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주사제용 세파로스포린계 항생제 LB10522의 in vitro 및 in vivo 항균력
백경숙(Kyung Sook Park),오정인(Jeong In Oh),김무용(Mu Yong Kim),김인철(In Chull Kim),곽진환(Jin Hwan Kwak) 대한약학회 1996 약학회지 Vol.40 No.1
The in vitro antibacterial activities of LB10522, a new catechol-substituted cephalosporin, were compared with those of cefpirome, ceftazidime, ceftriaxone, and cefoperazone against clinical isolates and laboratory standard anaerobes. LB10522 had broad spectrum antibacterial activities against both gram-positive and gram-negative microorganisms. It was most active against gram-positve bacteria among the reference cephalosporins tested. Against gram-negative strains such as the family Enterobacteriaceae, LB10522 showed an activity comparable to that of cefpirome. But LB10522 was more potent than ceftazidime, ceftriaxone and cefoperazone. In particular, Pseudomonas aeruginosa was highly susceptible to LB10522, which was 32-fold and 64-fold more active than ceftazidime and cefpirome, respectively. Against anaerobic strains, the activity of LB10522 was similar to those of reference compounds. LB10522 exhibited potent therapeutic activities against experimental local infections in mice. The therapeutic effect of LB10522 against urinary tract infection (UTI) caused by P. aeruginosa 1912E in mice was superior to that of cefpirome. Against experimental respiratory tract infection (RTI) caused by K. pneumoniae DT-S in mice, LB10522 was as effective as cefpirome. The in vivo efficacy of LB10522 was correlated well with its in vitro activity.
카테콜 치환체를 가진 세파로스포린계 항생제 LB10522의 작용기전
김무용,오정인,백경숙,김인철,곽진환,Kim, Mu-Yong,Oh, Jeong-In,Paek, Kyoung-Sook,Kim, In-Chull,Kwak, Jin-Hwan 대한약학회 1996 약학회지 Vol.40 No.1
LB10522 is a new parenteral broad spectrum cephalosporin with a catechol moiety at C-7 position of beta-lactam ring. This compound can utilize tonB-dependent iron transp ort system in addition to porin proteins to enter bacterial periplasmic space and access to penicillin-binding proteins (PBPs) which are the lethal targets of ${\beta}$-lactam antibiotics. The chelating activity of LB10522 to metal iron was measured by spectrophotometrically scanning the absorbance from 200 to 900nm. When $FeCl_3$ was added, optical density was increased between 450 and 800nm. LB10522 was more active against gram-negative strains in iron-depleted media than in iron-replete media. This is due to the increased expression of iron transport channels in iron-depleted condition. LB10522 showed a similar activity against E. coli DC2 (permeability mutant) and E. coli DCO (wild type strain) in both iron-depleted and iron-replete media, indicating a minimal permeaility barrier for LB10522 uptake. LB10522 had high affinities to PBP 3 and PBP 1A, 1B of E. coli. By blocking these proteins, LB10522 caused inhibition of cell division and the eventual death of cells. This result was correlated well with the morphological changes in E. coli exposed to LB10522. Although the in vitro MIC of LB10522 against P. aeruginosa 1912E mutant (tonB) was 8-times higher than that of the P. aeruginosa 1912E parent strain, LB10522 showed a similar in vivo protection efficacy against both strains in the mouse systemic infection model. This result suggested that tonB mutant, which requires a high level of iron for normal growth, might have a difficulty in surviving in their host with an iron-limited environment.
생쥐의 호흡기 감염에 대한 퀴놀론계 항생제 LB20304a의 치료 효과
안미정(Mi Jeong Ahn),김무용(Mu Yong Kim),백경숙(Kyoung Sook Paek),김인철(In Chull Kim),곽진환(Jin Hwan Kwak) 대한약학회 1996 약학회지 Vol.40 No.4
The therapeutic activity of LB20304a was examined on experimental respiratory tract infection (RTI) caused by Klebsiella pneumoniae DT-S in mice. A single oral dose of LB20304a (1.2mg/mouse) showed a rapid bacteriocidal activity in lung tissue at 4,7 and 24h after administration of drug. The in vivo activity of LB20304a was comparable to that of ciprofloxacin against K. pneumoniae infection, although in vitro MIC of LB20304a was four-fold higher than that of ciprofloxacin.
김낙두(Nak Doo Kim),김인철(In Chull Kim) 한국생약학회 1978 생약학회지 Vol.9 No.1
Total saponins and ether extracts of red and white ginseng ware obtained and their effects on blood pressure in cat and their histamine liberating activities in rabbits were measured. 1) Ether extract of red ginseng showed a transient hypotensive effect and subseqnently showed a remarkable and persistent hypotensive effect, whereas other three fractions, such as saponin fractions of red and white ginseng and ether extract of white ginseng showed only a initial transient hypotensive effects. 2) Histamine levels liberated into blood after administration of each fractions measured by the bioassay with guinea pig ileum. Ether extract of red ginseng immediately increased histamine contents in plasma but the histamine levels decreased to normal level within 10 min in spite of decreased blood pressure was sustained. Although white ginseng saponin lowered blood pressure immediately when it is admininstered, histamine release was observed after 10min. The results suggest that hypotensive effects of ginseng seems to have no correlation with the histamine liberating activity. Ginseng appears to show hypotensive effect via some other mechanisms.
김낙두(Nak Doo Kim),백철기(Chul Ki Baik),김인철(In Chull Kim) 한국생약학회 1977 생약학회지 Vol.8 No.3
Aspidium ether extract was obtained from Dryopteris crassirhizoma(Aspidiaceae), which is widely distributed in Korea and its vermicidal effect on the rats infected with Hymenolepis diminuta was investigated. Effects of Aspidium ether extract purchased from the market, several fractions obtained from the seed of Torreya nucifora and bithionol were also compared. Vermicidal effect of Aspidium against Hymenolepis diminuta was found only in one-third of the rats used for investigation and the effect of the fresh Aspidium ether extract was similar to that of Aspidium ether extract purchased from market. However, it was observed that the whole seeds of Torreya nucifera (Torreyaceae) and its residue from which oil fraction was removed as well as bithionol were highly effective against Hymenolepis diminuta.
새로운 플루오로퀴놀론계 항생제 LB20304a가 생쥐의 맹장내 세균총에 미치는 영향
안미정(Mi Jeong Ahn),백경숙(Kyoung Sook Paek),김무용(Mu Yong Kim),김인철(In Chull Kim),곽진환(Jin Hwan Kwak) 대한약학회 1996 약학회지 Vol.40 No.3
The influence of LB20304a, a new fluoroquinolone antibiotic agent, on microflora of caecum in mice was compared with those of ciprofloxacin and piperacillin after administration of drugs for 5 days. Selective medium (CCFMA) was used for the isolation of Clostridium difficile from the specimens of mouse caecum. The emergence of C. difficile in mouse caecum induced by LB20304a was lower than that by ciprofloxacin or piperacillin at day 1 and day 7 after completing administration of drugs.