PUB - Publikationen an der Universität Bielefeld

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 ofAspergillus sp.retrieved fromTecoma stans(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 metabolite3displayed the best viability inhibition on the MCF-7 breast cancer cells with IC₅₀= 225.21 µM, while5on the HepG2 hepatocellular carcinoma cells with IC₅₀= 161.81 µM.5demonstrated 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, metabolites4and5displayed promising antimicrobial activity especially onPseudomonas aeruginosawith MIC = 125 μg/ml. The observed effect may be likely related to their excellentin silicoinhibition 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.