Abstract
The cytotoxicity of the polyphenol 2,2´-bis[4,5-bis(4-hydroxybenzyl)-2-(4-hydroxyphenyl)cyclopent-4-en-1,3-dione], nostotrebin 6 (NOS-6), was tested under in vitro conditions using mouse fibroblasts (BALB/c cells). Identification of NOS-6 and its uptake into fibroblasts was examined by multi-stage mass spectrometry analysis with the following fragmentation pattern: MS (m/z) [M+H]+ 799.1 → MS2 399.1 → MS3 305.1 → MS4 277.1. Using several cell viability assays, the IC50 of NOS-6 after 24 h incubation was found to be 8.48 ± 0.16/12.15 ± 1.96 µM (neutral red/MTT assay) which was higher than that of doxorubicin. It was found that NOS-6 is capable of inducing both types of cell death, apoptosis and necrosis in a dose-dependent manner. The biological activities of the cyclopentenediones and preliminary data on NOS-6 cytotoxicity are discussed.
Highlights
Cyanobacteria and algae are producers of secondary metabolites and a number of these are phenolic compounds that induce diverse biological effects in mammals [1]
Amounts of 1.5 and 4.5 μg nostotrebin 6 (NOS-6) per 1 × 105 cells were found after 4 h incubation where 0.5 and 1 μM NOS-6 were present in the cultivation medium (Figure 1c)
After termination of the incubation period, 59% of NOS-6 was found in the cytosolic fraction and 41% was bound onto cell membranes
Summary
Cyanobacteria and algae are producers of secondary metabolites and a number of these are phenolic compounds that induce diverse biological effects in mammals [1]. Of these phenolics, phenolic acids and their esters [2,3], a large group of phenols derived from phloroglucinol (phlorotannins) [4] and halogenated and sulphated derivatives of phenols [5] have been found (reviewed in [1,6]). Secondary metabolites, including phenolic compounds, in cyanobacteria and algae and their biological activities were reviewed in [8]. X-ray crystallographic analysis of NOS-6 has shown its structure to be 2,2 ́-bis[4,5-bis(4hydroxybenzyl)-2-(4-hydroxyphenyl)cyclopent-4-en-1,3-dione]
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