A FLT3-inhibitory constituent from the rhizomes of <i>Anemarrhena asphodeloides</i>

Han, Sun‐Young; Chin, Young‐Won

doi:10.3109/14756366.2010.515215

Cited by 4 publications

(2 citation statements)

References 12 publications

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“…Some of the compounds evaluated in this study have been reported in previous studies. 26,27,31,32 Compounds 10,11,12,13,34,35,36,37,38,39, and 40 were synthesized by a total synthesis strategy, as described in previous studies. 26,27 In another prior investigation, a semisynthesis strategy was used to afford compounds 21, 22, 23, 24, and 26 from isolated prenylated flavanones.…”

Section: ■ Experimental Sectionmentioning

confidence: 99%

“…Previous studies have shown the potential antitumor properties of flavonoids . Flavonoids are common secondary metabolites and dietary phytochemicals found in plants with potential benefits for cancer therapy. − They are currently used widely as components in nutraceutical, cosmetic, and pharmaceutical applications . Flavonoids contain a phenylbenzopyrone (C 6 –C 3 –C 6 ) structural motif. , Classification of flavonoids is based on variations of ring C and contains several major subclasses, including chalcones, flavanones, flavones, flavonols, isoflavones, neoflavones, aurones, and anthocyanins. , The activity of these compounds is attributed to their ability to provide electrons from the phenolic hydroxy groups and the possession of a scaffold susceptible to charge-transfer interactions. , In addition, the potent antioxidant and free-radical scavenging activities of flavonoids appear to have health benefits .…”

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confidence: 99%

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Investigation of Selected Flavonoid Derivatives as Potent FLT3 Inhibitors for the Potential Treatment of Acute Myeloid Leukemia

et al. 2021

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Acute myeloid leukemia (AML) is an aggressive disease with a poor prognosis and a high degree of relapse seen in patients. Overexpression of FMS-like tyrosine kinase 3 (FLT3) is associated with up to 70% of AML patients. Wild-type FLT3 induces proliferation and inhibits apoptosis in AML cells, while uncontrolled proliferation of FLT3 kinase activity is also associated with FLT3 mutations. Therefore, inhibiting FLT3 activity is a promising AML therapy. Flavonoids are a group of phytochemicals that can target protein kinases, suggesting their potential antitumor activities. In this study, several plant-derived flavonoids have been identified with FLT3 inhibitory activity. Among these compounds, compound 40 (5,7,4′-trihydroxy-6-methoxyflavone) exhibited the most potent inhibition against not only FLT3 (IC50 = 0.44 μM) but also FLT3-D835Y and FLT3-ITD mutants (IC50 = 0.23 and 0.39 μM, respectively). The critical interactions between the FLT3 binding site and the compounds were identified by performing a structure–activity relationship analysis. Furthermore, the results of cellular assays revealed that compounds 28, 31, 32, and 40 exhibited significant cytotoxicity against two human AML cell lines (MOLM-13 and MV-4-11), and compounds 31, 32, and 40 resulted in cell apoptosis and G0/G1 cell cycle arrest. Collectively, these flavonoids have the potential to be further optimized as FLT3 inhibitors and provide valuable chemical information for the development of new AML drugs.

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Section: ■ Experimental Sectionmentioning

confidence: 99%

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confidence: 99%

Investigation of Selected Flavonoid Derivatives as Potent FLT3 Inhibitors for the Potential Treatment of Acute Myeloid Leukemia

et al. 2021

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Flavonoids as receptor tyrosine kinase FLT3 inhibitors

Chin

Kong

Han

2013

Bioorganic & Medicinal Chemistry Letters

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Inhibitory Effect of Turmeric Curcuminoids on FLT3 Expression and Cell Cycle Arrest in the FLT3-Overexpressing EoL-1 Leukemic Cell Line

et al. 2014

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Leukemia is a hematologic malignancy with a frequent incidence and high mortality rate. Previous studies have shown that the FLT3 gene is overexpressed in leukemic blast cells, especially in acute myeloid leukemia. In this study, a commercially available curcuminoid mixture (1), pure curcumin (2), pure demethoxycurcumin (3), and pure bisdemethoxycurcumin (4) were investigated for their inhibitory effects on cell growth, FLT3 expression, and cell cycle progression in an FLT3-overexpressing EoL-1 leukemic cell line using an MTT assay, Western blotting, and flow cytometry, respectively. The mixture (1) and compounds 2-4 demonstrated cytotoxic effects with IC50 values ranging from 6.5 to 22.5 μM. A significant decrease in FLT3 protein levels was found after curcuminoid treatment with IC20 doses, especially with mixture 1 and compound 2. In addition, mixture 1 and curcumin (2) showed activity on cell cycle arrest at the G0/G1 phase and decreased the FLT3 and STAT5A protein levels in a dose-dependent manner. Compound 2 demonstrated the greatest potential for inhibiting cell growth, cell cycle progression, and FLT3 expression in EoL-1 cells. This investigation has provided new findings regarding the effect of turmeric curcuminoids on FLT3 expression in leukemic cells.

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A FLT3-inhibitory constituent from the rhizomes of Anemarrhena asphodeloides

Cited by 4 publications

References 12 publications

Investigation of Selected Flavonoid Derivatives as Potent FLT3 Inhibitors for the Potential Treatment of Acute Myeloid Leukemia

Investigation of Selected Flavonoid Derivatives as Potent FLT3 Inhibitors for the Potential Treatment of Acute Myeloid Leukemia

Flavonoids as receptor tyrosine kinase FLT3 inhibitors

Inhibitory Effect of Turmeric Curcuminoids on FLT3 Expression and Cell Cycle Arrest in the FLT3-Overexpressing EoL-1 Leukemic Cell Line

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