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신규 퀴놀론 항균제 DW-116 의 in vitro 및 in vovp 항균활성
이진(Jin Lee),정용호(Yong Ho Chung),윤성준(Sung June Yoon),이덕근(Dug Keun Lee),황연하(Yun Ha Hwang),한경오(Kyung Oh Han),양희복(Hee Bog Yang) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.2
The in vitro and in vivo antibacterial activity of DW-116, a newly synthesized fluoroquinolone, were compared with those of other quinolones. DW-116 exhibited more potent antibacterial activity than rufloxacin and lower activity than ofloxacin and ciprofloxacin in in vitro assay. But, DW-116 particularly showed strong activity against the family of staphylococci including methicillin-sensitive staphylococcus and its activity was more active than that of ciprofloxacin. The time-kill curve studies showed rapid bactericidal activity for DW-116. The post-antibiotic effect of DW-116 was observed between 0.66 and 5 hours. The therapeutic efficacy of DW-116 against respiratory infection with P. aeruginosa was as strong as that of ciprofloxacin and its effect against urinary tract infection with E. coli was more effective than rufloxacin. The excellent therapeutic efficacy of DW-116 against these local infections is due to its good pharmacokinetic profiles.
마우스에서의 DW-166HC (Holmium-165-chitosan) 에 대한 급성독성
이원용(Won Yong Lee),이진(Jin Lee),문은이(Eun Yi Moon),남순철(Soon Chul Nam),이덕근(Dug Keun Lee),윤성준(Sung June Yoon) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.1
DW-166HC (^(166)Holmium-chitosan) is a complex of ^(166)Ho, (β- and γ- ray emitter, and chitosan, a polymer of glucosamine, with radiotherapeutic potential. The current study was performed to determine the acute toxicities of ^(165)Ho-chitosan in mice by two different routes of administration. The both sex mice were given a single intravenous bolus injection of ^(165)Ho-chitosan complex at doses of 12, 10, 6, 5 and 4 mg/kg or subcutaneous administration at doses of 600, 500, 400 and 300 mg/kg. Chitosan was dosed to control animals as 16 and 800 mg/kg, intravenously and subcutaneously, respectively. The doses of ^(165)Ho-chitosan complex were expressed as ^(165)holmium nitrate pentahydrate and the ratio of ^(165)Ho(NO₃)₃, ·5H₂0 to chitosan was 3/4. Severe convulsion and respiratory failure were followed by death within 10 min after intravenous dosing. Transient unilateral hindlimb hypokinesias were found in two mice of 5 mg/kg dosing group during the study period. No abnormalities were observed during the necropsy of survived animals in intravenous dosing group. Only one male animal was found dead in 500 mg/kg subcutaneously dosed group. Alopecia with or without cutaneous ulcer were found in most mice including control animals. During necropsy, omental adhesion was observed in all dose ranges and enlarged spleen was found in several animals including control group. It is suggested that the acute intravenous LD_(50)s for male and female mice were 4.90 and 6.03 mg/kg, respectively. The lowest lethal dose in male was 500 mg/kg by subcutaneous administration.
한대석(Dae Suk Han),이덕근(Dug Keun Lee) 한국생약학회 1985 생약학회지 Vol.16 No.3
The optimal condition for the determination of saikosaponin a and d, the major pharmacollogically active saponins of the roots of Bupleurum falcatum, was studied with the conversion of these saponins into diene saponins (saikosaponin b₁ and b₂). The complete separation and quantitative analysis of these saponins were performed by the method of high performance liquid chromatography using NH₂ column. The conversion of saikosaponin a and d into diene saponins under gastric pH was calculated. Thirty-three percent of saikosaponin a was converted to saikosaponin b₁ and 63 percent of saikosaponin d was converted to saikosaponin b₂.
문은이(Eun Yi Moon),이진(Jin Lee),최정하(Chung Ha Choi),이치우(Chi Woo Lee),정용호(Yong Ho Chung),윤성준(Sung June Yoon),이덕근(Dug Keun Lee) 한국응용약물학회 1996 Biomolecules & Therapeutics(구 응용약물학회지) Vol.4 No.3
DW-116 {1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid hydrochloride} is a new quinolone antibiotic with a broad antibacterial spectrum against G(+) and G(-) bacteria. DW-116 was evaluated for the appearance of micronucleus in polychromatic erythrocytes (PCEs) of mouse bone marrow cells after intraperitoneal and oral single administration. We prepared the bone marrow cells at 30hr after drug administration and they were used for measuring PCE with micronucleus. The results showed there was no statistically significant increase in the numbers of PCEs with micronucleus in all DW-116 administered groups compared with a negative control group. The results also showed that the ratio of normochromatic erythrocytes(NCEs) to PCEs of all DW-l16 administered groups was not significantly different from that of a negative control group. These results suggested that DW-116 may not cause any chromosomal damage and it has no in vivo mutagenic potential under these experimental conditions.
