E Silva Andressa K F, Dos Reis Antonielly C, Pinheiro Emanuelly E A, de Sousa Jonas N, de Alcântara Oliveira Felipe A, Moura Arkellau K S, de Sousa L Neto José, das Graças L Citó Antonia M, Siqueira-Júnior José P, Kaatz Glenn W, Barreto Humberto M
Postgraduate Program in Pharmaceutical Sciences, Federal University of Piaui, Teresina PI, Brazil.
Laboratory of Organic Geochemistry, Federal University of Piaui, Teresina, PI, Brazil.
Curr Drug Metab. 2021;22(2):114-122. doi: 10.2174/1389200221666200523155617.
Microbial resistance to antibiotics is a global public health problem, which requires urgent attention. Platonia insignis is a native species from the eastern Brazilian Amazon, used in the treatment of burns and wounds.
To evaluate the antimicrobial activity of the hydroalcoholic extract of P. insignis (PIHA), the ethyl acetate fraction (PIAE), and its subfraction containing a mixture of biflavonoids (BF). Moreover, the effect of these natural products on the antibiotic activity against S. aureus strains overexpressing efflux pump genes was also evaluated.
Minimal inhibitory concentrations were determined against different species of microorganisms. To evaluate the modulatory effect on the Norfloxacin-resistance, the MIC of this antibiotic was determined in the absence and presence of the natural products at subinhibitory concentrations. Inhibition of the EtBr efflux assays were conducted in the absence or presence of natural products.
PIHA showed a microbicidal effect against S. aureus and C. albicans, while PIAE was bacteriostatic for S. aureus. PIAE and BF at subinhibitory concentrations were able to reduce the MIC of Norfloxacin acting as modulating agents. BF was able to inhibit the efflux of EtBr efflux in S. aureus strains overexpressing specific efflux pump genes.
P. inignisis, a source of efflux pump inhibitors, including volkensiflavone and morelloflavone, which were able to potentiate the Norfloxacin activity by NorA inhibition, being also able to inhibit QacA/B, TetK and MsrA. Volkensiflavone and morelloflavone could be used as an adjuvant in the antibiotic therapy of multidrug resistant S. aureus strains overexpressing efflux pumps.
微生物对抗生素的耐药性是一个全球性的公共卫生问题，需要紧急关注。巴西番荔枝是一种原产于巴西东部亚马逊地区的物种，用于治疗烧伤和伤口。
评估巴西番荔枝水醇提取物（PIHA）、乙酸乙酯馏分（PIAE）及其含有双黄酮混合物的亚馏分（BF）的抗菌活性。此外，还评估了这些天然产物对过表达外排泵基因的金黄色葡萄球菌菌株抗生素活性的影响。
测定对不同微生物物种的最低抑菌浓度。为了评估对诺氟沙星耐药性的调节作用，在不存在和存在亚抑菌浓度的天然产物的情况下测定该抗生素的最低抑菌浓度。在不存在或存在天然产物的情况下进行溴化乙锭外排抑制试验。
PIHA对金黄色葡萄球菌和白色念珠菌有杀菌作用，而PIAE对金黄色葡萄球菌有抑菌作用。亚抑菌浓度的PIAE和BF能够降低诺氟沙星作为调节剂的最低抑菌浓度。BF能够抑制过表达特定外排泵基因的金黄色葡萄球菌菌株中溴化乙锭的外排。
巴西番荔枝是外排泵抑制剂的来源，包括 Volkensiflavone 和莫雷洛黄酮，它们能够通过抑制 NorA 增强诺氟沙星的活性，还能够抑制 QacA/B、TetK 和 MsrA。Volkensiflavone 和莫雷洛黄酮可作为过表达外排泵的多重耐药金黄色葡萄球菌菌株抗生素治疗的佐剂。
