Skip directly to search Skip directly to A to Z list Skip directly to page options Skip directly to site content

NIOSHTIC-2 Publications Search

Search Results

Studies of the binding of bisbenzylisoquinoline alkaloids to phosphatidylcholine vesicles and alveolar macrophages in relation to their antifibrogenic potential.

Authors
Ma-JK; Mo-C; Malanga-CJ; Ma-JY; Castranova-V
Source
Proceedings of the 3rd Symposium on Respirable Dust in the Mineral Industries, Pittsburgh, Pennsylvania, October 17-19, 1990. Frantz RL, Ramani, RV, eds., Littleton, CO: Society for Mining, Metallurgy, and Exploration, 1990 Oct; :153-158
Link
NIOSHTIC No.
00232443
Abstract
The relative lipophilicity and binding to phosphatidylcholine vesicles and rat alveolar macrophages of bisbenzylisoquinoline (BBIQ) alkaloids were compared and discussed in terms of their structures and antifibrogenic activities in silica (14808607) induced fibrosis. The BBIQs tested included tetrandrine (TE), fangchinoline (FA), berbamine (BE), cepharanthine (CE), tubocurine (TU), curine, cycleanine (CY) and methoxyadiantifoline (ME). ME, with nine methoxy groups, had the highest lipophilicity, followed by TE, CY, CE, FA and BE, with CU and TU, both containing two hydroxy groups, the least lipophilic. Relative binding affinities to dipalmitoyl-phosphatidylcholine lipid vesicles, measured by fluorescence and analyzed using the Scatchard equation, was consistent with the order of lipophilicity. An equilibrium dialysis method was employed to determined the binding affinities of the BBIQ alkaloids to Sprague-Dawley-rat alveolar macrophages. In this assay, TE was shown to have the greatest binding affinity, followed by ME and FA. No binding activity was detected for CU or TU. A statistical correlation between relative macrophage binding ability and antifibrotic activity was calculated. The authors conclude that the interaction of TE, ME and FA with alveolar macrophages may inhibit silica induced lung fibrosis, preventing further progression of silica induced pulmonary disease.
Keywords
Lung-cells; Alveolar-cells; Quinolines; Molecular-structure; Silicosis; Lung-fibrosis; Pulmonary-disorders; Respiratory-system-disorders; Medical-treatment; Mammalian-cells
CAS No.
14808-60-7
Publication Date
19911017
Document Type
Conference/Symposia Proceedings
Editors
Frantz-RL; Ramani-RV
Fiscal Year
1992
NTIS Accession No.
NTIS Price
ISBN No.
9780873350983
NIOSH Division
HELD
Priority Area
Respiratory-system-disorders
Source Name
Proceedings of the 3rd Symposium on Respirable Dust in the Mineral Industries, Pittsburgh, Pennsylvania, October 17-19, 1990
State
CO; WV
TOP