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Nuclear Factor Erythroid-2 Linked Factor (Nrf2) as a Potential Mediator of Hepatotoxicity 核因子-红细胞-2相关因子(Nrf2)作为肝毒性的潜在介质
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i4.796
Inam Sameh Arif, Israa Burhan Raoof, Hayder Hussein Luaibi
Hepatotoxicity is a term used to describe serious health complications of liver disease caused by a variety of factors. Nuclear factor erythroid-2 linked factor (Nrf2) as a potential mediator of hepatotoxicity via inflammatory and induction of oxidative stress, oxidation produces more toxic compounds caused more pathogenic cases; therefore, to maintain sufficient homeostasis, involve antioxidant materials and detoxification factors. Controlling cytokine activity in normal cells is a useful way to regulate the signaling pathway of Nrf2. Recent studies found a relation between each Nrf2 and NF-κB activation and drug-induced liver injury.  This review presents a detailed and conformation update of Nrf2 roles in hepatotoxicity which considers that drug-induced liver injury is the main problem to draw attention in medical clinics and to develop new drugs with less harmful to the liver. In addition to that. Kept each of normal oxidation and cytokines levels is crucial responses for cells alteration and remaining to survive.
肝毒性是一个术语,用于描述由多种因素引起的肝脏疾病的严重健康并发症。核因子-红细胞-2相关因子(Nrf2)作为肝毒性的潜在介质,通过炎症和诱导氧化应激,氧化产生的毒性化合物较多,引起的致病性病例较多;因此,维持足够的体内平衡,涉及抗氧化物质和解毒因子。调控正常细胞的细胞因子活性是调控Nrf2信号通路的有效途径。近年来研究发现Nrf2和NF-κB活化与药物性肝损伤有关。本文综述了Nrf2在肝毒性中的作用,认为药物性肝损伤是目前临床需要关注的主要问题,并开发对肝脏危害较小的新药。除此之外。维持正常的氧化和细胞因子水平是细胞改变和存活的关键反应。
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引用次数: 1
Design, Molecular Docking, Synthesis of Aromatic Amino Acids Linked to Cephalexin. 设计,分子对接,合成与头孢氨苄连接的芳香氨基酸。
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i3.794
Yasir F. Muhsin, Shakir M. Alwan, Ayad Kareem Khan
Infections caused by bacteria have a significant impact on public health. Chemical synthesis of new derivatives of cephalexin inked to amino acid (tryptophan or histidine) through an amide bond at the acyl side chain is achieved. This is a new approach of incorporating, tryptophan and histidine into the the primary amino group of cephalexin, in order to provide a bulky group very close to the β-lactam ring. This chemical addition act as isosteric group to the alkoximino that protect beta lactam ring from bacterial beta lactamase enzyme. The new derivatives may show resistance to β-lactamases, improve activity and pharmacokinetic properties and may give new life for old drugs that are susceptible to hydrolysis by most β-lactamases. The chemical structures of these derivatives were confirmed by: FTIR, 1H-NMR spectroscopy, elemental micro analysis and some physical properties. Molecular docking on serine beta lactamase and prediction of ADME parameters were recorded using GOLD suite and Swiss ADME software respectively. Docking scores of the new derivatives of Cephalexin on β-lactamases were higher than those of Cephalexin, which may indicate better activity
细菌引起的感染对公众健康有重大影响。通过酰基侧链上的酰胺键,实现了头孢氨苄与氨基酸(色氨酸或组氨酸)连接的新衍生物的化学合成。这是一种新的方法,将色氨酸和组氨酸结合到头孢氨苄的初级氨基中,以提供一个非常接近β-内酰胺环的庞大基团。这种化学加成物作为烷氧亚胺的等构基团,保护内酰胺环免受细菌内酰胺酶的侵害。新的衍生物可能对β-内酰胺酶产生抗性,提高活性和药代动力学性质,并可能使易被大多数β-内酰胺酶水解的旧药物获得新的生命。通过FTIR、1H-NMR、微量元素分析和一些物理性质证实了这些衍生物的化学结构。分别使用GOLD suite和Swiss ADME软件记录丝氨酸β内酰胺酶的分子对接和ADME参数的预测。头孢氨苄新衍生物与β-内酰胺酶的对接分数高于头孢氨苄,可能具有更好的活性
