DataSheet1_Study on the vasodilatory activity of lotus leaf extract and its representative substance nuciferine on thoracic aorta in rats.docx

Lotus (Nelumbo nucifera) leaves are widely used for both edible and medicinal applications. For its further utilization, we studied the vasodilatory activity of lotus leaf extract for the first time. In this study, we obtained the extracts using different ratios of water and ethanol, which was followed by polarity-dependent extraction. We found that the CH2Cl2 layer exhibited better vasodilatory activity (EC50 = 1.21 ± 0.10 μg/ml). HPLC and ESI-HRMS analysis of the CH2Cl2 layer using the standard product as a control revealed that nuciferine (Emax = 97.95 ± 0.76%, EC50 = 0.36 ± 0.02 μM) was the main component in this layer. Further research revealed that nuciferine exerts a multi-target synergistic effect to promote vasodilation, via the NO signaling pathway, K+ channel, Ca2+ channel, intracellular Ca2+ release, α and β receptors, etc. Nuciferine exhibits good vasodilatory activity, and it exhibits the potential to be utilized as a lead compound.

莲（Nelumbo nucifera）叶在食用与药用领域均拥有广泛应用。为推动其进一步开发利用，本研究首次探究了荷叶提取物的血管舒张活性。本研究采用不同水醇比例制备提取物，并随后开展极性梯度萃取。研究发现二氯甲烷（CH2Cl2）萃取层展现出更优异的血管舒张活性（半数有效浓度EC50=1.21±0.10 μg/ml）。以标准品为对照，通过高效液相色谱（HPLC）与电喷雾电离高分辨质谱（ESI-HRMS）对二氯甲烷萃取层进行分析，结果表明荷叶碱（nuciferine）为该萃取层的主要活性成分，其最大效应Emax=97.95±0.76%，半数有效浓度EC50=0.36±0.02 μM。进一步研究表明，荷叶碱可通过一氧化氮（NO）信号通路、钾离子（K+）通道、钙离子（Ca2+）通道、细胞内钙离子释放以及α、β受体等多种途径发挥多靶点协同作用，促进血管舒张。荷叶碱具备优良的血管舒张活性，具备开发为先导化合物的潜力。