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Preparation and Determination of Structure of L-3-Deoxymimosine-containing Peptides
Chae, Whigun,Lee, Eung-Seok 영남대학교 약품개발연구소 2000 영남대학교 약품개발연구소 연구업적집 Vol.10 No.-
L-3-Deoxymimosine-containing decapeptides were prepared for the development of protein tyrosine kinase(PTK) inhibitors. During the preparation of peptides, several side products were formed. Identification and determination of major peptides generated were reported.
Jeong, Tae Cheon,Lee, Eung-Seok,Chae, Whigun,Koh, Woo Suk,Kang, Boo-Hyon,Han, Sang Seop 영남대학교 약품개발연구소 2002 영남대학교 약품개발연구소 연구업적집 Vol.11 No.-
lmmunotoxic effects of 2-bromopropane were investigated in male Sprague-Dawley rats.The rats were treated orally daily with 2-bromopropane at 100, 330, or 1000 mg/kg for 28 consecutive days. Four days before necropsy, the rats were immunized intravenously with sheep red blood cells (SRBCs). The body and thymus weights were significantly reduced by treatment with 2-bromopropane at the highest dose. In addition, the numbers of splenic and thymic cells were decreased by 2-bromopropane. In hematology, the numbers of white blood cells, red blood cells, and platelets were significantly reduced. Among the serum clinical parameters, the levels of chloride ion were significantly increased by 2-bromopropane. The antibody respose to SRBCs was significantly suppressed at the highest dose. With immunized animals. immunophenotyping of splenic and thymic cells was performed to investigate the changes of the number of macrophages, B cells, and T cells in spleen and the number of CD4^+ and CD8^+ cells in thymus. The numbers of most cell types were significantly decreased in the spleen when animals were treated with 2-bromopropane at 100 mg/kg. Likewise, all cell types of thymus were significantly decreased by 2-bromopropane. The present results suggest that 2-bromopropane may have an immunotoxic potential in male Sprague-Dawley rate when the rats are exposed for 28 d.
Synthesis, Characterization and in Vitro Identification of N^7-Guanine Adduct of 2-Bromopropane
Zhao, Long-Xuan,Kim, Eun-Kyung,Lim, Hyun-Tae,Moon, Yoon-Soo,Kim, Nam-Hee,Kim, Tae-Hyung,Choi, Heesung,Chae, Whigun,Jeong, Tae Cheon,Lee, Eung-Seok 영남대학교 약품개발연구소 2002 영남대학교 약품개발연구소 연구업적집 Vol.11 No.-
Recently, we have reported that 2-bromopropane might have an immunotoxic potential in rats when exposed for 28 days. In the present studies, the possibility of 2i-deoxyguanosine adduct formation by 2-bromopropane was investigated in vitro to elucidate molecular mechanism of 2-bromopropane-induced immunosuppression. N^7-Guanine adduct of 2'-bromopropane (i.e., N^7-isopropyl guanine) was chemically synthesized and structurally characlerized by analysis of UV, ^H-NMR, ^12C-NMR, COSY and fast atom bombardment, mass spectrometry to use as a reference material. Incubation of 2'-deoxyguanosine with an excess amount of 2-bromopropane in PBS buffer solution, pH 7.4, AT 37℃ for 16 h, followed by a thermal hydrolysis, produced a detectable amount of N^7-isopropyl guanine by an HPLC and UV analysis. The present results suggest that 2-bromopropane might form a DNA adduct in N^7 position of 2'-deoxyguanosine at a physiological condition.
Synthesis, Characterization and in Vitro Identification of $N^7-Guanine$ Adduct of 2-Bromopropane
Zhao, Long-Xuan,Kim, Eun-Kyung,Lim, Hyun-Tae,Moon, Yoon-Soo,Kim, Nam-Hee,Kim, Tae-Hyung,Choi, Heesung,Chae, Whigun,Jeong, Tae-Cheon,Lee, Eung-Seok The Pharmaceutical Society of Korea 2002 Archives of Pharmacal Research Vol.25 No.1
Recently, we have reported that 2-bromopropane might have an immunotoxic potential in rats when exposed for 28 days. In the present studies, the possibility of 2i-deoxyguanosine abduct formation by 2- bromopropane was investigated in vitro to elucidate molecular mechanism of 2-bromopropane-induced immunosuppression. $N^7-Guanine adduct$ of 2'-bromopropane (i.e., $N^7-isopropyl$ guanine) was chemically synthesized and structurally characterized by analysis of UV,$^1H-NMR,{\;}^{13}C-NMR$, COSY and fast atom bombardment mass spectrometry to use as a reference material. Incubation of 2'-deoxyguanosine with an excess amount of 2-bromopropane in PBS buffer solution, pH 7.4, at $37^{\circ}C$ for 16 h, followed by a thermal hydrolysis, produced a detectable amount of $N^7-isopropyl$ guanine by an HPLC and UV analysis. The present results suggest that 2-bromopropane might form a DNA adduct in $N^7-position$ of 2'-deoxyguanosine at 3 Physiological condition.
Kim, Nam-Hee,Hyun, Sun-Hee,Jin, Chun-Hua,Lee, Sang-Kyu,Lee, Dong-Wook,Jean, Tae-Won,Park, Chang-Bon,Lee, Eung-Seok,Chae, Whigun,Jeong, Tae-Cheon The Pharmaceutical Society of Korea 2003 Archives of Pharmacal Research Vol.26 No.11
In the present studies, the acute toxic effects of 2-bromopropane (2-BP) and its analog, 1,2-dibromopropane (1,2-DBP), were investigated in female BALB/c mice. The mice were treated orally with either 2-BP at 2000 and 4000 mg/kg or 1,2-DBP at 300 and 600 mg/kg. Four days before necropsy, the mice were immunized intraperitoneally with sheep red blood cells (SRBCs). 1,2-DBP reduced the weights of the spleen and thymus weights and decreased the number of splenic cells. In addition, treatment with 1,2-DBP suppressed the antibody response to SRBCs. Meanwhile, only the antibody response was significantly suppressed by treatment with 2-BP. In the subsequent studies, the time course effects of 2-BP and 1 ,2-DBP on the hepatotoxic parameters were compared in female BALB/c mice. When mice were treated orally with either one of these chemicals for 6, 12, 24 and 48 h, the activities of serum alanine aminotransferase and aspartate aminotransferase elevated significantly only with 1,2-DBP 24 h after the treatment. The hepatic content of glutathione was reduced by 1,2-DBP. Meanwhile, these parameters were increased by 2-BP. The present results suggest that 1,2-DBP in the Solvent 5200 also contributes to the immnunotoxicity, although 2-BP is a major component.