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首页> 外文期刊>Toxicology Reports >Antimicrobial activity and acetylcholinestrase inhibition of novel synthesized pyrimidine derivatives versus Candida albicans trafficking to brain and kidney
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Antimicrobial activity and acetylcholinestrase inhibition of novel synthesized pyrimidine derivatives versus Candida albicans trafficking to brain and kidney

机译:新型合成嘧啶衍生物的抗微生物活性和乙酰胆碱酯酶抑制与白色念珠菌向大脑和肾脏的转运

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The expedient fungi Candida albicans ( C. albican s) is able to thrive in many host niches including blood stream, skin, mucosal surfaces, and different body organs. Herein, the assessment of novel synthesized pyrimidine derivatives as anti fungal agent was investigated. Female albino mice were injected intraperitoneally by C. albican s (1.5?×?10sup6/sup CFU). infected Mice then subjected to treatment with two different doses which was low (50?mg/kg) and high one (200?mg/kg) of diflucan in addition to the newly synthestic compounds (2-(4- (Pyridine- 2- yl) aminosulfonyle phenylamino) - 6 -(naphthalene-2- yl)-4-(pyridine-2- yl) n - 3 carbonitril) and (2-(4-(Pyrimidine-2- yl) aminosulfonyle phenylamino)- 6 -(naphthalene-2- yl)- 4 -(pyridine-2- yl) pyridine-3- carbonitril) donated as (C1 & C2, respectively). Three weeks later gene expression of renal alpha smooth muscle actin (α-SMA) and of cyclooxygenase-2 (COX-2) protein expression were assessed as well as serum malondialdehyde (MDA) and total antioxidant capacity in both kidney and brain tissues. Furthermore, acetylcholinestrase activity was assessed. Candida albicans significantly elevated serum MDA. On the other hand, C. albicans injection revealed a significantly reduction in total antioxidant capacity in kidney as well as in brain tissue. Furthermore, acetylcholine assessment declared a significant elevation. All biochemical parameters? upset were modulated upon new synthesized compounds treatment. Molecular analyses declared a significant down - regulation in renal α -smooth muscle actin gene expression in addition to, a significant down- regulation in COX-2 protein expression. From data recorded, it could be concluded that, C2 in a dose 200?mg ∕kg noticeably declared a significant effect comparing with the other treated groups revealing its promising effect as anti-fungal agent.
机译:权宜的真菌白色念珠菌(C. albican s)能够在许多宿主壁ni中壮成长,包括血液,皮肤,粘膜表面和不同的身体器官。在此,研究了新型合成的嘧啶衍生物作为抗真菌剂的评价。雌性白化病小鼠腹腔注射白色念珠菌(1.5?×?10 6 CFU)。然后,除了新合成的化合物(2-(4-(吡啶-2-)外,还用两种不同剂量的低剂量(50?mg / kg)和高剂量(200?mg / kg)的地氟康处理小鼠)。 yl)氨基磺酰基苯氨基)-6-(萘-2-基)-4-(吡啶-2-基)n-3碳腈)和(2-(4-(嘧啶-2-基)氨基磺酰基苯氨基)-6-捐赠的(萘-2-基)-4-(吡啶-2-基)吡啶-3-碳腈(分别为C1和C2)。三周后,评估了肾α平滑肌肌动蛋白(α-SMA)和环氧合酶-2(COX-2)蛋白的基因表达以及血清丙二醛(MDA)和肾脏和脑组织的总抗氧化能力。此外,评估了乙酰胆碱酯酶的活性。白色念珠菌显着升高血清MDA。另一方面,白色念珠菌注射显示肾脏和脑组织中的总抗氧化能力显着降低。此外,乙酰胆碱评估表明明显升高。所有生化参数?新合成的化合物治疗可调节心烦。分子分析表明,肾α-平滑肌肌动蛋白基因表达显着下调,此外,COX-2蛋白表达也显着下调。从记录的数据可以得出结论,与其他治疗组相比,剂量为200?mg / kg的C2显着宣告了显着的疗效,显示了其作为抗真菌剂的良好前景。

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