Licochalcone A suppresses the proliferation of sarcoma HT-1080 cells, as a selective R132C mutant IDH1 inhibitor

Hu, Chu-Jiao; Zuo, Yu; Liu, Ying; Xu, Heng; Liao, Weike; Dang, Yongjun; Luo, Cheng; Tang, Lei; Zhang, Hao

doi:10.1016/j.bmcl.2019.126825

Cited by 14 publications

(7 citation statements)

References 17 publications

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“…Licochalcone A (imidazole cyclopropyl amine) is a selective inhibitor of IDH1 R132C with IC 50 value of 5.176 μmol/L 186 . Compared with the R132C mutation, the R132H mutation is not conducive to the binding of licochalcone A to the IDH1 protein 186 . Licochalcone A can induce apoptosis and cell cycle arrest in HT-1080 cells 186 .…”

Section: Idh1 Inhibitorsmentioning

confidence: 89%

The regulatory mechanisms and inhibitors of isocitrate dehydrogenase 1 in cancer

Liu

et al. 2023

Acta Pharmaceutica Sinica B

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Section: Idh1 Inhibitorsmentioning

confidence: 89%

The regulatory mechanisms and inhibitors of isocitrate dehydrogenase 1 in cancer

Liu

et al. 2023

Acta Pharmaceutica Sinica B

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“…Moreover, LA (10–40 μM) blocked the cell cycle of MSTO-211H and H28 cells at the G1 phase by inhibiting cyclin D1 expression ( Kim et al, 2015 ). LA (5–20 μM) also led to cell cycle arrest of HT-1080 cells at the G2 phase by decreasing the levels of CDK1 and CDK2 via inhibition of R132C-mutant isocitrate dehydrogenase 1 ( Hu et al, 2020 ). Furthermore, LA (IC 50 = 10.7 µM) inhibited hypoxia-induced proliferation of the neuroblastoma cell lines SK-N-SH, TGW, and GOTO by inhibiting the TrkB/AKT signaling pathway ( Arita et al, 2020 ).…”

Section: Anticancer Effects Of Licochalcones On Tumor Cellsmentioning

confidence: 99%

Anticancer effects of licochalcones: A review of the mechanisms

et al. 2023

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Cancer is a disease with a high fatality rate representing a serious threat to human health. Researchers have tried to identify effective anticancer drugs. Licorice is a widely used traditional Chinese medicine with various pharmacological properties, and licorice-derived flavonoids include licochalcones like licochalcone A, licochalcone B, licochalcone C, licochalcone D, licochalcone E, and licochalcone H. By regulating the expression in multiple signaling pathways such as the EGFR/ERK, PI3K/Akt/mTOR, p38/JNK, JAK2/STAT3, MEK/ERK, Wnt/β-catenin, and MKK4/JNK pathways, and their downstream proteins, licochalcones can activate the mitochondrial apoptosis pathway and death receptor pathway, promote autophagy-related protein expression, inhibit the expression of cell cycle proteins and angiogenesis factors, regulate autophagy and apoptosis, and inhibit the proliferation, migration, and invasion of cancer cells. Among the licochalcones, the largest number of studies examined licochalcone A, far more than other licochalcones. Licochalcone A not only has prominent anticancer effects but also can be used to inhibit the efflux of antineoplastic drugs from cancer cells. Moreover, derivatives of licochalcone A exhibit strong antitumor effects. Currently, most results of the anticancer effects of licochalcones are derived from cell experiments. Thus, more clinical studies are needed to confirm the antineoplastic effects of licochalcones.

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“…In SCC-25 cells, LA inhibited proliferation by blocking the cell cycle at S and G2/M phases ( Zeng et al, 2014 ), while in HN22 and HSC4 cells, proliferation was blocked by inhibiting Sp1 expression and downstream related proteins, including p27, p21, Cyclin D1, Mcl-1 and Survivin ( Cho et al, 2014 ). As a selective inhibitor of R132C-mutant IDH1, LA inhibited the proliferation of sarcoma HT-1080 cells with an acceptable IC 50 = 5.176 μM ( Hu et al, 2020 ). Notably, 30 μmol/L LA treatment for 24 h significantly reduced cell viability of Arkansas P1 cells (ARP1) and Ontario Cancer Institute myeloma 5 cells (OCI-MY5) ( Bai et al, 2021 ).…”

Section: Anticancer Properties Of Lamentioning

confidence: 99%

Role of Licochalcone A in Potential Pharmacological Therapy: A Review

Xie

Jiang

et al. 2022

Front. Pharmacol.

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Licochalcone A (LA), a useful and valuable flavonoid, is isolated from Glycyrrhiza uralensis Fisch. ex DC. and widely used clinically in traditional Chinese medicine. We systematically updated the latest information on the pharmacology of LA over the past decade from several authoritative internet databases, including Web of Science, Elsevier, Europe PMC, Wiley Online Library, and PubMed. A combination of keywords containing “Licochalcone A,” “Flavonoid,” and “Pharmacological Therapy” was used to help ensure a comprehensive review. Collected information demonstrates a wide range of pharmacological properties for LA, including anticancer, anti-inflammatory, antioxidant, antibacterial, anti-parasitic, bone protection, blood glucose and lipid regulation, neuroprotection, and skin protection. LA activity is mediated through several signaling pathways, such as PI3K/Akt/mTOR, P53, NF-κB, and P38. Caspase-3 apoptosis, MAPK inflammatory, and Nrf2 oxidative stress signaling pathways are also involved with multiple therapeutic targets, such as TNF-α, VEGF, Fas, FasL, PI3K, AKT, and caspases. Recent studies mainly focus on the anticancer properties of LA, which suggests that the pharmacology of other aspects of LA will need additional study. At the end of this review, current challenges and future research directions on LA are discussed. This review is divided into three parts based on the pharmacological effects of LA for the convenience of readers. We anticipate that this review will inspire further research.

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Licochalcone A suppresses the proliferation of sarcoma HT-1080 cells, as a selective R132C mutant IDH1 inhibitor

Cited by 14 publications

References 17 publications

The regulatory mechanisms and inhibitors of isocitrate dehydrogenase 1 in cancer

The regulatory mechanisms and inhibitors of isocitrate dehydrogenase 1 in cancer

Anticancer effects of licochalcones: A review of the mechanisms

Role of Licochalcone A in Potential Pharmacological Therapy: A Review

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