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

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.

Berries polyphenols: Nano-delivery systems to improve their potential in cancer therapy

“…There is a wide variety of materials that can be used as nano-carriers, such as micelles, biodegradable polymers, drug-polymer polysaccharide conjugates, liposomes/vesicles, cubosomes, organometallic compounds, hydrogels and solid lipid NPs, among others [3,14,[17][18][19]. Nano-delivery systems must be innocuous, stable, non-immunogenic, non-thrombogenic, non-inflammatory, and biodegradable [16,19].…”

“…Low bioavailability has been related to poor absorption throughout the gastrointestinal tract (GT) (in their native form) and extensive metabolization by phase I/II detoxification enzymes and colonic microbiota, which lead to a wide range of new chemical structures before reaching their site of action [2,7]. In order to solve these problems and improve stability and/or bioavailability of berries phenolic compounds, nano-delivery systems have been proposed as effective tools that permit their effective transport in the tumor tissue [7,11,13,14].…”

Microbiological, antioxidant and lipoxygenase-1 inhibitory activities of fruit extracts of chosen Rosaceae family species

“…The method of lipid peroxidation assessment was described by Strugała et al 10 The lipid peroxidation level in the liposomes was measured as the concentration of a thiobarbituric acid reactive substance (TBARS). The antioxidant activity of the extracts tested was expressed with the parameters: IC 50 PC (Inhibition Concentration) [mg/mL] and TEAA (Trolox equivalent antioxidant activity expressed in micrograms of Trolox per gram of dry matter of the extract -μM TE/g d.m.).…”

“…The free-radical scavenging activity of 1,1diphenyl-2-picrylhydrazyl (DPPH • ) was measured according to the method described by us in an earlier work. 10 The free-radical scavenging activity of cation-radicals (2,2'-azino-bis(3ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS +• )) was assessed according to the method described by Re et al 11 The results are expressed as μM TE/g d.m. by reference to a standard curve.…”

“…The E. coli stock culture was kept in the refrigerator (−40°C) on a nutrient agar plate. Before each experiment, the strain was first allowed to reach room temperature, transferred to tryptic soy agar, and incubated at 37°C for 18 h. Then, bacterial cells were incubated in tryptic soy broth with varying concentrations (1,5,10,20,30,40,50,60,65,70,75, and 80 mg/mL) of ME or WE of the plants tested for 24 h at 37°C. Control cultures were incubated in the absence of plant extracts.…”