• 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.

• The Korean Journal of Pain
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• 제22권3호
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• pp.199-205
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• 2009

Background: A major ingredient of green tea is epigallocatechin-3-gallate (EGCG), and this is known to have many beneficial effects for cancer prevention and also on the cardiovascular system and neurodegenerative diseases through its anti-oxidant, anti-angiogenic, anti-inflammatory, lipid-lowering and neuroprotective properties. Its actions on nociception and the spinal nervous system have been examined in only a few studies, and in these studies EGCG showed an antinociceptive effect on inflammatory and neuropathic pain, and a neuroprotective effect in motor neuron disease. This study was performed to investigate the effect of EGCG on acute thermal pain and the development of morphine tolerance at the spinal level. Methods: The experimental subjects were male Sprague-Dawley rats and the Hot-Box test was employed. A single or double-lumen intrathecal catheter was implanted at the lumbar enlargement for drug administration. An osmotic pump was used to infuse morphine for 7 days for induction of morphine tolerance. EGCG was injected repeatedly for 7 days at twice a day through the intrathecal catheter. Results: Intrathecal EGCG increased the paw withdrawal latency (PWL) after repeated administration for 7 days at twice a day, but this did not happen with administering on single bolus injection of EGCG. In addition, the antinociceptive effect of intrathecal morphine was not affected by co-administration with EGCG. A continuous 7-day infusion of morphine caused a significant decrease of the PWL in the control group (M + S, morphine plus saline). In contrast, intrathecal EGCG injection over 7 days blocked the decrease of the PWL in the experiment group (M + E, morphine plus EGCG). Conclusions: Intrathecal ECGC produced a weak antinociceptive effect for acute thermal pain, but it did not change the morphine's analgesic effect. However, the development of antinociceptive tolerance to morphine was attenuated by administering intrathecal EGCG.

• 한국임상수의학회지
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• 제27권6호
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• pp.663-667
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• 2010

본 연구는 설치모델 동물에서 봉독의 항통각 효과를 평가하고, 한국산 봉독과 미국산 봉독의 항통각 효과를 비교하는 것이 주된 관심이다. 한국산 봉독은 특별히 고안된 봉독 추출기를 사용하여 일벌 (Apis mellifera L.)에 전기충격을 가하여 생봉독을 수집하였으며, 수집된 생봉독은 봉독 건조기를 이용하여 봉독을 건조하였다. 미국산 봉독은 미국 시그마회사에서 상업적으로 판매되는 건조 봉독을 이용하였다. 한국산 봉독과 미국산 건조봉독을 생리식염수에 희석하여 체중 kg당 6 mg과 0.6 mg, 0.06 mg을 마우스와 랫드에 피하로 투여하여 항진통 효과를 조사하였다. 항통각 효과는 한국산 봉독과 미국산 봉독은 서로 비슷하였으며, 봉독의 용량이 많을수록 항통각 효과가 크게 나타났다. 이상의 결과에서 한국산 건조 봉독은 통증 치료에 사용될 수 있을 것으로 생각된다.

• Advances in Traditional Medicine
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• 제6권4호
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• pp.344-348
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• 2006

The crude methanolic extract of the bark of Cerbera odollam Gaertn. was evaluated for its possible antinociceptive and neuropharmacological activities in animal models. At the dose of 250 and 500 mg/kg body weight, the extract showed a significant antinociceptive effect in acetic acid induced writhing in mice comparable to that produced by aspirin, used as standard drug (P<0.001). The extract significantly reduced the time of onset of sleep (P<0.01) and potentiated the pentobarbital induced sleeping time in mice at the dose of 400 mg/kg of body weight significantly (P<0.001). It also decreased the open field score in open field test significantly at the dose of 400 mg/kg of body weight (P < 0.05). The obtained results tend to suggest the probable antinociceptive and neuropharmacological activities of the crude extract.

• Natural Product Sciences
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• 제17권3호
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• pp.256-260
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• 2011

Polygoni multiflori Ramulus, the stem of Polygonum multiflorum Thunb., has been widely used as a traditional medicine for the treatment of many diseases. Presently, antinociceptive tests of the butanolic fraction of P. multiflorum (SPB) were performed using several thermal and chemical pain models. SPB had strong and dosedependent antinociceptive activities, both thermal and chemical, compared to the reference drugs Tramadol and Indomethacin. In combination with naloxone, the analgesic activity of SPB was unchanged indicating that the antinociceptive activity of SPB was not due to action as an opioid receptor agonist. The present results indicate the potential of SPB as an analgesic agent for pain control.

