RRC ID 12443
Author Nakamura J, Nakajima N, Matsumura K, Hyon SH.
Title Water-soluble taxol conjugates with dextran and targets tumor cells by folic acid immobilization.
Journal 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.
Volume 30(3)
Pages 903-9
Published 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
Times Cited 20
WOS Category ONCOLOGY
Resource
Human and Animal Cells MA104(RCB0994)