Enhanced intracellular delivery of doxorubicin by scavenger receptor‐mediated endocytosis for preferential killing of histiocytic lymphoma cells in culture

FEBS Letters

Basu, Sandip K.¹  Basu, Sunanda¹  Mukhopadhyay, Bratati¹  Mukhopadhyay, Amitabha¹ 

[1] National Institute of Immunology, Aruna Asaf Ali Marg, New Delhi 110067, India

关键词: Drug delivery;    Scavenger receptor;    Endocytosis;    Histiocytic malignancy;    Cancer chemotherapy;    BCA;    bicinchoninic acid;    BSA;    bovine serum albumin;    DXR;    doxorubicin;    FCS;    fetal calf serum;    MBSA;    maleylated BSA;    PBS;    phosphate-buffered saline;    TCA;    trichloroacetic acid;   

DOI  :  10.1016/0014-5793(94)80511-3

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

A conjugate of the antineoplastic drug doxorubicin (DXR) with maleylated bovine serum albumin (MBSA) was taken up by a human histiocytic lymphoma cell line (U937) through the high efficiency process of scavenger receptor-mediated endocytosis resulting in a sixfold higher intracellular concentration of the drug compared to that obtained when the free drug was administered. Compared to the free drug, the drug conjugate showed significantly higher cytotoxicity towards U937 cells presumably because of intracellular availability of a pharmacologically active form of the drug. The intracellular product released after lysosomal degradation of the drug conjugate was chromatographically identical to free DXR. These findings merit serious consideration in the development of new chemotherapeutic agents for the treatment of histiocytic malignancies.

【 授权许可】

Unknown