• Archives of Pharmacal Research
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• v.28 no.5
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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.

• Korean Journal of Pharmacognosy
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• v.20 no.3
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• pp.188-195
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• 1989

Hyangsayangwee-Tang, a combined preparation of crude drugs, which has been used for stomach and intestinal disorder, was examined for anti-spasmodic, anti-ulcerative and anti-emetive effects. Spontaneous motility of isolated ileum was strongly suppressed and inhibitory effects against contraction of isolated ileum induced by acetylcholine and barium chloride were shown in mice. And, contraction of isolated guinea-pig ileum by histamine was inhibited. In rats fundus preparations, Hyangsayangwee-Tang elicited strong relaxation and had antagonist effects against the spasm induced by acetylcholine and barium chloride. A significant inhibitory effect on the intestinal propulsion of barium sulfate in mice was shown. In pylorus-ligated rats, Hyangsangwee-Tang inhibited gastric secretion and showed a strong anti-peptic activity. Protective effects against gastric ulceration induced by pyloric ligation, water-immersion stress, histamine and aspirin were significantly recognized in mice and rats. Hyangsayangwee-Tang decreased cupric sulfate-induced vomitting in frogs.

• Korean Journal of Pharmacognosy
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• v.33 no.4 s.131
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• pp.389-394
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• 2002

Present study was carried out for development of a new supplementary product with gastroprotective effect. Natural Products mentioned that have GI protective property in Dongeuibogam and reports were evaluated anti-bacterial activity against Helicobacter pylori, then five heres were selected. The material used for the test were water extract of Alpinia oxyphlla (AO), Astragalus membranaceus (AM), Cinnamomum loureirii(CL), Citrus aurantium(CA), Amomum villosum(AV). They were tested individually on HCI ethanol-induced gastric lesion in rats, AV CL, AO showed the most significant effectiveness, respectively. Then two mixture different in their content ratio (P020701-1,-2) and complex with P020701-1 (CP) were made, and tested on HCI·ethanol, indomethacin-induced gastric lesion, aspirin-ligature, Shay ulcer and gastric secretion. P020701-1, -2 and CP showed significant effect on HCI ethanol, indomethacin-induced gastric lesion, and Shay ulcer. It can be regarded that the antigasuitic and anti-ulcerative effects of P020701- 1, -2 and CP are originated from reduction of total acid output identified by gastric secretion test.

• Journal of Microbiology and Biotechnology
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• v.15 no.2
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• pp.425-427
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• 2005

The steam distillate obtained from Thujopsis dolabrata var. hondai sawdust was fractionated by centrifugal thin-film evaporation, and the fractions were then investigated for antiplatelet activity using washed rabbit platelets. The biologically active constituent of T. dolabrata var. hondai sawdust was isolated by silica gel column and HPLC chromatographies and characterized as carvacrol by various spectral analyses. Carvacrol inhibited platelet aggregation induced by collagen, arachidonic acid, and platelet activating factor with IC$_{50}$ values of 12.6, 2.5, and 385.3 $\mu$M, respectively. However, carvacrol had no effect on thrombin, calcium ionophore A23l87, or phorbol l2-myristate l3-acetate induced platelet aggregation. Carvacrol was a much more potent inhibitor, as antiplatelet agents, compared with aspirin. These results suggest that carvacrol isolated from T. dolabrata var. hondai sawdust may be useful as a lead compound for inhibiting arachidonic acid-induced platelet aggregation.

