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采用超滤液相色谱-质谱联用技术筛选和鉴定参芪降糖颗粒中的 α-葡萄糖苷酶抑制剂。

Screening and identification of α-glucosidase inhibitors from Shenqi Jiangtang Granule by ultrafiltration liquid chromatography and mass spectrometry.

机构信息

College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou, China.

出版信息

J Sep Sci. 2018 Feb;41(3):797-805. doi: 10.1002/jssc.201700835. Epub 2017 Dec 27.

DOI:10.1002/jssc.201700835
PMID:29152897
Abstract

Shenqi Jiangtang Granule, a well-known traditional Chinese herbal preparation, has been widely used for the treatment of type II diabetes mellitus. In this work, an ultrafiltration liquid chromatography with quadrupole time-of-flight mass spectrometry method was proposed for the rapid identification of bioactive ingredients from Shenqi Jiangtang Granule using α-glucosidase as an example. First, the chemical profile of this preparation was clarified, including 37 saponins, 17 flavonoids, 37 lignans, and seven other compounds. After incubation with α-glucosidase in vitro, the methanol extract with an IC value of 0.19 mg/mL exhibited significant inhibitory activity. Then, 18 specific binding peaks were screened, and 15 peaks were identified. Among these, ten compounds were reported to have potential α-glucosidase inhibitory activity for the first time. Subsequently, the inhibitory activities of these active compounds were evaluated by ultraviolet spectrophotometry with p-nitrophenyl α-d-glucopyranoside as a substrate. As a result, gomisin J and gomisin D exhibited stronger α-glucosidase inhibitory activities than other active compounds with IC values of 77.69 and 133.85 μM, respectively. The results demonstrated that the integrated ultrafiltration liquid chromatography with mass spectrometry method was an effective and powerful tool for the discovery of active ingredients in Shenqi Jiangtang Granule.

摘要

参芪降糖颗粒是一种著名的中药制剂,广泛用于治疗 2 型糖尿病。本工作以α-葡萄糖苷酶为例,提出了一种超滤液相色谱-四极杆飞行时间质谱法,用于快速鉴定参芪降糖颗粒中的生物活性成分。首先,阐明了该制剂的化学成分,包括 37 种皂苷、17 种黄酮类化合物、37 种木脂素和 7 种其他化合物。体外孵育α-葡萄糖苷酶后,IC 值为 0.19mg/mL 的甲醇提取物表现出显著的抑制活性。然后,筛选出 18 个特定的结合峰,并鉴定出 15 个峰。其中,有 10 种化合物首次被报道具有潜在的α-葡萄糖苷酶抑制活性。随后,通过紫外分光光度法以对硝基苯-α-d-吡喃葡萄糖苷为底物评估这些活性化合物的抑制活性。结果表明,结合了质量光谱法的超滤液相色谱法是一种发现参芪降糖颗粒中活性成分的有效且强大的工具。

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