Borchert Verena E, Czyborra Peter, Fetscher Charlotte, Goepel Mark, Michel Martin C
Medizinische Klinik, Universitätsklinikum Essen, Essen, Germany.
Naunyn Schmiedebergs Arch Pharmacol. 2004 Mar;369(3):281-6. doi: 10.1007/s00210-004-0869-x. Epub 2004 Feb 13.
Since extracts from the plants Rhois aromatica and Solidaginis virgaurea are being used in the phytotherapy of bladder dysfunction including the overactive bladder syndrome, and since muscarinic receptors are the main pharmacological target in the treatment of bladder dysfunction, we have investigated whether these extracts can inhibit carbachol-induced, muscarinic receptor-mediated contraction of rat and human bladder. In vitro contraction experiments were performed with rat and human bladder strips. Radioligand binding and inositol phosphate accumulation studies were done with cells transfected with human M(2) or M(3) muscarinic receptors. Both extracts concentration-dependently (final concentrations 0.01-0.1%) inhibited carbachol-induced contraction of rat and human bladder with insurmountable antagonism. Radioligand binding experiments and inositol phosphate accumulation studies with cloned receptors demonstrated direct but non-competitive effects on muscarinic receptors. Reductions of KCl-induced bladder contraction demonstrated that inhibition by the higher extract concentrations also involved receptor-independent effects. We conclude that extracts from Rhois aromatica and Solidaginis virgaurea inhibit muscarinic receptor-mediated contraction of rat and human bladder. While this could contribute to the beneficial effects of these extracts in patients with bladder dysfunction, such therapeutic effects remain to be demonstrated in controlled clinical studies.
由于芳香蛇菰和兴安一枝黄花的植物提取物正被用于包括膀胱过度活动症在内的膀胱功能障碍的植物疗法,且毒蕈碱受体是膀胱功能障碍治疗中的主要药理学靶点,我们研究了这些提取物是否能抑制卡巴胆碱诱导的、毒蕈碱受体介导的大鼠和人类膀胱收缩。用大鼠和人类膀胱条进行体外收缩实验。对转染了人类M(2)或M(3)毒蕈碱受体的细胞进行放射性配体结合和肌醇磷酸积累研究。两种提取物均呈浓度依赖性(终浓度0.01 - 0.1%)抑制卡巴胆碱诱导的大鼠和人类膀胱收缩,具有不可克服的拮抗作用。对克隆受体进行的放射性配体结合实验和肌醇磷酸积累研究表明,其对毒蕈碱受体有直接但非竞争性的作用。高浓度提取物对氯化钾诱导的膀胱收缩的抑制作用表明,其抑制作用还涉及非受体依赖性效应。我们得出结论,芳香蛇菰和兴安一枝黄花的提取物抑制大鼠和人类膀胱毒蕈碱受体介导的收缩。虽然这可能有助于这些提取物对膀胱功能障碍患者产生有益作用,但这种治疗效果仍有待在对照临床研究中得到证实。