title: The Structure-Activity Relationship of Pterostilbene Against Candida albicans Biofilms.
abstract: Candida albicansbiofilms contribute to invasive infections and dramatic drug resistance, and anti-biofilm agents are urgently needed in the clinic. Pterostilbene (PTE) is a natural plant product with potentials to be developed as an anti-biofilm agent. In this study, we evaluated the structure-activity relationship (SAR) of PTE analogues againstC. albicansbiofilms. XTT (Sodium 2,3-bis(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide inner salt) reduction assay was used to evaluate the activity of the analogues againstC. albicansbiofilms. Knowing that hyphal formation is essential forC. albicansbiofilms, anti-hyphal assay was further carried out. By comparing a series of compounds tested in this study, we found that compounds withpara-hydroxy (-OH) in partition A exhibited better activity than those with other substituents in theparaposition, and the double bond in partition B andmeta-dimethoxy (-OCH₃) in partition C both contributed to the best activity. Consistent results were obtained by anti-hyphal assay. Collectively,para-hydroxy (-OH), double bond andmeta-dimethoxy (-OCH₃) are all needed for the best activity of PTE againstC. albicansbiofilms.
authors.affiliation: New Drug Research and Development Center, School of Pharmacy, Second Military Medical University, Shanghai 200433, China. dandanhu1989@163.com.
authors.forename: Dan-Dan
authors.initials: DD
authors.lastname: Hu
authors.affiliation: New Drug Research and Development Center, School of Pharmacy, Second Military Medical University, Shanghai 200433, China. zhangrili116@163.com.
authors.forename: Ri-Li
authors.initials: RL
authors.lastname: Zhang
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. zou_jinan@163.com.
authors.forename: Yong
authors.initials: Y
authors.lastname: Zou
authors.affiliation: New Drug Research and Development Center, School of Pharmacy, Second Military Medical University, Shanghai 200433, China. zhonghuasmmu@hotmail.com.
authors.forename: Hua
authors.initials: H
authors.lastname: Zhong
authors.affiliation: School of Chemistry and Chemical Engineering, Yan'an University, Yan'an 716000, China. sdzes2006@163.com.|ZhongshanWanYuan New Drug R & D Co., Ltd., Zhongshan 528451, China. sdzes2006@163.com.
authors.forename: En-Sheng
authors.initials: ES
authors.lastname: Zhang
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China. rosen_luo@163.com.|ZhongshanWanYuan New Drug R & D Co., Ltd., Zhongshan 528451, China. rosen_luo@163.com.
authors.forename: Xiang
authors.initials: X
authors.lastname: Luo
authors.affiliation: New Drug Research and Development Center, School of Pharmacy, Second Military Medical University, Shanghai 200433, China. wangyansmmu@126.com.
authors.forename: Yan
authors.initials: Y
authors.lastname: Wang
authors.affiliation: New Drug Research and Development Center, School of Pharmacy, Second Military Medical University, Shanghai 200433, China. jiangyuanying@126.com.
authors.forename: Yuan-Ying
authors.initials: YY
authors.lastname: Jiang
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D018441:Biofilms / Q000187:drug effects*; D002176:Candida albicans / Q000187:drug effects / Q000502:physiology*; D025301:Hyphae / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013267:Stilbenes / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D013267:Stilbenes; C107773:pterostilbene
keywords: Candida albicans; anti-biofilm; pterostilbene; structure-activity relationship