Abstract The compound α-mangostin (AMG) extracted from Garcinia mangostana L. has potent anticancer properties but its clinical application is limited because of its poor solubility. In this study, AMG-loaded nanoparticles (NMG) were synthesized using a new formula and their apoptosis activity against human cervical carcinoma (HeLa) cells was investigated in comparison with organic solvent-soluble AMG in free form. The NMG was successfully synthesized with a particle size of <50 nm, polydispersity index <0.3, and zeta potential of −35.2 mV. At a concentration of 10 μg/mL, AMG reduced cell survival by 60%, whereas NMG treatment resulted in >90% cell death (p < 0.05). The AMG- or NMG-treated cells also showed changes in the size and shape and exhibited enhanced intensity of blue-stained nuclei, as well as decreased cell density, especially in NMG-treated cells. After 24 h of incubation with AMG or NMG, the cells went through late apoptosis at a rate of approximately 34% in 20 μg/mL AMG treatment and 27% in 10 μg/mL NMG treatment (p < 0.05). Thus, HeLa cells underwent more pronounced cell death through apoptosis induction caused by the NMG treatment compared to that caused by AMG. Clearly, the new NMG improved AMG bioavailability while maintaining the desired activity.

中文翻译：

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载有α-芒果素的纳米颗粒在人宫颈癌细胞中诱导细胞凋亡

摘要 从山竹果中提取的化合物α-山竹素(AMG)具有很强的抗癌作用，但由于溶解性差而限制了其临床应用。在这项研究中，使用新配方合成了负载 AMG 的纳米粒子 (NMG)，并与游离形式的有机溶剂可溶性 AMG 进行了比较，研究了它们对人宫颈癌 (HeLa) 细胞的凋亡活性。成功合成了粒径 <50 nm、多分散指数 <0.3 和 -35.2 mV zeta 电位的 NMG。在 10 μg/mL 的浓度下，AMG 将细胞存活率降低 60%，而 NMG 处理导致 >90% 的细胞死亡（p < 0.05）。AMG 或 NMG 处理的细胞也显示出大小和形状的变化，并显示出蓝色染色的细胞核强度增强，以及细胞密度降低，特别是在 NMG 处理的细胞中。与 AMG 或 NMG 孵育 24 小时后，细胞以 20 μg/mL AMG 处理的约 34% 和 10 μg/mL NMG 处理的 27% 的速率经历晚期凋亡（p < 0.05）。因此，与由 AMG 引起的细胞凋亡相比，HeLa 细胞通过由 NMG 处理引起的细胞凋亡诱导经历了更明显的细胞死亡。显然，新的 NMG 提高了 AMG 的生物利用度，同时保持了所需的活性。