• Archives of Pharmacal Research
• /
• v.27 no.12
• /
• pp.1194-1201
• /
• 2004

Michael addition of certain nucleophiles on ${\alpha}$ , ${\beta}$-unsaturated ketones 1 led to the formation of adducts 2-7 as well as the reaction of arylidene derivatives with secondary amines afforded the amino compounds 9 and 11. Also, dialkylmalonates were treated with ${\alpha}$-cyano cinnamide to afford 13. On the other hand, double Michael cycloaddition of ethylcyanoacetate or tetrachlorophthalic anhydride to the suitable divinylketone were synthesized to produce 15-17. Selected compounds (13 and 6) were screened for muscle relaxant, anticonvulsant, and sedative activities using established pharmacological models. Their activities were compared with that of phenobarbital sodium taken as standard. Compound 6 was the most potent muscle relaxant while compounds 13a and 13c offered the highest anticonvulsant activity. Meanwhile compound 13c showed the highest potentiation of phenobarbital induced sleep in mice.

• YAKHAK HOEJI
• /
• v.37 no.2
• /
• pp.143-148
• /
• 1993

The objective of this study was to evaluate the sedative activity of four aporphine alkaloids (APA) and nine cyclopeptide alkaloids(CPA), which had been isolated from the seeds (sanjoin) of Zizyphus vulgaris var. spinosus, and the fruits and stem bark of Zizyphus jujuba var. inermis. The assessment of sedative activity was carried out, employing a hexobarbital-induced sleeping time method in mice. When the relative sedative potency of sanjoinine-A(CPA) was given as one unit, those of nuciferine (APA), lysicamine (APA), chlorpromazine (positive control), and sanjoinine -Ahl (an epimer of sanjoinine-A) were 13, 6.5, 5, and 3, respectively. The sedatvie activities of other CPAs were much lower than those of sanjoinine-A and -Ahl, and other APAs were not active. On heat treatment, nuciferine and lysicamine were degraded into some artifacts which exhibited no sedative activity, while sanjoinine-A was converted into sanjoinine-Ahl which showed more potent sedative activity. These results suggested that nuciferine and sanjoinine-A were major sedative components of native sanjoin, and that sanjoinine-A and its epimeric artifact, sanjoinineAhl were the active principles of roasted sanjoin. It provides a scientific basis for heat-processing (roasting) of this Oriental medicine.

• Korean Journal of Pharmacognosy
• /
• v.16 no.2
• /
• pp.65-72
• /
• 1985

These studies were conducted to investigate the effect of 'Inchungbaek' water extract on analgesic and sedative actions, the relaxing action of isolated ileums, vasodilating action and blood pressure. The results of these studies were summarized as follows: Analgesic and sedative actions of 'Inchungbaek' were recognized in mice and rats. The relaxing action of isolated ileums were seen in mice and rabbits, antagonist action was seen acetylcholine and $BaCl_2-induced$ contraction of isolated ileums, and then recognized direct action in the ileum smooth muscle. Hypotensive and vasodilating actions due to vascular smooth muscle relaxation were noted in rabbits and cats.

• Natural Product Sciences
• /
• v.18 no.4
• /
• pp.215-220
• /
• 2012

The stem of Lindera obtusiloba (Lauraceae), has been widely used as a traditional medicine for the treatment of abdominal pain, bruise and hepatocirrhosis. In the present study, antinociceptive and sedative properties of the methanol extract of L. obtusiloba (MLO) were evaluated. MLO demonstrated strong and dose-dependent antinociceptive activities on various experimental pain models including thermal nociception and chemical nociception, compared to tramadol and indomethacin, reference drugs. In combination test using naloxone, the diminished analgesic activity of MLO was observed, indicating the relation with opioid receptor. Moreover, MLO also decreases pentobarbital-induced sleep latency and increases sleeping time suggesting its hypnotic and sedative action. The present results indicate that MLO could be used as valuable antinociceptive and sedative agent for the treatment of various diseases.

• Korean Journal of Pharmacognosy
• /
• v.12 no.4
• /
• pp.190-194
• /
• 1981

It was prevously shown that 'Kamisamhwang-Tang' had been examined for effects of the anticonvulsion, antipyretic, analgesic and sedative. To investigate the effect on cardiovascular system and antibacterial activities, pharmacological studies have been carried out with each extract. The results of this investigation were summarized as follows: 1) 'Kamisamhwang-Tang' depressed central convulsion induced by strychnine, picrotoxine and caffeine in mice. 2) Antipyretic, analgesic and sedative action were observed. 3) Hypotensive effect was observed in rabbits. 4) Antibacterial activities was observed.

• Journal of Oriental Neuropsychiatry
• /
• v.34 no.4
• /
• pp.473-485
• /
• 2023

Objectives: The purpose of this study was to report the effectiveness of the combination of Korean medicine therapy on elderly patients with delirium due to overdose of sedative-hypnotics. Methods: The patient was diagnosed with delirium, which occurred after an overdose of sedative-hypnotics. The patient received Korean Medicine treatment, including herbal medicine, acupuncture, moxibustion and psychotherapy, and other treatments. The evaluation variables to check the effectiveness of the interventions were the Korean Version of the Delirium Rating Scale-Revised-98 (K-DRS-R-98) Mini-Mental State Examination-Korean (MMSE-K) Clinical Dementia Rating (CDR) and Manual Muscle Test (MMT). Results: During the hospitalization period, the K-DRS-R-98 score decreased from 31 to 4, MMSE-K score increased from 18 to 26. CDR score decreased from 2 to 0. MMT in the Right lower extremity was improved. Normal daily activities were possible. Conclusions: Combining Korean Medicine treatments, including herbal medicine, acupuncture, moxibustion, psychotherapy, and other treatments, may help alleviate delirium.

