University of Science and Technology of Hanoi, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet Road, Cau Giay, Hanoi, Vietnam.
Center for Research and Technology Transfer, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Hanoi, Vietnam.
Z Naturforsch C J Biosci. 2020 May 26;75(5-6):145-151. doi: 10.1515/znc-2020-0001.
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.
从藤黄属植物中提取的化合物 α-倒捻子素 (AMG) 具有很强的抗癌特性，但由于其溶解度差，其临床应用受到限制。在这项研究中，使用新配方合成了负载 AMG 的纳米颗粒 (NMG)，并将其对人宫颈癌 (HeLa) 细胞的凋亡活性与游离形式的有机溶剂可溶性 AMG 进行了比较。成功合成了粒径 <50nm、多分散指数 <0.3、zeta 电位为-35.2 mV 的 NMG。在浓度为 10μg/mL 时，AMG 使细胞存活率降低 60%，而 NMG 处理导致超过 90%的细胞死亡 (p<0.05)。经 AMG 或 NMG 处理的细胞大小和形状也发生了变化，蓝色染色核的强度增强，细胞密度降低，尤其是在 NMG 处理的细胞中。用 AMG 或 NMG 孵育 24 小时后，细胞分别在 20μg/mL AMG 处理和 10μg/mL NMG 处理中经历晚期凋亡，比率约为 34%和 27% (p<0.05)。因此，与 AMG 相比，NMG 处理更能通过诱导细胞凋亡使 HeLa 细胞发生更明显的细胞死亡。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。
