Gardiner S M, Chhabra S R, Harty C, Williams P, Pritchard D I, Bycroft B W, Bennett T
School of Biomedical Sciences, Queen's Medical Centre, University of Nottingham NG7 2UH, UK.
Br J Pharmacol. 2001 Aug;133(7):1047-54. doi: 10.1038/sj.bjp.0704174.
N-acylhomoserine lactones (AHLs) are small, diffusible signalling molecules, employed by Gram-negative bacteria to coordinate gene expression with cell population density. Recent in vitro findings indicate that AHLs may function as virulence determinants per se, through modification of cytokine production by eukaryotic cells, and by stimulating the relaxation of blood vessels. In the present study, we assessed the influence of AHLs on cardiovascular function in conscious rats, and draw attention to the ability of the N-(3-oxododecanoyl)-L-homoserine lactone (3-oxo-C12-HSL), a signal molecule produced by P. aeruginosa, to cause marked bradycardia. This bradycardic effect was blocked by atropine and atenolol, and did not occur in vitro. Furthermore, modification of the acyl side chain length resulted in the loss of activity, whereas removal of the homoserine lactone ring, did not. The bradycardic effect of 3-oxo-C12-HSL was also observed in endotoxaemic animals, albeit attenuated. In normal rats, 3-oxo-C12-HSL caused initial mesenteric and hindquarters vasoconstriction, but only slight, and delayed signs of vasodilatation in the renal and mesenteric vascular beds. Furthermore, administration of 3-oxo-C12-HSL (pre-treatment or 2 h post-treatment) together with LPS, did not modify the established regional haemodynamic effects of the LPS, 6 h after the onset of its infusion. Our observations do not provide any clear evidence for an ability of 3-oxo-C12-HSL to modify the haemodynamic responses to LPS infusion. However, they are not inconsistent with the hypothesis that some of the cardiovascular sequelae of bacterial infection may be modulated by an influence of bacterial quorum sensing signalling molecules on the host.
N-酰基高丝氨酸内酯(AHLs)是一类小分子、可扩散的信号分子,革兰氏阴性菌利用其根据细胞群体密度来协调基因表达。最近的体外研究结果表明,AHLs本身可能作为毒力决定因素发挥作用,其机制包括改变真核细胞细胞因子的产生以及刺激血管舒张。在本研究中,我们评估了AHLs对清醒大鼠心血管功能的影响,并关注了铜绿假单胞菌产生的信号分子N-(3-氧代十二烷酰基)-L-高丝氨酸内酯(3-氧代-C12-HSL)导致显著心动过缓的能力。这种心动过缓效应可被阿托品和阿替洛尔阻断,且在体外未出现。此外,酰基侧链长度的改变导致活性丧失,而高丝氨酸内酯环的去除则不会。在感染内毒素的动物中也观察到了3-氧代-C12-HSL的心动过缓效应,尽管有所减弱。在正常大鼠中,3-氧代-C12-HSL最初引起肠系膜和后肢血管收缩,但程度较轻,且在肾和肠系膜血管床中出现血管舒张的迹象较延迟。此外,在脂多糖(LPS)输注开始6小时后,将3-氧代-C12-HSL(预处理或治疗后2小时)与LPS联合给药,并未改变LPS已确立的局部血流动力学效应。我们的观察结果并未提供任何明确证据表明3-氧代-C12-HSL能够改变对LPS输注的血流动力学反应。然而,这些观察结果与细菌群体感应信号分子对宿主的影响可能调节细菌感染的一些心血管后遗症这一假说并不矛盾。