• Natural Product Sciences
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• 제18권4호
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• pp.215-220
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• 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.

• Advances in Traditional Medicine
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• 제7권5호
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• pp.485-493
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• 2008

The present study was carried out to elucidate the potential of, chloroform extract of Pandanus (P.) fascicularis Lamk (Family-Pandanaceae) leaves on antinociceptive, behavioral study and anti-inflammatory effects using various animal models The dried, powdered leaves of, P. fascicularis were extracted successively with petroleum ether ($60\;-\;80^{\circ}C$) and chloroform in soxhlet apparatus. The chloroform extract (yield 21.6% w/w with respected to dry powdered plant material) was selected for all experimental procedure. Two models were employed to investigate the effects on nociception, the tail immersion and hot plate method in Swiss albino mice and anti inflammatory effect were investigated by employing the carrageenan induced rat paw edema test in. adult Wister albino rats. Behavioral study was investigated by elevated plus maze method in Swiss albino mice. Results were revealed that the PFCE was found significant antinociceptive effect (P < 0.001) at the dose levels of 100, 200 and 400 mg/kg, orally in mice and produced remarkable antiinflammatory effect (P < 0.001) at the same dose levels used in the rats. Behavioral study of the PFCE has no significant anxiolysis effect when used orally. It concludes that, PFCE possessed remarkable antinociceptive effect and anti-inflammatory effect but no anxiolytic effect on animal models.

• The Korean Journal of Pain
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• 제19권2호
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• pp.142-145
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• 2006

Background: Nitric oxide (NO) is involved in the transmission and modulation of nociceptive information at the peripheral, spinal cord and supraspinal levels. We conducted this experiment to assess the antinociceptive effects of a nonselective nitric oxide synthase (NOS) inhibitor, N-nitro-L-arginine methyl ester (L-NAME), on the modulation of pain in rats subjected to the formalin test. Methods: Formalin 5% was injected in the right hind paw after intraperitoneal (IP) injection of various doses of L-NAME (0.5 mg/kg, 1.5 mg/kg with and without L-arginine 100 mg/kg, 5.0 mg/kg). The number of flinches was measured. Results: Formalin injected into the rat hind paw induced a biphasic nociceptive behavior. IP injected L-NAME diminished the nociceptive behaviors in a dose-dependent manner during phases 1 and 2. The concomitant injection of L-arginine reversed the antinocipetive effect of L-NAME. Conclusions: The data demonstrates that a nonselective NOS inhibitor, L-NAME, possesses antinociceptive properties in rats subjected to the formalin test, and the antinociceptive effect of L-NAME is reversed by the concomitant administration of L-arginine.

• 생약학회지
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• 제36권4호통권143호
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• pp.299-304
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• 2005

This study examined the antinociceptive properties of GCSB-5, a herbal formulation consisting of 6 Oriental herbs (Ledebouriellae Radix, Achyranthis Radix, Acanthopanacis Cortex, Cibotii Rhizoma, Glycine Semen, and Eucommiae Cortex) that are used in traditional medicine to treat various bone disorders, mainly of which involve analgesic processes. Peripheral and central analgesic models were established in experimental animals in order to evaluate the antinociceptive effects of the agent. GCSB-5 significantly inhibited the number of acetic-induced writhing (33.3%-34.3% inhibition at 100-600 mg/kg) but increased the pain threshold (38.0% increase at 300 mg/kg) in the Randall-Selitto test. However, GCSB-5 had no effect on the hot plate-induced nociception and hyperalgesia from the tail-pinch method. These results suggest that the antinociceptive effect of GCSB-5 may be mediated via peripheral mechanisms.

• Natural Product Sciences
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• 제9권2호
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• pp.97-101
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• 2003

This study was undertaken to evaluate the antinociceptive and antiinflammatory effects of the heartwood extract of Rhus verniciflua (Anacardiaceae) and the two major components, sulfuretin and fustin. The MeOH extract, its EtOAc-soluble portion and sulfuretin showed significant antinociceptive activity in writhing and hot plate test assays and antiinflammaory effects in carrageenan-induced hind paw edema in rats. In particular, treatment of sulfuretin with 10 mg/kg dose (i.p.) reduced writhing frequency by 48.0% (p<0.01) compared to that of a control group. Further, the treatment of sulfuretin (5, 10 mg/kg, i.p.) for 7 days prevented the carrageenan-induced hind paw edema significantly (p<0.01). The antiinflammatory effect of sulfuretin was also confirmed by microscopic observation of mast cell numbers in muscle. In addition, sulfuretin suppressed the cyclooxygenase- 2 (COX-2) activity $(IC_{50}\;=\;28.7\;{\mu}M)$ in lipopolysaccharide-activated macrophage cells. This result indicates that the inhibitory effect of sulfuretin on COX-2 may be one of the antinociceptive/antiinflammatory mechanism.

