<i>Retracted</i>: Curcumin derivative L6H4 inhibits proliferation and invasion of gastric cancer cell line BGC‐823

Mu, Jianfeng; Wang, Xiaodong; Dong, Lihua; Sun, Peng

doi:10.1002/jcb.27542

Cited by 15 publications

(9 citation statements)

References 24 publications

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“…In 2018, Mu et al tested the antiproliferative activity of compound L6H4 ( 22 , Figure 5 ) on gastric BGC-823 cancer cells [ 46 ]. The authors concluded that 22 was able to inhibit cell proliferation by inducing apoptosis and enhancing the expression levels of p53, p21, Bax, and Bcl-2, both in vitro and in vivo.…”

Section: Interference With P53 Pathway By Synthetic Chalconesmentioning

confidence: 99%

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Chalcones as Promising Antitumor Agents by Targeting the p53 Pathway: An Overview and New Insights in Drug-Likeness

et al. 2021

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The p53 protein is one of the most important tumor suppressors that are frequently inactivated in cancer cells. This inactivation occurs either because the TP53 gene is mutated or deleted, or due to the p53 protein inhibition by endogenous negative regulators, particularly murine double minute (MDM)2. Therefore, the reestablishment of p53 activity has received great attention concerning the discovery of new cancer therapeutics. Chalcones are naturally occurring compounds widely described as potential antitumor agents through several mechanisms, including those involving the p53 pathway. The inhibitory effect of these compounds in the interaction between p53 and MDM2 has also been recognized, with this effect associated with binding to a subsite of the p53 binding cleft of MDM2. In this work, a literature review of natural and synthetic chalcones and their analogues potentially interfering with p53 pathway is presented. Moreover, in silico studies of drug-likeness of chalcones recognized as p53–MDM2 interaction inhibitors were accomplished considering molecular descriptors, biophysiochemical properties, and pharmacokinetic parameters in comparison with those from p53–MDM2 in clinical trials. With this review, we expect to guide the design of new and more effective chalcones targeting the p53 pathway.

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Section: Interference With P53 Pathway By Synthetic Chalconesmentioning

confidence: 99%

“…The expression of p53 was increased at 10 µM L6H4 ( 22 ) after 48 h in in vitro assays. On the other hand, in vivo studies on male BALB/c nude mice showed an increase of p53 levels after treatment with 15 µM L6H4 ( 22 ) for 48 h [ 46 ].…”

Section: Interference With P53 Pathway By Synthetic Chalconesmentioning

confidence: 99%

Chalcones as Promising Antitumor Agents by Targeting the p53 Pathway: An Overview and New Insights in Drug-Likeness

et al. 2021

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“…Many studies showed that curcumin has anti-oxidation, anti-growth, antiarthritic and anti-inflammation actions [ 6 ]. In particular, it has been reported that curcumin induces apoptosis, inhibits cell proliferation and migration in human leukemia, colon, prostate, renal and non-small-cell lung cancer [ 7 – 9 ], suggesting that it might be a novel agent for the prevention and treatment of ESCC.…”

Section: Introductionmentioning

confidence: 99%

The natural polyphenol curcumin induces apoptosis by suppressing STAT3 signaling in esophageal squamous cell carcinoma

Liu

Wang

Zeng

et al. 2018

J Exp Clin Cancer Res

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BackgroundWe and others have previously shown that the STAT3 signaling pathway is activated in some esophageal squamous cell carcinoma (ESCC) cells and is required for the survival and growth of these primary ESCC-derived xenografts. It has also been shown that the natural polyphenol curcumin is an effective anti-tumor agent.MethodsLuciferase assay and immunoblotting were performed to examine whether curcumin suppressed STAT3 signaling. CCK-8 assay and xenografts were utilized for analyzing ESCC cell growth in culture and mice. Soft agar assay was carried out to determine the colony formation ability of ESCC cells in the presence or absence of curcumin. Cell death and cell cycle were assessed by In CELL Analyzer 2000. Immunohistochemistry and TUNEL assay were used for detecting apoptosis in ESCC tisuses. Molecular docking was performed to evaluate the interaction of curcumin with JAK2. JAK2 activity was assessed using an in vitro cell-free system. HE staining was used to evaluate the ESCC tissues.ResultsThe natural polyphenol curcumin inhibited STAT3 phosphorylation rapidly and blocked STAT3-mediated signaling in ESCC cells. It also induced growth arrest and apoptosis in cultured ESCC cells, which were attenuated by enforced expression of STAT3. Furthermore, curcumin preferentially blocked the growth of primary ESCC-derived xenografts that harbored activated STAT3.ConclusionsCurcumin is able to exert anti-tumor action through inhibiting the STAT3 signaling pathway. Giving its wide use in traditional medicines with low toxicity and few adverse reactions, it is conceivable that curcumin might be further explored as a unique STAT3 inhibitor for anti-cancer therapies.

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“…Therefore, application of curcumin Light might be an innovative concept to accompany established RCC treatment protocols. The relevance of curcumin alone to act on tumor cell invasion has already been shown on other tumor entities, whereby curcumin concentrations of 10 µM, 15 µM, 50 µM, or higher have been applied to stop invasion of gastric [37], breast [38], prostate [39], or hepatic cancer cells [40]. Ongoing experiments should, therefore, deal with the question of whether the beneficial effects of light exposure on curcumin may also hold true for these tumor types.…”

Section: Discussionmentioning

confidence: 91%

Low Dosed Curcumin Combined with Visible Light Exposure Inhibits Renal Cell Carcinoma Metastatic Behavior in Vitros

Rutz

Maxeiner

Justin

et al. 2020

Cancers

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Recent documentation shows that a curcumin-induced growth arrest of renal cell carcinoma (RCC) cells can be amplified by visible light. This study was designed to investigate whether this strategy may also contribute to blocking metastatic progression of RCC. Low dosed curcumin (0.2 µg/mL; 0.54 µM) was applied to A498, Caki1, or KTCTL-26 cells for 1 h, followed by exposure to visible light for 5 min (400–550 nm, 5500 lx). Adhesion to human vascular endothelial cells or immobilized collagen was then evaluated. The influence of curcumin on chemotaxis and migration was also investigated, as well as curcumin induced alterations of α and β integrin expression. Curcumin without light exposure or light exposure without curcumin induced no alterations, whereas curcumin plus light significantly inhibited RCC adhesion, migration, and chemotaxis. This was associated with a distinct reduction of α3, α5, β1, and β3 integrins in all cell lines. Separate blocking of each of these integrin subtypes led to significant modification of tumor cell adhesion and chemotactic behavior. Combining low dosed curcumin with light considerably suppressed RCC binding activity and chemotactic movement and was associated with lowered integrin α and β subtypes. Therefore, curcumin combined with visible light holds promise for inhibiting metastatic processes in RCC.

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Retracted: Curcumin derivative L6H4 inhibits proliferation and invasion of gastric cancer cell line BGC‐823

Cited by 15 publications

References 24 publications

Chalcones as Promising Antitumor Agents by Targeting the p53 Pathway: An Overview and New Insights in Drug-Likeness

Chalcones as Promising Antitumor Agents by Targeting the p53 Pathway: An Overview and New Insights in Drug-Likeness

The natural polyphenol curcumin induces apoptosis by suppressing STAT3 signaling in esophageal squamous cell carcinoma

Low Dosed Curcumin Combined with Visible Light Exposure Inhibits Renal Cell Carcinoma Metastatic Behavior in Vitros

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