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Protective Effects of N-Acetylcysteine on Dipentyl Phthalate Induced Cognitive Dysfunction and Brain Oxidative Stress in Mice n -乙酰半胱氨酸对邻苯二甲酸二戊酯诱导的小鼠认知功能障碍和脑氧化应激的保护作用
S. Gautam, S. Jain, Proteesh Rana, B. Banerjee, Pramod Kumari
Background: Dipentyl phthalate (DPeP) is a plasticizer compound commonly used in polyvinylchloride plastic to enhance softness and flexibility. They are not bound covalently to plastic polymers; therefore, they can dissolve into the environment and adversely affect the health of humans and animals. Objectives: The aim of this study was to investigate the effect of DPeP on cognition and protective effects of N-acetylcysteine (NAC) on DPeP induced alteration in cognitive behaviour and oxidative stress markers in mice. Methods: Mice were orally treated with 2 doses (33 mg/kg and 100 mg/kg) of DPeP for 28 days. Cognitive functions were assessed using spatial navigation tasks on the Morris water maze and the step-down latency in the passive avoidance apparatus. Oxidative stress was assessed by examining the levels of malondialdehyde, glutathione, ferric reducing antioxidant power, and 8-hydroxy-deoxyguanosine levels in the whole brain of mice. Results: There was a significant increase in latency in spatial navigation tasks and a significant decline in the step-down latency in passive avoidance apparatus in the DPeP-treated group compared to the control groups. There was also a significant increase in the levels of oxidative stress following DPeP administration as seen with the rise in the levels of malondialdehyde, 8-hydroxy-deoxyguanosine, and a fall in glutathione and ferric reducing antioxidant power levels. Conclusion: The present study demonstrated that DPeP adversely affects learning and memory functions in mice by oxidative stress-mediated neuronal damage. These effects were attenuated by pretreatment with N-acetylcysteine.
背景:邻苯二甲酸二戊酯(DPeP)是一种增塑剂化合物,通常用于聚氯乙烯塑料,以提高柔软性和柔韧性。它们不与塑料聚合物共价结合;因此,它们可以溶解到环境中,对人类和动物的健康产生不利影响。目的:探讨DPeP对小鼠认知功能的影响及n -乙酰半胱氨酸(NAC)对DPeP诱导小鼠认知行为和氧化应激标志物改变的保护作用。方法:小鼠口服2剂量(33 mg/kg、100 mg/kg) DPeP 28 d。通过Morris水迷宫的空间导航任务和被动回避装置的降压延迟来评估认知功能。通过检测小鼠全脑丙二醛、谷胱甘肽、铁还原抗氧化能力和8-羟基脱氧鸟苷水平来评估氧化应激。结果:与对照组相比,dpep治疗组空间导航任务潜伏期显著增加,被动回避装置降压潜伏期显著降低。在服用DPeP后,氧化应激水平也显著增加,丙二醛、8-羟基脱氧鸟苷水平上升,谷胱甘肽和铁的抗氧化能力水平下降。结论:本研究表明,DPeP通过氧化应激介导的神经元损伤对小鼠的学习记忆功能产生不利影响。用n -乙酰半胱氨酸预处理后,这些影响减弱。
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引用次数: 0
A Narrative Review of SARS-CoV-2 Pathogenesis, Transmission, and Clinical Manifestations SARS-CoV-2的发病机制、传播途径和临床表现综述
Amin Sharifan
Background: Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) has become a major global concern. As of writing this manuscript, there are over 224 million cases diagnosed, and 4.5 million recorded deaths with the Coronavirus Disease 2019 (COVID-19). Objectives: This article reviews the studies conducted on SARS-CoV-2 pathogenesis, transmission, and different clinical manifestations. Methods: An extensive online search was conducted on PubMed and Google Scholar search engines. The following keywords and their combinations were used to complete this review: “SARS-CoV-2”, “COVID-19”, “virology”, “mechanism of action”, “transmission”, “clinical manifestations”, “laboratory findings”, and “comorbidities.” Results: The SARS-CoV-2 spike glycoprotein recognizes the human angiotensin-converting enzyme 2 receptors, and through that, the virus can enter its host cell. The virus is mainly transmitted via respiratory and or airborne droplets. The severity of the COVID-19 clinical manifestations relies on the associated comorbidities and or old age, which ranges from littleto-no symptoms to severe and critical conditions. Fever, loss of appetite and or smell, fatigue, and dry cough are among the most reported symptoms. Underlying conditions may lead to severe or critical stages of COVID-19. Conclusion: The SARS-CoV-2 nucleocapsid and receptor-binding domain could be two potential targets for future vaccines and drugs. It appears that the virus is adapting to each region’s specific environment; therefore, new endemic variants are forming.
