School of Pharmacy, Naval Military Medical University, Shanghai 200433, China.
School of Pharmacy, Naval Military Medical University, Shanghai 200433, China; Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350000, China.
Chin J Nat Med. 2019 Aug;17(8):616-623. doi: 10.1016/S1875-5364(19)30064-0.
Loureirin A is a major active component of Draconis sanguis, a traditional Chinese medicine. This work aimed to investigate the activity of loureirin A against Candida albicans biofilms. 2, 3-Bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT)reduction assay and scanning electron microscopy were used to investigate the anti-biofilm effect. Minimal inhibitory concentration testing and time-kill curve assay were used to evaluate fungicidal activity. Cell surface hydrophobicity (CSH) assay and hyphal formation experiment were respectively carried out to investigate adhesion and morphological transition, two virulence traits of C. albicans. Real-time RT-PCR was used to investigate gene expression. Galleria mellonella-C. albicans and Caenorhabditis elegans-C. albicans infection models were used to evaluate the in-vivo antifungal effect. Human umbilical vein endothelial cells and C. elegans nematodes were used to evaluate the toxicity ofloureirin A. Our data indicated that loureirin A had a significant effect on inhibiting C. albicans biofilms, decreasing CSH, and suppressing hyphal formation. Consistently, loureirin A down-regulated the expression of some adhesion-related genes and hypha/biofilm-related genes. Moreover, loureirin A prolonged the survival of Galleria mellonella and Caenorhabditis elegans in C. albicans infection models and exhibited low toxicity. Collectively, loureirin A inhibits fungal biofilms, and this effect may be associated with the suppression of pathogenic traits, adhesion and hyphal formation.
龙牙草 A 是一种传统中药龙血竭的主要活性成分。本研究旨在探讨龙牙草 A 对白色念珠菌生物膜的作用。采用 2,3-双-(2-甲氧基-4-硝基-5-磺苯基)-2H-四唑-5-羧基苯胺(XTT)还原试验和扫描电子显微镜观察来研究抗生物膜作用。最小抑菌浓度试验和时间杀伤曲线试验用于评估杀菌活性。细胞表面疏水性(CSH)试验和菌丝形成实验分别用于研究黏附作用和白色念珠菌的形态转化，这是其两种毒力特征。实时 RT-PCR 用于研究基因表达。利用大蜡螟-白色念珠菌和秀丽隐杆线虫-白色念珠菌感染模型评估体内抗真菌作用。用人脐静脉内皮细胞和秀丽隐杆线虫线虫评估龙牙草 A 的毒性。研究数据表明，龙牙草 A 对抑制白色念珠菌生物膜、降低 CSH 和抑制菌丝形成有显著作用。一致地，龙牙草 A 下调了一些黏附相关基因和菌丝/生物膜相关基因的表达。此外，龙牙草 A 延长了大蜡螟和秀丽隐杆线虫在白色念珠菌感染模型中的存活时间，表现出低毒性。总之，龙牙草 A 可抑制真菌生物膜，这种作用可能与抑制致病特性、黏附和菌丝形成有关。
