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The new iron(III) 3‐oxo‐N‐(pyridin‐2‐yl)butanamide complex promotes Ehrlich solid tumor regression in mice via induction of apoptosis
Applied Organometallic Chemistry ( IF 3.7 ) Pub Date : 2019-11-13 , DOI: 10.1002/aoc.5282
Entsar A. Saad 1 , Shadia A. Elsayed 1 , Mohamed M. Hassanien 2 , Menna S. AL‐Adl 1
Affiliation  

Currently used chemotherapeutic drugs had serious adverse effects e.g. myelo‐suppression, anemia and nephrotoxicity. Thus, developing new alternatives is of great importance. We aimed to develop a new prospective antitumor complex combines iron metal ion and 3‐oxo‐N‐(pyridin‐2‐yl)butanamide ligand that may be effective with less toxicity towards healthy tissues. Anticancer activities of the developed complex were studied in vitro and in vivo using induced Ehrlich solid tumor in mice as animal model. In vitro, the complex (1 mmol/L) exhibited superoxide dismutase (SOD)‐like activity of 86.69 %, catalase‐like activity of 170 U/100 mL, and 99.06% mortality of Ehrlich ascites carcinoma (EAC) cells. Complex ability to interact with DNA was proved spectrophotometrically. Flow‐cytometrically, EAC cells treated with the complex showed higher apoptosis, caspase 3 activity, and p53 compared to the untreated EAC cells. In vivo, the complex showed prominent dose‐dependent antitumor activities. It reduced tumor volume and weight, prolonged mice life span, and reversed the hematological indices, malondialdehyde (MDA), total antioxidant capacity (TAC), ALT and urea levels towards normal. Finally, our findings indicate that the complex motivates Ehrlich solid tumor regression in mice via induction of apoptosis. Its effect was better than that of cisplatin.

中文翻译:

新型铁(III)3-氧代-N-(吡啶-2-基)丁酰胺复合物通过诱导细胞凋亡促进小鼠艾氏实体瘤消退

当前使用的化疗药物具有严重的不良反应,例如骨髓抑制,贫血和肾毒性。因此,开发新的替代方案非常重要。我们旨在开发一种新的前瞻性抗肿瘤复合物,该复合物结合了铁金属离子和3-氧代-N-(吡啶-2-基)丁酰胺配体,对健康组织的毒性可能较小。使用小鼠中诱发的艾氏实体瘤作为动物模型,在体内和体外研究了开发的复合物的抗癌活性。在体外,该复合物(1 mmol / L)表现出86.69%的超氧化物歧化酶(SOD)样活性,170 U / 100 mL的过氧化氢酶样活性以及Ehrlich腹水癌细胞(EAC)细胞的死亡率为99.06%。分光光度法证明了其与DNA相互作用的复杂能力。流式细胞仪分析,用复合物处理的EAC细胞显示出更高的凋亡,caspase 3活性,与未处理的EAC细胞相比p53。在体内,该复合物显示出显着的剂量依赖性抗肿瘤活性。它减少了肿瘤的体积和重量,延长了小鼠的寿命,并使血液学指标,丙二醛(MDA),总抗氧化能力(TAC),ALT和尿素水平恢复正常。最后,我们的研究结果表明,该复合物通过诱导细胞凋亡来促使小鼠Ehrlich实体瘤消退。其效果优于顺铂。我们的发现表明,该复合物通过诱导细胞凋亡来促使小鼠艾氏实体瘤消退。其效果优于顺铂。我们的发现表明,该复合物通过诱导细胞凋亡来促使小鼠艾氏实体瘤消退。其效果优于顺铂。
更新日期:2019-11-13
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