Antitumor Effects and Toxicities of Carboxymethylpullulan-Peptide-Doxorubicin Conjugates.
書誌事項
- タイトル別名
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- Antitumor Effects and Toxicities of Car
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In vivo antitumor effects of the conjugates of doxorubicin (DXR) with carboxymethylpullulan (CMPul) through tetrapeptide spacers were compared with those of DXR against tumor-bearing rats. CMPul-DXR conjugates bound through Gly-Gly-Phe-Gly and Gly-Phe-Gly-Gly spacers were found to be more potent than DXR after a single intravenous injection in rats bearing Walker 256 carcinosarcoma. These conjugates were also more effective than DXR in rats bearing Yoshida sarcoma. However, CMPul-DXR conjugate bound through Gly-Gly-Gly-Gly was less effective against Walker 256-bearing rats than DXR. Body weight loss of CMPul-DXR conjugates in rats, on the other hand, was less than that of DXR at a DXR dose of 10 mg/kg. Lethal doses of CMPul-DXR conjugates in CDF1 mice were about 3-times higher than that of DXR. These data suggest that the therapeutic index of CMPul-DXR conjugates bound through appropriate peptide spacers was increased more than that of DXR. However, CMPul-DXR conjugates tested were all less effective than DXR against Walker 256 cells in vitro. Also, 125I-labeled CMPul-DXR conjugate accumulated much less in the cells than 14C-DXR.
収録刊行物
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- Biological & Pharmaceutical Bulletin
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Biological & Pharmaceutical Bulletin 20 (10), 1061-1065, 1997
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679600423552
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- NII論文ID
- 110003638950
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- NII書誌ID
- AA10885497
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- COI
- 1:CAS:528:DyaK2sXntVKqsrk%3D
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- ISSN
- 13475215
- 09186158
- http://id.crossref.org/issn/09186158
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- NDL書誌ID
- 4326580
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- PubMed
- 9353565
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可