Tsai Yu-Chen, Miyajima Hiroki, Chou Ming-Yang, Fujita Satoshi
Department of Frontier Fiber Technology and Sciences, University of Fukui, Fukui 910-8507, Japan.
ROHER Technology Co., Taichung 41141, Taiwan.
Int J Mol Sci. 2025 Aug 29;26(17):8420. doi: 10.3390/ijms26178420.
(AC), a medicinal fungus native to Taiwan, contains bioactive compounds such as triterpenoids with anticancer properties. However, their high lipophilicity results in poor aqueous solubility and limited bioavailability, restricting their therapeutic application. To address this issue, a nanoparticle-based delivery system was developed using chitosan, alginate, and hyaluronic acid to encapsulate AC extracts. AC-loaded nanoparticles (AC-NPs) with a particle size less than 100 nm improved drug solubility and facilitated intracellular accumulation. Assessment of cytotoxicity revealed that AC-NPs significantly and more effectively suppressed the growth of breast cancer cells than free AC extracts. After 72 h, IC values for MDA-MB-231 (triple-negative) and MCF-7 (estrogen receptor-positive) were 46.9 and 75.6 μg/mL, respectively, with greater sensitivity observed in MDA-MB-231 cells. AC-NPs exhibited minimal toxicity toward normal mammary epithelial cells (NMuMG), indicating good biocompatibility. Fluorescently labeled AC-NPs showed rapid, time-dependent uptake in both cancer cell lines. Particularly, MDA-MB-231 cells exhibited rapid internalization, whereas MCF-7 cells likely benefited from hyaluronic acid-mediated targeting of CD44 receptors. In conclusion, AC-NPs enhanced the solubility, cellular uptake, and anticancer efficacy of AC while maintaining biocompatibility, thereby suggesting their robust potential as nanocarrier platforms for breast cancer therapy.
台湾原生药用真菌（AC）含有具有抗癌特性的三萜类等生物活性化合物。然而，它们的高亲脂性导致水溶性差和生物利用度有限，限制了其治疗应用。为了解决这个问题，利用壳聚糖、海藻酸盐和透明质酸开发了一种基于纳米颗粒的递送系统来包封AC提取物。粒径小于100nm的载AC纳米颗粒（AC-NPs）提高了药物溶解度并促进了细胞内积累。细胞毒性评估显示，与游离AC提取物相比，AC-NPs能显著且更有效地抑制乳腺癌细胞的生长。72小时后，MDA-MB-231（三阴性）和MCF-7（雌激素受体阳性）的IC值分别为46.9和75.6μg/mL，MDA-MB-231细胞的敏感性更高。AC-NPs对正常乳腺上皮细胞（NMuMG）表现出最小毒性，表明具有良好的生物相容性。荧光标记的AC-NPs在两种癌细胞系中均显示出快速的、时间依赖性摄取。特别是，MDA-MB-231细胞表现出快速内化，而MCF-7细胞可能受益于透明质酸介导的CD44受体靶向作用。总之，AC-NPs提高了AC的溶解度、细胞摄取和抗癌功效，同时保持了生物相容性，从而表明它们作为乳腺癌治疗纳米载体平台具有强大的潜力。
