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来自Saiga鹿角的TRPA1-激活:查,相互作用机制和生物活性

Chengwei Wang¹, Chunjie Wu^2,3, Linjiang Song⁴

¹State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.

International journal of molecular sciences

|March 13, 2025

概括

鉴定出了针对TRPA1通道的赛加羊角 (THPs). 这些THP激活TRPA1,增加RIN-14B细胞中细胞内和血清素的释放.

科学领域:

药理学药理学是指药理学的学科.
传统中国医药传统中国医药
分子生物学分子生物学

背景情况:

赛加羊角 (SAH) 是一种传统的中医药,其机制和活性成分尚不清楚.
暂时受体潜能安基林1 (TRPA1) 是一个关键的离子通道,涉及各种生理过程.

研究的目的:

从SAH消化物中识别与TRPA1.1相互作用的高 afinity (THPs).
研究已识别的THPs对TRPA1激活和血清素 (5-HT) 分泌的生物学影响.

主要方法:

在模拟的胃肠道条件下进行SAH消化.
结合流体染色学-质谱学 (AUF-LC/MS) 的亲和超过,用于选.
分子对接和生物活性数据库分析用于THP识别.
使用RIN-14B细胞进行细胞测试 (免疫光,ELISA,西部斑) 来评估TRPA1激活和5-HT通路调节.

主要成果:

从SAH消化器中确定了大约200种TRPA1结合.
确定了三种高 afinity (THP):RCWPDCR,FGFDGDF 和 WFCEGSF.
THPs激活TRPA1,导致RIN-14B细胞内细胞内Ca2+度增加和5-HT分泌.
通过对TPH1和Ddc进行上调和对SERT进行下调,THPs调节了5-HT合成途径.

结论:

针对TRPA1的亲和力分析成功识别了SAH.的生物活性.
已识别的THP激活TRPA1通道,并通过调节5-HT合成途径来增强5-HT释放.

关键词:

5HT的使用方法是: 5-HT 在AUF-LC/MS中.赛加鹿的鹿角是什么意思在 TRPA1 中,酸是一种酸.

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