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首页> 外文期刊>Journal of Young Pharmacists >Amelioration of 1, 2 Dimethylhydrazine Induced Tumor Promotion Response by Novel Benzimidazole Derivative Nanoparticle in Wistar Rats
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Amelioration of 1, 2 Dimethylhydrazine Induced Tumor Promotion Response by Novel Benzimidazole Derivative Nanoparticle in Wistar Rats

机译：Wistar大鼠新型苯并咪唑衍生物纳米粒子改善1,2二甲基肼诱导的肿瘤促进反应

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Background: Colon cancer is one of the most common malignancies in many regions of the world and is thought to arise from the accumulation of mutations in a single epithelial cell of the colon and rectum. The benzimidazole comprises a important pharmacophore and privileged structure in modern drug discovery. Various substituted benzimidazole derivatives have been found to possess potential anticancer properties. Objective: The study aimed to prove the anti-colon cancer activity of novel benzimidazole derivative 4-(1H-benzo[d]imidazol-2-yl)-6-phenylpyrimidin-2-amine loaded chitosan nanoparticle (BZI 3 nano) by an 1, 2 Dimethylhydrazine (DMH) Induced rat model in-vivo study and identify the targeting efficiency of BZI 3 nano to treat colorectal cancer. Method: The effect of novel benzimidazole derivative 4-(1H-benzo[d]imidazol-2-yl)-6-phenylpyrimidin-2-amine loaded chitosan nanoparticle (BZI 3 nano) on the formation of aberrant crypt foci (ACF), apoptosis, histopathology, body weight, organs weight and heamotological parameters were studied in 1,2-dimethylhydrazine (DMH)-induced colon cancer in rats. Results: BZI 3 nano (5 mg/kg, p.o) administration significantly reduced ACF number and increased the weight gain and apoptotic index compared to DMH treated group. The histological alterations induced by DMH were also significantly improved. Conclusion: In-vivo anticancer activities results revealed that the presence substituted benzimidazole derivative nanoparticle (BZI 3 nano) could have the anticancer potential of the scaffold and selective, good target for drug discovery, which can be regarded as promising anticancer potential.
机译：背景：结肠癌是世界上许多地区最常见的恶性肿瘤之一，被认为是由于结肠和直肠单个上皮细胞中的突变积累所致。苯并咪唑在现代药物发现中包含重要的药效基团和特权结构。已经发现各种取代的苯并咪唑衍生物具有潜在的抗癌特性。目的：本研究旨在证明新型苯并咪唑衍生物4-（1H-苯并[d]咪唑-2-基）-6-苯基嘧啶-2-胺负载的壳聚糖纳米粒子（BZI 3纳米）的抗结肠癌活性。 1，2二甲基肼（DMH）诱导的大鼠体内实验研究并确定BZI 3 nano靶向治疗结直肠癌的效率。方法：新型苯并咪唑衍生物4-（1H-苯并[d]咪唑-2-基）-6-苯基嘧啶-2-胺负载的壳聚糖纳米粒子（BZI 3纳米）对异常隐窝灶（ACF）形成的影响，在1,2-二甲基肼（DMH）诱导的大鼠结肠癌中研究了细胞凋亡，组织病理学，体重，器官重量和血液学参数。结果：与DMH治疗组相比，BZI 3纳米（5 mg / kg，p.o）给药显着减少了ACF数量，并增加了体重增加和凋亡指数。 DMH诱导的组织学改变也得到了明显改善。结论：体内抗癌活性结果表明，存在的取代苯并咪唑衍生物纳米粒子（BZI 3 nano）可以具有支架的抗癌潜力，并且具有选择性，是药物发现的良好靶标，可以认为是有希望的抗癌潜力。

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