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.
Phytochemistry. 2022 Jul;199:113209. doi: 10.1016/j.phytochem.2022.113209. Epub 2022 Apr 14.
Eleven undescribed isoquinoline alkaloids corybungines A-K including a protoberberine-type alkaloid, an isoquinoline alkaloid with a unique 6-norprotoberberine skeleton, one 13,14-seco-protoberberine-type alkaloid, two 1a,14-seco-protoberberine-type alkaloids with a 4-(hydroxymethyl)phenoxy moiety and six aporphine alkaloids, together with seven known alkaloids, have been isolated from the whole herb extract of Corydalis bungeana Turcz. Their structures and absolute configurations were elucidated based on an analysis of spectroscopic data and electronic circular dichroism (ECD) spectra. (R)-stephanine displayed high antagonistic activity against the dopamine D2 receptor with an IC value of 0.85 ± 0.09 μM in CHO-D2 cells. Additionally, corybungines D, F, H, (R)-roemerine, (R)-vireakine and (R)-tuduranine showed moderate D2 antagonism (IC 5.20-26.07 μM). The preliminary structure-activity relationships (SARs) of aporphine alkaloids were discussed.
从藏边罂粟全草提取物中分离得到 11 个未描述的异喹啉生物碱，包括一个原小檗碱型生物碱、一个具有独特的 6-去原小檗碱骨架的异喹啉生物碱、一个 13,14-裂原小檗碱型生物碱、两个具有 4-(羟甲基)苯氧基部分的 1a,14-裂原小檗碱型生物碱和六个阿朴啡生物碱，以及 7 个已知的生物碱。基于光谱数据分析和电子圆二色性（ECD）光谱，确定了它们的结构和绝对构型。（R）-石杉碱对多巴胺 D2 受体具有高拮抗活性，在 CHO-D2 细胞中的 IC 值为 0.85±0.09 μM。此外，corybungines D、F、H、（R）-roemerine、（R）-vireakine 和（R）-tuduranine 对 D2 受体具有中等拮抗活性（IC5.20-26.07 μM）。讨论了阿朴啡生物碱的初步构效关系（SAR）。
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