Anti-Cancer and Anti-Inflammatory Activities of Three New Chromone Derivatives from the Marine-Derived Penicillium citrinum

Three new and uncommon chromone analogs, epiremisporine F (1), epiremisporine G (2), and epiremisporine H (3), were isolated from marine-origin Penicillium citrinum. Among the isolated compounds, compounds 2-3 remarkably suppressed fMLP-induced superoxide anion generation by human neutrophils, with IC50 values of 31.68 +/- 2.53, and 33.52 +/- 0.42 mu M, respectively. Compound 3 exhibited cytotoxic activities against human colon carcinoma (HT-29) and non-small lung cancer cell (A549) with IC50 values of 21.17 +/- 4.89 and 31.43 +/- 3.01 mu M, respectively, and Western blot assay confirmed that compound 3 obviously induced apoptosis of HT-29 cells, via Bcl-2, Bax, and caspase 3 signaling cascades.

Automated summary

In this study, three new and uncommon chromone analogs were isolated from marine-origin Penicillium citrinum, among which compounds 2-3 exhibited remarkable suppression of superoxide anion generation by human neutrophils and cytotoxic activities against human cancer cells. Compound 3 was found to induce apoptosis of HT-29 cells via Bcl-2, Bax, and caspase 3 signaling cascades.