Reversal of multidrug resistance in human carcinoma cell line by agosterols, marine spongean sterols.

Authors
Aoki, S Setiawan, A Yoshioka, Y Higuchi, K Fudetani, R Chen, ZS Sumizawa, T Akiyama, S Kobayashi, M
Citation
S. Aoki et al., Reversal of multidrug resistance in human carcinoma cell line by agosterols, marine spongean sterols., TETRAHEDRON, 55(49), 1999, pp. 13965-13972
Citations number
8
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
TETRAHEDRON
ISSN journal
00404020 → ACNP
Volume
55
Issue
49
Year of publication
1999
Pages
13965 - 13972
Database
ISI
SICI code
0040-4020(199912)55:49<13965:ROMRIH>2.0.ZU;2-A
Abstract
We have isolated agosterol A (1) from a marine sponge of Spongia sp. as a r eversing substance to multidrug resistance (MDR) in human carcinoma cell li nes, KB-CZ and KB-CV60, overexpressing P-glycoprotein and MRP, respectively . Further investigation led us to isolate analogous sterols, agosterols B ( 2), C (5), A(4) (7), D-2 (10), A(5) (13) and C-6 (14) from the same sponge and determine their structures. From the structure-activity relationship st udy, each of the 3,4,6-acetoxyl groups and 11,22-hydroxyl groups was elucid ated to be crucial for reversing MDR in tumor cells. (C) 1999 Elsevier Scie nce Ltd. All rights reserved.