背景:严重急性呼吸综合征冠状病毒2 (SARS-CoV-2)已成为全球关注的主要问题。截至撰写本文时,2019年冠状病毒病(COVID-19)确诊病例超过2.24亿例,记录的死亡人数为450万人。目的:综述SARS-CoV-2的发病机制、传播途径和不同临床表现的研究进展。方法:在PubMed和Google Scholar搜索引擎上进行广泛的在线搜索。使用以下关键词及其组合完成本综述:“SARS-CoV-2”、“COVID-19”、“病毒学”、“作用机制”、“传播”、“临床表现”、“实验室结果”和“合并症”。结果:SARS-CoV-2刺突糖蛋白识别人血管紧张素转换酶2受体,并通过该受体进入宿主细胞。该病毒主要通过呼吸道飞沫和/或空气飞沫传播。COVID-19临床表现的严重程度取决于相关的合并症和/或老年,从几乎没有症状到严重和危重病症不等。发烧、食欲和/或嗅觉减退、疲劳和干咳是报告最多的症状。潜在条件可能导致COVID-19的严重或关键阶段。结论:SARS-CoV-2核衣壳和受体结合域可能是未来疫苗和药物的两个潜在靶点。病毒似乎正在适应每个地区的特定环境;因此,新的地方性变异正在形成。
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引用次数: 0
Successful Diflunisal Desensitization in a Transthyretin Amyloidosis Patient With Ibuprofen Allergy: A Case Report 对布洛芬过敏的转甲状腺素淀粉样变性患者成功的双氟尼拉脱敏1例报告
J. Aw, Siau Hui Low, Chuan Poh Lim, Kwok Wai Adrian Chan
Background: Amyloid diseases are hereditary and include transthyretin (TTR) amyloidosis where subunit protein mutations may occur in genes for TTR, leading to the deposition of fibrils (low molecular weight subunits (5 to 25 KD of proteins) in extracellular tissues. By reducing the formation of TTR amyloid, diflunisal, a nonsteroidal anti-inflammatory drug, can preserve the quality of life and significantly reduce disease progression. We present a case of a 61-year-old male patient with a history of ibuprofen allergy, diagnosed with TTR amyloidosis, complicated with peripheral neuropathy, cardiac, and liver amyloid. He developed bilateral mild eye swelling from the ibuprofen oral provocation test. With a similar structural backbone of carboxylic acid, he could develop pseudoallergy to diflunisal with an unknown likelihood of developing an allergic reaction. Objectives: This study aims to design successful diflunisal desensitization in a patient with TTR amyloidosis. Methods: The patient underwent a 14-step diflunisal desensitization procedure using 2 tablets of diflunisal 500 mg that was dissolved in 40 mL of sodium bicarbonate 8.4% injection to create serial 10-fold dilutions. Oral desensitization was administered in the escalation of the doses at 30-min intervals, with a starting dose of 0.1 mg until a final dose of 250 mg was reached. Results: The patient tolerated diflunisal desensitization and was continued on diflunisal treatment without any evidence of an allergic reaction. Conclusion: Diflunisal desensitization can be considered in patients with a history of ibuprofen allergy if there are no available alternative treatments. To the best of our knowledge, this is the first article describing a patient with angioedema to ibuprofen who could tolerate oral diflunisal after desensitization.
背景:淀粉样蛋白疾病是遗传性的,包括转甲状腺素(TTR)淀粉样变性,其中TTR基因的亚基蛋白突变可能发生,导致细胞外组织中原纤维(低分子量亚基(5至25 KD的蛋白质)的沉积。通过减少TTR淀粉样蛋白的形成,非甾体抗炎药双氟尼拉可以保持生活质量并显著减少疾病进展。我们报告一例61岁男性患者,有布洛芬过敏史,诊断为TTR淀粉样变性,并发周围神经病变,心脏和肝脏淀粉样变性。布洛芬口服激发试验后出现双侧轻度眼部肿胀。由于羧酸具有类似的结构主链,他可能对二氟尼柳产生假性过敏,发生过敏反应的可能性未知。目的:本研究旨在为TTR淀粉样变患者设计成功的双氟尼松脱敏治疗。方法:采用双氟尼拉500 mg 2片,溶解于8.4%碳酸氢钠注射液40 mL中,连续稀释10倍,进行14步双氟尼拉脱敏。口服脱敏以每隔30分钟剂量递增的方式进行,起始剂量为0.1 mg,直至达到最终剂量为250 mg。结果:患者耐受双氟尼拉脱敏,并继续双氟尼拉治疗,无任何过敏反应的证据。结论:对有布洛芬过敏史的患者,在没有其他治疗方法的情况下,可考虑使用双氟尼拉脱敏。据我们所知,这是第一篇描述布洛芬血管性水肿患者脱敏后能耐受口服双氟尼松的文章。
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引用次数: 1
Could Celastrol Be a Photosensitizer for Photodynamic Therapy to Combat SARS-CoV-2? 雷公藤红素可以作为光动力疗法对抗SARS-CoV-2的光敏剂吗?
