Abstract
The effect of Lonidamine, 1-(2,4 dichlorobenzyl)-1-H-indazol-3-carboxylic acid, on the uptake of Adriamycin by Ehrlich ascites tumor cells has been investigated. The uptake of Adriamycin is greatly stimulated by Lonidamine and the increase depends on the energy sources of the cell. In the presence of glucose the intracellular drug content is remarkably lower than that in its absence. This difference lies in the mechanism by which Lonidamine enhances the uptake of Adriamycin. The Adriamycin efflux is via an active transport process and, in the presence of glucose, both aerobic glycolysis and oxidative phosphorylation contribute to ATP synthesis. Although Lonidamine inhibits both these pathways, there is still sufficient ATP to extrude a certain amount of Adriamycin. The elevated intracellular concentration of Adriamycin depends not only on the Lonidamine-inhibited outward transport but also on higher membrane permeability which allows a low concentration of Adriamycin (18 μM) to interfere also with the oxidative metabolism of Ehrlich ascites tumor cells.
| Original language | English |
|---|---|
| Pages (from-to) | 421-431 |
| Number of pages | 11 |
| Journal | Experimental and Molecular Pathology |
| Volume | 49 |
| Issue number | 3 |
| DOIs | |
| Publication status | Published - 1988 |
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ASJC Scopus subject areas
- Clinical Biochemistry
- Molecular Biology
- Pathology and Forensic Medicine
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Modulation of adriamycin uptake by lonidamine in ehrlich ascites tumor cells. / Floridi, A.; Gambacurta, A.; Bagnato, A.; Bianchi, C.; Paggi, M. G.; Silvestrini, B.; Caputo, A.
In: Experimental and Molecular Pathology, Vol. 49, No. 3, 1988, p. 421-431.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Modulation of adriamycin uptake by lonidamine in ehrlich ascites tumor cells
AU - Floridi, A.
AU - Gambacurta, A.
AU - Bagnato, A.
AU - Bianchi, C.
AU - Paggi, M. G.
AU - Silvestrini, B.
AU - Caputo, A.
PY - 1988
Y1 - 1988
N2 - The effect of Lonidamine, 1-(2,4 dichlorobenzyl)-1-H-indazol-3-carboxylic acid, on the uptake of Adriamycin by Ehrlich ascites tumor cells has been investigated. The uptake of Adriamycin is greatly stimulated by Lonidamine and the increase depends on the energy sources of the cell. In the presence of glucose the intracellular drug content is remarkably lower than that in its absence. This difference lies in the mechanism by which Lonidamine enhances the uptake of Adriamycin. The Adriamycin efflux is via an active transport process and, in the presence of glucose, both aerobic glycolysis and oxidative phosphorylation contribute to ATP synthesis. Although Lonidamine inhibits both these pathways, there is still sufficient ATP to extrude a certain amount of Adriamycin. The elevated intracellular concentration of Adriamycin depends not only on the Lonidamine-inhibited outward transport but also on higher membrane permeability which allows a low concentration of Adriamycin (18 μM) to interfere also with the oxidative metabolism of Ehrlich ascites tumor cells.
AB - The effect of Lonidamine, 1-(2,4 dichlorobenzyl)-1-H-indazol-3-carboxylic acid, on the uptake of Adriamycin by Ehrlich ascites tumor cells has been investigated. The uptake of Adriamycin is greatly stimulated by Lonidamine and the increase depends on the energy sources of the cell. In the presence of glucose the intracellular drug content is remarkably lower than that in its absence. This difference lies in the mechanism by which Lonidamine enhances the uptake of Adriamycin. The Adriamycin efflux is via an active transport process and, in the presence of glucose, both aerobic glycolysis and oxidative phosphorylation contribute to ATP synthesis. Although Lonidamine inhibits both these pathways, there is still sufficient ATP to extrude a certain amount of Adriamycin. The elevated intracellular concentration of Adriamycin depends not only on the Lonidamine-inhibited outward transport but also on higher membrane permeability which allows a low concentration of Adriamycin (18 μM) to interfere also with the oxidative metabolism of Ehrlich ascites tumor cells.
UR - http://www.scopus.com/inward/record.url?scp=0024245504&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0024245504&partnerID=8YFLogxK
U2 - 10.1016/0014-4800(88)90013-5
DO - 10.1016/0014-4800(88)90013-5
M3 - Article
C2 - 3197818
AN - SCOPUS:0024245504
VL - 49
SP - 421
EP - 431
JO - Experimental and Molecular Pathology
JF - Experimental and Molecular Pathology
SN - 0014-4800
IS - 3
ER -