A comprehensive review on chemotherapeutic potential of galangin

Rampogu, Shailima; Gajula, Rajesh Goud; Lee, Keun Woo

doi:10.1016/j.biopha.2021.111808

Cited by 46 publications

(37 citation statements)

References 62 publications

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“…As is well-known, galangin has a wide range of biological activities such as anticancer, anti-inflammatory, antibacterial, antioxidation, and scavenging free radicals. 1 It could attenuate oxidative stress-mediated apoptosis in renal tubular epithelial cells. 2 In our recent screening experiment, galangin was found to possess an effective inhibitory effect on ferroptosis.…”

Section: Introductionmentioning

confidence: 99%

“…Galangin, a kind of bioflavonoid, is mainly extracted from the rhizome of Alpinis officinarum and honeybee propolis. As is well‐known, galangin has a wide range of biological activities such as anticancer, anti‐inflammatory, antibacterial, antioxidation, and scavenging free radicals 1 . It could attenuate oxidative stress‐mediated apoptosis in renal tubular epithelial cells 2 .…”

Section: Introductionmentioning

confidence: 99%

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Galangin inhibited ferroptosis through activation of the PI3K/AKT pathway in vitro and in vivo

et al. 2022

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Ferroptosis is an iron‐dependent form of nonapoptotic cell death characterized by the accumulation of lipid peroxides in cells. In recent years, extensive attention has been dedicated to exploring safe and effective natural ferroptosis regulators which can provide novel treatment strategies for ferroptosis‐related diseases. This study identified galangin, a natural flavonoid, as an effective inhibitor of ferroptosis, which could increase cell viability in RSL3‐inhibited HT1080 cells, decrease levels of lipid ROS and MDA, improve PTGS2 mRNA expression, and enhance the expression of glutathione peroxidase 4 (GPX4). Ferroptosis is widely present in ischemia‐reperfusion (IR) injury. This study found that galangin significantly ameliorated the pathological damage of liver tissue in mice with IR, reduced levels of serum ALT, AST, and MDA, and increased the expression of GPX4. The results of RNA‐seq exhibited ferroptosis was significant and the PI3K/AKT pathway deserved to explore the inhibition effects of galangin on ferroptosis. Indeed, galangin treatment significantly rescued RSL3‐inhibited phosphorylation levels of PI3K, AKT, and CREB proteins, and the ferroptosis inhibitory effects of galangin were counteracted by PI3K inhibitor LY294002. These findings indicated that galangin may exert its anti‐ferroptosis effects via activating the PI3K/AKT/CREB signaling pathway and it will hopefully serve as a promising effective measure to attenuate IR injury by inhibiting ferroptosis.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Galangin inhibited ferroptosis through activation of the PI3K/AKT pathway in vitro and in vivo

et al. 2022

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“…Galangin is a natural flavonoid present at high concentrations in Alpinia officinarum . Galangin has been reported as an herbal medicine possessing a wide range of pharmacological activities, including antiarthritic, antibacterial, anti-inflammatory, and anticancer in various types of cancers. , Galangin influences cell proliferation, apoptosis, and metastasis, , although the underlying molecular mechanisms have not been fully elucidated. A previous study showed that 46 μM or more galangin separated from propolis could significantly inhibit collagen-induced platelet aggregation in a dose-dependent manner when added to platelet-rich plasma, which is in line with our results.…”

Section: Resultsmentioning

confidence: 99%

Identification of Antithrombotic Natural Products Targeting the Major Substrate Binding Pocket of Protein Disulfide Isomerase

Liang

Cai

et al. 2022

J. Nat. Prod.

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Protein disulfide isomerase (PDI) is a vital oxidoreductase. Extracellular PDI promotes thrombus formation but does not affect physiological blood hemostasis. Inhibition of extracellular PDI has been demonstrated as a promising strategy for antithrombotic treatment. Herein, we focused on the major substrate binding site, a unique pocket in the PDI b′ domain, and identified four natural products binding to PDI by combining virtual screening with tryptophan fluorescence-based assays against a customized natural product library. These hits all directly bound to the PDI-b′ domain and inhibited the reductase activity of PDI. Among them, galangin showed the most prominent potency (5.9 μM) against PDI and as a broad-spectrum inhibitor for vascular thiol isomerases. In vivo studies manifested that galangin delayed the time of blood vessel occlusion in an electricity-induced mouse thrombosis model. Molecular docking and dynamics simulation further revealed that the hydroxyl-substituted benzopyrone moiety of galangin deeply inserted into the interface between the PDI-b′ substrate-binding pocket and the a′ domain. Together, these findings provide a potential antithrombotic drug candidate and demonstrate that the PDI b′ domain is a critical domain for inhibitor development. Besides, we also report an innovative highthroughput screening method for the rapid discovery of PDI b′ targeted inhibitors.

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“…The natural flavonoid galangin is extracted from the roots of Alpinia officinarum . In South Africa, this herb is used to treat infection [ 9 ]. Galangin is renowned for its multiple beneficial properties, including anti-proliferative, anti-oxidative, cardioprotective, and immunoprotective traits [ 10 ].…”

Section: Introductionmentioning

confidence: 99%

Galangin alleviates rheumatoid arthritis in rats by downregulating the phosphatidylinositol 3-kinase/protein kinase B signaling pathway

Deng

Wan

et al. 2022

Bioengineered

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Rheumatoid arthritis (RA) is a chronic autoimmune disease that greatly affect patients’ quality of life. Galangin extract is renowned for its anti-proliferative and anti-oxidative characteristics. However, galangin cytotoxicity studies are presently inadequate. We aimed to investigate the therapeutic potential of galangin on RA by investigating the PI3K/AKT signaling pathway.Fibroblast-like synovial cells (FLSs) were exposed to lipopolysaccharide (LPS) to establish an RA model in vitro . An ELISA assay was used to detect the levels of IL-1β, TNF-α, and IL-6. Cell viability and apoptosis were determined by CCK8/EdU and flow cytometry assays. A western blot assay was used to analyze the protein expression levels. An RA rat model was established to evaluate the function of galangin through histopathological examination. Our results found that galangin induced apoptosis, inhibited cell proliferation, and increased cell invasion of rheumatoid arthritis fibroblast-like synovial cells (RAFLSs). Galangin inactivated the PI3K/AKT signaling pathway and the inflammatory response. An agonist of PI3K signaling, 740Y‐P, restored the cellular functions of RAFLSs. Moreover, galangin suppressed the development of RA in vivo . Galangin effected its anti-arthritic influence through the PI3K/AKT signaling pathway. Galangin has potential as an alternative treatment for RA.

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A comprehensive review on chemotherapeutic potential of galangin

Cited by 46 publications

References 62 publications

Galangin inhibited ferroptosis through activation of the PI3K/AKT pathway in vitro and in vivo

Galangin inhibited ferroptosis through activation of the PI3K/AKT pathway in vitro and in vivo

Identification of Antithrombotic Natural Products Targeting the Major Substrate Binding Pocket of Protein Disulfide Isomerase

Galangin alleviates rheumatoid arthritis in rats by downregulating the phosphatidylinositol 3-kinase/protein kinase B signaling pathway

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