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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.
지상철(Sang Cheol Chi),박은석(Eun Seok Park),단현광(Hyun Kwang Tan),이윤석(Yun Seok Rhee) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.4
The effects of formulation variables of topical lotion on the skin permeation of ketoprofen were evaluated using excised rat skins. The formulation variables were the amounts of poloxamer 407, drug and ethanol, and penetration enhancers. The Keshary-Chien diffusion cells were used for the diffusion study. The flux of ketoprofen linearly decreased as the concentration of poloxamer increased from 5% to 15% in the preparation, and linearly increased as the amount of drug increased. Penetration enhancers such as fatty acids and fatty alcohols showed markedly enhancing effects at the level of 5%. Among them, the highest flux was shown in linolenic acid. From these results, optimum formula containing 3% ketoprofen, 5% poloxamer 407, 40% ethanol and 5% linolenic acid having the flux of 537.6 ㎍/㎠/hr were noted.
단현광(Hyun Kwang Tan),배준호(Joon Ho Bae),박은석(Eun Seok Park),지상철(Sang Cheol Chi) 한국응용약물학회 1998 Biomolecules & Therapeutics(구 응용약물학회지) Vol.6 No.1
The pharmacokinetic properties and antiinflammatory activity of 3% ketoprofen lotion (ID-lotion), formulated with poloxamer 407, were evaluated using rats. For the pharmacokinetic study, the lotion, at the dose of 4.5 mg/kg, was applied on the dorsal skin of rats and the drug concentration in plasma was determined using an HPLC method. As references, ketoprofen suspended in saline was administered orally, and Elotion, which is a 3% ketoprofen lotion in the Japanese market, was applied transdermally. Following the transdermal application of ID-lotion and E-lotion, C_(max) were 316±22.3 ng/ml and 163 ±12.2 ng/ml, respectively, at the same T_(max) of 2 hours postdose, while C_(max) and T_(max) after oral administration of the drug were 1,030 ±89.1 ng/ml and 0.25 hours, respectively. Relative bioavailabilities of ID-lotion and E-lotion were 69.3% and 34.2%, respectively. The antiinflammatory activity of the two 3% ketoprofen lotions was evaluated with carrageenen-induced edema method after 50 mg of the lotions was applied on the paw of rats. ID-lotion showed 67.6% inhibition of the edema formation, while E-lotion showed 34.7%. The calculated EDT after transdermal application of ID-lotion was 2.5 mg/kg, while that after oral administration was 7.0 mg/kg. Based on these results, the relative equiponderal availability of ID-lotion was 296% compared to the oral administration of ketoprofen.
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
랫트에서 한국형유산균인 Bifidobacterium breve K-110 , K-111 및 B. infantis K-525 균주제제의 경구투여 급성독성
이영경(Young Kyoung Rhee),한명주(Myung Joo Han),최응칠(Eung Chil Choi),김동현(Dong Hyun KIm) 한국응용약물학회 1998 Biomolecules & Therapeutics(구 응용약물학회지) Vol.6 No.4
Acute oral toxicity of Bifidobacterium breve K-110, Bifidobacterium breve K-111, Bifidobacterium infantis K-525 were studied in Sprague-Dawley rats of both sexes. In this study, we examined number of deaths, clinical signs, body weight and gross findings for 14 days after single oral administration of B. breve K-110, B. breve K-111 or B. infantis K-525 with different levels. They did not show any toxic effect in rats and oral LD_(50) value was over 5 g/㎏ in rats.
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.