Xu Y F, Lian D W, Chen Y Q, Cai Y F, Zheng Y F, Fan P L, Ren W K, Fu L J, Li Y C, Xie J H, Cao H Y, Tan B, Su Z R, Huang P
School of Chinese Materia Medica, Guangzhou University of Chinese Medicine, Guangzhou, People's Republic of China.
Department of Mammary Disease, The Second Affiliated Hospital, Guangzhou University of Chinese Medicine, Guangzhou, People's Republic of China.
Antimicrob Agents Chemother. 2017 May 24;61(6). doi: 10.1128/AAC.00122-17. Print 2017 Jun.
This study further evaluated the and anti- activities and potential underlying mechanism of patchouli alcohol (PA), a tricyclic sesquiterpene. In the assay, the capacities of PA to inhibit and kill were tested on three standard strains at different pH values and on 12 clinical isolates. The effects of PA on adhesion (and its , , and genes), motility (and its and genes), ultrastructure, and flagellation were investigated. Moreover, the resistance to and postantibiotic effect (PAE) of PA were determined. Furthermore, the effects of PA on eradication and gastritis were examined. Results showed that MICs of PA against three standard strains (pH 5.3 to 9) and 12 clinical isolates were 25 to 75 and 12.5 to 50 μg/ml, respectively. The killing kinetics of PA were time and concentration dependent, and its minimal bactericidal concentrations (MBCs) were 25 to 75 μg/ml. In addition, adhesion, motility, ultrastructure, and flagellation were significantly suppressed. PA also remarkably inhibited the expression of adhesion genes ( and ) and motility genes ( and ). Furthermore, PA treatment caused a longer PAE and less bacterial resistance than clarithromycin and metronidazole. The study showed that PA can effectively eradicate , inhibit gastritis, and suppress the expression of inflammatory mediators (COX-2, interleukin 1β, tumor necrosis factor alpha, and inducible nitric oxide synthase [iNOS]). In conclusion, PA can efficiently kill , interfere with its infection process, and attenuate gastritis with less bacterial resistance, making it a potential candidate for new drug development.
本研究进一步评估了三环倍半萜广藿香醇（PA）的抗菌活性及潜在作用机制。在体外试验中，测试了PA在不同pH值下对三种标准菌株及12株临床分离株的抑制和杀灭能力。研究了PA对幽门螺杆菌黏附（及其相关的cagA、vacA和iceA基因）、运动性（及其相关的flaA和flaB基因）、超微结构和鞭毛形成的影响。此外，还测定了PA对幽门螺杆菌的耐药性及抗生素后效应（PAE）。此外，还研究了PA对幽门螺杆菌根除及胃炎的影响。结果显示，PA对三种标准菌株（pH值5.3至9）和12株临床分离株的最低抑菌浓度（MIC）分别为25至75μg/ml和12.5至50μg/ml。PA的杀菌动力学具有时间和浓度依赖性，其最低杀菌浓度（MBC）为25至75μg/ml。此外，幽门螺杆菌的黏附、运动性、超微结构和鞭毛形成均受到显著抑制。PA还显著抑制了黏附基因（cagA和vacA）和运动性基因（flaA和flaB）的表达。此外，与克拉霉素和甲硝唑相比，PA治疗导致的PAE更长，细菌耐药性更低。动物研究表明，PA可有效根除幽门螺杆菌、抑制胃炎并抑制炎症介质（COX-2、白细胞介素1β、肿瘤坏死因子α和诱导型一氧化氮合酶[iNOS]）的表达。总之，PA可有效杀灭幽门螺杆菌，干扰其感染过程，并减轻胃炎，且细菌耐药性较低，使其成为新药开发的潜在候选药物。
