Biological Properties of Conjugates of Mitomycin C with Estradiol Benzoate and Estradiol: Their Stability Characteristics in Biological Media and Their Binding Abilities to Estrogen Receptor.

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  • Biological Properties of Conjugates of

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Conjugates of mitomycin C (MMC) with estradiol benzoate and estradiol via glutaric acid, abbreviated to EB-glu-MMC and E-glu-MMC, respectively, were investigated in vitro to determine their stability and MMC regeneration properties in biological media and on their binding to estrogen receptor. EB-glu-MMC and E-glu-MMC were added into a mixture of 1/15 M phosphate buffer, pH 7.4, (ionic strength=0.3), propylene glycol (PG) and rat plasma (4 : 5 : 1, v/v/v), named 10% plasma, or into a mixture of the buffer, PG and rat liver homogenate (9 : 10 : 1, v/v/w), named 5% liver homogenate, and each was incubated at 37°C. The conversion characteristics of EB-glu-MMC and E-glu-MMC were compared with those in the buffer-PG (1 : 1, v/v) mixture previously reported. In 10% plasma, the change of EB-glu-MMC to E-glu-MMC was accelerated enzymatically to some extent, while the enzymatic degradation of E-glu-MMC was not accelerated at all. In 5% liver homogenate, EB-glu-MMC changed quickly to E-glu-MMC, whereas the degradation of E-glu-MMC was accelerated very little. E-glu-MMC was considered to be rather stable against enzyme in the biological media. Competitive binding studies using the rat uterine estrogen receptor showed that the specific binding affinity of E-glu-MMC was 0.81% to that of estradiol, while E-glu-MMC hardly exhibited specific binding. E-glu-MMC was regarded as a hormone-drug conjugate showing a small specific binding affinity to the estrogen receptor. E-glu-MMC is considered to be an effective antitumor agent which gradually generates MMC in the body, and its receptor-mediated action to target cells such as estrogen receptor-positive tumor cells might be possible.

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