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한국 독사독으로부터의 혈전 용해제 개발에 관한 연구 1. 살모사 ( A. bromhoffi brevicaudus ) 사독 Protease 의 정제에 관한 연구
이문한(Mun Han Lee),김병재(Byoung Jae KIm),임종섭(Jong Seop Rim),이항(Hang Lee),이혜숙(Hye Suk Lee),김종호(Jong Ho Kim),채창수(Chang Su Chai) 한국응용약물학회 1995 Biomolecules & Therapeutics(구 응용약물학회지) Vol.3 No.2
Fibrinolytic and fibrinogenolytic activities of the venoms from the Korean snakes, Agkistrodon caliginosus, Agkistrodon saxatilis and Agkistrodon blomhoffi brevicaudus were compared by fibrin-plate method and polyacrylamide gel electrophoresis, respectively. The venom from A. blomhoffi brevicaudus showed the highest degree of fibrin(ogen)olytic activity, and a protease with the fibrin(ogen)olytic activity was purified by p-aminobenzamidine affinity chromatography and DEAF ion-exchange chromatography. The purified enzyme had a molecular weight of 50,800 and a capability to degrade the Bβ-chain of fibrinogen preferentially to the Aα-chain, but not the γ-chain. Fibrinolytic activity of the purified enzyme was approximately 3.8 plasmin unit/mg protein.
마이크로에멀젼으로 제제 설계된 피록시캄 외용제의 약물동력학적 특성 및 약효 평가
윤범진(Bum Jin Yun),박은석(Eun Seok Park),지상철(Sang Cheol Chi) 한국응용약물학회 1999 Biomolecules & Therapeutics(구 응용약물학회지) Vol.7 No.1
The pharmacological activities and pharmacokinetic aspects of a topical microemulsion (KDPM) containing 0.5% piroxicam were evaluated after its topical application compared with a commercially available 0.5% piroxicam gel (R gel). When the pharmacological activities were evaluated with the carrageenaninduced paw edema model, KDPM showed 55.6% edema inhibition, while R gel resulted in 37.1%. With the adjuvant-induced arthritis model, KDPM also resulted in the better pharmacological activities than R gel. The relative bioavailability of KDPM based on R gel was 176% in rabbits.
김재현,박창원,박정식,홍연탁 한국응용약물학회 1993 Biomolecules & Therapeutics(구 응용약물학회지) Vol.1 No.1
DNA adducts induced by putative chemical related to carcinogenesis were detected and determined by (32)^P-Postlabelling assay after exposure of 4 compounds comprising two azo dyes (amaranth, new coccine) and two flavonoid compounds (rutin, quercetin) to ICR mouse. DNA was isolated from mouse liver and digested enzymatically to deoxyribonucleoside 3'-monophosphate. The postincubation of DNA digests with nuclease P1 before (32)^P-labelling enhanced the technique's sensitivity. Nuclease P1 cleaves deoxyribonucleoside 3'-monophosphates of normal nucleotides to deoxyribonucleosides which do not serve as substrates for polynucleotide kinase, while most of adducts were found to be totally or partially resistant to the 3'-dephosphorylating action of nuclease Pl. The adducted deoxyribonucleoside 3'-monophosphate was converted to 5'-(32)^P-labelled deoxynucleoside 3',5'-bisphosphate by T4 polynucleotide kinase. The nucleotides were separated by anion-exchange thin layer chromatography(TLC) on polyethyleneimine cellulose by 4-dimensional or 2-dimensional TLC then detected by autoradiography. The results show that DNA adducts were detected in liver DNA of ICR mouse after administration of amaranth and quercetin by 2-dimensional and/or 4-dimensional TLC.
