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Antitumor activity and biochemical effects of topsentin
| Title: | Antitumor activity and biochemical effects of topsentin. |
 83 views 21 downloads |
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| Name(s): |
Burres, N. S., creator Barber, D. A., creator Gunasekera, Sarath P., creator Clement, J. J., creator Shen, L. L. |
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| Type of Resource: | text | |
| Genre: | Article | |
| Issuance: | single unit | |
| Date Issued: | 1991 | |
| Publisher: | Elsevier Inc. | |
| Extent: | 8 p. | |
| Physical Description: | ||
| Language(s): | English | |
| Identifier: | 3355144 (digitool), FADT3355144 (IID), fau:6670 (fedora), 10.1016/0006-2952(91)90031-Y (doi) | |
| Note(s): |
Topsentin, a bis(indolyl)imidazole marine natural product, inhibited the proliferation of cultured human and murine tumor cells at micromolar concentrations (ic50 values ranged from 4 to 40 μM) and was active against in vivo P388 leukemia tumors. Effects of 30 μM topsentin (1-hr exposures) on incorporation of radiolabeled precursors by P388 cells indicated inhibition of DNA synthesis (91%) and to a lesser extent RNA synthesis (57%), whereas synthesis of protein was unaffected (0%). Fluorescence spectral changes and competitive binding experiments with ethidium bromide indicated that topsentin interacted with DNA. No evidence for intercalation was observed in DNA unwinding studies, but competitive binding experiments with Hoechst 33342 and CC-1065 indicated that topsentin bound to DNA in the minor groove. The final published version of this manuscript is available at http://www.sciencedirect.com/science/journal/00062952 and may be cited as: Burres, N. S., Barber, D. A., Gunasekera, S. P., Shen, L. L., & Clement, J. J. (1991). Antitumor activity and biochemical effects of topsentin. Biochemical Pharmacology, 42(4), 745-751. doi:10.1016/0006-2952(91)90031-Y Florida Atlantic University. Harbor Branch Oceanographic Institute contribution #866. |
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| Subject(s): |
Marine natural products Antitumor agents |
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| Persistent Link to This Record: | http://purl.flvc.org/FCLA/DT/3355144 | |
| Links: | http://dx.doi.org/10.1016/0006-2952(91)90031-Y | |
| Restrictions on Access: | ©1991 Elsevier Inc. | |
| Host Institution: | FAU |
