【作者】 赵烽； 许卉； 张明浩； 刘珂；

【Author】 Feng Zhao, Hui Xu, Ming-Hao Zhang, Ke Liu Department of Medicinal Chemistry, School of Pharmacy, Yantai University, Yantai 264005

【机构】 烟台大学药学院天然药物化学教研室；

【摘要】 目的:考察木香倍半萜对LPS诱导的小鼠巨噬细胞释放NO的抑制活性,并探讨其构效关系。方法;采用LPS诱导小鼠巨噬细胞RAW 264．7释放NO,用Griess法测定木香提取物及木香倍半萜对LPS诱导的小鼠巨噬细胞释放NO的抑制率,用MTT法评价细胞毒性。结果:木香石油醚层和乙酸乙酯层提取物对活化的小鼠巨噬细胞释放NO具有明显的抑制作用,IC50分别为 0．10μg／ml和0．86 μg／ml。木香倍半萜对小鼠巨噬细胞释放NO的抑制活性和化学结构之间存在一定的构效关系规律,内酯环及环外双键对于木香倍半萜的NO释放抑制活性具有重要的意义。更多还原

【Abstract】 Objective: To evaluate the inhibitory activities of sesquiterpenes from Aucklandia lappa on LPS-induced NO release of mouse macrophage, and study the relationship between the chemical structures and the inhibitory activities. Methods: Determine the quantity of NO by Griess assay and calculate the inhibitory rate of NO release in mouse macrophage RAW 264.7. Evaluate the cytotoxicity by MTT method. Results: The petrol, EtOAc soluble fraction of Aucklandia lappa significantly inhibited NO release induced by LPS, IC50 values are 0.10 μg/ml and 0.86 μg/ml, respectively. Some revelation between the chemical structures and the NO release inhibitory activities were found, the lactone group is seemed to be very important for the NO release inhibitory activity.更多还原