• Biomolecules & Therapeutics
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• v.4 no.2
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• pp.111-121
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• 1996

Antiulcer effects of Artemisia herba extract (DA-9601) were evaluated in various types of experimental gastric ulcer induced in rats. And the effects of DA-9601 on mucus, basal and stimulated gastric acid secretion were also investigated in rats. DA-9601 (12.5∼400 mg/kg, p.o.) prevented the formation of gastric ulcers induced by 60% EtOH in 150 mM HC1, restraint water immersion stress, platelet activating factor (PAF), aspirin in 150 mM HCI with Pylorus-ligation and indomethacin. DA-9601 (4∼400 mg/kg, p.o.) significantly accelerated the healing rate of acetic acid-induced gastric ulcer and significantly stimulated mucus secretion in a dose-dependent manner. DA-9601 (20∼200 mg/kg, i.d.), however, did not inhibit basal gastric acid secretion in pylorus ligated rats and DA-9601 (200 mg/kg, i.d.) failed to influence histamine-, pentagastrin- and carbachol- stimulated gastric acid secretion. These results suggest that DA-9601 has inhibitory action on gastric lesion and ulceration through increasing mucus secretion in the stomach of rats without influencing basal and stimulated gastric acid secretion.

• Archives of Pharmacal Research
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• v.25 no.4
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• pp.528-533
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• 2002

To evaluate the antithrombotic and antiallergic properties of rhaponticin extracted from Rhei Rhizoma, the in vitro and ex vivo inhibitory activities of rhaponticin and its metabolite, rhapontigenin, were measured. These compounds inhibited in vitro ADP- and collagen-induced platelet aggregation. Rhapontigenin was more potent, with $IC_{50}$ values of 4 and $70{\;}{\mu}g/ml$, respectively. In ex vivo ADP- and collagen-induced rat platelet aggregation, these compounds also exhibited a potent inhibitory effect. The antiplatelet aggregation effects of rhaponticin and rhapontigenin were more potent than those of aspirin. Rhapontigenin showed significant protection from death due to pulmonary thrombosis in mice. Rhapontigenin also showed the strongest inhibitory activity against $\beta-hexosaminidase$ release induced by DNP-BSA. These compounds inhibited PCA reaction in mice. Rhapontigenin intraperitoneally administered showed the strongest inhibitory activity and significantly inhibited PCA at doses of 25 and 50 mg/kg, with inhibitory activities of 48 and 85%, respectively. The inhibitory activity of orally administered rhaponticin was stronger than that of intraperitoneally administered rhaponticin. These results suggest that rhaponticin, in the rhizome of Rhei Rhizoma, is a prodrug that has extensive antiallergic and antithrombotic properties.

• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.1
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• pp.218-223
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• 2005

According to the Chinese and Korean medicinal and herbal literature, SSG(Silsosangami) is effective for the treatment of inflammation, hyperlipemia and arteriosclerosis. The pharmacological action of SSG has been limitedly studied in regard to ischemic infarction. This herbal medicine has been shown to express diverse activities such as immunomodulating, anti-infarction, anti-allergic and anti-inflammatory effects. Antisclerotic effects of SSG in experimentally induced atherosclerosis in rabbits have also been reported. However, pharmacological mechanisms of SSG on lipid metabolism and atherosclerosis formation are poorly understood. The present paper reports the effect of extracts obtained from SSG on endotoxin-induced experimental DIC in rats. Also, these were tested for their effect on endotoxin-induced blood platelet aggregation, thrombin-induced conversion of fibrinogen and fibrinolysis in vitro experiments with aspirin as a positive agent. The anti-thrombic properties of SSG were also investigated by means of analytical parameters of bood composition. The extracts of SSG and its seven herbs, except Cnidii Rhizoma and Carthami Flos, inhibited the endotoxin-induced DIC and thrombosis in rats. Also the extract inhibited the endotoxin-induced decrease in blood platelets and fibrinogen, and endotoxin-induced increase in fibrin degradation products (FDP) on disseminated intravascular coagulation in normal rats.

