Abstract
Objective: Aspergillus fungus is a rich source of natural products with broad biological activities. This study was conducted to identify secondary metabolites from the rice culture of Aspergillus species isolated from Melaleuca subulata leaves and evaluated their anticancer activity.
 Methods: Ethyl acetate extract was fractionated on silica gel and Sephadex columns. Structures of the compounds were established using physical and chemical methods. Cytotoxic activities of the extract and pure compounds against two human cancer cell lines (Mcf-7and Hep G2) were evaluated using microculture tetrazolium assay as well as the mode of the cytotoxicity was evaluated. Molecular docking studies have been performed using the Hsp 90 enzyme as an anticancer target.
 Results: Methyl linoleate (1), arugosin C (2), ergosterol (3), sterigmatocystin (4), diorcinol (5), alternariol-5-O-methyl ether (6), averufin (7), averufanin (8), and alternariol (9) were identified from ethyl acetate extract. All tested compounds exhibit week activity against MCF-7 and Hep G2 cell lines but a mixture of compounds 7 and 8 is considered to be more active towards both MCF-7 and Hep G 2 in comparison to other compounds. Compound 4 exhibits moderate activity against Hep G2 only as well as the ethyl acetate extract exerts moderate activity against MCF-7 cell line Moreover, compound 4 and a mixture of 7 and 8 caused a decrease in the number of Hep G2 cancer cells due to apoptotic and necrotic processes. Most active anticancer candidates 7 and 8 showed binding to the active site similar to geldanamycin reference ligand.
 Conclusion: Secondary metabolites identified from Aspergillus sp. and their anticancer activity were evaluated. Molecular docking suggested active candidates as Hsp 90 inhibitors.
Highlights
Plant endophytes are considered as a fungal or bacterial microorganism that spends whole or part of its life in the living tissues of the plant without causing apparent symptoms of disease [1, 2]
This study aimed to investigate the metabolites from Aspergillus sp. isolated from leaf tissue of M. subulata and to evaluate the anticancer activity of the total ethyl acetate extract and the pure isolated compounds
Apoptotic and necrotic studies were done to detect the mode of cell death as well as molecular docking was applied to suggest the mechanism of anticancer activity of most active compounds
Summary
Plant endophytes are considered as a fungal or bacterial microorganism that spends whole or part of its life in the living tissues of the plant without causing apparent symptoms of disease [1, 2]. Sanguinarine, and gallic acid are examples for secondary metabolites obtained from the endophytic fungi known to possess significant biological activities like anticancer, antimicrobial, and antioxidant activities [3,4,5]. Some of the secondary metabolites isolated from Aspergillus species are well known as penicillin, viridivatin, mevinolin, pseurotin A, and cyclopiazonic acid [6]. Secondary metabolites isolated from different Aspergillus species have frequently attracted the interest of pharmacologists due to their broad range of biological activities as anticancer and antimicrobial effects as well as their structural diversity range from polyketides, terpenoids, and alkaloids [6,7,8,9,10]. Isolated from leaf tissue of M. subulata and to evaluate the anticancer activity of the total ethyl acetate extract and the pure isolated compounds. Apoptotic and necrotic studies were done to detect the mode of cell death as well as molecular docking was applied to suggest the mechanism of anticancer activity of most active compounds
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