Background: Cancer is a dangerous threat that creates extremely high rates of death and morbidity in various regions of the world. Finding suitable therapeutics to improve cancer therapy while avoiding side effects is critical. The most appropriate innovative therapeutics, which combine natural ingredients and nanomaterials, can improve the biological activity of cancer chemotherapeutics. Methods: Phenolic profiling using high-resolution mass spectrometry and the synthesis of zinc oxide nanoparticles was achieved through the reaction of zinc acetate with Euphorbia retusa extract. The characterization of ZnONPs was performed by UV, IR, Zeta potential, XRD, SEM, and TEM. The cytotoxic activity of the ZnONPs was evaluated using a SRB assay against lung, liver, and breast cancer cell lines. Moreover, the mechanism of cytotoxic activity was evaluated in the form of caspase-8 promoters and anti-inflammatory mechanisms using the Western blot method. Results: The high-resolution LC/MS/MS of the E. retusa led to the identification of 22 compounds in the plant for the first time. The Er-ZnONPs had hexagonal shapes, were approximately 100 nm in size, and consisted of aggregated particles of about 10 nm. The E. retusa ZnONPs exhibited cytotoxic activity against HA-549 (IC₅₀ = 22.3 µg/mL), HepG2 (IC₅₀ = 25.6), Huh-7 (IC₅₀ = 25.7), MCF-7 (IC₅₀ = 37.7), and MDA-MB-231 (IC₅₀ = 37). Conclusions: E. retusa are rich in phenolics that are capable of synthesizing ZnONPs, which possess cytotoxic activity, via caspase-8 promotion and anti-inflammatory mechanisms.

Endophytes are considered as a rich source of bioactive natural products. Many plants have not been investigated for their endophytic content yet, such as the medicinal plant Ficus carica. Recent studies confirmed antimicrobial and anticancer activities for the plant extract. To find out if its endophytes contribute to its reported activities, the bioactive endophyte Aspergillus neoniger was selected for investigation of its metabolites since it exerted antimicrobial and anticancer activities in preliminary screening assays. The fungal extract was subjected to bioactivity guided chromatographic fractionation for isolation of its bioactive metabolites. This resulted in the identification of four aurasperones (asperpyrone D, aurasperone D, dianhydroaurasperone C, aurasperone A) through spectroscopic analysis. Aurasperone D and asperpyrone D were found to be cytotoxic against human cervical cancer cells (50 % cytotoxic concentration=4.4 μg ml-1 and 3.0 μg ml-1 respectively). Aurasperone D exerted strong antiproliferative effect against human immortal erythroleukaemia cells 562 and human umbilical vein endothelial cells (concentration at which 50 % growth inhibition achieved is 5.3 and 4.7 μg ml-1) as well as asperpyrone D (concentration at which 50 % growth inhibition achieved is 4.9 and 5.4 μg ml-1). Dianhydroaurasperone C and aurasperone A, on the contrary, showed weak cytotoxic and antiproliferative effects. All compounds were tested for antimicrobial activity against several test strains including the plant pathogen Fusarium oxysporum. Results revealed that aurasperone D and asperpyrone D to be most active which suggests potential protective role of this endophyte on its host plant. These results suggest possible partial contribution of Aspergillus neoniger to the reported activity of the host plant

Background: Several plants have not been investigated for their endophytes, such as the medicinal plant Ficus carica for which anticancer activity has been confirmed. The endophyte Aspergillus neoniger was selected for investigation of its metabolites since it exerted anticancer activities in preliminary screening assays. Results: Bioactivity-guided chromatographic fractionation was performed on the endophytic extract and resulted in the identification of asperazine and asperazine A through spectroscopic analysis. Moderate cytotoxicity against HeLa cell lines (CC₅₀ = 18.4 µg mL⁻¹) and moderate antiproliferative effects against HUVEC and K-562 cell lines (GI₅₀ = 31.5 and 24.8 µg mL⁻¹, respectively) were observed for asperazine. Asperazine A on the other hand showed weak cytotoxic activity against HeLa cell lines (CC₅₀ = 34.6 µg mL⁻¹) as well as weak cytostatic activities against HUVEC and K-562 cell lines (GI₅₀ = 40.7 and 50.2 µg mL⁻¹, respectively) while no antimicrobial activity was detected for both compounds. Conclusions: These results suggest contribution of A. neoniger to the reported anticancer activity of the host plant and provides a new source of anticancer metabolites with therapeutic potential.

Background: The medicinal plant Ficus carica L., inhabiting southwest regions of Asia, is known for its wide ethnopharmacological applications. In traditional medicine, it has been applied as a treatment of respiratory, gastrointestinal and cardiovascular disorders, among others. Recent studies confirmed antimicrobial and anticancer activities for the plant extract. To find out whether endophytes of F. carica contribute to its biological activities, endophytes of the aerial parts of the plant were isolated and examined for anticancer and antimicrobial effects. Results: The isolated species were identified as Chaetomium globosum, Penicillium oxalicum, Alternaria alternata, Fusarium proliferatum and Aspergillus neoniger. An anticancer assay was carried out on the extracts of fungal strains against human umbilical vein endothelial cells (HUVEC), human immortalized myelogenous leukemia cell line (K-562) and human immortal cervical cancer cell line (HeLa). Results revealed antiproliferative effects for all endophytic strains against HUVEC and K-562 with GI₅₀ values ranging from 4.75 to 13.75 µg mL⁻¹ as well as cytotoxicity against HeLa with CC₅₀ ranging from 8.25 to 18.75 µg mL⁻¹. The antimicrobial activity of the extracts was tested against several test strains in agar diffusion assay, and MIC values were determined by the broth microdilution method. All strain extracts exerted antibacterial and antifungal activities with highest antifungal effect observed for A. neoniger extract (MIC = 3.75 µg mL⁻¹). Conclusions: These results support the assumption that endophytes of F. carica contribute to the plant’s reported antimicrobial and anticancer activities and its corresponding applications in traditional medicine.