研究喹啉衍生物的抗炎效果:N1-(5-甲基-5H-吲哚并[2,3-b]喹啉-11-基)苯-1,4-二胺盐酸盐载体可溶性淀粉纳米粒子对甲氨蝶呤诱导的实验模型炎症的抗炎作用。

IF 3.7 3区 生物学 Q1 BIOCHEMICAL RESEARCH METHODS Biological Procedures Online Pub Date : 2024-06-03 DOI:10.1186/s12575-024-00240-7
Dalia Medhat, Mona A El-Bana, Ibrahim El-Tantawy El-Sayed, Abdullah A S Ahmed, Mehrez E El-Naggar, Jihan Hussein
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引用次数: 0

摘要

背景:为了减轻化疗药物的负面影响,有必要利用具有抗炎特性的天然成分开发先进疗法:有必要利用具有抗炎特性的天然成分开发先进疗法,以减轻化疗药物的负面影响:结果:合成了具有生物活性的N1-(5-甲基-5H-吲哚并[2,3-b]喹啉-11-基)苯-1,4-二胺盐酸盐(NIQBD)。然后,以不同浓度(50 毫克、100 毫克和 200 毫克)的可溶性淀粉纳米颗粒(StNPs)作为载体,载入合成的 NIQBD。载入不同浓度 NIQBD 的 StNPs 分别称为 StNPs-1、StNPs-2 和 StNPs-3。据观察,StNPs-1、StNPs-2 和 StNPs-3 的平均尺寸分别为 246、300 和 328 nm。此外,从多分散指数(PDI)值来看,它们形成的颗粒也很均匀。StNPs-1、StNPs-2 和 StNPs-3 的 PDI 值分别为 0.298、0.177 和 0.262。对负载 NIQBD 的不同浓度 StNPs 针对 MTX 引起的肺部和肝脏炎症的潜在特性进行的体内研究表明,还原型谷胱甘肽(GSH)的水平在统计学上有了显著提高,同时丙二醛(MDA)、一氧化氮(NO)、高级氧化蛋白产物(AOP)等氧化剂的水平也有了显著降低、与 MTX 诱导的炎症组相比,还原型谷胱甘肽(GSH)水平增加,同时肺和肝组织中的氧化剂(如丙二醛(MDA)、一氧化氮(NO)、高级氧化蛋白产物(AOPP)、基质金属蛋白酶 9/Gelatinase B(MMP-9))和炎症介质(包括白细胞介素 1-β(IL-1β)、核因子卡巴-B(NF-κB))水平显著降低,血浆同型半胱氨酸(Hcy)水平也显著降低。浓度为 200 毫克/毫升的治疗结果非常明显。组织病理学检查证实了这些结果,治疗显示肺组织的炎症浸润和充血极少,中央静脉轻度充血,肝组织的 Kupffer 细胞轻度活化:结论:结合天然抗氧化剂补充剂治疗 MTX 可能有助于减少相关的氧化和炎症。
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Investigating the Anti-inflammatory Effect of Quinoline Derivative: N1-(5-methyl-5H-indolo[2,3-b]quinolin-11-yl)benzene-1,4-diamine Hydrochloride Loaded Soluble Starch Nanoparticles Against Methotrexate-induced Inflammation in Experimental Model.

Background: It is necessary to develop advanced therapies utilizing natural ingredients with anti-inflammatory qualities in order to lessen the negative effects of chemotherapeutics.

Results: The bioactive N1-(5-methyl-5H-indolo[2,3-b]quinolin-11-yl)benzene-1,4-diamine hydrochloride (NIQBD) was synthesized. After that, soluble starch nanoparticles (StNPs) was used as a carrier for the synthesized NIQBD with different concentrations (50 mg, 100 mg, and 200 mg). The obtained StNPs loaded with different concentrations of NIQBD were coded as StNPs-1, StNPs-2, and StNPs-3. It was observed that, StNPs-1, StNPs-2, and StNPs-3 exhibited an average size of 246, 300, and 328 nm, respectively. Additionally, they also formed with homogeneity particles as depicted from polydispersity index values (PDI). The PDI values of StNPs-1, StNPs-2, and StNPs-3 are 0.298, 0.177, and 0.262, respectively. In vivo investigation of the potential properties of the different concentrations of StNPs loaded with NIQBD against MTX-induced inflammation in the lung and liver showed a statistically substantial increase in levels of reduced glutathione (GSH) accompanied by a significant decrease in levels of oxidants such as malondialdehyde (MDA), nitric oxide (NO), advanced oxidation protein product (AOPP), matrix metalloproteinase 9/Gelatinase B (MMP-9), and levels of inflammatory mediators including interleukin 1-beta (IL-1β), nuclear factor kappa-B (NF-κB) in both lung and liver tissues, and a significant decrease in levels of plasma homocysteine (Hcy) compared to the MTX-induced inflammation group. The highly significant results were obtained by treatment with a concentration of 200 mg/mL. Histopathological examination supported these results, where treatment showed minimal inflammatory infiltration and congestion in lung tissue, a mildly congested central vein, and mild activation of Kupffer cells in liver tissues.

Conclusion: Combining the treatment of MTX with natural antioxidant supplements may help reducing the associated oxidation and inflammation.

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来源期刊
Biological Procedures Online
Biological Procedures Online 生物-生化研究方法
CiteScore
10.50
自引率
0.00%
发文量
16
审稿时长
>12 weeks
期刊介绍: iological Procedures Online publishes articles that improve access to techniques and methods in the medical and biological sciences. We are also interested in short but important research discoveries, such as new animal disease models. Topics of interest include, but are not limited to: Reports of new research techniques and applications of existing techniques Technical analyses of research techniques and published reports Validity analyses of research methods and approaches to judging the validity of research reports Application of common research methods Reviews of existing techniques Novel/important product information Biological Procedures Online places emphasis on multidisciplinary approaches that integrate methodologies from medicine, biology, chemistry, imaging, engineering, bioinformatics, computer science, and systems analysis.
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