Synergistic anti-glioma effect of Hydroxygenkwanin and Apigenin in vitro

Wang, Yi; Xu, You; Yin, Lian; Xu, Lina; Peng, Jin Yong; Zhou, Hang; Kang, Wei

doi:10.1016/j.cbi.2013.10.009

Cited by 32 publications

(25 citation statements)

References 37 publications

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“…The flower buds of D. genkwa contain an abundance of flavonoids and daphne diterpene esters, including the flavonoid hydroxygenkwanin (HGK) [28,29]. A previous study found that HGK could induce mitochondrial injury in brain cancer cells and concurrently trigger DNA breakage and cell cycle arrest, ultimately inducing apoptosis [30,31]. However, research on the bioactivity of HGK has been limited, and there are no published studies on its efficacy against other types of cancer.…”

Section: Introductionmentioning

confidence: 99%

Suppression of Hepatocellular Carcinoma Progression through FOXM1 and EMT Inhibition via Hydroxygenkwanin-Induced miR-320a Expression

et al. 2019

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Daphne genkwa, a Chinese medicinal herb, is used frequently in Southeast Asian countries to treat diseases; the flavonoid hydroxygenkwanin (HGK) is extracted from its flower buds. The bioactivity of HGK, particularly as an anti-liver cancer agent, has not been explored. In this study, human hepatocellular carcinoma (HCC) cell lines and an animal xenograft model were employed to investigate both the activity of HGK against liver cancer and its cellular signaling mechanisms. HCC cells treated with HGK were subjected to cell function assays. Whole transcriptome sequencing was used to identify genes whose expression was influenced by HGK, and the flavonoid's cancer suppression mechanisms were further investigated through gain-and loss-of-function assays. Finally, in vitro findings were tested in a mouse xenograft model. The data showed that HGK induced the expression of the microRNA miR-320a, which in turn inhibited the expression of the transcription factor 'forkhead box protein M1' (FOXM1) and downstream FOXM1-regulated proteins related to epithelial-mesenchymal transition, thereby leading to the suppression of liver cancer cell growth and invasion. Significant inhibition of tumor growth was also observed in HGK-treated mice. Hence, the present study demonstrated the activity of HGK against liver cancer and validated its potential use as a therapeutic agent.

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Section: Introductionmentioning

confidence: 99%

Suppression of Hepatocellular Carcinoma Progression through FOXM1 and EMT Inhibition via Hydroxygenkwanin-Induced miR-320a Expression

et al. 2019

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“…Genkwanin shows significant anti‐tumor activity by enhancing host immunity and decreasing inflammatory cytokine levels (Wang et al, ); this compound also exhibits antioxidant properties and immunomodulatory effects on splenocytes, NK and CTL cells (Nasr‐Bouzaiene et al, ). Hydroxygenkwanin possesses anti‐glioma and anti‐rheumatoid arthritic activities (Jiang et al, ; Wang et al, ). Moreover, umbelliferone (7‐hydroxy coumarin) contains a natural well‐known skeleton that has a wide spectrum of bioactivity, such as anti‐oxidant, antihyperlipidemic and antidiabetic properties (Pan, Li, Jin, Yang, & Qin, ; Suwannaphet, Meeprom, Yibchok‐Anun, & Adisakwattana, ).…”

Section: Introductionmentioning

confidence: 99%

Simultaneous determination of three flavonoids and one coumarin by LC–MS/MS: Application to a comparative pharmacokinetic study in normal and arthritic rats after oral administration of Daphne genkwa extract

