Studies evaluating the phytoconstituents and therapeutic potential of species belonging to Orobanche (Family Orobanchaceae) are rather limited. The present study was designed to evaluate the chemical composition, antioxidant, enzyme inhibition and cytotoxic properties of the aerial parts of Orobanche nana Noë ex Rchb. Extracts were prepared by sequential maceration in dichloromethane, ethyl acetate and ethanol and finally an aqueous extraction by infusion were performed. NMR and LC-DAD-MS analysis allowed the identification of different phytoconstituents including the characteristic compounds of Orobanche like verbascoside, poliumoside, orobanone and orobanchoside. The ethanol extract displayed the highest total phenolic (115.63 mg GAE/g) and flavonoids (16.53 mg RE/g) contents, antiradical (DPPH = 623.70 mg TE/g; ATBS = 843.50 mg TE/g) and ions reducing (Cu++ = 725.39; Fe+++ = 617.70) properties while the aqueous extract exerted the best chelating power (19.54 mg EDTAE/g). It was determined that EtOH and Water extracts applied to HepG2 cells decreased the levels of anti-apoptotic proteins p-NFκB, BCL-2 and BCL-XL, while increasing the levels of apoptotic proteins BAX and p-53, thus inhibiting cell survival. In addition, Orobanche nana played an active role in the rearrangement of overexpress MMPs that cause disruption of ECM homeostasis. We employed Network Pharmacology to investigate the mechanisms through which Orobanche nana's compounds impact Kidney and Liver diseases. These findings suggested that O. nana could be a promising source of bioactive molecules with potential therapeutic applications.