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使用无标签细胞表型试验发现来自Stephania epigaea的多巴胺D1受体对抗剂

Hongjian Kang¹, Hongming Tang¹, Jixia Wang²

¹State Key Laboratory of Phytochemistry and Natural Medicines, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian 116023, China; University of Chinese Academy of Sciences, Beijing 100049, China.

|August 20, 2025

概括

研究人员发现了来自传统中药Stephania epigaea的新型多巴胺D1受体 (D1R) 抗剂. 这些化物可能解释了S. epigaea的缓解疼痛和肠道效应,有助于开发D1R抗药物.

科学领域:

药理学
自然产品化学
神经科学

背景情况:

斯蒂芬尼 (S. epigaea) 是一种用于治疗腹痛和疟疾的中国传统药物.
多巴胺系统,特别是多巴胺D1受体 (D1R),与疼痛和肠道调节有关.
通过S. epigaea成分与D1R相互作用的机制在很大程度上是未知的.

研究的目的:

来识别针对D1R的S. epigaea的化物.
评估这些针对D1R的类化合物的效能和结构-活性关系 (SAR).
阐明S. epigaea治疗作用的潜在机制.

主要方法:

使用HEK293-D1R细胞模型和无标签的表型试验对S. epigaea的24种化物进行查.
通过同刺激测定,对D1R抗活性进行表征,包括IC50的确定和动态结合概况.
确定化合物的分子对接与人类D1R晶体结构以分析SAR.

主要成果:

六种类化合物,包括卡普胺, (-) - 离散素, (+) - 科里达林,N - 甲基乌罗氨酸, (+) - 异氨酸和O - 甲基布尔博卡,被确定为新型D1R抗剂.
卡波里明和 (-) - 分泌素显示出强烈的D1R抗作用 (IC50分别为0. 16±0. 02μM和0. 25±0. 01μM).
N- 甲基氨酸也显示了D1R抗活性 (IC50 = 1. 65 ± 0. 20μM),所有已确认的抗剂都具有竞争力.

结论:

这项研究确定了S. epigaea的强有力的D1R抗剂,为其传统用途提供了机制性见解.
这些发现为开发基于D1R抗剂的新疗法提供了有价值的信息.
已识别的化物及其SARs有助于理解天然产品对多巴胺基系统的调节.

关键词:

类化合物敌对者多巴胺D1受体没有标签的细胞表型检测斯蒂芬尼亚

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