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Molecules 2017, 22(3), 360; doi:10.3390/molecules22030360

The Structure-Activity Relationship of Pterostilbene Against Candida albicans Biofilms

1
New Drug Research and Development Center, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
2
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China
3
School of Chemistry and Chemical Engineering, Yan’an University, Yan’an 716000, China
4
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)
View Full-Text   |   Download PDF [23815 KB, uploaded 27 February 2017]   |  

Abstract

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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

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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