The aim of this study is to evaluate the therapeutic potential and general toxicity of anthraquinones from six strains of either T. harzianum or T. virens.  For initial assessment measures, biocontrol activities against major phytopathogens Rhizoctonia solani and Botrytis cinerea were tested and screened. Results show that emodin and ω-hydroxypachybasin from T. harzianum R16 showed significant antifungal activities. Since emodin is well studied in the literature but not ωHP, we chose ωHP for further investigation of its therapeutic potential and general toxicity using human lung cancer cell line A549 and mice, respectively. The IC₅₀ of ωHP against A549 was 11.95 μg mL^-1. The elucidated mechanism demonstrated that ωHP inhibited the growth and propagation of A549 by inducing G2/M arrest and apoptosis. The toxicity data showed that with either 5 or 20 mg Kg^-1 ωHP i.p. injection, mice behavioral responses such as motor coordination, spontaneous locomotor activity, and nociceptive pain were not influenced. In long-term effect (daily injection for 14 days), the physiological, hematological, liver, and kidney functions were not altered either. Taken together, ωHP exhibited prominent anticancer potential and no significant general toxicity was observed in ωHP-treated adult male mice, indicating that ωHP could be an ideal therapeutic agent and/or be safely used as a bioagricultural agent someday.