梓醇全丙酰化产物的微波辅助合成及其神经保护作用初探

张秋霞; 程晓东; 李振兴; 董春红; 蒋士卿; 孙雨安; 王国庆

doi:10.12187/2021.04.010

CN 41-1437/TS ISSN 2096-1553

张秋霞 , 程晓东 , 李振兴 , 董春红 , 蒋士卿 , 孙雨安 , 王国庆

张秋霞, 程晓东, 李振兴, 等. 梓醇全丙酰化产物的微波辅助合成及其神经保护作用初探[J]. 轻工学报, 2021, 36(4): 78-85. doi: 10.12187/2021.04.010

引用本文: 张秋霞, 程晓东, 李振兴, 等. 梓醇全丙酰化产物的微波辅助合成及其神经保护作用初探[J]. 轻工学报, 2021, 36(4): 78-85. doi: 10.12187/2021.04.010

ZHANG Qiuxia, CHENG Xiaodong, LI Zhenxing, et al. Microwave-assisted synthesis of catalpol perpropionylated derivative product and its neuroprotective effect[J]. Journal of Light Industry, 2021, 36(4): 78-85. doi: 10.12187/2021.04.010

Citation: ZHANG Qiuxia, CHENG Xiaodong, LI Zhenxing, et al. Microwave-assisted synthesis of catalpol perpropionylated derivative product and its neuroprotective effect[J]. Journal of Light Industry, 2021, 36(4): 78-85. doi: 10.12187/2021.04.010

梓醇全丙酰化产物的微波辅助合成及其神经保护作用初探

1. 郑州轻工业大学材料与化学工程学院, 河南郑州 450001;
2. 平顶山学院化学与环境工程学院, 河南平顶山 467000;
3. 河南中医药大学中医药科学院, 河南郑州 450002

作者简介: 张秋霞(1971-),女,河南省平顶山市人,郑州轻工业大学硕士研究生,平顶山学院高级实验师,主要研究方向为化学合成与分析.;

基金项目: 国家自然科学基金国际合作与交流基金项目（8151101082）；河南省高等学校重点科研项目（20A350004）
中图分类号: TP393

Microwave-assisted synthesis of catalpol perpropionylated derivative product and its neuroprotective effect

1. College of Materials and Chemical Engineering, Zhengzhou University of Light Industry, Zhengzhou 450001, China;
2. School of Chemical and Environmental Engineering, Pingdingshan University, Pingdingshan 467000, China;
3. Academy of Chinese Medicine Science, He'nan University of Chinese Medicine, Zhengzhou 450002, China
Received Date: 2020-07-20

