• Proceedings of the PSK Conference
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• 2000.04a
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• pp.70-81
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• 2000

DA-5018 is a synthetic capsaicin derivative under development as a non-narcotic a analgesic ag$\varepsilon$nt. DA-50 18 showed a potent analgesic activity against acute and chronic pain m model(Tablel, 2.), but it had a narrow margin of safety. DA-5018 did not bind to opioid(${\kappa}, {\delta}, {\mu}$), NKl, CGRP receptors in vitro and its analgesic effect was not antagonized by naloxone, a and it did not develop analgesic tolerance. In addition DA-5018 had no inhibitory effects against c cyclooxygenase and 5-lipooxygenase activities. DA-5018 significantly increased the relcase of substance P from the slices of the rat spinal cord. These results suggest that DA-50 18 is not a narcotic nor aspirin-like analgesic and the release of substance P is one of analgesic mechanism of action of DA-5018. We found that DA-5018 was almost ten times more potent and was at l least IOO-times less irritable compared to capsaicin. Accordingly development of topical formula was adopted. Topical formula was desiged and screened by flux test of DA-5018 using hairless mouse skin and several formulas were selected. With these topical formulas we a assessed the analgesic efficacy and carried out the toxicity, skin irritation and pharmacokinetic studies. In streptozotocin-induced hyperalgesic rat and 50 % galactose-fed hyperalgesic rat as diabetic pain models, DA-5018 cream increased the pain thresh이ds up to 77.0% and 24.4% respectively, while Zostrix-HP(capsaicin cream) incr$\varepsilon$as cd by 65.9% and 21.0%. DA-5018 c cream showed a good analgesic effect as welI in FCA-induced arthritic rat. DA-5018 cream did not show any toxicological signs in acute and chronic toxicity test and had little skin irritation in car swclIing and scratching t$\varepsilon$st. Pharmacokinetics of DA-50 18 were studied after topical application of ${14}^C$-Iabelled or unlabelIed DA-5018 cream. Plasma and skin concentrations c except applied skin wcre below the dctection limit and after 7-day cummulative application, plasma concentrations were also below detection limit DA-50 18 may have an advantag$\varepsilon$ ov$\varepsilon$r c capsaicin and is now being developed as a topical agent for the treatment of pains. DA-50 18 cream was approved for Korean IND and is now under a Phase II clinical study for arthritic pain a after finising Phase I study. DA-50 18 was also liscensed out to Stiefel Company in America in

• Natural Product Sciences
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• v.9 no.4
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• pp.256-259
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• 2003

The pet ether extract of Caesalpinia pulcherrima, leaves was studied for its antinociceptive, anti-inflammatory and antipyretic property. The extract at doses of 50 and 200 mg/kg, p.o., significantly (p<0.05) reduced the number of writhing induced by acetic acid and inhibited the late phase (20-30 min) in formalin test in mice. The extract failed to increase the pain threshold level in tail immersion test in mice. In carrageenan induced paw edema in rats and in acetic acid induced increase in vascular permeability test in mice, the extract (50-600 mg/kg, p.o.) failed to produce any significant activity. While in cotton pellet granuloma test, the extract at doses of 200 and 600 mg/kg (p.o.) significantly (p<0.05) reduced the granuloma formation and was comparable to reference drug, dexamethasone. In ethylpheylpropiolate ear edema test 0.5 mg and 1 mg/ear application of extract significantly (p<0.05) inhibited ear edema. In yeast induced hyperthermia in rats, the extract did not produce any reduction in temperature. The results suggest that the extract acts peripherally to produce analgesic action and anti-inflammatory activity through steroidal mechanism.

• The Korea Journal of Herbology
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• v.27 no.5
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• pp.37-44
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• 2012

Objectives : The present study was undertaken to determine whether the ethanol extact of Citri Pericarpium (CP, Pericarp of Citrus unshiu Markovich, Rutaceae) is effective against atopic dermatitis according to it's storage period. Methods : To evaluate antiallergic effect of CP and OCP (Old Citri Pericarpium) evaluated in vivo their inhibitory effects against passive cutaenous anaphylaxis (PCA) reaction induced by IgE-antigen complex and scratching behaviors by compound 48/80. The Anti-atopic effects were measured by contact dermatitis, prurient animal model and PCA reaction. Contact dermatitis in mice as a model of the Type IV reaction caused by Oxazolone. Results : The results showed that anti-pruritus effects, analgesic effects of CP was depends on its hesperetin contents. And It also showed that keep longer in storage appeared to be higher in hesperetin contents. Both CP and OCP(Old CP) have a dose-dependent analgesic action in acetic acid induced writhing syndrome. OCP Potently inhibited PCA reaction in mice, although OCP weakly inhibited in long term contact dermatitis model in mice. Conclusions : These results suggest that the Proportional to the storage period, Citri Pericarpium possesses analgesic effects and anti-allergic effects.