• Journal of Life Science
• /
• v.10 no.4
• /
• pp.374-379
• /
• 2000

This study was attempted to evaluate an agonistic activity to benzodiazepine receptor of several medicinal pants, which have been used as sedatives in oriental medicine. The activities of the methanol extracts of composite preparation of oriental drugs were compared with those of the simple drugs, furthermore, the active fraction was found out from the simple preparation. Inhibitory effects of composite preparations, Cyperus rotundus/Acorus gramineus, Thuja orientalis/Euphoria longan, Thuja orientalis/Albizzia julibrissin, on the binding of ${[^3H]}$Ro15-1788, a selective benszodiazepine receptor antagonist to benzodiazepine receptor of rat cortices, were observed to be lower than those of corresponding simple preparations. These unexpected results suggest that some components of the composite druge may rather act as an obstacle, not to show the sinergistic effect. The methanol extracts of Cyperus rotundus having the highest activity were fractionated using polar and nonpolar solvents to give ethylacetate and hexane fractions, respectively. The ethylacetate fraction containing relatively polar components exhibited much higher activity than the hexane fraction, which consiste of nonpolar agonist, binding to benzodiazepine receptor. However, in the presence of GABA, this fraction inhibited ${[^3H]}$flunitrazepan binding, and these positive GABA shift supported the strong possibility of agonistic activity to benzodiazepine receptro. As a result, it may be concluded that the substance or substances with neurochemical properties as a benzodiazepine receptor agonist may contribute to the sedative property of Cyperus rotundus.

• YAKHAK HOEJI
• /
• v.44 no.1
• /
• pp.22-28
• /
• 2000

The extracts of Euphoria longan, Ziryphus jujuba, Thuja orientalis, Polygala tenuifolia, Acorus gramineus, Cyperus rotundus, Poria cocos, Uncaria rhynchophylla, and Albizzia julibrissin, which have been used as sedative drugs in Korean folk medicine, were evaluated for their effects on neurotransmission and antioxidative system in vitro. Among the tested drugs, Acorus gramineus showed most inhibitory activities on monoamine oxidase, xanthine oxidase, aldehyde oxidase, and lipid peroxidation and Uncaria rhynchophylla also inhibited most effectively GABA transaminase and DPPH radical.

• Korean Journal of Pharmacognosy
• /
• v.16 no.1
• /
• pp.18-25
• /
• 1985

Experimental studies were conducted to investigate for the effect of Tongkyu-tang on analgesic, antipyretic, sedative, anti-inflammatory, isolated ileum and anti-histamine actions. Tongkyu-Tang was composed of sixteen crude drugs including Astragali Radix, which has been used for the treatment of common cold, headache, rhinitis, nasal obstruction, rhincospasm, etc. The following results have been obtained; analgesic and antipyretic actions were obtained. Prolonged action against the hypnotic duration of pentobarbital were significantly noted in mice. Anti-inflammatory effects in the paw edema induced by 1% carrageenin and 1% dextran were significantly shown in rats. Spontaneous motilities of isolated ileum of mice were strongly suppressed, and contractions of isolated ileum of mice and guinea-pigs induced by acetylcholine chloride, barium chloride and histamine were remarkably inhibited. Antihistamine actions were noted. Considering the above experimental results, it is suggested that effects of Tongkyu-tang based on the Oriental Medical References were similarly consistent with the actual experimental results.

• Korean Journal of Pharmacognosy
• /
• v.17 no.2
• /
• pp.113-122
• /
• 1986

In order to investigate the pharmacological activities of the combined preparation of crude drugs, Chunghyulgangki-Tang was studied. Chunghyulgangki-Tang has been widely used to cerebral apoploxy, hypertension and arteriosclerosis, etc. In this study, water extract of Chunghyulgangki-Tang was conducted in attempt to investigate for analgesic, sedative, antipyretic, isolated ileum and heart, blood vessels and blood pressure action in mice, frogs, rats, guinea-pigs and rabbits. The following results were obtained; Analgesic action by the acetic acid stimulating method in mice was recognized. Sedative activities by the wheel cage method and rotor rod method in mice were shown. Prolonged action against the hypnotic duration induced by thiopental-Na was significantly noted in mice. The effect of antipyretic in endotoxin febrile rats was significantly recognized. Spontaneous motility of the isolated ilem of mice was suppressed and contractions of the isolated ileum of mice and guinea-pigs induced by acetylcholine chloride, barium chloride and histamine were remarkably inhibited. Acceleration of isolated heart motility was shown in frogs. Vaso-dilating and hypotensive actions were recognized in rabbits. According to the above results, effects based on the oriental medicinal references were approximate to the actural experimental results.