Structure Antimutagenicity Relationship of Anthraquinones

Mohammed, Magdy M D

doi:10.4172/2329-6836.1000228

Cited by 5 publications

(5 citation statements)

References 79 publications

(112 reference statements)

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“…Anthraquinones have antimutagenic and anticarcinogenic activities. In addition, emodin, chrysophanol, and rhein have inhibitory effects on benzo[α]pyrene-mediated DNA damage in the HepG2 hepatoma cell line [25]. Nevertheless, in this study, emodin, chrysophanol, and rhein showed effects that are antagonistic to endoxifen's action on MCF-7 and ZR-75-1 breast cancer cell lines.…”

Section: Discussionmentioning

confidence: 60%

Inhibition of tamoxifen's therapeutic effects by emodin in estrogen receptor-positive breast cancer cell lines

et al. 2019

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PurposeThis study was aimed to investigate the combination effect of endoxifen and emodin on estrogen receptor (ER) positive breast cancer cell lines and to explain the mechanism of the combination effect.MethodsWe conducted this study on MCF-7 (ER+/human epidermal growth factor receptor-2 [HER2]−), T47D (ER+/HER2−), ZR-75-1 (ER+/HER2+), and BT474 (ER+/HER2+) cell lines, which confirmed combination effect of endoxifen and emodin. Optimal concentrations for combination were determined to study the effects on proliferation of MCF-7 and ZR-75-1 cells. Analysis of the combination effect was carried out in the CompuSyn software. The combination of downstream mechanisms, and combined effects of other similar compounds were tested on the MCF-7 and ZR 75-1 cell lines. Protein expression was confirmed by western blot.ResultsThe combination of endoxifen and emodin had antagonistic effects on MCF-7 and ZR-75-1cell lines (combination index > 1). We validated the antagonistic effect in T47D and BT474 cell lines. During the combined treatment, the results showed elevated amounts of cyclin D1 and phosphorylated extracellular signal-regulated kinase (pERK). Analysis of drug interactions showed antagonistic effect between endoxifen and chemical compounds similar to emodin, such as chrysophanol or rhein, in MCF-7 and ZR-75-1 cells.ConclusionAddition of emodin attenuated tamoxifen's treatment effect via cyclin D1 and pERK up-regulation in ER-positive breast cancer cell lines.

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Section: Discussionmentioning

confidence: 60%

Inhibition of tamoxifen's therapeutic effects by emodin in estrogen receptor-positive breast cancer cell lines

et al. 2019

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“…However, when all antimutagenicity data were evaluated together, it was found that the presence of −CH 3 , and chloride (−Cl) substitutions at C1 did not always enhance the antimutagenic activity of 4‐TZD compounds (Table 2). This underlines that both the number, and the position of these groups are important for the antimutagenicity of 4‐TZDs [45] …”

Section: Resultsmentioning

confidence: 72%

“…This underlines that both the number, and the position of these groups are important for the antimutagenicity of 4-TZDs. [45] From a biological perspective, NaN 3 , NPDA, and 9-AA are direct-acting mutagens, and some of the newly synthesized 4-TZDs show significant antimutagenic activity against each of these mutagens (Table 2). The mutagenicity of NaN 3 is due to the production of an organic metabolite (L-azidoalanine) that enters the nucleus, and interacts with DNA, causing point mutations in the genome.…”

Section: Mutagenic and Antimutagenic Effects Of C1-c10mentioning

confidence: 99%

In Vitro Genotoxic and Antigenotoxic Effects of Ten Novel Synthesized 4‐Thiazolidinone Derivatives

Alaylar,

Güllüce,

Turhan

et al. 2023

Chemistry & Biodiversity

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Heterocyclic compounds are found in a variety of drug molecules, and bioactive natural products. 4‐Thiazolidinones (4‐TZDs), which represent an important class of heterocyclic compounds, are of great interest today with their diverse bioactivities. In this study, ten novel 4‐TZD derivatives (C1–C10) were synthesized, characterized by spectroscopic techniques, and their genotoxic, and antigenotoxic properties were investigated in vitro using the Ames Salmonella/microsome mutagenicity assay in the concentration range of 0.2–1.0 mM/plate. The results revealed that none of the compounds were mutagenic on the three different Salmonella typhimurium strains up to the highest concentration tested. Furthermore, in our study, C1, C4, C6, and C9 showed significant, ranging from moderate to strong, antigenotoxic effects against mutagen‐induced DNA damage at relatively higher doses. Among these, C4 had the best potential to inhibit the number of revertant colonies induced by 9‐aminoacridine (9‐AA), with a maximum inhibition rate of 47.9 % for 1.0 mM/plate. As a result, preliminary knowledge about the safety of the use of ten novel synthesized 4‐TZD compounds likely to exhibit many bioactivities was obtained in this study. In addition, the significant in vitro antimutagenic activity of some derivatives increases the importance of studies for the development of new pharmacological agents for cancer prevention.

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“…The increase reactive oxygen species formation is linked to the binding of the α, β‐unsaturated carbonyl functional group of the AQs to the sulfhydryl (‐SH) group of proteins, resulting to cellular stress (Guin, Das, & Mandal, ). The degree of AQs toxicity depends mostly on the type of the substituents attached to the main anthracene as slight structural changes can lead to reduce or increase toxicity (Mohammed, ).…”

Section: Resultsmentioning

confidence: 99%

Antidiabetic potential of anthraquinones: A review

Mohammed

Ibrahim

Tajuddeen

et al. 2019

Phytotherapy Research

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The present study was designed to review the antidiabetic potential of anthraquinones (AQs) with emphasis on the extent of blood glucose reduction, the half maximal inhibitory concentration values (in vitro studies), the proposed mechanisms of action, and the structure activity relationship studies. We sourced relevant data from the major scientific databases (Pubmed, Science Direct, Medline, and Google Scholar). According to our search, 25 AQs have shown variable antidiabetic potential, whereas one AQ (morindone‐6‐O‐β‐D‐primeveroside) showed no blood glucose‐lowering ability. Emodin and rhein showed the most promising antidiabetic potential in various models. The proposed mechanisms of antidiabetic action include upregulation of insulin receptor substrates‐1, phosphoinositide‐3‐kinase, and Akt‐ser473 expression and elevation of glucagon‐like peptide‐1 level in diabetic animal models linked to the potent protein tyrosine phosphatase 1B and dipeptidyl peptidase‐4 inhibitions. In addition, activation of peroxisome proliferator‐activated receptors gamma and inhibition of α‐glucosidase activity are other possible targets proposed as the mechanism of AQs antidiabetic action. The position and the number of hydroxyl group showed great influence on the overall antidiabetic potential of AQs. AQs hold promising antidiabetic activity despite scanty information. We hope that the present study will serve as a template to further explore the antidiabetic potential of AQs and subsequent antidiabetic drug development.

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Structure Antimutagenicity Relationship of Anthraquinones

Cited by 5 publications

References 79 publications

Inhibition of tamoxifen's therapeutic effects by emodin in estrogen receptor-positive breast cancer cell lines

Inhibition of tamoxifen's therapeutic effects by emodin in estrogen receptor-positive breast cancer cell lines

In Vitro Genotoxic and Antigenotoxic Effects of Ten Novel Synthesized 4‐Thiazolidinone Derivatives

Antidiabetic potential of anthraquinones: A review

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