Cytostatic Activity of Aeroplysinin-1 against Lymphoma and Epithelioma Cells

1989 ◽  
Vol 44 (7-8) ◽  
pp. 680-688 ◽  
Author(s):  
M. H. Kreuter ◽  
A. Bernd ◽  
H. Holzmann ◽  
W. Müller-Klieser ◽  
A. Maidhof ◽  
...  

(±)-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.

1987 ◽  
Vol 243 (1) ◽  
pp. 189-194 ◽  
Author(s):  
M Bachmann ◽  
W J Mayet ◽  
H C Schröder ◽  
K Pfeifer ◽  
K H Meyer zum Büschenfelde ◽  
...  

45 S RNP (ribonucleoprotein) particles from calf thymus or L5178y mouse lymphoma cells contain the poly(A)-modulated and oligo(U)-binding endoribonuclease VII [Bachmann, Zahn & Müller (1983) J. Biol. Chem. 258, 7033-7040]. From these particles a 4.5 S RNA was isolated that possesses an oligo(U) sequence. By using monospecific and non-cross-reacting antibodies directed against the La or Ro antigen, both proteins were identified in the endoribonuclease VII-RNP complex after phosphorylation in vitro. In a second approach, endoribonuclease VII activity was identified in immunoaffinity-purified Ro RNPs after preparative isoelectric focusing. Therefore we conclude that the 4.5 S RNA belongs to the Ro RNAs. The results indicate a possible function of endoribonuclease VII in activating stored mRNAs.


2006 ◽  
Vol 17 (3) ◽  
pp. 228-232 ◽  
Author(s):  
Daniel Araki Ribeiro ◽  
Mariângela Esther Alencar Marques ◽  
Daisy Maria Fávero Salvador

Chloroform and eucalyptol are widely used in clinical dentistry as gutta-percha solvents. However, these compounds may represent a hazard to human health, especially by causing injury to genetic apparatus and/or inducing cellular death. In this study, the genotoxic and cytotoxic potentials associated with exposure to chloroform and eucalyptol were assessed on mouse lymphoma cells in vitro by the single cell gel (comet) assay and trypan blue exclusion test, respectively. Both gutta-percha solvents proved to be cytotoxic at the same levels in concentrations of 2.5, 5 and 10 muL/mL (p<0.05). On the other hand, neither of the solvents induced DNA breakage. Taken together, these results suggest that although both tested compounds (chloroform and eucalyptol) are strong cytotoxicants, it seems that they are not likely to increase the level of DNA damage on mammalian cells.


2011 ◽  
Vol 2011 ◽  
pp. 1-7
Author(s):  
A. B. Ivanova ◽  
D. I. Batovska ◽  
I. T. Todorova ◽  
B. A. Stamboliyska ◽  
J. Serly ◽  
...  

Based on the structure of three previously established lead compounds, fifteen selected chalcones were synthesized and evaluated for their multidrug resistance (MDR) reversal activity on mouse lymphoma cells. The most active chalcones were stronger revertants than the positive control, verapamil. In the model of combination chemotherapy, the interactions between the anticancer drug doxorubicin and two of the most effective compounds were measured in vitro, on human MDR1 gene transfected mouse lymphoma cells, showing that the type of interaction for one of these compounds was indifferent while that for the other one was additive. Furthermore, two chalcones inhibited 50% of cell proliferation in concentration of around 0.4 μg/mL and were from 2- to 100-fold more active than the most chalcones. The structure-activity relationships were obtained and discussed in view of their usefulness for the design of chalcone-like P-gp modulators and drugs able to treat resistant cancers.


1985 ◽  
Vol 40 (11-12) ◽  
pp. 922-924
Author(s):  
Stephan Paul Jost ◽  
Jane Cole ◽  
Brian C. Goodwin

Abstract Three growth rate experiments involving several sampling points were performed to investigate the previous finding that very low concentrations of HgCl2 inhibit the growth of murine lymphoblasts in vitro. However, results presented here do not confirm this, there being no significant differences between the three independent growth rate experiments.


2006 ◽  
Vol 33 (12) ◽  
pp. 912-917 ◽  
Author(s):  
D. A. RIBEIRO ◽  
M. E. A. MARQUES ◽  
D. M. F. SALVADORI

Sign in / Sign up

Export Citation Format

Share Document