Endophytes are prolific producers of privileged secondary metabolites with diverse therapeutic potential, although their anticancer and antimicrobial potential still have a room for further investigation. Herein, seven known secondary metabolites namely, arugosin C (1), ergosterol (2), iso-emericellin (3), sterigmatocystin (4), dihydrosterigmatocystin (5), versicolorin B (6), and diorcinol (7) were isolated from the rice culture of retrieved from (L.) Juss. ex Kunth leaves. Their anticancer and antimicrobial activities were evaluated in MTT and agar well diffusion assays, respectively. The cytotoxicity results showed that metabolite displayed the best viability inhibition on the MCF-7 breast cancer cells with IC = 225.21 µM, while on the HepG2 hepatocellular carcinoma cells with IC = 161.81 µM. demonstrated a 60% apoptotic mode of cell death which is virtually correlated to its high docking affinity to Hsp90 ATP binding cleft (binding score -8.4 Kcal/mol). On the other side, metabolites and displayed promising antimicrobial activity especially on with MIC = 125 μg/ml. The observed effect may be likely related to their excellent inhibition of the bacterial DNA-gyrase kinase domain (binding score -10.28 Kcal/mol). To the best of our knowledge, this study is the first to report the promising cytotoxic and antibacterial activities of metabolites 3, 4, and 5 which needs further investigation and renovation to therapeutic leads.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8548774PMC
http://dx.doi.org/10.3389/fchem.2021.760083DOI Listing

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