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载有柚皮素的纳米颗粒调节肺腺癌细胞中缺氧诱导因子驱动的氧感应通路。

Naringenin-loaded nanoparticles modulate HIF-driven oxygen-sensing pathways in lung adenocarcinoma cells.

作者信息

Ragab Eman M, El Gamal Doaa M, Mohamed Tarek M, Khamis Abeer A

机构信息

Biochemistry Division, Chemistry Department, Faculty of Science, Tanta University, Tanta, 31527, Egypt.

出版信息

BMC Res Notes. 2025 Feb 12;18(1):64. doi: 10.1186/s13104-025-07133-2.

Abstract

BACKGROUND

Hypoxia is a common symptom of lung cancer. Proliferation and neovascularization mediated by hypoxia-inducible factors (HIF) influence several adaptations. It has recently been established that naringenin (NAR) and its nanoparticles are chemo-preventive flavonoids in lung cancer.

AIM

Adjust HIF activity by reviving oxygen-sensing enzyme activity while considering possible therapeutic targets.

METHOD

The bindings of NAR to target proteins were examined using computational modeling techniques. Additionally, NAR nanoparticles (NARNPs) were synthesized and characterized. Normal fibroblast cells and A549 cells were used to determine cytotoxicity. Colorimetric analysis of α-ketoglutarate detection for hydroxylases.

RESULTS

According to molecular modeling, NAR and target proteins have a high affinity. The PHD and FIH activities in A549 are significantly stimulated.

CONCLUSION

NAR and NARNPs diminish hypoxia in lung cancer by stimulating oxygen-sensing hydroxylases.

摘要

背景

缺氧是肺癌的常见症状。缺氧诱导因子(HIF)介导的增殖和新血管形成影响多种适应性变化。最近已证实,柚皮素(NAR)及其纳米颗粒是肺癌的化学预防类黄酮。

目的

在考虑可能的治疗靶点的同时,通过恢复氧传感酶活性来调节HIF活性。

方法

使用计算建模技术检测NAR与靶蛋白的结合。此外,合成并表征了NAR纳米颗粒(NARNPs)。使用正常成纤维细胞和A549细胞测定细胞毒性。通过比色分析检测羟化酶的α-酮戊二酸。

结果

根据分子建模,NAR与靶蛋白具有高亲和力。A549中的PHD和FIH活性受到显著刺激。

结论

NAR和NARNPs通过刺激氧传感羟化酶来减轻肺癌中的缺氧状况。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/06da/11817823/ec570060c49b/13104_2025_7133_Fig1_HTML.jpg

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