• Natural Product Sciences
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• 제17권4호
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• pp.303-308
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• 2011

Spirodela polyrrhiza L. Schleid. (Lemnaceae), also known as 'duckweed', is a traditional medicine in Korea. The whole plant is used to treat many diseases, including the common cold, edema, acute nephritis, and urticaria. The present study investigated antinociceptive properties of the EtOAc soluble fraction of S. polyrrhiza (ESP). The antinociceptive activities of ESP were studied using experimental models of pain, including thermal nociception methods, such as the tail immersion test and the hotplate test. Moreover, we studied chemical nociception induced by intraperitoneal acetic acid and subplantar formalin in mice. ESP exhibited dose-dependent antinociceptive activity in both thermal and chemical pain models. In a drug combination test using the opioid receptor antagonist naloxone, diminished analgesic activities of ESP were observed, indicating that the antinociceptive activity of ESP is mediated by opioid receptors.

• Journal of Dairy Science and Biotechnology
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• 제24권2호
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• pp.21-24
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• 2006

The ubiquitous presence of lactoferrin(LF) receptor in human as reported by the research group of Prof. Bo Lonnerdal, Univ. California (Suzuki, Y. A.,2001) encouraged us to search for the unknown physiological roles of Lf. Under the collaboration with Prof. Etsumori Harada, Tottori Univ., and his research group, we have found two novel biological activities of LF as the control of the lipid metabolism and the effect on the central nervous system. Relating to the lipid metabolism, LF could, in animal experiments, reduce triglyceride and total cholesterol both in blood and liver (Takeuchi, T et αl., 2003). LF increased plasms HDL-C and lowered LDL-C. In the central nervous system, LF showed anti-nociceptive activity mediated by ${\mu}$-opioid receptor in the rat spinal cord (Hayashida, K. et al., 2003). LF enhanced analgesic action of morphine synergistically via nitric oxide synthesis (Hayashida, K., et al., 2003) LF showed opioid-mediated suppressive effect on distress induced by maternal separation in rat pups (Takeuchi, T., et al., 2003).

• Advances in Traditional Medicine
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• 제3권3호
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• pp.123-128
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• 2003

Stephania hernandifolia belonging to the family Menispermaceae is the biggest storehouse of diphenylbisbenzylisoquinoline (DBBI) alkaloids. Exhaustive chemical processing of the bulb of S. hernandifolia by the application of modern separation techniques yielded a DBBI alkaloid which was identified as cycleanine using spectroscopic methods (UV, IR, $^1HNMR$. $^{13}CNMR$, Mass). Cycleanine showed significant anti-inflammatory activity against carrageenin induced paw oedema, comparable to that produced by diclofenac sodium, used as standard drug. It exhibited potent analgesic effects against chemical and thermal noxious stimuli. It was also found to possess anticonvulsive activity in the strychnine induced convulsion model.

• Archives of Pharmacal Research
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• 제22권2호
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• pp.184-188
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• 1999

A series of 4-amino Capsaincin anallogs 15, 17 and 19 were prepared to investigate the bioisosteric effect of 4-amino group, and all these compounds exhibited moderate or weak potency from their analgesic test. From our previous results and others, 4-hydroxyl group as well as 3-methoxy substituent could be crucial for high analgesic activity. This biological results also shows that the activity is sensitive to alkyl chain length in hydrophobic region and the phenylacetic amides 19 are more active than the corresponding urea derivatives 17.

