• Archives of Pharmacal Research
• /
• 제19권3호
• /
• pp.246-247
• /
• 1996

In the previous reports (Park et al., 1991, and 1993), we described the synthesis and analgesic effects of various homovanillic amides as analogs of capsaicin. In the study, we tried to enhance the analgesic actvity of capsaicin by structural modification. Our study has been performed in three directions. First, the amide bond of capsaicin was transposed. Second, a phenyl ring was introduced to replace a double bond of capsaicin. Finally, aminoethylation was performed on 4-hydroxy group of capsaicin to improve oral bioavailability. These studies have led to N-(3-phenylpropyl)homovanillic amide 2 which has high analgesic activity. Our continuing efforts in this area have focused on the introduction of various substituents on the phenyl ring of 2 as well as their pharmacological studies. We report herein the synthesis of homovanillic amide derivatives and their analgesic activity.

• Advances in Traditional Medicine
• /
• 제8권2호
• /
• pp.196-203
• /
• 2008

The methanol extract of the root of Artanema sesamoides Family Scrophuilariaceae (MEAS) was investigated for possible analgesic and anti-inflammatory effects in animals. Three models were used to study the extract effects on nociception, which were acetic acid-induced writhing response, hot-plate method and the tail flick test in mice. The antiinflammatory effects were evaluated using carrageenan, dextran, histamine and serotonin induced rat paw oedema (acute) and cotton pellet induced granuloma (chronic) models in rats. Results of the study revealed that the extract exhibited significant (P < 0.001) analgesic effect at a dose of 50, 100 and 200 mg/kg b.w p.o in mice in all the models. In acute model, the MEAS also exhibited significant (P < 0.001) antiinflammatory effect in all the above mentioned doses. In chronic model (cotton pellet induced granuloma) the MEAS 200 mg/kg and indomethacin 10 mg/kg showed that inhibition of granuloma formation 25.0% and 47.7% respectively (P < 0.001). The MEAS and indomethacin were effectively preventing the transudation of the fluid. Thus, the present study revealed that the methanol extract of the root of Artanema sesamoides exhibited significant analgesic and antiinflammatory activity.

• 약학회지
• /
• 제51권6호
• /
• pp.508-516
• /
• 2007

Thymus magnus is an endemic (Ulleung Island) species in Korea. This plant is used as diaphoretics and carminatives in traditional medicine. In the literature, few scientific assays were realized on this species, such as antibiotic (Streptococcus pneumoniae, Staphylococcus aureus, Salmonella enteritidis, and S. typhimurium) and antifungal activities. In order to clarify whether essential oil of T. magnus have pharmacological effects, anti-inflammatory, sedative, anti-depressant, analgesic, and sleep-prolonged effects were investigated using animal models. From this study, the following conclusions were attained; 1) Essential oil of T. magnus did not show any acute toxicity on mice when orally administered at the dose of 2-3 g/kg body weight. 2) Essential oil of T. magnus possessed strong anti-inflammatory activity, similar to that of a positive control prednisolone. 3) Essential oil of T. magnus had excellent analgesic activity, comparable to that of aspirin. 4) The essential oil of T. magnus possessed strong sleep-prolonged effect on pentobarbital induced-sleep test in mice model. 5) In the hot plate test, the essential oil of T. magnus had moderate effect. 6) And the essential oil of T. magnus had no significant effects in forced-swimming test and open-field test.

• 한국식품영양과학회지
• /
• 제23권4호
• /
• pp.672-672
• /
• 1994

• 약학회지
• /
• 제37권6호
• /
• pp.631-637
• /
• 1993

In the previous report, it was described that the butanol fraction of the root bark extract of Aralia elata had potent antigastritic and antiulcerative effects in rats, In this pharmacological profile, the fraction revealed low acute toxicities in mice and rats, no central nervous system activities, moderate analgesic action, weak inhibitory action in carrageenin edema of rats and no direct effects on isolated smooth muscles of rats and guinea-pigs. Slight lowering of blood pressure as given i.v. in rabbit was observed.

• Archives of Pharmacal Research
• /
• 제12권3호
• /
• pp.149-153
• /
• 1989

Seven 2, 3-diphenyl-5-methoxyindole derivatives were synthesized. The effect of structural variation of these molecules on biological activities was examined. None of the tested compounds was found to be toxic up 5 gm/Kg body weight. Four compounds demonstrated smooth muscle relaxant effects and one showed a persistent hypotensive effect. Only the parent compound, 2, 3-diphenyl-5-methoxyindole, showed a significant analgesic effect.

