Radiosensitizing Effect of Schinifoline from Zanthoxylum schinifolium Sieb et Zucc on Human Non-Small Cell Lung Cancer A549 Cells: A Preliminary in Vitro Investigation

Abstract

Schinifoline (SF), a 4-quinolinone derivative, was found in Zanthoxylum schinifolium for the first time. 4-Quinolinone moieties are thought to have cytotoxic activity and are often used as a tubulin polymerization inhibitors, heterogeneous enzyme inhibitors and antiplatelet agents. However, very little information respect to radiosensitization has focused on SF. This work aimed to investigate the radiosensitizing effect of SF on A549 cells. The cell viability results indicated cytotoxicity of SF on A549 cells, with IC50 values of 33.7 ± 2.4, 21.9 ± 1.9 and 16.8 ± 2.2 μg/mL, respectively, after 6, 12, 24 h treatment with different concentrations, and the 10% or 20% IC50 concentration during 12 h was applied in later experiments. The results of cell proliferative inhibition and clonogenic assay showed that SF enhanced the radiosensitivity of A549 cells when applied before phase, thus improving the radiosensitivity of A549, leading to cell apoptosis. This paper is the first study that describes the in vitro radiosensitising, cell cycle and apoptotic-inducing effects of schinifoline.

β-Elemene enhances the efficacy of gefitinib on glioblastoma multiforme cells through the inhibition of the EGFR signaling pathway

“…Concurrently, the apoptotic percentage of prostate cancer cells was increased by β-elemene in a dose-and time-dependent manner (35,36). In addition, β-elemene could induce apoptosis and arrest non-small cell lung cancer cells at the G2/M phase (37). Furthermore, previous studies have demonstrated that β-elemene induced apoptosis in human glioma cells through inhibiting the molecular complex Hsp90/Raf-1 and upregulating Bax, Fas/FasL and downregulating Bcl-2 (25,38).…”

On the Inhibitability of Natural Products Isolated from Tetradium ruticarpum towards Tyrosine Phosphatase 1B (PTP1B) and α-Glucosidase (3W37): An In Vitro and In Silico Study

“…The cell viability results indicated cytotoxicity of SF on A549 cells with IC 50 values of 33.7 ± 2.4, 21.9 ± 1.9, and 16.8 ± 2.2 μg/mL after 6, 12, and 24 h treatment, respectively, with different concentrations. The results of cell proliferative inhibition and clonogenic assay showed that SF enhanced the radio-sensitivity of A549 cells when applied before 60 Co γ-irradiation, and this effect was mainly time- and concentration-dependent [ 29 ]. Other studies showed that schinifoline have no antibacterial activity on Staphyloccocus aureus (ATCC25923), Staphylococcus epidermidis (ATCC12228), and Bacillus subtilis (ATCC6633) and no cytotoxicity against four human cancer cell lines (HepG2, Hela, BEL7402, and BEL7403) [ 30 ], nor Jurkat T cells clone E6.1 [ 31 ], using the MTT method.…”

Comparative Study of Bioactivity and Safety Evaluation of Ethanolic Extracts of Zanthoxylum schinifolium Fruit and Pericarp

“…The combined yield of ZSP and ZSF has been reported to be 34.1% using a similar method, consistent with our results [ 34 ]. The yield for ZSP was previously reported to be 8% using ultrasonic methanolic extraction [ 24 ]; while the ZS root yielded 1% with methanol and 5% with 95% ethanol [ 22 , 28 ]; ZS stem yielded 2.3–4.4% with methanol [ 21 , 23 , 27 ], and ZS leaves yielded 12–22.7% with 80% methanol [ 25 , 26 ]. Extraction is the step of recovering and separating compounds from plant material and the extraction solvent, which is composed of water and organic solvents, allows for the simultaneous extraction of compounds soluble in water and organic solvents [ 35 ].…”

“…However, it can cure leprosy, strengthen teeth, and prevent hair fall. Moreover, it can brighten the eyes, relieve stomach ache, and prevent dysentery caused by cold [ 21 , 22 , 23 , 24 ]. There are several phytochemical compounds that are obtained from ZS and possess beneficial bioactivities.…”

“…There are several phytochemical compounds that are obtained from ZS and possess beneficial bioactivities. For example, the anti-KSHV activity of megastigmane sesquiterpenoids; NF-κB inhibitory activity of glycosides and alkaloids; radio-sensitizing effects of 4-quinolinone derivatives; as well as the anticancer activity, apoptogenic activity, monoamine oxidase inhibitory, and antiplatelet aggregation activities of coumarins derived from ZS have been investigated [ 21 , 22 , 23 , 24 , 25 , 26 , 27 , 28 ]. Additionally, the vascular smooth muscle proliferation inhibitory effect, antioxidant, cytotoxicity, antibacterial, anti-melanogenic, anti-inflammatory, and insecticidal activities have been reported in ZS extracts [ 29 , 30 , 31 , 32 , 33 ].…”