Chemopreventive potential of 3-[2,6-bis(4-fluorophenyl)-3-methylpiperidin-4-ylideneamino]-2-thioxoimidazolidin-4-one on 7,12-dimethylbenz[a]anthracene (DMBA) induced hamster buccal pouch carcinogenesis

Thanusu, J.; Kanagarajan, V.; Nagini, Siddavaram; Gopalakrishnan, Mahesh

doi:10.3109/14756361003724786

Cited by 8 publications

(4 citation statements)

References 48 publications

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“…Enzymatic antioxidants (SOD, CAT and GPx) and non-enzymatic antioxidants (GSH and vitamin E) play prominent role in the protection of tissues against ROS mediated oxidative damage. Diminished activities of plasma GPx, SOD and CAT and plasma GSH and vitamin E levels were reported in various forms of cancers including oral cancer (Thanusu et al, 2010;Silvan et al, 2011). Our results corroborate these observations.…”

Section: Discussionsupporting

confidence: 82%

Anti-tumor Initiating Potential of Andrographolide in 7,12-dimethylbenz[a]anthracene Induced Hamster Buccal Pouch Carcinogenesis

Manoharan¹,

Singh²,

Suresh³

et al. 2012

Asian Pacific Journal of Cancer Prevention

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The aim of the study was to investigate the chemopreventive potential of andrographolide in 7,12-dimethylbenz(a) anthracene (DMBA)-induced hamster buccal pouch carcinogenesis. Oral tumors developed in the buccal pouch of golden Syrian hamsters at a 100% incidence on painting with 0.5% DMBA in liquid paraffin three times a week for 14 weeks. Marked abnormalities in the status of detoxification enzymes, lipid perxodiation and antioxidants were noticed in hamsters treated with DMBA alone. Oral administration of andrographolide at a dose of 50 mg/ kg bw to hamsters treated with DMBA not only completely prevented the tumor formation but also restored the status of the above mentioned biomarkers. The present study thus demonstrates the chemopreventive potential of andrographolide in DMBA-induced hamster buccal pouch carcinogenesis, which is probably due to its antioxidant potential as well as modulating effect on xenobiotic metabolising enzymes during DMBA-induced oral carcinogenesis.

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Section: Discussionsupporting

confidence: 82%

Anti-tumor Initiating Potential of Andrographolide in 7,12-dimethylbenz[a]anthracene Induced Hamster Buccal Pouch Carcinogenesis

Manoharan¹,

Singh²,

Suresh³

et al. 2012

Asian Pacific Journal of Cancer Prevention

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“…Chemical compounds with 2-thioxoimidazolidinone or 2-acetamidoacrylate moiety showed anti-cancer effects in previous studies 17 – 20 . Newly synthesized β-phenylacrylic acid derivatives, MHYs, also contain 2-thioxoimidazolidinone or 2-acetamidoacrylate moiety, respectively, suggesting these compounds may exert anti-cancer activity (Fig.…”

Section: Resultsmentioning

confidence: 94%

“…Previous studies showed that thioxoimidazolidinone derivatives exerted chemopreventive potential on hamster buccal pouch carcinogenesis and a potent anti-cancer activity to prostate cancer cells 17 , 18 . Furthermore, ethyl pyruvate and its functional analog 2-acetamidoacrylate inhibited tumor growth in mice 19 .…”

Section: Introductionmentioning

confidence: 99%

Novel β-phenylacrylic acid derivatives exert anti-cancer activity by inducing Src-mediated apoptosis in wild-type KRAS colon cancer

