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Exploratory Research Laboratories 1, Daiichi Pharmaceutical Co., Ltd., 16-13, Kitakasai 1-Chome, Edogawa-ku, Tokyo 134, Japan
It is known that 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (CPT-11), a semisynthesized derivative of camptothecin (CPT), has a potent antitumor activity in vivo, but 7-ethyl-10-hydroxycamptothecin (SN-38), a metabolite of CPT-11, shows much stronger cytotoxicity in vitro than CPT-11. In this study, we demonstrated that the relaxation of SV40 DNA plasmids by type I DNA topoisomerase prepared from P388 murine leukemia cells was inhibited by 50% by SN-38 at approximately 1 µM, although CPT-11 at 1 mM slightly inhibited the relaxation. SN-38 and CPT showed strong, time-dependent inhibitory activity against DNA synthesis of P388 cells. However, CPT-11 weakly inhibited DNA synthesis independently of time with coincident inhibition of the total thymidine uptake by the cells. By alkaline and neutral elution assays, it was demonstrated that SN-38 caused much more frequent DNA single-strand breaks in P388 cells than did CPT-11. The same content of SN-38 and a similar frequency of single-strand breaks were detected in the cells treated with SN-38 at 0.1 µM or with CPT-11 at 100 µM. Therefore, single-strand breaks by CPT-11 seem to be due to SN-38 produced from CPT-11 in cells. These results indicate that CPT-11 itself possesses a marginal antiproliferative effect but that SN-38 plays an essential role in the mechanism of action of CPT-11.
1 To whom requests for reprints should be addressed.
Received 1/10/91. Accepted 6/ 4/91.
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B. Vladu, J. M. Woynarowski, G. Manikumar, M. C. Wani, M. E. Wall, D. D. Von Hoff, and R. M. Wadkins 7- and 10-Substituted Camptothecins: Dependence of Topoisomerase I-DNA Cleavable Complex Formation and Stability on the 7- and 10-Substituents Mol. Pharmacol., February 1, 2000; 57(2): 243 - 251. [Abstract] [Full Text]
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I. F. Pollack, M. Erff, D. Bom, T. G. Burke, J. T. Strode, and D. P. Curran Potent Topoisomerase I Inhibition by Novel Silatecans Eliminates Glioma Proliferation in Vitro and in Vivo Cancer Res., October 1, 1999; 59(19): 4898 - 4905. [Abstract] [Full Text] [PDF]
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H. S. Friedman, W. P. Petros, A. H. Friedman, L. J. Schaaf, T. Kerby, J. Lawyer, M. Parry, P. J. Houghton, S. Lovell, K. Rasheed, et al. Irinotecan Therapy in Adults With Recurrent or Progressive Malignant Glioma J. Clin. Oncol., May 1, 1999; 17(5): 1516 - 1516. [Abstract] [Full Text] [PDF]
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H. M. Dodds, M.-C. Haaz, J.-F. Riou, J. Robert, and L. P. Rivory Identification of a New Metabolite of CPT-11 (Irinotecan): Pharmacological Properties and Activation to SN-38 J. Pharmacol. Exp. Ther., July 1, 1998; 286(1): 578 - 583. [Abstract] [Full Text]
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X.-Y. Chu, Y. Kato, K. Niinuma, K.-I. Sudo, H. Hakusui, and Y. Sugiyama Multispecific Organic Anion Transporter Is Responsible for the Biliary Excretion of the Camptothecin Derivative Irinotecan and its Metabolites in Rats J. Pharmacol. Exp. Ther., April 1, 1997; 281(1): 304 - 314. [Abstract] [Full Text]
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