Keele Research Repository

Ovarian cancer is the second leading cause of death among women in the gynaecological category of cancers. The current post surgery treatment which involves the use of platinum-based therapy with its attendant adverse drug-resistance often results in the return of the cancer. This study explored the role of phytochemicals as the major source of new drugs by evaluating the anti-ovarian cancer activities of three selected Nigerian medicinal plants (Acalypha wilkesiana, Margaritaria discoidea and Rutidea parviflora). Using a bioassay-guided approach, an investigation of the cell growth inhibition of the extracts/fractions of these plants on four human ovarian cancer cell lines, A2780, OVCAR 4, OVCAR 8, and CIS-A2780 showed that these plant extracts had promising anti-ovarian cancer activities. The bioactive compounds of the plants were isolated by HPLC, identified by mass spectrometry/NMR spectroscopy and investigated for cytotoxicity. Gallic acid (IC50 range of 6.2 ± 0.3–26.9 ± 4.1 μM) was the active compound in A. wilkesiana. The significantly bioactive compounds of M. discoidea were securinine (IC50 range of 2.7 ± 0.7–8.7 ± 0. μM), betulinic acid (IC50 of 16.0 ± 1.9 μM), and gallic acid. While palmatine (IC50 range of 5.5 ± 0.9–7.9 ± 0.5 μM) was the major active compound in R. parviflora.Palmatine and securinine showed induction of apoptosis via increased caspase 3/7 activity. Palmatine demonstrated PAPR cleavage by western blot analysis. These studies have provided scientific evidence for the potential treatment of ovarian cancer with these traditional medicinal plants and hit compounds for future optimization towards clinical trials.