Zhou

Yan

2018

Biomedical Chromatography

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A selective and sensitive liquid chromatography-tandem mass spectrometry method was developed and validated for investigating the pharmacokinetics of umbelliferone, apigenin, genkwanin and hydroxygenkwanin after oral administration of Daphne genkwa extract. Plasma samples were treated by protein precipitation with acetonitrile. Analytes were detected by triple-quadrupole MS/MS with an ESI source in negative selection reaction monitoring mode. The transitions of m/z 161 → 133 for umbelliferone, m/z 269 → 117 for apigenin, m/z 283 → 268 for genkwanin and m/z 299 → 284 for hydroxygenkwanin were confirmed for quantification. Chromatographic separation was conducted using an Eclipse XDB-C column, and the applied isocratic elution program allowed for simultaneous determination of the four analytes for a total run time of 2.5 min. The linearity was validated over the plasma concentration ranges of 1.421-1421 ng/mL for umbelliferone, 0.845-845 ng/mL for apigenin, 1.025-1025 ng/mL for genkwanin and 0.845-845 ng/mL for hydroxygenkwanin. The extraction recovery rate was >82.7% for each analyte. No apparent matrix effect was observed during the bioanalysis. After full validation, the proposed method was successfully applied to compare the pharmacokinetics of these analytes between normal and arthritic rats.

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“…Apoptosis is mediated by caspases, which are cysteine proteases that cleave target proteins at aspartic acid (Kim et al, 2013). In the present study, we investigated the influence of CRM197 and shRNA-VCAM-1 on the activation of caspase-3, 8, and 9, which contribute most in the apoptosis of glioma cells (Wang et al, 2013b;Guo et al, 2014;Xie et al, 2014). Caspase-3 is a common proteolytic enzyme involved in both the extrinsic and intrinsic apoptotic pathways (Wang et al, 2013c).…”

Section: Discussionmentioning

confidence: 99%

“…It has been well established that caspase-3, 8, and 9 contribute most in the apoptosis of glioma cells (Wang et al, 2013b;Guo et al, 2014;Xie et al, 2014). To determine the involvement of apoptosis-related proteins and activation of caspases, we examined expression and activation of caspase 3, 8, and 9 in glioblastoma cells following treatments of CRM197, shRNA-VCAM-1 or combination of both.…”

Section: Journal Of Cellular Physiologymentioning

confidence: 99%

CRM197 in Combination With shRNA Interference of VCAM-1 Displays Enhanced Inhibitory Effects on Human Glioblastoma Cells

Lin

Wang

et al. 2015

J. Cell. Physiol.

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CRM197 is a naturally nontoxic diphtheria toxin mutant that binds and inhibits heparin-binding epidermal growth factor-like growth factor. CRM197 serves as carrier protein for vaccine and other therapeutic agents. CRM197 also inhibits the growth, migration, invasion and induces apoptosis in various tumors. Vascular cell adhesion molecule-1 (VCAM-1) is an important cell surface adhesion molecule associated with malignancy of gliomas. In this work, we aimed to investigate the role and mechanism of CRM197 combined with shRNA interference of VCAM-1 (shRNA-VCAM-1) on the migration, invasion and apoptosis of glioblastoma cells. U87 and U251 human glioblastoma cells were treated with CRM197 (10 μg/ml) and shRNA interfering technology was employed to silence VCAM-1 expression. Cell viability, migration, invasiveness and apoptosis were assessed with CCK8, Transwell and Annexin V-PE/7-AAD staining. Activation of cleaved caspase-3, 8 and 9, activity of matrix metalloproteinase-2/9 (MMP-2/9) and expression of phosphorylated Akt (p-Akt) were also checked. Results showed that CRM197 and shRNA-VCAM-1 not only significantly inhibited the cell proliferation, migration, invasion, but also promoted the apoptosis of U87 and

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Synergistic anti-glioma effect of Hydroxygenkwanin and Apigenin in vitro

Cited by 32 publications

References 37 publications

Suppression of Hepatocellular Carcinoma Progression through FOXM1 and EMT Inhibition via Hydroxygenkwanin-Induced miR-320a Expression

Suppression of Hepatocellular Carcinoma Progression through FOXM1 and EMT Inhibition via Hydroxygenkwanin-Induced miR-320a Expression

Simultaneous determination of three flavonoids and one coumarin by LC–MS/MS: Application to a comparative pharmacokinetic study in normal and arthritic rats after oral administration of Daphne genkwa extract

CRM197 in Combination With shRNA Interference of VCAM-1 Displays Enhanced Inhibitory Effects on Human Glioblastoma Cells

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