Han Yan-qi, Xu Jun, Gong Su-xiao, Zhang Tie-jun, Liu Chang-xiao
Yao Xue Xue Bao. 2016 Aug;51(8):1302-8.
The chemical constituents of Corydalis Rhizoma were identified in the 60% ethanol extract using high performance liquid chromatography/electrospray ionization quadruple time-of-flight mass spectrometry (HPLC-QTOF/MS). The stimulation and inhibition effects of Corydalis Rhizoma and its representative compounds (protopine, palmatine, tetrahydropalmatine) on G protein-coupled receptor (GPCR), including 5-hydroxytryptamine 1A receptor(5-HT(1A)), μ opioid receptor (OPRM1), β(2) adrenergic receptor (ADRB2), dopamine receptor (D(2)), acetylcholine receptor (M(2)) and thromboxane-prostaglandin receptor (TP) were explored using the fluorescence assay of intracellular calcium ion. As a result, 31 compounds were obtained and 28 alkaloid compounds were identified. The results of GPCR experiments showed that Corydalis Rhizoma could activate 5-HT(1A), OPRM1, ADRB2 receptors and block D(2) receptor. Protopine showed antagonism on D2 and M2 receptors, tetrahydropalmatine could agitate ADRB2 receptor and antagonize D(2) and TP receptors, while palmatine showed no significant biological activity on the 6 GPCRs. In conclusion, Corydalis Rhizoma may exert biological activity by multi-components acting on multi-targets.
采用高效液相色谱/电喷雾电离四级杆飞行时间质谱（HPLC-QTOF/MS）对延胡索60%乙醇提取物中的化学成分进行鉴定。采用细胞内钙离子荧光测定法，研究延胡索及其代表性化合物（原阿片碱、巴马汀、四氢巴马汀）对G蛋白偶联受体（GPCR）的激动和抑制作用，包括5-羟色胺1A受体（5-HT(1A)）、μ阿片受体（OPRM1）、β(2)肾上腺素能受体（ADRB2）、多巴胺受体（D(2)）、乙酰胆碱受体（M(2)）和血栓素-前列腺素受体（TP）。结果，共得到31种化合物，鉴定出28种生物碱化合物。GPCR实验结果表明，延胡索可激活5-HT(1A)、OPRM1、ADRB2受体，并阻断D(2)受体。原阿片碱对D2和M2受体表现出拮抗作用，四氢巴马汀可激动ADRB2受体，并拮抗D(2)和TP受体，而巴马汀对6种GPCRs未表现出明显的生物学活性。综上所述，延胡索可能通过多成分作用于多靶点发挥生物学活性。