• Korean Journal of Pharmacognosy
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• v.14 no.4
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• pp.178-192
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• 1983

Polygalae Radix was used as diuretics, analgesics and expertorants in oriental medicine. The root of Polygala tenuifolia Willd. (Polygalaceae) is comprised saponin (Onjisaponin A,B,C,D,E,F and G) polygalitol, onsitin and sugars. The pharmacological action of crude Polygala-saponin (PS) obtained from the roots are studied. The following results were obtained; 1) The median lethal dose $(LD_{50})$ of PS in mice is presented 71.1mg/kg s.c. and 694. 5mg/kg p.o.. 2) PS demonstrated diuretic action of relatively long acting duration in mice. 3) The diuretic mechanism of PS was found due to inhibitory effect of renal tubular reabsorption of electrolytes and glomerular vascular dilatation. 4) The group, administered simultaneously PS and cefadroxil monobydrate was significantly increased with PS alone group on diuretic action. Synergistic effect cefadroxil monohydrate on the diuretic action of PS seems due to competitive inhibition of plasma protein binding with PS. 5) PS demonstrated analgesic action by the acetic acid stimulating method and Randall-Selitto test in mice. 6) PS presented antipyretic action against febrile treated with the typhoid vaccine. 7) PS was significantly prolonged against the hypnotic duration of pentobarbital in mice. 8) Onset time convulsion and death induced by picrotoxin and strychnine in mice were not delayed. According to the above results, the PS was identified as a pharmacological active component obtained from roots of Polygala tenuifolia Willd.

• Journal of Physiology & Pathology in Korean Medicine
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• v.24 no.5
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• pp.827-830
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• 2010

The purpose of this research was to investigate the pharmacological effects of Dansameum (DSE) water extract which is composed with Salviae Radix, Santali Lignum and Amomi Semen. DSE was administered orally at the concentartion of 100 and 500 mg/kg. DSE decreased the writhing syndrome induced by acetic acid and the permeability of evans blue into peritoneal cavity. Also, DSE inhibited the production of nitric oxide from murine macrophages. Futhermore, DSE protected the liver injury induced by galactosamine in vitro system and $CCl_4$ in vivo system. These results suggest that DSE has a diverse effects such as analgesic action, inflammatory action and liver protective action.

• Korean Journal of Pharmacognosy
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• v.14 no.1
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• pp.9-16
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• 1983

Experimental studies were implemented to evaluate clinical efficacy of 'Daeshiho-Tang' and to validate Oriental medicine description of the recipe which has been widely used in metabolic diseases and febrile diseases. Following results were obtained; 1. Suppressive action was shown on convulsion due to cerebrocortical causes but no such action was noted either myelic or diencephatic causes in mice. 2. Analgesic and antipyretic actions were recognized in mice, rats and rabbits. 3. Antispasmodic actions were recognized on contraction of the ileum induced by $BaCl_2$ and histamine in mice and guinea-pigs. 4. Transport accelerating action of the small intestine was gained in mice.

• YAKHAK HOEJI
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• v.46 no.5
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• pp.348-351
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• 2002

In this report, anti-inflammatory, analgesic and cytotoxic effects of the water extracts of Pini Resina, which has been as an additive to oral hygienic products together with sodium chloride in community, were investigated. The water extracts of Pini Resina, pretreated Pini Resina and Ramus Mori Albae-added Pini Resina all showed relatively low cytotoxicity. All samples showed concentration-dependent increase in electron-donating capacity to DPPH, especially, Ramus Mori Albae-added Pini Resina was the highest in the extent. Arachidonic acid release from the cell membrane was significantly inhibited by the presence of the samples above, among those, Ramus Mori Albae-added Pini Resina was the most effective in the inhibitory action of the release.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.303-303
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• 1994

ICV infusion of morphine (MOR) produces strong analgesia in man and animals. The analgesic effect is thought to be mediated by the centrifugal inhibtory control, But neural mechanisms of the analgesic effect of ICV morphine are not well understood. For example, in the previous studies, ICV morphine does not inhibit nociceptive transmission in the spinal cord. On the contrary, ICV MOR often excites activity of dorsal horn neuron in the spinal cord. In the present study, we found that ICV MOR had dust actions on activity of dorsal horn neuron that it produced both inhibition and excitation of dorsal horn neurons. Since MOR exerts i Is action via three different types of opioid receptors, we further sought to investigate if there are differential effects of opioid receptor agonists on dorsal horn neurons when administered ICV.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.339.3-340
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• 2002

Capsaicin is hot taste ingredient of chili pepper and was isolated in 1876 and in 1919 its structure is sympathized compound. induces pain and when persistently dosed. the fact will bring insensible condition to other chemical and mechanical thermal stimulation by incapacitating sensory neuron is known. The analgesic effect by desensitization of such capsaicin is differ from the mechanism by analgesic action by opiate receptor of the existing analgesia or by prostaglandin mediation and the efficacy was known as similar with morphine. (omitted)

• YAKHAK HOEJI
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• v.35 no.2
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• pp.123-130
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• 1991

Effects of Allolobophora caliginosatrapezoides (Ac) polysaccharide fractions on the inflammation and hypersensitivity were studied in vivo. It showed that Ac polysaccharide fractions have the significant inhibitory activities of inflammation and hypersensitivity; They inhibited significantly the carrageenin-induced paw edema and acetic acid-induced writhing syndrome. They also inhibited significantly the Arthus reaction and delayed hypersensitivity in the sheep red blood cell-sensitized mice in accordance with the inhibition of haemaglutinin titer, haemolysin titer, plaque-forming cells and rosette-forming cells. They also improved markedly the oxazolone-induced dermatitis in rats dose-dependently. As the above results, it exhibited that Ac polysaccharide fraction inhibited not only humoral immune response, but also cell-mediated immune response. It seemed that methanol and ether extracts have also another physiological active agents.