CLC number: TP393

摘要: 以梓醇、丙酸酐为原料，吡啶为溶剂和缚酸剂，利用微波辅助法合成梓醇全丙酰化衍生物（CP-6），通过正交试验对其合成条件进行优化，并采用四甲基偶氮唑盐微量酶反应比色法对其神经保护活性进行初步筛查.结果表明：当丙酸酐与梓醇物质的量比为18∶1，反应温度为80℃，反应时间为6 h，梓醇在吡啶中的质量浓度为25 g/L时，梓醇全丙酰化产物的相对含量可达98.51%；CP-6具有神经保护作用，是一种潜在的神经保护剂.
- 微波辅助合成 /
- 梓醇全丙酰化产物 /
- 神经保护剂
Abstract: Using catalpol and propionyl anhydride as raw materials, pyridine as solvent and acid binding agent, catalpol perpropionyl product (CP-6) was synthesised by microwave-assisted method. The synthesis conditions were optimized by orthogonal test, and the neuroprotective activity was initially screened by the colorimetric method of the tetramethylazolyzol salt trace enzyme reaction. The test results showed that when the molar ratio of propionic anhydride to catalpol was 18:1, the reaction temperature in the microwave reactor was 80℃, the reaction time was 6 h, and the mass concentration of catalpol in pyridine was 25 g/L, the relative content of CP-6 in the reaction system could reach 98. 51%. MTT method was used to screen the neuroprotec tive activity of CP-6, and the results showed that CP-6 had neuroprotective effect and may be a potential neu roprotective agent.
- microwave-assisted synthesis (MCAS) /
- catalpol perpropionylated derivativeproduct /
- neroprotective agent
1. [1]
  吉雪琪,孙鹏,祁建军,等. 地黄生长期根叶中梓醇及总环烯醚萜苷含量变化[J]. 中国中药杂志,2014,39(3):466.
2. [2]
  HUANG C L, CUI Y L, JI L L, et al. Catalpol decreases peroxynitrite formation and conse quently exerts cardioprotective effects against ischemia/reperfusion insult[J]. Pharmaceutical Biology,2013,51(4):463.
3. [3]
  谭灵莉,崔丹丹,祝慧凤,等. 梓醇对脑缺血后神经血管单元构筑的影响[J]. 中国药理学通报,2014,30(1):44.
4. [4]
  LEONG P K, CHEN J H, KO K M. Natural products and drug discovery:an integrated approach[M]. Netherlands:Academic Press, Elsevier, 2018:73-104.
5. [5]
  WAN D, YANG X, WANG Y, et al. Catalpol stimulates VEGF production via the JAK2/STAT3 pathway to improve angiogenesis in rats' stroke model[J]. Journal of Ethnopharmacolo gy, 2016,191:169.
6. [6]
  LIU L, GAO H W, WANG H B, et al. Catalpol promotes cellular apoptosis in human HCT116 colorectal cancer cells via microRNA-200 and the down regulation of PI3K-Akt signaling pathway[J]. Oncology Letters,2017,14(3):1168.
7. [7]
  LIN C, LU Y, YAN X J, et al. Catalpol pro tects glucose-deprived rat embryonic cardiac cells by inducing mitophagy and modulating estrogen receptor[J]. Biomedicine and Phar macotherapy, 2017,89:973.
8. [8]
  WANG J H, XIE H, ZHAO T K, et al. Catal pol regulates cholinergic nerve system function through effect on choline acetyl-transferase not M receptor affinity[J]. Biomedicine and Phar macotherapy, 2015, 69:291.
9. [9]
  PUNGITORE C R, LEÓN L G, GARCÍA C, et al. Novel antiprolifterative anlogs of the Taq DNA polymerase inhibitor catalpol[J]. Bioor ganic and Medicinal Chemistry Letters, 2007, 17(5):1332.
10. [10]
  DONG C H, LIU S L, CHENG X D, et al. Design, synthesis, and preliminary biological evaluation of catalpol propionates as antiaging drugs[J]. BMC Chemistry, 2019,13(109):1.
11. [11]
  王国庆,褚铭林,李振兴,等. ESI-HRMS法在梓醇丙酰化产物合成过程分析中的应用[J]. 轻工学报,2018,33(3):1.
12. [12]
  GAN S, ZAKARIA S, CHIA C H, et al. Syn thesis of kenaf cellulose carbamate using micro wave irradiation for preparation of cellu-lose membrane[J]. Carbohydrate Polymers, 2014, 106(15):160.
13. [13]
  ZHANG W S, LU P, WANG Z M, et al. Microwave-assisted suzuki coupling reaction for rapid synthesis of conjugated polymer poly (9, 9-dihexylfluorene) s as an example[J]. Journal of Polymer Science Part A:Polymer Chemistry, 2013,51(9):1950.
14. [14]
  河南中医药大学. 一种丙酰化的梓醇衍生物及其制备方法和应用:201810734124. 0[P]. 2018-02-07.
1. [1]
  张嫚 , 张国治 , 张康逸 , 何梦影 . 超声辅助酶解法制备小麦ACE抑制肽及其稳定性研究. 轻工学报, 2024, 0(0): -.
2. [2]
  张嫚 , 张国治 , 张康逸 , 何梦影 . 超声辅助酶解法制备小麦ACE抑制肽及其稳定性研究. 轻工学报, 2024, 39(5): 29-39. doi: 10.12187/2024.05.004
3. [3]
  章存勇 , 庄海锋 , 时雅琪 , 邹鹏 , 丁乃红 , 纵坤 , 贾良元 , 郭东锋 . 国内外雪茄烟叶热解产物差异性研究. 轻工学报, 2024, 0(0): -.
4. [4]
  章存勇 , 庄海锋 , 时雅琪 , 邹鹏 , 丁乃红 , 纵坤 , 贾良元 , 郭东锋 . 国内外雪茄烟叶热解产物差异性研究. 轻工学报, 2024, 39(5): 118-126. doi: 10.12187/2024.05.014

