Simulated gastrointestinal digestion/Caco-2 cell transport: Effects on biological activities and toxicity of a Brazilian propolis.

The objective was to assess the effect of gastrointestinal digestion/Caco-2 cell transport on biological activities and toxicity of the ethanolic extract of organic propolis from southern Brazil (EEOP1). As principal results, the EEOP1 deactivated the ROO ^• , HOCl and O ₂ ^•- reactive oxygen species, attenuated NF-κB transcription factor activation, and decreased the release of TNF-α and IL-6 in macrophages after Caco-2 cell transport, while CXCL2/MIP-2 release was reduced after gastrointestinal digestion. Furthermore, the phytochemical profile monitored by HPLC-ESI-QTOF-MS changed, especially for lignans, lignan-precursors and phenolic acids. Conversely, the antimicrobial activity was observed only in the non-digested EEOP1. The EEOP1 lethal dose to kill 50 % of the Galleria mellonella larvae was 1.1 g/kg, and its digested fraction had no toxic effect. Hence, there is indication that some phytochemicals present in the EEOP1 are resistant to the gastrointestinal tract and maintain their biological activities, as expected for a functional food ingredient.
Competing Interests: Declaration of Competing Interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Ana Sofia Martelli Chaib Saliba reports financial support was provided by Coordenação de Aperfeiçoamento de Pessoal de Nível Superior. Severino Matias de Alencar reports financial support was provided by Conselho Nacional de Desenvolvimento Científico e Tecnológico. Severino Matias de Alencar reports financial support was provided by Fundação de Amparo à Pesquisa do Estado de São Paulo. The remaining authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
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