Departamento de Física e Química, Faculdade de Engenharia de Ilha Solteira, Universidade Estadual Paulista, Ilha Solteira, São Paulo, Brasil.
Departamento de Biologia e Zootecnia, Faculdade de Engenharia de Ilha Solteira, Universidade Estadual Paulista, Ilha Solteira, São Paulo, Brasil.
Nat Prod Res. 2022 Sep;36(18):4696-4703. doi: 10.1080/14786419.2021.2000409. Epub 2021 Nov 5.
This work aimed to synthesize poly (D, L-lactic-co-glycolic acid) (PLGA) microparticles containing hinokinin (HNK) and to evaluate their cytotoxic activity against tumoral SiHa cells and non-tumoral HaCaT cells. Hinokinin was incorporated into PLGA (PLGA-HNK) with an encapsulation efficiency of 84.18 ± 2.32%. PLGA and PLGA-HNK were characterized by SEM microscopy and showed spherical morphology with an average size of ∼3.33. Encapsulation efficiency was determined by a calibration curve using UV-vis spectroscopy. PLGA-HNK more active inhibiting proliferation of SiHa cells (IC = 14.68 µM) than free HNK (IC = 225.5 µM). In relation to HaCaT cells, PLGA-HNK showed no significant difference compared to the negative control. These results led to an increase in HNK bioavailability and thereby, biological activity. prediction analysis suggests that HNK is cytotoxic against SiHa cells with E6 and MDM2 inhibition as possible main mechanism of action.
本研究旨在合成含有扁柏素（hinokinin，HNK）的聚（D，L-乳酸-共-乙醇酸）（PLGA）微球，并评估其对肿瘤 SiHa 细胞和非肿瘤 HaCaT 细胞的细胞毒性活性。HNK 被包封到 PLGA 中（PLGA-HNK），包封效率为 84.18±2.32%。通过扫描电子显微镜（SEM）对 PLGA 和 PLGA-HNK 进行了表征，它们均呈现出平均粒径约为 3.33μm 的球形形态。通过使用紫外可见分光光度法建立校准曲线来确定包封效率。PLGA-HNK 对 SiHa 细胞的增殖抑制作用比游离 HNK（IC=225.5μM）更有效（IC=14.68μM）。与 HaCaT 细胞相比，PLGA-HNK 与阴性对照相比没有显著差异。这些结果导致 HNK 的生物利用度增加，从而提高了其生物活性。预测分析表明，HNK 通过抑制 E6 和 MDM2 对 SiHa 细胞具有细胞毒性作用，这可能是其主要作用机制。
