Abstract
One of the most potent inhibitors of RNA-dependent DNA polymerase activity so far described (rifazacyclo-16) was not correspondingly as active in focus inhibition. This discrepancy was thought to be due to the inability of the drug to penetrate the cell membrane. It has been found that a very low level of amphotericin B allows this drug, as well as the previously described 2′,6′-dimethyl-N(4′)benzyl-N(4′)-[desmethyl] rifampicin, to exhibit a very high capability to inhibit focus formation. Since these two drugs are highly lipophilie, their activity may be expected to be dependent upon any lipophilic components in the medium, such as serum or detergents. The use of amphotericin B as well as serum in tissue cultures is common, and could account for some of the variability in focus inhibition reported in the literature.
Keywords: focus formation, drug transport, lipophilicity
Full text
PDFSelected References
These references are in PubMed. This may not be the complete list of references from this article.
- CIRILLO V. P., HARSCH M., LAMPEN J. O. ACTION OF THE POLYENE ANTIBIOTICS FILIPIN, NYSTATIN AND N-ACETYLCANDIDIN ON THE YEAST CELL MEMBRANE. J Gen Microbiol. 1964 May;35:249–259. doi: 10.1099/00221287-35-2-249. [DOI] [PubMed] [Google Scholar]
- Calvin M., Joss U. R., Hackett A. J., Owens R. B. Effect of rifampicin and two of its derivatives on cells infected with Moloney sarcoma virus. Proc Natl Acad Sci U S A. 1971 Jul;68(7):1441–1443. doi: 10.1073/pnas.68.7.1441. [DOI] [PMC free article] [PubMed] [Google Scholar]
- DEMEL R. A., VAN DEENENL PENETRATION OF LIPID MONOLAYERS BY POLYENE ANTIBIOTICS. CORRELATION WITH SELECTIVE TOXICITY AND MODE OF ACTION. J Biol Chem. 1965 Jun;240:2749–2753. [PubMed] [Google Scholar]
- Hackett A. J., Owens R. B., Calvin M., Joss U. Inhibition of MSV viral function by rifampicin derivatives. Medicine (Baltimore) 1972 May;51(3):175–180. doi: 10.1097/00005792-197205000-00003. [DOI] [PubMed] [Google Scholar]
- Hackett A. J., Sylvester S. S. Cell line derived from Balb-3T3 that is transformed by murine leukaemia virus: a focus assay for leukaemia virus. Nat New Biol. 1972 Oct 11;239(93):164–166. doi: 10.1038/newbio239164a0. [DOI] [PubMed] [Google Scholar]
- Kobbayashi G. S., Medoff G., Schlessinger D., Kwan C. N., Musser W. E. Amphotericin B potentiation of rifampicin as an antifungal agent against the yeast phase of Histoplasma capsulatum. Science. 1972 Aug 25;177(4050):709–710. doi: 10.1126/science.177.4050.709. [DOI] [PubMed] [Google Scholar]
- Manning J. S., Hackett A. J., Darby N. B., Jr Effect of polycations on sensitivity of BALD-3T3 cells to murine leukemia and sarcoma virus infectivity. Appl Microbiol. 1971 Dec;22(6):1162–1163. doi: 10.1128/am.22.6.1162-1163.1971. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Medoff G., Kobayashi G. S., Kwan C. N., Schlessinger D., Venkov P. Potentiation of rifampicin and 5-fluorocytosine as antifungal antibiotics by amphotericin B (yeast-membrane permeability-ribosomal RNA-eukaryotic cell-synergism). Proc Natl Acad Sci U S A. 1972 Jan;69(1):196–199. doi: 10.1073/pnas.69.1.196. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Robinson H. L., Robinson W. S. Inhibition of growth of uninfected and rous sarcoma virus-infected chick-embryo fibroblasts by rifampicin. J Natl Cancer Inst. 1971 Apr;46(4):785–788. [PubMed] [Google Scholar]