• 한국자원식물학회지
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• 제19권6호
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• pp.660-664
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• 2006

The aerial part of Siegesbeckia pubescens (Compositae) has been used to treat rheumatoid arthritis and hypertension in the Oriental medicine. This crude drug has been used without process (SP-0) or with three times-process of steaming and drying (SP-3) or the nine times of that process (SP-9). To search for the antinociceptive anti-inflammatory components from this crude drug, activity-directed fractionation was performed on this crude drug. Since the $CHCl_3$ extract was shown to have a more potent effect than other extracts, it was subjected to silica gel & ODS column chromatography to yield two diterpene compounds (1). Compound 1 was structurally identified as ent-16 (H, 17-hydroxykauran-19-oic acid, which were tentatively named siegeskaurolic acid A. A main diterpene, siegeskaurolic acid A was tested for the antiiflammatory antinociceptive effects using both hot plate- and writhing anti-nociceptive assays and carrageenan-induced anti-inflammatory assays in mice and rats. Pretreatment with siegeskaurolic acid A (20 and 30mg/kg) significantly reduced the stretching episodes, action time of mice and carrageenan-induced edema. These results support that siegeskaurolic acid is a main diterpene responsible for antinociceptive and antiiflammatory action of S. pubescens. In addition, the assays on SP-0, SP-3 and SP-9 produced the experimental results that SP-9 had more significant effects than other two crude drugs. These results suggest that the processing on the original plant may lead to the higher pharmacological effect.

• Bulletin of the Korean Chemical Society
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• 제31권11호
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• pp.3265-3271
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• 2010

A series of 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazolines have been synthesized to meet the structural requirements essential for anti-inflammatory and antinociceptive properties. The synthesized series of heterocycles, 6,7,8,9-tetrahydro-5H-5-hydroxyphenyl-2-benzylidine-3-substituted hydrazino thiazolo (2,3-b) quinazoline by the reaction of 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl thiazolo (2,3-b) quinazolin-3(2H)-one with appropriate hydrazine hydrate and ketones/aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid as presented in Scheme 1. Their antinociceptive activity were evaluated by tailflick technique, anti-inflammatory was evaluated by carrageenan-induced paw edema test and their ulcerogenicity index determined by reported protocol. The compounds exhibited the lowest ulcer index ($0.51{\pm}1.63$, $0.48{\pm}1.28$ and $0.50{\pm}1.53$, respectively. The 6,7,8,9-tetrahydro-5H-5-hydroxy phenylhydroxy-2-benzylidine-3-(N'-3-pentylidenehydrazino) thiazolo (2,3-b) quinazoline and 6,7,8,9-tetrahydro-5H-5-hydroxy phenyl-2-benzylidine-3-(N'-2-pentylidene-hydrazino) thiazolo (2,3-b) quinazoline exhibited the most potent antinociceptive and anti-inflammatory activities.

• Biomolecules & Therapeutics
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• 제5권2호
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• pp.211-214
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• 1997

In the present study, we investigated the mechanisms of antinociceptive effect and thermoregulatory action of capsaicin in guinea pigs. The administration of capsaicin (5 mg/kg, s.c.) caused a significant decrease in frequency of eye wiping, an indicative of nociceptive threshold. This antinociceptive effect of calsaicin was abolished by co-administration of capsazepine (30 mg/kg, s.c.) with capsaicin, suggesting the involvement of a vanilloid receptor in the antinociceptive action of capsaicin. The administration of capsaicin (1 mg/kg, s.c.) produced a significant decrease in body temperature of guinea pigs. The maximum decrease in body temperature by 2 degrees was shown 1 hour after the treatment, and this decrease was not reversed by coadministration of capsazepine. In conclusion, it is suggested that the mechanism of action of capsaicin-induced thermoregulation involves different pathways from that of capsaicin-induced antinociception.

• Advances in Traditional Medicine
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• 제9권4호
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• pp.320-325
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• 2009

The pharmacological interest coupled with traditional uses (antidiarrhoeal, antiseptic, analgesic etc) prompted us to test for anti-inflammatory, antinociceptive and diuretic activitities of Trema (T.) orientalis Linn. The crude methanolic leaves extract of T. orientalis was investigated for its possible anti-inflammatory activities using carrageenin induced rat paw edema model and cotton pellet implantation method in mice. Then the extract analyzed for its antinociceptive activities by acetic acid induced writhing model in mice. The extract possessed significant anti-inflammatory activity in both models at the doses of 200 and 400 mg/kg body weight of mice. Moreover, the extract showed significantly reduced the number of acetic acid-induced abdominal constriction in mice of 200 and 400 mg/kg body weight. The extract also showed positive diuretic activity in albino mice.

• Advances in Traditional Medicine
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• 제7권3호
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• pp.274-279
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• 2007

The crude ethanol extract of leaves of Sonneratia caseolaris Linn. (Sonneratiaceae) was screened for its antinociceptive and antidiarrhoeal activities. The extract produced significant writhing inhibition in acetic acid induced writhing in mice at dose of 250 and 500 mg/kg body weight (P<0.01) comparable to the standard drug diclofenac sodium at the dose of 25 mg/kg of body weight. When tested for its antidiarrhoeal effects on castor oil induced diarrhea in mice, it increased mean latent period and decreased the frequency of defecation significantly at the dose of 500 mg/kg body weight (P < 0.05) comparable to the standard drug loperamide at the dose of 50 mg/kg of body weight. The overall results tend to suggest the antinociceptive and antidiarrhoeal activities of the extract.