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뇨중 Urinary Dipeptidase 의 근원에 대한 고찰
박행순,김도하,박성광,강성귀,Marlyn Burks,James M . Mullins,Benedict J . Campbell ( Haeng Soon Park,Doh Ha Kim,Sung Kwang Park,Sung Kyew Kang,Marlyn Burks,James M . Mullins,Benedict J . Campbell ) 생화학분자생물학회 1992 BMB Reports Vol.25 No.4
Urinary dipeptidase, an enzyme with β-lactamase activity, was purified from the urine of healthy individuals. The purified enzyme was monophoretic when examined in polyacrylamide gel electrophoresis at pH 8.3, and its molecular mass estimated by HPLC was 227,000 daltons. It catalyzed the hydrolysis of the β-lactam antibiotic, N-formimidoyl-thienamycin (imipenem) with K_m=15.8 mM and V_(max)= 55 μ㏖/min/㎎. Lineweaver-Burk analysis of urinary dipeptidase-catalyzed hydrclysis of imipenem in the presence of cilastatin (Z-S-[6-carboxy-6-{ [2,2-dimethyl-(S)-cyclopropyl carboxy]-amino}-5-hexenyl]-L-cysteine) demonstrated reversible, competitive inhibition. The K_i for the competitive inhibitor, cilastatin, was 6 M. Renal dipeptidase was solubilized with n-butanol from membranes prepared from the kidneys of renal stone patients and purified. The two enzymes showed many properties in common including molecular mass, substrate specificity, kinetic parameters, inhibition by cilastatin, pH optima, electrophoretic mobility, and immunological cross-reactivity. Disintegration of kidney tubules and release of peptidase activity into the urine of rabbits treated with sublethal levels of the nephrotoxic agent, cephaloridine, suggest that the urinary dipeptidase originates from the proximal tubules of mammalian kidneys.
에어탈 정(아세클로페낙 100 mg)에 대한 세니탈 정의 생물학적 동등성
김수진,오인준,박행순,서세민,서순팔,이용복 전남대학교 약품개발연구소 1998 약품개발연구지 Vol.7 No.1
Bioequivalence of two aoeclofenac tablets, the Airtal^(TM) (Daewoong Pharmaceutical Co., Ltd.) and the Senital^(TM) (Hana Pharmaceutical Co.. Ltd.), was evaluated according to the guideline of KFDA. Fourteen normal male volunteers (age 20∼29 years old) were divided into two groups and a randomized 2×2 cross-over study was employed. After one tablet containing 100 ㎎ of aceclofenac was orally administered, blood was taken at predetermined time intervals and the concentration of aceclofenac in plasma was determined with an HPLC method using UV detector. The pharmacokinetic parameters (C_(max), T_(max) and AUC_t were calculated and ANOVA was utilized for the statistical analysis of parameters. The results showed that the differences in C_(max), T_(max) and AUC_t between two tablets were 3.69%. 2.99% and 0.51%, respectively. The powers (1-β) for C_(max), T_(max) and AUC_t were 87.85%. 98.70% and more than 99%, respectively. Detectable differences (Δ) and confidence intervals were all less than ±20%. All of these parameters met the criteria of KFDA for bioequivalence, indicating that Senital^(TM) tablet is bioequivalent to Airtal^(TM) tablet.
조영창,이광열,강복윤,박행순 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.5
Phenylarsine oxide (PAO), a membrane-permeable trivalent arsenical, is widely used as an inhibitor of protein tyrosine phosphatases. It reacts with vicinal sulfhydryl groups of proteins to form stable ring structures. Here we show the regulatory function of PAO in immune responses from macrophages. PAO significantly induced the secretion of interleukin (IL)-12p40 in lipopolysaccharide-stimulated macrophages. The mRNA expression and the gene promoter activity of IL-12p40 were enhanced by PAO. These results suggest that PAO may enhance IL-12p40 production at the transcriptional level. Furthermore, the effects of PAO on several signaling molecules regulating IL-12p40 expression were investigated. PAO attenuated the induced binding activity of cAMP response element (CRE), but not of NF-κB. Moreover, CRE promoter activity was dose-dependently inhibited by PAO and the increased secretion of IL-12p40 by PAO was reduced by forskolin, a cAMP activator. These results suggest that PAO enhances IL-12p40 production by inhibiting CRE activity.
척출 냉혈동물 심방의 Alpha-Adrenoceptors에 관한 연구(I) 개구리 심방의 clonidine, oxymetazoline 및 phenylephrine에 대한 반응
최수형(Soo Hyung Choi),박행순(Haeng Soon Park),신동호(Dong Ho Shin) 대한약학회 1988 약학회지 Vol.32 No.2
Effects of the selective alpha-adrenoceptor agonists, clonidine, oxymetazoline and phenylephrine, on heart rate and contractile force were investigated in the isolated frog atria and it was attempted to examine the influence of adrenoceptor antagonist upon those. Clonidine produced dose-dependent negative chronotropic and positive inotropic effects. The negative chronotropic effect was significantly attenuated in the presence of prazosin and yohimbine but not propranolol. The positive inotropic effect was significantly attenuated by prazosin, yohimbine and propranolol. Oxymetazoline produced dose-dependent negative chronotropic and inotropic effects. The negative chronotropic effect was significantly attenuated in the presence of prazosin, which was partially augmented by yohimbine but was not affected by propranolol. The negative inotropic effect was not affected by propranolol but it was partially augmented by yohimbine and was partially attenuated by prazosin. Phenylephrine produced dose-dependent positive chronotropic and inotropic effects. The positive chronotropic and inotropic effect were significantly attenuated in the presence of propranolol but were not affected by prazosin and yohimbine. These results suggest that the negative chronotropic effect by clonidine and oxymetazoline is mediated by alpha-adrenoceptors, the positive chronotropic and inotropic effects by phenylephrine are mediated by beta-adrenoceptors, and alpha-adrenoceptors mediated the inhibitory chronotropic responses exists in the isolated frog atria.
하이트린 정(테라조신 2 mg)에 대한 테라신 정의 생물학적 동등성
김수진,임동구,오인준,신상철,박행순,문재동,이용복 전남대학교 약품개발연구소 1999 약품개발연구지 Vol.8 No.1
Bioequivalence of two terazosin tablets, the Hytrine^(TM) (Il-Yang Pharmaceutical Co., Ltd.) and the Terasin^(TM) (Daewon Pharmaceutical Co., Ltd.), was evaluated according to the guideline of KFDA. Sixteen normal male volunteers (21∼30 years old) were divided into two groups and a randomized 2×2 cross-over study was employed. After one tablet containing 2 ㎎ of terazosin was orally administered, blood was taken at predetermined time intervals and the concentration of terazosin in serum was determined with a HPLC method using spectrofluorometric detector. The pharmacokinetic parameters (AUC_t, C_(max) and T_(max)) were calculated and ANOVA was utilized for the statistical analysis of the parameters. The results showed that the differences in AUC_t, C_(max) and T_(max) between two tablets were 6.02%, 3.44% and -3.67%, respectively. The powers (1-β) for AUC_t, C_(max) and T_(max), were 98.05%, 98.34% and 29.81%, respectively. Detectable differences (Δ) and confidence intervals were all less than t 20% except T_(max), AUC_t and C_(max) met the criteria of KFDA for bioequivalence, indicating that Terasin^(TM) tablet is bioequivalent to Hytrine^(TM) tablet.