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Molecules 2017, 22(3), 360;

The Structure-Activity Relationship of Pterostilbene Against Candida albicans Biofilms

New Drug Research and Development Center, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China
School of Chemistry and Chemical Engineering, Yan’an University, Yan’an 716000, China
ZhongshanWanYuan New Drug R & D Co., Ltd., Zhongshan 528451, China
Authors to whom correspondence should be addressed.
Academic Editor: Jean-Marc Sabatier
Received: 5 November 2016 / Revised: 12 February 2017 / Accepted: 22 February 2017 / Published: 27 February 2017
(This article belongs to the Special Issue Structure-Activity Relationship of Natural Products)
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Candida albicans biofilms 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 against C. albicans biofilms. 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 against C. albicans biofilms. Knowing that hyphal formation is essential for C. albicans biofilms, anti-hyphal assay was further carried out. By comparing a series of compounds tested in this study, we found that compounds with para-hydroxy (–OH) in partition A exhibited better activity than those with other substituents in the para position, and the double bond in partition B and meta-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 and meta-dimethoxy (–OCH3) are all needed for the best activity of PTE against C. albicans biofilms. View Full-Text
Keywords: Candida albicans; pterostilbene; anti-biofilm; structure-activity relationship Candida albicans; pterostilbene; anti-biofilm; structure-activity relationship

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Hu, D.-D.; Zhang, R.-L.; Zou, Y.; Zhong, H.; Zhang, E.-S.; Luo, X.; Wang, Y.; Jiang, Y.-Y. The Structure-Activity Relationship of Pterostilbene Against Candida albicans Biofilms. Molecules 2017, 22, 360.

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