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应用草药芯片平台筛选与血管内皮生长因子结合的草药提取物。

Screening of herbal extracts binding with vascular endothelial growth factor by applying HerboChip platform.

作者信息

Liu Yang, Liang Jia-Ming, Guo Guo-Xia, Qiu Yu-Huan, Yu Le-Le, Tsim Karl Wah-Keung, Qin Qi-Wei, Chan Gallant Kar-Lun, Hu Wei-Hui

机构信息

College of Marine Sciences, South China Agricultural University, Guangzhou, 510642, China.

Nansha-South China Agricultural University Fishery Research Institute, Guangzhou, 511464, China.

出版信息

Chin Med. 2024 Sep 9;19(1):122. doi: 10.1186/s13020-024-00987-x.

DOI:10.1186/s13020-024-00987-x
PMID:39252102
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11382504/
Abstract

BACKGROUND

Traditional Chinese medicine (TCM) has been hailed as a rich source of medicine, but many types of herbs and their functions still need to be rapidly discovered and elucidated. HerboChip, a target-based drug screening platform, is an array of different fractions deriving from herbal extracts. This study was designed to identify effective components from TCM that interact with vascular endothelial growth factor (VEGF) as a target using HerboChip.

METHODS

Selected TCMs that are traditionally used as remedies for cancer prevention and wound healing were determined and extracted with 50% ethanol. Biotinylated-VEGF was hybridized with over 500 chips coated with different HPLC-separated fractions from TCM extracts and straptavidin-Cy5 was applied to identify plant extracts containing VEGF-binding fractions. Cytotoxicity of selected herbal extracts and their activities on VEGF-mediated angiogenic functions were evaluated.

RESULTS

Over 500 chips were screened within a week, and ten positive hits were identified. The interaction of the identified herbal extracts with VEGF was confirmed in cultured endothelial cells. The identified herbs promoted or inhibited VEGF-mediated cell proliferation, migration and tube formation. Results from western blotting analysis demonstrated the identified herbal extracts significantly affected VEGF-triggered phosphorylations of eNOS, Akt and Erk. Five TCMs demonstrated potentiating activities on the VEGF response and five TCMs revealed suppressive activities.

CONCLUSIONS

The current results demonstrated the applicability of the HerboChip platform and systematically elucidated the activity of selected TCMs on angiogenesis and its related signal transduction mechanisms.

摘要

背景

中药被誉为丰富的药物来源，但许多草药种类及其功能仍有待快速发现和阐明。HerboChip是一种基于靶点的药物筛选平台，是由草药提取物衍生而来的不同馏分的阵列。本研究旨在使用HerboChip鉴定以血管内皮生长因子（VEGF）为靶点的中药有效成分。

方法

确定传统上用于预防癌症和促进伤口愈合的所选中药，并用50%乙醇提取。将生物素化的VEGF与500多个涂有中药提取物不同高效液相色谱分离馏分的芯片杂交，并应用链霉亲和素-Cy5鉴定含有VEGF结合馏分的植物提取物。评估所选草药提取物的细胞毒性及其对VEGF介导的血管生成功能的活性。

结果

一周内筛选了500多个芯片，鉴定出10个阳性结果。在培养的内皮细胞中证实了所鉴定的草药提取物与VEGF的相互作用。所鉴定的草药促进或抑制VEGF介导的细胞增殖、迁移和管形成。蛋白质印迹分析结果表明，所鉴定的草药提取物显著影响VEGF触发的eNOS、Akt和Erk的磷酸化。5种中药表现出对VEGF反应的增强活性，5种中药表现出抑制活性。

结论

目前的结果证明了HerboChip平台的适用性，并系统地阐明了所选中药对血管生成及其相关信号转导机制的活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/e3bbb84caee4/13020_2024_987_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/ed08d373e706/13020_2024_987_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/03589b427d83/13020_2024_987_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/22f54416c627/13020_2024_987_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/21b88e50ad11/13020_2024_987_Fig4a_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/343d89cd5010/13020_2024_987_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/45ff0de3a136/13020_2024_987_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/e3bbb84caee4/13020_2024_987_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/ed08d373e706/13020_2024_987_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/03589b427d83/13020_2024_987_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/22f54416c627/13020_2024_987_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/21b88e50ad11/13020_2024_987_Fig4a_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/343d89cd5010/13020_2024_987_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/45ff0de3a136/13020_2024_987_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f106/11382504/e3bbb84caee4/13020_2024_987_Fig7_HTML.jpg

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