Comprehensive Study on the Chemical Profile and Anti-Tumor Activity of Secondary Metabolites Produced by Aspergillus niger

Objective: Chemical investigation of the extract of sponge-derived fungus, Aspergillus niger, was performed by liquid chromatography coupled with QExactive mass spectrometry for the first time. Method: A total number of 444 constituents were detected, 288 of which were identified positively or tentatively by the comprehensive utilization of accurate molecular weight and fragmentation information acquired from quadrupole orbitrap mass spectrometry. The identified compounds were divided into several types, namely, organic acid, alkaloid, saccharide, amino acid and cyclopeptide, terpenoid, polyketone, phenylpropanoid and other types of compounds. Systematic diagnostic ions and featured fragment patterns were summarized for each type, based on which 8 novel compounds belonging to the same type were characterized. Results: This work provided a rapid approach for the research of micro constituents in a complex analyte. Furthermore, the anti-tumor activity of the extract was evaluated on two different cell lines-Bel-7402 and Hela-S3 in vitro. The tumor-inhibitory effect of the Aspergillus niger extract was confirmed and may be mainly derived from its pro-apoptotic action. Moreover, the extract exerted more significant cytotoxicity in Bel-7402 cells than Hela-S3 cells, indicative of its selectivity on specific tumor cells. Conclusion: The evidence suggested that the Aspergillus niger extract may potentially serve as a remedy for the prevention and therapy of hepatic and breast carcinoma.