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从紫堇属植物中分离得到具有结构多样性的异喹啉和酰胺生物碱,具有多巴胺 D2 受体拮抗作用。

Structurally diverse isoquinoline and amide alkaloids with dopamine D2 receptor antagonism from Corydalis bungeana.

机构信息

Key Laboratory of Separation Science for Analytical Chemistry, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, People's Republic of China; University of Chinese Academy of Sciences, Beijing 100049, People's Republic of China.

Key Laboratory of Separation Science for Analytical Chemistry, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, People's Republic of China.

出版信息

Fitoterapia. 2022 Jun;159:105175. doi: 10.1016/j.fitote.2022.105175. Epub 2022 Mar 13.

Abstract

Four new isoquinoline alkaloids including a benzophenanthridine alkaloid (1), a morphine derivative (2), a narceine-type alkaloid (3) and a simple isoquinoline alkaloid (4), a new amide alkaloid (5) and a new phthalic acid derivative (6), together with eleven known alkaloids (7-17) were obtained from the whole herbs extract of Corydalis bungeana Turcz. Their structures and absolute configurations were elucidated by extensive spectroscopic data analysis including HRESIMS, NMR and electronic circular dichroism (ECD) and ECD calculation. Compounds 1-17 were evaluated for dopamine D2 receptor activity in CHO-D2 cells. Among them, 16 showed the highest antagonistic activity on the D2 receptor with an IC value of 2.04 ± 0.01 μM. Compounds 14 and 15 exhibited moderate antagonism with IC values of 13.66 ± 2.28 and 31.72 ± 2.52 μM, respectively.

摘要

从紫堇属全草提取物中分离得到了四个新的异喹啉生物碱,包括一个苯并菲啶生物碱(1)、一个吗啡衍生物(2)、一个那可丁型生物碱(3)和一个简单的异喹啉生物碱(4)、一个新的酰胺生物碱(5)和一个新的邻苯二甲酸衍生物(6),以及 11 个已知生物碱(7-17)。通过广泛的光谱数据分析,包括 HRESIMS、NMR 和电子圆二色性(ECD)和 ECD 计算,确定了它们的结构和绝对构型。对 1-17 进行了多巴胺 D2 受体活性评价。其中,16 对 D2 受体表现出最高的拮抗活性,IC 值为 2.04±0.01 μM。化合物 14 和 15 表现出中等拮抗活性,IC 值分别为 13.66±2.28 和 31.72±2.52 μM。

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