et al. 2018

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Many stress conditions including chemotherapy treatment is known to activate Src and under certain condition Src can induce the apoptotic signal via c-Jun N-terminal kinase (JNK) activation. Here we report that the newly synthesized β-phenylacrylic acid derivatives, MHY791 and MHY1036 (MHYs), bind to epidermal growth factor receptor (EGFR) tyrosine kinase domains and function as EGFR inhibitors, having anti-cancer activities selectively in wild-type KRAS colon cancer. Mechanistically, MHYs-induced Src/JNK activation which enhanced their pro-apoptotic effects and therefore inhibition of Src by the chemical inhibitor PP2 or Src siRNA abolished the response. In addition, MHYs generated reactive oxygen species and increased ER stress, and pretreatment with antioxidant-inhibited MHY-induced ER stress, Src activation, and apoptosis. Furthermore, the irreversible EGFR inhibitor PD168393 also activated Src while the reversible EGFR inhibitor gefitinib showed the opposite effect, indicating that MHYs are the irreversible EGFR inhibitor. Collectively, Src can play a key role in apoptosis induced by the novel EGFR inhibitor MHYs, suggesting that activation of Src might prove effective in treating EGFR/wild-type KRAS colon cancer.

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“…Several studies have been conducted to determine the therapeutic dose and also to determine their IC 50 on a variety of cancer cells. 24 In this study, we determined viability rates and IC 50 on cancer cells. The results of these study showed that the viability rate of the cells in the control group was highest, which is 100%.…”

Section: Figure 3 Cells Viability Percent In Different Concentrations Of 2-thioxo Imidazolidin-4-onesmentioning

confidence: 99%

The Effect of 2-Thioxo Imidazolidin-4-Ones (2- Thiohydantion) on Anticancer Activity: An in Vitro Study

2020

IJFMT

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Background and Purpose: Cancer is one of the most common factors of death in society today. Despite much research into cancer and its treatment, it is still one of the greatest health problems. The biggest obstacle to cancer treatment is that they are inherently resistant to chemotherapy or become drug resistant during treatment. For this reason, researchers around the world have made great efforts to identify new natural or synthetic compounds with anticancer properties. So the aim of this study is to find out the effect of 2-Thioxo imidazolidin-4-ones (2-Thiohydantion) on anticancer activity. Materials and Methods:Imidazoles are compounds that have antibacterial, antifungal and antitumor properties in many studies. Through the results of this study, we discovered effectiveness of the new compound of 2-Thioxo imidazolidin-4-ones (2 Thiohydantion) as an anticancer agent against a cell line that is a cancer model system. To determine the IC 50 of this compound, we treated the cancer cells by different concentrations (10, 20, 30, 40, 80 and 160 μg / ml) and then the cells were evaluated by MTT assay after 24 and 48 hour intervals.Results: After preparing the required compound, MTT assay showed that the IC 50 of 2-Thioxo imidazolidin-4-ones (2-Thiohydantion) compound on MCF7 cells, 135 and 40 μg / ml, respectively, after 24 and 48 h, respectively. In addition, the toxicity of these compounds on normal cells was evaluated, which is very different from their toxicity for cancer cells, and this is a very important feature. 2-Thioxo imidazolidin-4ones (2-Thiohydantion) has the ability to stimulate cell death in cancer cells, and these results provide new insights into the use of these compounds in cancer treatment. Conclusion:So 2-Thioxo imidazolidin-4-ones (2-Thiohydantion) at different concentrations significantly reduced the growth of cancer cells compared to the control group (50% inhibition of cell growth). Future studies will need to investigate the mechanism of this cytotoxicity as well as the possible anticancer effectiveness of this compound in vitro and in vivo.

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Chemopreventive potential of 3-[2,6-bis(4-fluorophenyl)-3-methylpiperidin-4-ylideneamino]-2-thioxoimidazolidin-4-one on 7,12-dimethylbenz[a]anthracene (DMBA) induced hamster buccal pouch carcinogenesis

Cited by 8 publications

References 48 publications

Anti-tumor Initiating Potential of Andrographolide in 7,12-dimethylbenz[a]anthracene Induced Hamster Buccal Pouch Carcinogenesis

Anti-tumor Initiating Potential of Andrographolide in 7,12-dimethylbenz[a]anthracene Induced Hamster Buccal Pouch Carcinogenesis

Novel β-phenylacrylic acid derivatives exert anti-cancer activity by inducing Src-mediated apoptosis in wild-type KRAS colon cancer

The Effect of 2-Thioxo Imidazolidin-4-Ones (2- Thiohydantion) on Anticancer Activity: An in Vitro Study

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