Siu Kan Law
The Article Abstract is not available.
文章摘要不可用。
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引用次数: 1
Evaluation of Antioxidant and Anticoagulation Activity of Piper chaba Hunter Stem 番椒茎抗氧化和抗凝血活性的评价
S. Mahmud, Azi Mohammed Didarul Islam, M. Billah, Mahbubur Rahman, R. Biswas, Md. Emdadul Islam
Background: Piper chaba Hunter, a flowering vine of the Piperaceae family, has long been used in South Asian countries for culinary purposes and traditionally in fat-rich meat preparation. The curative potential of this herb is of great interest to be studied. Objectives: The antioxidant and anticoagulation potential, as well as total phenolic and flavonoid content, were evaluated using cold and boiled water extract separately from the dried and ground stem. Methods: Antioxidant potential was evaluated by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay and ferric reducing antioxidant power (FRAP) assay. The anticoagulation activity was evaluated by serine protease inhibition assay and prothrombin time (PT) assay. Folin–Ciocalteu (FC) reagent and aluminum complex (AlCl3 ) were used to assess total phenolic content and total flavonoid content, respectively. Results: DPPH scavenging assay revealed the IC50 value of 125.52 µg.mL-1 and 157.94 µg.mL-1 for boiled and cold water extract, respectively. Potent ferric reducing potential (FRAP) was observed as 142.87 µM and 135.37 µM of ferrous equivalent per 100 µg for boiled and cold water extract, respectively. The IC50 value of serine protease inhibitory activity was found as 182 µg.mL-1 and 161.12 µg.mL-1 for cold and boiled water extract, respectively. The PT time was 27.00 min for boiled water extract and 24.68 min for cold water extract. Significant phenolic and flavonoid content was also found in the test sample. Conclusion: P. chaba stem extract possesses potent antioxidant and anticoagulation activity, which can neutralize oxidative free radicals and have a vasodilation effect in oxidative and inflammatory diseases.
背景:Piper chaba Hunter是胡椒科的一种开花藤蔓,长期以来在南亚国家用于烹饪目的,传统上用于富含脂肪的肉类制备。这种草药的治疗潜力值得研究。目的:研究干茎和磨碎茎的冷水和开水提取物的抗氧化和抗凝血潜能,以及总酚和总黄酮含量。方法:采用2,2 -二苯基-1-苦味酰肼(DPPH)自由基清除法和铁还原抗氧化能力(FRAP)法评价抗氧化能力。采用丝氨酸蛋白酶抑制试验和凝血酶原时间(PT)试验评价其抗凝活性。用Folin-Ciocalteu (FC)试剂和铝配合物(AlCl3)分别测定总酚含量和总黄酮含量。结果:DPPH清除试验显示IC50值为125.52µg。mL-1和157.94µg。煮沸和冷水提取液分别为mL-1。煮沸和冷水提取物的有效铁还原电位(FRAP)分别为每100µg 142.87µM和135.37µM铁当量。丝氨酸蛋白酶抑制活性的IC50值为182µg。mL-1和161.12µg。冷水提取液和开水提取液分别为mL-1。沸水浸提液PT时间为27.00 min,冷水浸提液PT时间为24.68 min。在测试样品中还发现了显著的酚类和类黄酮含量。结论:恰巴茎提取物具有较强的抗氧化和抗凝血活性,对氧化性和炎症性疾病具有中和氧化自由基和舒张血管的作用。
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引用次数: 0
Molecular Characterization of a cDNA Encoding of an Anionic Cysteine-Free Antimicrobial Peptide From the Iranian Scorpion Odontobuthus Doriae Venom Glands 伊朗蝎毒腺阴离子半胱氨酸抗菌肽cDNA编码的分子特征
A. Jalali, Masoud Mahdavinia, H. Galehdari, M. Baradaran, Davood Valdi-Biranvand, Maryam Naderi Soork
Background: The venom peptides from the scorpion fauna of Iran have been poorly characterized so far. Objectives: In this study, we identified a cDNA encoding of an anionic cysteine-free antimicrobial peptide from the Iranian yellow scorpion odontobuthus doriae (O.doriae). Methods: The cDNA sequence of an anionic antimicrobial-peptide (AMP) was determined from the venom gland cDNA library of Iranian yellow scorpion O.doriae and was named ODAMP5. This sequence was characterized by a software. Then, the structure and function of its putative peptide were predicted in a bioinformatics manner. The library was constructed from 6 scorpion venom glands. The cDNA related to ODAMP5 was isolated from one positive clone of the library. Results: The analysis of ODAMP5 reveals a 51-residue mature peptide with an anionic property that was stable in physiological states. ODAMP5 was similar to anionic peptide Aba-2 from Androctonus bicolor and according to its structure, it can be a member of helical structure AMPs with a new type of putative conserved domain. Putative ODAMP5 has a small size which makes it convenient for synthesis. Conclusion: Furthermore, we created a framework to express the ODAMP5 peptide for future biomedical and pharmacological studies. ODAMP5 may be a new suitable therapeutic strategy for bacterial infection among a few recognized scorpion venom peptides without disulfide bridges.  
