Abstract
Drug resistance to the classically used chemotherapeutic drugs is the major challenge in their treatment of cancer needing the discovery of novel anticancer drugs. In terms of finding novel therapeutics, endophytes are quite promising as they are an excellent source of novel structures, which exhibit bioactivity. The present study demonstrated a dose-dependent antiproliferative activity of mycelial-derived secondary metabolites from a macroalgae associated endophyte Aspergillus unguis AG 1.1(G). The antiproliferative activity of A. unguis mycelial extract (AUME) was observed on different human cancer cell lines. PI live/dead assay further confirmed the cytotoxic potential of the mycelial extract. Furthermore, A. unguis mycelial extract caused mitochondrial membrane aberration and generated ROS production as well indicating its potential to induce cell death by apoptosis. The metabolic profiling of the mycelial extract using GC-MS and LC-MS/MS revealed the presence of fatty acids, a benzoquinolinone derivative, imidazolidinedione derivative, diethyl phthalate and phthalate acid ester, a difuraxanthone, two prenylxanthone analogues and a phthalide derivative and some unknown metabolites. Presence of 4-(4-Hydroxy-3,5-dimethoxy-phenyl)-3,4-dihydro-1H-benzo[h]quinolin-2-one, 1-hydroxy-3,5-dimethoxy-2-prenylxanthone, 1,6-dihydroxy-3-methoxy-2-prenylxanthone and 3-butylidene-7-hydroxyphthalide in AUME could be correlated to the notable cytotoxicity exhibited by the endophyte. The additional presence of many unidentified compounds heightened the prospects of finding some novel bioactive metabolites. Our results indicated that secondary metabolites produced by A. unguis AG 1.1 (G) have therapeutic potential as anticancer agents.
Highlights
Cancer is the major cause of morbidity and mortality worldwide
We reported that Aspergillus species, the predominantly present endophytes in marine macroalgae isolated from the Konkan coast are producing secondary metabolites with potential antibacterial, antioxidant and cytotoxic activities
We investigated whether the cytotoxic secondary metabolites produced by the potential isolate, A. unguis AG 1.1 (G) were mycelial bound or cell-free
Summary
Cancer is the major cause of morbidity and mortality worldwide. Global statistics estimated the death of 9.6 million people due to cancer in 2018 (Bray et al, 2018). Natural products derived from plants, marine organisms and microorganism contribute to more than 60% of the currently used anticancer agents. The bioactive metabolites such as alkaloids, terpenoids, flavonoids, sterols and polysaccharide from natural sources are widely reported for their anticancer activity (Seelinger et al, 2012; Rayan et al, 2017). Endophytes are the promising tools for red biotechnology as they are the rich source of bioactive compounds of therapeutic value. Some of these compounds are identical natural products synthesized by the associated host plant. Secondary metabolites serve complex roles; some are involved in crosskingdom talk, others are in conjunction with fungal life cycle such as sporulation, while some suppress the host immune system (Pusztahelyi et al, 2015; Zeilinger et al, 2016)
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