A Review and Technological Survey of Antioxidant and Anti-inflammatory Properties of Naringenin and β-Cyclodextrin Complexes in Inflammation and Diabetic Cardiomyopathy
Ana Victoria Alves Peres
LAFMOL–Laboratory of Functional and Molecular Studies in Physiopharmacology, Department of Biophysics and Physiology, Federal University of Piauí, Teresina 64049-550, Brazil.
Higo José Neri da Silva
LAFMOL–Laboratory of Functional and Molecular Studies in Physiopharmacology, Department of Biophysics and Physiology, Federal University of Piauí, Teresina 64049-550, Brazil.
Natália de Assis Rocha
LAFMOL–Laboratory of Functional and Molecular Studies in Physiopharmacology, Department of Biophysics and Physiology, Federal University of Piauí, Teresina 64049-550, Brazil.
Boris Timah Acha
LAFMOL–Laboratory of Functional and Molecular Studies in Physiopharmacology, Department of Biophysics and Physiology, Federal University of Piauí, Teresina 64049-550, Brazil.
Clailson da Silva Pinheiro
LAFMOL–Laboratory of Functional and Molecular Studies in Physiopharmacology, Department of Biophysics and Physiology, Federal University of Piauí, Teresina 64049-550, Brazil.
José Guilherme Veras de Assunção
LAFMOL–Laboratory of Functional and Molecular Studies in Physiopharmacology, Department of Biophysics and Physiology, Federal University of Piauí, Teresina 64049-550, Brazil.
Leonardo da Rocha Sousa
LAFMOL–Laboratory of Functional and Molecular Studies in Physiopharmacology, Department of Biophysics and Physiology, Federal University of Piauí, Teresina 64049-550, Brazil.
Daniel Dias Rufino Arcanjo *
LAFMOL–Laboratory of Functional and Molecular Studies in Physiopharmacology, Department of Biophysics and Physiology, Federal University of Piauí, Teresina 64049-550, Brazil.
*Author to whom correspondence should be addressed.
Abstract
Inflammation is a rapid and self-limiting biological response to tissue injury, infection, or chemical stimuli, mediated by signalling pathways such as toll-like receptor 4 (TLR4) and nuclear factor kappa B (NF-κB). Dysregulation of these pathways promotes excessive production of nitric oxide, cytokines, and reactive oxygen species, establishing a feedback loop that contributes to oxidative stress and is implicated in chronic conditions, including diabetes and hypertension. Given the limitations and adverse effects of conventional therapies, natural compounds have gained attention as alternative pharmacological agents. Among these, naringenin and its glycosylated form, naringenin-7-O-β-D-glucoside, exhibit notable antioxidant and anti-inflammatory properties; however, their clinical application is limited by low bioavailability. Complexation with β-cyclodextrin has emerged as a promising strategy to enhance their physicochemical and pharmacokinetic profiles. This study aimed to conduct a comprehensive review and technological survey of the therapeutic applications of naringenin and its β-cyclodextrin complexes in inflammation and diabetic cardiomyopathy. A systematic search was performed in the Virtual Health Library, PubMed, ScienceDirect, and Web of Science, as well as patent databases including EPO, INPI, and WIPO, using predefined descriptors. After applying inclusion and exclusion criteria, 31 articles and 12 patents were selected. The studies consistently demonstrated that naringenin modulates NF-κB, MAPK, PI3K/Akt, and oxidative stress pathways, reducing inflammatory cytokine production and improving cardiometabolic outcomes in preclinical models. β-cyclodextrin complexation significantly enhanced solubility, bioavailability, and anti-inflammatory efficacy. Patent analysis revealed limited technological innovation, particularly regarding glycosylated derivatives such as naringenin-7-O-glucoside. The findings indicate that naringenin demonstrates significant therapeutic potential; however, studies involving its glycosylated form complexed with β-cyclodextrin remain scarce. These results highlight a critical gap and reinforce the need for further investigation into advanced delivery systems to improve efficacy in cardiometabolic and inflammatory disorders.
Keywords: Naringenin-7-O-glucoside, flavonoids, oxidative stress, natural products, patent analysis, cyclodextrin complex