Role of Licochalcone A in Potential Pharmacological Therapy: A Review

Li, Mengting; Xie, Long; Jiang, Hai-Mei; Huang, Qun; Tong, Rongsheng; Li, Xiang; Xie, Xin; Li, Hongmei

doi:10.3389/fphar.2022.878776

Cited by 26 publications

(33 citation statements)

References 113 publications

(123 reference statements)

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“…Kaempferol suppresses proliferation, migration and invasion of fibroblast-like synoviocytes, and alleviates inflammation ( Yoon et al, 2013 ; Lee et al, 2018 ; Pan et al, 2018 ). Naringenin ( Hajizadeh et al, 2021 ; Wang et al, 2021 ), formononetin ( Machado Dutra et al, 2021 ), isorhamnetin ( Gong et al, 2020 ), and licochalcone A ( de Freitas et al, 2020 ; Li et al, 2022 ) have been reported to have antioxidant, anti-inflammatory, anti-cancer and osteogenic effects, showing great potential as agents for the treatment of RA.…”

Section: Discussionmentioning

confidence: 99%

Therapeutic effects of shaogan fuzi decoction in rheumatoid arthritis: Network pharmacology and experimental validation

et al. 2022

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Shaogan Fuzi Decoction (SGFD), one of the classical prescriptions of Chinese Medicine, has a long history in the treatment of rheumatoid arthritis (RA), but definitive studies on its efficacy and mechanism of action are lacking. This study aims to elucidate the pharmacodynamic role of SGFD against RA and the potential mechanisms based on a combination of network pharmacology and experimental verification. The RA model in rats was induced by intradermal injection of bovine type Ⅱ collagen and incomplete Freund’s adjuvant at the tail root. SGFD was administered once a day by oral gavage for 4 weeks. After SGFD administration, rat’s arthritis index (AI) score and paw swelling decreased to some extent, and synovial inflammation, vascular hyperplasia, and cartilage destruction of the ankle joint were improved. Simultaneously, thymus and spleen index and serum levels of C-reactive protein (CRP) were lowered. Network pharmacology revealed that quercetin, kaempferol, naringenin, formononetin isorhamnetin and licochalcone A were the potentialiy active components, and IL6, TP53, TNF, PTGS2, MAPK3 and IL-1β were potential key targets for SGFD in the treatment of RA. Ingredients-targets molecular docking showed that the components had the high binding activity to these target proteins. The mechanism of SGFD for RA involves various biological functions and is closely correlated with TNF signaling pathway, Osteoclast differentiation, T cell receptor signaling pathway, mitogen-activated protein kinase (MAPK) signaling pathway, NF-κB signaling pathway, toll-like receptor signaling pathway, and so on. Western blot and ELISA showed that the expression of toll-like receptor 4 (TLR4), nuclear factor kappa-B (NF-κB) p65, phosphorylated c-Jun N-terminal kinase (p-JNK), p-p38, phosphorylated extracellular regulated kinase (p-ERK) and TNF-α was significantly upregulated in the synovium of RA rats, and the levels of serum inflammatory factors were significantly increased. SGFD inhibits the activation of the TLR4/NF-κB/MAPK pathway and the expression/production of pro-inflammatory cytokines. In summary, SGFD could improve the symptoms and inflammatory response in collagen-induced arthritis (CIA) rat model. The mechanism might be related to the regulation of TLR4/MAPKs/NF-κB signaling pathway and the reduction of inflammatory factor release, which partially confirms the results predicted by network pharmacology.

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Section: Discussionmentioning

confidence: 99%

Therapeutic effects of shaogan fuzi decoction in rheumatoid arthritis: Network pharmacology and experimental validation

et al. 2022

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“…The UV spectra of the chalcone compounds were recorded on a photodiode array UV−vis detector (SPD-M20A, 230 V, Shimadzu, Kyoto, Japan). 1 H NMR and 13 C NMR spectra of the chalcone derivatives were recorded on a Bruker AVANCE 500/125 MHz instrument using DMSO-d 6 or CDCl 3 as solvents. Solvent peaks appeared at 2.50 ppm (DMSO) and 7.28 ppm (CDCl 3 ) in the 1 H NMR spectrum and at 40.0 ppm (DMSO) and 77.0 ppm (CDCl 3 ) in the 13 C NMR spectrum.…”

Section: ■ Experimental Sectionmentioning

confidence: 99%

“…Licochalcone A, a flavonoid isolated from the roots of Glycyrrhiza uralensis Fisch. ex DC., 1,2 has garnered significant attention in medicinal research in the past few decades. 1,3,4 Numerous studies have explored the pharmacological effects of licochalcone A, unveiling its potential as a therapeutic agent.…”

