대한핵의학회지 (1967년~2009년)
대한핵의학회지 2004;38(4)325~329
생쥐 간 S9 분획을 이용한 방사성추적자 대사물질의 새로운 체외 측정방법
(A Novel In Vitro Method for the Metabolism Studies of Radiotracers Using Mouse Liver S9 Fraction)
Author 류은경, 최연성, 김동현, 이상윤, 최 용, 이경한, 김병태,
Eun Kyoung Ryu, M.S., Yearn Seong Choe, Ph.D., Dong Hyun Kim, B.S., Sang-Yoon Lee, Ph.D., Yong Choi, Ph.D.,Kyung-Han Lee, M.D., Byung-Tae Kim, M.D.
Affiliation 성균관대학교 의과대학 생명의공학과, 삼성서울병원 핵의학과
Department of Nuclear Medicine, Samsung Medical Center, Department of Biomedical Engineering, Sungkyunkwan University School of Medicine, Seoul, Korea
Abstract

Purpose: Usefulness of mouse liver S9 fraction was evaluated for the measurement of the metabolites in the in vitro metabolism study of 18F-labeled radiotracers. Materials and Methods: Mouse liver S9 fraction was isolated at an early step in the course of microsome preparation. The in vitro metabolism studies were carried out by incubating a mixture containing the radiotracer, S9 fraction and NADPH at 37 oC, and an aliquot of the mixture was analyzed at the indicated time points by radio-TLC. Metabolic defluorination was further confirmed by the incubation with calcium phosphate, a bone mimic. Results: The radiotracer [18F]1 underwent metabolic defluorination within 15 min, which was consistent with the results of the in vivo method and the in vitro method using microsome. Radiotracer [18F]2 was metabolized to three metabolites including 4-[18F]fluorobenzoic acid within 60 min. It is likely that the one of these metabolites at the origin of radio-TLC was identical with the one that obtained from the in vivo and in vitro (microsome) method. Compared with the in vitro method using microsome, the method using S9 fraction gave a similar pattern of the metabolites but with a different ratio, which can be explained by the presence of cytosol in the S9 fraction. Conclusion: These results suggest that the findings of the in vitro metabolism studies using S9 fraction can reflect the in vivo metabolism of novel radiotracers in the liver. Moreover, this method can be used as a tool to determine metabolic defluorination along with calcium phosphate absorption method. (Korean J Nucl Med 38(4):325-329, 2004)

Keyword radiotracer, metabolism, S9 fraction, in vitro method, calcium phosphate
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