Inhibitory effects of indirubin‐3′‐monoxime against human osteosarcoma

Zhang, Yi; Song, Lu; Li, Jiazhen; Zhang, Yan; Lu, Xin; Zhang, Bin

doi:10.1002/iub.2058

Cited by 9 publications

(3 citation statements)

References 41 publications

(88 reference statements)

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“…In addition, it has an enhanced anti-proliferative and pro-apoptotic effect. Regarding the metastatic potential of cancer, I3M led to decreased cell migration and invasion 13 , 30 , 31 . The inhibitory effect of I3M on tumour proliferation has also been studied in vivo.…”

Section: Discussionmentioning

confidence: 99%

“…However, indirubin promotes the expression of the thrombopoietin receptor, a transmembrane protein, in peripheral blood mononuclear cells 41 . The structure of the cell membrane and extracellular matrix could also be altered via mechanisms that influence cancer cell migration and invasion 31 , with implications for impedance measurement and hence adhesion capacity values.…”

Section: Discussionmentioning

confidence: 99%

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Synergistic effect of plasma-activated medium and novel indirubin derivatives on human skin cancer cells by activation of the AhR pathway

Rebl

Sawade

Hein

et al. 2022

Sci Rep

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Due to the increasing number of human skin cancers and the limited effectiveness of therapies, research into innovative therapeutic approaches is of enormous clinical interest. In recent years, the use of cold atmospheric pressure plasma has become increasingly important as anti-cancer therapy. The combination of plasma with small molecules offers the potential of an effective, tumour-specific, targeted therapy. The synthesised glycosylated and non glycosylated thia-analogous indirubin derivatives KD87 and KD88, respectively, were first to be investigated for their pharmaceutical efficacy in comparison with Indirubin-3'-monoxime (I3M) on human melanoma (A375) and squamous cell carcinoma (A431) cells. In combinatorial studies with plasma-activated medium (PAM) and KD87 we determined significantly decreased cell viability and cell adhesion. Cell cycle analyses revealed a marked G2/M arrest by PAM and a clear apoptotic effect by the glycosylated indirubin derivative KD87 in both cell lines and thus a synergistic anti-cancer effect. I3M had a pro-apoptotic effect only in A431 cells, so we hypothesize a different mode of action of the indirubin derivatives in the two skin cancer cells, possibly due to a different level of the aryl hydrocarbon receptor and an activation of this pathway by nuclear translocation of this receptor and subsequent activation of gene expression.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Synergistic effect of plasma-activated medium and novel indirubin derivatives on human skin cancer cells by activation of the AhR pathway

Rebl

Sawade

Hein

et al. 2022

Sci Rep

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“…Among the synthetic indirubin analogs, indirubin-3′-monoxime (compound 1 ) has been reported to inhibit growth of human MCF-7 breast cancer cells [ 124 , 125 ], osteosarcoma [ 82 ], and cholangiocarcinoma cells [ 81 ]. Compound 1 also suppressed the production of interleukin (IL)-1β, IL-6, NO, inducible nitric oxide synthase (iNOS), and cyclooxygenase 2 (COX-2) expression via downregulation of NF-κB and JNK signaling pathways in lipopolysaccharide (LPS)-treated murine RAW264.7 macrophage cells [ 112 ].…”

Section: Indirubin Oxime-based Kinase Inhibitorsmentioning

confidence: 99%

Oximes: Novel Therapeutics with Anticancer and Anti-Inflammatory Potential

et al. 2021

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Oximes have been studied for decades because of their significant roles as acetylcholinesterase reactivators. Over the last twenty years, a large number of oximes have been reported with useful pharmaceutical properties, including compounds with antibacterial, anticancer, anti-arthritis, and anti-stroke activities. Many oximes are kinase inhibitors and have been shown to inhibit over 40 different kinases, including AMP-activated protein kinase (AMPK), phosphatidylinositol 3-kinase (PI3K), cyclin-dependent kinase (CDK), serine/threonine kinases glycogen synthase kinase 3 α/β (GSK-3α/β), Aurora A, B-Raf, Chk1, death-associated protein-kinase-related 2 (DRAK2), phosphorylase kinase (PhK), serum and glucocorticoid-regulated kinase (SGK), Janus tyrosine kinase (JAK), and multiple receptor and non-receptor tyrosine kinases. Some oximes are inhibitors of lipoxygenase 5, human neutrophil elastase, and proteinase 3. The oxime group contains two H-bond acceptors (nitrogen and oxygen atoms) and one H-bond donor (OH group), versus only one H-bond acceptor present in carbonyl groups. This feature, together with the high polarity of oxime groups, may lead to a significantly different mode of interaction with receptor binding sites compared to corresponding carbonyl compounds, despite small changes in the total size and shape of the compound. In addition, oximes can generate nitric oxide. This review is focused on oximes as kinase inhibitors with anticancer and anti-inflammatory activities. Oximes with non-kinase targets or mechanisms of anti-inflammatory activity are also discussed.

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