Choi B R, Kumar S K, Zhao C, Zhang L T, Kim C Y, Lee S W, Jeon J-H, Soní K K, Kim S H, Park N C, Kim H K, Park J K
Department of Urology, Chonbuk National University and Research Institute of Clinical Medicine of Chonbuk National University-Biomedical Research Institute and Clinical Trial Center of Medical Device of Chonbuk National University, Jeonju, Republic of Korea.
Department of Urology, Renji Hospital, Jiao Tong University School of Medicine, and Shanghai Institute of Andrology, Shanghai, China.
Int J Impot Res. 2015 Nov-Dec;27(6):225-32. doi: 10.1038/ijir.2015.23. Epub 2015 Oct 8.
The objective was to investigate the cellular effect and action mechanism of Artemisia capillaris extract (ACE) and its component, scopoletin, on penile corpus cavernosum smooth muscle (PCCSM). In vitro study with PCCSM, the precontracted PCCSM with phenylephrine was treated with ACE or scopoletin. Cyclic nucleotides in the perfusate were measured by radioimmunoassay and expression of protein and mRNA of endothelial nitric oxide synthase (eNOS) and neuronal nitric oxide synthase in the perfused PCCSM were measured by western blot and real-time PCR, respectively. The interaction of ACE or scopoletin with udenafil was also evaluated. ACE and scopoletin exerted a significant and concentration-dependent relaxation in PCCSM. The perfusion with ACE or scopoletin significantly increased cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) and the perfusion with ACE or scopoletin increased the expression of eNOS mRNA and protein. Furthermore, ACE or scopoletin enhanced udenafil-inducing relaxation in PCCSM. ACE and scopoletin relaxed the PCCSM mainly by activating nitric oxide-cGMP system and cAMP pathway and they may be additive therapeutic candidates for ED patients who do not completely respond to udenafil.
目的是研究茵陈蒿提取物(ACE)及其成分东莨菪素对阴茎海绵体平滑肌(PCCSM)的细胞效应和作用机制。在对PCCSM进行的体外研究中,用苯肾上腺素预收缩的PCCSM用ACE或东莨菪素处理。通过放射免疫测定法测量灌注液中的环核苷酸,并用蛋白质印迹法和实时PCR分别测量灌注的PCCSM中内皮型一氧化氮合酶(eNOS)和神经元型一氧化氮合酶的蛋白质和mRNA表达。还评估了ACE或东莨菪素与伐地那非的相互作用。ACE和东莨菪素在PCCSM中发挥了显著的、浓度依赖性的舒张作用。用ACE或东莨菪素灌注可显著增加环磷酸腺苷(cAMP)和环磷酸鸟苷(cGMP),且用ACE或东莨菪素灌注可增加eNOS mRNA和蛋白质的表达。此外,ACE或东莨菪素增强了伐地那非诱导的PCCSM舒张作用。ACE和东莨菪素主要通过激活一氧化氮-cGMP系统和cAMP途径使PCCSM舒张,对于对伐地那非不完全反应的勃起功能障碍患者,它们可能是联合治疗的候选药物。