三萜类化合物的有效性及其与抗生素对菌株的协同作用。
effectiveness of triterpenoids and their synergistic effect with antibiotics against strains.
作者信息
Hamza Muhammad, Nadir Maha, Mehmood Nadir, Farooq Adeel
机构信息
Department of Surgery, Rawalpindi Medical College, Rawalpindi, Pakistan.
Department of Science, National Institute of Science and Technical Education, Islamabad, Pakistan.
出版信息
Indian J Pharmacol. 2016 Nov-Dec;48(6):710-714. doi: 10.4103/0253-7613.194851.
OBJECTIVES
The aim of this study is to evaluate the effect of four triterpenoids such as oleanolic acid, ursolic acid, cycloastragenol, and beta-boswellic acid alone and in combination with antibiotics against strains.
MATERIALS AND METHODS
Sixteen clinical strains of from infected wounds were isolated. Eight were methicillin-sensitive (MSSA), and the other eight were methicillin-resistant (MRSA). The activity was also seen in reference American Type Culture Collection strains. The activity of all the triterpenoids and antibiotics against was evaluated by broth microdilution method. The effectiveness was judged by comparing the minimum inhibitory concentrations (MICs) of the compounds with antibiotics. The combination of antibiotics with compounds was evaluated by their fractional inhibitory concentrations (FIC).
RESULTS
Against both clinical and reference MSSA strains, none of the compounds exhibited comparable activity to antibiotics vancomycin or cefradine except for ursolic acid (MIC 7.8 μg/ml). Against MRSA, all compounds (MIC 16-128 μg/ml) showed lesser activity than vancomycin (MIC 5.8 μg/ml). Among triterpenoid-antibiotic combinations, the most effective were ursolic acid and vancomycin against clinical strain MSSA (FIC 0.17). However, overall, different combinations between triterpenoids and antibiotics showed 95%-46% ( < 0.05) reduction in MICs of antibiotics compared to when antibiotics were used alone. Cefradine, a drug not suitable for treating MRSA (MIC = 45 μg/ml), showed a remarkable decrease in its MIC (87% P< 0.01) when it was used in combination with oleanolic acid or ursolic acid in both clinical and reference strains.
CONCLUSION
The tested triterpenoids are relatively weaker than antibiotics. However, when used in combination with antibiotics, they showed remarkable synergistic effect and thus can help in prolonging the viability of these antibiotics against infections. Furthermore, reduction in MIC of cefradine with oleanolic acid indicates their potential use against MRSA.
目的
本研究旨在评估齐墩果酸、熊果酸、环黄芪醇和β-乳香酸这四种三萜类化合物单独使用以及与抗生素联合使用对菌株的作用效果。
材料与方法
从感染伤口分离出16株临床菌株。其中8株对甲氧西林敏感（MSSA），另外8株对甲氧西林耐药（MRSA）。在美国典型培养物保藏中心的参考菌株中也观察到了这种活性。通过肉汤微量稀释法评估所有三萜类化合物和抗生素对[具体菌株名称未给出]的活性。通过比较化合物与抗生素的最低抑菌浓度（MIC）来判断有效性。通过分数抑菌浓度（FIC）评估抗生素与化合物的组合。
结果
除熊果酸（MIC 7.8μg/ml）外，针对临床和参考MSSA菌株，没有一种化合物表现出与抗生素万古霉素或头孢拉定相当的活性。针对MRSA，所有化合物（MIC 16 - 128μg/ml）的活性均低于万古霉素（MIC 5.8μg/ml）。在三萜类化合物 - 抗生素组合中，最有效的是熊果酸与万古霉素针对临床菌株MSSA（FIC 0.17）。然而，总体而言，与单独使用抗生素相比，三萜类化合物与抗生素的不同组合使抗生素的MIC降低了95% - 46%（P < 0.05）。头孢拉定是一种不适合治疗MRSA的药物（MIC = 45μg/ml），当它与齐墩果酸或熊果酸在临床和参考菌株中联合使用时，其MIC显著降低（87%，P < 0.01）。
结论
所测试的三萜类化合物相对抗生素较弱。然而，当与抗生素联合使用时，它们表现出显著的协同作用，因此有助于延长这些抗生素对[具体感染名称未给出]感染的有效性。此外，齐墩果酸使头孢拉定的MIC降低表明它们在对抗MRSA方面的潜在用途。
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