Review on the Diverse Biological Effects of Glabridin

Drug Design Development and Therapy, Journal Year: 2023, Volume and Issue: Volume 17, P. 15 - 37

Published: Jan. 1, 2023

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

Language: Английский

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Flavonoids and Gastric Cancer Therapy: From Signaling Pathway to Therapeutic Significance

Drug Design Development and Therapy, Journal Year: 2024, Volume and Issue: Volume 18, P. 3233 - 3253

Published: July 1, 2024

Gastric cancer (GC) is a prevalent gastrointestinal tumor characterized by high mortality and recurrence rates. Current treatments often have limitations, prompting researchers to explore novel anti-tumor substances develop new drugs. Flavonoids, natural compounds with diverse biological activities, are gaining increasing attention in this regard. We searched from PubMed, Web of Science, SpringerLink other databases find the relevant literature last two decades. Using "gastric cancer", "stomach cancers", "flavonoid", "bioflavonoid", "2-Phenyl-Chromene" as keywords, were searched, then analyzed summarized mechanism flavonoids treatment GC. It was revealed that involves inhibiting growth, proliferation, invasion, metastasis, well inducing cell death through various processes such apoptosis, autophagy, ferroptosis, pyroptosis. Additionally, combining chemotherapeutic agents like 5-FU platinum can potentially reduce chemoresistance. Flavonoids also demonstrated enhanced activity when used combination products. Consequently, review proposes innovative perspectives for development anti-GC agents.

Language: Английский

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Structural Insights into the Substrate Recognition of Ginsenoside Glycosyltransferase Pq3‐O‐UGT2

Advanced Science, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 29, 2025

Abstract Ginsenosides are a group of tetracyclic triterpenoids with promising health benefits, consisting ginseng aglycone attached to various glycans. Pq3‐O‐UGT2, an important UDP‐dependent glycosyltransferase (UGT), catalyzes the production Ginsenoside Rg3 and Rd by extending glycan chain Rh2 F2, respectively, higher selectivity for F2. However, mechanism underlying its substrate recognition remains unclear. In this study, crystal structures Pq3‐O‐UGT2 in complex acceptor substrates solved. The revealed Nα5‐oriented binding pocket shaped unique conformation Nα5‐Nα6 linker. Hydrophobic interactions play pivotal role both while hydrogen bonds specifically aid F2 due additional glucose moiety. hydrophobic nature also enables recognize flavonoids. Overall, study provides novel insights into mechanisms ginsenoside UGTs, advancing understanding their function specificity.

Language: Английский

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Glycyrrhizin and its derivatives: an emerging secondary metabolite arsenal of Glycyrrhiza glabra

Medicinal Chemistry Research, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 31, 2025

Language: Английский

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Mechanistic inhibition of gastric cancer-associated bacteria Helicobacter pylori by selected phytocompounds: A new cutting-edge computational approach

Heliyon, Journal Year: 2023, Volume and Issue: 9(10), P. e20670 - e20670

Published: Oct. 1, 2023

Helicobacter pylori (H. pylori) is a persistent bacterial inhabitant in the stomachs of approximately half global populace. This bacterium directly linked to chronic gastritis, leading heightened risk duodenal and gastric ulcer diseases, predominant factor for cancer - second most common cause cancer-related deaths globally. The increasing prevalence antibiotic resistance necessitates exploration innovative treatment alternatives mitigate H. menace.Initiating our study, we curated list thirty phytochemicals based on previous literature subjected them molecular docking studies. Subsequently, eight phytocompounds-Glabridin, Isoliquiritin, Sanguinarine, Liquiritin, Glycyrrhetic acid, Beta-carotin, Diosgenin, Sarsasapogenin-were meticulously chosen superior binding scores. These were further an extensive computational analysis encompassing ADMET profiling, drug-likeness evaluation, principal component (PCA), dynamic simulations (MDs) comparison with conventional drug, Mitomycin.The natural compounds investigated demonstrated affinities targets compared standard Mitomycin. Notably, phytocompounds Diosgenin Sarsasapogenin stood out due their exceptional pharmacokinetic properties, including favorable profiles.Our comprehensive technologically-advanced approach showcases potential identified as pioneering therapeutic agents against pylori-induced malignancies. In light promising silico results, recommend these candidates advancing pylori-targeted drug development. Given potential, strongly advocate subsequent vitro vivo studies validate efficacy this formidable gastrointestinal bacterium.