• The Korean Journal of Physiology and Pharmacology
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• v.7 no.2
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• pp.65-71
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• 2003

Increasing evidences suggest that ischemia-induced vascular damage is an integral step in the cascade of the cellular and molecular events initiated by cerebral ischemia. In the present study, employing a mouse brain endothelioma-derived cell line, bEnd.3, and oxygen-glucose deprivation (OGD) as an in vitro stroke model, the role of nuclear factor kappa B (NF-${\kappa}B$) activation during ischemic injury was investigated. OGD was found to activate NF-${\kappa}B$ and to induce bEnd.3 cell death in a time-dependent manner. OGD phosphorylated neither 32 Ser nor 42 Tyr of $I{\kappa}B{\alpha}$. OGD did not change the amount of $I{\kappa}B{\alpha}$. The extents of OGD-induced cell death after 8 h, 10 h, 12 h and 14 h of OGD were 10%, 35%, 60% and 85%, respectively. Reperfusion following OGD did not cause additional cell death, indicating no reperfusion injury after ischemic insult in cerebral endothelial cells. Three known as NF-${\kappa}B$ inhibitors, including pyrrolidine dithiocarbamate (PDTC) plus zinc, aspirin and caffeic acid phenethyl ester (CAPE), inhibited OGD-induced NF-${\kappa}B$ activation and increased OGD-induced bEnd.3 cell death in a dose dependent manner. There were no changes in the protein levels of bcl-2, bax and p53 which are modulated by NF-${\kappa}B$ activity. These results suggest that NF-${\kappa}B$ activation might be a protective mechanism for OGD-induced cell death in bEnd.3.

• Maxillofacial Plastic and Reconstructive Surgery
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• v.30 no.1
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• pp.30-40
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• 2008

The objectives of this study was to check up the effect of celecoxib, COX-2 inhibitor, on the pathogenesis of oral squamous cell carcinoma. After mefenamic acid, aspirin and celecoxib, COX-2 inhibitor, were inoculated to HN 22 cell line, the following results were obtained through tumor cell viability by wortmannin, growth curve of tumor cell line, apoptotic index, PGE2 synthesis, total RNA extraction, RT-PCR analysis and TEM features. 1. When wortmannin and celecoxib were given together, the survival rate of tumor cells was lowest about 47 %. So wortmannin had an effect on the decrease of survival rate of tumor cells. 2. In growth curve, the slowest growth was observed in celecoxib inoculated group. 3. The synthesis of PGE2 was decreased in all group and the obvious suppression and highest apoptotic index was observed in celecoxib inoculated group. 4. Suppression of expression of COX-2 mRNA was evident in celecoxib inoculated group. But that of COX-1,2 mRNA was observed in mefenamic acid inoculated group and aspirin inoculated group. 5. In celecoxib inoculated group, mRNA expression of AKT1 was decreased and that of PTEN & expression of caspase 3 and 9 was evidently increased. Depending on above results, when celecoxib was inoculated to oral squamous cell carcinoma cell line, an increase of mRNA expression of caspase 3,9 and PTEN is related to a decrease of mRNA expression of AKT1. Wortmannin had an effect on the decrease of survival rate of tumor cells. Celecoxib might induce apoptosis of tumor cell by suppression of AKT1 pathway and COX-2 inhibition. This results suggested that COX-2 inhibitor might be significantly effective in chemoprevention of oral squamous cell carcinoma.

• The Korean Journal of Pharmacology
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• v.23 no.1
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• pp.51-56
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• 1987

Cyclobuxine D was extracted from Buxus microphylla var. koreana Nakai. The effects of cyclobuxine D on the biosynthesis of prostaglandins from arachidonic acid in guinea pig lung, prostaglandin production and leukocyte migration in carrageenin-induced inflammation was investigated. These effects of cyclobuxine D were compared with those of aspirin and dexamethasone. Cyclobuxine D does not inhibit significantly cyclooxygenase in guinea pig lung but reduces prostaglandin concentration and leukocyte migration in inflammatory exudates. These effects of cyclobuxine D differ from that of aspirin which inhibits biosynthesis of prostaglandin in vitro and has a relative small effect on leukocyte migration. Dexamethasone, which does not inhibit cyclooxygenase in vitro, has an effect similar to that of cyclobuxine D on leukocyte migration and prostaglandin production in inflammatory exudates.