Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing, PR China.
College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, PR China.
Drug Deliv. 2020 Dec;27(1):1176-1187. doi: 10.1080/10717544.2020.1801892.
Icaritin (ICT) and hydrous icaritin (HICT) are two similar flavonoids compounds isolated from Genus. This is the first comparative study on their and antitumor effects. Nanorods (NRs) were prepared for ICT and HICT by anti-solvent precipitation method using D-alpha tocopherol acid polyethylene glycol succinate (TPGS) as a stabilizer. The prepared ICT-NRs and HICT-NRs had similar diameter (155.5 nm and 201.7 nm), high drug loading content (43.30 ± 0.22% and 41.08 ± 0.19%), excellent stability and a similar sustaining drug release manner. Nanorods improved the toxicity against 4 different cancer cells in contrast to free ICT or free HICT; however, no significant difference was observed in this regard between ICT-NRs and HICT NRs. In the study on the anticancer efficacy on MCF-7 and PLC/PRE/5 tumor-bearing mice model, HICR-NRs displayed certain advantage over ICT NRs with higher tumor inhibition rate.
二氢杨梅素(ICT)和水合二氢杨梅素(HICT)是从 属中分离得到的两种相似的黄酮类化合物。这是对它们的 和抗肿瘤作用的首次比较研究。通过反溶剂沉淀法,使用 D-α生育酚聚乙二醇琥珀酸酯(TPGS)作为稳定剂,分别制备 ICT 和 HICT 的纳米棒(NRs)。所制备的 ICT-NRs 和 HICT-NRs 具有相似的直径(155.5nm 和 201.7nm)、高载药量(43.30±0.22%和 41.08±0.19%)、良好的稳定性和相似的持续药物释放方式。纳米棒提高了对 4 种不同癌细胞的 毒性,与游离 ICT 或游离 HICT 相比;然而,在这方面,ICT-NRs 和 HICT-NRs 之间没有观察到显著差异。在 MCF-7 和 PLC/PRE/5 荷瘤小鼠模型的抗癌功效研究中,HICR-NRs 显示出比 ICT-NRs 更高的肿瘤抑制率,具有一定优势。