Christian Omar E, Perry Dreyona A, Telchy Alaa I, Walton Preston N, Williams Daniel
Department of Chemistry and Biochemistry, North Carolina Central University, Durham, NC 27707, USA.
Department of Biological Sciences and Biomedical Sciences, North Carolina Central University, Durham, NC 27707, USA.
Antibiotics (Basel). 2024 Dec 19;13(12):1229. doi: 10.3390/antibiotics13121229.
BACKGROUND/OBJECTIVES: is the third most common sexually transmitted infection (STI), which may become untreatable soon if resistance continues to drastically increase. Due to increases in resistance to recommended antibiotics, alternative sources of novel compounds to combat this threat are being explored. Interestingly, marine sponges have proven to produce a plethora of bioactive compounds that display anticancer, antiviral, antifungal, and antibacterial activity.
In this study, the extracts of the sponge collected from Saint Thomas, US Virgin Islands were examined to determine their antibacterial activity against , , and .
The ethyl acetate sponge extracts significantly inhibited growth of , while none inhibited and . The bioassay-guided purification of the ethyl acetate extract resulted in the isolation of 6-desmethyl-6-ethylspongosoritin A (1) and plakortone B (2). To determine if the pure sponge metabolite could improve the efficacy of ceftriaxone against a high-level ceftriaxone (HTX)-resistant gonococcal strain, an antibiotic checkerboard assay was done by combining various concentrations of either precursor fractions or the purified compound 2 with ceftriaxone. Plakortone B (2) and ceftriaxone acted in synergy against gonococcal strains and inhibited growth by increasing membrane permeability when exposed for 4 h and 24 h.
This suggests that marine sponges may serve as a source for novel bioactive compounds against antibiotic-resistant strains of , as well as improve the efficacy of currently prescribed antibiotics.
背景/目的：淋病是第三常见的性传播感染（STI），如果耐药性继续急剧增加，它可能很快就会变得无法治疗。由于对推荐抗生素的耐药性增加，正在探索对抗这种威胁的新型化合物的替代来源。有趣的是，事实证明海洋海绵能产生大量具有抗癌、抗病毒、抗真菌和抗菌活性的生物活性化合物。
在本研究中，对从美属维尔京群岛圣托马斯收集的海绵提取物进行了检测，以确定它们对淋病奈瑟菌、金黄色葡萄球菌和大肠杆菌的抗菌活性。
乙酸乙酯海绵提取物显著抑制淋病奈瑟菌的生长，而对金黄色葡萄球菌和大肠杆菌均无抑制作用。对乙酸乙酯提取物进行生物测定指导的纯化，得到了6-去甲基-6-乙基海绵松素A（1）和软海绵素B（2）。为了确定纯海绵代谢物是否能提高头孢曲松对高水平头孢曲松（HTX）耐药淋病奈瑟菌菌株的疗效，通过将各种浓度的前体馏分或纯化化合物2与头孢曲松组合进行了抗生素棋盘试验。软海绵素B（2）和头孢曲松对淋病奈瑟菌菌株具有协同作用，在暴露4小时和24小时时通过增加膜通透性来抑制生长。
这表明海洋海绵可能是针对抗生素耐药淋病奈瑟菌菌株的新型生物活性化合物的来源，同时也能提高目前处方抗生素的疗效。
