青蒿挥发油羟丙基--环糊精包合物的制备及其抗病毒活性分析

陆兆光; 万琴; 孟瑾; 吴云; 王振中; 萧伟

doi:10.13422/j.cnki.syfjx.20181406

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青蒿挥发油羟丙基--环糊精包合物的制备及其抗病毒活性分析

药剂与炮制 | 更新时间：2024-01-04

- 青蒿挥发油羟丙基--环糊精包合物的制备及其抗病毒活性分析
- Preparation of Hydroxypropyl--cyclodextrin Inclusion Complex of Volatile Oil in Artemisiae Annuae Herba and Analysis of Its Antiviral Activity
- 中国实验方剂学杂志 2018年24卷第18期页码：11-15
- 作者机构：
- 作者简介：
- 基金信息：
  
  国家“重大新药创制”科技重大专项（2013ZX09402203）
- DOI：10.13422/j.cnki.syfjx.20181406
  中图分类号： R285;R283.6
- 纸质出版日期：2018
- 稿件说明：
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陆兆光, 万琴, 孟瑾, 等. 青蒿挥发油羟丙基--环糊精包合物的制备及其抗病毒活性分析[J]. 中国实验方剂学杂志, 2018,24(18):11-15.

LU Zhao-guang, WAN Qin, MENG Jin, et al. Preparation of Hydroxypropyl--cyclodextrin Inclusion Complex of Volatile Oil in Artemisiae Annuae Herba and Analysis of Its Antiviral Activity[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(18): 11-15.
陆兆光, 万琴, 孟瑾, 等. 青蒿挥发油羟丙基--环糊精包合物的制备及其抗病毒活性分析[J]. 中国实验方剂学杂志, 2018,24(18):11-15. DOI： 10.13422/j.cnki.syfjx.20181406.

LU Zhao-guang, WAN Qin, MENG Jin, et al. Preparation of Hydroxypropyl--cyclodextrin Inclusion Complex of Volatile Oil in Artemisiae Annuae Herba and Analysis of Its Antiviral Activity[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(18): 11-15. DOI： 10.13422/j.cnki.syfjx.20181406.

摘要

目的：制备及表征青蒿挥发油羟丙基-β-环糊精（HP-β-CD）包合物，对包合物的体外抗病毒活性进行研究。方法：采用饱和水溶液法、研磨法、单相溶液法制备青蒿挥发油HP-β-CD包合物，通过显微鉴别、薄层色谱法、红外光谱法和紫外分光光度法对包合物进行表征，采用体外细胞培养法研究青蒿挥发油及其包合物抗呼吸道合胞病毒（RSV），柯萨奇病毒A16型（CA16）的活性。结果：单相溶液法为最佳包合方法，在HP-β-CD与青蒿挥发油的投料比8∶1，乙醇体积分数100%，包合温度25℃，包合时间2 h时包合效果最佳，包合率80.62%，表征手段表明包合物已生成。体外抗病毒结果表明青蒿挥发油与包合物对RSV的半数有效浓度（EC50）分别为3.12，0.28 mg·L-1，对CA16的EC50分别为9.14，0.59 mg·L-1。结论：单相溶液法制备青蒿挥发油HP-β-CD包合物的工艺稳定可行，该工艺可显著提高青蒿挥发油的包合率，且包合物的抗RSV和CA16活性较包合前更强。

Abstract

Objective: To prepare and characterize the inclusion complex of volatile oil in Artemisiae Annuae Herba and hydroxypropyl-β-cyclodextrin(HP-β-CD)

and investigate in vitro antiviral activity of this inclusion complex. Method: HP-β-CD inclusion complex of volatile oil in Artemisiae Annuae Herba were prepared by saturated aqueous solution method

hand grinding method and single phase solution method.Some analytical methods were applied for characterization of the inclusion complex.The inhibitory effects of volatile oil in Artemisiae Annuae Herba and its HP-β-CD inclusion complex on respiratory syncytial virus(RSV) and cossac virus type A16(CA16) were investigated by in vitro cell culture method. Result: Single phase solution method was the best inclusion method

and its best inclusion ratio was 80.62% when ratio of HP-β-CD and volatile oil was 8:1

concentration of ethanol was 100%

inclusion temperature was 25℃ and inclusion time was 2 h.A series of evident characteristics suggested the formation of this inclusion complex.The median effective concentration(EC50) of volatile oil in Artemisiae Annuae Herba and its HP-β-CD inclusion complex to RSV were 3.12

0.28 mg·L-1

respectively;and EC50 were 9.14

0.59 mg·L-1 against CA16

respectively. Conclusion: The preparation process of HP-β-CD inclusion complex of volatile oil in Artemisiae Annuae Herba by single phase solution method is stable and feasible

and it can significantly increase inclusion rate of volatile oil in Artemisiae Annuae Herba.Antiviral activity on RSV and CA16 of the inclusion complex is stronger than before inclusion.

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