• 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.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.410.2-411
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• 2002

Ketoprofen (KP), a potent analgesic and non-steroidal anti-inflammatory drug, has some disadvantages such as gastro-intestinal irritation. short half-life (1.5-4 hour) in plasma and low solubility in aqueous solution. In order to minimize these disadvantages. we have recently prepared a KP prodrug, KP-polyethylene glycol conjugate (KPEG750, PEG Mw=750), and investigated its pharmacokinetic behavior. anti-inflammatory and analgesic effect. (omitted)

• Natural Product Sciences
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• 제11권2호
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• pp.63-66
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• 2005

A rare flavonol glycoside identified as $eupalitin-3-O-{\beta}-D-glucoside$ (I) was isolated from Tephrosia spinosa (Leguminosae) and its anti-inflammatory activity was evaluated against carrageenin induced paw edema. The compound exhibited significant activity when compared to the standard drug indomethacin.

• 한국임상약학회지
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• 제20권3호
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• pp.205-212
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• 2010

The prescription sheets for outpatients from July 2008 to June 2009 from 7 community pharmacies in Ulsan City were surveyed for the anti-inflammatory drug (AID) prescription pattern. The AID prescription rate of pediatricians and ENT physicians were 30.0% and 34.8%, respectively. The oral steroidal anti-inflammatory drugs (SAIDs) were prescribed as much as 3.9% by pediatricians and 10.3% by ENT physicians. The chiefly prescribed oral SAID was prednisolone in pediatric clinics and methylprednisolone in ENT clinics. Meanwhile the prescription rate of oral non-steroidal anti-inflammatory drug (NSAID) was 22.5% by pediatricians and 21.4% in ENT physicians. The most favorable NSAIDs were propionate derivatives in both clinics. In case of externally-applied SAIDs, the prescription rate of pediatricians was 3.6% and that of ENT physicians was 2.8%. Among them, nasal spray, inhalant and gargle formulations for upper respiratory infection (URI) treatment occupied 35.8% of externally-applied SAIDs in pediatric clinics and 59.7% in ENT clinics. Further, it was observed that ENT physicians favored much stronger SAIDs in Group III of ATC classification (75.4% of externally-applied SAIDs) than pediatricians (49.2%). In the survey of AID combination rate, pediatric clinics showed much lower rate (1.4% of total AID prescriptions) than ENT clinics (7.5%). Among them, the combination rate of oral SAID and oral NSAID by ENT physicians (52.2% of total AID combinations) was much higher than pediatricians (36.6%), which might be over-prescription of AID agents. In conclusion, the AID prescription rate as well as AID combination rate, especially in SAID prescriptions, was much higher in ENT than pediatric clinics, which implies the higher confidency on AID drugs of ENT physicians even though the severity of patient's symptom could be considered.

• 약학회지
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• 제44권4호
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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.

• 생약학회지
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• 제44권2호
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• pp.154-160
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• 2013

Ceramium boydenii belongs to euphorbia humitusa of red algae, and is distributed along the coast of Jeju island. This study was conducted to examine the anti-inflammatory effect and action mechanism of C. boydenii in the human keratinocyte cell line HaCaT. The 80% EtOH extract of C. boydenii inhibits the production of MDC (macrophage derived chemokine), an inflammatory chemokine, induced by IFN-${\gamma}$ and TNF-${\alpha}$ in a concentration dependent manner. It also suppressed the phosphorylation and nuclear translocation of STAT1, a key transcription factor in IFN-${\gamma}$ and TNF-${\alpha}$ signaling pathway, at the effective concentrations. These results suggest that C. boydenii demonstrates the anti-inflammatory activity via the suppression of STAT1 activation and has the significant value as an anti-inflammatory source.