• 대한한방내과학회지
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• 제36권3호
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• pp.236-251
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• 2015

Objectives: To investigate the anti-inflammatory, analgesic, anti-pyretic and anti-histamine activities of 20 herbal medicines to test their efficacy in common cold treatment. Methods: For all experiments, the herbal medicines were extracted with 80% ethanol and freeze-dried. To determine the anti-oxidative properties, we tested DPPH-free radical-scavenging activity and xanthine oxidase inhibitory activity. To determine anti-inflammatory and analgesic potential, we investigated acetic acid-induced vascular permeability and writhing test in ICR mice. For anti-pyretic activities, an LPS-induced pyrexia study was conducted in rabbits. To evaluate the anti-histamine activity, we examined compound 48/80-induced systemic anaphylaxis in ICR mice and the release of β-hexosaminidase on rat basophilic leukemia (RBL-2H3) cells. Results: Ephedrae herba, Forsythiae fructus, Cinnamomi ramulus, and Cimicifugae rhizome showed potent free-radical scavenging activities. Gentianae macrophyllae radix inhibited acetic acid-induced vascular permeability. Schizonepetae spica and Cimicifugae rhizome inhibited acetic acid. Cinnamomi ramulus and Angelicae decursivae radix inhibited LPS-induced pyrexia. Angeliace dahuricae radix and Asari radix inhibited compound 48/80. Scutellariae radix, Cinnamomi ramulus, Ephedrae herba, and Zingiberis rhizoma crudus potently inhibited the release of β-hexosaminidase. Conclusions: We examined the anti-inflammatory, analgesic, anti-pyretic and anti-histamine activities of 20 herbal medicines;We examined the anti-inflammatory, analgesic, anti-pyretic and anti-histamine activities of 20 herbal medicines Codonopsis pilosulae radix, Zingiberis rhizoma crudus, and Cinnamomi ramulus showed novel efficacy. These results suggest that some of herbal medicines may be very effective in treating common cold.

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 춘계총회 및 학술대회
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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

• Journal of Acupuncture Research
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• 제24권6호
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• pp.75-88
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• 2007

Objectives : We investigated the effects of Hominis placenta Herbal acupuncture on rheumatoid arthritis. Methods : We investigated the Type II collagen-induced arthritis test, vascular permeability test, phenyl benzoquinone-induced writhing test, hot plate test, carbon clearance test, determination of prostaglandin $E_2$ content and cyclooxygenase-2 activity test. Results : Hominis placenta Herbal acupuncture suppressed Type II collagen-induced arthritis in DBA/1J mice and vascular permeability with 10.2% inhibition in ICR mice. We see the phenyl benzoquinone-induced writhing test and the hot plate test in the analgesic activity test. In the phenyl benzoquinone-induced writhing test, Hominis placenta Herbal acupuncture showed that it increased its analgesic effect more than the control(test?) by 85.5%. In the hot plate test, it was also shown that the analgesic effect increased more than the control(test) by 32.1%. In the carbon clearance test, the immuno-stimulatory effect showed more than the control(test) by 8.0%. The formation of prostaglandin $E_2$ was also reduced more than the control(test) by 10.1%. Finally, cyclooxygenase-2 activity was inhibitedwith 36.3%. Conclusions : Hominis placenta Herbal acupuncture may be useful for the treatment of rheumatoid arthritis after injection.

• 대한한방내과학회지
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• 제19권1호
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• pp.57-72
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• 1998

This study has been carried out to investigate the effects of Ukgansan(UGS) extract on anti-convulsive, antipyretic, analgesic, sedative and GABAergic system of experimental animals. The results of this study were as follows : 1. UGS extract prolonged significantly the beginning time to convulsion and death induced by strychnine. 2. UGS extract prolonged significantly the time to death induced by electrical shock of ECT unit.(3 sec, 200 F, 25 mA) 3. On the experiment of hypothermic effects of UGS extract on the rectal temperature of mouse, UGS extract decreased significantly the rectal temperature of mouse 4. On the experiment of antipyretic effects of UGS extract on the febrile induced by the subcutaneous injection of $150\;{\mu}g/kg$ endotoxin in mouse, UGS extract decreased significantly the rectal temperature of mouse. 5. On the experiment of analgesic effects of UGS extract on the writhing syndrome induced by intraperitoneal injection 0.7% acetic acid 1 ml/100g in mouse, the writhing syndrome induced by acetic acid was reduced significantly by administration of UGS extract. 6. On the experiment of effects of UGS extract on spontaneous motor activity measured by wheel cage method in mice, the spontaneous motor activity was reduced significantly by administration of UGS extract. 7. On the experiment of effects of UGS extract on the activity of GABA-transaminase(GABA-T) in mouse brains after 21 days of oral administration of UGS extract. the activity of GABA-T was reduced significantly by administration of UGS extract. 8. On the experiment of effects of UGS extract on the activity concentration of GABA in mouse brain after 21 days of oral administration of UGS extract, the activity concentration of GABA was reduced significantly by administration of UGS extract. 9 On the experiment of effect of UGS water extract on the activity of GAD in mouse brain after 21 days of oral administration of UGS extract, the activity of GAD was reduced significantly by administration of UGS extract. According to the these results, Ukgansan extracts reveal the effects on the anti-convulsive, antipyretic, analgesic, sedative and GABAergic system.

