Tripathi Nancy, Roy Arnab, Agnivesh Puja Kumari, Bhardwaj Nivedita, Kumari Sanju, Kalia Nitin Pal, Jain Shreyans K
Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (BHU), Varanasi, Uttar Pradesh, India.
Department of Biological Sciences, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India.
Chem Biodivers. 2025 Apr;22(4):e202401272. doi: 10.1002/cbdv.202401272. Epub 2024 Dec 5.
The surge in multidrug resistance in Staphylococcus aureus is the pressing need to identify novel alternatives to combat antimicrobial resistance effectively. Bakuchiol is a bioactive prenylated phenolic meroterpene largely abundant in the seeds of Psoralea corylifolia. In this study, we present the biological assessment of bakuchiol derived from P. corylifolia as an antimicrobial agent. S. aureus, a significant opportunistic pathogen, attracts global concern for its biofilm formation and resilience against numerous antibiotics, escaping antibiotic pressure. The primary screening of bakuchiol as an antimicrobial agent against S. aureus delineated its potential as a strong bactericidal agent with a minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of 2 and 8 µg/mL, respectively. Importantly, bakuchiol also exhibited low toxicity against HepG2 cells, showing a favorable selectivity index (SI) of 14.4. Furthermore, bakuchiol demonstrated comparable activity (MIC = 2 µg/mL) against a laboratory-generated ciprofloxacin-resistant mutant of S. aureus. Bakuchiol could significantly inhibit the biofilm formation of S. aureus in a dose-dependent manner with minimum biofilm inhibitory concentration (MBIC) of 0.956 µg/mL. Bakuchiol effectively inhibited DNA gyrase supercoiling activity at a concentration eight times the MIC, establishing DNA gyrase inhibition as the mechanism of action for bakuchiol. Our findings suggest bakuchiol as a potential therapeutic agent for S. aureus-mediated nosocomial infections.
金黄色葡萄球菌多重耐药性的激增迫切需要找到新的替代方法来有效对抗抗菌药物耐药性。补骨脂酚是一种具有生物活性的异戊烯基化酚类半萜,大量存在于补骨脂的种子中。在本研究中,我们对从补骨脂中提取的补骨脂酚作为抗菌剂进行了生物学评估。金黄色葡萄球菌是一种重要的机会致病菌,因其生物膜形成以及对多种抗生素的耐药性而引起全球关注,逃避了抗生素压力。补骨脂酚作为抗金黄色葡萄球菌抗菌剂的初步筛选表明其具有作为强效杀菌剂的潜力,其最低抑菌浓度(MIC)和最低杀菌浓度(MBC)分别为2和8μg/mL。重要的是,补骨脂酚对HepG2细胞也表现出低毒性,显示出良好的选择性指数(SI)为14.4。此外,补骨脂酚对实验室产生的耐环丙沙星金黄色葡萄球菌突变体表现出相当的活性(MIC = 2μg/mL)。补骨脂酚能以剂量依赖的方式显著抑制金黄色葡萄球菌的生物膜形成,最低生物膜抑制浓度(MBIC)为0.956μg/mL。补骨脂酚在浓度为MIC的8倍时有效抑制DNA回旋酶超螺旋活性,确定DNA回旋酶抑制为补骨脂酚的作用机制。我们的研究结果表明补骨脂酚是治疗金黄色葡萄球菌介导的医院感染的潜在治疗剂。