Review on the Diverse Biological Effects of Glabridin

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Review on the Diverse Biological Effects of Glabridin

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Author(s): Jianhong Zhang ¹ ^, ² , Xinhui Wu ³ , Baiyin Zhong ¹ , Qicheng Liao ¹ , Xin Wang ¹ , Yuankang Xie ¹ , Xiao He ¹

Publication date (Electronic): 10 January 2023

Journal: Drug Design, Development and Therapy

Publisher: Dove

Keywords: glabridin, tyrosinase inhibitor, P-gp, anti-inflammation, anti-oxidation, anti-microorganism

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Abstract

Glabridin is a prenylated isoflavan from the roots of Glycyrrhiza glabra Linne and has posed great impact on the areas of drug development and medicine, due to various biological properties such as anti-inflammation, anti-oxidation, anti-tumor, anti-microorganism, bone protection, cardiovascular protection, neuroprotection, hepatoprotection, anti-obesity, and anti-diabetes. Many signaling pathways, including NF-κB, MAPK, Wnt/β-catenin, ERα/SRC-1, PI3K/AKT, and AMPK, have been implicated in the regulatory activities of glabridin. Interestingly, glabridin has been considered as an inhibitor of tyrosinase, P-glycoprotein (P-gp), and CYP2E1 and an activator of peroxisome proliferator-activated receptor γ (PPARγ), although their molecular regulating mechanisms still need further investigation. However, poor water solubility and low bioavailability have greatly limited the clinical applications of glabridin. Hopefully, several effective strategies, such as nanoemulsions, microneedles, and smartPearls formulation, have been developed for improvement.

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Most cited references 145

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A molecular modeling approach to identify effective antiviral phytochemicals against the main protease of SARS-CoV-2

Rajib Islam, Md. Rimon Parves, Archi Sundar Paul … (2020)

Abstract The main protease of SARS-CoV-2 is one of the important targets to design and develop antiviral drugs. In this study, we have selected 40 antiviral phytochemicals to find out the best candidates which can act as potent inhibitors against the main protease. Molecular docking is performed using AutoDock Vina and GOLD suite to determine the binding affinities and interactions between the phytochemicals and the main protease. The selected candidates strongly interact with the key Cys145 and His41 residues. To validate the docking interactions, 100 ns molecular dynamics (MD) simulations on the five top-ranked inhibitors including hypericin, cyanidin 3-glucoside, baicalin, glabridin, and α-ketoamide-11r are performed. Principal component analysis (PCA) on the MD simulation discloses that baicalin, cyanidin 3-glucoside, and α-ketoamide-11r have structural similarity with the apo-form of the main protease. These findings are also strongly supported by root-mean-square deviation (RMSD), root-mean-square fluctuation (RMSF), radius of gyration (Rg), and solvent accessible surface area (SASA) investigations. PCA is also used to find out the quantitative structure-activity relationship (QSAR) for pattern recognition of the best ligands. Multiple linear regression (MLR) of QSAR reveals the R2 value of 0.842 for the training set and 0.753 for the test set. Our proposed MLR model can predict the favorable binding energy compared with the binding energy detected from molecular docking. ADMET analysis demonstrates that these candidates appear to be safer inhibitors. Our comprehensive computational and statistical analysis show that these selected phytochemicals can be used as potential inhibitors against the SARS-CoV-2. Communicated by Ramaswamy H. Sarma

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The inhibitory effects of quercetin on obesity and obesity-induced inflammation by regulation of MAPK signaling.

Min Jung Seo, Yeon Lee, Ji Hyun Hwang … (2015)

Quercetin is a flavonoid found in fruits, vegetables, leaves and grains. It has inhibitory, antiviral, antiasthma, anticancer and antiinflammatory effects. Research has suggested that obesity is linked to metabolic disorders. In this study, we examined the inhibitory effect of quercetin on lipid accumulation and obesity-induced inflammation using 3T3-L1, RAW264.7, zebrafish and mouse models. Quercetin suppressed protein levels of the key adipogenic factors C/EBPβ, C/EBPα, PPARγ and FABP4 and the TG-synthesis enzymes lipin1, DGAT1 and LPAATθ. Activation of m-TOR and p70S6K, which are related to insulin and adipogenesis, was down-regulated during adipogenesis in 3T3-L1 cells. Recent research suggested that MAPK signaling factors were involved in adipogenesis and inflammation and that the adipokines MCP-1 and TNF-α attracted macrophages into adipose tissue. Our data showed that quercetin inhibited the MAPK signaling factors ERK1/2, JNK and p38MAPK and MCP-1 and TNF-α in adipocytes and macrophages. Quercetin also inhibited secretion of the inflammatory cytokines IL-1β and IL-6 and stimulated that of IL-10, an antiinflammatory cytokine. In this study, we confirmed the inhibitory effects of quercetin in adipogenesis and inflammation using a mouse model. In mice, quercetin reduced body weight (almost 40%) and suppressed expression of adipogenic, lipogenic and inflammation-related cytokines. Our data demonstrated that quercetin inhibits lipid accumulation and obesity-induced inflammation in the cell and animal models. Our study suggested that quercetin may represent a potential therapeutic agent for other metabolic disorders by regulating obesity and obesity-induced inflammation.

