Clinical Microbiology & Antimicrobial Research Laboratory, CSIR- Institute of Microbial Technology, Sector 39-A, Chandigarh, 160036, India.
Academy of Scientific & Innovative Research (AcSIR), Ghaziabad, Uttar Pradesh, 201002, India.
Commun Biol. 2024 Nov 12;7(1):1489. doi: 10.1038/s42003-024-06996-8.
The survival of modern medicine depends heavily on the effective prevention and treatment of bacterial infections, are threatened by antibacterial resistance. The increasing use of antibiotics and lack of stewardship have led to an increase in antibiotic-resistant pathogens, so the growing issue of resistance can be resolved by emphasizing chemically synthesized antibiotics. This study discovered SMJ-2, a synthetic indole derivative, is effective against all multidrug-resistant gram-positive bacteria. SMJ-2 has multiple targets of action, but the primary mechanism inhibits respiratory metabolism and membrane potential disruption. SMJ-2 was discovered to interfere with the mevalonate pathway, ultimately preventing the synthesis of farnesyl diphosphate, a precursor to the antioxidant staphyloxanthin, eventually releasing reactive oxygen species, and leading phagocytic cells to destroy pathogens. Additionally, no discernible biochemical and histopathological alterations were found in the mouse acute toxicity model. This study emphasizes mechanistic insights into SMJ-2 as a potential antibacterial with an unusual method of action.
现代医学的生存严重依赖于细菌感染的有效预防和治疗,但却受到抗菌药物耐药性的威胁。抗生素的过度使用和管理不善导致了抗生素耐药病原体的增加,因此,通过强调化学合成抗生素来解决日益严重的耐药问题。本研究发现,合成吲哚衍生物 SMJ-2 对所有多药耐药革兰氏阳性菌均有效。SMJ-2 具有多种作用靶点,但主要机制是抑制呼吸代谢和破坏膜电位。SMJ-2 被发现干扰甲羟戊酸途径,最终阻止法呢基二磷酸的合成,法呢基二磷酸是抗氧化剂金葡素的前体,最终释放活性氧,导致吞噬细胞破坏病原体。此外,在小鼠急性毒性模型中未发现明显的生化和组织病理学改变。本研究强调了 SMJ-2 作为一种具有非典型作用机制的潜在抗菌药物的机制见解。