姜黄素-羟丙基--环糊精包合物的制备及其体外抗肿瘤活性评价

李宁; 王雪婷; 蒋少鸿; 张子娜; 王汀

doi:10.13422/j.cnki.syfjx.20181891

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姜黄素-羟丙基--环糊精包合物的制备及其体外抗肿瘤活性评价

药剂 | 更新时间：2024-01-04

- 姜黄素-羟丙基--环糊精包合物的制备及其体外抗肿瘤活性评价
- Preparation of Inclusion Complex of Curcumin with Hydroxypropyl--cyclodextrin and Evaluation of Its Antitumor Activity
- 中国实验方剂学杂志 2018年24卷第19期页码：31-36
- 作者机构：
- 作者简介：
- 基金信息：
  
  安徽省高校自然科学研究项目（KJ2016SD28）
- DOI：10.13422/j.cnki.syfjx.20181891
  中图分类号： R96;R943
- 纸质出版日期：2018
- 稿件说明：
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李宁, 王雪婷, 蒋少鸿, 等. 姜黄素-羟丙基--环糊精包合物的制备及其体外抗肿瘤活性评价[J]. 中国实验方剂学杂志, 2018,24(19):31-36.

LI Ning, WANG Xue-ting, JIANG Shao-hong, et al. Preparation of Inclusion Complex of Curcumin with Hydroxypropyl--cyclodextrin and Evaluation of Its Antitumor Activity[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(19): 31-36.
李宁, 王雪婷, 蒋少鸿, 等. 姜黄素-羟丙基--环糊精包合物的制备及其体外抗肿瘤活性评价[J]. 中国实验方剂学杂志, 2018,24(19):31-36. DOI： 10.13422/j.cnki.syfjx.20181891.

LI Ning, WANG Xue-ting, JIANG Shao-hong, et al. Preparation of Inclusion Complex of Curcumin with Hydroxypropyl--cyclodextrin and Evaluation of Its Antitumor Activity[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(19): 31-36. DOI： 10.13422/j.cnki.syfjx.20181891.

摘要

目的：优选姜黄素-羟丙基-β-环糊精（CUR-HP-β-CD）包合物的制备工艺，并对其体外抗肿瘤活性进行评价。方法：采用乙醇-水共溶剂孵育-冻干法制备CUR-HP-β-CD包合物；以包合率为评价指标，运用正交试验优化CUR-HP-β-CD包合物的制备工艺；采用紫外分光光度法和荧光分光光度法验证包合物的形成；利用噻唑蓝（MTT）法检测CUR和CUR-HP-β-CD包合物对不同肿瘤细胞（人子宫颈癌细胞株HeLa细胞和人肝癌细胞株HepG2细胞）处理不同时间（24 h和48 h）后细胞活性的影响。结果：CUR-HP-β-CD包合物的最佳制备工艺为CUR与HP-β-CD的摩尔比1：3，溶剂比（无水乙醇-水）1：9，包合温度40℃，包合时间12 h；CUR包合率42.2%，其冻干品经鉴别已形成包合物。MTT试验结果表明随着药物浓度的增加，CUR和CUR-HP-β-CD包合物能明显降低HeLa细胞和HepG2细胞的活性，且二者的半抑制浓度接近，说明CUR-HP-β-CD包合物对肿瘤细胞的增殖具有很好的抑制作用。结论：优选的包合物制备工艺简单可行、重复性好，制备的CUR-HP-β-CD包合物很好地保留了CUR的生物活性。

Abstract

Objective: To optimize the preparation process of curcumin-hydroxypropyl-β-cyclodextrin(CUR-HP-β-CD) inclusion complex and to evaluate its in vitro antitumor activity. Method: CUR-HP-β-CD inclusion complex was prepared by the procedure of ethanol-water cosolvent incubation-lyophilization;the preparation technology was optimized by orthogonal test with inclusion rate as index.CUR-HP-β-CD inclusion complex was characterized by ultraviolet spectrophotometry(UV) and fluorescence spectrophotometry.The cell viability of different types of cancer cells(human cervical cancer cell line HeLa cells and human hepatoma cell line HepG2 cells) was measured by microculture tetrazolium(MTT) assay through exposing cells to different concentrations of CUR-HP-β-CD inclusion complex for different times(24 h and 48 h). Result: The optimum process for preparation of CUR-HP-β-CD was as follows:the molar ratio of CUR to HP-β-CD of 1:3

the cosolvent ratio (absolute ethanol-water) of 1:9

the reaction temperature at 40℃ and the reaction time for 12 h;under these conditions

the inclusion rate was 42.2%

its lyophilized product had formed CUR-HP-β-CD inclusion complex.Both CUR-HP-β-CD inclusion complex and free CUR reduced the viability of HeLa and HepG2 cells in a dose-dependent manner

and their half-inhibitory concentrations were close

showing that CUR-HP-β-CD inclusion complex still exhibited significant cytotoxicity to cancer cells. Conclusion: The optimized technique is simple and reproducible.Besides

CUR-HP-β-CD inclusion complex retains the bioactivity of CUR.

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