• 동의생리학회지
• /
• 제14권2호통권20호
• /
• pp.127-137
• /
• 1999

The current experiment was carried out to investigate the analgesic effects of several herbal drugs in acetic acid - induced pain model. In a single drug group : after administration of herbal drugs(1g/kg or 3g/kg) orally for 30 minutes, 1% acetic acid $(250{\mu}l)$ was administered into abdominal cavity of mouse. And then the number of times of writhing response was measured for 30 minutes. In a combination drug group : after administration of herbal drugs (1g/kg and it's compound 2g/kg) orally for 30 minutes, 1% acetic acid $(250{\mu}l)$ was administered into abdominal cavity of mouse. And then the number of times of writhing response was measured for 30 minutes. The results were summarized as follows; 1. Water extracts of Akebiae caulis(木通) and Stephaniae tetrandrae radix(防己) decreased significantly the number of writhing response. 2. Methanol extracts of Achyranthis bidentatae radix(牛膝), Carthami flos(紅花), Akebiae caaulis(木通), Stephaniae tetrandrae radix(防己), Myrrha(沒藥), Corydalidis tuber(玄胡索) and Persicae semen(桃仁) decreased significantly the number of writhing response. 3. Water extracts of Achyranthis bidentatae radix(牛膝) plus Akebiae caulis(木通), Achyranthis bidentatae radix(牛膝) plus Stephaniae tetrandrae radix(防己) and Achyranthis bidentatae radix(牛膝) plus Ledebouriellae radix(防風) decreased the number of writhing response significantly. 4. Methanol extracts of Achyranthis bidentatae radix(牛膝) plus Myrrha(沒藥), Achyranthis bidentatae radix(牛膝) plus Stephaniae tetrandrae radlx(防己) and Achyranthis bidentatae radix(牛膝) plus Ledebouriellae radix(防風) decreased the number of writhing response significantly.

• 한방안이비인후피부과학회지
• /
• 제3권1호
• /
• pp.41-57
• /
• 1990

In order to investigate the effects of Hwang Keum Jag Yag Tang (HJT) water extract on the plasma cortisol concentration in the rabbit and on the analgesic effect in the mouse were administered. The results were summarized as follow: 1. Intravenous administration of HJT water extract at the dose of 0.2ml/kg remarkably increased plasma cortisol concentration after two hour. 2. Intravenous administration of HJT water extract at the dose of 0.4ml/kg significantly increased plasma cortisol concentration after one hour. 3. Intravenous administration of HJT water extract at the dose of 0.2ml/kg, all the experimental period, significantly increased plasma sodium concentration. 4. Intravenous administration of HJT water extract at the dose of 0.4m1/kg significantly decreased plasma potassium concentration. 5. Intravenous administration of HJT water extract at the dose of 0.2ml/kg and 0.4ml/kg, all the experimental period, significantly decreased plasma calcium concentration. 6. The analgesic effect of HJT water extract showed inhibitory effect more than at 0.1ml/20g. According to the results, Hwang Keum Jag Yag Tang water extract remarkably increased plasma cortisol concentration and showed analgesic effect.

• 생약학회지
• /
• 제16권1호
• /
• pp.31-35
• /
• 1985

Intraperitoneal administration of ginseng butanol fraction(GBF) to chronic morphinization in male Sprague-Dawley rats inhibited the development of tolerance to the analgesic effect and hyperthermic action of morphine. Rats were rendered tolerant to morphine by subcutaneous multiple morphine injections for a period of 8 days. The development of tolerance was evidenced by the decreased analgesic response to morphine and inhibition of tolerance by the greater analgesic response. Concomitant administration of morphine with GBF blocked the tolerance to the hyperthermic effect of morphine as evidenced by elevation of body temperature by morphine. Dopamine receptor sensitivity was enhanced in morphine tolerant rats as measured by apomorphine induced in spontaneous motor activity. GBF administration also blocked dopamine receptor supersensitivity induced by chronic morphinization.

• 생약학회지
• /
• 제17권3호
• /
• pp.223-231
• /
• 1986

Experimental studies were conducted to investigate for the effect of Mahaengkamsuk-tang on analgesic, antipyretic, antiinflammatory, secretion of respiratory tract, isolated ileum. Mahaengkamsuk-tang was composed of Ephedrae Herba, Armenicae Semen, Glycyrrhizae Radix, Gypsum Fibrosum. The following results has been obtained; analgesic and antipyretic actions were obtained. Anti-inflammatory effects in the paw edema induced by 1% dextran was significantly shown in rats. Spontaneous motilities of isolated ileum of mice were strongly suppressed, and contractions of isolated ileum of mice induced by acetylcholine chloride, barium chloride and histamine were remarkably inhibited. Expectorant effect was shown in rabbits. Continuous hypotensive action was seen.