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ANTİTÜBERKÜLER AJAN OLARAK N'-(2-(5-((TEOFİLİN-7-İL)METİL)-4-ETİL-1,2,4-TRİAZOL-3-İLTİO)ACETİL)İZONİKOTİNOHİDRAZİT
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-08-10 DOI: 10.52794/hujpharm.1011368
Andrey Gotsulya, Volodymyr Zazharskyi̇, Volodymyr Parchenko, Pavlo Davydenko, Oleh Kuli̇shenko, Tetiana Brytanova
Makale, izoniazid ve N'-(2-(5-((teofilin-7-il)metil)-4-etil-1,2,4-triazol-3-iltio)asetil)izonikotinohidrazit. Deri altı uygulama için hesaplanan N'-(2-(5-((teofilin-7-il)metil)-4-etil-1,2,4-triazol-3-iltiyo)asetil)izonikotinohidrazid dozu, etkili ve güvenli bir tüberkülosidal ilaç olarak veterinerlik uygulamaları için beklentiler.
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引用次数: 1
Effectiveness of Edamame (Glycine max L. Merril) Membrane in Accelerating The Wound Healing Process of Deep-Partial Thickness Burn 毛豆(Glycine max L. Merril)膜促进深部分厚度烧伤创面愈合的作用
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-08-03 DOI: 10.52794/hujpharm.1111499
I. Sutejo
The gold standard for deep-partial thickness burns is early excision and skin graft; however, many hospitals in Indonesia still use conventional treatment due to the high cost of surgery and the requirement of qualified medical professionals. This research aimed to study the effectiveness of edamame (Glycine max. L Merill) membrane as therapeutic innovation in deep-partial thickness burns. Forty-eight male Wistar rats with deep-partial thickness burns were assigned randomly to four groups, including control and treatment (silver sulfadiazine, the membrane with 40% and 60% edamame extract). Measuring wound healing parameters such as macroscopic evaluation, histopathologic, and hydroxyproline was examined on days 4, 10, and 16. Treatment groups of membrane edamame significantly improved wound healing than the control group. Macroscopically, histopathological findings and hydroxyproline assay confirmed the efficacy of the edamame membrane at 60%, which provided the best healing results. This study showed that edamame membrane is effective as deep-partial thickness burns wound dressing.
深度部分厚度烧伤的金标准是早期切除和植皮;然而,由于手术费用高和对合格医疗专业人员的要求,印度尼西亚的许多医院仍然使用传统治疗方法。本研究旨在研究毛豆(Glycine max.)膜治疗深部分厚度烧伤的创新。将48只深部分厚度烧伤雄性Wistar大鼠随机分为对照组和治疗组(磺胺嘧啶银、毛豆提取物40%和60%膜)。在第4、10和16天检测伤口愈合参数,如宏观评价、组织病理学和羟脯氨酸。膜毛豆治疗组较对照组明显改善创面愈合。从宏观上看,组织病理学检查和羟脯氨酸测定证实毛豆膜的疗效为60%,其愈合效果最好。研究表明毛豆膜是一种有效的深部分厚度烧伤创面敷料。
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引用次数: 0
Chemobrain: Mysteries and the importance of their revelation 化学大脑:奥秘及其揭示的重要性
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-08-03 DOI: 10.52794/hujpharm.1100269
M. Tuncer
Chemotherapy can be associated with both acute and delayed toxic effects on the central nervous system. Among the most commonly reported neurotoxic adverse effects in adult and pediatric cancer patients treated with chemotherapy are mood alterations and neurocognitive symptoms, such as disruption of memory, impaired attention, concentration, processing speed, and executive function. As a consequence of cancer therapy, these cognitive deficits that occur at any point during or following chemotherapy are called chemotherapy-related cognitive dysfunction or "chemobrain". Notably, such symptoms can be progressive even after cessation of therapy and might significantly compromise the quality of life in affected patients who are unable to return to their prior social and academic level of performance. Trying to unpick the chemobrain’s pathophysiology has become a major challenge since patients undergoing chemotherapy have an increased risk of depression, anxiety, and other mood disorders, all of which can have a negative and interacting effect on cognitive function. The purpose of this review is to define and review what is known about this poorly understood phenomenon and unravel the mysteries of “chemobrain”, and summarize therapeutic avenues.