点击查看大图

计量

PDF下载量: 9
文章访问数: 703
引证文献数: 0

通讯作者: 陈斌, bchen63@163.com

1.
沈阳化工大学材料科学与工程学院沈阳 110142

张秋霞, 程晓东, 李振兴, 等. 梓醇全丙酰化产物的微波辅助合成及其神经保护作用初探[J]. 轻工学报, 2021, 36(4): 78-85. doi: 10.12187/2021.04.010

引用本文: 张秋霞, 程晓东, 李振兴, 等. 梓醇全丙酰化产物的微波辅助合成及其神经保护作用初探[J]. 轻工学报, 2021, 36(4): 78-85. doi: 10.12187/2021.04.010

梓醇全丙酰化产物的微波辅助合成及其神经保护作用初探

作者简介:张秋霞(1971-),女,河南省平顶山市人,郑州轻工业大学硕士研究生,平顶山学院高级实验师,主要研究方向为化学合成与分析.

1. 郑州轻工业大学材料与化学工程学院, 河南郑州 450001;
2. 平顶山学院化学与环境工程学院, 河南平顶山 467000;
3. 河南中医药大学中医药科学院, 河南郑州 450002

收稿日期: 2020-07-20

基金项目: 国家自然科学基金国际合作与交流基金项目（8151101082）；河南省高等学校重点科研项目（20A350004）

关键词:

摘要: 以梓醇、丙酸酐为原料，吡啶为溶剂和缚酸剂，利用微波辅助法合成梓醇全丙酰化衍生物（CP-6），通过正交试验对其合成条件进行优化，并采用四甲基偶氮唑盐微量酶反应比色法对其神经保护活性进行初步筛查.结果表明：当丙酸酐与梓醇物质的量比为18∶1，反应温度为80℃，反应时间为6 h，梓醇在吡啶中的质量浓度为25 g/L时，梓醇全丙酰化产物的相对含量可达98.51%；CP-6具有神经保护作用，是一种潜在的神经保护剂.

English Abstract

Microwave-assisted synthesis of catalpol perpropionylated derivative product and its neuroprotective effect

1. College of Materials and Chemical Engineering, Zhengzhou University of Light Industry, Zhengzhou 450001, China;
2. School of Chemical and Environmental Engineering, Pingdingshan University, Pingdingshan 467000, China;
3. Academy of Chinese Medicine Science, He'nan University of Chinese Medicine, Zhengzhou 450002, China

Received Date: 2020-07-20

Abstract: Using catalpol and propionyl anhydride as raw materials, pyridine as solvent and acid binding agent, catalpol perpropionyl product (CP-6) was synthesised by microwave-assisted method. The synthesis conditions were optimized by orthogonal test, and the neuroprotective activity was initially screened by the colorimetric method of the tetramethylazolyzol salt trace enzyme reaction. The test results showed that when the molar ratio of propionic anhydride to catalpol was 18:1, the reaction temperature in the microwave reactor was 80℃, the reaction time was 6 h, and the mass concentration of catalpol in pyridine was 25 g/L, the relative content of CP-6 in the reaction system could reach 98. 51%. MTT method was used to screen the neuroprotec tive activity of CP-6, and the results showed that CP-6 had neuroprotective effect and may be a potential neu roprotective agent.

参考文献 (14) 相关文章 (4)