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引用次数: 6
Misuse of antibiotics in Iraq: A review of Iraqi published studies 伊拉克滥用抗生素:伊拉克已发表研究综述
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i2.805
Khulood Saadoon Salim, Atheer S. Alsabah, Hassanian S. Taghi
Misuse of antibiotics is one of the health problems worldwide. In Iraq, prevalence of self- medication with antibiotics increases resistant organisms, this will lead to bad impacts on health and economic aspects in the future. Aim of study is to review the published articles on the antibiotics misuse in Iraq, in   addition to assess the level of the population’s knowledge towards   antibiotics misuse and the suggested recommendation to reduce this problem. Method: In this study 12 articles conducted in different regions of Iraq were reviewed to   assess antibiotic misuse in a period from 2014-2020.Results: The results demonstrated high prevalence of antibiotic misuse among Iraqi population ranging from (45%- 92%). In addition, poor knowledge among   population towards antibiotics misuse also reported. Bad attitudes of pharmacists and physicians regarding antibiotics prescribing and dispensing were registered. Conclusion:  The review focuses on important health issue in Iraq that effect on health & economic system. New legislations and restriction need to apply to limit this problem.
抗生素滥用是世界范围内的健康问题之一。在伊拉克,普遍使用抗生素自行用药增加了耐药生物体,这将在未来对健康和经济方面造成不良影响。本研究的目的是审查已发表的关于伊拉克抗生素滥用的文章,并评估伊拉克人民对抗生素滥用的认识水平和减少这一问题的建议。方法:回顾性分析2014-2020年伊拉克不同地区的12篇抗生素滥用文献。结果:结果表明,伊拉克人口中抗生素滥用的发生率很高,范围为(45%- 92%)。此外,还报告了人们对抗生素滥用的认识不足。药师和医师对抗生素处方和调剂的不良态度进行了登记。结论:综述了影响伊拉克卫生和经济系统的重要卫生问题。需要新的立法和限制来限制这一问题。
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引用次数: 0
Study the antibacterial effect of N_butanol extract of Urtica dioica 研究白荨麻疹正丁醇提取物的抑菌作用
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i1.800
Ahmed Abdulaziz Ahmed, Baydaa Hameed Abdulah, Yaser Mustafa Kamal
Since ancient times Urtica dioica has been used as an herbal medicine in Western Asia. The current study demonstrates the anti-bacterial effect of N_butanol extraction of Urtica dioica. The antibacterial effect was tested against some of gram-positive bacteria and gram-negative bacteria isolated   from hospitalized patients having urinary tract infection. Staphylococcus aureus, Escherichia coli, Klebsiella pneumonia and Pseudomonas aeruginosa was used. Urticasea is a family of plant known for their medicinal activity from folk medicine. Urtica dioica is a member of urticasea and it is known for it is antibacterial effect. Methods The leaves of Urtica dioica were collected in Iraq from jisr dayla district in Baghdad province in april 2019.The N_butanol extraction was compared with the drug ciprofloxacin. Disc diffusion method was used to determine the sensitivity of the samples. Results The N_ butanol extract shows weak inhibitory effect on Escherichia coli while other strain does not affect by extract comparing with ciprofloxacin. Conclusion The N_butanol extract of urtica dioica have weak antibacterial effect when compared with ciproflxacine
自古以来,杜鹃花在西亚就被用作草药。本研究证实了荨麻疹正丁醇提取物的抑菌作用。对尿路感染住院患者分离的革兰氏阳性菌和革兰氏阴性菌进行抑菌试验。使用金黄色葡萄球菌、大肠杆菌、肺炎克雷伯菌和铜绿假单胞菌。荨麻疹是一种以民间医学的药用活性而闻名的植物。荨麻疹是荨麻疹的一种,以其抗菌作用而闻名。方法2019年4月在伊拉克巴格达省jisr dayla地区采集菊苣叶。对正丁醇提取液与环丙沙星进行了比较。采用圆盘扩散法测定样品的灵敏度。结果与环丙沙星相比,正丁醇提取物对大肠埃希菌的抑制作用较弱,其他菌株的抑制作用不明显。结论与环丙沙星相比,白花荨麻疹n_丁醇提取物的抑菌作用较弱
