Irigenin inhibits glioblastoma progression through suppressing YAP/β-catenin signaling

Xu, Jiayun; Sun, Shanshan; Zhang, Wei; Dong, Jianhong; Huang, Changgang; Wang, Xin; Jia, Mengxian; Yang, Hao; Wang, Yongjie; Jiang, Yuanyuan; Cao, Lei; Huang, Zhihui

doi:10.3389/fphar.2022.1027577

Cited by 4 publications

(2 citation statements)

References 51 publications

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“…To complete the cell cycle, a successful G2/M phase is crucial, and uncontrolled cell proliferation might result from imbalanced cell-cycle regulation, which is a hallmark of cancer cells, including GBM [ 30 , 31 ]. Several anticancer drugs have been found to induce G2/M cell-cycle arrest and apoptosis in different GBM cell lines, effectively suppressing proliferation [ 32 , 33 ]. Moreover, the observation that, upon compound 5 treatment, G2/M phase arrest was observed in DBTRG, but not in LN299 cells can be explained by considering that these GBM cell lines possess a diverse genetic background and, in turn, possibly different mechanisms leading to tumor development [ 34 ], which might impact the cells’ capacity to respond to drugs.…”

Section: Resultsmentioning

confidence: 99%

Biological Evaluation and In Vitro Characterization of ADME Profile of In-House Pyrazolo[3,4-d]pyrimidines as Dual Tyrosine Kinase Inhibitors Active against Glioblastoma Multiforme

et al. 2023

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The therapeutic use of tyrosine kinase inhibitors (TKIs) represents one of the successful strategies for the treatment of glioblastoma (GBM). Pyrazolo[3,4-d]pyrimidines have already been reported as promising small molecules active as c-Src/Abl dual inhibitors. Herein, we present a series of pyrazolo[3,4-d]pyrimidine derivatives, selected from our in-house library, to identify a promising candidate active against GBM. The inhibitory activity against c-Src and Abl was investigated, and the antiproliferative profile against four GBM cell lines was studied. For the most active compounds endowed with antiproliferative efficacy in the low-micromolar range, the effects toward nontumoral, healthy cell lines (fibroblasts FIBRO 2-93 and keratinocytes HaCaT) was investigated. Lastly, the in silico and in vitro ADME properties of all compounds were also assessed. Among the tested compounds, the promising inhibitory activity against c-Src and Abl (Ki 3.14 µM and 0.44 µM, respectively), the irreversible, apoptotic-mediated death toward U-87, LN18, LN229, and DBTRG GBM cell lines (IC50 6.8 µM, 10.8 µM, 6.9 µM, and 8.5 µM, respectively), the significant reduction in GBM cell migration, the safe profile toward FIBRO 2-93 and HaCaT healthy cell lines (CC50 91.7 µM and 126.5 µM, respectively), the high metabolic stability, and the excellent passive permeability across gastrointestinal and blood–brain barriers led us to select compound 5 for further in vivo assays.

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Section: Resultsmentioning

confidence: 99%

Biological Evaluation and In Vitro Characterization of ADME Profile of In-House Pyrazolo[3,4-d]pyrimidines as Dual Tyrosine Kinase Inhibitors Active against Glioblastoma Multiforme

et al. 2023

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“…Taxifolin is a class of flavonoids that have antioxidant, anti-inflammatory, antibacterial, and bone loss prevention effects [ 69 , 70 ]. Irigenin is a class of isoflavonoids, which has mainly been derived from Belamcanda chinensis in previous studies, and it has important medicinal values, including antioxidant, anti-inflammatory, and antitumor properties [ 71 ]. In the present work, irigenin, an important compound, was identified using the root tissue of B. vivipara ; this is the first time this has been done for B. vivipara .…”

Section: Discussionmentioning

confidence: 99%

Revealing Medicinal Constituents of Bistorta vivipara Based on Non-Targeted Metabolomics and 16S rDNA Gene Sequencing Technology

He,

Tang,

Cao

et al. 2024

Molecules

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Bistorta vivipara is a medicinal plant with a long history, but there are few studies on the effects of its medicinal components and endophytic bacteria on the accumulation of secondary metabolites. Therefore, in this study, non-targeted metabolomics techniques and 16s rDNA techniques were used to study B. vivipara from different regions. A total of 1290 metabolites and 437 differential metabolites were identified from all samples. Among them, flavonoids, isoflavonoids, and benzopyrans are the main medicinal components of B. vivipara; these have potential anticancer, antiviral, and antioxidant properties, as well as potential applications for the treatment of atrial fibrillation. In addition, irigenin, an important medicinal component, was identified for the first time. The endophytic bacterial communities in the root tissues of B. vivipara from different regions were also different in composition and richness. Hierarchical clustering heat map analysis showed that Proteobacteria and Actinobacteriota bacteria significantly affected the accumulation of many medicinal components in the roots of B. vivipara.

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Integrating serum metabolomics analysis and network pharmacology to reveal the potential mechanism of Shengmai Jianghuang San in the treatment of nasopharyngeal carcinoma

Zeng,

Zhu,

et al. 2024

Biomedical Chromatography

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Shengmai Jianghuang San (SMJHS) is a traditional Chinese herbal compound reported to inhibit Nasopharyngeal Carcinoma (NPC) progression and enhance radiosensitivity. However, the specific active ingredients and regulatory mechanisms of SMJHS against NPC, particularly under hypoxic conditions, remain unclear. In this study, Sprague–Dawley (SD) rats were gavaged with Shengmai Jianghuang San (SMJHS), and their blood was collected from the abdominal aorta. UHPLC‐Q‐Exactive orbitrap MS/MS was used to identify the metabolite profiles of SMJHS drug‐containing serum. A molecular network of the active compositions in SMJHS targeting NPC was constructed through network pharmacology and molecular docking. The HIF‐1α/VEGF pathway was in key positions. The effects of SMJHS on the proliferation, migration, and radiosensitivity of hypoxic NPC cells were assessed by in vitro experiments. NPC cell lines stably overexpressing HIF‐1α were established using a lentivirus to investigate the regulation of HIF‐1α/VEGF signaling in hypoxic NPC cells by SMJHS. Through a combination of network pharmacological analysis, cellular biofunctional validation, and molecular biochemical experiments, our study found that SMJHS had an anti‐proliferative effect on NPC cells cultured under hypoxic conditions, inhibiting their migration and increasing their radiosensitivity. Additionally, SMJHS suppressed the expression of HIF‐1α and VEGFA, exhibiting potential as an effective option for improving NPC treatment.

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Irigenin inhibits glioblastoma progression through suppressing YAP/β-catenin signaling

Cited by 4 publications

References 51 publications

Biological Evaluation and In Vitro Characterization of ADME Profile of In-House Pyrazolo[3,4-d]pyrimidines as Dual Tyrosine Kinase Inhibitors Active against Glioblastoma Multiforme

Biological Evaluation and In Vitro Characterization of ADME Profile of In-House Pyrazolo[3,4-d]pyrimidines as Dual Tyrosine Kinase Inhibitors Active against Glioblastoma Multiforme

Revealing Medicinal Constituents of Bistorta vivipara Based on Non-Targeted Metabolomics and 16S rDNA Gene Sequencing Technology

Integrating serum metabolomics analysis and network pharmacology to reveal the potential mechanism of Shengmai Jianghuang San in the treatment of nasopharyngeal carcinoma

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