Abstract

As a representative bioactive component in Brazil green propolis, Artepillin C (ArtC; 3, 5-diprenyl-4-hydroxycinnamic acid) has been reported a wide variety of physiological activities including anti-tumor, anti-inflammatory, and antimicrobial activity etc. However, it seems incompatible that ArtC in vivo was characterized as low absorption efficiency and low bioavailability. In order to obtain the elucidation, we further investigated the physicochemical basis of ArtC interacting with human serum albumin (HSA) in vitro. We found a unique dynamic mode interaction between ArtC and HSA, which is completely different from other reported propolis bioactive components. Thermodynamic analysis showed that hydrophobic interactions and electrostatic forces are the main driving force. The competitive assay indicates that the binding site of ArtC with HSA is close to the Sudlow’s site I. The findings of this study reveal the unique physicochemical transport mechanism of ArtC in the human body, which helps to further understand the uniqueness of the representative functional components of Brazilian green propolis in the human body.

Highlights

  • As a representative bioactive component in Brazil green propolis, Artepillin C (ArtC; 3, 5-diprenyl4-hydroxycinnamic acid) has been reported a wide variety of physiological activities including antitumor, anti-inflammatory, and antimicrobial activity etc

  • The results showed that fluorescence quenching of human serum albumin (HSA) by ArtC was observed during the interaction process

  • As one of the most significant components in Brazilian green ­propolis[10], the binding interaction between ArtC and HSA is unique dynamic mode, which is different with other propolis components

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Summary

Introduction

As a representative bioactive component in Brazil green propolis, Artepillin C (ArtC; 3, 5-diprenyl4-hydroxycinnamic acid) has been reported a wide variety of physiological activities including antitumor, anti-inflammatory, and antimicrobial activity etc. We found a unique dynamic mode interaction between ArtC and HSA, which is completely different from other reported propolis bioactive components. The findings of this study reveal the unique physicochemical transport mechanism of ArtC in the human body, which helps to further understand the uniqueness of the representative functional components of Brazilian green propolis in the human body. Brazilian green propolis contains a variety of chemical components and is reported to have multiple biomedical activities, such as antibacterial activities, antioxidant, antiulcer, antiinflammatory, antigenotoxicity and a­ ntimutagenicity[5,6,7,8,9] etc. The potential binding site of bioactive compound in HSA is necessary to be interpreted by competitive experiments

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