Chrysin a promising anticancer agent: recent perspectives

Shahbaz, Muhammad; Naeem, Hammad; Imran, Muhammad; Ul Hassan, Hammad; Alsagaby, Suliman A.; Al Abdulmonem, Waleed; Waqar, Ahmed Bilal; Ghorab, Ahmed H.; Abdelgawad, Mohamed A.; Ghoneim, Mohammed M.; Hussain, Muzzamal; Al Jbawi, Entessar; Ihsan, Amna

doi:10.1080/10942912.2023.2246678

Cited by 12 publications

(3 citation statements)

References 119 publications

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“…3 h). Pharmacological degradation of HIF1α by Chrysin 39 , 40 also led to the accumulation of LC3B-II and p62 in Daoy and UW228 cells (Fig. 3 i).…”

Section: Resultsmentioning

confidence: 87%

REST-dependent downregulation of von Hippel-Lindau tumor suppressor promotes autophagy in SHH-medulloblastoma

Singh,

Cheng,

Swaminathan

et al. 2024

Sci Rep

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The RE1 silencing transcription factor (REST) is a driver of sonic hedgehog (SHH) medulloblastoma genesis. Our previous studies showed that REST enhances cell proliferation, metastasis and vascular growth and blocks neuronal differentiation to drive progression of SHH medulloblastoma tumors. Here, we demonstrate that REST promotes autophagy, a pathway that is found to be significantly enriched in human medulloblastoma tumors relative to normal cerebella. In SHH medulloblastoma tumor xenografts, REST elevation is strongly correlated with increased expression of the hypoxia-inducible factor 1-alpha (HIF1α)—a positive regulator of autophagy, and with reduced expression of the von Hippel-Lindau (VHL) tumor suppressor protein – a component of an E3 ligase complex that ubiquitinates HIF1α. Human SHH-medulloblastoma tumors with higher REST expression exhibit nuclear localization of HIF1α, in contrast to its cytoplasmic localization in low-REST tumors. In vitro, REST knockdown promotes an increase in VHL levels and a decrease in cytoplasmic HIF1α protein levels, and autophagy flux. In contrast, REST elevation causes a decline in VHL levels, as well as its interaction with HIF1α, resulting in a reduction in HIF1α ubiquitination and an increase in autophagy flux. These data suggest that REST elevation promotes autophagy in SHH medulloblastoma cells by modulating HIF1α ubiquitination and stability in a VHL-dependent manner. Thus, our study is one of the first to connect VHL to REST-dependent control of autophagy in a subset of medulloblastomas.

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“…3 h). Pharmacological degradation of HIF1α by Chrysin 39 , 40 also led to the accumulation of LC3B-II and p62 in Daoy and UW228 cells (Fig. 3 i).…”

Section: Resultsmentioning

confidence: 87%

REST-dependent downregulation of von Hippel-Lindau tumor suppressor promotes autophagy in SHH-medulloblastoma

Singh,

Cheng,

Swaminathan

et al. 2024

Sci Rep

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“…Over the years, it has garnered interest for its potential health benefits, including its potential anticancer properties. Chr has been shown to exert its anticancer effects through various mechanisms, such as inhibiting tumor cell proliferation, inducing apoptosis, inhibiting inflammation, and modulating certain enzyme activities and signaling pathways [2,3]. However, its effectiveness in cancer treatment is restricted due to its water-repelling characteristics, poor absorption, swift breakdown, and fast metabolism.…”

Section: Introductionmentioning

confidence: 99%

Optimizing Chrysin’s Anticancer Efficacy on MDA-MB-231 Cells: Synthesis and Characterization of Chrysin-Loaded Gold/Chitosan Nanoparticles

Dilfy,

Mubark,

Ahad

2023

TPB

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This study showcases the creation of nanostructures that carry Chrysin (Chr), using gold (AuNPs) nanoparticles encased in chitosan. The Au particles were derived by reducing AuCl4 − with tripolyphosphate (TPP) and CS. These gold/chitosan nanoparticles (Au/CS NPs) were analyzed using UV-Vis spectroscopy. Their size was identified as approximately 45.23± 4.32 nm through DLS, and the crystal makeup of gold was verified by XRD. FE-SEM imaging confirmed these NPs to be round, with an average size around 42 nm. Measurements showed that the drug capacity for Chr was about 20 ± 3.70% and its encapsulation efficiency stood at roughly 88.7 ± 4.50%. The nanocarrier's drug release behavior was observed in both acidic and neutral conditions (with pH levels of 5.4 and 7.4), and it was notably responsive to the acidic environment. Moreover, MTT test showed the Chr-infused NPs were more toxic to the MDA-MB-231 breast cancer cells than Chr alone. Based on this data, further exploration of these Au/CS NPs is recommended to enhance the therapeutic potential of Chr.

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“…However, the search for therapeutic agents that can be used in treatment continues due to high side effects. In recent years, natural products like flavonoids have become interesting in cancer treatment because they are less toxic and, therefore, cause fewer side effects [3].…”

Section: Introductionmentioning

confidence: 99%

Chrysin Mediates the Induction of Apoptosis in Breast Cancer Cells via the Inhibition of the WNT/β-Catenin Signaling Pathway

Çetinkaya

2023

Preprint

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Chrysin, a flavonoid compound, has attracted interest as a therapeutic agent due to its anti-inflammatory, antidiabetic, antidepressant, and particularly its anticancer properties. Although studies have presented findings regarding the anticancer properties of chrysin, research on its molecular mechanisms of action remains largely insufficient. This research aimed to deeply investigate chrysin's effects on the breast cancer cell line, MDA-MB-231, in terms of proliferation, invasion, colony formation, and apoptosis. The XTT test results confirmed chrysin's cytotoxic effect on MDA-MB-231 cells, indicating a 48-hour IC50 value of 115.77 µM. Chrysin induced apoptosis in cells, as evidenced by Annexin V assay, and also reduced their colony-forming and invasion. Gene expression analyses showed elevated levels of APC, AXIN1, AXIN2, GSK3A, GSK3B, CK1α, CTNNB1, as well as apoptosis-related genes CASP3, -7, -9, and BAX. This increase was corroborated by the observed rise in protein levels of caspase 3/7 and GSK3B. Moreover, molecular docking results showed that chrysin interacted with genes in the WNT/β-catenin pathway and exhibited drug-like ADME properties. In conclusion, chrysin exhibits potential anticancer effects against MDA-MB-231 cells. It is hoped that these findings will advance preclinical and clinical studies on chrysin's potential in breast cancer treatment.

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Chrysin a promising anticancer agent: recent perspectives

Cited by 12 publications

References 119 publications

REST-dependent downregulation of von Hippel-Lindau tumor suppressor promotes autophagy in SHH-medulloblastoma

REST-dependent downregulation of von Hippel-Lindau tumor suppressor promotes autophagy in SHH-medulloblastoma

Optimizing Chrysin’s Anticancer Efficacy on MDA-MB-231 Cells: Synthesis and Characterization of Chrysin-Loaded Gold/Chitosan Nanoparticles

Chrysin Mediates the Induction of Apoptosis in Breast Cancer Cells via the Inhibition of the WNT/β-Catenin Signaling Pathway

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