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

Abstract

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.

Keywords:

• Coixol-CDP inclusion compound
• pharmacodynamics
• non-small cell lung cancer (NSCLC)

Authors’ contributions

X.C.W., S.Q.D., and B.P. contributed to the study conception and design. X.C.W., X.Y.S., L.C., and R.W. performed compound synthesis and identification. X.C.W., X.Y.S., M.Y.W., C.H.G., and R.R.X. performed cell culture and Western blots. X.C.W., X.Y.S., S.Q.D., and B.P. analyzed and interpreted the data. X.C.W., X.Y.S., S.Q.D., and B.P. wrote the first draft of the manuscript. All authors contributed to the manuscript revision and approved the submitted version.

Disclosure statement

No potential conflict of interest was reported by the authors.

Data availability statement

The datasets used and/or analyzed are available from the corresponding author upon reasonable request.

Additional information

Funding

This study was funded by the China Postdoctoral Science Foundation (2018M632401) and the Jiangsu Province Postgraduate Research & Practice Innovation Program (SJCX22_1830). The funding organization did not play a role in study design and execution, data interpretation, or manuscript writing.