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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概要
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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℃. 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.
- 公益社団法人日本薬学会の論文
- 1997-10-15
著者
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Onishi Hiraku
Department Of Drug Delivery Research Hoshi University
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Onishi Hiraku
Department Of Clinical Pharmacy Hoshi University
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Machida Yoshiharu
Department Of Drug Delivery Research Hoshi University
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Machida Yoshiharu
Dep. Of Drug Delivery Res. Hoshi Univ.
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Machida Yoshiharu
Department Of Clinical Pharmacy Hoshi University
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ISHIKI Nobuyuki
Department of Drug Delivery Research, Hoshi University
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Ishiki Nobuyuki
Department Of Drug Delivery Research Hoshi University
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