Cellular Interaction and in Vitro Antitumor Activity of Lipophilic Mitomycin C Prodrugs(Pharmaceutical)
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概要
- 論文の詳細を見る
Cellular interaction and in vitro antitumor activities of lipophilic prodrugs of mitomycin C (MMC) were studied in order to clarify their mode of action. Five lipophilic derivatives with various lipophilic promoieties (benzylcarbonyl, benzyloxycarbonyl, pentyloxycarbonyl, nonyloxycarbonyl, and cholesteryloxycarbonyl grpups) were tested. All the derivatives except for cholesteryloxycarbonyl MMC were converted to MMC in the supernatant of tumor cell homogenate. Lipophiiic derivatives, especially nonyloxycarbonyl MMC and cholesteryloxycarbonyl MMC, associated with Ehrlich ascites carcinoma (EAC) cells more readily than MMC. While the association percentage remained almost constant during the course of incubation at 4℃, it increased with incubation period at 37℃, suggesting metabolic consumption of lipophilic derivatives in the tumor cells. Association percentages of derivatives at 4℃ were closely correlated to their partition coefficients between chloroform and water. The apparent distribution ratio of benzyloxycarbonyl MMC between EAC cells and the incubation medium also correlated with their volume ratio. These results suggested that lipophilic derivatives were incorporated into tumor cells through partition equilibrium between lipid components of tumor cells and the medium. In vitro antitumor activities of lipophilic MMC derivatives were studied using EAC and L1210 leukemia cell culture. In the continuous exposure experiment, lipophilic derivatives which were converted to MMC in tumor cells showed equal or somewhat lower growth inhibitory activity as compared with MMC. In the case of 1h or 5min exposure, nonyloxycarbonyl MMC was more active than MMC, indicating that the growth-inhibitory effects of lipophilic derivatives are closely related to both cellular interaction and conversion rate to MMC.
- 公益社団法人日本薬学会の論文
- 1987-09-25
著者
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Hashida Mitsuru
Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Hayashi Yoshie
Department Of Pharmacy Kyoto University Hospital Faculty Of Medicine Kyoto University
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Hayashi Yoshie
Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Matsumoto Satoshi
Department Of Pathology Nara Medical University
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Hashida M
Departments Of Drug Delivery Research Graduate School Of Pharmaceutical Sciences Kyoto University
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Sasaki Hitoshi
Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Sezaki Hitoshi
Department Of Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Sezaki Hitoshi
Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Hashida M
Department Of Drug Delivery Research Graduate School Of Pharmaceutical Sciences Kyoto University
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Sasaki H
Nagasaki Univ. School Of Medicine Nagasaki Jpn
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Matsumoto Satoshi
Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
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Matsumoto Satoshi
Department Of Agricultural Chemistry University Of Tokyo
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