• 생약학회지
• /
• 제27권3호
• /
• pp.282-287
• /
• 1996

Cnidii rhizoma is one of the most important crude drugs used particularly for the treatment of female genital inflammatory diseases in traditional oriental medicine. In this study, its anti-inflammatory and analgesic activities were examined employing animal models. It was found that $H_2O$ extract and n-BuOH fraction inhibited significantly the edema formation after the subplantar injection of carrageenin at oral doses of 100 and 200 mg/kg in a dose-dependent fashion, where MeOH extract showed significant anti-inflammatory activity at a oral dose of 200 mg/kg. In Freund's complete adjuvant-induced arthritis, H2O extract and n-BuOH fraction exerted their significant inhibitory activity on the edema formation at oral doses of 100 and 200 mg/kg. The $H_2O$ extract and n-BuOH fraction also showed significant analgesic activity in a dose-dependent manner in acetic acid-induced writhing test.

• Natural Product Sciences
• /
• 제13권4호
• /
• pp.347-354
• /
• 2007

In this study, we investigated the potential of Resina Pini (RP) for anti-inflammatory and analgesic agents to treat inflammatory diseases such as gingivitis and periodontitis. Crude RP (RP1), recrystallized RP (RP2), and Ramus Mori Albae-treated RP (RP3), plus their respective water extracts (RP1-WE, RP2-WE and RP3-WE) were prepared for in vitro and in vivo tests. We couldn't find any signs of heavy metals pollution in all the RP samples. RP2-WE exhibited the highest viability of human gingival fibroblasts (HGF) and the strongest scavenging activity on superoxide anion. RP1, RP2 and RP3, RP2 showed potent scavenging activity on DPPH free radical. RP2-WE displayed a stronger inhibition on hyaluronidase (HAase) activity and RP3 also displayed potent HAase inhibition. RP2-WE, RP3-WE, RP3 and RP2 were reduced admirably the production of $PGE_2$ in HGF. In addition, RP2-WE and RP3-WE exhibited potent inhibitory activities on arachidonic acid-induced ear edema in mouse. Moreover, RP-2 prevented completely acetic acid-induced writhing by 100.0% and RP1, RP3, RP1-WE and RP2-WE also exhibited excellent protective activities against writhing. While aminopyrine, the positive control, showed 76.9% analgesic effect at the same dose. Taken together, these results suggest that recrystallized aqueous extract of Resina Pini could be a promising drug for the treatment of periodontal diseases.

• Bulletin of the Korean Chemical Society
• /
• 제28권12호
• /
• pp.2235-2240
• /
• 2007

3-Aryloxy methyl-4-(N-pyrazin-2'yl carboxamido)-5-mercapto-1,2,4-triazoles (3a1-a14) were prepared starting from potassium dithio carbazinates (2a1-a14). These triazoles were then employed in the synthesis of 3-aryloxy methyl-4-(N-pyrazin-2'yl carboxamido)-5-hydrazino-1,2,4-triazoles (4a1-a14). All the newly synthesized compounds were characterized by analytical, IR, NMR spectral studies. The compounds were screened for their antibacterial, antifungal, anti-inflammatory and analgesic properties. Most of the compounds have shown significant antifungal activity while few have shown excellent anti-inflammatory and analgesic activity. An attempt is made to study the structure activity relationship (SAR).