背景:迄今为止,来自伊朗蝎子动物群的毒液肽的特征很差。目的:在本研究中,我们从伊朗黄蝎odontobuthus doriae (odooriae)中鉴定了一段阴离子型无半胱氨酸抗菌肽的cDNA编码。方法:从伊朗黄蝎蛇毒腺cDNA文库中测定一个阴离子抗菌肽(AMP)的cDNA序列,命名为ODAMP5。该序列通过软件表征。然后,用生物信息学的方法预测了其推定肽的结构和功能。该文库由6个蝎子毒腺构建而成。从该文库的一个阳性克隆中分离到与ODAMP5相关的cDNA。结果:对ODAMP5的分析揭示了一个具有51个残基的成熟肽,其阴离子性质在生理状态下是稳定的。ODAMP5与双色雄虾的阴离子肽Aba-2相似,根据其结构,它可能是螺旋结构AMPs的成员,具有一种新型的保守结构域。假定的ODAMP5体积小,便于合成。结论:构建了ODAMP5肽的表达框架,为今后的生物医学和药理学研究提供了基础。在已知的几种不含二硫桥的蝎毒肽中,ODAMP5可能是一种新的适合治疗细菌感染的策略。
{"title":"Molecular Characterization of a cDNA Encoding of an Anionic Cysteine-Free Antimicrobial Peptide From the Iranian Scorpion Odontobuthus Doriae Venom Glands","authors":"A. Jalali, Masoud Mahdavinia, H. Galehdari, M. Baradaran, Davood Valdi-Biranvand, Maryam Naderi Soork","doi":"10.18502/pbr.v8i3.11034","DOIUrl":"https://doi.org/10.18502/pbr.v8i3.11034","url":null,"abstract":"Background: The venom peptides from the scorpion fauna of Iran have been poorly characterized so far. \u0000Objectives: In this study, we identified a cDNA encoding of an anionic cysteine-free antimicrobial peptide from the Iranian yellow scorpion odontobuthus doriae (O.doriae). \u0000Methods: The cDNA sequence of an anionic antimicrobial-peptide (AMP) was determined from the venom gland cDNA library of Iranian yellow scorpion O.doriae and was named ODAMP5. This sequence was characterized by a software. Then, the structure and function of its putative peptide were predicted in a bioinformatics manner. The library was constructed from 6 scorpion venom glands. The cDNA related to ODAMP5 was isolated from one positive clone of the library. \u0000Results: The analysis of ODAMP5 reveals a 51-residue mature peptide with an anionic property that was stable in physiological states. ODAMP5 was similar to anionic peptide Aba-2 from Androctonus bicolor and according to its structure, it can be a member of helical structure AMPs with a new type of putative conserved domain. Putative ODAMP5 has a small size which makes it convenient for synthesis. \u0000Conclusion: Furthermore, we created a framework to express the ODAMP5 peptide for future biomedical and pharmacological studies. ODAMP5 may be a new suitable therapeutic strategy for bacterial infection among a few recognized scorpion venom peptides without disulfide bridges. \u0000 ","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-10-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91238143","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 2
Prophylactic Effect of Chloroquine and Hydroxychloroquine on COVID-19 Treatment 氯喹和羟氯喹对COVID-19治疗的预防作用
A. Ataie, Razieh Mansouri, H. Khaleghzadeh-Ahangar, R. Ataee, Fatemeh Alibabaei
Background: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a highly transmissible and pathogenic coronavirus that emerged in late 2019 and has caused a pandemic of acute respiratory disease, named ‘coronavirus disease 2019’ (COVID-19), which has threatened human health and public safety. Objectives: Hydroxychloroquine (HCQ) is an anti-malaria drug with controversial antiviral properties. Some in vitro studies have approved its antiviral effects. Many efforts have been made to prevent and treat COVID-19, but effective drugs for complete eradication of COVID-19 have not been found yet and all available drugs are supportive. Methods: We tried to review some new aspects of HCQ efficacy in the prevention and treatment of COVID-19 infection. Also, some data from recent clinical trials were studied. It has been shown that HCQ may improve some symptoms of patients, but in severe or critical stages, it did not have significant therapeutic effects and did not reduce the rate of mortality. Results: In this review article, we explained some results of