Factors Influencing Glabridin Stability

Ao, Mingzhang; Shi, Yue; Cui, Yuming; Guo, Wentao; Wang, Jing; Yu, Liang

doi:10.1177/1934578x1000501214

Cited by 21 publications

(31 citation statements)

References 10 publications

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“…Ao et al [47] have evaluated various factors influencing Glab stability, such as temperature, pH, light exposure, and humidity. While Glab was found to be unstable under basic conditions (pH > 7), it remained stable at neutral pH.…”

Section: Phytochemical Characterization Of Glabridinmentioning

confidence: 99%

Phytochemistry and biological properties of glabridin

Simmler¹,

Pauli²,

Chen³

2013

Fitoterapia

215

150

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Glabridin, a prenylated isoflavonoid of G. glabra L. roots (European licorice, Fabaceae), has been associated with a wide range of biological properties such as antioxidant, anti-inflammatory, anti-atherogenic, regulation of energy metabolism, estrogenic, neuroprotective, anti-osteoporotic, skin-whitening. While glabridin is one of the most studied licorice flavonoids, a comprehensive literature survey linked to its numerous bioactivities is unavailable. The present review provides a comprehensive description of glabridin as a key chemical and biological marker of G. glabra, by covering both its phytochemical characterization and reported biological activities. Both glabridin and standardized licorice extracts have significant impact on food, dietary supplements (DSs) and cosmetic markets, as evidenced by the amount of available patents and scientific articles since 1976, when glabridin was first described. Nevertheless, a thorough literature survey also reveals that information about the isolation and chemical characterization of this important marker is scattered and less detailed than expected. Accordingly, the first part of this review gathers all analytical and spectroscopic data required for the comprehensive phytochemical characterization of glabridin. The four most frequently described and most relevant bioactivities of glabridin are its anti-inflammatory, anti-atherogenic, estrogenic-like effects, and its capacity to regulate energy metabolism. While all bioactivities reported for glabridin belong to a wide array of targets, its principal biological properties are likely interconnected. To this end, the current state of the literature suggests that the biological activity of glabridin mainly results from its capacity to down-regulate intracellular reactive oxygen species, bind to antioxidant effectors, and act on estrogen receptors, potentially as a plant-based Selective Estrogen Receptor Modulator (phytoSERM).

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Section: Phytochemical Characterization Of Glabridinmentioning

confidence: 99%

Phytochemistry and biological properties of glabridin

Simmler¹,

Pauli²,

Chen³

2013

Fitoterapia

215

150

View full text Add to dashboard Cite

show abstract

“…Glabridin itself has not been developed as a therapeutic drug because of several limitations, but its derivatives show potential. Glabridin has low physicochemical stability [ 13 ] and low bioavailability [ 14 ]; light, temperature, humidity, and pH all influence the stability of glabridin [ 13 ]. In addition, the extraction of glabridin from licorice is complicated and unlucrative because of glabridin’s low content and high decomposition rate in the preparation process [ 13 ].…”

Section: Introductionmentioning

confidence: 99%

“…Glabridin has low physicochemical stability [ 13 ] and low bioavailability [ 14 ]; light, temperature, humidity, and pH all influence the stability of glabridin [ 13 ]. In addition, the extraction of glabridin from licorice is complicated and unlucrative because of glabridin’s low content and high decomposition rate in the preparation process [ 13 ]. Other compounds isolated from licorice root with glabridin backbone—hispaglabridin A and B and 4′-O-methylglabridin—demonstrated comparable anti-oxidative properties [ 7 ], and 3″,4″-dihydro-glabridin showed superior stability and tyrosinase inhibitory effects [ 15 ].…”

Section: Introductionmentioning

confidence: 99%

Discovery and preclinical efficacy of HSG4112, a synthetic structural analog of glabridin, for the treatment of obesity

Choi

Kang

et al. 2020

Int J Obes

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Background HSG4112 is a clinical-stage drug candidate for the treatment of obesity. Here, we report its discovery and preclinical efficacy. Methods In high-fat diet (HFD)-induced obese male C57BL/6J mice, we tested the weight loss effect of synthetic compounds derived from a structure–activity relationship (SAR) study of glabridin, a natural compound known to reduce body weight and influence energy homeostasis. After selecting HSG4112 as our optimized compound from this discovery method, we characterized its pharmacological effects on parameters related to obesity through in vivo metabolic and biochemical measurements, histology and gene expression analysis, and indirect calorimetry. Results Through the SAR study, we identified four novel components of glabridin pertinent for its anti-obesity activity, and found that HSG4112, an optimized structural analog of glabridin, markedly supersedes glabridin in weight reduction efficacy and chemical stability. Six-week administration of HSG4112 to HFD-induced obese mice led to dose-dependent normalization of obesity-related parameters, including body weight, muscle and adipose tissue weight, adipocyte size, and serum leptin/insulin/glucose levels. The weight reduction induced by HSG4112 was partially mediated by decreased food intake and mainly mediated by increased energy expenditure, with no change in physical activity. Accordingly, the pattern of transcriptional changes was aligned with increased energy expenditure in the liver and muscles. Following significant body weight reduction, robust amelioration of histopathology and blood markers of fatty liver were also observed. Conclusions Our study demonstrates the key chemical components of glabridin pertinent to its weight loss effects and suggests HSG4112 as a promising novel drug candidate for the pharmacological treatment of obesity.

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“…However, the practical application of glabridin is extremely limited owing to its poor aqueous solubility and, thus, poor bioavailability, as well as its unpredictable stability. 10…”

Section: Introductionmentioning

confidence: 99%

β-Lactoglobulin as a Nanotransporter for Glabridin: Exploring the Binding Properties and Bioactivity Influences

et al. 2018

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Based on the fact that β-lactoglobulin (β-lg) can solubilize readily in water and bind many small hydrophobic molecules, a novel nanocomplexed glabridin with β-lg was developed by an antisolvent precipitation method. After binding to β-lg, the solubility of glabridin in aqueous solution was enhanced 21 times. Fluorescence spectroscopy of β-lg revealed that the interaction of glabridin with β-lg made the environment of Trp and Tyr residues on β-lg more hydrophilic. The morphology and crystal form of the nanocomplexed glabridin with β-lg was characterized and the changes in β-lg conformation was also been investigated. In combination with molecular docking modeling, the results revealed that glabridin was bound to β-lg by hydrophobic forces and hydrogen-bond interactions. Furthermore, the nanocomplexed glabridin with β-lg had a better 2,2-diphenyl-1-picrylhydrazyl radical-scavenging capacity and 2,2′-azino-bis-3-ethylbenzthiazoline-6-sulfonic acid radical-scavenging capacity compared to free glabridin at the same concentration during in vitro tests. Thus, nanocomplexing with β-lg, by virtue of its ability to enhance the solubility of glabridin in aqueous systems, provides a suitable opportunity as a nanocarrier molecule.

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Factors Influencing Glabridin Stability

Cited by 21 publications

References 10 publications

Phytochemistry and biological properties of glabridin

Phytochemistry and biological properties of glabridin

Discovery and preclinical efficacy of HSG4112, a synthetic structural analog of glabridin, for the treatment of obesity

β-Lactoglobulin as a Nanotransporter for Glabridin: Exploring the Binding Properties and Bioactivity Influences

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