Inhibition of P-glycoprotein by flavonoid derivatives in adriamycin-resistant human myelogenous leukemia (K562/ADM) cells

Tomomi Ikegawa, Hisakazu Ohtani, Noriko Koyabu, Motoharu Juichi, Yukiko Iwase, Chihiro Ito, Hiroshi Furukawa, Mikihiko Naito, Takashi Tsuruo, Yasufumi Sawada

研究成果: Article査読

58 被引用数 (Scopus)

抄録

We investigated the effects of natural flavones, quercetin and morin, and their pentamethyl, pentaethyl, pentapropyl, pentabutyl and pentaallyl ethers, on the function of P-glycoprotein (P-gp) assessed by an increase in the uptake of [3H]vincristine by human myelogenous leukemia (K562) cells and adriamycin-resistant human myelogenous leukemia (K562/ADM) cells. Pentamethyl, pentaethyl, pentapropyl and pentaallyl ethers of morin and quercetin (20 μM) all increased the uptake of [3H]vincristine by K562/ADM cells, while quercetin, morin and their pentabutyl ethers had no effect. Pentamethylquercetin, pentaallylquercetin and pentaethylmorin remarkably increased the uptake of [3H]vincristine by K562/ADM cells by 10.6, 10.8 and 14.4-fold, respectively. These inhibitory potencies for P-gp were more potent than typical P-gp inhibitors, cyclosporine A and verapamil. Taking into consideration that these flavonoid derivatives possess antitumor promoter activity, they may become candidates of effective multidrug resistance-reversing agents in cancer chemotherapy.

本文言語English
ページ(範囲)89-93
ページ数5
ジャーナルCancer Letters
177
1
DOI
出版ステータスPublished - 2002 3 8
外部発表はい

ASJC Scopus subject areas

  • 腫瘍学
  • 癌研究

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