recent studies, including clinical trials on the effects of HCQ on the prevention and treatment of COVID-19 infection. Some studies have revealed HCQ’s beneficial effects in outpatients, and some data showed its hazardous impacts on the heart. The available evidence suggests that CQ or HCQ does not improve clinical outcomes in COVID-19. Well-designed randomized trials are required for assessing the efficacy and safety of HCQ and CQ for COVID. Conclusion: It was suggested that the dose of HCQ administration must be adjusted and monitored correctly; furthermore, the levels of some myocardial biomarkers, such as troponin must be measured in mild to moderate, severe, and critical infection. Also, combination therapy with other drugs, such as azithromycin may have better anti-inflammatory and antiviral effects.
背景:严重急性呼吸综合征冠状病毒2型(SARS-CoV-2)是一种高传染性和致病性的冠状病毒,于2019年底出现,引发了一场名为“冠状病毒病2019”(COVID-19)的急性呼吸道疾病大流行,已威胁到人类健康和公共安全。目的:羟氯喹(Hydroxychloroquine, HCQ)是一种具有抗病毒特性的抗疟疾药物。一些体外研究已经证实了它的抗病毒作用。为预防和治疗COVID-19作出了许多努力,但尚未找到彻底根除COVID-19的有效药物,所有现有药物都是支持性的。方法:综述HCQ在预防和治疗COVID-19感染方面的一些新进展。此外,还研究了近期临床试验的一些数据。已有研究表明,HCQ可以改善患者的某些症状,但在重症或危重期,它没有显著的治疗效果,也没有降低死亡率。结果:在这篇综述文章中,我们解释了一些最近的研究结果,包括HCQ预防和治疗COVID-19感染的临床试验。一些研究揭示了HCQ对门诊病人的有益作用,一些数据显示了它对心脏的有害影响。现有证据表明,CQ或HCQ并不能改善COVID-19的临床结果。评估HCQ和CQ对COVID的疗效和安全性需要精心设计的随机试验。结论:建议正确调整和监测HCQ给药剂量;此外,一些心肌生物标志物的水平,如肌钙蛋白,必须在轻度至中度、重度和危重感染时测量。此外,与阿奇霉素等其他药物联合治疗可能具有更好的抗炎和抗病毒效果。
{"title":"Prophylactic Effect of Chloroquine and Hydroxychloroquine on COVID-19 Treatment","authors":"A. Ataie, Razieh Mansouri, H. Khaleghzadeh-Ahangar, R. Ataee, Fatemeh Alibabaei","doi":"10.18502/pbr.v8i2.11023","DOIUrl":"https://doi.org/10.18502/pbr.v8i2.11023","url":null,"abstract":"Background: Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a highly transmissible and pathogenic coronavirus that emerged in late 2019 and has caused a pandemic of acute respiratory disease, named ‘coronavirus disease 2019’ (COVID-19), which has threatened human health and public safety. \u0000Objectives: Hydroxychloroquine (HCQ) is an anti-malaria drug with controversial antiviral properties. Some in vitro studies have approved its antiviral effects. Many efforts have been made to prevent and treat COVID-19, but effective drugs for complete eradication of COVID-19 have not been found yet and all available drugs are supportive. \u0000Methods: We tried to review some new aspects of HCQ efficacy in the prevention and treatment of COVID-19 infection. Also, some data from recent clinical trials were studied. It has been shown that HCQ may improve some symptoms of patients, but in severe or critical stages, it did not have significant therapeutic effects and did not reduce the rate of mortality. \u0000Results: In this review article, we explained some results of recent studies, including clinical trials on the effects of HCQ on the prevention and treatment of COVID-19 infection. Some studies have revealed HCQ’s beneficial effects in outpatients, and some data showed its hazardous impacts on the heart. The available evidence suggests that CQ or HCQ does not improve clinical outcomes in COVID-19. Well-designed randomized trials are required for assessing the efficacy and safety of HCQ and CQ for COVID. \u0000Conclusion: It was suggested that the dose of HCQ administration must be adjusted and monitored correctly; furthermore, the levels of some myocardial biomarkers, such as troponin must be measured in mild to moderate, severe, and critical infection. Also, combination therapy with other drugs, such as azithromycin may have better anti-inflammatory and antiviral effects.","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-10-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74448406","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Effects of Hydroalcoholic Extract of Lepidium Sativum L. on Carbon Tetrachloride-Induced Hepatotoxicity in Mice 枸杞子水醇提取物对四氯化碳致小鼠肝毒性的影响
