Zhang Jianmei, Zhou Jinyi, Yuan Qiaoyun, Zhan Changyi, Shang Zhi, Gu Qian, Zhang Ji, Fu Guangbo, Hu Weicheng
Jiangsu Collaborative Innovation Center of Regional Modern Agriculture & Environmental protection, Jiangsu Key Laboratory for Eco-Agricultural Biotechnology around Hongze Lake, Huaiyin Normal University, Huaian 223300, China.
Department of Urology, The Affiliated Huaian No.1 People's Hospital of Nanjing Medical University, Huaian, 223300, China.
J Ginseng Res. 2021 Mar;45(2):228-235. doi: 10.1016/j.jgr.2020.01.007. Epub 2020 Feb 5.
Ginsenoside compound K (GK) is a major metabolite of protopanaxadiol-type ginsenosides and has remarkable anticancer activities and . This work used an ionic cross-linking method to entrap GK within O-carboxymethyl chitosan (OCMC) nanoparticles (Nps) to form GK-loaded OCMC Nps (GK-OCMC Nps), which enhance the aqueous solubility and stability of GK.
The GK-OCMC Nps were characterized using several physicochemical techniques, including x-ray diffraction, transmission electron microscopy, zeta potential analysis, and particle size analysis via dynamic light scattering. GK was released from GK-OCMC Nps and was conducted using the dialysis bag diffusion method. The effects of GK and GK-OCMC Nps on PC3 cell viability were measured by using the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide assay. Fluorescent technology based on Cy5.5-labeled probes was used to explore the cellular uptake of GK-OCMC Nps.
The GK-OCMC NPs had a suitable particle size and zeta potential; they were spherical with good dispersion. drug release from GK-OCMC NPs was pH dependent. Moreover, the cytotoxicity study and cellular uptake assays indicated that the GK-OCMC Nps significantly enhanced the cytotoxicity and cellular uptake of GK toward the PC3 cells. GK-OCMC Nps also significantly promoted the activities of both caspase-3 and caspase-9.
GK-OCMC Nps are potential nanocarriers for delivering hydrophobic drugs, thereby enhancing water solubility and permeability and improving the antiproliferative effects of GK.
人参皂苷Compound K(GK)是原人参二醇型人参皂苷的主要代谢产物,具有显著的抗癌活性。本研究采用离子交联法将GK包裹于O-羧甲基壳聚糖(OCMC)纳米粒(Nps)中,形成载GK的OCMC纳米粒(GK-OCMC Nps),以提高GK的水溶性和稳定性。
采用多种物理化学技术对GK-OCMC Nps进行表征,包括X射线衍射、透射电子显微镜、zeta电位分析以及通过动态光散射进行粒径分析。采用透析袋扩散法测定GK从GK-OCMC Nps中的释放情况。采用3-(4,5-二甲基-2-噻唑基)-2,5-二苯基-2-H-四氮唑溴盐法测定GK和GK-OCMC Nps对PC3细胞活力的影响。基于Cy5.5标记探针的荧光技术用于探究GK-OCMC Nps的细胞摄取情况。
GK-OCMC NPs具有合适的粒径和zeta电位;呈球形,分散性良好。GK-OCMC NPs的药物释放具有pH依赖性。此外,细胞毒性研究和细胞摄取试验表明,GK-OCMC Nps显著增强了GK对PC3细胞的细胞毒性和细胞摄取。GK-OCMC Nps还显著促进了caspase-3和caspase-9的活性。
GK-OCMC Nps是递送疏水性药物的潜在纳米载体,可提高水溶性和通透性,增强GK的抗增殖作用。