Apigenin (4′,5,7-trihydroxyflavone) (Api) is an important component of the human diet, being distributed in a wide number of fruits, vegetables and herbs with the most important sources being represented by chamomile, celery, celeriac and parsley. This study was designed for a comprehensive evaluation of Api as an antiproliferative, proapoptotic, antiangiogenic and immunomodulatory phytocompound. In the set experimental conditions, Api presents antiproliferative activity against the A375 human melanoma cell line, a G2/M arrest of the cell cycle and cytotoxic events as revealed by the lactate dehydrogenase release. Caspase 3 activity was inversely proportional to the Api tested doses, namely 30 μM and 60 μM. Phenomena of early apoptosis, late apoptosis and necrosis following incubation with Api were detected by Annexin V-PI double staining. The flavone interfered with the mitochondrial respiration by modulating both glycolytic and mitochondrial pathways for ATP production. The metabolic activity of human dendritic cells (DCs) under LPS-activation was clearly attenuated by stimulation with high concentrations of Api. Il-6 and IL-10 secretion was almost completely blocked while TNF alpha secretion was reduced by about 60%. Api elicited antiangiogenic properties in a dose-dependent manner. Both concentrations of Api influenced tumour cell growth and migration, inducing a limited tumour area inside the application ring, associated with a low number of capillaries.
Melissa officinalis L. has attracted an increased interest in recent years due to its multiple pharmacological effects. This study aimed to compare two M. officinalis ethanolic extracts, obtained from leaves and stems, with regard to their antioxidant activity, total phenolic content, and cytotoxic effects. M. officinalis ethanolic extracts showed a very good antioxidant activity in the DPPH test, correlated with the content in total phenols: higher in the case of M. officinalis from leaves extract (32.76 mg GAE/g) and lower for M. officinalis from stems extract (8.4 mg GAE/g). The lemon balm extracts exerted a cytotoxic effect on breast cancer cells (MDA-MB-231) even at low concentrations (100 μg/mL), whereas, in the case of healthy HaCat cells, M. officinalis leaves extract only displayed cytotoxicity at much higher concentrations (500 and 1000 μg/mL) and M. officinalis stems extracts were highly cytotoxic (starting at 100 μg/mL). In addition, the extracts exerted inhibitory effects on cell migration and proliferation. These results provide information that confirms the high potential of M. officinalis as a source of chemopreventive agents. Moreover, these data can be considered a solid background for further in vivo studies involving mice bearing breast tumors.
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