• 생약학회지
• /
• 제32권3호통권126호
• /
• pp.242-247
• /
• 2001

The anti-inflammatory activity of water extract of Mahaengeuigam-Tang(MHEGTWE) was examined using the carrageenin and acetic acid induced edema, croton oil induced granuloma pouch, and adjuvant arthritis in rats. In addition, the acute toxicity, analgesic and antipyretic effects of MHEGTWE were investigated by the general experimental methods. In acute toxicity test in mice, MHEGTWE showed 10% mortality at 2400 mg/kg(p.o), but it did not showed at 1200 mg/kg(i.p). It was also showed significant analgesic action on the writhing syndrome induced by 0.7% acetic acid at 600 mg/kg(p.o) and its antipyretic activity was observed in the typhoid vaccine induced fevered rats at 300 mg/kg(p.o). By the oral administration of the MHEGTWE, the significant anti-inflammatory activity was observed on 1% carrageenin induced edema, and it significantly inhibited the granuloma and exudate formation in rats. In the adjuvant arthritis experiment, the MHEGTWE decreased the hind paw edema in rats for 19 days. The results suggest that MHEGTWE has analgesic, anti-inflammatory and antipyretic action.

• Biomolecules & Therapeutics
• /
• 제5권1호
• /
• pp.87-93
• /
• 1997

DA-5018, a new capsaicin derivative, showed potent analgesic effect comparable to that of morphine in various experimental acute pain models. in this study, whether the analgesic mechanism of DA-5018 is related to opiate receptors or prostanoids was investigated. The affinity of DA-5018 for opiate receptor was determined by receptor binding assay. The Ki values of DA-5018 for nonspecific and specific $\mu$, $textsc{k}$, $\delta$-opiate receptor was 299$\pm$8.88, 735$\pm$215, 2930$\pm$ 163, 1550$\pm$813 nM, respectively and DA-5018 exhibited lower affinity than morphine. DA-5018 (10-"~3$\times$10-′M) inhibited electrically-evoked contractions of the guinea ply ileum and rat vas deferens, and these inhibition was not antagonized by naloxone(10 nM), an opiate receptor antagonist. Antagonism of analgesic effect of 7A-5018 by naloxone was examined by tail pinch test. Analgesic action of DA-5018(0.1 ~2 mg/kg, 5.c.) was not antagonized by naloxone(1 mg/rg, i.p.). These results indicate that pharmacological action of DA-5018 is not related with opiate receptor. Cyclooxygenase and 5-lipoxygenase activities in rat peritoneal neutrophil treated with A23187 and arachidonic acid were measured by radioimmunoassay. DA-5018 stimulated the cyclooxygenase activity and the concentration show-ing the two fold increase of activity was 124$\mu$M. DA-5018 slightly inhibited 5-lipoxygenase activity and these results together indicate that analgesic action of 3A-5018 is not mediated through inhibition of cyclooxy genase or lipoxygenase. These results suggest that the analgesic effect of DA-5018 is not due to blocking opiate receptor or to inhibiting the synthesis of prostanoids in the arachidonic acid metabolism pathway.

• 생약학회지
• /
• 제31권1호
• /
• pp.45-50
• /
• 2000

The root of Pseudostellaria heterophylla Pax et Hoffm. (Caryophyllaceae) is a herbal medicine called Taejasam(太子蔘) and used as a good tonic in China that strengthens the functions of the lung and the stomach like Ginseng in Korea. It has been known to have the antitussive activity for tuberculosis, appetizing effect and antifatigue activity, and so on. Especially it has been known to generate body fluids for the severe thirst and the shortage of water in body after a febrile disease for a long time. Recently some components of cyclic peptides, pseudostellarins A,B,C,D,E,F,G, that inhibit the activity of tyrosinase, were separated from this root. In this report several biological activities including acute toxicity, analgesic activity, antifatigue activity, bile juice increasing activity, hepatoprotective activity and antiinflammatory activity were investigated. These results showed as such; $LD_{50}$ of methanol extracts was above 10,000 mg/kg. The analgesic effect was revealed in the writhing test using rats. The BuOH fractions showed a prominent antifatigue effect against immobilized stress, significant hepatoprotective activities against $CCl_4$ intoxication and inhibitory effect on carrageenin-induced edema in rat's paw.

