Jiangsu Key Laboratory for Pharmacology and Safety Evaluation of Chinese Materia Medica, Jiangsu Collaborative Innovation Center of Traditional Chinese Medicine Prevention and Treatment of Tumor, School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China.
School of Artificial Intelligence and Information Technology, Nanjing University of Chinese Medicine, Nanjing, China.
Pharm Biol. 2020 Dec;58(1):208-218. doi: 10.1080/13880209.2020.1732429.
It is common sense that chewing a mint leaf can cause a cooling feeling, while chewing ginger root will produce a burning feeling. In Traditional Chinese Medicine (TCM), this phenomenon is referred to as 'cold/hot' properties of herbs. Herein, it is reported that TCM with different "cold/hot" properties have different effects on the variation of cells. To explore the intrinsic 'cold/hot' properties of TCM from the perspective of cellular and molecular biology. A375 cells were selected using Cancer Cell Line Encyclopaedia (CCLE) analysis and western blots. Hypaconitine and baicalin were selected by structural similarity analysis from 56 and 140 compounds, respectively. A wireless thermometry system was used to measure cellular temperature change induced by different compounds. Alteration of intracellular calcium influx was investigated by means of calcium imaging. The IC values of GSK1016790A, HC067047, hypaconitine, and baicalin for A375 cells are 8.363 nM, 816.4 μM, 286.4 μM and 29.84 μM, respectively. And, 8 μM hypaconitine induced obvious calcium influx while 8 μM baicalin inhibited calcium influx induced by TRPV4 activation. Cellular temperature elevated significantly when treated with GSK1016790A or hypaconitine, while the results were reversed when cells were treated with HC067047 or baicalin. The changes in cellular temperature are speculated to be caused by the alteration of intracellular calcium influx mediated by TRPV4. In addition, the 'cold/hot' properties of compounds in TCM can be classified by using cellular temperature detection.
常识告诉我们,咀嚼薄荷叶会产生清凉感,而咀嚼生姜则会产生灼热感。在中医(TCM)中,这种现象被称为草药的“寒/热”属性。在这里,据报道,具有不同“寒/热”属性的 TCM 对细胞变化有不同的影响。为了从细胞和分子生物学的角度探索 TCM 的内在“寒/热”特性。使用癌症细胞系百科全书(CCLE)分析和 Western blot 从 A375 细胞中选择 TCM。通过结构相似性分析,从 56 种和 140 种化合物中分别选择了乌头碱和黄芩苷。使用无线测温系统测量不同化合物引起的细胞温度变化。通过钙成像研究细胞内钙内流的变化。GSK1016790A、HC067047、乌头碱和黄芩苷对 A375 细胞的 IC 值分别为 8.363 nM、816.4 μM、286.4 μM 和 29.84 μM。并且,8 μM 乌头碱诱导明显的钙内流,而 8 μM 黄芩苷抑制 TRPV4 激活诱导的钙内流。用 GSK1016790A 或乌头碱处理时,细胞温度显著升高,而用 HC067047 或黄芩苷处理时,结果相反。细胞温度的变化推测是由 TRPV4 介导的细胞内钙内流的改变引起的。此外,还可以通过检测细胞温度来对 TCM 中化合物的“寒/热”属性进行分类。