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

Context Coix [Coix lacryma-jobi L. var. mayuen (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.Objective This study prepar...

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Main Authors: Xing-Chen Wang, Xin-Yu Shen, Lin Chen, Rong Wei, Ming-Yuan Wei, Cai-Hong Gu, Rong-Rong Xu, Sheng-Qing Ding, Bo Pan
Format: Article
Language:English
Published: Taylor & Francis Group 2024-12-01
Series:Pharmaceutical Biology
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Online Access:https://www.tandfonline.com/doi/10.1080/13880209.2023.2294331
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Summary:Context Coix [Coix lacryma-jobi L. var. mayuen (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.Objective This study prepared a water-soluble coixol-β-cyclodextrin polymer (CDP) inclusion compound and evaluated its anticancer effect.Materials and methods 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.Results 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 IC50 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.Discussion and conclusions These findings offer a new perspective for the potential clinical application of Coix in NSCLC therapy and its future research.
ISSN:1388-0209
1744-5116