Growing evidence indicates that the endophytic fungus Aspergillus is one of rich sources of natural products with a broad spectrum of biological activities. In our effort to isolate and to identify biologically active metabolites from naturally occurring sources, two endophytic fungi have been isolated from the tissues of Ipomoea carnea. Among the two isolates, one fungus displayed pronounced antimicrobial activity, against pathogenic microbes include Gram+ve bacteria; Staphylococcus aureus and Bacillus subtilis, Gram–ve bacteria; Pseudomonas aeruginosa and Escherichia coli and Yeasts; Candida albicans with inhibition zone range from 16-19 mm. The most potent isolate has been identified genetically by sequencing of 18S rRNA gene as Aspergillus terreus AH1. Bio guided-fractionation and isolation of Aspergillus terreus AH1 extract led to identification of five compounds namely; (+)-asterrelenin (1), (±)-periplanamide B (2), butyrolactone I (3), pyranterrone D (4), and Arenarin A (5). The identified compounds showed a strong antibiofilm activity against human pathogenic bacteria such as Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli and Bacillus subtilis. Moreover, the compound ((±)-periplanamide B) has strong activity against some carcinoma cells such as HCT116, HePG 2 and MCF7