Abstract:

Objective: To compare inhibitory activity of andrographolide solid lipid nanoparticles(AND-SLNs) and free andrographolide(AND) to cell lines of oral squamous cell carcinoma (HN6 cell line) and oral leukoplakia(Leuk1 cell line). Methods: The drug quantitative uptaken and functional impact about drugs action of HN6 and Leuk1, were examined with high performance liquid chromatography（HPLC）, MTS assay and flow cytometry. Results: Absorption of AND-SLNs in HN6 cells were more than that of AND. The inhibitory activity of AND-SLNs on cell proliferation to HN6 and Leuk1, were significantly more than that of AND. The drugs’ half maximal inhibitory concentration (IC50) after treatment for 48 h were as followed: HN6 48 h IC50 of AND-SLNs was 6.09 μg/mL, while that of AND was 13.75 μg/mL. Leuk1 48 h IC50 of AND-SLNs was 0.72 μg/mL, while that of AND was 26.14 μg/mL. According to 48 h IC50, the bioactivity of AND-SLNs on arresting on cell proliferation cycle at cell phase (G0/G1) was obviously stronger than that of AND（P<0.05）. The biological effects of AND-SLNs on inducing cell apoptosis, after treated by 6 h or 12 h, were obvious stronger than AND（P<0.05）. Conclusion: The bioactivity about inhibition cell proliferation, blocking cell cycle and inducing cell apoptosis of AND-SLNs, were stronger than AND, and AND-SLNs might be a novel drug for prevention and treatment of leukoplakia cancerization.

Key words: andrographolide(AND), andrographolide solid lipid nanoparticles(AND-SLNs), oral leukoplakia, oral squamous cell carcinoma (OSCC)

摘要：

目的：研究穿心莲内酯（andrographolide, AND）纳米化（穿心莲内酯纳米粒，andrographolide solid lipid nanoparticles, AND-SLNs）后，对口腔鳞癌的HN6细胞株和口腔白斑的Leuk1细胞株抑制作用的变化。方法：利用高效液相色谱（high performance liquid chromatography，HPLC）法、四氮唑蓝盐化合物细胞增殖实验（MTS法）、流式细胞仪，对比分析AND-SLNs和AND对HN6细胞、Leuk1细胞摄取药物能力和细胞增殖的影响。结果：HN6细胞对AND-SLNs的药物摄取量显著高于AND。经AND-SLNs和AND分别作用48 h后，HN6细胞的半抑制浓度（IC50）分别为6.09 μg/mL和13.75 μg/mL，Leuk1细胞对2种药物的IC50分别为 0.72 μg/mL和26.14 μg/mL，说明经纳米化后的AND对肿瘤细胞增殖的抑制性明显增强。AND-SLNs和AND作用12 h后，AND-SLNs阻滞周期的活性强于AND，将细胞明显阻滞于G0/G1期（P<0.05）；作用 6 h或12 h后，AND-SLNs诱导细胞凋亡的活性强于AND（P<0.05）。结论：AND-SLNs能促进细胞摄取AND，进而提高AND抑制细胞增殖、阻滞细胞周期、诱导细胞凋亡的活性，具有更强的抗口腔鳞癌和白斑细胞增殖的作用，因此AND-SLNs有望成为防治白斑癌变的新剂型。

关键词: 穿心莲内酯, 穿心莲内酯纳米粒, 口腔白斑, 口腔鳞癌

CLC Number: 

• R782

• R739.8