PDF(Pubmed)
Abstract：
Curcumin is one of the natural anticancer drugs but its efficiency is limited by low stability, insufficient bioavailability, poor solubility, and poor permeability. Dorema aucheri (Bilhar) is a herb with precious pharmaceutical properties. This study aimed to develop a nanoliposome-based curcumin and Bilhar extract codelivery system. The nanocompounds were synthesized using the lipid thin-film hydration method and characterized by transmission electron microscopy, and dynamic light scattering techniques, and their cytotoxicity and apoptotic effect on the primary oral cancer cell line were evaluated via 2,5-diphenyl-2H-tetrazolium bromide assay and flow cytometry. Moreover, the expression of the epidermal growth factor receptor (EGFR) gene in the treated cells was assessed using the real-time polymerase chain reaction technique. Based on the results, nanoliposomes had a size of 91 ± 10 nm with a polydispersity index of 0.13. Free curcumin, the extract, and the curcumin-extract combination showed dose-dependent toxicity against cancer cells; yet, the extract (IC50: 86 µg/ml) and curcumin-extract (IC50: 65 µg/ml) activities were much more than curcumin (IC50: 121 µg/ml). Also, the curcumin and extract loaded on liposomes showed a dose and time-dependent cytotoxicity. After loading the curcumin-extract compound on nanoliposomes, their IC50 decreased from 180 µg/ml (within 24 hr) to 43 µg/ml (within 72 hr), indicating their sustainable release and activity. Likewise, this compound induced the highest apoptosis percentage (95%) in cancerous cells and inhibited the expression of the EGFR gene in the cells by 81% ± 3%. These findings demonstrated the effectiveness of the Bilhar extract against oral cancer cells. Also, in combination with curcumin, it showed an additive activity that considerably improved after loading on nanoliposomes.
摘要：
姜黄素是天然抗癌药物之一,但其功效受到稳定性低的限制,生物利用度不足,溶解性差，渗透性差。Doremaaucheri（Bilhar）是一种具有珍贵药学特性的草药。本研究旨在开发基于纳米脂质体的姜黄素和Bilhar提取物共递送系统。使用脂质薄膜水合方法合成了纳米化合物，并通过透射电子显微镜对其进行了表征，和动态光散射技术，并通过2,5-二苯基-2H-四唑溴化物测定和流式细胞术评估其对原发性口腔癌细胞系的细胞毒性和凋亡作用。此外，使用实时聚合酶链反应技术评估表皮生长因子受体(EGFR)基因在处理细胞中的表达.根据结果,纳米脂质体的尺寸为91±10nm，多分散指数为0.13。免费姜黄素,提取物，姜黄素-提取物组合对癌细胞显示出剂量依赖性毒性；然而，提取物（IC50：86µg/ml）和姜黄素提取物（IC50：65µg/ml）的活性远高于姜黄素（IC50：121µg/ml）。此外，脂质体上的姜黄素和提取物显示出剂量和时间依赖性的细胞毒性。在纳米脂质体上加载姜黄素提取物化合物后，它们的IC50从180微克/毫升（24小时内）下降到43微克/毫升（72小时内），表明它们的可持续释放和活动。同样，该化合物在癌细胞中诱导最高的凋亡百分比（95％），并抑制细胞中EGFR基因的表达81％±3％。这些发现证明了Bilhar提取物对口腔癌细胞的有效性。此外，与姜黄素结合，在纳米脂质体上加载后，它显示出显著提高的添加剂活性。
