論文 - 詳細
| RRC ID | 12443 |
|---|---|
| 著者 | Nakamura J, Nakajima N, Matsumura K, Hyon SH. |
| タイトル | Water-soluble taxol conjugates with dextran and targets tumor cells by folic acid immobilization. |
| ジャーナル | Anticancer Res |
| Abstract |
BACKGROUND:Paclitaxel (taxol) is a very effective anticancer drug. However, the solution used to enhance the water solubility of paclitaxel, a mixture of polyoxyethylene castor oil (Cremphor EL) and dehydrated ethanol, causes irritation. Our aim is to develop a water-soluble taxol with a high anticancer effect. MATERIALS AND METHODS:Taxol derivatives (conjugation with aminated dextran, Dex-TXL) were synthesized for the water-solublization of taxol and folic acid (FA) was ionically and covalently conjugated with Dex-TXL. In addition, their anticancer activity was investigated in vitro with KB cells (a folate receptor-overexpressing carcinoma cell line of the oral cavity). RESULTS:The high solubility of Dex-TXL conjugates (2700 times higher than that of intact taxol) needed no additional Cremophor EL or dehydrated ethanol. Dex-TXL showed 2-3 times greater anticancer effect when conjugated with FA. CONCLUSION:These results suggest that conjugation with dextran and FA could bring about an improvement in taxol anticancer therapy. |
| 巻・号 | 30(3) |
| ページ | 903-9 |
| 公開日 | 2010-3-1 |
| PII | 30/3/903 |
| PMID | 20393013 |
| MeSH | Adsorption Antineoplastic Agents, Phytogenic / chemistry* Antineoplastic Agents, Phytogenic / pharmacokinetics Antineoplastic Agents, Phytogenic / pharmacology Caco-2 Cells Carrier Proteins / metabolism Dextrans / chemistry* Dextrans / pharmacokinetics Folate Receptors, GPI-Anchored Folic Acid / chemistry* Folic Acid / pharmacokinetics Humans KB Cells Paclitaxel / analogs & derivatives* Paclitaxel / chemistry Paclitaxel / pharmacokinetics Paclitaxel / pharmacology Receptors, Cell Surface / metabolism Solubility Water / chemistry |
| IF | 1.994 |
| 引用数 | 20 |
| WOS 分野 | ONCOLOGY |
| リソース情報 | |
| ヒト・動物細胞 | MA104(RCB0994) |