한국 Streptomyces sp. 로 부터 분리한 방향족 화합물과 지질 화합물의 세포독성 연구
신석우(Suck Woo Shin),염곤(Kon Ryeom) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.2
In an effort to screen new selective antitumor agents from the broth of soil microorganism, cytotoxicity oriented screening was performed against tumor cells and 3 compounds (Compound 1, 2 and 3) were isolated from Streptomyces parvullus ISP 5048 and their chemical structures were determined. Among these compounds, Compound 2 showed the highest cytotoxicity against P388D1 and L1210. While the IC_(50) values of compound 2 against P388D1 and L1210 were 0.073 ㎍/㎖ and 0.07 ㎍/㎖, respectively, and the IC_(50) value of Compound 3 was 0.17 ㎍/㎖ against human lung cancer cells, A549, the cytotoxicity of Compound 2 and 3 against normal cell line, Vero E6 cell was about 4- and 8-fold lower than that of adriamycin. Based on the chemical analysis data, Compound 3 was octacosamicine A, a known antibiotic, which was reported by Dobasih et al. (1988). Taken together the results demonstrated that Compound 2 and Compound 3 has the possibility to be developed as antitumor agent because of its potent cytotoxicity as well as high selectivity against various cancer cell lines.
Pyrimidine Nucleoside 유도체들의 합성 및 약물학적 효능 검색
신혜순(Hea Soon Shin),이희주(Hee Joo Lee) 한국응용약물학회 1995 Biomolecules & Therapeutics(구 응용약물학회지) Vol.3 No.3
Several acyclonucleoside analogues of pyrimidine base and N¹-derivatives of 5-fluorouracil have been synthesized and evaluated for their biological effects. When tested with in vitro Lekemia L1210 cells, the 5-fluorouracil derivatives exhibited slightly higher antitumor activity than the parent 5-fluorouracil. When tested against Herpes Simplex Virus type 1 and type 2 cultured in the Vero cell, the 5-fluorouracil derivatives showed weak antiviral activity.
정요찬(Yo Chan Jeong),윤효인(Hyo In Yun),조명행(Myung Haing Cho),박병권(Byung Kweon Park),박일현(Il Hyun Park),김복환(Bok Hwan Kim),송동호(Dong Ho Song) 한국응용약물학회 1996 Biomolecules & Therapeutics(구 응용약물학회지) Vol.4 No.3
The purpose of this study was to determine pharmacokinetic parameters and tissue distribution pattern of urinary trypsin inhibitor(UTI) in Sprague-Dawley rats. Na^(125)I was conjugated to UTI to make ^(125)I-UTI and the concentrations were determined by γ counter. With the aid of nonlinear least-square regression analysis for i.v. bolus injection of 1,000 unit UTI including ^(125)I-UTI, the temporal concentration curves were best fitted by 2-compartment open model. The distribution phase half-life was 0.39±0.02 hours whereas the elimination half-life was 12.99±1.05 hours in male rats. The volume of distribution and total body clearance in male rats were 0.28±0.01 l/kg and 83.16±1.15 ml/kg/h, respectively. We could not find any difference of pharmacokinetic parameters of UTI between male and female rats. UTI were distributed widely in rat organs. In both male and female rats, the kidney was the highest distributed organ. Amount of UTI in 24 hour cumulative urine in male rats was 36.22±8.74% and that in 48 hours was 43.32±10.55%. Excretion via feces was very scanty, with the 24 hours cumulative amount being only 2.76±0.97%. This data suggest the main excretion route of UTI is urine.
