Ma Chaoyu, Du Faya, Yan Lan, He Gonghao, He Jianchang, Wang Chengying, Rao Gaoxiong, Jiang Yuanying, Xu Guili
Department of Pharmacy, Kunming General Hospital of Chengdu Military Region, 212 Da-Guan Road, Kunming 650032, China.
School of Pharmacy, Kunming Medical University, 1168 Yu-Hua Road, Kunming 650500, China.
Molecules. 2015 Sep 29;20(10):17913-28. doi: 10.3390/molecules201017913.
Roemerine (RM) is an aporphine alkaloid isolated from the fresh rattan stem of Fibraurea recisa, and it has been demonstrated to have certain antifungal activity. This study aimed to investigate the antifungal activity of RM and the underlying mechanisms in Candida albicans (C. albicans). The in vitro antifungal activity of RM was evaluated by a series of experiments, including the XTT reduction assay, confocal laser scanning microscopy assay, scanning electron microscope assay. Results showed that 1 μg/mL RM inhibited biofilm formation significantly (p < 0.01) both in Spider medium and Lee's medium. In addition, RM could inhibit yeast-to-hyphae transition of C. albicans in a dose-dependent manner. The biofilm-specific and hypha-specific genes such as YWP1, SAP5, SAP6, HWP1, ECE1 were up-regulated and EFG1 was down-regulated after 8 μg/mL RM treatment. Furthermore, the toxicity of RM was investigated using C. elegans worms, three cancer cells and one normal cell. The date showed that RM had no significant toxicity. In conclusion, RM could inhibited the formation of C. albicans biofilm in vitro, but it had no fungicidal effect on planktonic C. albicans cells, and the anti-biofilm mechanism may be related to the cAMP pathway.
罗默碱(RM)是从黄藤新鲜藤茎中分离得到的一种阿朴啡生物碱,已被证明具有一定的抗真菌活性。本研究旨在探讨RM对白色念珠菌的抗真菌活性及其潜在机制。通过一系列实验评估了RM的体外抗真菌活性,包括XTT还原试验、共聚焦激光扫描显微镜试验、扫描电子显微镜试验。结果表明,1μg/mL的RM在蜘蛛培养基和李氏培养基中均能显著抑制生物膜形成(p<0.01)。此外,RM能以剂量依赖的方式抑制白色念珠菌的酵母-菌丝转变。用8μg/mL的RM处理后,生物膜特异性基因和菌丝特异性基因如YWP1、SAP5、SAP6、HWP1、ECE1上调,而EFG1下调。此外,还使用秀丽隐杆线虫、三种癌细胞和一种正常细胞研究了RM的毒性。数据表明RM没有明显毒性。总之,RM能在体外抑制白色念珠菌生物膜的形成,但对浮游的白色念珠菌细胞没有杀菌作用,其抗生物膜机制可能与cAMP途径有关。