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confidence: 99%

“…ex DC., 1,2 has garnered significant attention in medicinal research in the past few decades. 1,3,4 Numerous studies have explored the pharmacological effects of licochalcone A, unveiling its potential as a therapeutic agent. 1,3,4 Notably, this compound can mitigate acute lung, kidney, and liver inflammation by engaging in the regulation of multiple signaling pathways, such as mitogen-activated protein kinase, nuclear factor kappa-B (NF-κB), nucleotide-binding oligomerization domain-like receptor thermal protein domain associated protein 3, and nuclear factor erythroid 2-related factor 2.…”

mentioning

confidence: 99%

“…Licochalcone A, a flavonoid isolated from the roots of Glycyrrhiza uralensis Fisch. ex DC., , has garnered significant attention in medicinal research in the past few decades. ,, Numerous studies have explored the pharmacological effects of licochalcone A, unveiling its potential as a therapeutic agent. ,, Notably, this compound can mitigate acute lung, kidney, and liver inflammation by engaging in the regulation of multiple signaling pathways, such as mitogen-activated protein kinase, nuclear factor kappa-B (NF- κ B), nucleotide-binding oligomerization domain-like receptor thermal protein domain associated protein 3, and nuclear factor erythroid 2-related factor 2. ,, Moreover, licochalcone A exhibits promising hypoglycemic activity, inhibitory effects on dipeptidyl peptidase 4 (DPP4), and protective properties against diabetic nephropathy in animal models of type 2 diabetes mellitus. − These findings underscore the potential of optimizing this natural product as a potent DPP4 inhibitor with anti-inflammatory effects.…”

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confidence: 99%

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Licochalcone A Derivatives as Selective Dipeptidyl Peptidase 4 Inhibitors with Anti-Inflammatory Effects

Shi

Mei

et al. 2023

J. Nat. Prod.

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A set of 22 analogs of licochalcone A was designed and synthesized to explore their potentials as dipeptidyl peptidase 4 (DPP4) inhibitors with anti-inflammatory effects. The anti-DPP4 effects of these analogs were evaluated using the fluorescent substrate Gly-Pro-N-butyl-4-amino-1,8-naphthalimide (GP-BAN). The nitro-substituted analogue 27 exhibited the most potent activity (K i = 0.96 μM). A structure–activity relationship investigation revealed that 4-hydroxyl and 5-chloro substituents are essential for DPP4 inhibition, while the 3′-nitro substituent improved both DPP4 inhibition and microsomal stability. Furthermore, compound 27 demonstrated good selectivity for DPP4 over other proteases, including dipeptidyl peptidase 9 (DPP9), thrombin, prolyl endopeptidase (PREP), and fibroblast activation protein (FAP). The cytotoxic effect of 27 was evaluated in cancer cell lines HepG-2 and Caco-2 and in somatic RAW264.7 cells and RPTECs. Compound 27 showed no toxicity to normal cells and weak toxicity to cancer cells. In a living cell imaging assay, 27 blocked the dipeptidase activity of DPP4 in both Caco-2 and HepG-2 cells. This compound also dose-dependently suppressed the expression levels of the chemokines tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β).

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Efficacy and safety of irinotecan combined with raltitrexed or irinotecan monotherapy for salvage chemotherapy of esophageal squamous cell cancer: A prospective, open label, randomized phase II study

Dai

Tao

Wang³

et al. 2023

Cancer Medicine

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Background: Esophageal squamous cell cancer (ESCC) accounts for approximately 90% of esophageal cancer cases in China. There are no standard regimens for second or third–line chemotherapy of metastatic squamous esophageal cancer. The objective of this study was to investigate the security and effectiveness of irinotecan combined with raltitrexed or irinotecan monotherapy for salvage chemotherapy of ESCC.Methods: One hundred and twenty–eight patients with metastatic ESCC confirmed by histopathology were enrolled into this study. These patients had failure of the first–line chemotherapy combination of fluorouracil or platinum or paclitaxel and had not undergone chemotherapy with irinotecan or raltitrexed previously. Patients were randomly divided into irinotecan combined with raltitrexed group (experiment group) and irinotecan monotherapy group (control group). Overall survival (OS) and progression–free survival (PFS) were the primary endpoint.Results: In the control group, the median PFS (mPFS) and median OS (mOS) of patients were 3.37 and 5.3 months. In the experiment group, mPFS and mOS were 3.91 and 7.0 months. There was statistical significance of PFS and OS between two groups (PFS P = 0.002, OS P = 0.01). In subgroup analysis, in the second–line treatment, the mPFS of control and experiment group, was 3.90 and 4.60 months, mOS was 6.95 and 8.5 months, which was statistically significant differences between the two groups. (PFS P = 0.001, OS P = 0.005), In the third–line and beyond treatment, mPFS of control and experiment group was 2.80 and 3.19 months, mOS were 4.5 and 4.8 months. But there was no significant difference of PFS or OS between the two groups (PFS P = 0.19, OS P = 0.31). There was no statistical significance of toxicity side effects between two groups.Conclusions: The PFS and OS of irinotecan plus raltitrexed may be better than that of irinotecan monotherapy, especially in second line treatment, which should be confirmed with a phase III study including much more patients.

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Role of Licochalcone A in Potential Pharmacological Therapy: A Review

Cited by 26 publications

References 113 publications

Therapeutic effects of shaogan fuzi decoction in rheumatoid arthritis: Network pharmacology and experimental validation

Therapeutic effects of shaogan fuzi decoction in rheumatoid arthritis: Network pharmacology and experimental validation

Licochalcone A Derivatives as Selective Dipeptidyl Peptidase 4 Inhibitors with Anti-Inflammatory Effects

Efficacy and safety of irinotecan combined with raltitrexed or irinotecan monotherapy for salvage chemotherapy of esophageal squamous cell cancer: A prospective, open label, randomized phase II study

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