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引用次数: 0
Nrf2 as a modulator of oxidative stress Nrf2作为氧化应激的调节剂
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i4.798
Inam Sameh Arif, Yassir Mustafa Kamal, Israa Burhan Raoof
Nrf2 is active protein presents in the cytoplasm in the cells of the body. In the presence of an activators, Nrf2 can enter the nucleus which bind to Antioxidant Responses Elements (ARE) or otherwise named human ARE (hARE) which control the whole antioxidants activity in human cell. Many factors may contribute to defective or overwhelmed cellular antioxidants activities for instances aging and cellular damages. These cellular damages can be produced by free radicals or oxidative stress. In the mechanism, if Nrf2 activated in the nucleus, can caused the production of collaborative antioxidants enzymes especially: catalase, glutathione (GLT) and superoxide dismutase (SOD) as a responsible for detoxification of free radical inside the cells.
Nrf2是存在于机体细胞细胞质中的活性蛋白。在激活因子存在的情况下,Nrf2可以进入细胞核,与抗氧化反应元件(anti - oxide Responses Elements, ARE)结合,或称为人类抗氧化反应元件(human ARE, hARE),后者控制人类细胞的整个抗氧化活性。许多因素可能导致细胞抗氧化剂活性缺陷或过度,例如衰老和细胞损伤。这些细胞损伤可由自由基或氧化应激产生。在机制上,如果Nrf2在细胞核中被激活,可以引起协同抗氧化剂酶的产生,特别是过氧化氢酶、谷胱甘肽(GLT)和超氧化物歧化酶(SOD),这些酶负责细胞内自由基的解毒。
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引用次数: 3
Nano-carriers as a Selective Treatment for Cancer 纳米载体作为癌症的选择性治疗
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i1.802
Ghaidaa S. Hameed, Methaq Hamad Sabar
Among many therapeutic treatments for cancer, nano-carriers are the focus of our review to illustrate the update usage of this drug delivery approach, the most likely side effects and the reality of their potential application with minimum adverse effects. Here, we demonstrate the types of these nano-carriers based on their nature with detailed recent studies about their use. The variation in the skeleton of these nanoparticles enable the selection of the suitable type with higher specifications than others.  However, the poor in vivo testing is the main stumbling block for completion of their manufacturing. This review will help the researchers to find the road map for further investigation to finally aid the pharmaceutical companies in manufacturing these nano-carriers in appropriate dosage forms to save the life of millions of people in the world.   
在许多癌症治疗方法中,纳米载体是我们综述的重点,以说明这种药物传递方法的最新用法,最可能的副作用以及它们潜在应用的现实,并且副作用最小。在这里,我们根据这些纳米载体的性质展示了它们的类型,并详细介绍了它们的用途。这些纳米颗粒骨架的变化使得选择合适的类型具有更高的规格。然而,较差的体内测试是完成其制造的主要障碍。这一综述将有助于研究人员找到进一步研究的路线图,最终帮助制药公司以适当的剂型制造这些纳米载体,以拯救世界上数百万人的生命。
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引用次数: 1
Isolation of umbelliferone from leaves of Conocarpus erectus L. cultivated in Iraq 伊拉克直立木叶片伞形虫的分离
Pub Date : 2022-04-18 DOI: 10.32947/ajps.v20i4.778
Tahany Amir Tawfeeq, Ghaith Ali Jasim, Abdulmutalib A. Nasser
Conocarpus erectus L. is a perennial, evergreen shrub belonging to Combretaceae family. In this study we investigate the phytoconstituents in the leaves of C.erectus. Preliminary tests of alcoholic extract proved the presence of flavonoids, coumarins, saponin, terpens, tannin and absence of alkaloids. Umbelliferone was detected in the ethyl acetate fraction of the extracted plant by TLC and isolated as a light yellowish powder by preparative TLC. Identification of it was done by HPLC, HPTLC and chemical structure elucidated by IR and UV.
