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一种从黄芩中鉴定、筛选和测定潜在神经氨酸酶抑制剂的活性整合策略。

An activity-integrated strategy of the identification, screening and determination of potential neuraminidase inhibitors from Radix Scutellariae.

作者信息

Liu Wei, Wang Huilin, Zhu Bo, Yin Chengqian, Chen Shuyang, Li Jin, Yu Xie-An, Azietaku John Teye, An Mingrui, Gao Xiu-Mei, Chang Yan-Xu

机构信息

Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China.

Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin, China.

出版信息

PLoS One. 2017 May 9;12(5):e0175751. doi: 10.1371/journal.pone.0175751. eCollection 2017.

DOI:10.1371/journal.pone.0175751
PMID:28486473
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5423611/
Abstract

Small molecules isolated from herbal medicines (HMs) were identified as the potential neuraminidase inhibitors which are effective in influenza prevention and treatment. Unfortunately, current available screen methods of small molecules isolated from HMs are inefficient and insensitive. Here a novel Ultra Performance Liquid Chromatography coupled with diode-array detectors and auto-fraction collector / time-of-flight mass spectrometry (UPLC-DAD-FC/Q-TOF-MS) screening method with high efficiency was developed and validated to separate, collect, enrich, identify and quantify potential neuraminidase inhibitors from Radix Scutellariae. The results showed that 26 components with neuraminidase inhibitory activity were identified from Radix Scutellariae extracts. It was also found that the influence of origins on the quality of RS was more than that of cultivated time on the basis of the concentration of the effective components. These results brought novel insights into quality evaluation of Radix Scutellariae. It was demonstrated that new activity-integrated strategy was a suitable technique for the identification, screening and determination of potential neuraminidase inhibitors in herbal medicine and will provide novel potential strategies in other drug screening from herbal medicine.

摘要

从草药中分离出的小分子被鉴定为潜在的神经氨酸酶抑制剂，对预防和治疗流感有效。不幸的是，目前从草药中分离小分子的现有筛选方法效率低下且不灵敏。在此，开发并验证了一种高效的新型超高效液相色谱联用二极管阵列检测器和自动馏分收集器/飞行时间质谱（UPLC-DAD-FC/Q-TOF-MS）筛选方法，用于从黄芩中分离、收集、富集、鉴定和定量潜在的神经氨酸酶抑制剂。结果表明，从黄芩提取物中鉴定出26种具有神经氨酸酶抑制活性的成分。还发现，基于有效成分的浓度，产地对黄芩质量的影响大于栽培时间。这些结果为黄芩的质量评价带来了新的见解。结果表明，新的活性整合策略是一种适用于鉴定、筛选和测定草药中潜在神经氨酸酶抑制剂的技术，并将为从草药中筛选其他药物提供新的潜在策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/8ec6a332050f/pone.0175751.g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/ac494cdf0329/pone.0175751.g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/8caf4f7e29cb/pone.0175751.g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/84de6c278c05/pone.0175751.g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/d4c926ec75a3/pone.0175751.g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/dbf23f08b967/pone.0175751.g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/98a929b1e58a/pone.0175751.g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/8ec6a332050f/pone.0175751.g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/ac494cdf0329/pone.0175751.g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/8caf4f7e29cb/pone.0175751.g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/84de6c278c05/pone.0175751.g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/d4c926ec75a3/pone.0175751.g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/dbf23f08b967/pone.0175751.g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/98a929b1e58a/pone.0175751.g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55cd/5423611/8ec6a332050f/pone.0175751.g007.jpg

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