Phytochemical Characterization and In Vitro Biological Activities of Macleania rupestris (Ericaceae): Insights into Nutraceutical Potential

TL;DR

This study explores the chemical makeup and health benefits of Macleania rupestris, a neotropical berry, finding it has potential for nutraceutical use due to its biocompatibility and antioxidant properties.

Contribution

The first comprehensive phytochemical and biological evaluation of Macleania rupestris, revealing its nutraceutical potential and biocompatibility.

Findings

M. rupestris contains anthocyanins, flavonols, and coumaroyl iridoids with antioxidant properties.

The extract showed low antiproliferative activity and high hemocompatibility in vitro.

Anti-inflammatory effects were observed, but no significant leishmanicidal activity was detected.

Abstract

The Ericaceae family encompasses several berries with recognized health-promoting properties; however, Macleania rupestris, a neotropical species endemic to the Andean region, remains poorly characterized. Background/Objectives: This study aimed to identify the chemical composition of M. rupestris ethanolic extracts and evaluate their biological activities, including antitumoral, hemolytic, anti-inflammatory, and leishmanicidal effects. Methods: The M. rupestris ethanolic extracts were obtained from lyophilized fruits and analyzed by HPLC-MS/MS for phytochemical profiling. Bioactivities were assessed in vitro using tumor and non-tumor cell lines (MTT assay), erythrocyte hemolysis assays, RAW 264.7 macrophage inflammation models, and Leishmania mexicana promastigotes. Results: The chemical analysis revealed anthocyanins (cyanidin-3-glucoside, malvidin-3-glucoside, petunidin-3-glucoside, delphinidin-3-arabinoside), flavonols (quercetin and myricetin derivatives), and coumaroyl iridoids. The extract showed modest antiproliferative activity (IC50 10.4–22.5 mg/mL) across tumor cell lines with low therapeutic indices, indicating limited selectivity. In contrast, hemolytic activity was negligible (<5% at all tested concentrations), suggesting high biocompatibility. Anti-inflammatory assays indicated a dose-dependent reduction in nitric oxide (NO) production, while no significant leishmanicidal activity was detected. Conclusions: This study provides the first comprehensive evaluation of the previously listed M. rupestris bioactivities. While its antitumoral effects appear limited, its strong hemocompatibility and presence of antioxidant metabolites highlight its potential for biomedical and nutraceutical applications where biocompatibility is critical. Further studies are needed to optimize bioactivity and explore potential synergistic effects.

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