문은이(Eun Yi Moon),이진(Jin Lee),이원용(Won Yong Lee),최청하(Chung Ha Choi),이덕근(Dug Keun Lee),유제만(Jei Man Ryu),정용호(Yong Ho Chung),윤성준(Sung June Yoon),박경배(Kyung Bae Park) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.3
DW-166HC (^(166)Holmium (^(166)Ho)-Chitosan complex) is a new radiopharmaceutic anticancer agent with a broad anti-tumorigenic spectrum, especially against human hepatic cancer. DW-166HC was evaluated for the appearance of micronucleus in polychromatic erythrocytes (PCEs) of mouse bone marrow cells after subcutaneous arid intravenous single administration. Bone marrow cells were prepared at 24 hr and 48 hr after DW-166HC-I (^(165)Ho-Chitosan complex : cold compound) administration and at 24 hr, 72 hr and 2 weeks after DW-166HC (^(166)Ho-Chitosan complex : hot compound) administration. The results showed there was no statistically significant increase of the numbers of PCEs with micronucleus in all DW-166HC-I administered groups compared with a negative control group but there was statistically significant increase of the numbers of PCEs with micronucleus at 24 hr arid 72 hr in all DW-166HC administered groups, which was recovered after 2 weeks from the drug administration. The results also showed the ratio of normochromatic erythrocytes (NCEs) to PCEs of all DW-166HC-I administered groups was not significantly different from that of a negative controi group but there was significant difference of this ratio at 24hr and 72 hr in all DW-166HC administered groups compared with that of negative group, which was also recovered after two weeks from the drug administration. These results suggested that DW-166HC-I may not cause any chromosomal damage but DW-166HC has in vivo mutagenic potential because of its radioactivity.
기니픽과 마우스에서 신규 퀴놀론 항균제 DW-116 의 항원성 시험
권현진(Hyun Jin Kwon),한형미(Hyung Mee Han),김필선(Pil Sun Kim),이흠숙(Heum Sook Lee),정용호(Yong Ho Chung),윤성준(Sung June Yoon),이문선(Moon Sun Lee),이덕근(Dug Keun Lee) 한국응용약물학회 1998 Biomolecules & Therapeutics(구 응용약물학회지) Vol.6 No.2
Antigenic potential of DW-116, a newly synthesized fluoroquinolone, was examined by conducting active systemic anaphylaxis (ASA), passive cutaneous anaphylaxis (PCA) and passive hemagglutination (PHA) tests. In ASA test, mild to moderate signs of anaphylactic responses were observed in the groups sensitized with low (2 mg/body) and high (10 mg/body) doses of DW-116 alone and the group sensitized with DW-116 plus adjuvant. Some moderate to severe anaphylactic reactions were observed in the group sensitized with a DW-116-bovine serum albumin (BSA) conjugate plus adjuvant when challenged with a DW116-guinea pig serum albumin (GSA) conjugate. However these reactions were considered to be a cross-reaction between BSA and GSA since similar reactions were induced when challenged by GSA alone. In heterologous PCA test using mice and rats, positive responses were not detected in any of the experimental groups. In PHA test, positive responses were observed in the groups sensitized with low and high doses of DW-116 alone and the group sensitized with DW-116 plus adjuvant. However, these responses were not considered to be drug-specific because some positive responses were also seen in the negative control group. From these results, it was concluded that DW-116 is not likely to have specific antigenic potential in clinical use.
문은이(Eun Yi Moon),최청하(Chung Ha Choi),성승규(Seung Kyoo Seong),이진(Jin Lee),유제만(Jei Man Ryu),이문선(Moon Sun Lee),정상헌(Sang Hun Jung),정용호(Yong Ho Chung),이덕근(Dug Keun Lee),윤성준(Sung June Yoon) 한국응용약물학회 1998 Biomolecules & Therapeutics(구 응용약물학회지) Vol.6 No.4
DW2282, (S)-(+)-4-phenyl-1-[N-(4-aminobenzoyl)-indolin-5-sulfonyl]-4,5-dihydro-2-imidazolone hydrochloride, is a novel anticancer agent thought to have an unique mechanism of action on the inhibition of tumor growth. In this study, we estimated in vivo antitumor activities and pharmacokinetics of DW2282 depending on various vehicles. The inhibition rate of tumor growth was increased by 50, 100 and 200 mg/kg of DW2282 in a dose-dependent manner. When DW2282 dissolved in 4 sorts of vehicles was orally single dosed to rats at 50 mg/kg, Cmax of DW2282 in 0.5% CMC.Na was a half as high as those in PG, PG+CP and PG+CP+DW. When DW2282 was orally administered to mice for 5 days, antitumor activity of 130 mg/kg suspended in 0.5% CMC.Na was as effective as that of 65 mg/kg dissolved in the rest of vehicles. Taken together, it is thought that antitumor activities of DW2282 are resulted from the absorption extent of it and related to the vehicle used.