A Comprehensive Study on the Biological Activity of Elderberry Extract and Cyanidin 3-O-Glucoside and Their Interactions with Membranes and Human Serum Albumin.

Paulina Strugała,Sabrina Loi,Piotr Kuropka,Barbara Bażanów,Aleksandra Włoch,Alicja Kucharska,Janina Gabrielska

doi:10.3390/molecules23102566

Abstract

In our research we used the extract from dietary supplement of elderberry (EE) and its dominant anthocyanin—cyanidin 3-O-glucoside (Cy 3-gluc). By interacting with a model membrane that reflects the main lipid composition of tumor membranes, the extract components, including Cy 3-gluc, caused an increase in packing order, mainly in the hydrophilic region of the membrane. It can thus be stated that EE caused a rigidifying effect, which is fundamental for understanding its anticancer and antioxidant activity. This study represents the first attempt to unravel the mechanism of interaction of elderberry extract with membranes. The results of the interaction with human serum albumin (HSA) proved that the studied substance quenches the fluorescence of HSA through a static mechanism in which the main interaction forces are Van der Waals and hydrogen bonding. The antioxidant activity of EE and Cy 3-gluc on liposomal membranes, antiradical properties and ability to inhibited the activity of the enzymes cyclooxygenase-1 and cyclooxygenase-2 were also demonstrated. Moreover, the anticancer activity of EE and Cy 3-gluc on human breast adenocarcinoma cell line were investigated. In addition, EE also exhibited the ability to form lipid aggregates in the form of liposomal capsules that can be applied as carriers of active biological substances, and the highest efficacy of EE encapsulation was obtained for multilayered liposome formulations.

Highlights

IntroductionIts nutritional and therapeutic values are mainly due to the presence of polyphenol compounds, especially a subgroup, the anthocyanins
Elderberry has been used in folk medicine as analgesic, antivirus, anti-inflammatory and heart disorders, haemostatic, antitussive, antiparasitic and to soothe burns [1] to treat various illnesses such as stomach ache, sinus congestion, constipation, diarrhea, sore throat, common cold, and rheumatism [2], and to prevent or delay the onset of chronic age-related diseases [3,4].Its nutritional and therapeutic values are mainly due to the presence of polyphenol compounds, especially a subgroup, the anthocyanins
Where F0 and F refer to fluorescence intensities of human serum albumin (HSA) prior to and after addition of the quencher where F0 and F refer to fluorescence intensities of HSA prior to and after addition of the quencher (EE), (EE), Kq is a bimolecular quenching constant, τ0 is the lifetime of fluorophore in the absence of

Summary

Introduction

Its nutritional and therapeutic values are mainly due to the presence of polyphenol compounds, especially a subgroup, the anthocyanins. In vitro data on the antioxidative, antiviral and possible anti-inflammatory, antibacterial and antiproliferative, effects are very promising, there are insufficient clinical data and further studies are required [5]. The compounds have met with increasing attention due to a strong body of evidence that supports their bioactivities. In spite of the large body of studies on the biological activity of flavonoids, including anthocyanins, the mechanism of their activity on the molecular level is not sufficiently known. To a large extent such a mechanism depends on their ability to interact with the biological membrane, which is the first natural barrier on their way into the cell interior [6,7]

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