• Archives of Pharmacal Research
• /
• 제21권4호
• /
• pp.406-410
• /
• 1998

Biflavonoid is one of unique classes of naturally-occurring bioflavonoids. Certain biflavonoids including amentoflavone were previously reported to have inhibitory effect on the group 11 phospholipase $A_2$ activity. Amentoflavone was also found to inhibit cyclooxygenase from guinea-pig epidermis without affecting lipoxygenase. In this study, anti-inflammatory and analgesic activities of amentoflavone were evaluated. When amentoflavone was administered intraperitoneally, it showed a potent anti-inflammatory activity as determined by amelioration of croton-oil induced mouse ear edema. It also showed a potent anti-inflammatory activity in the rat carrageenan paw edema model ($ED_{50}$=42 mg/kg) compared to the activity of prednisolone (35 mg/kg) and indomethacin (10 mg/kg). However, amentoflavone did not show a significant inhibitory activity against rat adjuvant-induced arthritis, a chronic inflammatory model. In addition, amentoflavone was found to possess a potent analgesic activity in the acetic acid writhing test ($ED_{50}$=9.6 mg/kg) compared to the activity of indomethacin (3.8 mg/kg). These results suggest that amentoflavone may be a potential lead for a new type of anti-inflammatory agents having dual inhibitory activity of group 11 phospholipase $A_2$ and cyclooxygenase.

• Advances in Traditional Medicine
• /
• 제6권2호
• /
• pp.121-125
• /
• 2006

The crude ethanol extract of the stem bark of Trewia polycarpa (Family: Euphorbiaceae) was subjected to acetic acid induced writhing inhibition, Brine Shrimp lethality bioassay and 1, 1-diphenyl-2-picryl hydrazyl free radical scavenging assay for screening of analgesic, cytotoxic and antioxidant activity respectively. The extract produced significant (P < 0.001) writhing inhibition in acetic acid induced writhing in mice at the dose of 125, 250 and 500 mg/kg body weight respectively, which were comparable to the standard drug diclofenac sodium. The extract showed significant lethality to Brine Shrimp and the $LC_{50}$ value was $8\;{\mu}g/ml$. The extract showed prominent free radical scavenging activity ($IC_{50}$ about ${\sim}10\;{\mu}g/ml$) compare to standard drug ascorbic acid ($IC_{50}about\;{\sim}15\;{\mu}g/ml$). The results tend to suggest that the crude ethanol extract of the bark might possess analgesic, cytotoxic and antioxidant activities or active constituent(s) responsible for the activities.

• 생약학회지
• /
• 제38권1호
• /
• pp.22-26
• /
• 2007

Leaves and stem of Viburnum sargentii for. sterile(Caprifoliaceae) has been used as therapeutic agents as a pain of the joints, skin disease as styptics, analgesics for traditional folk medicines. The present study describes the preliminary evaluation of biological activities-analgesic, anti-inflammatory, hepatoprotective activities, of its methanol extract, ethyl acetate fraction and butanol fraction. Among them butanol fraction showed the highest activity in inflammation and writhing test.

• BMB Reports
• /
• 제43권12호
• /
• pp.801-806
• /
• 2010

The existence of glycine residues in long-chain scorpion toxins has been well documented. However, their role as analgesics has not been evaluated. To address this issue, we investigated the functional role of glycines in the C-terminal end of Chinese-scorpion toxin from Buthus martensii Karsch (BmK AGP-SYPU2) using site-directed mutagenesis and analgesic activity assays. Recombinant BmK AGP-SYPU2 and its mutants were efficiently expressed in E. coli and purified to homogeneity using immobilized metal ion affinity chromatography (IMAC) and cation exchange chromatography. The mouse-twisting test was used to detect the analgesic activity of BmK AGP-SYPU2 and its mutants. As a result, we identified glycines at the C-terminal end that, when altered, significantly affected analgesic activity. Also, Mut6566 was significantly decreased compared to BmK AGP-SYPU2. These data indicate that the glycines at the C-terminal end are important for the analgesic activity of BmK AGP-SYPU2.