The Long-lasting Antiproliferative Effect of 15-Deoxyspergualin through its Spermidine Moiety.

• KAWADA MANABU

  Institute for Chemotherapy, M. C. R. F

• SOMENO TETSUYA

  Institute for Chemotherapy, M. C. R. F

• IINUMA HIRONOBU

  Institute for Chemotherapy, M. C. R. F

• MASUDA TOHRU

  Institute for Chemotherapy, M. C. R. F

• ISHIZUKA MASAAKI

  Institute for Chemotherapy, M. C. R. F

• TAKEUCHI TOMIO

  Institute for Chemotherapy, M. C. R. F

抄録

15-Deoxyspergualin (DSG) inhibited growth of mouse EL-4 lymphoma cells with an IC₅₀ 0.02 μg/ml. Even though the cells were treated with DSG for only 4 hours and then washed, the antiproliferative effect lasted long with an IC₅₀ 0.4μg/ml. DSG has spermidine and guanidine moieties in its structure. One decomposed element containing guanidine moiety inhibited the growth at higher doses than DSG, but the effect did not last long unlike DSG. While another element containing spermidine moiety did not affect the growth, it diminished the long-lasting antiproliferative effect of DSG by pretreatment of the cells. Pretreatment with polyamines such as putrescine, spermidine, and spermine also diminished the effect of DSG. Furthermore, N-alkylation of spermidine moiety in DSG abolished the antiproliferative effect. These results suggested that DSG binds to the cells through its spermidine moiety and exerts its long-lasting antiproliferative effect.

収録刊行物

• The Journal of Antibiotics

  The Journal of Antibiotics 53 (7), 705-710, 2000

  公益財団法人 日本感染症医薬品協会

キーワード

• Drug Discovery
• Pharmacology

詳細情報

• CRID: 1390282679127405440
• NII論文ID: 10008467337
• NII書誌ID: AA0069330X
• DOI: 10.7164/antibiotics.53.705
• COI: 1:CAS:528:DC%2BD3cXltl2htbo%3D
• ISSN: 18811469
• ISSN: 00218820
• PubMed: 10994812
• 本文言語コード: en
• データソース種別:
  • JaLC
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可