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김효진,윤윤정,김현미,차은영,이혜석,김정한,이규양,이석영,천혜경,유성은,이상섭,신재국,류광현 대한약학회 2005 Archives of Pharmacal Research Vol.28 No.11
KR-33028 (N-[4-cyano-benzo[b]thiophene-2-carbonyl]guanidine) is a new cardioprotective agent for preventing ischemia-reperfusion injury. This study was performed to identify the metabolic pathway of KR-33028 in human liver microsomes and to compare its metabolism with that of cryopreserved human hepatocytes. Human liver microsomal incubation of KR-33028 in the presence of NADPH and UDPGA resulted in the formation of four metabolites, M1, M2, M3, and M4. M1 and M2 were identified as 5-hydroxy-KR-33028 and 7-hydroxy-KR-33028, respectively, on the basis of LC/MS/MS analysis with the synthesized authentic standard. M3 and M4 were suggested to be dihydroxy-KR-33028 and hydroxy-KR-33028-glucuronide, respectively. Metabolism of KR-33028 in cryopreserved human hepatocytes resulted in the formation of M1, M2, and M4. These data show a good correlation between major metabolites formed in human liver microsomes and cryopreserved human hepatocytes. In addition, KR- 33028 was found to inhibit moderately the metabolism of CYP1A2 substrates. Based on the results obtained metabolic pathway of KR-33028 is proposed.
Leaf Condition of Rice (Oryza sativa L.) in Response to Cold Stress during Ripening Stage
황원하,이정건,정재혁,이혜석,최경진 한국작물학회 2019 Journal of crop science and biotechnology Vol.22 No.5
Cold stress can decrease yield and quality of rice. Although many studies have investigated the impact of cold stress on rice, researches on physiological changes of rice plants under low temperature during ripening stage are insufficient. Thus, the objective of this study was to analyze changes of leaf condition in rice plant during ripening stage in response to low temperature. Results showed that photosynthesis activity of flag leaf was decreased continuously after heading and that it was reduced more in cold condition. Chlorophyll content in flag leaf was also reduced in control and cold conditions after heading. In control condition, chlorophyll content showed a significant correlation with nitrogen content in leaf. However, chlorophyll content under cold condition showed a high correlation with Malondialdehyde content. These results strongly suggest that the leaf lipid peroxidation by cold stress can induce the decrease of leaf chlorophyll content and photosynthesis activity during ripening stage in rice.
김조훈,지혜영,이승석,유성은,김선오,이동하,임홍,이혜석 대한약학회 2002 Archives of Pharmacal Research Vol.25 No.5
KR-31543,(2S,3R,4S)-6-amino-4-[N-(4-chlorophenyl)-N-(2-methyl-2H-tetrazol-5-ylmethyl)amino]- 3,4-dihydro-2-dimethoxymethyl-3-hydroxy-2-methyl-2H-1-benzopyran is a new neuroprotetive agent for ischemia-reperfusion damage. The in vitro and in vivo metabolism of KR-31543 in rats has been studied by LC-electrospray mass spectrometry. Rat liver microsomal incubation of KR-31543 in the presence of NADPH resulted in the formation of a metabolite M1. M1 was identified as N-(4-chlorophenyl)-N-(2-methyl-2H-tetrazol-5-ylmethyl)amine on the basis of LCMS/ MS analysis with the synthesized authentic standard. Rat CYP3A1 and 3A2 are the major CYP isozymes involved in the formation of M1.