Language: Английский

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Progress in the development of TRPV1 small-molecule antagonists: Novel Strategies for pain management

European Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 261, P. 115806 - 115806

Published: Sept. 9, 2023

Language: Английский

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The protective effect of natural medicines in rheumatoid arthritis via inhibit angiogenesis

Frontiers in Pharmacology, Journal Year: 2024, Volume and Issue: 15

Published: May 31, 2024

Rheumatoid arthritis is a chronic immunological disease leading to the progressive bone and joint destruction. Angiogenesis, accompanied by synovial hyperplasia inflammation underlies Delaying or even blocking angiogenesis has emerged as an important target of RA treatment. Natural medicines long history treating RA, numerous reports have suggested that natural strong inhibitory activity on angiogenesis, thereby improving progression RA. could regulate following signaling pathways: HIF/VEGF/ANG, PI3K/Akt pathway, MAPKs NF-κB PPARγ JAK2/STAT3 etc., inhibiting angiogenesis. Tripterygium wilfordii Hook. f. (TwHF), sinomenine, total glucoside Paeonia lactiflora Pall. Are currently most representative all products worthy development utilization. In this paper, main factors affecting were discussed different types inhibit systematically summarized. Their specific anti-angiogenesis mechanisms are also reviewed which aiming provide new perspective options for management targeting

Language: Английский

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LKB1: An emerging therapeutic target for cardiovascular diseases

Life Sciences, Journal Year: 2022, Volume and Issue: 306, P. 120844 - 120844

Published: July 27, 2022

Language: Английский

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Liquiritin inhibits H₂O₂‐induced oxidative stress injury in H9c2 cells via the AMPK/SIRT1/NF‐κB signaling pathway

Journal of Food Biochemistry, Journal Year: 2022, Volume and Issue: 46(10)

Published: Aug. 5, 2022

Heart failure (HF) is a serious disease with high mortality. Oxidative stress plays vital role in its occurrence and development. Licorice commonly used to treat HF traditional Chinese medicine. Liquiritin, the main ingredient of licorice, has antioxidant anti-inflammatory properties, but mechanism against oxidative cardiomyocytes not been reported. Establishment damage model H9c2 cells by hydrogen peroxide (H2 O2 ). Liquiritin (5, 10, 20 μmol/L) could significantly prevent loss cell viability decrease apoptosis rate. It can reduce levels reactive oxygen species (ROS), malonedialdehyde (MDA), lactate dehydrogenase (LDH), tumor necrosis factor-alpha (TNF-α), interleukin-1β (IL-1β), interleukin-6 (IL-6), increase activity ATP, superoxidedismutase (SOD), glutathione (GSH-px), reductase (GR) catalase (CAT) alleviate inflammation dose-dependent manner. was found be related AMP-Activated Protein Kinase (AMPK) pathway molecular docking. Western blotting (WB) quantitative reverse transcription PCR (RT-qPCR) confirmed that liquiritin promote AMPKα phosphorylation sirtuin 1 (SIRT1) protein expression, inhibit nuclear factor kappa B p65 (NF-κB p65). Compound C, EX 527, PDTC effects liquiritin, indicating effect achieved regulating AMPK/SIRT1/NF-κB signaling pathway. PRACTICAL APPLICATIONS: one most common cardiovascular diseases, treatment remains worldwide problem. food dietary supplement widely medicine (TCM). active components which pharmacological effects. This study revealed licorice cardiomyocytes, provided scientific basis for as an heart failure.

Language: Английский

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Liquiritin Protects Against Cardiac Fibrosis After Myocardial Infarction by Inhibiting CCL5 Expression and the NF-κB Signaling Pathway

Drug Design Development and Therapy, Journal Year: 2022, Volume and Issue: Volume 16, P. 4111 - 4125

Published: Dec. 1, 2022

Purpose: Despite significant advances in interventional treatment, myocardial infarction (MI) and subsequent cardiac fibrosis remain major causes of high mortality worldwide. Liquiritin (LQ) is a flavonoid extract from licorice that possesses variety pharmacological properties. However, to our knowledge, the effects LQ on after MI have not been reported detail. The aim research was explore potential role mechanism MI-induced damage. Methods: models were established by ligating left anterior descending branch coronary artery. Next, rats orally administered once day for 14 days. Biochemical assays, histopathological observations, ELISA, Western blotting analyses then conducted. Results: improved heart appearance ECG, decreased weight index reduced levels cardiac-specific markers such as CK, CK-MB, LDH, cTnI BNP. Meanwhile, infarct size hemodynamic parameters LVEDP, LVSP ±dp/dt max . Moreover, H&E staining showed attenuated pathological damage caused MI. Masson alleviated cell disorder while reducing collagen deposition. also oxidative stress inflammation. demonstrated significantly down-regulated expressions Collagen I, III, TGF-β 1, MMP-9, α-SMA, CCL5, p-NF-κB. Conclusion: protected against following improving function, attenuating inflammatory response, which may be associated with inhibition CCL5 expression NF-κB pathway. Keywords: liquiritin, fibrosis, infarction, expression, signaling pathway A Letter Editor has published this article

Language: Английский

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