| Summary: | Xanthone derivatives have shown promising antitumor properties, and 1-carbaldehyde-3,4-dimethoxyxanthone (<b>1</b>) has recently emerged as a potent tumor cell growth inhibitor. In this study, its effect was evaluated (MTT viability assay) against a new panel of cancer cells, namely cervical cancer (HeLa), androgen-sensitive (LNCaP) and androgen-independent (PC-3) prostate cancer, and nonsolid tumor derived cancer (Jurkat) cell lines. The effect of xanthone <b>1</b> on macrophage functions was also evaluated. The effect of xanthone <b>1</b>-conditioned THP-1 human macrophage supernatants on the metabolic viability of cervical and prostate cancer cell lines was determined along with its interference with cytokine expression characteristic of M1 profile (IL-1 ≤ β; TNF-α) or M2 profile (IL-10; TGF-β) (PCR and ELISA). Nitric oxide (NO) production by murine RAW264.7 macrophages was quantified by Griess reaction. Xanthone <b>1</b> (20 μM) strongly inhibited the metabolic activity of the cell lines and was significantly more active against prostate cell lines compared to HeLa (<i>p</i> < 0.05). Jurkat was the cell most sensitive to the effect of xanthone <b>1</b>. Compound <b>1</b>-conditioned IL-4-stimulated THP-1 macrophage supernatants significantly (<i>p</i> < 0.05) inhibited the metabolic activity of HeLa, LNCaP, and PC-3. Xanthone <b>1</b> did not significantly affect the expression of cytokines by THP-1 macrophages. The inhibiting effect of compound <b>1</b> observed on the production of NO by RAW 264.7 macrophages was moderate. In conclusion, 1-carbaldehyde-3,4-dimethoxyxanthone (<b>1</b>) decreases the metabolic activity of cancer cells and seems to be able to modulate macrophage functions.
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