| 基于在线HPLC-自由基清除检测-ESI-IT-TOF-MSn技术的蓝刺头抗氧化成分筛选及其构效关系研究 |
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| 引用本文： | 董馨,王弘,马飞祥,高建萍,陈世忠,薛培凤. 基于在线HPLC-自由基清除检测-ESI-IT-TOF-MSn技术的蓝刺头抗氧化成分筛选及其构效关系研究[J]. 中国药学, 2021, 30(4): 267-279. DOI: 10.5246/jcps.2021.04.022 |
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| 作者姓名： | 董馨 王弘 马飞祥 高建萍 陈世忠 薛培凤 |
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| 摘 要： | 蓝刺头是治疗骨质疏松的传统蒙药,其所含的有效成分不明确是限制其现代化、国际化发展的关键因素.传统活性物质筛选策略费时费力,本研究采用在线HPLC-自由基清除检测-ESI-IT-TOF-MS"技术对蓝刺头中有效成分进行筛选,实现分离、鉴定、活性筛选一体化.此外,该技术还有助于阐明活性成分间的构效关系.由于骨质疏松发病过程...
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| 关 键 词： | 蓝刺头 抗氧化剂 构效关系 在线HPLC-自由基清除检测 ESI-IT-TOF-MSn |
| 收稿时间： | 2020-03-29 |
A strategy for structure-activity relationship study on antioxidants in Echinops latifolius Tausch extracts by online HPLC-radical scavenging detection coupled with ESI-IT-TOF-MSn |
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| Xin Dong,Hong Wang,Feixiang Ma,Jianping Gao,Shizhong Chen,Peifeng Xue. A strategy for structure-activity relationship study on antioxidants in Echinops latifolius Tausch extracts by online HPLC-radical scavenging detection coupled with ESI-IT-TOF-MSn[J]. Journal of Chinese Pharmaceutical Sciences, 2021, 30(4): 267-279. DOI: 10.5246/jcps.2021.04.022 |
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| Authors: | Xin Dong Hong Wang Feixiang Ma Jianping Gao Shizhong Chen Peifeng Xue |
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| Abstract: | Echinops latifolius Tausch (ELT) is the traditional Mongolian medicine for the treatment of osteoporosis, and the ambiguous composition of active ingredients is an important factor in restricting the modernization and globalization of this herb. Considering the traditional activity screening strategy is time-consuming and labor intensive, online HPLC active ingredient detection coupled with ESI-IT-TOF-MSn strategy was employed in this study to isolate, identify and screen active compounds from the herbal medicines at the same time. The structure-activity relationship of these compounds was elucidated as well. Owing to the association of osteoporosis progression and oxidative stress, the antioxidants screening from ELT could be a good interpretive of the active substance in this herb. Meanwhile, DPPH equivalent method was an indicative of the most powerful antioxidant in ELT. Consequently, the screening and identification of the antioxidants in ELT was performed by using on-line HPLC-radical scavenging detection coupled with ESI-IT-TOF-MSn strategy, and the structure-activity relationship was investigated based on DPPH equivalent method. Finally, 20 constituents (including apigenin glucosides, caffeic acid, biscaffeoylquinic acids, biscaffeoylquinic acid methyl esters, ect.) were characterized in ELT extracts, and 18 components showed appreciable radical scavenging capacity. In addition, the structure-activity relationship study was carried out based on 14 compounds isolated from our laboratory, and the structural requirements of the compounds on antioxidant activity were obtained: (1) compounds with phenolic hydroxyl groups could have antioxidant activity; (2) the antioxidant activity could not be facilitated by the number of hydroxyl groups, but affected by the number of caffeoyl groups; (3) the substitution position of caffeoyl on quinic acid had a greater influence on DPPH activity; (4) methoxy groups could reduce the antioxidant activity. Collectively, this work provided the biochemical perspective to link active compounds and anti-osteoporosis action of ELT, and further explained how ELT worked in osteoporosis patients with bone loss. |
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| Keywords: | Echinops latifolius Tausch Antioxidants Structure-activity relationship Online HPLC-radical scavenging detection ESI-IT-TOF-MSn |
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