Bioactivity-guided evaluation of F7 fraction derived from Acalypha cuspidata on ovarian cancer models in vitro and in vivo

Based on previous research, this study aimed to perform a bioactivity-guided evaluation of F7 fraction obtained from an ethyl acetate extract of Acalypha cuspidata (Jacq.) and to determine its anticancer activity on the SKOV-3 ovarian cancer cell line through in vitro and in vivo assays. Thus, ethyl acetate extract from A. cuspidata (9.8 g) was fractionated into 11 fractions (F1–F11) by open column chromatography, and chromatography-obtained fractions were evaluated using the WST-1 assay. Transmission electron microscopy, flow cytometry, Annexin V binding assay, and experimental model of the Nu / Nu mouse were carried out to analyze fraction 7 (F7) anti-tumor activity. The results showed that among the eleven fractions obtained, only F4 and F7 fractions showed lower cytotoxicity against SKOV-3 ovarian cancer cells and the best ability to selectively target cancer cells without affecting BEAS-2B non-cancer cell line. Toxicity data in primary culture of rat hepatocytes indicated that F7 fraction is less toxic than F4, hence, F7 was selected for further studies. F7 fraction (half maximal inhibitory concentration, IC 50 , 28 μg / mL)-treated SKOV-3 cells had morphological hallmarks of apoptosis, such as chromatin condensation, reduction in cellular size, phosphatidylserine externalization, and drastic damage to the mitochondria. In a xenograft mouse model of ovarian cancer, treatment with F7 fraction (40 mg/kg) was associated with a marked reduction in tumor growth compared with the vehicle-treated group, supporting the potential antitumor activity of this bioactive fraction. F7 fraction derived from A. cuspidata has cytotoxic and antitumor activity against ovarian cancer models. Studies are required to characterize the chemical composition of F7 fraction, elucidate the underlying molecular mechanisms, and evaluate safety and pharmacological parameters.