Hydroquinone Exhibits In Vitro and In Vivo Anti-Cancer Activity in Cancer Cells and Mice

Abstract

Hydroquinone (HQ, 1,4-benzenediol) is a hydroxylated benzene metabolite with various biological activities, including anti-oxidative, neuroprotective, immunomodulatory, and anti-inflammatory functions. However, the anti-cancer activity of HQ is not well understood. In this study, the in vitro and in vivo anti-cancer activity of HQ was investigated in various cancer cells and tumor-bearing mouse models. HQ significantly induced the death of A431, SYF, B16F10, and MDA-MB-231 cells and also showed a synergistic effect on A431 cell death with other anti-cancer agents, such as adenosine-2′,3′-dialdehyde and buthionine sulfoximine. In addition, HQ suppressed angiogenesis in fertilized chicken embryos. Moreover, HQ prevented lung metastasis of melanoma cells in mice in a dose-dependent manner without toxicity and adverse effects. HQ (10 mg/kg) also suppressed the generation of colon and reduced the thickness of colon tissues in azoxymethane/dextran sodium sulfate-injected mice. This study strongly suggests that HQ possesses in vitro and in vivo anti-cancer activity and provides evidence that HQ could be developed as an effective and safe anti-cancer drug.

Synthesis and Antitumor Activity Evaluation of Compounds Based on Toluquinol

“…At first sight, they clearly indicate a relevant role of the methyl group of toluquinol in the cytotoxic activity of this compound, since compounds lacking this methyl group ( 2 – 7 ) exhibited significantly increased IC 50 values for all the tested cell lines. In this regard, substitution of the methyl group of toluquinol by a trifluoromethyl group (compound 2 ) caused a 6- to 30-fold increase in the IC 50 values for all the cell types, approaching the recently reported IC 50 values for 1,4-hydroquinone in tumor cell lines [15]. These results are also in agreement with our previous results showing that substitution of the methyl group of toluquinol with either a carboxylic acid (as in gentisic acid) or a sulfonic acid (as in calcium dobesilate) provoked a notable decrease in the growth inhibitory activity of the compounds, as deduced from the higher IC 50 values obtained for them in endothelial and tumor cells [6].…”

Structural and In Silico Characterization of Small Molecules Isolated from Eichhornia crassipes

“…Benzene-1,4-diol (compound 1) and nonanedioic acid (compound 2) possess various bioactive properties. Benzene-1,4-diol (1) has anticancer activities against various Evidence-Based Complementary and Alternative Medicine cells [20]. Its derivatives such as hydroquinone 5-O-cinnamoyl ester and some alkyl and prenylated derivatives have also been reported to have cytotoxic activities against lung cancer [20][21][22], meaning that more optimization of the compound has a potential to develop more drug lead options against cancers.…”

“…Benzene-1,4-diol (1) has anticancer activities against various Evidence-Based Complementary and Alternative Medicine cells [20]. Its derivatives such as hydroquinone 5-O-cinnamoyl ester and some alkyl and prenylated derivatives have also been reported to have cytotoxic activities against lung cancer [20][21][22], meaning that more optimization of the compound has a potential to develop more drug lead options against cancers. Nonanedioic acid (2) has antitumor properties in humans [23], antineoplastic and antileukemic activities [24], immunoregulatory and antiproliferative activities against cancer cells [25,26], and cytotoxic activities and anti-inflammatory and antioxidant activities [27].…”

Bifidobacterium β-Glucosidase Activity and Fermentation of Dietary Plant Glucosides Is Species and Strain Specific

“…increased the bioavailability of acylglycones. Hydroquinone has been linked to anticancer activity in vitro and in vivo [ 36 ] and has been shown to confer antimycobacterial and antileishmanial activity in vitro [ 37 ].…”