Conocarpus erectus L.是一种多年生、常绿灌木,属于combretacaceae科。在本研究中,我们研究了直立人叶片中的植物成分。初步试验表明,酒精提取物中含有黄酮类化合物、香豆素、皂苷、萜烯、单宁,不含生物碱。薄层色谱法在提取物的乙酸乙酯部位检测到伞形花酮,制备薄层色谱法分离到伞形花酮为淡黄色粉末。用高效液相色谱、高效液相色谱对其进行了鉴定,并用红外光谱和紫外光谱对其结构进行了表征。
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引用次数: 2
Types of Attractive Dosage Forms for Primary School Students and Associated Factors in Baghdad/ Iraq 巴格达/伊拉克小学生有吸引力的剂型类型及相关因素
Pub Date : 2022-04-18 DOI: 10.32947/ajps.v20i4.770
Sura Zuhair Mahmood, Nora Zawar. Yousif, Zeina Dawood Salman
The lack of age-appropriate and child -friendly formulation of medication for children poses a major challenge to pediatric therapeutic practice, adherence, and health care delivery worldwide, however, formulation acceptability and preferences facilitate medication   adherence in children, and they are important factors in achieving the intended treatment outcomes in which this study looks ahead. The present study aims to determine the various medication trends of children through their parents and caregivers, child preference of certain dosage form (chewable gel) in comparison with another solid dosage forms and its popularity among Iraqi primary school, furthermore the study highlights different variables influence student preference for chewable gel.  A total of 230 Iraqi primary school students were randomly selected and interviewed with the presence of their parents. It was observed that (51.3%) of the parents/caregivers reported that the liquid dosage form is the most dosage form that commonly used, (72%) of consumers revealed that the capsules and tablets are not easy to swallow, furthermore,   this study revealed that (68.6%)  of school students preferred to take medication as chewable gel over than other oral solid dosage forms ,and this preference varied significantly with several socioeconomic and other factors.
缺乏适合儿童年龄和儿童友好型的儿童药物配方对儿科治疗实践、依从性和全球卫生保健服务构成了重大挑战,然而,配方可接受性和偏好促进了儿童的药物依从性,它们是实现预期治疗结果的重要因素,本研究展望了未来。本研究旨在通过儿童的父母和照顾者来确定儿童的各种用药趋势,儿童对某种剂型(咀嚼凝胶)的偏好与另一种固体剂型的偏好以及它在伊拉克小学中的受欢迎程度,此外,研究强调了不同变量影响学生对咀嚼凝胶的偏好。随机抽取230名伊拉克小学生,在其父母在场的情况下进行访谈。研究发现,51.3%的家长/护理人员表示液体剂型是最常用的剂型,72%的消费者表示胶囊和片剂不容易吞咽,68.6%的在校学生更喜欢咀嚼凝胶剂型,而不是其他口服固体剂型,这种偏好与社会经济和其他因素存在显著差异。
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引用次数: 0
Synthesis, Antibacterial study and ADME Evaluation of Novel Isonicotinoyl Hydrazide Derivative Containing 1,3,4-Oxadiazole Moiety 新型1,3,4-恶二唑异烟碱酰肼衍生物的合成、抑菌研究及ADME评价
Pub Date : 2022-04-18 DOI: 10.32947/ajps.v20i4.781
Mazen Mohammed Jwaid, Karima Fadhil Ali, Mayada Hadi Abd-alwahab
Novel derivative of isoniazid containing 1,3,4-oxadiazole pharmacophore has been synthesized. The chemical structure of the compound was characterized and confirmed by using FT-IR and 1H-NMR spectroscopy.   The desired compound was tested against gram-positive and gram-negative bacteria using agar well-diffusion technique for their ability as antibacterial agent and showed good antibacterial activity against gram-negative bacteria and gram-positive bacteria. In addition, ADME evaluations were performed using Swiss ADME to predict if the synthesized compound can be given orally, the bioavailability, topological polar surface area, and drug-likeness. The result showed that all tested compounds absorbed orally and fulfilled the Lipinski rule.
