Abstract
Cinnamic acid (CA) and ferulic acid (FA) are naturally occurring phenolic acids claimed to exert beneficial effects against disorders related to oxidative stress, including cancer. One such malignancy that still remains a therapeutic challenge mainly due to its heterogeneity and inaccessibility to therapeutic agents is Glioblastoma multiforme (GBM). Here, the influence of CA and FA on the surface charge density of human GBM cell line LN-229 was studied using the electrophoretic light scattering technique. Also, the cytotoxicity of both phenolic acids was determined by metabolic activity-assessing tetrazolium test (MTT) analysis after exposure to CA and FA for 24 h and 48 h. Results showed that both compounds reduced cell viability of LN-229 cells, with more pronounced effect evoked by CA as reflected in IC50 values. Further analyses demonstrated that, after treatment with both phenolic acids, the negative charge of membranes decreased at high pH values and the positive charge of the membranes increased at low pH values compared to the data obtained for untreated cells. Afterward, a four-equilibrium model was applied to estimate the total surface concentrations of both acidic and basic functional groups and their association constants with solution ions in order to calculate theoretical values of membrane surface charge densities. Then, the theoretical data were compared to the experimental data in order to verify the mathematical model. As such, our results indicate that application of electrochemical methods to determine specific drug–membrane interactions might be crucial for predicting their pharmacological activity and bioavailability.
Highlights
Occurring phenolic acids and their analogues present potentially beneficial effects to human health in terms of numerous oxidative stress-related diseases including cancer
Compounds with a comparable structure frequently interact with biological membranes in a different way, owing to the complex correlation between permeability and liposolubility, which can be further modified by pH changes [8]
The major aim of the present paper is to investigate the effect of cinnamic acid (CA) and its hydroxy derivative—ferulic acid (FA)—on the surface charge density of human glioblastoma multiforme (GBM) cell membranes using the electrophoretic light scattering (ELS) technique
Summary
Occurring phenolic acids and their analogues present potentially beneficial effects to human health in terms of numerous oxidative stress-related diseases including cancer. Preclinical investigations have revealed that using a combination of phenolic acids with traditional chemoradiotherapy or other polyphenols may be potentially efficient in reducing the spread of cancer [1]. It has been demonstrated that their biological characteristics such as transport, distribution, selectivity, activity, and toxicity is at least partially determined by their interaction with biological membranes [6]. These compounds are sometimes able to interact with/pass through the biological membranes [7], but such ability depends largely on substitutes contained in their main structure. Compounds with a comparable structure frequently interact with biological membranes in a different way, owing to the complex correlation (which can be modified by pH changes) between permeability and liposolubility, which can be further modified by pH changes [8]
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