New Benzofuran N -Acylhydrazone Reduces Cardiovascular Dysfunction in Obese Rats by Blocking TNF-Alpha Synthesis

Gizele Cabral Costa; Tadeu Lima Montagnoli; Jaqueline Soares Da Silva; Allan Kardec Nogueira de Alencar; Luis Eduardo Reina Gamba; Bryelle Eccard Oliveira Alves; Marina Moraes Carvalho da Silva; Margarete Manh?es Trachez; José Hamilton M do Nascimento; Pedro Moreno Pimentel-Coelho; Rosália Mendez-Otero; Lidia Moreira Lima; Eliezer J Barreiro; Roberto Takashi Sudo; Gisele Zapata-Sudo

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New Benzofuran N -Acylhydrazone Reduces Cardiovascular Dysfunction in Obese Rats by Blocking TNF-Alpha Synthesis

机译：通过阻断TNF-α合成，新的苯并呋喃N-酰基肼缩小了肥胖大鼠的心血管功能障碍

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Introduction: Diabetic obese patients are susceptible to the development of cardiovascular disease, including hypertension and cardiac dysfunction culminating in diabetic cardiomyopathy (DC), which represents a life-threatening health problem with increased rates of morbidity and mortality. The aim of the study is to characterize the effects of a new benzofuran N -acylhydrazone compound, LASSBio-2090, on metabolic and cardiovascular alterations in Zucker diabetic fatty (ZDF) rats presenting DC. Methods: Male non-diabetic lean Zucker rats (ZL) and ZDF rats treated with vehicle (dimethylsulfoxide) or LASSBio-2090 were used in this study. Metabolic parameters, cardiovascular function, left ventricle histology and inflammatory protein expression were analyzed in the experimental groups. Results: LASSBio-2090 administration in ZDF rats reduced glucose levels to 85.0 ± 1.7 mg/dL ( p 0.05). LASSBio-2090 also lowered the cholesterol and triglyceride levels from 177.8 ± 31.2 to 104.8 ± 5.3 mg/dL and from 123.0 ± 11.4 to 90.9 ± 4.8 mg/dL, respectively, in obese diabetic rats ( p 0.05). LASSBio-2090 normalized plasma insulin, insulin sensitivity and endothelial function in aortas from diabetic animals ( p 0.05). It also enhanced systolic and diastolic left-ventricular function and reverted myocardial remodeling by blocking the threefold elevation of TNF-α levels in hearts from ZDF rats. Conclusion: LASSBio-2090 alleviates metabolic disturbance and cardiomyopathy in an obese and diabetic rat model, thus representing a novel strategy for the treatment of cardiovascular complications in obesity-associated type 2 diabetes mellitus.

机译：简介：糖尿病肥胖患者易患心血管疾病的发展，包括糖尿病心肌病（DC）中的高血压和心脏功能障碍，这代表了危及生命的健康问题，其发病率和死亡率增加。该研究的目的是表征新的苯并呋喃N-酰基腙化合物，Lassbio-2090，ZUCKER糖尿病脂肪（ZDF）大鼠代谢和心血管改变的作用。方法：在本研究中使用雄性非糖尿病瘦Zucker大鼠（ZL）和用载体（二甲基磺酰甲醚）或Lassbio-2090处理的ZDF大鼠。在实验组中分析了代谢参数，心血管功能，左心室组织学和炎症蛋白表达。结果：Lassbio-2090在ZDF大鼠中给药降低葡萄糖水平至85.0±1.7mg / dL（P <0.05）。 Lassbio-2090还将胆固醇和甘油三酯水平从177.8±31.2至104.8±5.3mg / dl降低，分别在肥胖糖尿病大鼠中分别为123.0±11.4至90.9±4.8mg / dl（P <0.05）。 Lassbio-2090标准化血浆胰岛素，糖尿病动物主动脉胰岛素敏感性和内皮功能（P <0.05）。它还通过阻断来自ZDF大鼠的心中的TNF-α水平的三倍高度来增强收缩和舒张左心室功能并再次改造心肌重塑。结论：Lassbio-2090减轻了肥胖和糖尿病大鼠模型中的代谢紊乱和心肌病，从而代表了肥胖相关型2型糖尿病患者心血管并发症的新策略。