合成了含1,3,4-恶二唑药效团的新型异烟肼衍生物。利用红外光谱和核磁共振光谱对化合物的化学结构进行了表征和确认。采用琼脂孔扩散技术对所制备的化合物进行了抑菌实验,结果表明所制备的化合物对革兰氏阴性菌和革兰氏阴性菌均具有良好的抑菌活性。此外,使用瑞士ADME进行ADME评估,以预测合成的化合物是否可以口服,生物利用度,拓扑极性表面积和药物相似性。结果表明,所有化合物均可经口吸收,符合利平斯基规则。
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引用次数: 5
Organogel investigations as a floating oral system with depot property 有机凝胶作为一种具有仓库特性的漂浮口服系统的研究
Pub Date : 2022-04-18 DOI: 10.32947/ajps.v20i4.783
Zainab Saad Kaddoori, Masar Basim Mohsin Mohamed, Nawfal Am. Numan
In this work we investigate span 40, span 60 and SA as a gelators and olive oil (OO) as apolar liquid phase to discover the ability of organogel formed to be floating in acidic media and gain a unique gastroretentive dosage form. In addition, take advantage of the chemical   and physical properties of cinnarizine (CN) as a model drug suitable for gastroretentive systems. The floating parameters were studied where the floating lag time and floating duration for organogel in both solid and liquid states. Organogels charecterization were accomplished through the folowing investigatational techniques and analytical methods: table top rheology, optical microscope, Fourier-transform infrared spectroscopy (FTIR) and in- vitro release study. The results showed that all organogels immediately floated and they were floating in both states. Moreover, table top rheology showed that the transition temperature was reversible and higher than 37 ºC except for 7% w/w and 10% w/w SA in OO organogels where, optical images of organogel showed fibrillar network. The FTIR showed peaks associated to carbonyl groups indicated to form gelator-gelator interactions. Moreover, in vitro release study of organogel system showed continuous release CN for 9-12 hours.  
在这项工作中,我们研究了span 40、span 60和SA作为凝胶,橄榄油(OO)作为极性液相,以发现形成的有机凝胶在酸性介质中漂浮的能力,并获得独特的胃保留剂型。此外,利用肉桂利嗪(CN)的化学和物理性质,作为一种适合于胃保留系统的模型药物。研究了有机凝胶在固体和液体状态下的漂浮滞后时间和漂浮持续时间。通过桌面流变学、光学显微镜、傅里叶变换红外光谱(FTIR)和体外释放研究等研究技术和分析方法完成了有机凝胶的表征。结果表明,所有的有机凝胶都立即漂浮起来,并且在两种状态下都漂浮着。此外,桌面流变学表明,除了7% w/w和10% w/w的SA外,OO有机凝胶的转变温度是可逆的,且高于37℃,其中有机凝胶的光学图像显示为纤维状网络。FTIR显示与羰基相关的峰表明形成凝胶-凝胶相互作用。体外释放研究表明,有机凝胶体系连续释放CN 9-12小时。
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引用次数: 3
期刊
Al Mustansiriyah Journal of Pharmaceutical Sciences
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