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In vitro determination of the efficacy of scorpion venoms as anti-cancer agents against colorectal cancer cells: a nano-liposomal delivery approach

机译:蝎毒作为大肠癌细胞抗癌药的体外测定:纳米脂质体递送方法

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The use of liposomes in biological and medicinal sciences is a relatively new approach. The liposomal strategy greatly depends on the technological advancement in the formation of vesicles of various sizes and properties. In the current study, we encapsulated the venoms obtained from medically important scorpions such as Androctonus bicolor (AB), Androctonus crassicauda (AC), and Leiurus quinquestriatus (LQ). To begin with, our first and foremost aim was to prepare biocompatible and biodegradable nanovesicles. Additionally, we intended to enhance the anti-cancer potential of these encapsulated venoms. The liposomal venoms were prepared by rehydration and dehydration methods. Morphology, particle size, and size distribution of the liposomes were examined by scanning electron microscope (SEM), transmission electron microscope (TEM), and Zetasizer. We found that the prepared liposomes had a smooth surface and a spherical/ovoid shape and existed mainly as single unilamellar vesicles (SUVs). Furthermore, the liposomal formulation of all three venoms exhibited excellent stability and good encapsulation efficiency (EE). Additionally, the anti-cancer potential of the encapsulated venoms was also evaluated on a colorectal cancer cell line (HCT-8). The venom-loaded liposomes showed elevated anti-cancer properties such as low rate of cell survival, higher reactive oxygen species (ROS) generation, and enhancement in the number of apoptotic cells. In addition to this, cell cycle analysis revealed G0/G1 enrichment upon venom treatment. The effect of treatment was more pronounced when venom–liposome was used as compared to free venom on the HCT-8 cell line. Furthermore, we did not observe any interference of liposomal lipids used in these preparations on the progression of cancer cells. Considering these findings, we can conclude that the encapsulated scorpion venoms exhibit better efficacy and act more vigorously as an anti-cancer agent on the colorectal cancer cell line when compared with their free counterpart.
机译:在生物和医学科学中使用脂质体是一种相对较新的方法。脂质体策略在很大程度上取决于形成各种大小和性质的囊泡的技术进步。在当前的研究中,我们封装了从医学上重要的蝎子(如双色Androctonus bicolor(AB),Androctonus crassicauda(AC)和Leirus quinquestriatus(LQ))获得的毒液。首先,我们的首要目标是制备生物相容性和可生物降解的纳米囊泡。另外,我们打算增强这些封装的毒液的抗癌潜力。脂质体毒液通过补液和脱水方法制备。通过扫描电子显微镜(SEM),透射电子显微镜(TEM)和Zetasizer检查脂质体的形态,粒径和尺寸分布。我们发现,所制备的脂质体具有光滑的表面和球形/卵形的形状,并且主要以单层囊泡(SUVs)的形式存在。此外,所有三种毒液的脂质体制剂均表现出优异的稳定性和良好的包封效率(EE)。此外,还对结直肠癌细胞系(HCT-8)评估了包囊毒液的抗癌潜力。载有毒液的脂质体显示出较高的抗癌特性,例如较低的细胞存活率,较高的活性氧(ROS)生成以及凋亡细胞数量的增加。除此之外,细胞周期分析显示毒液处理后G0 / G1富集。与HCT-8细胞系上的游离毒液相比,使用毒液脂质体治疗的效果更为明显。此外,我们没有观察到这些制剂中使用的脂质体脂质对癌细胞进程的任何干扰。考虑到这些发现,我们可以得出结论,与游离的蝎蝎毒相比,包裹的蝎毒表现出更好的功效,并且在结直肠癌细胞系中作为抗癌剂发挥更大的作用。

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