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L. 载有精油的 PLGA 作为癌症治疗的纳米制剂候选物。

L. Essential Oil-Loaded PLGA as a Nanoformulation Candidate for Cancer Treatment.

机构信息

Department of Pharmacognosy and Natural Product Chemistry, Institute of Health Sciences, Bezmialem Vakıf University, Istanbul 34093, Turkey.

Department of Physics, Faculty of Science, Istanbul University, Istanbul 34134, Turkey.

出版信息

Molecules. 2022 Mar 15;27(6):1899. doi: 10.3390/molecules27061899.

Abstract

The aim of this study was to obtain essential oil (LNEO) from the L. plant, and to prepare LNEO-loaded poly lactic-co-glycolic acid (PLGA) nanoparticles (NPs) as an approach in cancer treatment. The components of the obtained LNEO were analyzed using GC-MS. The LNEO-NPs were synthesized by the single-emulsion method. The LNEO-NPs were characterized using UV-Vis spectrometry, Dynamic Light Scattering (DLS), Scanning Electron Microscopy (SEM), and a DNA binding assay, which was performed via the UV-Vis titration method. According to the results, the LNEO-NPs had a 211.4 ± 4.031 nm average particle size, 0.068 ± 0.016 PdI, and -7.87 ± 1.15 mV zeta potential. The encapsulation efficiency and loading capacity were calculated as 59.25% and 25.65%, respectively, and the in vitro drug release study showed an LNEO release of 93.97 ± 3.78% over the 72 h period. Moreover, the LNEO was intercalatively bound to CT-DNA. In addition, the mechanism of action of LNEO on a dual PI3K/mTOR inhibitor was predicted, and its antiproliferative activity and mechanism were determined using molecular docking analysis. It was concluded that LNEO-loaded PLGA NPs may be used for cancer treatment as a novel phytotherapeutic agent-based controlled-release system.

摘要

本研究旨在从 L. 植物中提取精油(LNEO),并制备 LNEO 负载的聚乳酸-共-羟基乙酸(PLGA)纳米颗粒(NPs),作为癌症治疗的一种方法。采用 GC-MS 分析所得 LNEO 的成分。采用单乳液法合成 LNEO-NPs。采用紫外可见分光光度法、动态光散射(DLS)、扫描电子显微镜(SEM)和 DNA 结合试验对 LNEO-NPs 进行表征,DNA 结合试验通过紫外可见滴定法进行。结果表明,LNEO-NPs 的平均粒径为 211.4 ± 4.031nm、PDI 为 0.068 ± 0.016、zeta 电位为-7.87 ± 1.15mV。包封效率和载药量分别计算为 59.25%和 25.65%,体外药物释放研究表明 LNEO 在 72 小时内释放 93.97 ± 3.78%。此外,LNEO 与 CT-DNA 发生插层结合。此外,通过分子对接分析预测了 LNEO 对双 PI3K/mTOR 抑制剂的作用机制,并确定了其增殖活性和作用机制。结果表明,LNEO 负载的 PLGA NPs 可作为一种新型植物治疗剂控释系统,用于癌症治疗。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8396/8951774/4eeb206db9aa/molecules-27-01899-g001.jpg

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