Yoneda T, Ogawa T, Sakuda M
Gan To Kagaku Ryoho. 1985 Jun;12(6):1306-11.
Incubation of FT-207 with cytosol obtained from OKK cells but not from HEPM cells in vitro resulted in marked formation of the active metabolite, 5-FU. Degradation of 5-FU measured by FBA formation was very low in OKK cytosol but high in HEPM cytosol. High activity of 5-FU formation and low activity of 5-FU degradation in tumor cells might be responsible for increased 5-FU levels in the tumors of patients. Inhibition of OKK cell growth by FT-207 occurred in parallel with an appearance of 5-FU in the nucleus. We presume that a factor present in OKK cytosol is a soluble enzyme.
FT - 207与体外从OKK细胞而非HEPM细胞获得的胞质溶胶一起孵育,导致活性代谢物5 - 氟尿嘧啶(5 - FU)的显著形成。通过FBA形成测定的5 - FU降解在OKK胞质溶胶中非常低,但在HEPM胞质溶胶中很高。肿瘤细胞中5 - FU形成的高活性和5 - FU降解的低活性可能是患者肿瘤中5 - FU水平升高的原因。FT - 207对OKK细胞生长的抑制与细胞核中5 - FU的出现同时发生。我们推测OKK胞质溶胶中存在的一种因子是一种可溶性酶。