Distribution and metabolism of 14C-sulfoquinovosylacylpropanediol (14C-SQAP) after a single intravenous administration in tumor-bearing mice.
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| Abstract |
Sulfoquinovosylacylpropanediol (SQAP) is a novel potent radiosensitizer that inhibits angiogenesis in vivo and results in increased oxigenation and reduced tumor volume. We investigated the distribution, metabolism, and excretion of SQAP in male KSN-nude mice transplanted with a human pulmonary carcinoma, Lu65. For the metabolism analysis, a 2 mg (2.98 MBq)/kg of [glucose-U-14C]-SQAP (CP-3839) was intravenously injected. The injected SQAP was decomposed into a stearic acid and a sulfoquinovosylpropanediol (SQP) in the body. The degradation was relatively slow in the carcinoma tissue.1,3-propanediol[1-14C]-SQAP (CP-3635) was administered through intravenous injection of a 1 mg (3.48 MBq)/kg dose followed by whole body autoradiography of the mice. The autoradiography analysis demonstrated that SQAP rapidly distributed throughout the whole body and then quickly decreased within 4 hours except the tumor and excretion organs such as liver, kidney. Retention of SQAP was longer in tumor parts than in other tissues, as indicated by higher levels of radioactivity at 4 hours. The radioactivity around the tumor had also completely disappeared within 72 hours.
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| Authors | Tatsushi Ruike, Yoshihiro Kanai, Kazuki Iwabata, Yuki Matsumoto, Hiroshi Murata, Masahiro Ishima, Keisuke Ohta, Masahiko Oshige, Shinji Katsura, Koji Kuramochi, Shinji Kamisuki, Hiroeki Sahara, Masahiko Miura, Fumio Sugawara, Kengo Sakaguchi |
| Journal | Xenobiotica; the fate of foreign compounds in biological systems (Xenobiotica) Vol. 49 Issue 3 Pg. 346-362 (Mar 2019) ISSN: 1366-5928 [Electronic] England |
| PMID | 29543539 (Publication Type: Journal Article) |
| Chemical References |
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