Evaluation of antitumor activities of hyaluronate binding antitumor drugs: Synthesis, characterization and antitumor activity

被引：66

作者：

Akima, K ^{[1
]}

Ito, H ^{[1
]}

Iwata, Y ^{[1
]}

Matsuo, K ^{[1
]}

Watari, N ^{[1
]}

Yanagi, M ^{[1
]}

Hagi, H ^{[1
]}

Oshima, K ^{[1
]}

Yagita, A ^{[1
]}

Atomi, Y ^{[1
]}

Tatekawa, I ^{[1
]}

机构：

[1] KYORIN UNIV,SCH MED,DEPT SURG 1,MITAKA,TOKYO 181,JAPAN

来源：

JOURNAL OF DRUG TARGETING | 1996年 / 4卷 / 01期

关键词：

metastasis; HA-mitomycin C complex; lymph nodes; HA receptor (CD44); metabolic study; drug targeting;

D O I：

10.3109/10611869609046255

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

To enhance the selective delivery of antitumor drugs into regional lymph nodes and cancerous tissues via a hyaluronate (HA) receptor (CD44), we synthesized HA-mitomycin C complex and HA-epirubicin complex. To investigate the specific distribution of HA into regional lymph nodes and to evaluate the HA receptor on lewis lung carcinoma cells, we also synthesized C-14-labelled HA and fluorescent HA (FR-HA). The metabolic studies of C-14-HA and HA-epirubicin complex were performed in rats. The specific distribution of both compounds to the lymph nodes were observed after sc treatment. Internalization mechanism of HA into carcinoma cells (lewis lung carcinoma) via HA receptor was investigated using fluorescent HA (FR-HA) in vitro. Internalization of FR-HA following binding to the cell surfaces was observed. HA-Mitomycin C (MMC) exhibited potent anti-metastatic effects against lewis lung carcinoma implanted in mice at an extremely low dose (0.01 mg/kg) whereas free MMC had no effects.

引用

页码：1 / &

页数：9

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