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U251细胞
ACS Chemical Neuroscience · 2023 · IF 5

Monacolin K Induces Apoptosis of Human Glioma U251 Cells by Triggering ROS-Mediated Oxidative Damage and Regulating MAPKs and NF-κB Pathways

Xiaoyi Shi,Meng Li,Qiming Huang,Liuming Xie,Zhibing Huang

Monacolin K (MK), a polyketo secondary metabolic compound of the mold genus Monascus, can promote the apoptosis of malignant cancer cells, possessing potential antitumor properties. However, its mechanism of action on gliomas remains unclear. Here, we explored and investigated the potential of the monacolin K’s antitumor effect on human glioma U251 cells and its possible molecular mechanism. Results showed that the application of 10 μM monacolin K inhibited the proliferation of U251 cells, with an inhibitory rate of up to 53.4%. Additionally, monacolin K induced the generation of reactive oxygen species and activated mitochondria-mediated pathways, including decreased MMP, activation of caspase3/caspase9, decreased Na+/K+-ATPase and Ca2+-ATPase activities, and disruption of the antioxidant system, resulting in the disruption of intracellular reduction–oxidation homeostasis. Monacolin K also activated MAPK and NF-κB pathways, upregulating P38 activity and downregulating JNK/ERK/P65/IκBα expression, ultimately leading to apoptosis of U251 cells. Importantly, monacolin K was not cytotoxic to normal human cells, hUC-MSCs. We concluded that monacolin K can induce apoptosis in U251 cells by triggering ROS-mediated oxidative damage and regulating MAPKs and NF-κB pathways.

CAS / MDL: 75330-75-5 85622-93-1
研究领域: 肿瘤学 · 细胞生物学 · 药理学
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JOURNAL OF CHROMATOGRAPHY A · 2023 · IF 4.1

Construction of lipid raft-coupled agarose gels as bioaffinity chromatography materials and validation with tropomyosin-related kinase A-targeted drugs

Hao Chi,Sheng Tian,Xiu Li,Yuchu Chen,Qiumin Xu,Qixiao Wang,Wenwan Shi,Michael Adu-Frimpong,Shanshan Tong

In order to improve the separation process of affinity chromatography that has silica as the main carrier material, we sought to construct Lipid [email protected] 4B affinity chromatography model. We extracted the lipid rafts from U251 cells with a descaler method and sucrose density gradient centrifugation. Afterwards, it was discovered via immunofluorescence that the lipid rafts contain a large amount of tropomyosin-related kinase A (TrkA) protein. Also, agarose powder in the lyophilised state was pretreated, before the lipid rafts were coupled to the agarose gel in a coupling buffer of alkaline pH. CNBr-Sepharose 4B affinity gel packing was characterised using UV spectrophotometric, immunofluorescence and scanning electron microscopic techniques, wherein and the results showed that the lipid rafts were successfully coupled to the agarose gels. Three compounds were used to verify the specific sorption of Sepharose 4B and CNBr-Sepharose 4B, which showed no specific sorption on the materials. Of note, the prepared Lipid [email protected] 4B agarose gels packed with TrkA-rich target proteins could be successfully validated for the active drug gefitinib with high affinity sorption efficiency and eluted with good recovery and reproducibility. This study broadens the range of affinity chromatography carrier materials and provides a reference for research in active drug screening.

研究领域: 生物化学 · 药学 · 生物技术 · 分析化学
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Tomography · 2017 ·Vol. 3 ·期 1 ·1-8 · IF 0

Ferritin–EGFP Chimera as an Endogenous Dual-Reporter for Both Fluorescence and Magnetic Resonance Imaging in Human Glioma U251 Cells

E. Mark Haacke

A unique hybrid protein ferritin–enhanced green fluorescent protein (EGFP) was built to serve as an endogenous dual reporter for both fluorescence and magnetic resonance imaging (MRI). It consists of a human ferritin heavy chain (an iron-storage protein) at the N terminus, a flexible polypeptide in the middle as a linker, and an EGFP at the C terminus. Through antibiotic screening, we established stable human glioma U251 cell strains that expressed ferritin–EGFP under the control of tetracycline. These cells emitted bright green fluorescence and were easily detected by a fluorescent microscope. Ferritin–EGFP overexpression proved effective in triggering obvious intracellular iron accumulation as shown by Prussian blue staining and by MRI. Further, we found that ferritin–EGFP overexpression did not cause proliferation differences between experimental and control group cells when ferritin–EGFP was expressed for <96 hours. Application of this novel ferritin–EGFP chimera has a promising future for combined optical and MRI approaches to study in vivo imaging at a cellular level.

研究领域: 医学影像学 · 分子生物学 · 神经科学 · 癌症研究
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BIOCHEMICAL SYSTEMATICS AND ECOLOGY · 2023 · IF 1.6

Chemical composition and cytotoxicity of Salicornia europaea L

Dongyu Gu,Chen Fang,Jing Liu,Zhongai Jiang,Gang Li,Minjing Li,Min Zhang,Yun Huang

Salicornia europaea L. is an economic plant which can grow in saline-alkali land, beach and other heavy saline soil . In this study, the inhibitory activities of S. europaea extracts against tumor cell growth including human non-small cell lung cancer cell A549 , human liver cancer cell HepG2, and brain glioma cell U251 were screened. The results showed that the ethanol extract of S. europaea had an inhibitory effect on the proliferation of A549 cells, and the inhibition of tumor cells showed time-dose relationship. Moreover, the ethanol extract of S. europaea was extracted and fractionated with different organic solvents and the activity results indicated that the petroleum ether fraction with IC 50 of 96.5 μg mL −1 possessed the best activity against A549 cells. Then seven compounds, including 30-norhederagenin ( 1 ), 24-methylenecycoartanol ( 2 ), pheophorbide A ( 3 ), stigmasterol ( 4 ), β -sitosterol ( 5 ), α-spinasterol ( 6 ), phytol ( 7 ) were isolated and identified from the petroleum ether fraction of S. europaea . Besides, the oil obtained from the petroleum ether fraction was analyzed by GC-MS, and fourteen compounds were identified. The compounds identified from the petroleum ether fraction mainly consisted of triterpenes , sterols, fatty acids, and their lipids .

CAS / MDL: 298-93-1
研究领域: 药理学 · 植物科学 · 癌症研究 · 生物化学
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