Teucrium polium extract (TPE) is a natural product with potent anticancer activity because of its terpenoid and flavonoid content. The aim of this study was to synthesize solid lipid nanoparticles (SLN) containing T. polium extract (TPE-SLNs) and to evaluate its anti-cancer effect. Formulations of TPE-SLNs were prepared using high-shear homogenization followed by the ultra-sonication technique. Then the TPE-SLNs were characterized by dynamic light scattering (DLS), Zetasizer and field-emission scanning electron microscopy (FESEM), and Fourier transform infrared spectroscopy methods. After confirming the presence of nanoparticles, its anti-proliferative activity was evaluated on Ntra-2 cancer cells and compared to human foreskin fibroblasts (HFF) as a normal cell line by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The pro-apoptotic (flow cytometry) and quantitative PCR (qPCR) and anti-angiogenic (chick chorioallantoic membrane (CAM)) and anti-inflammatory (qPCR) effects of TPE-SLNs were assessed by various methods. TPE-SLNs (85.5 nm, PDI: 0.39, and zeta potential: −25.5 mv) were inhibited by the proliferation of Ntra-2 cancer cells with half-maximal inhibitory concentration (IC₅₀; 106.58 µg/ml). Moreover, by increasing the expression of caspase-3,9 and decreasing the expression of interleukin 6 (IL-6), IL-1b, and Bcl-2 genes, apoptosis and anti-inflammatory effects were observed. Reduction of angiogenesis was observed by the reduction of genes involved in angiogenesis and reduction of vascular and embryonic factors in the CAM assay. Activation of various mechanisms of inhibiting cancer cells in the treatment of nanoparticles was demonstrated in the present study. Therefore, these nanoparticles can be recommended for therapeutic purposes.

中文翻译：

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Teucrium polium 提取物负载的固体脂质纳米颗粒：设计和体外抗癌研究

Teucrium polium提取物 (TPE) 是一种天然产物，由于其萜类化合物和黄酮类化合物的含量而具有强大的抗癌活性。本研究的目的是合成含有T. polium 的固体脂质纳米颗粒 (SLN)提取物（TPE-SLNs）并评估其抗癌作用。TPE-SLNs 的配方是使用高剪切均质和超声技术制备的。然后通过动态光散射 (DLS)、Zetasizer 和场发射扫描电子显微镜 (FESEM) 以及傅里叶变换红外光谱方法对 TPE-SLN 进行表征。在确认纳米颗粒的存在后，通过 MTT（3-（4,5-二甲基噻唑-2-基））评估其对 Ntra-2 癌细胞的抗增殖活性，并与作为正常细胞系的人包皮成纤维细胞（HFF）进行比较-2,5-二苯基溴化四唑）测定。通过各种方法评估了 TPE-SLN 的促凋亡 (流式细胞术) 和定量 PCR (qPCR) 以及抗血管生成 (鸡绒毛尿囊膜 (CAM)) 和抗炎 (qPCR) 的作用。TPE-SLN（85.5 nm，PDI：₅₀ ; 106.58 微克/毫升）。此外，通过增加 caspase-3,9 的表达并降低白细胞介素 6 (IL-6)、IL-1b 和 Bcl-2 基因的表达，观察到细胞凋亡和抗炎作用。在CAM测定中，通过参与血管生成的基因的减少以及血管和胚胎因子的减少，观察到血管生成的减少。本研究证明了纳米颗粒治疗中各种抑制癌细胞的机制的激活。因此，可以推荐这些纳米颗粒用于治疗目的。