Synthesis of coumarin analogs appended with quinoline and thiazole moiety and their apoptogenic role against murine ascitic carcinoma

Prashanth, T.; Avin, B.R. Vijay; Thirusangu, Prabhu; Ranganatha, V. Lakshmi; Prabhakar, B.T.; Chandra, Joya; Khanum, Shaukath Ara

doi:10.1016/j.biopha.2019.108707

Cited by 46 publications

(15 citation statements)

References 35 publications

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“…EAC cells were provided by Dr. Prabhakar B.T (Molecular Biomedicine Laboratory, Post Graduate Department of Studies and Research in Biotechnology Sahyadri Science College Kuvempu University, Shimoga, Karnataka, India). Cell line phenotypes were confirmed and characterized annually for morphological and cell line specific markers as described previously [ 39 ].…”

Section: Methodsmentioning

confidence: 99%

Targeted Inhibition of Anti-Inflammatory Regulator Nrf2 Results in Breast Cancer Retardation In Vitro and In Vivo

et al. 2021

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Nuclear factor erythroid-2 related factor-2 (Nrf2) is an oxidative stress-response transcriptional activator that promotes carcinogenesis through metabolic reprogramming, tumor promoting inflammation, and therapeutic resistance. However, the extension of Nrf2 expression and its involvement in regulation of breast cancer (BC) responses to chemotherapy remain largely unclear. This study determined the expression of Nrf2 in BC tissues (n = 46) and cell lines (MDA-MB-453, MCF-7, MDA-MB-231, MDA-MB-468) with diverse phenotypes. Immunohistochemical (IHC)analysis indicated lower Nrf2 expression in normal breast tissues, compared to BC samples, although the difference was not found to be significant. However, pharmacological inhibition and siRNA-induced downregulation of Nrf2 were marked by decreased activity of NADPH quinone oxidoreductase 1 (NQO1), a direct target of Nrf2. Silenced or inhibited Nrf2 signaling resulted in reduced BC proliferation and migration, cell cycle arrest, activation of apoptosis, and sensitization of BC cells to cisplatin in vitro. Ehrlich Ascites Carcinoma (EAC) cells demonstrated elevated levels of Nrf2 and were further tested in experimental mouse models in vivo. Intraperitoneal administration of pharmacological Nrf2 inhibitor brusatol slowed tumor cell growth . Brusatol increased lymphocyte trafficking towards engrafted tumor tissue in vivo, suggesting activation of anti-cancer effects in tumor microenvironment. Further large-scale BC testing is needed to confirm Nrf2 marker and therapeutic capacities for chemo sensitization in drug resistant and advanced tumors.

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Section: Methodsmentioning

confidence: 99%

Targeted Inhibition of Anti-Inflammatory Regulator Nrf2 Results in Breast Cancer Retardation In Vitro and In Vivo

et al. 2021

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“…Thus, the results of Western-blot analysis demon strated that compounds 1 and 2 induce apoptosis in human leukemia HL-60 and K562 cells. and affected caspase activated DNase, and H2A histone family member X (γ-H2AX) in murine ascitic carcinoma cells [20]. Since the studied compounds in the leukemia cells increased the level of the mitochondrial pro-apoptotic proteins Bim protein (induces Bax/Bak oligomerization on mitochondria [4]) and EndoG (nuclease that specifically degrades the DNA), and decreased the level of the mitochondrial anti-apoptotic Bcl-2 protein, we suggest a mitochondria-dependent action of these compounds.…”

Section: Resultsmentioning

confidence: 99%

Apoptosis induction in human leukemia cells by novel 2-amino-5-benzylthiazole derivatives

Finiuk¹,

Ivasechko²,

Klyuchivska³

et al. 2019

Ukr.Biochem.J

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“…Blocking this natural defence mechanism allows for abnormal cellular proliferation and accumulation of genetic abnormalities, resulting in cancer and the frequent occurrence of medication resistance. 29 Apoptosis is a substantial path in anti-tumour drug response.…”

Section: Discussionmentioning

confidence: 99%

“…It also resulted in the release of cytochrome c from the mitochondria, which inhibits matrix metalloproteinase and translocates into the cytoplasm through the activation of caspase 9 and extracellular caspase 3. 33 Prashanth et al, 29 activation. 34 Our outcomes revealed that the average value of the concentra- and influencing cell invasion.…”

Section: Ta B L E 1mentioning

confidence: 99%

In vivo biological evaluation of sodium salt of ethyl (E)‐2‐cyano‐3‐(7‐hydroxy‐4‐methyl‐2‐oxoquinoline‐1(2H)‐yl)‐3‐(4‐hydroxyphenyl) acrylate as anticancer agent

Mohammed

El-Aziz

El‐Deen

et al. 2021

Clin Exp Pharma Physio

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Nowadays, quinoline scaffold is among the most vital construction compounds for the development of new drugs. The purpose of this research is to evaluate the anti-cancer activity of sodium salt of ethyl (E)-2-cyano-3-(7-hydroxy-4-methyl-2-oxoquinoline-1(2H)-yl)-3-(4-hydroxyphenyl) acrylate against Ehrlich ascites carcinoma (EAC) cells residing in female mice's peritoneal cavity. The docking study exhibited a favourable interaction between the compound and the receptors 1MOY and 3KJF of osteopontin and caspase 3, respectively. The compound's sodium salt showed potential antioxidant and anti-cancer effects against Ehrlich ascites carcinoma (EAC) cells in vivo.Herein, the results elucidated that treatment with the compound's sodium salt exerted significant chemopreventive and chemotherapeutic effects, which reduced both EAC cell volume and count. Our results revealed that treatment with the sodium salt of the compound demonstrated a remarkable in vivo apoptotic effect through elevation of the expression of caspase 3 and reduction of osteopontin levels. Histopathological examination confirmed that the compound's sodium salt improved liver and kidney tissues without any apparent adverse effects.

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Synthesis of coumarin analogs appended with quinoline and thiazole moiety and their apoptogenic role against murine ascitic carcinoma

Cited by 46 publications

References 35 publications

Targeted Inhibition of Anti-Inflammatory Regulator Nrf2 Results in Breast Cancer Retardation In Vitro and In Vivo

Targeted Inhibition of Anti-Inflammatory Regulator Nrf2 Results in Breast Cancer Retardation In Vitro and In Vivo

Apoptosis induction in human leukemia cells by novel 2-amino-5-benzylthiazole derivatives

In vivo biological evaluation of sodium salt of ethyl (E)‐2‐cyano‐3‐(7‐hydroxy‐4‐methyl‐2‐oxoquinoline‐1(2H)‐yl)‐3‐(4‐hydroxyphenyl) acrylate as anticancer agent

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