation of hexobarbital (HB)-induced hypnosis. Through liquid chromatography of an ether soluble fraction. monitoring by bioassay, three sequiterpenes, germacrone (A), curzerenone (B) and germacrone epoxide (C) were isolated as active consituents. A single treatment (100-200 mg/kg, i.p.) of each compound showed not only a significant prolongation of HB-induced sleeping time but also a significant inhibition of aminopyrine N-demethylase activity in mice, and further exhibited a typical type I binding spectra with oxidized rat hepatic cytochrome P-450 induced by phenobarbital. All of the compounds provoked a sleep episode at a subhypnotic dose of HB, implying that they possess CNS depressant properties.

• Journal of Applied Biological Chemistry
• /
• v.57 no.1
• /
• pp.17-22
• /
• 2014

Nardostachys chinensis (N. chinensis) has been used in traditional medicine as a sedative and analgesic. It has been reported that N. chinensis extract has an antioxidant activity. However, the mechanism has not been elucidated. In this study, we showed that FOXO3a was activated by N. chinensis extract. FOXO3a is a transcriptional factor that involved in cell cycle arrest, DNA repair, apoptosis, and detoxification of reactive oxygen spices (ROS). Protein level of FOXO3a was increased by N. chinensis extract whereas phospho-FOXO3a (Thr 32) was not changed. Promoter activities of target genes of FOXO3a such as MnSOD, p27, and GADD45 were increased by N. chinensis extract. Among target genes, protein level of MnSOD was increased by N. chinensis extract, and this leads to removal of ROS level in human embryonic fibroblast (HEF) cells. These results suggested that N. chinensis extract has an antioxidant activity by upregulation of MnSOD through FOXO3a activation.

• The Korean Journal of Pharmacology
• /
• v.19 no.1
• /
• pp.77-84
• /
• 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.

• Korean Journal of Pharmacognosy
• /
• v.17 no.4
• /
• pp.292-301
• /
• 1986

The combined preparations of the traditional Korean prescriptions, Sahyangsohap-won (A1) and Woohwangporyong-hwan (B1) were evaluated on pharmacological actions in rats and mice, in parallel with the preparations of their modified prescriptions (A2 and B2). The acute toxicities of the four preparations were very low of which $LD_{50}$ values were more than 4g/kg, p.o. and no systematic symptoms were found at the doses. All the preparations showed sedative action by prolongation of sleeping time induced with hexobarbital sodium. The action was more potent in the modified preparations than in the original ones. All the preparations had no anticonvulsant action both in chemoshock seizures induced by pentetrazole and strychnine and in electroshock seizure. In rat fundus preparation, A1 and A2 elicited strong contraction at the concentration of $1{\times}10^{-3}\;g/ml$ in bath, whereas B1 and B2 did neither contraction nor relaxation at the same concentration. The four preparations had no inhibitory effect against acetylcholine induced spasm. In rat intestinal preparation, the four preparations exhibited neither contraction nor relaxation. However, A1 and A2 had antagonistic effect against spasm at the concentration of $1{\times}10^{-3}\;g/ml$. Single administration of each preparation at the dose of 0.24g/kg, p.o. stimulated the secretion of pepsin in rat stomach without inciting the secretion of gastric juice. Their stimulating actions were more marked in B1 and B2 than in A1 and A2, and were more promptly exhibited in the modified preparations (A2 and B2). Accelerating action of bile secretion by single administration of each preparation was found at the dose of 0.24g/kg, p.o. in rats. All the preparations except A2 also stimulated the secretion of bile acid.

• YAKHAK HOEJI
• /
• v.53 no.6
• /
• pp.303-313
• /
• 2009

Traditionally, Cham dang-gui (Angelica gigas Nakai) is one of the most popular herbal medicines in Asian countries including Korea. A. gigas has been used as a functional food product for treatment anemia, women's health care, a sedative, an anodyne or a tonic agent. Decursin and decursinol angelate isolated from the roots of A. gigas are pyranocoumarin compounds. Recently, as the global herbal medication market is increasing, investigations about pharmacological effects of decursin and decursinol angelate are rapidly increasing. We summarized previous studies about pharmacological effects of decursin and decursinol angelate, and reviewed relation with pharmacological effects of decursin and decursinol angelate on human disorder, focused on the approach for new drug development. Pharmacological effects of decursin and decursinol angelate were classified as anti-tumor activity, anti-bacterial activity, improvements of the circulating system, inhibition of cytochrome P-450 activity, anti-inflammation activity, anti-oxidant activity and cognitive-enhancing activites. The activity of A. gigas with improvement of the circulating system may have wide therapeutic potential for circulatory diseases, including diabetes, hyperlipidemia and atherosclerosis. Also, anti-inflammation activity A. gigas may be beneficial for the treatment and prevention of asthma, atopic dermatitis and rheumatism arthritis. This relation could potentially lead to the development of herbal new drugs. In order to development a new drug containing decursin and decursinol angelate, it is also necessary to consider the safety profile, and the information in this review would contribute to development a new drug from herbal medicine.