• 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.

• The Korean Journal of Pain
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• 제33권4호
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• pp.318-325
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• 2020

Background: Chemotherapy-induced peripheral neuropathy (CIPN) is a major side effect of anti-cancer drugs. Neurotensin receptors (NTSRs) are widely distributed within the pain circuits in the central nervous system. The purpose of this study was to determine the role of NTSR1 by examining the effects of an NTSR1 agonist in rats with CIPN and investigate the contribution of spinal serotonin receptors to the antinociceptive effect. Methods: Sprague-Dawley rats (weight 150-180 g) were used in this study. CIPN was induced by injecting cisplatin (2 mg/kg) once a day for 4 days. Intrathecal catheters were placed into the subarachnoid space of the CIPN rats. The antiallodynic effects of intrathecally or intraperitoneally administered PD 149163, an NTSR1 agonist, were evaluated. Furthermore, the levels of serotonin in the spinal cord were measured by high-performance liquid chromatography. Results: Intrathecal or intraperitoneal PD 149163 increased the paw withdrawal threshold in CIPN rats. Intrathecal administration of the NTSR1 antagonist SR 48692 suppressed the antinociceptive effect of PD 149163 given via the intrathecal route, but not the antinociceptive effect of intraperitoneally administered PD 149163. Intrathecal administration of dihydroergocristine, a serotonin receptor antagonist, suppressed the antinociceptive effect of intrathecally administered, but not intraperitoneally administered, PD 149163. Injecting cisplatin diminished the serotonin level in the spinal cord, but intrathecal or intraperitoneal administration of PD 149163 did not affect this reduction. Conclusions: NTSR1 played a critical role in modulating CIPN-related pain. Therefore, NTSR1 agonists may be useful therapeutic agents to treat CIPN. In addition, spinal serotonin receptors may be indirectly involved in the effect of NTSR1 agonist.

• The Korean Journal of Physiology and Pharmacology
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• 제16권3호
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• pp.187-192
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• 2012

In the present study, the antinociceptive profiles of hop extract were characterized in ICR mice. Hop extract administered orally (from 25 to 100 mg/kg) showed an antinociceptive effect in a dose-dependent manner as measured in the acetic acid-induced writhing test. Antinociceptive action of hop extract was maintained at least for 60 min. Moreover, cumulative response time of nociceptive behaviors induced with intraplantar formalin injection was reduced by hop extract treatment during the 2nd phases. Furthermore, the cumulative nociceptive response time for intrathecal injection of substance P ($0.7{\mu}g$) or glutamate ($20{\mu}g$) was diminished by hop extract. Intraperitoneal pretreatment with naloxone (an opioid receptor antagonist) attenuated antinociceptive effect induced by hop extract in the writhing test. However, methysergide (a 5-HT serotonergic receptor antagonist) or yohimbine (an ${\alpha}_2$-adrenergic receptor antagonist) did not affect antinociception induced by hop extract in the writhing test. Our results suggest that hop extract shows an antinociceptive property in various pain models. Furthermore, the antinociceptive effect of hop extract may be mediated by opioidergic receptors, but not serotonergic and ${\alpha}_2$-adrenergic receptors.

• 한국약용작물학회지
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• 제18권4호
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• pp.238-243
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• 2010

In the present study, the antinociceptive profiles of Viola tricolor L. (V. tricolor L.) extract were examined in ICR mice. V. tricolor L. extract administered orally (200mg/kg) showed an antinociceptive effect as measured by the tail-flick and hot-plate tests. In addition, V. tricolor L. extract attenuated the writhing numbers in the acetic acid-induced writhing test. Furthermore, the cumulative nociceptive response time for intrathecal (i.t.) injection of substance P (0.7 ${\mu}g$) was diminished by V. tricolor L. extract. Intraperitoneal (i.p.) pretreatment with yohimbine (${\alpha}_2$-adrenergic receptor antagonist) attenuated antinociceptive effect induced by V. tricolor L. extract in the writhing test. However, naloxone (opioid receptor antagonist) or methysergide (5-HT serotonergic receptor antagonist) did not affect antinociception induced by V. tricolor L. extract in the writhing test. Our results suggest that V. tricolor L. extract shows an antinociceptive property in various pain models. Furthermore, this antinociceptive effect of V. tricolor L. extract may be mediated by ${\alpha}_2$-adrenergic receptor, but not opioidergic and serotonergic receptors.