M. Shokrzadeh, Reza Khalvati, M. Hosseinzadeh, Mona Ayatifard, E. Habibi
Background: Carbon tetrachloride (CCl4 ) as an organic solvent causes symptoms of acute and chronic liver injury, including necrosis, fat changes, liver cancer, and cirrhosis. Lepidium sativum contains flavonoids, alkaloids, and antioxidant components. Objectives: This study aims to investigate the hepatic protection of L. Sativum Extract (LSE) on CCl4 -induced hepatotoxicity in mice.  Methods: A total of 25 male mice were randomly divided into five groups (n=5): control (olive oil), CCl4 , and 3 LSE groups. Except for the control group, all the mice received CCl4 (50%, 0.5 mL/kg) intraperitoneally twice a week for 4 weeks. The mice in the LSE groups were treated daily with LSE (200, 400, and 600 mg/kg) via IP injection. The animals were sacrificed 24 h after the last dose, and liver function parameters, such as Alkaline Phosphatase (ALP), Alanine Aminotransferase (ALT), Aspartate Aminotransferase (AST), and Glutathione (GSH) were determined. Furthermore, 0.1 g of liver tissue was removed for histochemical analysis. Results: Significant differences were observed in GSH, ALP, AST, and ALT levels between the CCI4 and the control groups. Compared to the CCl4 group, LSE treatment significantly decreased plasma ALT (P<0.05), AST in all doses (P<0.001), and ALP in 600 mg/kg (P<0.001). In addition, LSE treatment significantly increased GSH in 400 mg/kg (P<0.01) and 600 mg/kg (P<0.001). Conclusion: LSE has hepatic protective activity against CCl4 -induced injuries. The possible anti-hepatotoxic mechanisms may be related to the presence of flavonoids, triterpenes, alkaloids, tannin, and coumarins in the LSE by inhibiting the free radicals mediated damage.  
背景:四氯化碳(CCl4)作为一种有机溶剂可引起急性和慢性肝损伤症状,包括坏死、脂肪改变、肝癌和肝硬化。枸杞含有类黄酮、生物碱和抗氧化成分。目的:研究大蒜提取物(LSE)对CCl4所致小鼠肝毒性的保护作用。方法:雄性小鼠25只,随机分为5组(n=5):对照组(橄榄油)、CCl4组和LSE组。除对照组外,其余小鼠均腹腔注射CCl4 (50%, 0.5 mL/kg),每周2次,连续4周。LSE组小鼠每日通过IP注射LSE(200、400、600 mg/kg)。末次给药后24 h处死动物,测定肝功能指标,如碱性磷酸酶(ALP)、丙氨酸转氨酶(ALT)、天冬氨酸转氨酶(AST)、谷胱甘肽(GSH)。此外,取肝组织0.1 g进行组织化学分析。结果:CCI4组与对照组GSH、ALP、AST、ALT水平差异均有统计学意义。与CCl4组相比,LSE治疗显著降低了血浆ALT (P<0.05)、AST (P<0.001)和ALP (P<0.001)。此外,400 mg/kg和600 mg/kg LSE处理显著提高了GSH (P<0.01)和600 mg/kg (P<0.001)。结论:LSE对CCl4所致肝损伤具有保护作用。其抗肝毒性机制可能与LSE中黄酮类、三萜、生物碱、单宁和香豆素等物质抑制自由基介导的损伤有关。
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引用次数: 0
Proposed Pharmacological Treatments for COVID-19: Previously Confirmed Drugs 建议的COVID-19药物治疗:先前确认的药物
Fatemeh Bahoosh Feyzabadi, A. Nikjoo, Mohammad Reza Lagzian, Hessamedin Babaei, Melika Nasehi
Background: The outbreak of severe acute respiratory syndrome coronavirus-2, also called ‘coronavirus disease 2019’ (COVID-19), first appeared in December 2019 in Wuhan, China. COVID-19 is caused by an enveloped single-stranded RNA virus, which has affected more than 14 million people around the world and caused a high rate of mortality. It is notable that discovering new drugs and vaccines against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is time-consuming. Therefore, reviewing drugs, which have been previously designed for other purposes can be helpful and effective. Objectives: Studying the effects of previously approved drugs is important; thus, in this article, we reviewed studies on proposed drugs against COVID-19. Methods: The articles and information were collected from Google Scholar, ScienceDirect, and Scopus databases. We did our research based on keywords, like “therapeutics”, “pharmacology”, “Coronavirus”, “COVID-19”, “SARS”, and “MERS-CoV”. We also applied some filters, such as title/abstract, and ignored factors that could lead to bias and selective selection. Results: There is currently no cure for coronavirus, and most treatments have been effective to relieve symptoms. The treatment methods and drugs addressed in this article are chosen either from previous drugs against MERS and SARS, drugs that disrupt the life cycle of the coronavirus, or drugs that have been reviewed in retrospective studies and clinical trials. Conclusion: Prevention and treatment of COVID-19 remain a challenge, in particular for coronavirus and the treatments based on boosting the immune system and preventing virus replication. Epidemiological studies have shown that COVID-19 and SARS-COV transmission are relatively similar. This can help to select the appropriate drug. Thus, anti-inflammatory and antiviral drugs, such as remdesivir are used. Antimalarial drugs, such as hydroxychloroquine (HCQ) and chloroquine (CQ) along with estrogen receptor inhibitors, such as toremifene citrate, which has shown effective results against SARS and MERS, can influence the treatment process. However, more clinical trials are needed to determine the efficacy and side effects of drugs.
背景:2019年12月,中国武汉首次爆发了严重急性呼吸综合征冠状病毒-2,也称为“冠状病毒病2019”(COVID-19)。COVID-19是由一种包膜单链RNA病毒引起的,该病毒已影响到全球1400多万人,并造成了很高的死亡率。值得注意的是,开发针对严重急性呼吸综合征冠状病毒2 (SARS-CoV-2)的新药和疫苗非常耗时。因此,回顾以前为其他目的而设计的药物可能是有帮助和有效的。目的:研究先前批准的药物的作用是重要的;因此,在本文中,我们回顾了针对COVID-19的拟议药物的研究。方法:文献资料来源于Google Scholar、ScienceDirect和Scopus数据库。我们根据“治疗学”、“药理学”、“冠状病毒”、“COVID-19”、“SARS”和“MERS-CoV”等关键词进行了研究。我们还应用了一些过滤器,如标题/摘要,并忽略了可能导致偏见和选择性选择的因素。结果:目前还没有治愈冠状病毒的方法,大多数治疗方法都能有效缓解症状。本文所讨论的治疗方法和药物要么是以往针对中东呼吸综合征和SARS的药物,要么是破坏冠状病毒生命周期的药物,要么是在回顾性研究和临床试验中经过审查的药物。结论:COVID-19的预防和治疗仍然是一个挑战,特别是在冠状病毒和基于增强免疫系统和防止病毒复制的治疗方面。流行病学研究表明,COVID-19和SARS-COV的传播方式相对相似。这有助于选择合适的药物。因此,使用抗炎和抗病毒药物,如瑞德西韦。抗疟疾药物,如羟氯喹(HCQ)和氯喹(CQ),以及雌激素受体抑制剂,如柠檬酸托瑞米芬,已经显示出对SARS和MERS有效的效果,可以影响治疗过程。然而,需要更多的临床试验来确定药物的疗效和副作用。
{"title":"Proposed Pharmacological Treatments for COVID-19: Previously Confirmed Drugs","authors":"Fatemeh Bahoosh Feyzabadi, A. Nikjoo, Mohammad Reza Lagzian, Hessamedin Babaei, Melika Nasehi","doi":"10.18502/pbr.v8i2.11024","DOIUrl":"https://doi.org/10.18502/pbr.v8i2.11024","url":null,"abstract":"Background: The outbreak of severe acute respiratory syndrome coronavirus-2, also called ‘coronavirus disease 2019’ (COVID-19), first appeared in December 2019 in Wuhan, China. COVID-19 is caused by an enveloped single-stranded RNA virus, which has affected more than 14 million people around the world and caused a high rate of mortality. It is notable that discovering new drugs and vaccines against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is time-consuming. Therefore, reviewing drugs, which have been previously designed for other purposes can be helpful and effective. \u0000Objectives: Studying the effects of previously approved drugs is important; thus, in this article, we reviewed studies on proposed drugs against COVID-19. \u0000Methods: The articles and information were collected from Google Scholar, ScienceDirect, and Scopus databases. We did our research based on keywords, like “therapeutics”, “pharmacology”, “Coronavirus”, “COVID-19”, “SARS”, and “MERS-CoV”. We also applied some filters, such as title/abstract, and ignored factors that could lead to bias and selective selection. \u0000Results: There is currently no cure for coronavirus, and most treatments have been effective to relieve symptoms. The treatment methods and drugs addressed in this article are chosen either from previous drugs against MERS and SARS, drugs that disrupt