Multi-resistant Staphylococcus aureus ( S. aureus ) infection is a significant global health concern owing to its high mortality and morbidity rates. Coagulase (Coa), a key enzyme that activates prothrombin to initiate host coagulation, has emerged as a promising target for anti-infective therapeutic approaches. This study identified sinigrin as a potent Coa inhibitor that significantly inhibited S. aureus -induced coagulation at concentration as low as 32 mg/L. Additionally, at a higher concentration of 128 mg/L, sinigrin disrupted the self-protection mechanism of S. aureus . Thermal shift and fluorescence-quenching assays confirmed the direct binding of sinigrin to the Coa protein. Molecular docking analysis predicted specific binding sites for sinigrin in the Coa molecule, and point mutation experiments highlighted the importance of Arg-187 and Asp-222 as critical binding sites for both Coa and sinigrin. In vivo studies demonstrated that the combination of sinigrin with oxacillin exhibited greater antibacterial efficacy than oxacillin alone in the treatment of S. aureus -induced pneumonia in mice. Furthermore, sinigrin was shown to reduce bacterial counts and inflammatory cytokine levels in the lung tissues of S. aureus -infected mice. In summary, sinigrin was shown to directly target Coa, resulting in the attenuation of S. aureus virulence, which suggests the potential of sinigrin as an adjuvant for future antimicrobial therapies.
Ru Zhao,Xinyu Yang,Aoqi Zhang,Tieyang Zhou,Yunwei Zhou,Lei Yang
Microwave-mediated immiscible binary solvent extraction (MIBSE) was applied to simultaneously extract oil and epigoitrin from Orychophragmus violaceus seeds . The upper phase of n -hexane was used to obtain oil, and the lower phase of ethanol solution was used to obtain epigoitrin. Factors potentially affecting the yields of oil and epigoitrin were systematically investigated. The optimum conditions were an ethanol volume fraction of 65%, liquid–solid ratio of lower-phase of 20 mL/g, liquid–solid ratio of upper-phase of 12 mL/g, microwave irradiation power of 393 W, and microwave irradiation time of 29 min. The actual yields of oil and epigoitrin were 34.08% ± 1.38% and 11.86 ± 0.47 mg/g, respectively. GC–MS analysis illustrated that the seed oils obtained by MIBSE and Soxhlet extraction exhibited similar fatty acid compositions. The separated epigoitrin was determined by HPLC analyses, which obtained a purity of 91.25% ± 3.83%, follwed by NMR determinations.
In the present study, microwave-assisted biphasic extraction (MABE) was first and successfully applied to the simultaneous extraction of oil and sinigrin from field pennycress ( Thlaspi arvense ) through a one-pot process. Four potentially influencing factors on the yields of oil and sinigrin, including the ratio of lower phase to solid, ratio of upper phase to solid, microwave irradiation power, and microwave irradiation time, were selected for further optimization by Box–Behnken design, and the optimal extraction conditions were obtained as follows: ratio of lower phase to solid of 21 mL/g, ratio of upper phase to solid of 12 mL/g, microwave irradiation power of 389 W, and microwave irradiation time of 33 min. Under the optimal extraction conditions, the yields of oil (23.46 % ± 0.78 %) and sinigrin (18.42 ± 0.35 mg/g) from T. arvense seeds were maximized. The GC–MS analysis illustrated that the T. arvense seed oil obtained by MABE using n -hexane and water biphasic solvents and Soxhlet extraction using n -hexane solvent exhibited a similar fatty acid composition. The seed oil acquired by the efficient MABE demonstrated a higher quality due to its lower acid value and higher iodine value. Scanning electron microscopy results showed that the cell structure of seed tissues was obviously disrupted compared with untreated raw material and that treated by the conventional extraction method. In general, the results indicated that the proposed MABE is an efficient method for the extraction of oil and sinigrin from T. arvense seeds.
危险品化学品经营许可证（带存储）