de la Peña June Bryan I, Kim Chong Ah, Lee Hye Lim, Yoon Seo Young, Kim Hee Jin, Hong Eun Young, Kim Gun Hee, Ryu Jong Hoon, Lee Yong Soo, Kim Kyeong Man, Cheong Jae Hoon
Department of Pharmacy, Uimyung Research Institute for Neuroscience, Sahmyook University, 26-21 Kongneung-2-dong, Nowon-gu, Seoul, 139-742, Republic of Korea.
Arch Pharm Res. 2014 Feb;37(2):263-9. doi: 10.1007/s12272-013-0229-9. Epub 2013 Aug 8.
Cirsium japonicum (CJ) has been shown to possess antidepressant-like properties. In the present study, we sought to identify which constituent of CJ might be responsible for its antidepressant effects and determine probable mechanism of action. The ethanol extract of CJ was administered to mice then behavioral changes were evaluated in the forced-swimming test (FST) and open-field test (OFT). In addition, its effects on norepinephrine (NE) reuptake and intracellular chloride (Cl(-)) flux were determined, in vitro. The effects of CJ's major constituents (linarin, pectolinarin, chlorogenic acid, luteolin) were also evaluated. CJ showed antidepressant-like effect by significantly reducing immobile behavior of mice in the FST, without increasing locomotor activity in the OFT. CJ had no effect on monoamine (NE) uptake, but it significantly promoted Cl(-) ion influx in human neuroblastoma cells. This CJ-induced Cl(-) influx was significantly blocked by co-administration of the competitive GABAA receptor antagonist, bicuculline. Among the major constituents of the CJ extract, only luteolin produced similar antidepressant-like effect, in vivo, and Cl(-) ion influx, in vitro. Altogether, the present results suggest that the antidepressant-like effect of CJ was most probably induced by its constituent luteolin, mediated through potentiation of the GABAA receptor-Cl(-) ion channel complex.
大蓟已被证明具有抗抑郁样特性。在本研究中，我们试图确定大蓟的哪种成分可能对其抗抑郁作用负责，并确定其可能的作用机制。将大蓟的乙醇提取物给予小鼠，然后在强迫游泳试验（FST）和旷场试验（OFT）中评估行为变化。此外，还在体外测定了其对去甲肾上腺素（NE）再摄取和细胞内氯离子（Cl⁻）通量的影响。还评估了大蓟主要成分（木犀草素、pectolinarin、绿原酸、木犀草素）的作用。大蓟通过显著减少FST中小鼠的不动行为而表现出抗抑郁样作用，而在OFT中不增加运动活性。大蓟对单胺（NE）摄取没有影响，但它显著促进了人神经母细胞瘤细胞中的Cl⁻离子内流。竞争性GABAA受体拮抗剂荷包牡丹碱共同给药可显著阻断这种大蓟诱导的Cl⁻内流。在大蓟提取物的主要成分中，只有木犀草素在体内产生了类似的抗抑郁样作用，在体外产生了Cl⁻离子内流。总之，目前的结果表明，大蓟的抗抑郁样作用很可能是由其成分木犀草素诱导的，通过增强GABAA受体-Cl⁻离子通道复合物介导。
