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김도현,박무인,유찬희,김규종,문원,박선자,장희경 고신대학교의과대학 2008 고신대학교 의과대학 학술지 Vol.23 No.2
저자들은 65세 남자 환자의 위 중부체부 대만부 전벽에 발생한 점막하 종양에 대하여 3년간 추적관찰 중 크기증가소견으로 쐐기 절재술을 시행하였으며, 조직검사 및 면역 조직 화학 검사에서 위 신경초종으로 진단한 1예를 경험하였기에 보고하는 바이다. Gastric schwannoma is a very rare gastrointestinal benign tumor, which represents only 0.2% of all gastric tumors and 4% of all benign gastric tumors. We report a case of gastric schwannoma with enlargement of size through serial endoscopic examination. Endoscopic examination showed a hard mass of 4 x 3 cm in size with normal overlying gastric mucosa on the great curvature of the mid-body of stomach. The pathological finding revealed a picture of spindle cell tumor. Immunohistochemical stain was strongly positive for S-100 protein and non-reactive for CD34, C-kit and smooth muscle actin, thus leading to the diagnosis of gastric schwannoma.
Transport of a New Erectogenic Udenafil in Caco-2 Cells
Ji, Hye-Young,Shim, Hyun-Joo,Yoo, Moo-Hi,Park, Eun-Seok,Lee, Hye-Suk 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.9
P-glycoprotein, an ATP-dependent efflux pump, is a membrane transporter that influences the absorption and excretion of drugs. There is a striking overlap between the substrates for CYP3A4 and P-glycoprotein. This study was designed to assess whether udenafil, a substrate of CYP3A4, is also a P-glycoprotein substrate. Udenafil stimulated P-glycoprotein ATPase activity, a putative measure of P-glycoprotein affinity, although with lower affinity than a proven substrate, verapamil. Bidirectional transport studies of udenafil using Caco-2 cell monolayers showed that its efflux (15.9-22.8 ${\times}$ $10^{-6}$ cm/s) was significantly higher than its influx (3.7-9.1 ${\times}$ $10^{-6}$ cm/s). P-glycoprotein inhibitors such as cyclosporine, tariquidar and verapamil significantly increased the influx of udenafil and decreased the efflux of udenafil. These results indicate that udenafil is a substrate for P-glycoprotein. The low bioavailability, variable absorption and drug-drug interactions of udenafil may be related to the variability of CYP3A4 and P-glycoprotein expression and to possible CYP3A4 and P-glycoprotein interactions.
HPLC를 이용한 생체 시료중의 새로운 플라보노이드 유도체인 DA-6034의 분석
이종진,손미원,유무희,장민선,김원배,이강춘 성균관대학교 약학연구소 1998 成均藥硏論文集 Vol.10 No.1
A high performance liquid chromatographic method was developed for the determination of DA-6034 in biological fluids using internal standard. Plasma containing DA-6034 and internal standard was extracted by liquid-liquid extraction at an acidic pH. After evaporation of the organic layer, the drug and internal standard were reconstituted with mobile phase and injected into the column. They were separated by high performance liquid chromatography on inertsil ODS Ⅱ column at 334㎚. The detection limit of DA-6034 in plasma was 0.02㎍/㎖. In this method, the range of recovery and coefficients of variation were 96∼110% and 0.40∼3.78%, respectively. There was no interference from endogenous substances. Urine and bile were analysed using the deproteinization method and the detection limit of DA-6034 was 1㎍/ℓ.
Erectogenic Effect of the Selective Phosphodiesterase Type 5 Inhibitor DA-8159
Oh, Tae-Young,Kang, Kyung-Koo,Ahn, Byoung-Ok,Yoo, Moo-hi,Kim, Won-Bae The Pharmaceutical Society of Korea 2000 Archives of Pharmacal Research Vol.23 No.5
DA-8159, a new phosphodiesterase 5 inhibitor, was assessed for its erectogenic potential by a penile erection test in rats, the relaxation of isolated rabbit corpus cavernosum (CC), and estimation of the intracavernous pressure (ICP) in the anesthetized dog. Oral administration of DA-8159 (0.3 to 1 ${\mu}g/kg$ ) increased the number of erections in rats with increasing dosage, with the highest penile erection index at 10 ${\mu}g/kg$ DA-8159 induced the relaxation of phenylephrine (PHE)-induced contractions in the rabbit CC and decreased the $IC_{50}$ of the nitric oxide donor sodium nitroprusside (SNP) in a dose-dependent fashion. In pentobarbital-anesthetized dogs, the intravenous administration of DA-8159 (1~300 ${\mu}g/kg$ ) potentiated the increase in ICP induced by the intracavernosal SNP in a dose-related manner. These findings suggest that DA-8159 has significant therapeutic potential in the treatment of erectile dysfunction.