• 대한한방내과학회지
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• 제18권2호
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• pp.65-82
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• 1997

This study has been carried out to investigate the effects of Cheonmagudeungyeum(CGY) extract on anti-convulsive, antipyretic, analgesic, sedative and GABAergic system of experimental animals. The results of this study were as follows : 1. CGY extract prolonged significantly the beginning time to convulsion and death induced by strychnine. 2. CGY extract prolonged significantly the time to death induced by electrical shock of ECT unit(3 sec, 200 F, 25 mA) 3. On the experiment of hypothermic effects of CGY extract on the rectal temperature of mice, CGY extract decreased the rectal temperature of mice. 4. On the experiment of antipyretic effects of CGY extract on the febrile induced by the subcutaneous injection of $150\;{\mu}g/kg$ endotoxin in mice, CGY extract decreased significantly the rectal temperature of mice. 5. On the experiment of analgesic effects of CGY extract on the writhing syndrome induced by intraperitoneal injection 0.7% acetic acid 1 ml/100g in mice, the writhing syndrome induced by acetic acid was reduced significantly by administration of CGY extract. 6. On the experiment of effects of CGY extract on spontaneous motor activity measured by wheel cage method in mice, the spontaneous motor activity was reduced significantly by administration of CGY extract 7. On the experiment of effects of CGY extract on the activity of GABA - transaminase (GABA-T) in mouse brains after 21 days of oral administration of CGY extract, the activity of GABA-T was reduced significantly by administration of CGY extract. 8. On the experiment of effects of CGY extract on the activity concentration of GABA in mouse brain after 21 days of oral administration of CGY extract, the activity concentration of GABA was reduced significantly by administration of CGY extract. 9. On the experiment of effect of CGY water extract on the activity of GAD in mouse brain after 21 days of oral administration of CGY extract, the activity of GAD was reduced significantly by administration of CGY extract. According to the these results, Cheonmagudeungyeum extracts reveal the effects on the anti-convulsive, antipyretic, analgesic, sedative and GABAergic system.

• 약학회지
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• 제43권4호
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• pp.411-418
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• 1999

Intracerebroventricular (ICV) infusion of morphine (MOR) produces strong analgesia in man and animals. The analgesic effect is thought to be mediated by the centrifugal inhibitory control. But neural mechanisms of the analgesic effect of ICV morphine are not well understood. In the present study, we found that ICV MOR had dual actions on the activity of dorsal horn heurons: it produced both inhibition and excitation of dorsal horn neurons. Since MOR exerts its 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 intracerebroventricularly. Effects of ICV MOR were tested in 28 dorsal horn neurons of the spinal cord in the cat. ICV MOR inhibited, excited and did not affect the heat responses of dorsal horn neurons. ICV DAMGO and DADLE, $\mu$- and $\delta$-opioid agonist, respectively, exhibited the excitation of dorsal horn neurons. In contract, U-50488, a k-opioid agonist, exhibited both the inhibition and excitation of dorsal horn neurons. These results suggest that opioid receptors have different actions on activity of dorsal horn neuron and that the inhibitory action of k-opioid agonist may subserve the analgesia often produced by ICV MOR.