- (±)-Aeroplysinin-1, an optically active 1.2-dihydroarene-1.2-diol. was isolated from the marine sponges Verongia aerophoba (+-isomer) and lanthella ardis (--isomer). For the experiments presented we used the +-isomer from Verongia aerophoba. Here we describe the hitherto unknown biological and pharmacological property of this compound to display pronounced anticancer activity against L5178y mouse lymphoma cells (ED50: 0.5 μm). Friend erythroleukemia cells (ED50: 0.7μm) , human mamma carcinoma cells (ED50: 0.3μm) and human colon carcinoma cells (ED50: 3.0 μm) in vitro. Furthermore, aeroplysinin caused a preferential inhibition of [3H]thymidine (dThd) incorporation rates in L5178y mouse lymphoma cells if compared with murine spleen lymphocytes in vitro. At concentrations between 1.1 and 28.5 μm, the [3H]dThd incorporation rates in L5178y cells were suppressed to 28% -0% but only to 78% -18% in murine spleen lymphocytes. The same differential effect in vitro was found with the following epithelial cells: 14.70 μm of the compound were required to inhibit normal human fibroblasts to 50% , but only 2.9 μm in the assays with human malign keratinocytes or malignant melanoma cells to observe the same inhibitory effect. Moreover, aeroplysinin-1 displayed antileukemic activity in vivo using the L5178y cell/NMRI mouse system; administered at a dose of 50 mg/kg for five consecutive days, the T/C (% ) value was determined to be 338. Preliminary toxicology studies revealed an acute LD50 of 202 mg/kg and a subacute LD50 of 150 mg/kg. Aeroplysinin-1 is neither a direct mutagen nor a premutagen in the umu/Salmonella typhimurium test system.
MetadatenAuthor: | Matthias-Heinrich Kreuter, August BerndORCiDGND, Hans HolzmannGND, Wolfgang Müller-KlieserGND, Armin Maidhof, Norbert Weißmann, Zoran Kljajić, Renato Batel, Heinz C. SchröderORCiDGND, Werner E. G. MüllerGND |
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URN: | urn:nbn:de:hebis:30:3-799050 |
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DOI: | https://doi.org/10.1515/znc-1989-7-822 |
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ISSN: | 0939-5075 |
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ISSN: | 1865-7125 |
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Parent Title (German): | Zeitschrift für Naturforschung, C |
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Publisher: | Verlag der Zeitschrift für Naturforschung |
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Place of publication: | Tübingen |
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Document Type: | Article |
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Language: | English |
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Date of Publication (online): | 2014/06/02 |
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Year of first Publication: | 1989 |
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Publishing Institution: | Universitätsbibliothek Johann Christian Senckenberg |
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Release Date: | 2024/02/07 |
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Tag: | Aeroplysinin-1; Epithelioma Cells; Lymphoma Cells |
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Volume: | 44.1989 |
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Issue: | 7-8 |
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Page Number: | 9 |
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First Page: | 680 |
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Last Page: | 688 |
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Institutes: | Medizin |
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Dewey Decimal Classification: | 5 Naturwissenschaften und Mathematik / 57 Biowissenschaften; Biologie / 570 Biowissenschaften; Biologie |
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| 6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit |
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Sammlungen: | Universitätspublikationen |
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Licence (German): | Creative Commons - Namensnennung-Nicht kommerziell-Keine Bearbeitung 3.0 |
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