Protective effects of xanthohumol against the genotoxicity of benzo(a)pyrene (BaP), 2-amino-3-methylimidazo[4,5-f]quinoline (IQ) and tert-butyl hydroperoxide (t-BOOH) in HepG2 human hepatoma cells

Plazar, Janja; Žegura, Bojana; Lah, Tamara T.; Filipič, Metka

doi:10.1016/j.mrgentox.2007.03.013

Cited by 68 publications

(52 citation statements)

References 42 publications

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“…Similarly, according to the literature 3 , as xanthohumol is known to be an effective inhibitor of cytochrome P450 enzymes, our results display that synergism of all of the components in an extract have different influence with different enzymes. Up to this time, proteases, tyrosinase and -lactamase enzymes have not studied yet for H. lupulus plant, whereas, applications of these enzymes are widely used and new inhibitors need to be find out.…”

Section: Discussionsupporting

confidence: 87%

“…Until now, in vitro assays of bioactive components of Humulus lupulus as chemopreventive agents have been studied by many researchers [1][2][3][4] . Among main components, xanthohumol (XH) has received the major attention because it appears to inhibit of initiation, promotion and progression stages of carcinogenesis in vitro, so appearing as a broad-spectrum chemopreventive agent [5][6][7] .…”

Section: Introductionmentioning

confidence: 99%

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Antiproliferative activity ofHumulus lupulusextracts on human hepatoma (Hep3B), colon (HT-29) cancer cells and proteases, tyrosinase,β-lactamase enzyme inhibition studies

Önder

Türkoğlu

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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The aims of this study were to examine the antiproliferation of Humulus lupulus extracts on human hepatoma carcinoma (Hep3B) and human colon carcinoma (HT-29) cell lines along with enzyme inhibitory effects of the crude extracts. Potential cell cytotoxicity of six different H. lupulus extracts were assayed on various cancer cells using MTT assay at 24, 48 and 72 h intervals. Methanol-1 extract has inhibited the cell proliferation with doses of 0.6-1 mg/mL in a time dependent (48 and 72 hours) manner in Hep3B cells with 70% inhibition, while inhibitory effect was not seen in colon cancer cells. Acetone extract has increased the cell proliferation at low doses of 0.1 mg/mL for 72 h in Hep3B cells and 0.1-0.2 mg/mL for 48 and 72 h in HT29 cells. The inhibitory effects of the extracts were compared by relative maximum activity values (V max ) using proteases such as -chymotrypsin, trypsin and papain, tyrosinase and -lactamase (penicillinase).

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Section: Discussionsupporting

confidence: 87%

Section: Introductionmentioning

confidence: 99%

Antiproliferative activity ofHumulus lupulusextracts on human hepatoma (Hep3B), colon (HT-29) cancer cells and proteases, tyrosinase,β-lactamase enzyme inhibition studies

Önder

Türkoğlu

et al. 2015

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…4 Flavonoid 1 displays these structural specificities, and, indeed, the high antioxidant potential of this compound was recently published in vitro. 12,13 The ability of compound 1 to scavenge superoxide radical was evaluated by chemiluminescence measurement using a xanthine/xanthine oxidase assay. Compound 1 ( Figure 1A,B) Figure 1C) showed significant fluorescence reduction (to 71.9 ( 9.2%), in comparison to the corresponding control.…”

Section: Resultsmentioning

confidence: 99%

Antioxidant Effects of Xanthohumol and Functional Impact on Hepatic Ischemia−Reperfusion Injury

et al. 2009

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Therapeutic effects of dietary flavonoids have been attributed mainly to their antioxidant capacity. Xanthohumol (1), a prominent flavonoid of the hop plant, Humulus lupulus, was investigated for its antioxidant potential and for its effect on NF-κB activation. To examine the biological relevance of 1, a hepatic ischemia/reperfusion model was chosen as a widely accepted model of oxidative stress generation. The impact of 1 on endogenous antioxidant systems, on the NF-κB signal transduction pathway as well as on apoptotic parameters, and on hepatic tissue damage was evaluated. Compound 1 markedly decreased the level of reactive oxygen species in vitro. Furthermore, levels of enzymatic and nonenzymatic antioxidants were restored after pretreatment in postischemic hepatic tissue, and lipid peroxidation was attenuated. NF-κB activity was reduced in vitro as well as in hepatic tissue after ischemia/reperfusion upon pretreatment with 1. In addition, the phosphorylation of Akt was markedly inhibited. Surprisingly, 1 decreased the expression of the antiapoptotic protein Bcl-X and increased caspase-3 like-activity, a proapoptotic parameter. Moreover, hepatic tissue damage as well as TNF-α levels increased in xanthohumol-pretreated liver tissue after ischemia/reperfusion. In summary, xanthohumol did not protect against ischemia/reperfusion injury in rat liver, despite its antioxidant and NF-κB inhibitory properties.

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“…Chemically, XH belongs to the prenylated chalcones (open C-ring flavonoids) class, and is the main prenylflavonoid of hops (0.1-1% on dry weight) (Stevens and Page, 2004). XH is an antioxidant (Miranda et al, 2000) and a broadspectrum cancer chemopreventive agent that prevents carcinogenesis in the initiation, promotion, and progression phase (Gerhauser et al, 2002;Pan et al, 2005;Plazar et al, 2007). It also inhibits adipogenesis (Yang et al, 2007) and osteoporosis (Tobe et al, 1997), and potentially influences AIDS (Wang et al, 2004) and malaria (Frolich et al, 2005), at least in vitro.…”

Section: Introductionmentioning

confidence: 99%

Effect of xanthohumol on melanogenesis in B16 melanoma cells

et al. 2008

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Xanthohumol (XH), the principal prenylflavonoid of the hop plant (Humulus lupulus L.), dose-dependently inhibited isobutylmethylxanthine (IBMX)-induced melanogenesis in B16 melanoma cells, with little cytotoxicity at the effective concentrations. Decreased melanin content was accompanied by reduced tyrosinase enzyme activity, protein and mRNA expression. The levels of tyrosinase-related protein 1 and 2 mRNAs were decreased by XH. XH also inhibited α-melanocyte stimulating hormone-or forskolin-induced increases in melanogenesis, suggesting an action on the cAMP-dependent melanogenic pathway. XH downregulated the protein and mRNA expression of microphthalmia-associated transcription factor (MITF), a master transcriptional regulator of key melanogenic enzymes. These results suggest that XH might act as a hypo-pigmenting agent through the downregulation of MITF in the cAMP-dependent melanogenic pathway.

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Protective effects of xanthohumol against the genotoxicity of benzo(a)pyrene (BaP), 2-amino-3-methylimidazo[4,5-f]quinoline (IQ) and tert-butyl hydroperoxide (t-BOOH) in HepG2 human hepatoma cells

Cited by 68 publications

References 42 publications

Antiproliferative activity ofHumulus lupulusextracts on human hepatoma (Hep3B), colon (HT-29) cancer cells and proteases, tyrosinase,β-lactamase enzyme inhibition studies

Antiproliferative activity ofHumulus lupulusextracts on human hepatoma (Hep3B), colon (HT-29) cancer cells and proteases, tyrosinase,β-lactamase enzyme inhibition studies

Antioxidant Effects of Xanthohumol and Functional Impact on Hepatic Ischemia−Reperfusion Injury

Effect of xanthohumol on melanogenesis in B16 melanoma cells

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