化疗可与中枢神经系统的急性和延迟毒性作用有关。在接受化疗的成人和儿童癌症患者中,最常报道的神经毒性不良反应是情绪改变和神经认知症状,如记忆中断、注意力、注意力、处理速度和执行功能受损。作为癌症治疗的结果,这些在化疗期间或之后发生的认知缺陷被称为化疗相关认知功能障碍或“化疗脑”。值得注意的是,即使在停止治疗后,这些症状也可能是进行性的,并且可能严重损害受影响患者的生活质量,使其无法恢复到以前的社交和学业表现水平。试图解开化学脑的病理生理学已经成为一项重大挑战,因为接受化疗的患者抑郁、焦虑和其他情绪障碍的风险增加,所有这些都可能对认知功能产生负面和相互作用的影响。本综述的目的是定义和回顾对这一知之甚少的现象的了解,揭示“化学脑”的奥秘,并总结治疗途径。
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引用次数: 0
QUALITY BY DESIGN APPROACH FOR OPTIMIZATION AND DEVELOPMENT OF ORODISPERSIBLE FILMS OF LORNOXICAM INCLUSION COMPLEXES 采用质量设计方法对氯诺昔康包合物的光分散膜进行优化和研制
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-08-03 DOI: 10.52794/hujpharm.1072840
Archana Nerella, Nagabhushanam Mv
Lornoxicam is a non-steroidal anti-inflammatory drug, indicated in the treatment of osteoarthritis and rheumatoid arthritis. Lornoxicam is a poor water-soluble drug and hence possesses dissolution limited bioavailability. The aim of the current research work was to develop and characterize orodispersible films of Lornoxicam to enhance its bioavailability by employing Quality-by-Design (QbD) approach. Solvent casting method was used to formulate the Lornoxicam mouth dissolving films. Three formulation factors viz. amount of polymer, amount of PEG 400 and type of polymer were varied at different levels. The responses selected were disintegration time and percent drug dissolved after 5mins. Under the response surface methodology, historical data design was employed to perform the statistical analysis using Design Expert software. The developed films were found to have good elasticity, folding endurance and favorable tensile strength. The disintegration time was found to be 9 to 17 seconds and drug dissolved after 5 minutes was 49 to 95%. The statistical analysis of the results by ANOVA elucidated that there was a significant effect of all the formulation factors on the selected responses (p
氯诺昔康是一种非甾体抗炎药,用于治疗骨关节炎和类风湿性关节炎。氯诺昔康是一种水溶性较差的药物,因此具有溶出度有限的生物利用度。本研究的目的是开发和表征氯诺昔康的非分散膜,通过质量设计(QbD)方法提高其生物利用度。采用溶剂铸造法制备氯诺昔康口腔溶膜。聚合物用量、peg400用量、聚合物种类3个配方因素均有不同程度的变化。选择崩解时间和5min后药物溶出率。在响应面法下,采用历史数据设计,利用design Expert软件进行统计分析。结果表明,该显影膜具有良好的弹性、折叠耐久性和良好的拉伸强度。崩解时间为9 ~ 17 s, 5 min后药物溶出率为49% ~ 95%。方差分析(ANOVA)结果的统计分析表明,所有配方因素对选择的反应都有显著影响(p
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引用次数: 0
Synthesis, Cytotoxic Effect Assessment and Molecular Docking Studies of Disubstituted Thiadiazole Including Oxadiazole as Hybrid Component 以恶二唑为杂化组分的二取代噻二唑的合成、细胞毒作用评价及分子对接研究
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-07-05 DOI: 10.52794/hujpharm.1069664
F. Hassanzadeh, E. Jafari, Sara Zarei̇, H. Sadeghi-aliabadi
Oxadiazole and thiadiazole are of interest building blocks used in drug design. Considering importance of mentioned scaffolds some of the thiadiazole-oxadiazolederivatives were synthesized by three steps in this study.Firstly, thiol functions of 2-amino-5-mercapto-1, 3, 4-thiadiazole was alkylated by benzyl chloride derivatives to give compounds (1a-c). The reaction of chloroacethylchloride with amine group of compounds (1a–c) terminates to amide derivatives(2a-c). Definitive products were produced by treatment of corresponding amide derivatives with 5-(4-chlorophenyl)-1, 3, 4-oxadiazole-2-thiol.Synthesized compounds were evaluated by MTT assay against two cell lines. The final molecules were docked in the active sites of the epidermal growth factor receptor tyrosine kinase to assay the possible interactions.Final products showed range of cytotoxic activity of moderate to good against tested cell lines. Compound (3a) demonstrated a higher cytotoxic activity against MCF-7 (IC50: 26 µM) and Lncap (IC50: 37 µM) cell lines in comparison with other compounds. The highest docking score was -10.55kcal/mol for compound3a.
