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김동욱(Dong Wook Kim),박은석(Eun Seok Park),지상철(Sang Cheol Chi) 한국응용약물학회 1999 Biomolecules & Therapeutics(구 응용약물학회지) Vol.7 No.2
The effects of various drugs on the alleviation of the symptoms of chemical burns were evaluated in mice to formulate topical antiblister preparations. After a chemical burn was induced on the mouse dorsal skin with 2-chloroethylethyl sulfide, the drug was applied on the disease site. The effectiveness of the drug was evaluated by determining blister size, necrosis score of skin and appearance of the chemical burns induced. It showed that steroids and aminoglycoside antibiotics had a tendency to protect skin cell, and antihistamines decreased the size of chemical burns. While oleaginous base resulted in deleterious effect, hydrophilic base didn`t show a significant difference on the alleviation of the chemical burn symptoms compared to the control.
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.
Glucose - diethyldithiocarbamate 가 흰쥐의 약물 대사 효소에 미치는 영향
최병기(Byung Ki Choi),신혜주(Hye Joo Shin) 한국응용약물학회 2000 Biomolecules & Therapeutics(구 응용약물학회지) Vol.8 No.4
The modulation of cytochrome P450(P450) activities and glutathione S-transferase (GST) was investigated after i.p. administration of glucose-diethyldithiocarbamate (Glu-DDTC) to rats. P450 1A2 and 2E1 activities were inhibited by 60% 4 hr after the administration of 200 mg Glu-DDTC/kg and those activities were recovered to original levels 24 hr after dosing. In contrast, GST activities were enhanced up to 24 hr after dosing. These results seem to be due to the bifunctional activity of Glu-DDTC. Glu-DDTC acts as an inhibitor of P450 enzymes as well as inducer of GST enzyme. Glu-DDTC inhibited PNP hydroxylation (P450 2E1) and ethoxycoumarin O-deethylation (P450 1A2) in a dose-dependent manner up to 200 mg/kg wherease it did not affect testosterone 6β-hydroxylation (P450 3A) and pentoxyresorufin O-dealkylation (P450 2B) activities. Induction of GST activity toward 1-chloro-2,4-dinitrobenzene (CDNB) and 1,2-dichloro-4-nitrobenzenen (DCNB) was dependent on the dose of Glu-DDTC and no species difference in the GST induction was seen between rat and mouse. Amoung GST subunits, Ya, Ybl and partially Yb2 were induced by Glu-DDTC as conjugated by western blotting. The levels Yp, Yk and Yc subunits were not affected by Glu-DDTC treatment. Therefore the enhanced activity of GST toward CDNB and DCNB might be due to the induction of Ya, Yb1 and partially Yb2 subunits. In conclusion, Glu-DDTC selectively inhibited P450 1A2 and P450 2E1 activities whereas it enhanced Ya, Yb1 subunits and partially Yb2 subunits of GST and the antimutagenic activity of this compound might be attributed from the modulation of these enzyme activities in animals.
CJ-50001 (recombinant human granulocyte-colony stimulating factor) 의 흰주와 개에서의 약물동태학적 연구
김성남(Sung Nam Kim),신재규(Jae Kyu Shin),이수정(Soo Jung Lee),정용환(Yong Hwan Jung),하석훈(Suk Hoon Ha),김기완(Ki Wan Kim),고형곤(Hyung Kon Koh),김제학(Je Hak Kim) 한국응용약물학회 1998 Biomolecules & Therapeutics(구 응용약물학회지) Vol.6 No.4
The pharmacokinetics of CJ-50001 (recombinant human granulocyte-colony stimulating factor, developed by R&D center of Cheil Jedang Corp.) were investigated in rats and dogs. The serum concentrations of CJ-50001 were measured by a sandwich enzyme immunoassay. After single intravenous (iv) administration of CJ-50001 to rats at a dose of 5 ㎍/kg, the mean terminal half-life and area under the concentration-time curve (AUC) were 0.96 h and 124.49 ㎍·/ml, respectively. After single subcutaneous (sc) administration at the same dose, maximum serum concentration was observed at about 2 hours after administration, and the mean terminal half-life, AUC and the bioavailability were 1.11 h, 63.58 ㎍·h/ml and 51.07%, respectively. In repeated dosing studies, CJ-50001 was administered iv and sc to rats at a daily dose of 5 ㎍/kg for 7 days. The pharmacokinetic parameters, such as mean AUC and terminal half-life, were not significantly different from those of single administration. Following single iv and sc administration of CJ50001 to dogs at a dose of 5 ㎍/kg, mean AUCs were much higher than those of rats, due to the decreased clearence (CL). After sc administration to dogs, maximum serum concentration was observed at 2∼4 hours after administration and the bioavailability was 54.60%.
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.
곽혜선(Hye Sun Gwak),전인구(In Koo Chun) 한국응용약물학회 2000 Biomolecules & Therapeutics(구 응용약물학회지) Vol.8 No.4
Physicochemical properties of aspalatone (acetylsalicylic acid maltol ester, AM), which has been recently found to have an antithrombotic effect, were studied in terms of solubility, dissolution, partition coefficient (Pc) and stability. The solubility of AM at 37℃ was about 1.2 mg/ml and the P_c value for n-octanol/ water and chloroform/water was 11.4 and 382.6, respectively. Dissolution rates of AM at pH 1.2 and 6.8 were more than 80% within 30 min. The degradation of AM followed apparent first-order kinetics, and was dependent on temperature, pH and ionic strength. From the pH-rate profile, the optimal pH was found to be at around 4.0. Half-lives at pH 1.2 and 6.8 were 33.5 and 44.4 hr, respectively. The degradation rate of AM at pH 1.2 was somewhat faster than that of aspirin, but at pH 7.0, the degradation rate of AM was slower than that of aspirin.
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 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.