Wang Jie, Yao Qi-Feng, Amin Muhammad, Nong Xu-Hua, Zhang Xiao-Yong, Qi Shu-Hua
Key Laboratory of Tropical Marine Bio-resources and Ecology, Guangdong Key Laboratory of Marine Material Medical, RNAM Center for Marine Microbiology, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou, China.
South China Sea Bio-Resource Exploitation and Utilization Collaborative Innovation Center, Guangzhou, China.
J Antibiot (Tokyo). 2017 Jun;70(6):763-770. doi: 10.1038/ja.2017.45. Epub 2017 Apr 5.
Penicillenols (A1, A2, B1, B2, C1 and C2) were isolated from Aspergillus restrictus DFFSCS006, and could differentially inhibit biofilm formation and eradicate pre-developed biofilms of Candida albicans. Their structure-bioactivity relationships suggested that the saturation of hydrocarbon chain at C-8, R-configuration of C-5 and trans-configuration of the double bond between C-5 and C-6 of pyrrolidine-2,4-dione unit were important for their anti-biofilm activities. Penicillenols A2 and B1 slowed the hyphal growth and suppressed the transcripts of hypha specific genes HWP1, ALS1, ALS3, ECE1 and SAP4. Moreover, penicillenols A2 and B1 were found to act synergistically with amphotericin B against C. albicans biofilm formation.
从局限曲霉DFFSCS006中分离出了青霉烯醇(A1、A2、B1、B2、C1和C2),它们能够差异性地抑制白色念珠菌生物膜的形成,并根除预先形成的生物膜。它们的构效关系表明,吡咯烷-2,4-二酮单元C-8位烃链的饱和、C-5位的R构型以及C-5和C-6之间双键的反式构型对其抗生物膜活性很重要。青霉烯醇A2和B1减缓了菌丝生长,并抑制了菌丝特异性基因HWP1、ALS1、ALS3、ECE1和SAP4的转录本。此外,发现青霉烯醇A2和B1与两性霉素B对白色念珠菌生物膜形成具有协同作用。