한국 독사독으로부터의 혈전 용해제 개발에 관한 연구 2. 살모사 ( A. bromhoffi brevicaudus ) 사독 Protease 의 특성과 혈전 용해능에 관한 연구
김병재(Byoung Jae KIm),이문한(Mun Han Lee),임종섭(Jong Seop Rim),이항(Hang Lee),이혜숙(Hye Suk Lee),김종호(Jong Ho Kim),채창수(Chang Su Chai) 한국응용약물학회 1995 Biomolecules & Therapeutics(구 응용약물학회지) Vol.3 No.2
The biochemical properties of the fibrinolytic protease of 50,800 Da isolated from the venom of Agkistrodon blomhoffi brevicaudus were characterized. The enzyme hydrolyzed the carboxyl side of arginine in the synthetic chromogenic peptides, N-Benzoyl-Phe-Val-Arg-pNA and N p-Tosyl-Gly-Pro-Arg-pNA, and the enzyme activity was inhibited by phenylmethylsulfonylfluoride indicating that the enzyme belongs to the serine protease family. The protease showed maximum activity at pH 7.5 and inhibited by ZnCl₂, CuSO₄, but not by soybean trypsin inhibitor, pepstatin A, 2-mercaptoethanol and EDTA. The Km value determined with Np-Tosyl-Gly-Pro-Arg-pNA was 0.2 mM. The thrombolytic activity of the purified enzyme was evaluated by platelet aggregation test in rabbits. While the platelet count ratio in blood of the rabbits injected with thrombin alone declined from 1.0 to 0.6 within 7 min and maintained around 0.6 for 24 hours thereafter, the ratio rapidly recovered from around 0.6 to 0.8 in 1 hr, to 1.0 in 24 hrs when the rabbits were sequentially treated with thrombin and the purified enzyme. The result showed that the serine protease from A. blomhoffi brevicoudus of 50,800 Da had a thrombolytic activity in vivo and the enzyme might be developed as a therapuetic agent for the treatment of thrombic disease.
랫드에서 fluoroquinolone 항균제 DW-116 의 단회 경구투여에 의한 태반통과와 약물동태연구
김종춘(Jong Chun Kim),윤효인(Hyo In Yun),신호철(Ho Chul Shin),허정두(Jeong Du Hur),이종화(Jong Hwa Lee),정문구(Moon Koo Chung) 한국응용약물학회 2002 Biomolecules & Therapeutics(구 응용약물학회지) Vol.10 No.1
N/A The present study was conducted to investigate the placental transfer and pharmacokinetics of the fluoroquinolone antibacterial DW-116 in pregnant rats. The placental transfer and pharmacokinetics of DW-116 were examined after a single oral dose of 500 ㎎ [^14C]DW-116/㎏ on gestational day 18. Maternal and fetal tissues were collected at 0.17.0.5, 1, 2, 4, 8, and 24 h after dosing. Maximum radioactivity was detected in maternal plasma, placenta, and whole fetus at 1 h, and in amniotic plasma at 4 h after dosing. Thereafter, radioactivity gradually disappeared from these tissues and was 16∼28% of maximum levels at 24 h after dosing. Radioactivity in whole fetus were higher than those in the maternal plasma and placenta. The T_(1/2,abs), T_(1/2,β), AUC, T_max, and C_max in the maternal plasma were approximately 6 min, 13.3 h, 1620 ug^*hr/ml, 0.5 h, and 136 ug/ml, respectively. Those in the placenta were approximately 20 min, 12.3 h, 2150 ug^*h/ml, 1.0 h, and 172 ug/ml, respectively. Those in the whole fetus were 13 min, 12.8 h, 2549 ug^*h/ml, 1 h, and 191 ug/ml, respectively. In the amniotic fluid of maternal uterus, the T_(1/2,abs), T_(1/2,β), AUC, T_max, and C_max were approximately 1.3 h, 9.3 h, 2508 ug^*h/ml, 4.4 h, and 135 ug/ml, respectively. While DW-116 disappeared biphasically from maternal plasma, whole fetus and placenta, it was eliminated monophasically from amniotic fluid. In conclusion, this study demonstrated that the absorption and distribution of DW- 116 in maternal plasma and placenta were extensively rapid, and that the test chemical well passed the blood-placenta barrier and was transferred to the fetus.
유전자 재조합 사람형 erythropoietin, GC-rhEPO의 약물동태 및 조직분포
김선돈 ( Sun Don Kim ),한성규 ( Seong Kyu Han ),이호성 ( Ho Sung Lee ),김성남 ( Seong Nam Kim ),정원휘 ( Wo Nee Chong ),백대현 ( Dae Hyun Baek ),조은성 ( Eun Sung Cho ),허재욱 ( Jae Wook Huh ),류판동 ( Pan Dong Ryu ) 한국응용약물학회 2000 Biomolecules & Therapeutics(구 응용약물학회지) Vol.8 No.2