Xu Xiajing, Guo Yongli, Chen Menglin, Li Ning, Sun Yi, Ren Shumeng, Xiao Jiao, Wang Dongmei, Liu Xiaoqiu, Pan Yingni
School of Chinese Materia Medica, Key Laboratory for TCM Material Basis Study and Innovative Drug Development of Shenyang City, Shenyang Pharmaceutical University, Shenyang 110016, China.
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China.
Chin Herb Med. 2023 Jun 8;16(1):151-161. doi: 10.1016/j.chmed.2022.11.009. eCollection 2024 Jan.
To identify phytochemical constituents present in the extract of flowers of and evaluate their anti-oxidant and anti-hyperglycemic capacities.
The AlCl colorimetric method and Prussian Blue assay were used to determine the contents of total flavonoids and total phenolic acids in extraction layers, and the bioactive layers was screened through anti - oxidative activity . The Waters ACQUITY UPLC system and a Waters ACQUITY UPLC BEH C column (2.0 mm × 150 mm, 5 μm) were used to identify the ingredients. And anti-oxidative ingredients were screened by off-line UPLC-QTOF-MS/MS-free radical scavenging. The ameliorative role of it was further evaluated in a high-fat, streptozotocin-induced type 2 diabetic rat model and the study was carried out on NADPH oxidase (PDB ID: 2CDU) by molecular docking.
Combined with the results of activity screening , the anti - oxidative part was identified as the ethyl acetate layer. A total of 24 chemical constituents were identified by liquid chromatography-mass spectrometry in the ethyl acetate layer and 13 main anti-oxidative active constituents were preliminarily screened out through off-line UPLC-QTOF-MS/MS-free radical scavenging. experiments showed that flowers of could significantly reduce the blood glucose level of diabetic mice and alleviate liver cell damage. Based on the results of docking analysis related to the identified phytocompounds and oxidase which involved in type 2 diabetes, quercetin 3--rutinoside, kaempferol-3--rhamnoside, isorhamnetin-3--glucoside, and isoquercitrin showed a better inhibitory profile.
The ethyl acetate layer was rich in flavonoids and phenolic acids and had significant anti-oxidant activity, which could prevent hyperglycemia. This observed activity profile suggested flowers as a promising new source of tea to develop alternative natural anti-diabetic products with a high safety margin.
鉴定[植物名称]花提取物中的植物化学成分，并评估其抗氧化和降血糖能力。
采用氯化铝比色法和普鲁士蓝法测定提取物各层中总黄酮和总酚酸的含量，并通过抗氧化活性筛选生物活性层。使用沃特世ACQUITY UPLC系统和沃特世ACQUITY UPLC BEH C18柱（2.0 mm×150 mm，5μm）鉴定成分。通过离线UPLC-QTOF-MS/MS自由基清除筛选抗氧化成分。在高脂、链脲佐菌素诱导的2型糖尿病大鼠模型中进一步评估其改善作用，并通过分子对接对NADPH氧化酶（PDB ID：2CDU）进行研究。
结合活性筛选结果，确定抗氧化部分为乙酸乙酯层。通过液相色谱-质谱法在乙酸乙酯层中鉴定出24种化学成分，并通过离线UPLC-QTOF-MS/MS自由基清除初步筛选出13种主要抗氧化活性成分。实验表明，[植物名称]花可显著降低糖尿病小鼠的血糖水平，减轻肝细胞损伤。基于与鉴定出的植物化合物和参与2型糖尿病的氧化酶相关的对接分析结果，槲皮素3 - -芸香糖苷、山奈酚-3 - -鼠李糖苷、异鼠李素-3 - -葡萄糖苷和异槲皮苷表现出较好的抑制作用。
乙酸乙酯层富含黄酮类和酚酸类化合物，具有显著的抗氧化活性，可预防高血糖。这种观察到的活性特征表明，[植物名称]花有望成为开发具有高安全边际的替代天然抗糖尿病产品的新茶源。
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