Antitumor Activity of Novel Azole compound against Ehrlich Ascites Carcinoma in Swiss Albino Mice

El-Ablack, Fawzia Z.; Hashem, Ahmed M.; Elgazzar, Usama Bhgat

doi:10.33552/icbc.2020.02.000510

Cited by 2 publications

(4 citation statements)

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“…Different mechanisms have been proposed for the antitumor action of the thiazole-based derivatives. It was reported that they acted as apoptosis inducers [6,21,25,29], affected inosine monophosphate dehydrogenase (IMPDH) [29], induced reactive oxygen species (ROS) production [30], inhibited lipid peroxidation and caused DNA damage [5]. In the present study, we investigated the effect of thiazole derivative BF1 and its complexes with poly(PEGMA-co-DMM) on the stability of DNA in human breast adenocarcinoma MDA-MB-231 cells.…”

Section: Discussionmentioning

confidence: 98%

“…The thiazole-based compounds were created for targeting pathological cells, including tumor cells [5][6][7][8][9][10][11][12]. However, these compounds are often not easy to use because they are not soluble in water and the mechanisms of their action are not known.…”

Section: Discussionmentioning

confidence: 99%

“…The thiazole derivatives are characterized by a wide range of biological activities (anticancer, antibacterial, antifungal, antiviral, anti-inflammatory, neuroprotective) [1,[5][6][7][8][9][10][11]. Anticancer activity was reported for tiazofurin, dasatinib, and a furan-thiazole hybrid [11,12].…”

Section: Introductionmentioning

confidence: 99%

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Effect of a novel thiazole derivative and its complex with a polymeric carrier on stability of DNA in human breast cancer cells

Finiuk¹,

Klyuchivska²,

Ivasechko³

et al. 2021

Ukr.Biochem.J

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thiazole derivatives are perspective antitumor compounds characterized by a broad range of bioactivity, while polymeric carriers are widely used to enhance the efficiency of biological action of drugs, improve their biocompatibility and water solubility. Previously, we identified that the thiazole-based derivative BF1 (N-(5-benzyl-1,3-thiazol-2-yl)-3,5-dimethyl-1-benzofuran-2-carboxamide) possessed differential toxicity towards targeted tumor cell lines. the aim of the present work was to investigate the action in vitro of BF1 and its complex with the polymeric carrier (PC) poly(PEGMA-co-DMM) (BF1-РС complex) towards human breast adenocarcinoma cells of the MDa-MB-231 and McF-7 lines. DNa comet analysis, diphenylamine DNa fragmentation assay, gel retardation assay of plasmid DNa, DNa intercalation assay using methyl green dye and fluorescent microscopy were used to study the effects of BF1 on DNA stability in breast cancer cells. The ІС 50 of cytotoxic action towards MDA-MB-231 cells was 26.5 ± 2.9 µМ for BF1, while the ІС 50 for the BF1-PC complex was 6.9 ± 0.4 µМ, and the PC demonstrated low toxicity (ІС 50 ˃ 50 µМ). The BF1-PC complex possessed higher toxicity towards MCF-7 cells than free BF1, with ІС 50 of 9.6 ± 0.8 µМ and 15.8 ± 0.9 µМ, respectively. BF1 and BF1-pc induced an increase in the number of damaged cells of the MDa-MB-231 line with blebbing of plasma membrane, condensed chromatin and/or fragmented nucleus and micronuclei formation. Both BF1 and the BF1-pc complex induced single-strand breaks in DNa and its fragmentation in treated MDa-MB-231 cells. the studied compounds were not bound to plasmid DNa and did not intercalate into DNa molecules.

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Section: Discussionmentioning

confidence: 98%

Section: Discussionmentioning

confidence: 99%

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Effect of a novel thiazole derivative and its complex with a polymeric carrier on stability of DNA in human breast cancer cells

Finiuk¹,

Klyuchivska²,

Ivasechko³

et al. 2021

Ukr.Biochem.J

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“…To the best of our understanding and knowledge, EAC inhibition by geraniol is the first report by our group. However, in the recent past, it has been reported that thiazole derivative decreases the number of EAC tumor cells by 75%, 62.5%, 45% at 75, 50, and 25 mg/kg of body weight respectively, whereas cisplatin reduced the number tumor cells upto 85% at 10 mg/kg of body weight (ELAblack, Elgazzar, & Hashem, 2020). Further, sildenafil and cisplatin reduced the Ehrlich tumor volume by 30.4% and 58.8% at 5 and 7.5 mg/kg of body weight, respectively (El‐Naa, Othman, & Younes, 2016).…”

Section: Discussionmentioning

confidence: 99%

Geraniol exerts its antiproliferative action by modulating molecular targets in lung and skin carcinoma cells

Fatima

Wani

Meena

et al. 2021

Phytotherapy Research

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Geraniol, an acyclic monoterpene present in several plant species' essential oils, is utilized as a food additive. It possesses potent antiproliferative and antitumor effects ascribed to its antiinflammatory, and antioxidant properties. The study aimed to understand geraniol's mechanism in human lung and skin cancer cells by employing molecular and cell target-based assays. SRB, NRU, MTT assays, qRT-PCR, molecular docking, and EAC model were used. Geraniol inhibits the proliferation of PC-3, A431, and A549 cells (~50%) and suppresses the activity of ornithine decarboxylase (15.42 ± 0.61 μM) and hyaluronidase (57.61 ± 8.53 μM) in A549 cells; LOX-5 (25.44 ± 3.50 μM) and hyaluronidase (90.71 ± 2.38 μM) in A431 cells. The qRT-expression analysis of the targeted gene depicts non-significant change at the transcriptional level of LOX-5 in A431 cells.A robust binding interaction of geraniol with molecular targets was observed in the molecular docking studies. In Ehrlich Ascites Carcinoma model, geraniol inhibit tumor growth by 50.08% at 75 mg/kg bw and was found to be safe up to 1,000 mg/kg bw in a toxicity study. Geraniol has two prenyl units allied head-to-tail and functionalized with one hydroxyl group at its tail end could be responsible for the antiproliferative activity. These observations provide evidence for geraniol to be used as a new prototype to develop a novel anticancer agent.

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Antitumor Activity of Novel Azole compound against Ehrlich Ascites Carcinoma in Swiss Albino Mice

Cited by 2 publications

References 0 publications

Effect of a novel thiazole derivative and its complex with a polymeric carrier on stability of DNA in human breast cancer cells

Effect of a novel thiazole derivative and its complex with a polymeric carrier on stability of DNA in human breast cancer cells

Geraniol exerts its antiproliferative action by modulating molecular targets in lung and skin carcinoma cells

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