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

Yi-Cheng Chu,Hsiang-Ruei Liao,Shu-Ling Fu,Chun-Hao Chang,Jih-Jung Chen

doi:10.3390/md19080408

Abstract

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 μM, 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 μM, 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.

Highlights

Marine fungi have been a major source of special structures and bioactive secondary metabolites for lead compounds
Human neutrophils play a significant role in host defenses against pathogen invasion and are the main acute inflammatory mediators [9,10]
After different stimuli, activated neutrophils produce a series of cytotoxins, such as superoxide anion (O2–), granule proteases, and bioactive lipids [9,11,12]

Summary

Introduction

Marine fungi have been a major source of special structures and bioactive secondary metabolites for lead compounds. A large number of natural products with biological activities are found in the genus Penicillium [1,2,3,4,5,6,7]. The marine fungus Penicillium citrinum was found to produce many new bioactive compounds, such as antibacterial dihydroisocoumarins [2], benzopyrans [6], benzophenones [7], antifungal citrinin [4], anticancer benzophenones [7,8], and anti-inflammatory chromone derivatives [8]. After different stimuli, activated neutrophils produce a series of cytotoxins, such as superoxide anion (O2–), granule proteases, and bioactive lipids [9,11,12]. An inadequately triggered oxidative burst may cause lipid peroxidation, tissue injury, and inflammatory diseases [13]

Methods

Results

Conclusion