Preparation, characterization, and anticancer effects of an inclusion complex of coixol with β-cyclodextrin polymers

• Published in: Pharmaceutical biology 2024-12, Vol.62 (1), p.2294331-2294331
• Main Authors: Wang, Xing-Chen, Shen, Xin-Yu, Chen, Lin, Wei, Rong, Wei, Ming-Yuan, Gu, Cai-Hong, Xu, Rong-Rong, Ding, Sheng-Qing, Pan, Bo
• Format: Article
• Language: English
• Subjects: Apoptosis; beta-Cyclodextrins - pharmacology; Cancer; Carcinoma, Non-Small-Cell Lung - drug therapy; Cell cycle; Cell proliferation; Coix; Coixol-CDP inclusion compound; Flow cytometry; Freeze drying; Humans; Lung Neoplasms - drug therapy; non-small cell lung cancer (NSCLC); Non-small cell lung carcinoma; pharmacodynamics; Polymers - pharmacology; Small cell lung carcinoma; Therapeutic applications; Water; Western blotting; β-Cyclodextrin
• ISSN: 1388-0209; 1744-5116
• DOI: 10.1080/13880209.2023.2294331

[ L. var. (Roman.) Stapf (Poaceae)], a crop of medicinal and edible significance, contains coixol, which has demonstrated anticancer properties. However, the limited solubility of coixol restricts its potential therapeutic applications. This study prepared a water-soluble coixol-β-cyclodextrin polymer (CDP) inclusion compound and evaluated its anticancer effect. The coixol-CDP compound was synthesized through a solvent-stirring and freeze-drying technique. Its coixol content was quantified using HPLC, and its stability was tested under various conditions. The anticancer effects of the coixol-CDP compound (4.129, 8.259, 16.518, and 33.035 mg/L for 24, 48, and 72 h) on the proliferation of non-small cell lung cancer (NSCLC) A549 cells were evaluated using an MTT assay; cell morphology was examined by Hoechst nuclear staining; apoptosis and cell cycle was detected by flow cytometry; and the expression of apoptosis-related proteins was assessed by Western blots. The water-soluble coixol-CDP inclusion compound was successfully prepared with an inclusion ratio of 86.6% and an inclusion yield rate of 84.1%. The coixol content of the compound was 5.63% and the compound remained stable under various conditions. Compared to coixol alone, all 24, 48, and 72 h administrations with the coixol-CDP compound exhibited lower IC values (33.93 ± 2.28, 16.80 ± 1.46, and 6.93 ± 0.83 mg/L) in A549 cells; the compound also showed stronger regulatory effects on apoptosis-related proteins. These findings offer a new perspective for the potential clinical application of in NSCLC therapy and its future research.