Baicalein Exerts Anticancer Effect in Nasopharyngeal Carcinoma In Vitro and In Vivo

Abstract

Baicalein, an active ingredient separated from Astragalus membranaceus, has shown its anticancer ability in various cancers. However, its effect on nasopharyngeal carcinoma has not been explored yet. The present study aimed to investigate the effect of baicalein on the growth, proliferation, apoptosis, and cell cycle of human nasopharyngeal carcinoma cells, as well as transplanted nude mouse xenograft. The results showed that baicalein inhibited the growth and proliferation of CNE1 and CNE2 cells in a time- and concentration-dependent manner. It also caused a significant increase in the number of cells in the G0/G1 phase and a decrease in the G2/M phase, thereby reducing the number of cells entering mitosis and inhibiting the proliferation of tumor cells. Baicalein also significantly induced apoptosis of CNE1 and CNE2 cells. Western blots showed that baicalein decreased the expression of Bcl-xl and Mcl-1 and increased the expression of Bax, Bad, and caspase 3, 8, and 9. In CNE1- and CNE2-transplanted tumors of mice, baicalein significantly inhibited tumor growth. In conclusion, baicalein could inhibit the growth and proliferation of human nasopharyngeal carcinoma cells, change their cell cycle, and induce apoptosis. Baicalein also effectively limits both CNE1- and CNE2-transplanted tumors in nude mice. Downregulation of Bcl-xl and Mcl-1 proteins and upregulation of Bax and Bad may be involved in the mechanism.

Baicalein Potentiated M1 Macrophage Polarization in Cancer Through Targeting PI3Kγ/ NF-κB Signaling

“…The application of baicalein, as a main bioactive ingredient extracted from the root of medical herb Scutellaria baicalensis , has been studied in the treatment of a variety of cancers, such as breast cancer, NSCLC, nasopharyngeal carcinoma, hepatocellular carcinoma, and the underlying mechanisms mainly focus on inducing apoptosis and autophagy, cell cycle arrest, inhibiting proliferation and invasion of tumor cells ( Bie et al, 2017 ; Yan et al, 2018 ; Guo et al, 2019 ; Nik Salleh et al, 2020 ; Zhang et al, 2020 ). In addition to malignant cells, increasing evidence demonstrated the dominant role of the large proportions of immune cells within the TME in orchestrating tumor progression and resistance to anti-tumor drugs ( Cassetta and Pollard, 2018 ).…”

Baicalein Inhibits Metastatic Phenotypes in Nasopharyngeal Carcinoma Cells via a Focal Adhesion Protein Integrin β8

“…Baicalein, a flavonoid compound from dry roots of S. baicalensis, has anticancer activities both in vitro and in vivo. Baicalein exerted inhibitory effects on cell growth and cell cycle of numerous cancers through various molecular pathways such as PI3K/Akt [31], Wnt/β-catenin [27], and caveolin-1/AKT/mTOR [24], and the upregulation of p53 and caspases [22]. A previous study on NPC with baicalein showed that a decrease in cell viability of an EBV-positive NPC cell line was mediated through the downregulation of transcription factor specificity protein 1 (Sp1) and reduction in the EBNA1 activity in a doseand time-dependent manner [25].…”

“…Baicalein is one of the major bioactive flavonoids predominantly found in dried roots of the traditional herb Scutellaria baicalensis, Georgi [15]. It has various biological activities, including antiviral, antibacterial, anti-thrombotic, antidiabetic, anti-inflammation, and anticancer activities [16][17][18][19][20][21][22]. In addition, baicalein inhibits various types of cancers through distinct cellular signaling pathways [15,[21][22][23][24][25][26][27]].…”

“…It has various biological activities, including antiviral, antibacterial, anti-thrombotic, antidiabetic, anti-inflammation, and anticancer activities [16][17][18][19][20][21][22]. In addition, baicalein inhibits various types of cancers through distinct cellular signaling pathways [15,[21][22][23][24][25][26][27]]. Baicalein, for example, inhibits cell proliferation and induces apoptosis and senescence via the phosphatidylinositol 3kinase/Akt signaling pathway in human colorectal cancer [21], via the Wnt/β-catenin pathway in osteosarcoma [27], via the caveolin-1/AKT/mTOR pathway in prostate cancer cells [24], and via the inhibition of Bcl-XL and Mcl-1 and activation of Bax, Bad, caspase-3, -8, and -9 in NPC [22].…”

“…In addition, baicalein inhibits various types of cancers through distinct cellular signaling pathways [15,[21][22][23][24][25][26][27]]. Baicalein, for example, inhibits cell proliferation and induces apoptosis and senescence via the phosphatidylinositol 3kinase/Akt signaling pathway in human colorectal cancer [21], via the Wnt/β-catenin pathway in osteosarcoma [27], via the caveolin-1/AKT/mTOR pathway in prostate cancer cells [24], and via the inhibition of Bcl-XL and Mcl-1 and activation of Bax, Bad, caspase-3, -8, and -9 in NPC [22]. Additionally, baicalein reduces metastatic potentials and epithelialmesenchymal transition (EMT) of metastatic breast cancer cells [23].…”