• Journal of the Korean Applied Science and Technology
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• v.19 no.4
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• pp.281-290
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• 2002

Dermorphin is a hepta peptide(H-Tyr-DAla-Phe-Gly-Tyr-Pro-Ser-$NH_{2}$)with exceptionally potent and long-lasting peripheral and central activity. Dermorphin analogues, dermorphionyl(DMP)-Lys-$NH_{2}$ and DMP-Lys-Lys-$NH_{2}$ have been prepared in order to examine the effect of opiod activity. Dermorphin analogues were synthesized by the solid phase method. The crude peptide was purified by gel filter on a Sephadex LH-20, characterized with HPLC and amino acid analyzer. Analgesic potency was estimated by writhing syndrome method and Randall-Selitto method. As a result, dermorphin analogues have lower potency than that of morphine.

• Biomolecules & Therapeutics
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• v.5 no.1
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• pp.67-73
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• 1997

Analgesic effect of DA-5018, a new capsaicin derivative, was evaluated in various rat models of experimentally induced acute pain. DA-5018(0.2∼10.0 mg/kg, p.o.) prevented the writhing syndromes induced by acetic acid or phenol-p-benzoquinone(PBQ). It increased the pain threshold of inflamed paw when tested by the Randall-Selitto method at the dose of 2.0∼20.0 mg/kg by oral administration. And also it showed antinociceptive activities in tail-pinch(1.0∼20.0 mg/kg, p.o.) and tail-flick test(5.0∼50.0 mg/kg, p.o.). the potency and efficacy of DA-5018 were comparable to morphine · HCI in all the models mentioned above. Acetaminophen exhibited the inhibition of acetic acid-induced writhing syndromes and also analgesic activity in Randall-Selitto test, but it showed the limited efficacy in tail-pinch and tail-flick test. These results mean that DA-5018 has a broader analgesic activity profile than acetaminophen. And we found out that the analgesic activity of DA-5018 was 100 times more potent when administered centrally than administered orally in tail-flick test. These results suggest that DA-5018 has an orally active analgesic activity, and central nervous system may be involved in the action of DA-5018.

• YAKHAK HOEJI
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• v.38 no.3
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• pp.345-350
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• 1994

Fourteen melandrin derivatives(I-XIV) were investigated on analgesic, anti-inflammatory and antiviral activities . Compound I [N-(p-hydroxybenzoyl)-5-hydroxyanthranilic acid methvl ester], Xll [N-(2-phenoxypropionyl)-5-hydroxy anthranilic acid propyl ester and XIV [N-(2-phenoxypropionyl)-5-hydroxyanthranilic acid exhibited analgesic activity in tail pressure and Randall-Selitto method. But no anti-inflammatory activity was shown. Compound I exhibited weak antiviral activity on Herpes simplex virus type I F strain by virus-induced cytopathic effect(CPE) assay and it's selectivity index(Sl) was 8.17.

• Korean Journal of Pharmacognosy
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• v.30 no.2
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• pp.137-144
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• 1999

Torilin was isolated from haxane fraction of Torilis Fructus extract. Torilin produced inhibition of the acetic acid-induced and phenylquinone-induced writhing syndrome at the oral doses of 30 and 90 mg/kg in mice. It also increased the pain threshold at the oral doses of 30, 90 and 270 mg/kg in the tail pressure method and the Randall-Selitto method. However, it did not show a hypothermic action at the oral doses of 30 and 90 mg/kg in mice. The compound exhibited strong anticarrageenan activity at the oral doses of 90 and 270 mg/kg in rats, and had inhibitory effect on the vascular permeability at the oral doses of 30 and 90 mg/kg in mice. It also showed potent inhibition of leucocyte emigration in CMC-pouch at the doses of 3 and 9 mg/rat, sc. The acute toxicity of torilin was very weak: the $LD_{50}$ values were more than 5000 mg/kg, po and 2000 mg/kg, ip in mice. From the above mentioned results, it was suggested that torilin had potent analgesic and anti-inflammatory activities.

• Korean Journal of Pharmacognosy
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• v.36 no.4 s.143
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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.

• 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.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.178-178
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• 1998

We reported that the hexane fraction of Torilis Fructus have an anti-inflammatory and analgesic effect. Therefore, in order to isolate the active compound, the hexan fraction of Torilis Fructus was chromatographed on silica gel column. The subfraction of hexane fraction was crystallized as colorless stout needles. The chemical structure of this compound was verified to be torilin through m.p., UV, IR, GC-MS, and NMR spectral data. In pharmacological tests, torilin exhibited strong anticarrageenan activity at the dose of 90 and 270 mg/kg, p.o. in rats, and it had inhibitory effect on the vascular permeability at the dose of 30 and 90 mg/kg, p.o. in mice. Torilin showed potent inhibition of leucocyte emigration in CMC-pouch at the dose of 3 and 9 mg/rat, s.c. Torilin have the analgesic effect at the dose of 30, 90 and 270 mg/kg, p.o. in both of the acetic acid- and phenyl-p-benzoquinone-induced writhing syndrome. It also increased the pain threshold at the dose of 30, 90 and 270 mg/kg, p.o. in the tail pressure method and the Randall-Selitto method. Torilin did not show a hypothermic action at the dose of 30 and 90 mg/kg, p.o. in mice. The acute toxicity of torilin was very weak: the LD$\_$50/ value was more than 5000 mg/kg, p.o. and 2000 mg/kg, Lp. in mice. From the above mentioned results, it was suggested that torilin had potent anti-inflammatory and analgesic activities in animals.

• YAKHAK HOEJI
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• v.44 no.4
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• pp.300-307
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• 2000

Expression of xenobiotic-metabolizing enzymes can be altered by xenobiotics, which represents changes in the production of reactive metabolic intermediates as well as toxicities in tissues. Metabolic intermediates derived from xenobiotics are considered to produce the reactive oxygen species including drug free radicals and hydroxyl free radicals, which would be ultimately responsible for drug-induced toxicities. The effects of 1,2-benzothiazine anti-inflammatory agents on the expression of xenobiotic-metabolizing enzymes including major cytochrome P450s, microsomal epoxide hydrolase (mEH) and glutathione S-transferase (GST) were studied in the liver with the aim of providing the part of information on potential production of reactive metabolites and hepatotoxicity by the agents. The synthetic compounds 24, 36 and 39 exhibited anti-inflammatory effects in rats as assessed by the Randall-Selitto method. The anti-inflammatory effect was detected as early as at 30 min after gavaging the agents with the ED5O being noted at 80 mg/kg, which was comparable to that of ibuprofen. Treatment of rats with each compound (100 mg/kg, 3d) resulted in no significant induction in the immunochemically-detectable cytochromes P45O 1A1/2, P450 2B1/2, P45O 2 Cl1 and P45O 2El. Changes in the mEN expression were also minimal, as evidenced by both Western blot and Northern blot analyses. Hepatic GST expression was slightly increased by the agents: GST Ya protein and mRNA expression was ～1.5-fold increased after treatment with compounds 24 and 39, whereas GST Yb1/2 and Yc1/2 mRNA levels were elevated 2- to 3-fold. In summary the effects of the synthetic 1,2-benzothiazines on the expression of major P45O, mEH and G57 were not significant, providing evidence that metabolic activation of the agents, potential drug interaction and hepatotoxicity would be minimal.