TY  - JOUR
A1  - Kreuter, Matthias-Heinrich
A1  - Bernd, August
A1  - Holzmann, Hans
A1  - Müller-Klieser, Wolfgang
A1  - Maidhof, Armin
A1  - Weißmann, Norbert
A1  - Kljajić, Zoran
A1  - Batel, Renato
A1  - Schröder, Heinz C.
A1  - Müller, Werner E. G.
T1  - Cytostatic activity of aeroplysinin-1 against lymphoma and epithelioma cells
T2  - Zeitschrift für Naturforschung, C
N2  - (±)-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.
KW  - Aeroplysinin-1
KW  - Lymphoma Cells
KW  - Epithelioma Cells
Y1  - 2014
UR  - http://publikationen.ub.uni-frankfurt.de/frontdoor/index/index/docId/79905
UR  - https://nbn-resolving.org/urn:nbn:de:hebis:30:3-799050
SN  - 0939-5075
SN  - 1865-7125
VL  - 44.1989
IS  - 7-8
SP  - 680
EP  - 688
PB  - Verlag der Zeitschrift für Naturforschung
CY  - Tübingen
ER  -