새로운 플라보노이드 유도체인 DA-6034의 TNBS 유발성 염증성대장염 모델에서의 치료효과
손미원,고준일,김희기,장동경,유무희,김원배,이강춘,송인성 성균관대학교 약학연구소 1998 成均藥硏論文集 Vol.10 No.1
The efficacy of DA-6034, a new flavonoid derivative, was investigated in comparison with sulfasalazine in a trinitrobenzene sulfonic acid (TNBS)-induced rat colitis. Under light anaesthesia with ether, rats were subjected to intracolonic administration of 30㎎ TNBS in 50% ethanol (0.5㎖) and were then sacrificed at 7 or 21 days after colitis induction. The TNBS control group (the saline treated colitic rat) exhibited ulceration and inflammation of the distal colon with formation of granuloma and pathologic connections. Moreover, an increase in colonic myeloperoxidase (MPO) activity (investigated as an index of leukocyte adhesion and accumulation) and an elevated colonic leukotriene B_4(LTB_4) level were observed. The colitic rats received DA-6034 (0.3∼30㎎/㎏) or sulfasalazine (50∼100㎎/㎏), prednisolone (0.3∼3㎎/㎏) after the induction of colitis until they were sacrificed. Oral treatment with DA-6034 resulted in significant reductions of macroscopic colonic damage, colonic inflammation. DA-6034 had a more potent effect than sulfasalazine and prednisolone on macroscopic colonic damage, while it has similar effect with prednisolone on the reduction of colonic LTB_4 synthesis and MPO activity. This study show, therefore, that DA-6034 is effective in attenuating the colonic lesion in an TNBS-induced colitis model. Furthermore, the results suggest that the effect of DA-6034 is partially related to its action on LTB_4 synthesis and MPO inhibition.
Kim, You-Sun,Son, Mi-Won,Ko, Jun-Il,Cho, Hyeon,Yoo, Moo-Hi,Kim, Won-Bae,Song, In-Sung,Kim, Chung-Yong The Pharmaceutical Society of Korea 1999 Archives of Pharmacal Research Vol.22 No.4
Inflammatory bowel disease (IBD) is a multifactorial disorder with unknown etiology and pathogenesis. DA-6034,$ 7-carboxymethyloxy-3^{l}, 4^{l},$ 5-trimethoxy flavone, is a synthetic flavonoid known to possess anti-inflammatory activity. This study was performed to evaluate the oral therapeutic effect of DA-6034 in three experimental animal models of IBD : two chemical-induced IBD models of rats and the human leukocyte antigen (HLA)-B27 transgenic rat model known to develop spontaneous colitis without the use of exogenous agents. Acute chemical colitis was induced by intracolonic instillation of 1.2 ml of 4% acetic acid solution. Prednisolone (1 mg/kg), sulfasalazine (100 mg/kg) and DA-6034 (0.3~3 mg/kg) were orally administered twice daily for 6 days in these rats. In addition, chronic chemical colitis was induced by intracolonic administration of trinitrobenzene sulfonic acid (TNBS) 30 mg in 50% ethanol and agents were orally administered for 6 or 20 days. In chemical-induced IBD models, all of these agents reduced the severity of colitis and specially, DA-6034 (3 mg/kg) showed more potent effect than other drugs in macroscopic lesion score. In HLA-B27 transgenic rats, DA-6034 (3 mg/kg) and prednisolone (0.5 gm/kg) were treated orally twice daily for 6 weeks. The HLA-B27 transgenic rats showed only mild colitis, compared with the chemical-induced colitis models. DA-6034 ameliorated the loose stool and decreased microscopic damage, which is the important indicator of this model. In conclusion, oral therapy of DA-6034 attenuated the macroscopic and histologic damages of the colon in all three experimental models of IBD, which suggest that DA-6034 could be a promising drug in the treatment of IBD.
HPLC를 이용한 생체시료중의 새로운 플라보노이드 유도체인 DA-6034의 분석
이종진(Jong Jin Lee),손미원(Mi Won Son),유무희(Moo Hi Yoo),장민선(Min Sun Jang),김원배(Won Bae Kim),이강춘(Kang Chun Lee) 대한약학회 1998 약학회지 Vol.42 No.2
A high performance liquid chromatographic method was developed for the determination of DA-6034 in biological fluids using internal standard. Plasma containing DA-6034 and internal standard was extracted by liquid-liquid extraction at an acidic pH. After evaporation of the organic layer, the drug and internal standard were reconstituted with mobile phase and injected into the column. They were separated by high performance liquid chromatography on inertsil ODS II column at 334 nm. The detection limit of DA-6034 in plasma was 0.02 mcg/ml. In this method, the range of recovery and coefficients of variation were 96-110% and 0.40-3.78%, respectively. There was no interference from endogenous substances. Urine and bile were analysed using the deproteinization method and the detection limit of DA-6034 was 1mcg/l.