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

IF 3.9 3区 医学 Q1 MEDICAL LABORATORY TECHNOLOGY Pharmaceutical Biology Pub Date : 2024-12-01 Epub Date: 2023-12-21 DOI:10.1080/13880209.2023.2294331
Xing-Chen Wang, Xin-Yu Shen, Lin Chen, Rong Wei, Ming-Yuan Wei, Cai-Hong Gu, Rong-Rong Xu, Sheng-Qing Ding, Bo Pan
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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.

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薏苡仁酚与β-环糊精聚合物包合物的制备、表征和抗癌作用
背景:薏苡[Coix lacryma-jobi L. var. mayuen (Roman.) Stapf (Poaceae)]是一种药用和食用作物,含有薏苡仁酚,具有抗癌功效。然而,薏苡仁醇的有限可溶性限制了其潜在的治疗应用:本研究制备了一种水溶性薏苡酚-β-环糊精聚合物(CDP)包合物,并评估了其抗癌效果:通过溶剂搅拌和冷冻干燥技术合成了薏苡醇-CDP化合物。材料和方法:通过溶剂搅拌和冷冻干燥技术合成了薏苡仁酚-CDP 化合物,采用高效液相色谱法对其薏苡仁酚含量进行了定量,并测试了其在各种条件下的稳定性。采用 MTT 法评估了薏苡仁酚-CDP 复合物(4.129、8.259、16.518 和 33.035 mg/L,24、48 和 72 h)对非小细胞肺癌(NSCLC)A549 细胞增殖的抗癌作用;采用 Hoechst 核染色法检测了细胞形态;采用流式细胞仪检测了细胞凋亡和细胞周期;采用 Western 印迹法评估了细胞凋亡相关蛋白的表达:结果:成功制备了水溶性薏苡仁酚-CDP包合物,其包合率为86.6%,包合率为84.1%。化合物中的薏苡仁酚含量为 5.63%,并且在各种条件下均保持稳定。与单独使用薏苡仁酚相比,薏苡仁酚-CDP 复合物在 A549 细胞中 24、48 和 72 小时给药的 IC50 值较低,分别为 33.93 ± 2.28、16.80 ± 1.46 和 6.93 ± 0.83 mg/L;该化合物对细胞凋亡相关蛋白的调节作用也更强:这些发现为 Coix 在 NSCLC 治疗中的潜在临床应用及其未来研究提供了新的视角。
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来源期刊
Pharmaceutical Biology
Pharmaceutical Biology 医学-药学
CiteScore
6.70
自引率
2.60%
发文量
191
审稿时长
1 months
期刊介绍: Pharmaceutical Biology will publish manuscripts describing the discovery, methods for discovery, description, analysis characterization, and production/isolation (including sources and surveys) of biologically-active chemicals or other substances, drugs, pharmaceutical products, or preparations utilized in systems of traditional medicine. Topics may generally encompass any facet of natural product research related to pharmaceutical biology. Papers dealing with agents or topics related to natural product drugs are also appropriate (e.g., semi-synthetic derivatives). Manuscripts will be published as reviews, perspectives, regular research articles, and short communications. The primary criteria for acceptance and publication are scientific rigor and potential to advance the field.
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