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《Drug Design, Development and Therapy》 |2020年第1期|共14页
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Gizele Cabral Costa; Tadeu Lima Montagnoli; Jaqueline Soares Da Silva; Allan Kardec Nogueira de Alencar; Luis Eduardo Reina Gamba; Bryelle Eccard Oliveira Alves; Marina Moraes Carvalho da Silva; Margarete Manh?es Trachez; José Hamilton M do Nascimento; Pedro Moreno Pimentel-Coelho; Rosália Mendez-Otero; Lidia Moreira Lima; Eliezer J Barreiro; Roberto Takashi Sudo; Gisele Zapata-Sudo;
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type 2 diabetes mellitusdiabetic cardiomyopathyanti-TNF-α therapycardiac dysfunctionheart hypertrophyZucker diabetic fatty rat;

机译：2型糖尿病MELLITUSDIBETICACTIBERICYOPATINI-TNF-α治疗卡片功能障碍HEACROFTOLYZURE糖尿病脂肪大鼠;

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1. Effects of TNF-alpha blocking on experimental periodontitis and type 2 diabetes in obese diabetic Zucker rats [J] . Grauballe Morten Bay, Ostergaard Jakob Appel, Schou Soren, Journal of clinical periodontology . 2015,第9期

机译：TNF-α阻断对肥胖糖尿病Zucker大鼠实验性牙周炎和2型糖尿病的影响
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机译：血管紧张素受体阻滞剂和钙通道阻滞剂组合对Dahl大鼠的ox-LDL水平和心血管功能障碍的影响。
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机译：肿瘤坏死因子（TNF）受体1型介导的TNF-α信号传导的阻滞保护wistar大鼠免受饮食诱导的肥胖和胰岛素抵抗。
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机译：通过心血管信号分析评估每日短时站立预防大鼠悬浮后心血管功能障碍的有效性
5. Transversus Abdominis Plane Blocks Versus Erector Spinae Plane Blocks: Reducing Opioid Consumption Postoperatively for Colorectal Surgery [D] . Entzeroth, Timothy R. 2021

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6. New Benzofuran N-Acylhydrazone Reduces Cardiovascular Dysfunction in Obese Rats by Blocking TNF-Alpha Synthesis [O] . Gizele Cabral Costa, Tadeu Lima Montagnoli, Jaqueline Soares Da Silva, 2020

机译：通过阻断TNF-α合成新的苯并呋喃N-酰基腙在肥胖大鼠中减少心血管功能障碍
7. >New Benzofuran N-Acylhydrazone Reduces Cardiovascular Dysfunction in Obese Rats by Blocking TNF-Alpha Synthesis [O] . Gizele Cabral Costa, Tadeu Lima Montagnoli, Jaqueline Soares da Silva, 2020

机译：> New Benzofuran N - 通过阻断TNF-α合成来减少肥胖大鼠的心血管功能障碍

1. 水介质中N-芳基-N'-(2-苯并呋喃甲酰基)硫脲及1-芳甲酰基-4-(2'-苯并呋喃甲酰基)氨基硫脲的合成 [J] . 王喜存 ,张彰 ,权正军 . 有机化学 . 2006,第007期

2. N'-叔丁基-3,5-二氯苯甲酰基-N-吡唑酰基肼的合成工艺研究 [J] . 许良忠 ,杨曦 . 青岛科技大学学报（自然科学版） . 2017,第0z1期

3. N'-叔丁基-N'-取代苯甲酰基-N-(苯并二氢吡喃-5-甲酰基)肼的设计合成及晶体结构 [J] . 黄治强 ,宋红健 ,崔志鹏 . 有机化学 . 2009,第006期

4. 液-液相转移催化法合成N-芳氧基乙酰基-N′(2-氯苯甲酰基)肼 [J] . 杨春文 ,伍家卫 . 甘肃联合大学学报（自然科学版） . 2002,第003期