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Phytochemical and Pharmacological Role of Liquiritigenin and Isoliquiritigenin From Radix Glycyrrhizae in Human Health and Disease Models

Mahesh Ramalingam, Hyojung Kim, Yunjong Lee … (2018)

The increasing lifespan in developed countries results in age-associated chronic diseases. Biological aging is a complex process associated with accumulated cellular damage by environmental or genetic factors with increasing age. Aging results in marked changes in brain structure and function. Age-related neurodegenerative diseases and disorders (NDDs) represent an ever-growing socioeconomic challenge and lead to an overall reduction in quality of life around the world. Alzheimer’s disease (AD) and Parkinson’s disease (PD) are most common degenerative neurological disorders of the central nervous system (CNS) in aging process. The low levels of acetylcholine and dopamine are major neuropathological feature of NDDs in addition to oxidative stress, intracellular calcium ion imbalance, mitochondrial dysfunction, ubiquitin-proteasome system impairment and endoplasmic reticulum stress. Current treatments minimally influence these diseases and are ineffective in curing the multifunctional pathological mechanisms. Synthetic neuroprotective agents sometimes have negative reactions as an adverse effect in humans. Recently, numerous ethnobotanical studies have reported that herbal medicines for the treatment or prevention of NDDs are significantly better than synthetic drug treatment. Medicinal herbs have traditionally been used around the world for centuries. Radix Glycyrrhizae (RG) is the dried roots and rhizomes of Glycyrrhiza uralensis or G. glabra or G. inflata from the Leguminosae/Fabaceae family. It has been used for centuries in traditional medicine as a life enhancer, for the treatment of coughs and influenza, and for detoxification. Diverse chemical constituents from RG have reported including flavanones, chalcones, triterpenoid saponins, coumarines, and other glycosides. Among them, flavanone liquiritigenin (LG) and its precursor and isomer chalcone isoliquiritigenin (ILG) are the main bioactive constituents of RG. In the present review, we summarize evidence in the literature on the structure and phytochemical properties and pharmacological applications of LG and ILG in age-related diseases to establish new therapeutics to improve human health and lifespan.

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Author and article information

Journal

Journal ID (nlm-ta): Drug Des Devel Ther

Journal ID (iso-abbrev): Drug Des Devel Ther

Journal ID (publisher-id): dddt

Title: Drug Design, Development and Therapy

Publisher: Dove

ISSN (Electronic): 1177-8881

Publication date (Electronic): 10 January 2023

Publication date Collection: 2023

Volume: 17

Pages: 15-37

Affiliations

[1 ]Department of Hepatobiliary Surgery, First Affiliated Hospital of Gannan Medical University , Ganzhou, 341000, People’s Republic of China

[2 ]Ganzhou Key Laboratory of Hepatocellular Carcinoma, First Affiliated Hospital of Gannan Medical University , Ganzhou, 341000, People’s Republic of China

[3 ]Department of General Surgery, The First Affiliated Hospital of Gannan Medical University , Ganzhou, 341000, People’s Republic of China

Author notes

Correspondence: Xiao He, Email hexiao@gmu.edu.cn

[*]

These authors contributed equally to this work

Article

Publisher ID: 385981

DOI: 10.2147/DDDT.S385981

PMC ID: 9840373

PubMed ID: 36647530

SO-VID: f4fa0d38-6c25-430d-a497-596f43509ce7

License:

This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms ( https://www.dovepress.com/terms.php).

History

Date received : 12 August 2022

Date accepted : 05 January 2023

Page count

Figures: 5, Tables: 1, References: 145, Pages: 23

Funding

Funded by: Natural Science Foundation of Jiangxi Province, open-funder-registry 10.13039/501100004479;

Funded by: the Science and Technology research project of the Education Department of Jiangxi Province;

Funded by: the Science and Technology project of the First Affiliated Hospital of Gannan Medical University;

This study was financially supported by Natural Science Foundation of Jiangxi Province (Grant NO. 20212BAB216067), the Science and Technology research project of the Education Department of Jiangxi Province (Grant NO. GJJ211516 and GJJ201523), and the Science and Technology project of the First Affiliated Hospital of Gannan Medical University (Grant NO. YJYB202102 and YJYB202103).

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Review on the Diverse Biological Effects of Glabridin

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Abstract

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Most cited references 145

A molecular modeling approach to identify effective antiviral phytochemicals against the main protease of SARS-CoV-2

The inhibitory effects of quercetin on obesity and obesity-induced inflammation by regulation of MAPK signaling.

Phytochemical and Pharmacological Role of Liquiritigenin and Isoliquiritigenin From Radix Glycyrrhizae in Human Health and Disease Models

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