• 생약학회지
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• 제39권2호
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• pp.104-109
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• 2008

We previously reported that anti-inflammatory properties of poncirin, isolated from fruit of Poncirus trifoliata, might be the result from the inhibition of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), tumor necrosis $factor-{\acute{a}}$ ($TNF-{\alpha}$) and interlukin-6 (IL-6) expression via the down-regulation of $NF{-\kappa}B$ binding activity. In this study, we investigated whether poncirin has an inhibitory effect on the production of pro-inflammatory mediators ex vivo and whether poncirin could relieve the symptoms of dextran sulfate sodium (DSS)-induced colitis in mice model of inflammatory bowel disease. Poncirin significantly inhibited the productions of NO, IL-6 and $TNF-{\alpha}$ in lipopolysaccharide (LPS)-induced mouse peritoneal macrophage. In addition, poncirin-treated mice when compared to control mice not receiving treatment recovered better from the weight loss caused by DSS-induced colitis. Changes in disease activity index (DAI) of poncirin-treated mice were also more favorable than for control mice and were comparable with mice treated with a typical anti-inflammatory-drug, 5-aminosalichylic acid (5-ASA). In addition, suppression of plasma NO and IL-6 productions of poncirin-treated mice was also observed in DSS-induced colitis. These results suggest that poncirin has potentially useful anti-inflammatory effects mediated by suppression of inflammatory mediator productions.

• Archives of Pharmacal Research
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• 제28권5호
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• pp.509-517
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• 2005

A series of structurally diverse amide derivatives of [6-(3,5-dimethyl-4- chloro-pyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic acid were prepared and tested for their in vivo analgesic and anti-inflammatory activity by using p-benzoquinone-induced writhing test and carrageenan induced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds, 7c, 7d and 7k were found to be equipotent to aspirin (as an analygesic) and indometacin (as an anti-inflammatory drug), respectively. The other amide derivatives generally resulted in lower activity on comparision with reference compounds.

• 한방재활의학과학회지
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• 제33권3호
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• pp.17-32
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• 2023

Objectives The purpose of this study was to investigate the antioxidant, anti-inflammatory and cartilage regeneration effects of Euiiin-tang water extract (EIIT) in the treatment of monosodium iodoacetate (MIA)-induced osteoarthritis in rats. Methods Animal models were divided into five groups. The normal group didn't do any treatments causing osteoarthritis. The control group was orally administerd distilled water instead of the drug, the positive control group used indomethacin 5 mg/kg, the EIIT 100 group used EIIT 100 mg/kg and the EIIT 200 group used EIIT 200 mg/kg, and seven rats were placed per group. We administered drug to rats for 2 weeks and analyzed oxidative stress-related proteins in joint tissue. Inflammation mediators and inflammatory cytokines induced by the activity of inflammation-related proteins were analyzed. In addition, the expression of anti-inflammatory cytokines and collagen-related factors were analyzed, and H&E staining and Safranin-O staining were performed to see the effect on histopathological changes. Results 1) Oxidative stress-related proteins were significantly reduced. 2) Inflammationrelated proteins, inflammatory mediators and inflammatory cytokines were significantly reduced. 3) Anti-inflammatory cytokines were significantly increased. 4) Collagen proteolysis factors significantly decreased, and collagen degradation inhibitory factor was significantly increased. 5) EIIT administration significantly reduced cartilage degeneration and deformation in H&E staining, and reduced proteoglycan destruction in Safranin-O staining. Conclusions From the above experimental results, it judges that Euiiin-tang has antioxidant, anti-inflammatory, and cartilage regeneration effects on osteoarthritis in rats induced by MIA.

• 셀메드
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• 제4권1호
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• pp.4.1-4.4
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• 2014

Gynura segetum, family Asteraceae is a cultivated species and can be found growing in the tropical regions of Indonesia and Malaysia. The plant is known for its use for the treatment of cancer, inflammation, diabetes, hypertension and skin afflictions. In the current study, anti-inflammatory effect of Gynura segetum leaf has been investigated. The present study investigated the in vivo anti-inflammatory effect of Gynura segetum leaf by using hen's egg test-chorioallantoic membrane (HET-CAM) assay. Different solvent extract of Gynura segetum leaf were tested, the most active methanol extract was further fractionated and tested. Among the extracts tested, the methanol extract showed a significant good anti-inflammatory effect (76.8% inhibition at 50 ${\mu}g/disc$) on the HET-CAM assay as compared with the anti-inflammatory drug indomethacin (82.1% inhibition). However, the fractionated sample exhibited a significantly lower activity in comparison to crude methanol extract. The results demonstrated that Gynura segetum leaf displayed remarkable anti-inflammatory effects, which support the folkloric uses of this plant for treatment of inflammation.