5. N-芳基-5-芳基-2-呋喃甲酰胺和N-5-芳基-2-呋喃甲酰基-N'-芳氧基乙酰基肼的合成及生物活性的研究 [J] . 王喜存 ,陈继畴 ,王秀春 . 高等学校化学学报 . 1998,第008期

6. N-苯并噻唑N'-取代苯甲酰基特丁基肼类化合物的合成及生物活性研究 [C] . 任叶果 ,侯仲轲 ,张立杰 . 中国化工学会农药专业委员会年会 . 2002

7. 三唑肟醚、磷酰基肟酯及N-（芳氧乙酰基），N-[三氟氯菊酰基]肼类化合物的合成及生物活性研究 [A] . 蒙柳 . 2008

1. N－(2,3－二氢－2,4－二甲基苯并呋喃－5－酰基)－N＇－叔丁基－N＇－(取代苯甲酰基)肼类杀虫剂的制备及应用 [P] . 中国专利： CN100567282C . 2009.12.09

2. N－(2,3－二氢－2,4－二甲基苯并呋喃－5－酰基)－N＇－叔丁基－N＇－(取代苯甲酰基)肼类杀虫剂的制备及应用 [P] . 中国专利： CN101190905A . 2008-06-04

3. compound or a pharmaceutically acceptable salt, solvate or hydrate thereof, pharmaceutical composition, and, methods to inhibit angiogenesis, to inhibit or reduce the polymerization of tubulin or the stability of tubulin in a cell, to inhibit pde4 activity in a cell , to inhibit tumor necrosis factor-alpha (tnf-alpha) activity in a cell, to treat or ameliorate an inflammatory disorder, to treat or ameliorate cancer, to inhibit cancer cell proliferation, to mark, block or destroy tumor vasculature function, to mark, block or destroy tumor vessel endothelium, to mark, block or destroy tumor vasculature function and inhibit angiogenesis in a tumor and to treat or ameliorate a central nervous system disorder [P] . 外国专利： BRPI0514857A . 2008-05-06

机译：化合物或其药学上可接受的盐，溶剂化物或水合物，药物组合物以及抑制血管生成，抑制或降低微管蛋白聚合或微管蛋白稳定性的方法，抑制细胞中pde4活性，抑制肿瘤的方法细胞中的坏死因子-α（tnf-alpha）活性，用于治疗或改善炎症性疾病，治疗或改善癌症，抑制癌细胞增殖，标记，阻断或破坏肿瘤血管功能，标记，阻断或破坏肿瘤血管内皮，标记，阻断或破坏肿瘤的脉管系统功能并抑制肿瘤中的血管生成，并治疗或改善中枢神经系统疾病

4. compound or a pharmaceutically acceptable salt, solvate or hydrate thereof, pharmaceutical composition, and methods for inhibiting angiogenesis, for inhibiting or reducing tubulin polymerization or tubulin stability in a cell, for inhibiting pde4 activity in a cell , to inhibit tumor necrosis factor-alpha (tnf-alpha) activity in a cell, to treat or ameliorate an inflammatory disorder, to treat or ameliorate cancer, to inhibit cancer cell proliferation, to mark, block or destroy Tumor vasculature function, to tag, block or destroy tumor vessel endothelium, to tag, block or destroy tumor vasculature function and inhibit angiogenesis in a tumor, and to treat or ameliorate a central nervous system disorder [P] . 外国专利： BRPI0514890A . 2007-11-27

机译：化合物或其药学上可接受的盐，溶剂化物或水合物，药物组合物以及抑制血管生成，抑制或降低细胞微管蛋白聚合或微管蛋白稳定性，抑制细胞中pde4活性，抑制肿瘤坏死因子-α（细胞中的tnf-alpha）活性，以治疗或改善炎症性疾病，以治疗或改善癌症，抑制癌细胞的增殖，标记，阻断或破坏肿瘤血管功能，标记，阻断或破坏肿瘤血管内皮，标记，阻断或破坏肿瘤血管系统功能并抑制肿瘤中的血管生成，并治疗或改善中枢神经系统疾病

5. Compounds, use of a compound, processes for treating depression, anxiety, psychosis, tardive dyskinesia, parkinson's disease, obesity, hypertension, tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive illness, alzheimer's disease, senile dementia , obsessive compulsive behavior, panic attacks, social phobias, diseases and food anorexia, cardiovascular and cerebrovascular diseases, diabetes mellitus not dependent on insulin, hyperglycemia, constipation, arrhythmia, diseases of the neuroendocrine system, tension and spasticity in humans and for preparation of compounds, and pharmaceutical composition. [P] . 外国专利： BR9714237A . 2000-04-18

机译：化合物，化合物的用途，治疗抑郁症，焦虑症，精神病，迟发性运动障碍，帕金森氏病，肥胖症，高血压，抽动秽语综合征，性功能障碍，吸毒，吸毒，认知疾病，阿尔茨海默氏病，老年性痴呆，强迫症行为的方法，惊恐发作，社交恐怖症，疾病和食物性厌食症，心血管和脑血管疾病，不依赖胰岛素的糖尿病，高血糖症，便秘，心律不齐，神经内分泌系统疾病，人的紧张和痉挛以及化合物的制备以及药物组合物。

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New Benzofuran N -Acylhydrazone Reduces Cardiovascular Dysfunction in Obese Rats by Blocking TNF-Alpha Synthesis

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