OBJECTIVE To prepare warangalone-loaded thermosensitive liposomes (WLTSL) and evaluate its inhibitory effect on breast cancer cells in vitro. METHODS MTT assay was used to assess the changes in proliferation of 3 breast cancer cell lines (MDA-MB-231, MCF7, and SKBR3) following treatment with warangalone, soy isoflavone and genistein. Colony-forming assay and wound healing assay was used to assess colony forming activity and migration of MDA-MB-231 cells treated with warangalone. The effect of warangalone on the expression of MMP2 and MMP9 in MDA-MB-231 cells was examined with Western blotting. The thermosensitive liposomes (TSL) and WLTSL were prepared using a thin film hydration method, and the morphology, size, encapsulation efficiency and stability of the prepared liposomes were characterized using transmission electron microscopy, dynamic light scattering scanning and UV spectrophotometry. MTT assay was used to examine the inhibitory effect of WLTSL on mouse breast cancer cells (4T1) in vitro. RESULTS Warangalone showed stronger anti-proliferation effects than soy isoflavones and genistein in the 3 human breast cancer cell lines and significantly inhibited colony formation by MDA-MB-231 cells. Treatment with warangalone significantly inhibited migration of the breast cancer cells and down-regulated the cellular expressions of MMP2 and MMP9. The prepared TSL and WLTSL presented with a homogeneous, irregular spherical morphology, with a mean particle size of 56.23±0.61 nm, a polymer dispersity index of 0.241±0.014, a Zeta potential of -40.40±0.46 mV, and an encapsulation efficiency was 87.68±2.41%. WLTSL showed a good stability at 4 ℃ and 37 ℃ and a stronger inhibitory effect than warangalone in 4T1 cells. CONCLUSIONS Warangalone inhibits the proliferation, migration and invasion of breast cancer cells, and the prepared WLTSL possesses good physical properties and strong anti-breast cancer activity.

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瓦兰甘酮脂质体的制备及其对乳腺癌细胞的抑制作用[J].


目的制备瓦兰酮热敏脂质体（WLTSL）并评价其对乳腺癌细胞的体外抑制作用。方法采用MTT法评估3种乳腺癌细胞系（MDA-MB-231、MCF7和SKBR3）在用warangalone、大豆异黄酮和金雀异黄酮处理后增殖的变化。使用集落形成测定和伤口愈合测定来评估用瓦朗酮处理的MDA-MB-231细胞的集落形成活性和迁移。采用Western blotting检测瓦兰糖龙对MDA-MB-231细胞中MMP2和MMP9表达的影响。采用薄膜水合法制备了热敏脂质体（TSL）和WLTSL，并利用透射电子显微镜、动态光散射扫描和紫外分光光度法对制备的脂质体的形貌、尺寸、包封率和稳定性进行了表征。采用MTT法检测WLTSL对小鼠乳腺癌细胞(4T1)的体外抑制作用。结果 Warangalone 在 3 种人乳腺癌细胞系中表现出比大豆异黄酮和染料木黄酮更强的抗增殖作用，并显着抑制 MDA-MB-231 细胞的集落形成。 Warangalone 治疗显着抑制乳腺癌细胞的迁移并下调 MMP2 和 MMP9 的细胞表达。制备的TSL和WLTSL呈现均匀、不规则的球形形貌，平均粒径为56.23±0.61 nm，聚合物分散指数为0.241±0.014，Zeta电位为-40.40±0.46 mV，包封率为87.68 ±2.41%。 WLTSL在4℃和37℃下表现出良好的稳定性，并且在4T1细胞中比warangalone具有更强的抑制作用。 结论 瓦兰酮可抑制乳腺癌细胞的增殖、迁移和侵袭，制备的WLTSL具有良好的物理性质和较强的抗乳腺癌活性。