Erianin against Staphylococcus aureus Infection via Inhibiting Sortase A

With continuous emergence and widespread of multidrug-resistant Staphylococcus aureus infections, common antibiotics have become ineffective in treating these infections in the clinical setting. Anti-virulence strategies could be novel, effective therapeutic strategies against drug-resistant bacterial infections. Sortase A (srtA), a transpeptidase in gram-positive bacteria, can anchor surface proteins that play a vital role in pathogenesis of these bacteria. SrtA is known as a potential antivirulent drug target to treat bacterial infections. In this study, we found that erianin, a natural bibenzyl compound, could inhibit the activity of srtA in vitro (half maximal inhibitory concentration—IC₅₀ = 20.91 ± 2.31 μg/mL, 65.7 ± 7.2 μM) at subminimum inhibitory concentrations (minimum inhibitory concentrations—MIC = 512 μg/mL against S. aureus). The molecular mechanism underlying the inhibition of srtA by erianin was identified using molecular dynamics simulation: erianin binds to srtA residues Ile182, Val193, Trp194, Arg197, and Ile199, forming a stable bond via hydrophobic interactions. In addition, the activities of S. aureus binding to fibronectin and biofilm formation were inhibited by erianin, when co-culture with S. aureus. In vivo, erianin could improve the survival in mice that infected with S. aureus by tail vein injection. Experimental results showed that erianin is a potential novel therapeutic compound against S. aureus infections via affecting srtA. View Full-Text

Keywords: sortase A; Staphylococcus aureus; erianin; inhibitor; molecular mechanism

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Ouyang, P.; He, X.; Yuan, Z.-W.; Yin, Z.-Q.; Fu, H.; Lin, J.; He, C.; Liang, X.; Lv, C.; Shu, G.; Yuan, Z.-X.; Song, X.; Li, L.; Yin, L. Erianin against Staphylococcus aureus Infection via Inhibiting Sortase A. Toxins 2018, 10, 385. https://doi.org/10.3390/toxins10100385

AMA Style

Ouyang P, He X, Yuan Z-W, Yin Z-Q, Fu H, Lin J, He C, Liang X, Lv C, Shu G, Yuan Z-X, Song X, Li L, Yin L. Erianin against Staphylococcus aureus Infection via Inhibiting Sortase A. Toxins. 2018; 10(10):385. https://doi.org/10.3390/toxins10100385

Chicago/Turabian Style

Ouyang, Ping, Xuewen He, Zhong-Wei Yuan, Zhong-Qiong Yin, Hualin Fu, Juchun Lin, Changliang He, Xiaoxia Liang, Cheng Lv, Gang Shu, Zhi-Xiang Yuan, Xu Song, Lixia Li, and Lizi Yin. 2018. "Erianin against Staphylococcus aureus Infection via Inhibiting Sortase A" Toxins 10, no. 10: 385. https://doi.org/10.3390/toxins10100385

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Erianin against Staphylococcus aureus Infection via Inhibiting Sortase A

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