恶二唑和噻二唑是药物设计中的重要组成部分。考虑到上述支架的重要性,本研究采用三步法合成了部分噻二唑-恶二唑衍生物。首先,将2-氨基-5-巯基- 1,3,4 -噻二唑的硫醇官能团与氯化苄衍生物烷基化,得到化合物(1a-c)。氯乙基氯与胺基化合物(1a-c)的反应终止生成酰胺衍生物(2a-c)。最终产物是用5-(4-氯苯基)- 1,3,4 -恶二唑-2-硫醇处理相应的酰胺衍生物。合成的化合物用MTT法对两种细胞系进行评价。最终的分子被停靠在表皮生长因子受体酪氨酸激酶的活性位点,以测定可能的相互作用。最终产品对被试细胞系的细胞毒活性在中等到良好之间。与其他化合物相比,化合物(3a)对MCF-7 (IC50: 26µM)和Lncap (IC50: 37µM)具有更高的细胞毒活性。化合物3a的对接分数最高,为-10.55kcal/mol。
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引用次数: 0
Neuroprotective Effect of farnesol against Rotenone Induced Parkinson’s Disease in Drosophila melanogaster 法尼醇对鱼藤酮诱导的帕金森病的神经保护作用
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-06-10 DOI: 10.52794/hujpharm.1080352
Jayaram Saravanan, P. Krishnamurthy
The aim of this study is to evaluate the neuroprotective role of farnesol against rotenone induced neurotoxicity in Drosophila melanogaster by survival rate study, negative geotaxis assay and estimation of in vivo antioxidant parameters. To induce neurotoxicity in flies, 500µmol of rotenone was used. After successful induction the flies were treated with 300 µmol and 600 µmol of farnesol for the duration of experimental period. The survival rate study was carried out to estimate the effect of farnesol on longevity of flies and negative geotaxis assay was carried out to determine the effect of farnesol on locomotor function of flies. The results indicated that 300 µmol and 600 µmol of farnesol extended the longevity and locomotor functions of the flies in a dose dependent manner. The in vivo antioxidant studies revealed that farnesol increased the activity of catalase and SOD and decreased lipid peroxidation. Based on the effect of farnesol on survival rate, longevity assay and antioxidant assay, we conclude that farnesol might possess significant neuroprotective property.
本研究通过对鱼藤酮致黑腹果蝇神经毒性的存活率研究、负向地向性实验和体内抗氧化指标的评估,探讨法尼醇对鱼藤酮致黑腹果蝇神经毒性的神经保护作用。用500µmol鱼藤酮诱导果蝇神经毒性。诱导成功后,分别用300µmol和600µmol法尼醇处理果蝇。通过成活率研究来评估法尼醇对果蝇寿命的影响,通过负地向性实验来确定法尼醇对果蝇运动功能的影响。结果表明,300µmol和600µmol法尼醇均能延长果蝇的寿命和运动功能,且呈剂量依赖性。体内抗氧化实验表明,法尼醇能提高过氧化氢酶和超氧化物歧化酶的活性,降低脂质过氧化。通过对小鼠存活率、寿命和抗氧化性能的影响,我们认为法尼醇可能具有显著的神经保护作用。
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引用次数: 0
İLAÇ TESLİMATINDA MEVCUT YENİ NANOTAŞIYICILAR: BİR İNCELEME
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-06-10 DOI: 10.52794/hujpharm.1075668
Niharika Lal, Praveen Kumar Gaur, Sameer Rastogi̇, Kanak Lata
Nanoteknolojinin merkezlenmiş ilaç taşıma sistemlerinde (DDS) kullanımı, geleneksel ilaç taşıma araçları çeşitleriyle ilgili engeller nedeniyle büyük çaplı araştırmaların zorluğudur. Hedeflenen bir İlaç Dağıtım sistemi, ilaçların taşınmasını ve yakınlardaki farkındalığı artırabilir. Çoğu kanser terapötikleri için hedeflenen taşıma süreçleri, birkaç on yılın ötesinde dik bir yukarı doğru itme olduğunu kanıtlamıştır. Ancak, çok sayıda başarılı bilim-öncesi araştırmayla karşılaştırıldığında, en iyi pasif merkezli Nanotaşıyıcılar (NC'ler) bilimsel kullanım için akredite edilmişti ve aktif olarak merkezli NC'lerin hiçbiri bilimsel denemelerin ötesinde üstünlüğe sahip değildi. Burada, kısıtlı bilimsel çeviri ve başarısı için yetenek güdülerine karar vermek için merkezli taşıma süreçlerinin arkasındaki ilkeleri gözden geçiriyoruz. Yeni aktif merkezli NC'lerin iyileştirilmesi için dikkate alınması gereken standartları ve endişeleri savunuyoruz. Ayrıca, stratejilere odaklanan isabetli bir tümörün iyileştirilmesi için olası talimatları vurgularız.
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引用次数: 0
HR-LCMS Analysis and Antihyperlipidemic Effect of Ethanolic Leaf Extract of Momordica charantia L. 苦瓜叶乙醇提取物的HR-LCMS分析及降血脂作用。
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-05-30 DOI: 10.52794/hujpharm.1063583
P. Karale, S. Dhawale, M. Karale
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引用次数: 0
Alzheimer Hastalığının Gelişimsel Sürecinde ve Tedavisinde Potansiyel Öneme Sahip Tıbbi Bitkiler ve Fitokimyasallar
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-05-09 DOI: 10.52794/hujpharm.1014770
Sevgi Gezici, Nazım Şekeroğlu
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引用次数: 0
Epilepsi Tedavisinde Valproik Asit Kullanımı ve Biyolojik Matrislerdeki Tayini
Q4 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2022-04-20 DOI: 10.52794/hujpharm.1062609
Oğuz Özbek, Ömer Işildak
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引用次数: 0
期刊
Hacettepe University Journal of the Faculty of Pharmacy
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