氟喹诺酮类药物对外周血淋巴细胞谷胱甘肽系统活性的影响

I. Kovalenko, O. K. Onufrovych, O. Melnyk, O. Korchynska, Z. Vorobets, N. Vorobets
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引用次数: 2

摘要

氟喹诺酮类药物对致病性菌群具有抑制作用,在化脓性炎症并发症的致病因治疗中起着重要作用。由于其抗菌活性范围广、毒性低、药代动力学特性好,被广泛用于治疗不同部位的细菌感染。这些药物具有超宽范围的活性,对革兰氏阳性和革兰氏阴性,好氧和厌氧微生物,衣原体,支原体,分枝杆菌有活性[1-4]。氟喹诺酮类药物是通过在分子中引入一个、两个或四个氟原子的4-喹诺酮类药物合成的[1,2]。这些合成抗生素具有特定的作用机制,即抑制细菌细胞的DNA旋切酶(拓扑异构酶II)和拓扑异构酶IV的活性,这种酶负责细菌DNA结构的稳定性,并参与细胞分裂[2,3,5]。在氟喹诺酮类药物的作用下,细菌细胞的DNA被分解,其空间结构被破坏,从而导致复制、转录、翻译和细胞死亡过程受损。氟喹诺酮类药物的药效学包括抗菌(杀菌)、抗生素后和免疫调节作用[7,8]。第二代药物(如环丙沙星)对多种革兰氏阴性需氧微生物以及金黄色葡萄球菌、沙门氏菌、大肠杆菌均有活性[6]。对结核分枝杆菌也有活性。对肺炎球菌、肠球菌、衣原体的态度一般活跃。其生物利用度为80%。第三代氟喹诺酮类药物对肺炎球菌和细胞内病原体,特别是支原体和衣原体具有高度活性[6]。因此。与其他氟喹诺酮类药物相比,左氧氟沙星对肺炎球菌、衣原体、支原体具有优势。更常见的是用于治疗呼吸道感染,以及泌尿生殖道和皮肤感染。新型IV代氟喹诺酮类药物,特别是莫西沙星,与前几代氟喹诺酮类药物相比,对革兰氏阳性微生物具有明显更高的活性[6]。莫西沙星对葡萄球菌、链球菌最有效。就肺炎球菌而言,它的活性是环丙沙星的4-16倍。莫西沙星对衣原体、支原体、脲原体等多耐药菌株起作用,特别是对结核分枝杆菌,生物利用度为90%。可以假设氟喹诺酮类抗生素进入人体后也会对真核细胞,特别是血细胞产生影响。它
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Effect of Fluoroquinolones on the Activity of the Glutathione System in the Peripheral Blood Lymphocytes
An important role in the etiotropic therapy of purulent-inflammatory complications take fluoroquinolones which are active against pathogenic microflora. Due to their wide range of antimicrobial activity, low toxicity, good pharmacokinetics properties, they are widely use in the treatment of bacterial infections of different localization. These are drugs of ultra-wide range of activity, active against gram-positive and gram-negative, aerobic and anaerobic microorganisms, chlamydia, mycoplasma, mycobacteria [1-4]. Fluoroquinolones are synthesized by introducing into the molecule 4-quinolones – one, two or four fluorine atoms [1,2]. These synthetic antibiotics have a specific mechanism of action, which is to inhibit the activity of DNA gyrase (topoisomerase II) and topoisomerase IV of bacterial cells – the enzyme responsible for the stability of the DNA structure of the bacteria and is involved in cell division [2,3,5]. Under the action of fluoroquinolones, the bacterial cell's DNA is despiralized, its spatial structure is disrupted and, as a consequence, the process of replication, transcription, translation, and cell death is impaired. The pharmacodynamics of fluoroquinolones include antibacterial (bacteriocidal), postantibiotic and immunomodulatory effects [7,8]. Drugs 2nd generations (for example, ciprofloxacin) are active in a wide range of gram-negative aerobic microorganisms as well as Staphylococcus aureus, salmonella, Escherichia coli [6]. Also active against mycobacterium tuberculosis. Moderately active in attitude to pneumococci, enterococci, chlamydia. Its bioavailability is 80%. Third-generation fluoroquinolones are highly active against pneumococci and intracellular pathogens, in particular mycoplasma and chlamydia [6]. Thus. levofloxacin has advantages over other fluoroquinolones against pneumococci, chlamydia, mycoplasma. More frequent it is used for the treatment of respiratory infections, as well as infections of the urogenital tract, skin. New, IV generation fluoroquinolones, in particular moxifloxacin have considerably anymore activity against gram-positive microorganisms compared to previous generations of fluoroquinolones [6]. Moxifloxacin is most active against staphylococci, streptococci. In relation to pneumococci, it is in 4-16 times more active than ciprofloxacin. Moxifloxacin acts on polyresistant strains such as chlamydia, mycoplasma, ureaplasma in particular on mycobacterium of tuberculosis, which bioavailability is 90%. It is possible to assume that antibiotics of fluorchinolone if they enter human body also have influence on eukaryotic cells, in particular blood cells. It
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