• Advances in Traditional Medicine
• /
• v.9 no.2
• /
• pp.142-148
• /
• 2009

Anxiety disorders are one of the serious problems which need proper therapy devoid of side effects of presently available medicines. The present study evaluates the anxiolytic and sedative activity of leaf galls of Piper nigrum Linn. in Swiss Albino mice. The pet. ether, chloroform, ethyl acetate and ethanol extracts of leaf galls of Piper nigrum Linn were obtained by continuous soxhlet extraction. The prepared extracts were found to be safe up to 2000 mg/kg body weight of mice in the acute toxicity study. Each extract was assessed for anxiolytic activity in Swiss Albino mice by elevated plus Maze, open field test, rota rod test and phenobarbitone induced sleeping time test. In the Elevated Plus Maze test, the pet.ether extract and chloroform extract at a dose of 50 mg/kg b.w. orally, significantly (P < 0.01) increased the number of entries and time spent in open arm comparable with standard diazepam at the dose of 10 mg/kg. b.w. p.o. In the open field test, pet. ether extract (50 mg/kg b.w. p.o.) showed significant increase (P < 0.01) in ambulation and activity in the center. Chloroform extract (50 mg/kg b.w p.o.) was significant (P < 0.05) for both ambulation and center activity. Pet. ether extract (50 mg/kg b.w. p.o) also showed significant activity (P < 0.01) in rota rod test. All the results are comparable with standard diazepam at the dose of 1 mg /kg b.w, p.o. Moreover all the extracts showed significant (P < 0.01) increase in the phenobarbitone induced sleeping time among which pet.ether showed more prominent activity (36%) comparable with control. The results revealed that, the active pet.ether extract and chloroform extract of leaf galls of Piper nigrum Linn is worthwhile to develop the bioactive principle for anxiolytic activity.

• YAKHAK HOEJI
• /
• v.50 no.6
• /
• pp.351-357
• /
• 2006

Polygoni Radix (Polygonaceae) has been used as renal disoder hematopoietic, menstrual irregularity and antiaging in Korean folk medicine. Specially aerial parts has been used for insomnia and sedative agent. In order to investigate the efficacy of antioxidant activity on these aerial parts, the bio-activity guided fraction and isolation of physiologically active substance were performed. H$_2$O, 30%, 60%, 100% MeOH were examined antioxidant activity by DPPH method. It was revealed that 30%, 60% MeOH fractions have significantly antioxidant activity. From 60% MeOH fraction, six known flavonoid glycosides (quercetin, quercetin 3-O-${\beta}$-D-galactopyranosyl-4'-O-glucopyrano side-3'-methyl ether, quercetin 3-O-${\alpha}$-L-rhannopyranoside, quercetin 3-O- ${\alpha}$-L-rhamnopyranoside-4'-methylethor, quorcetin 3-O-${\beta}$-D-galactopyranoside, quercetin 3-O-${\beta}$-D-galactopyranoside) and 3,4-Oihydrocinnarnic acid were isolated. To investigate the antioxidant activities of each com-pounds, we measured radical scavening activity with DPPH method and anti-lipid peroxidative efficacy on low density lipo-protein (LDL) with TBARS assay and anti-acetylcholinestrase activity with Ellman's Test. Four compounds (ll, IV Vl, Vll) of quercetin glycosides showed significant activity.

• YAKHAK HOEJI
• /
• v.43 no.2
• /
• pp.251-262
• /
• 1999

In order to investigate pharmacological properties of New Wonbang Woohwangchungsimwon Pill (NSCH) and Wonbang Woohwangchungsimwon Pill (SCH), the effects of NSCH and SCH 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 effects of NSCH and SCH treatments with ischemia-induced brain damage. The ATP in brain tissue was decreased in vehicle-treated ischemic gerbils. This decrease was prevented by SCH treatment. In contrast to what was inhibited by NSCH and SCH treatments. While NSCH and SCH had no effects on the hexobarbital-induced sleeping time, they prevented the seizures induced by electric shock and strychnine. NSCH and SCH showed sedative effect in rotarod and spontaneous activity test. Furthermore, NSCH and SCH showed anti-stress effect. Our findings suggest that the pharmacological profiles of NSCH on cerebral ischemia and central nervous system are similar to those of SCH.

• YAKHAK HOEJI
• /
• v.29 no.1
• /
• pp.1-10
• /
• 1985

The ether fraction obtained from dry fruit of Cornus officinalis was investigated for the anti-inflammatory action, acute toxicity and central nervous system activities. From several pharmacological examinations, it was found that the ether fraction suppressed considerably carrageenin edema at the dose of 600mg/kg p.o. in rats, inhibited the granuloma formation in rats as given 100mg/kg p.o. for 7 days and decreased the swelling of both of complete adjuvant injected and noninjected (contralateral) paws of the rats at the dose of 100mg/kg p.o. given for 14 days. The $LD_{50}$ of the fraction are estimated to be more than 2,000mg/kg p. o. and 642mg/kg i. p. in mice. And the fraction did not show any sedative, stimulative, analgesic and anticonvulsant action but exhibited hypothermic action. These results might be concluded that the ether fraction of Corni fructus showed anti-inflammatory action in both of acute and chronic type models without any considerable central nervous depressant activity and exhibited very weak acute toxicity in mice.

• Natural Product Sciences
• /
• v.19 no.2
• /
• pp.179-185
• /
• 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.