Abstract
Background: Previous studies have demonstrated that geranyl metabolites, found mainly in marine organisms, exhibit interesting antimicrobial and antifungal activities. In addition, linear geranyl derivatives have been synthesized as drugs and reported cytotoxic and anticancer activities.
 Aims: Considering the biological testing and the structural features of these compounds, we evaluated seven linear geranylphenol derivatives on the human breast cancer cell line MDA-MB-231, and the human gastric cancer cell line MKN74.
 Results: We found that compounds 2, 5 and 7 were cytotoxic for both cancer cell lines. From them, the most potent was compound 2, with an IC50=7.5 μM for MKN74 cells, and compound 7, with an IC50=14.73 μM for MDA-MB-231 cells. By nuclear staining and inmunocytochemistry, we detected that the three compounds induced cell death, and by Western blot analysis, we observed a remarkable decrease in the expression of cyclin D1 and the retinoblastoma protein, key regulators of the cell cycle.
 Conclusion: Considering that compounds 2 and 7 were the most potent compounds inducing cell death, and were able to decrease the expression of retinoblastoma protein and cyclin D1, proteins usually altered in different types of cancers, they appear as promising therapeutic agents against cancer.
 Bangladesh Journal of Medical Science Vol.19(3) 2020 p.486-500
Highlights
In this report, considering the interesting antiproliferative effect and apoptotic activity of mono and digeranylmethoxyphenols, we present the cytotoxic effect of linear geranylmethoxyphenol derivatives, on the human breast cancer cell line MDA-MB-231, a highly aggressive, invasive and poorly differentiated adenocarcinoma, and the gastric cancer cell line MKN74, a moderately-differentiated tubular adenocarcinoma
The cytotoxic effect of compounds [1,2,3,4,5,6,7] were evaluated in the breast cancer cell line MDA-MB-231 and the gastric cancer cell line MKN74, since these cells are widely used to characterize the behavior of the respective human cancers
Seven different linear geranylmethoxyphenol derivatives were tested as potential cytotoxic compounds in the human breast and gastric cancer cell lines, MDA-MB-231 and MKN74, respectively
Summary
2-geranylhydroquinone (Figure 1A) are a sub-class of secondary metabolites whose terpene portion may have a length of up to 8 isoprene units 1 They are found mainly in marine organisms, such as brown algae 2–5,sponges [1,6], corals 7, gorgonians 8 and ascidians . Aims: Considering the biological testing and the structural features of these compounds, we evaluated seven linear geranylphenol derivatives on the human breast cancer cell line MDA-MB-231, and the human gastric cancer cell line MKN74. Conclusion: Considering that compounds 2 and 7 were the most potent compounds inducing cell death, and were able to decrease the expression of retinoblastoma protein and cyclin D1, proteins usually altered in different types of cancers, they appear as promising therapeutic agents against cancer.
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