the life cycle of the coronavirus, or drugs that have been reviewed in retrospective studies and clinical trials. \u0000Conclusion: Prevention and treatment of COVID-19 remain a challenge, in particular for coronavirus and the treatments based on boosting the immune system and preventing virus replication. Epidemiological studies have shown that COVID-19 and SARS-COV transmission are relatively similar. This can help to select the appropriate drug. Thus, anti-inflammatory and antiviral drugs, such as remdesivir are used. Antimalarial drugs, such as hydroxychloroquine (HCQ) and chloroquine (CQ) along with estrogen receptor inhibitors, such as toremifene citrate, which has shown effective results against SARS and MERS, can influence the treatment process. However, more clinical trials are needed to determine the efficacy and side effects of drugs.","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-10-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86465937","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of Novel Bis-Coumarin Derivatives as Potential Acetylcholinesterase Inhibitors: An In Vitro, Molecular Docking, and Molecular Dynamics Simulations Study 新型双香豆素衍生物作为潜在乙酰胆碱酯酶抑制剂的合成:体外、分子对接和分子动力学模拟研究
Zhila Zare‐Akbari, Ladan Edjali, Moosa Eshaghi
Background: Alzheimer disease is a progressive and irreversible disease that finally leads to death. It destroys cognitive skills and memory, and eventually, the patient cannot do the simplest things. Objectives: Cholinesterases (ChEs) which has the capability to control cholinergic transmission would result in elevating acetylcholine levels in the brain, by inhibiting CHEs. Coumarins have been shown to exhibit the inhibitory effect of cholinesterase, where the aromatic component results in designing novel candidates that can inhibit Ab accumulation. Methods: The condensation of aryl aldehydes and 4-hydroxycoumarin. Besides, we applied ZnO nanoparticles as an effective heterogeneous catalyst in [bmim]BF4 . To determine the inhibitory activity, we used a substrate, i.e., acetylthiocholine iodide, to assay the tested compounds. Moreover, we applied Ellman’s assay. Results: The present research is an in vitro work. It explores the possible binding mode of these compounds inside the Acetylcholinesterase (AChE) enzyme. Moreover, regarding the synthesized coumarin derivatives, we also performed docking and Molecular Dynamics (MD) simulation studies. The results indicate a satisfactory inhibitory activity for the assayed compounds against AChE with IC50 values from 0.100 to 0.02 µM. In this sense, the stability of protein-ligand complexes and the interaction of the compounds can be understood by performing a molecular docking with molecular dynamics simulation of 5000 ps in the solvent system for AChE. Conclusion: Finally, it is worth mentioning that we also tested coumarin derivatives (L14 and L15), leading to potent and effective AChE inhibitors.
背景:阿尔茨海默病是一种进行性和不可逆的疾病,最终导致死亡。它会破坏认知能力和记忆力,最终,病人连最简单的事情都做不了。目的:胆碱酯酶(cholinesterase, ChEs)具有控制胆碱能传递的能力,可通过抑制胆碱酯酶使脑内乙酰胆碱水平升高。香豆素已显示出胆碱酯酶的抑制作用,其中芳香成分导致设计新的候选物,可以抑制Ab积累。方法:芳醛与4-羟基香豆素的缩合反应。此外,我们还将ZnO纳米颗粒作为[bmim]BF4的有效非均相催化剂。为了确定抑制活性,我们使用底物,即乙酰硫代胆碱碘化,来测定所测试的化合物。此外,我们还采用了Ellman法。结果:本研究为体外实验。它探讨了这些化合物在乙酰胆碱酯酶(AChE)内可能的结合模式。此外,我们还对合成的香豆素衍生物进行了对接和分子动力学(MD)模拟研究。结果表明,化合物对乙酰胆碱酯具有良好的抑制活性,IC50值为0.100 ~ 0.02µM。从这个意义上说,可以通过在溶剂体系中模拟5000 ps的分子动力学进行分子对接来理解蛋白质-配体复合物的稳定性和化合物之间的相互作用。结论:最后,值得一提的是,我们还测试了香豆素衍生物(L14和L15),得到了有效的乙酰胆碱酯酶抑制剂。
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引用次数: 1
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2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research
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