Synthesis of peptidomimetics as antibiotic adjuvants for combination with aztreonam to combat MDR Pseudomonas aeruginosa

Ma, Xican; Guo, Wei; Zhu, Xi; Li, Zhiwen; Li, Yinghong; Guo, Zhihao; Wang, Yanxiang; Pang, Jing; Yuan, Min; Li, Zhenjun; You, Xuefu; Lu, Xi; Liu, Yishuang; Song, Danqing

doi:10.1016/j.ejmech.2023.115778

Cited by 1 publication

(1 citation statement)

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“…Based on the excellent antibacterial activity and high yield of compound 4 , it was further evaluated in vivo in the VRE- G. mellonella infection model with the anti-VRE antibiotic Q/D as the positive control, as described previously. , As shown in Figure , the treatment with 4 significantly increased the survival rate in a dose-dependent manner from 0.2 mg/kg to 10 mg/kg. Compared with Q/D, 4 exhibited stronger activity with a survival rate of 100% at 10 mg/kg, indicating that this cis -decalin-bearing molecule could be a candidate for future antibiotic drug development.…”

Section: Resultsmentioning

confidence: 99%

Bioactivity-Based Molecular Networking-Guided Isolation of Epicolidines A–C from the Endophytic Fungus Epicoccum sp. 1-042

Chang,

Li,

Huang

et al. 2024

J. Nat. Prod.

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Bioactivity-based molecular networking-guided fractionation enabled the isolation of three new polycyclic tetramic acids bearing cis-decalin, epicolidines A−C (1−3), along with one known compound, PF 1052 (4), from the endophytic fungus Epicoccum sp. 1-042 collected in Tibet, China. Their structures were assigned on the basis of extensive spectroscopic data, partial hydrolysis, advanced Marfey's method, quantum chemistry calculations, and X-ray diffraction analysis. Compounds 2−4 displayed promising activities against Gram-positive bacteria in vitro. Particularly, compound 4 displayed remarkable potential against vancomycin-resistant Enterococcus faecium (VRE) with an MIC value of 0.25 μg/mL, lower than the MIC (0.5 μg/mL) of the antibiotic combination quinupristin/dalfopristin (Q/D). In a further in vivo study, compound 4 increased the survival rate to 100% in the VRE-G. mellonella infection model at a concentration of 10 mg/kg.

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Section: Resultsmentioning

confidence: 99%