Distribution and metabolism of <sup>14</sup>C-sulfoquinovosylacylpropanediol (<sup>14</sup>C-SQAP) after a single intravenous administration in tumor-bearing mice
Creators: name: Ruike, Tatsushi
name: Kanai, Yoshihiro
name: Iwabata, Kazuki
name: Matsumoto, Yuki
name: Murata, Hiroshi
name: Ishima, Masahiro
name: Ohta, Keisuke
name: Oshige, Masahiko
name: Katsura, Shinji
name: Kuramochi, Koji
name: Kamisuki, Shinji
name: Hiroeki Sahara
name: Miura, Masahiko
name: Sugawara, Fumio
name: Sakaguchi, Kengo
Publisher: name: Taylor & Francis
Year: 2018
Subjects: subject: Biochemistry
subject: Cell Biology
subject: Molecular Biology
subject: Physiology
subject: FOS: Biological sciences
subject: FOS: Biological sciences
subject: Pharmacology
subject: 39999 Chemical Sciences not elsewhere classified
subject: FOS: Chemical sciences
subject: FOS: Chemical sciences
subject: Marine Biology
subject: Cancer
subject: Computational Biology

description: 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-<sup>14</sup>C]-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-<sup>14</sup>C]-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. 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-<sup>14</sup>C]-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-<sup>14</sup>C]-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.