RRC ID 42293
Author Jin GZ, Quan HJ, Koyanagi J, Takeuchi K, Miura Y, Komada F, Saito S.
Title 4'-O-Alkyaloenin derivatives and their sulfates directed toward overcoming multidrug resistance in tumor cells.
Journal Cancer Lett
Abstract The cytotoxic effects on HCT 116, Hep G2 and HCT 116/VCR 100-1-1 cell lines of synthetic 4'-O-alkylaloenins (2-17), 4'-O-benzylaloenin (18) and 4'-O-allylaloenin (19) were examined by MTT assay, and compared with that of aloenin (1) isolated from Aloe arborescens Mill. Var. natalensis Berger which showed no marked effect (IC50 value: > 100 microM). The cytotoxic effects of 4'-O-alkylaloenin sulfates (21-29) were also examined on the same cell lines. The introduction of a longer alkyl group at the O-4' position of 1 resulted in a higher cytotoxic action on HCT 116 and Hep G2 cells. Among 4'-O-alkylaloenins 2-17, 4'-O-tetradecylaloenin 14 was the most cytotoxic to both on HCT 116 cells (IC50 value: 5.3+/-2.3 microM) and Hep G2 cells (IC50 value: 4.0+/-0.6 microM). Also among 4'-O-alkylaloenin sulfates 21-29, 4'-O-dodecylaloenin sulfate 29 was the most cytotoxic to both on HCT 116 (IC50 value: 4.8+/-0.2 microM) and Hep G2 cells (IC50 value: 4.0+/-0.5 microM). 4'-O-Alkylaloenins 7-14 and 4'-O-alkylaloenin sulfates 24-29 were also cytotoxic to Hep G2 and HCT 116/VCR 100-1-1 cell lines, which overexpress P-glycoprotein, as well as HCT 116 cell lines which scarcely express it.
Volume 218(1)
Pages 15-20
Published 2005-1-31
DOI 10.1016/j.canlet.2004.07.025
PII S0304-3835(04)00576-2
PMID 15639336
MeSH ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism Carcinoma, Hepatocellular / pathology Colorectal Neoplasms Coloring Agents / chemistry Drug Resistance, Multiple* Drug Resistance, Neoplasm Drug Screening Assays, Antitumor Glucosides / chemistry Glucosides / pharmacology* Humans Liver Neoplasms / pathology Sulfates Tetrazolium Salts / chemistry Thiazoles / chemistry Tumor Cells, Cultured
IF 7.36
Times Cited 10
Human and Animal Cells