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First Results from a Screening of 300 Naturally Occurring Compounds: 4,6-dibromo-2-(2′,4′-dibromophenoxy)phenol, 4,5,6-tribromo-2-(2′,4′-dibromophenoxy)phenol, and 5-epi-nakijinone Q as Substances with the Potential for Anticancer Therapy

1
Faculty Medical and Life Sciences, Campus Villingen-Schwenningen, Hochschule Furtwangen University, 78120 Furtwangen, Germany
2
Department of Hematology, Oncology and Clinical Immunology, University Hospital Düsseldorf, 40225 Düsseldorf, Germany
3
Institute for Molecular Medicine I, University Hospital Düsseldorf, 40225 Düsseldorf, Germany
4
Institute of Pharmaceutical Biology and Biotechnology, Heinrich Heine University, 40225 Düsseldorf, Germany
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Mar. Drugs 2019, 17(9), 521; https://doi.org/10.3390/md17090521
Received: 24 August 2019 / Accepted: 2 September 2019 / Published: 5 September 2019
There is a variety of antineoplastic drugs that are based on natural compounds from ecological niches with high evolutionary pressure. We used two cell lines (Jurkat J16 and Ramos) in a screening to assess 300 different naturally occurring compounds with regard to their antineoplastic activity. The results of the compounds 4,6-dibromo-2-(2′,4′-dibromophenoxy)phenol (P01F03), 4,5,6-tribromo-2-(2′,4′-dibromophenoxy)phenol (P01F08), and 5-epi-nakijinone Q (P03F03) prompted us to perform further research. Using viability and apoptosis assays on the cell lines of primary human leukemic and normal hematopoietic cells, we found that P01F08 induced apoptosis in the cell lines at IC50 values between 1.61 and 2.95 μM after 72 h. IC50 values of peripheral blood mononuclear cells (PBMNCs) from healthy donors were higher, demonstrating that the cytotoxicity in the cell lines reached 50%, while normal PBMNCs were hardly affected. The colony-forming unit assay showed that the hematopoietic progenitor cells were not significantly affected in their growth by P01F08 at a concentration of 3 μM. P01F08 showed a 3.2-fold lower IC50 value in primary leukemic cells [acute myeloid leukemia (AML)] compared to the PBMNC of healthy donors. We could confirm the antineoplastic effect of 5-epi-nakijinone Q (P03F03) on the cell lines via the induction of apoptosis but noted a similarly strong cytotoxic effect on normal PBMNCs. View Full-Text
Keywords: marine sponge derived natural products; polybrominated diphenyl ethers; sesquiterpene aminoquinone; bioactive natural products; cytotoxic activity; apoptosis; peripheral blood mononuclear cells; primary leukemic cells; acute myeloid leukemia; drug leads marine sponge derived natural products; polybrominated diphenyl ethers; sesquiterpene aminoquinone; bioactive natural products; cytotoxic activity; apoptosis; peripheral blood mononuclear cells; primary leukemic cells; acute myeloid leukemia; drug leads
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Mayer, S.; Prechtl, M.; Liebfried, P.; Cadeddu, R.-P.; Stuhldreier, F.; Kohl, M.; Wenzel, F.; Stork, B.; Wesselborg, S.; Proksch, P.; Germing, U.; Haas, R.; Jäger, P. First Results from a Screening of 300 Naturally Occurring Compounds: 4,6-dibromo-2-(2′,4′-dibromophenoxy)phenol, 4,5,6-tribromo-2-(2′,4′-dibromophenoxy)phenol, and 5-epi-nakijinone Q as Substances with the Potential for Anticancer Therapy. Mar. Drugs 2019, 17, 521.

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