Exploring the therapeutic potential of Momordica charantia: Phytochemical characterization, nanoencapsulation, and antitumor applications
Antitumor potential, cytotoxicity, nanocapsules, phenolic compounds.
The search for antitumor agents of natural origin has driven the development of new therapeutic strategies, particularly when combined with nanotechnology, which can improve the stability, bioavailability, and delivery of bioactive compounds. In this study, hydroethanolic extracts from the leaves and fruits of Momordica charantia were characterized regarding their phytochemical profile and biological activities, subsequently nanoencapsulated in chitosan/tripolyphosphate (CS/TPP) systems, and evaluated for their physicochemical properties and cytotoxic potential. Extract yield, total phenolic content (TPC), total flavonoid content (TFC), antioxidant capacity through DPPH and total antioxidant capacity (TAC) assays, α-amylase inhibitory activity, and toxicity against Artemia salina were determined. The nanoformulations were characterized according to encapsulation efficiency, morphology by scanning electron microscopy (SEM), and biochemical composition by Raman spectroscopy, followed by evaluation of cell viability through the MTT assay in HeLa and RAW264.7 cells. The leaf extract exhibited higher levels of phenolic compounds (1.18 ± 0.05 mg GAE/g) and flavonoids (56.73 ± 2.78 mg QE/g), as well as greater total antioxidant capacity (30.44 ± 0.51 mg AAE/g), whereas both extracts showed similar antioxidant activity in the DPPH assay (IC₅₀ = 0.207 mg/mL). The leaf extract also demonstrated greater α-amylase inhibitory activity (258.42% at a concentration of 50 mg/mL), while the Artemia salina assay revealed high toxicity for both extracts, with an immediate effect observed for the leaf extract and a concentration-dependent effect for the fruit extract. The nanocapsules exhibited high encapsulation efficiency (84.53% for the fruit extract and 81.00% for the leaf extract), predominantly spherical morphology, particle size ranging from 140 to 225 nm, and preservation of the main spectral signatures of metabolites after nanoencapsulation. Cytotoxic activity was concentration-dependent in both cell lines. In HeLa cells, nanocapsules containing the fruit extract showed the highest cytotoxic activity (IC₅₀ = 44.90 mg/mL), followed by formulations containing the leaf extract (IC₅₀ = 54.30 mg/mL) and blank chitosan nanocapsules (IC₅₀ = 77.88 mg/mL). In RAW264.7 cells, the formulation containing the leaf extract exhibited the highest cytotoxic activity (IC₅₀ = 23.96 mg/mL), followed by blank chitosan nanocapsules (IC₅₀ = 36.00 mg/mL) and fruit extract formulation (IC₅₀ = 59.06 mg/mL). Overall, these results demonstrate that M. charantia represents a promising source of bioactive compounds and that chitosan-based nanoencapsulation preserves these metabolites, providing suitable physicochemical characteristics and enhancing its potential application as a strategy for the development of antitumor therapies.